Assay Detail
Functional
CHEMBL763904
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In vitro antagonist activity, Inhibition of angiotensin II (50 nM) mediated increase in cytosolic [Ca2+] conc. in PLC-PRF-5 cells
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | PLC-PRF-5 |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Synthesis and pharmacological evaluation of new pyrazolidine-3, 5-diones as AT(1) angiotensin II receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 7.64 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1513 | IRBESARTAN | 4.0 | 1 | 8.52 |
| CHEMBL91113 | — | — | 1 | 7.92 |
| CHEMBL90872 | — | — | 1 | 7.82 |
| CHEMBL315444 | — | — | 1 | 7.66 |
| CHEMBL88924 | — | — | 1 | 7.58 |
| CHEMBL90483 | — | — | 1 | 7.55 |
| CHEMBL315873 | — | — | 1 | 7.42 |
| CHEMBL92225 | — | — | 1 | 7.28 |
| CHEMBL90411 | — | — | 1 | 7.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1513 | IRBESARTAN | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL91113 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL90872 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL315444 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL88924 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL90483 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL315873 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL92225 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL90411 | — | IC50 | = | 89.0 | nM | 7.05 |