Assay Detail
Binding
CHEMBL679799
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Inhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cells
14
Total Activities
14
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
Design of a potent combined pseudopeptide endothelin-A/endothelin-B receptor antagonist, Ac-DBhg16-Leu-Asp-Ile-[NMe]Ile-Trp21 (PD 156252): examination of its pharmacokinetic and spectral properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 6.63 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1790519 | — | — | 1 | 9.00 |
| CHEMBL262993 | — | — | 1 | 8.40 |
| CHEMBL2369736 | — | — | 1 | 7.52 |
| CHEMBL328942 | — | — | 1 | 7.24 |
| CHEMBL1793926 | — | — | 1 | 6.70 |
| CHEMBL1793932 | — | — | 1 | 6.60 |
| CHEMBL1793929 | — | — | 1 | 6.58 |
| CHEMBL1793925 | — | — | 1 | 6.58 |
| CHEMBL1793933 | — | — | 1 | 6.16 |
| CHEMBL1793928 | — | — | 1 | 6.06 |
| CHEMBL1793924 | — | — | 1 | 5.57 |
| CHEMBL2367550 | — | — | 1 | 5.52 |
| CHEMBL1793934 | — | — | 1 | 5.50 |
| CHEMBL1793927 | — | — | 1 | 5.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1790519 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL262993 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2369736 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL328942 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL1793926 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL1793932 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL1793929 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL1793925 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL1793933 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL1793928 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL1793924 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL2367550 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL1793934 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL1793927 | — | IC50 | = | 4500.0 | nM | 5.35 |