Assay Detail
Functional
CHEMBL869036
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Ability to block pore formation in human THP1 cells assessed as inhibition of YO-PRO-1 diiodide dye uptake
29
Total Activities
29
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | THP-1 |
| Confidence | 1 — Organism |
| Curated By | Intermediate |
Publication
Structure-activity relationship studies on a series of novel, substituted 1-benzyl-5-phenyltetrazole P2X7 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 6.33 | 7.30 |
| pIC50 | 6 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL210835 | — | — | 1 | 7.30 |
| CHEMBL380239 | — | — | 1 | 6.90 |
| CHEMBL207370 | — | — | 1 | 6.80 |
| CHEMBL437703 | — | — | 1 | 6.80 |
| CHEMBL377219 | — | — | 1 | 6.70 |
| CHEMBL380023 | — | — | 1 | 6.70 |
| CHEMBL210144 | — | — | 1 | 6.60 |
| CHEMBL210284 | — | — | 1 | 6.40 |
| CHEMBL427223 | — | — | 1 | 6.40 |
| CHEMBL208234 | — | — | 1 | 6.30 |
| CHEMBL208560 | — | — | 1 | 6.30 |
| CHEMBL378749 | — | — | 1 | 6.10 |
| CHEMBL209608 | — | — | 1 | 5.90 |
| CHEMBL210320 | — | — | 1 | 5.87 |
| CHEMBL207909 | — | — | 1 | 5.70 |
| CHEMBL207908 | — | — | 1 | 5.70 |
| CHEMBL209607 | — | — | 1 | 5.10 |
| CHEMBL210272 | — | — | 1 | - |
| CHEMBL210367 | — | — | 1 | - |
| CHEMBL209780 | — | — | 1 | - |
| CHEMBL426137 | — | — | 1 | - |
| CHEMBL378928 | — | — | 1 | - |
| CHEMBL441479 | — | — | 1 | - |
| CHEMBL210834 | — | — | 1 | - |
| CHEMBL377837 | — | — | 1 | - |
| CHEMBL210889 | — | — | 1 | - |
| CHEMBL206904 | — | — | 1 | - |
| CHEMBL207525 | — | — | 1 | - |
| CHEMBL384209 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL210835 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL380239 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL207370 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL437703 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL377219 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL380023 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL210144 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL210284 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL427223 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL208234 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL208560 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL378749 | — | IC50 | = | 794.33 | nM | 6.10 |
| CHEMBL209608 | — | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL210320 | — | IC50 | = | 1348.96 | nM | 5.87 |
| CHEMBL207909 | — | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL207908 | — | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL209607 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL210272 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL210367 | — | pIC50 | - | — | - | |
| CHEMBL209780 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL426137 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL378928 | — | pIC50 | - | — | - | |
| CHEMBL441479 | — | pIC50 | - | — | - | |
| CHEMBL210834 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL377837 | — | pIC50 | - | — | - | |
| CHEMBL210889 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL206904 | — | pIC50 | - | — | - | |
| CHEMBL207525 | — | pIC50 | - | — | - | |
| CHEMBL384209 | — | IC50 | > | 10000.0 | nM | - |