Assay Detail
Binding
CHEMBL677396
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Binding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
52
Total Activities
52
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 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 | 52 | 6.31 | 8.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL262993 | — | — | 1 | 8.46 |
| CHEMBL405599 | — | — | 1 | 8.40 |
| CHEMBL94983 | — | — | 1 | 7.89 |
| CHEMBL319660 | — | — | 1 | 7.77 |
| CHEMBL433349 | — | — | 1 | 7.68 |
| CHEMBL97470 | — | — | 1 | 7.60 |
| CHEMBL319719 | — | — | 1 | 7.46 |
| CHEMBL421190 | — | — | 1 | 7.44 |
| CHEMBL328942 | — | — | 1 | 7.40 |
| CHEMBL385492 | — | — | 1 | 7.17 |
| CHEMBL94907 | — | — | 1 | 7.00 |
| CHEMBL330144 | — | — | 1 | 6.85 |
| CHEMBL265116 | — | — | 1 | 6.70 |
| CHEMBL97431 | — | — | 1 | 6.64 |
| CHEMBL386181 | — | — | 1 | 6.60 |
| CHEMBL329609 | — | — | 1 | 6.50 |
| CHEMBL411797 | — | — | 1 | 6.42 |
| CHEMBL2370255 | — | — | 1 | 6.32 |
| CHEMBL384728 | — | — | 1 | 6.30 |
| CHEMBL96822 | — | — | 1 | 6.27 |
| CHEMBL216082 | — | — | 1 | 6.24 |
| CHEMBL263295 | — | — | 1 | 6.19 |
| CHEMBL433406 | — | — | 1 | 6.07 |
| CHEMBL317099 | — | — | 1 | 6.04 |
| CHEMBL318020 | — | — | 1 | 6.00 |
| CHEMBL323331 | — | — | 1 | 6.00 |
| CHEMBL94689 | — | — | 1 | 5.96 |
| CHEMBL407933 | — | — | 1 | 5.70 |
| CHEMBL319537 | — | — | 1 | 5.68 |
| CHEMBL2370254 | — | — | 1 | 5.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL262993 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL405599 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL94983 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL319660 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL433349 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL97470 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL319719 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL421190 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL328942 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL385492 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL94907 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL330144 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL265116 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL97431 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL386181 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL329609 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL411797 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL2370255 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL384728 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL96822 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL216082 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL263295 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL433406 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL317099 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL323331 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL318020 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL94689 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL407933 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL319537 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL2370254 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL405178 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL415238 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL327523 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL413179 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL264579 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL405709 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL2370253 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL265734 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL414082 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL384052 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL2370247 | — | IC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL262229 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL269428 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL2370245 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL94525 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL431433 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL327590 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2370246 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL94730 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL439435 | — | IC50 | > | 10000.0 | nM | - |