Assay Detail
Binding
CHEMBL650318
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Binding affinity against AT1 in human hepatoma cell line, PLC-PRF-5
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
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 |
|---|---|---|---|
| Ki | 21 | 7.02 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1513 | IRBESARTAN | 4.0 | 1 | 8.70 |
| CHEMBL91113 | — | — | 1 | 8.00 |
| CHEMBL90872 | — | — | 1 | 7.89 |
| CHEMBL315444 | — | — | 1 | 7.60 |
| CHEMBL90483 | — | — | 1 | 7.60 |
| CHEMBL313392 | — | — | 1 | 7.50 |
| CHEMBL315873 | — | — | 1 | 7.50 |
| CHEMBL92225 | — | — | 1 | 7.40 |
| CHEMBL88924 | — | — | 1 | 7.38 |
| CHEMBL90411 | — | — | 1 | 6.80 |
| CHEMBL90999 | — | — | 1 | 6.42 |
| CHEMBL327594 | — | — | 1 | 6.40 |
| CHEMBL88471 | — | — | 1 | 6.40 |
| CHEMBL90187 | — | — | 1 | 5.70 |
| CHEMBL90887 | — | — | 1 | 5.50 |
| CHEMBL90885 | — | — | 1 | 5.48 |
| CHEMBL328484 | — | — | 1 | - |
| CHEMBL90629 | — | — | 1 | - |
| CHEMBL91069 | — | — | 1 | - |
| CHEMBL90257 | — | — | 1 | - |
| CHEMBL88131 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1513 | IRBESARTAN | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL91113 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL90872 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL315444 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL90483 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL313392 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL315873 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL92225 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL88924 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL90411 | — | Ki | = | 158.0 | nM | 6.80 |
| CHEMBL90999 | — | Ki | = | 381.0 | nM | 6.42 |
| CHEMBL327594 | — | Ki | = | 402.0 | nM | 6.40 |
| CHEMBL88471 | — | Ki | = | 398.0 | nM | 6.40 |
| CHEMBL90187 | — | Ki | = | 1995.0 | nM | 5.70 |
| CHEMBL90887 | — | Ki | = | 3162.0 | nM | 5.50 |
| CHEMBL90885 | — | Ki | = | 3301.0 | nM | 5.48 |
| CHEMBL328484 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL90629 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL91069 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL90257 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL88131 | — | Ki | > | 10000.0 | nM | - |