Assay Detail
Binding
CHEMBL681510
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Isoindolines: a new series of potent and selective endothelin-A receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 7.20 | 8.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL50232 | — | — | 1 | 8.39 |
| CHEMBL295440 | — | — | 1 | 8.27 |
| CHEMBL47868 | — | — | 1 | 8.21 |
| CHEMBL298212 | — | — | 1 | 7.92 |
| CHEMBL49312 | — | — | 1 | 7.85 |
| CHEMBL440853 | — | — | 1 | 7.66 |
| CHEMBL295140 | — | — | 1 | 7.54 |
| CHEMBL301371 | — | — | 1 | 7.51 |
| CHEMBL430572 | — | — | 1 | 7.24 |
| CHEMBL301723 | — | — | 1 | 7.18 |
| CHEMBL296974 | — | — | 1 | 7.17 |
| CHEMBL49850 | — | — | 1 | 7.11 |
| CHEMBL300000 | — | — | 1 | 7.07 |
| CHEMBL49040 | — | — | 1 | 7.02 |
| CHEMBL48652 | — | — | 1 | 7.02 |
| CHEMBL298664 | — | — | 1 | 7.02 |
| CHEMBL417903 | — | — | 1 | 6.96 |
| CHEMBL298922 | — | — | 1 | 6.92 |
| CHEMBL263723 | — | — | 1 | 6.51 |
| CHEMBL48261 | — | — | 1 | 6.48 |
| CHEMBL52110 | — | — | 1 | 5.96 |
| CHEMBL297353 | — | — | 1 | 5.48 |
| CHEMBL432499 | — | — | 1 | - |
| CHEMBL49007 | — | — | 1 | - |
| CHEMBL430759 | — | — | 1 | - |
| CHEMBL299095 | — | — | 1 | - |
| CHEMBL47563 | — | — | 1 | - |
| CHEMBL298569 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL50232 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL295440 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL47868 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL298212 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL49312 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL440853 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL295140 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL301371 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL430572 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL301723 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL296974 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL49850 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL300000 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL49040 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL48652 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL298664 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL417903 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL298922 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL263723 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL48261 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL52110 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL297353 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL432499 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL49007 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL430759 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL299095 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL47563 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL298569 | — | IC50 | > | 10000.0 | nM | - |