Assay Detail
Functional
CHEMBL1046312
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Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced fluorescent ethidium accumulation at 10 uM
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Synthesis and structure-activity relationships of pyrazolodiazepine derivatives as human P2X7 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.08 | 6.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL28324 | — | — | 1 | 6.96 |
| CHEMBL577979 | — | — | 1 | 6.75 |
| CHEMBL570992 | — | — | 1 | 6.60 |
| CHEMBL568802 | — | — | 1 | 6.51 |
| CHEMBL577975 | — | — | 1 | 6.28 |
| CHEMBL577761 | — | — | 1 | 6.13 |
| CHEMBL570672 | — | — | 1 | 6.10 |
| CHEMBL577974 | — | — | 1 | 6.07 |
| CHEMBL571076 | — | — | 1 | 5.97 |
| CHEMBL570854 | — | — | 1 | 5.93 |
| CHEMBL570852 | — | — | 1 | 5.89 |
| CHEMBL577977 | — | — | 1 | 5.85 |
| CHEMBL570177 | — | — | 1 | 5.84 |
| CHEMBL569036 | — | — | 1 | 5.37 |
| CHEMBL570438 | — | — | 1 | 4.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL28324 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL577979 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL570992 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL568802 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL577975 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL577761 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL570672 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL577974 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL571076 | — | IC50 | = | 1070.0 | nM | 5.97 |
| CHEMBL570854 | — | IC50 | = | 1180.0 | nM | 5.93 |
| CHEMBL570852 | — | IC50 | = | 1280.0 | nM | 5.89 |
| CHEMBL577977 | — | IC50 | = | 1420.0 | nM | 5.85 |
| CHEMBL570177 | — | IC50 | = | 1450.0 | nM | 5.84 |
| CHEMBL569036 | — | IC50 | = | 4310.0 | nM | 5.37 |
| CHEMBL570438 | — | IC50 | = | 13000.0 | nM | 4.89 |