Assay Detail
Functional
CHEMBL679796
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cells
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Oryctolagus cuniculus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Structure-activity relationships of the potent combined endothelin-A/endothelin-B receptor antagonist Ac-DDip16-Leu-Asp-Ile-Ile-Trp21: development of endothelin-B receptor selective antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 6.54 | 8.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL262993 | — | — | 1 | 8.31 |
| CHEMBL405599 | — | — | 1 | 7.85 |
| CHEMBL319660 | — | — | 1 | 7.54 |
| CHEMBL94983 | — | — | 1 | 7.52 |
| CHEMBL328942 | — | — | 1 | 7.16 |
| CHEMBL319719 | — | — | 1 | 7.16 |
| CHEMBL97470 | — | — | 1 | 6.89 |
| CHEMBL265116 | — | — | 1 | 6.80 |
| CHEMBL263295 | — | — | 1 | 6.70 |
| CHEMBL323331 | — | — | 1 | 6.64 |
| CHEMBL433406 | — | — | 1 | 6.55 |
| CHEMBL97431 | — | — | 1 | 6.47 |
| CHEMBL94907 | — | — | 1 | 6.38 |
| CHEMBL433349 | — | — | 1 | 6.37 |
| CHEMBL2370255 | — | — | 1 | 6.37 |
| CHEMBL318020 | — | — | 1 | 6.35 |
| CHEMBL411797 | — | — | 1 | 6.28 |
| CHEMBL216082 | — | — | 1 | 6.08 |
| CHEMBL386181 | — | — | 1 | 5.77 |
| CHEMBL319537 | — | — | 1 | 5.72 |
| CHEMBL96822 | — | — | 1 | 5.68 |
| CHEMBL317099 | — | — | 1 | 5.68 |
| CHEMBL2370254 | — | — | 1 | 5.37 |
| CHEMBL329609 | — | — | 1 | 5.22 |
| CHEMBL405709 | — | — | 1 | - |
| CHEMBL94525 | — | — | 1 | - |
| CHEMBL431433 | — | — | 1 | - |
| CHEMBL2370253 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL262993 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL405599 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL319660 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL94983 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL328942 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL319719 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL97470 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL265116 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL263295 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL323331 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL433406 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL97431 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL94907 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL433349 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL2370255 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL318020 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL411797 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL216082 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL386181 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL319537 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL96822 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL317099 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL2370254 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL329609 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL405709 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL94525 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL431433 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2370253 | — | IC50 | > | 10000.0 | nM | - |