Assay Detail
Binding
CHEMBL682962
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Binding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cells
31
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Oryctolagus cuniculus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Structure-activity relationships of C-terminal endothelin hexapeptide antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 5.71 | 7.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1788127 | — | — | 1 | 7.22 |
| CHEMBL313760 | — | — | 1 | 6.85 |
| CHEMBL313984 | — | — | 2 | 6.70 |
| CHEMBL406279 | — | — | 1 | 6.38 |
| CHEMBL2370070 | — | — | 1 | 6.24 |
| CHEMBL313056 | — | — | 1 | 6.03 |
| CHEMBL315047 | — | — | 1 | 6.00 |
| CHEMBL327350 | — | — | 1 | 5.85 |
| CHEMBL86814 | — | — | 1 | 5.75 |
| CHEMBL313382 | — | — | 1 | 5.75 |
| CHEMBL438194 | — | — | 1 | 5.46 |
| CHEMBL87243 | — | — | 1 | 5.44 |
| CHEMBL431874 | — | — | 1 | 5.17 |
| CHEMBL85341 | — | — | 1 | 5.16 |
| CHEMBL330489 | — | — | 1 | 5.10 |
| CHEMBL86737 | — | — | 1 | 5.10 |
| CHEMBL289687 | — | — | 1 | 5.05 |
| CHEMBL315658 | — | — | 1 | 5.04 |
| CHEMBL315780 | — | — | 1 | 4.85 |
| CHEMBL273391 | — | — | 1 | 4.74 |
| CHEMBL312916 | — | — | 1 | - |
| CHEMBL315328 | — | — | 1 | - |
| CHEMBL87252 | — | — | 1 | - |
| CHEMBL431218 | — | — | 1 | - |
| CHEMBL316092 | — | — | 1 | - |
| CHEMBL315384 | — | — | 1 | - |
| CHEMBL87724 | — | — | 1 | - |
| CHEMBL89736 | — | — | 1 | - |
| CHEMBL314239 | — | — | 1 | - |
| CHEMBL89416 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1788127 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL313760 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL313984 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL406279 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL2370070 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL313984 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL313056 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL315047 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL327350 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL313382 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL86814 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL438194 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL87243 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL431874 | — | IC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL85341 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL330489 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL86737 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL289687 | — | IC50 | = | 8900.0 | nM | 5.05 |
| CHEMBL315658 | — | IC50 | = | 9100.0 | nM | 5.04 |
| CHEMBL315780 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL273391 | — | IC50 | = | 18400.0 | nM | 4.74 |
| CHEMBL315328 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL87252 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL312916 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL431218 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL316092 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL315384 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL87724 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL89736 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL314239 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL89416 | — | IC50 | > | 10000.0 | nM | - |