Assay Detail
Binding
CHEMBL3707863
Review assay metadata, readout intent, target linkage, and publication context from the same page.
FLIPR Assay: Ca2+ Flux: 1321N1 cells expressing the recombinant human, rat or mouse P2X7 channel was cultured in HyQ DME/(HyClone/Dulbecco's Modified Eagle Medium) high glucose supplemented with 10% Fetal Bovine Serum (FBS) and appropriate selection marker. Cells were seeded at a density of 25000 cells/well (96-well clear bottom black walled plates) in 100 ul volume/well. On the day of the experiment, cell plates were washed with assay buffer, containing (in mM): 130 NaCl, 2 KCl, 1 CaCl2, 1 MgCl2, 10 HEPES, 5 glucose; pH 7.40 and 300 mOs. After the wash, cells were loaded with the Calcium-4 dye (Molecular Device) and incubated in the dark for 60 minutes. Test compounds were prepared at 250x the test concentration in neat DMSO. Intermediate 96-well compound plates were prepared by transferring 1.2 uL of the compound into 300 uL of assay buffer. A further 3x dilution occurred when transferring 50 uL/well of the compound plate to 100 uL/well in the cell plate.
92
Total Activities
90
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | 1321-N1 |
| 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 |
|---|---|---|---|
| IC50 | 92 | 6.20 | 8.34 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3663287 | — | — | 1 | 8.34 |
| CHEMBL3663296 | — | — | 1 | 8.29 |
| CHEMBL3663316 | — | — | 2 | 8.25 |
| CHEMBL3663294 | — | — | 2 | 8.25 |
| CHEMBL3663253 | — | — | 1 | 8.16 |
| CHEMBL3663289 | — | — | 1 | 8.09 |
| CHEMBL3663286 | — | — | 1 | 8.02 |
| CHEMBL3663260 | — | — | 1 | 7.97 |
| CHEMBL3663291 | — | — | 1 | 7.93 |
| CHEMBL3663257 | — | — | 1 | 7.80 |
| CHEMBL3663284 | — | — | 1 | 7.80 |
| CHEMBL3663277 | — | — | 1 | 7.75 |
| CHEMBL3663240 | — | — | 1 | 7.30 |
| CHEMBL3663242 | — | — | 1 | 7.19 |
| CHEMBL3663239 | — | — | 1 | 6.99 |
| CHEMBL3663254 | — | — | 1 | 6.91 |
| CHEMBL3663297 | — | — | 1 | 6.90 |
| CHEMBL3663295 | — | — | 1 | 6.88 |
| CHEMBL3663256 | — | — | 1 | 6.87 |
| CHEMBL3663270 | — | — | 1 | 6.81 |
| CHEMBL3663298 | — | — | 1 | 6.80 |
| CHEMBL3663259 | — | — | 1 | 6.76 |
| CHEMBL3663255 | — | — | 1 | 6.73 |
| CHEMBL3663290 | — | — | 1 | 6.55 |
| CHEMBL3663237 | — | — | 1 | 6.52 |
| CHEMBL3663244 | — | — | 1 | 6.50 |
| CHEMBL3663252 | — | — | 1 | 6.43 |
| CHEMBL3663288 | — | — | 1 | 6.40 |
| CHEMBL3663292 | — | — | 1 | 6.40 |
| CHEMBL3639621 | — | — | 1 | 6.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3663287 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL3663296 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL3663316 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL3663294 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL3663253 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL3663289 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL3663286 | — | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL3663294 | — | IC50 | = | 10.3 | nM | 7.99 |
| CHEMBL3663260 | — | IC50 | = | 10.6 | nM | 7.97 |
| CHEMBL3663291 | — | IC50 | = | 11.8 | nM | 7.93 |
| CHEMBL3663257 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3663284 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3663277 | — | IC50 | = | 17.6 | nM | 7.75 |
| CHEMBL3663316 | — | IC50 | = | 36.1 | nM | 7.44 |
| CHEMBL3663240 | — | IC50 | = | 49.5 | nM | 7.30 |
| CHEMBL3663242 | — | IC50 | = | 64.6 | nM | 7.19 |
| CHEMBL3663239 | — | IC50 | = | 102.6 | nM | 6.99 |
| CHEMBL3663254 | — | IC50 | = | 122.2 | nM | 6.91 |
| CHEMBL3663297 | — | IC50 | = | 125.9 | nM | 6.90 |
| CHEMBL3663295 | — | IC50 | = | 132.7 | nM | 6.88 |
| CHEMBL3663256 | — | IC50 | = | 134.6 | nM | 6.87 |
| CHEMBL3663270 | — | IC50 | = | 154.5 | nM | 6.81 |
| CHEMBL3663298 | — | IC50 | = | 158.5 | nM | 6.80 |
| CHEMBL3663259 | — | IC50 | = | 174.6 | nM | 6.76 |
| CHEMBL3663255 | — | IC50 | = | 187.9 | nM | 6.73 |
| CHEMBL3663290 | — | IC50 | = | 282.5 | nM | 6.55 |
| CHEMBL3663237 | — | IC50 | = | 300.6 | nM | 6.52 |
| CHEMBL3663244 | — | IC50 | = | 316.2 | nM | 6.50 |
| CHEMBL3663252 | — | IC50 | = | 375.0 | nM | 6.43 |
| CHEMBL3663288 | — | IC50 | = | 396.3 | nM | 6.40 |
| CHEMBL3663292 | — | IC50 | = | 398.1 | nM | 6.40 |
| CHEMBL3639621 | — | IC50 | = | 543.3 | nM | 6.26 |
| CHEMBL3663305 | — | IC50 | = | 707.9 | nM | 6.15 |
| CHEMBL3663278 | — | IC50 | = | 743.0 | nM | 6.13 |
| CHEMBL3663293 | — | IC50 | = | 794.3 | nM | 6.10 |
| CHEMBL3663279 | — | IC50 | = | 824.1 | nM | 6.08 |
| CHEMBL3663261 | — | IC50 | = | 1064.1 | nM | 5.97 |
| CHEMBL3663282 | — | IC50 | = | 1142.9 | nM | 5.94 |
| CHEMBL3663262 | — | IC50 | = | 1213.4 | nM | 5.92 |
| CHEMBL3663249 | — | IC50 | = | 1220.4 | nM | 5.91 |
| CHEMBL3663265 | — | IC50 | = | 1303.2 | nM | 5.88 |
| CHEMBL3663306 | — | IC50 | = | 1370.9 | nM | 5.86 |
| CHEMBL3663307 | — | IC50 | = | 1556.0 | nM | 5.81 |
| CHEMBL3663247 | — | IC50 | = | 1584.9 | nM | 5.80 |
| CHEMBL3663243 | — | IC50 | = | 1650.1 | nM | 5.78 |
| CHEMBL3663246 | — | IC50 | = | 1995.3 | nM | 5.70 |
| CHEMBL3663232 | — | IC50 | = | 2564.5 | nM | 5.59 |
| CHEMBL3663263 | — | IC50 | = | 2606.2 | nM | 5.58 |
| CHEMBL3663266 | — | IC50 | = | 2779.7 | nM | 5.56 |
| CHEMBL3663313 | — | IC50 | = | 3047.9 | nM | 5.52 |