Assay Detail
Functional
CHEMBL932852
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human recombinant P2X7 receptor assessed as inhibition of BzATP-induced calcium flux by FLIPR assay
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and in vitro activity of 1-(2,3-dichlorophenyl)-N-(pyridin-3-ylmethyl)-1H-1,2,4-triazol-5-amine and 4-(2,3-dichlorophenyl)-N-(pyridin-3-ylmethyl)-4H-1,2,4-triazol-3-amine P2X7 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 38 | 7.17 | 8.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL401822 | — | — | 1 | 8.04 |
| CHEMBL402132 | — | — | 1 | 7.96 |
| CHEMBL430223 | — | — | 1 | 7.93 |
| CHEMBL257045 | — | — | 1 | 7.90 |
| CHEMBL258111 | — | — | 1 | 7.86 |
| CHEMBL271462 | — | — | 1 | 7.83 |
| CHEMBL257897 | — | — | 1 | 7.82 |
| CHEMBL270678 | — | — | 1 | 7.75 |
| CHEMBL403222 | — | — | 1 | 7.70 |
| CHEMBL402133 | — | — | 1 | 7.68 |
| CHEMBL410039 | — | — | 1 | 7.55 |
| CHEMBL257523 | — | — | 1 | 7.54 |
| CHEMBL255614 | — | — | 1 | 7.51 |
| CHEMBL271030 | — | — | 1 | 7.51 |
| CHEMBL270438 | — | — | 1 | 7.49 |
| CHEMBL402411 | — | — | 1 | 7.40 |
| CHEMBL256883 | — | — | 1 | 7.34 |
| CHEMBL270679 | — | — | 1 | 7.34 |
| CHEMBL401531 | — | — | 1 | 7.33 |
| CHEMBL271679 | — | — | 1 | 7.32 |
| CHEMBL403763 | — | — | 1 | 7.31 |
| CHEMBL402412 | — | — | 1 | 7.24 |
| CHEMBL272933 | — | — | 1 | 7.17 |
| CHEMBL270436 | — | — | 1 | 7.17 |
| CHEMBL245754 | — | — | 1 | 7.11 |
| CHEMBL255638 | — | — | 1 | 6.99 |
| CHEMBL270421 | — | — | 1 | 6.93 |
| CHEMBL377219 | — | — | 1 | 6.91 |
| CHEMBL271464 | — | — | 1 | 6.81 |
| CHEMBL403907 | — | — | 1 | 6.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL401822 | — | IC50 | = | 9.12 | nM | 8.04 |
| CHEMBL402132 | — | IC50 | = | 10.96 | nM | 7.96 |
| CHEMBL430223 | — | IC50 | = | 11.75 | nM | 7.93 |
| CHEMBL257045 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL258111 | — | IC50 | = | 13.8 | nM | 7.86 |
| CHEMBL271462 | — | IC50 | = | 14.79 | nM | 7.83 |
| CHEMBL257897 | — | IC50 | = | 15.14 | nM | 7.82 |
| CHEMBL270678 | — | IC50 | = | 17.78 | nM | 7.75 |
| CHEMBL403222 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL402133 | — | IC50 | = | 20.89 | nM | 7.68 |
| CHEMBL410039 | — | IC50 | = | 28.18 | nM | 7.55 |
| CHEMBL257523 | — | IC50 | = | 28.84 | nM | 7.54 |
| CHEMBL255614 | — | IC50 | = | 30.9 | nM | 7.51 |
| CHEMBL271030 | — | IC50 | = | 30.9 | nM | 7.51 |
| CHEMBL270438 | — | IC50 | = | 32.36 | nM | 7.49 |
| CHEMBL402411 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL256883 | — | IC50 | = | 45.71 | nM | 7.34 |
| CHEMBL270679 | — | IC50 | = | 45.71 | nM | 7.34 |
| CHEMBL401531 | — | IC50 | = | 46.77 | nM | 7.33 |
| CHEMBL271679 | — | IC50 | = | 47.86 | nM | 7.32 |
| CHEMBL403763 | — | IC50 | = | 48.98 | nM | 7.31 |
| CHEMBL402412 | — | IC50 | = | 57.54 | nM | 7.24 |
| CHEMBL272933 | — | IC50 | = | 67.61 | nM | 7.17 |
| CHEMBL270436 | — | IC50 | = | 67.61 | nM | 7.17 |
| CHEMBL245754 | — | IC50 | = | 77.62 | nM | 7.11 |
| CHEMBL255638 | — | IC50 | = | 102.33 | nM | 6.99 |
| CHEMBL270421 | — | IC50 | = | 117.49 | nM | 6.93 |
| CHEMBL377219 | — | IC50 | = | 123.03 | nM | 6.91 |
| CHEMBL271464 | — | IC50 | = | 154.88 | nM | 6.81 |
| CHEMBL403907 | — | IC50 | = | 288.4 | nM | 6.54 |
| CHEMBL404091 | — | IC50 | = | 354.81 | nM | 6.45 |
| CHEMBL270019 | — | IC50 | = | 363.08 | nM | 6.44 |
| CHEMBL271602 | — | IC50 | = | 478.63 | nM | 6.32 |
| CHEMBL404339 | — | IC50 | = | 616.6 | nM | 6.21 |
| CHEMBL409519 | — | IC50 | = | 1621.81 | nM | 5.79 |
| CHEMBL403105 | — | IC50 | = | 1862.09 | nM | 5.73 |
| CHEMBL258112 | — | IC50 | = | 3388.44 | nM | 5.47 |
| CHEMBL257516 | — | IC50 | > | 10000.0 | nM | - |