Assay Detail
Binding
CHEMBL677308
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Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Butenolide endothelin antagonists with improved aqueous solubility.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 8.75 | 10.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL291058 | — | — | 1 | 10.30 |
| CHEMBL69986 | — | — | 1 | 10.05 |
| CHEMBL308646 | — | — | 1 | 9.70 |
| CHEMBL302974 | — | — | 1 | 9.70 |
| CHEMBL304762 | — | — | 1 | 9.54 |
| CHEMBL69832 | — | — | 1 | 9.52 |
| CHEMBL8981 | PD-156707 | — | 1 | 9.52 |
| CHEMBL408055 | — | — | 1 | 9.42 |
| CHEMBL303484 | — | — | 1 | 9.15 |
| CHEMBL68269 | — | — | 1 | 9.00 |
| CHEMBL304802 | — | — | 1 | 8.70 |
| CHEMBL302493 | — | — | 1 | 8.70 |
| CHEMBL307330 | — | — | 1 | 8.55 |
| CHEMBL305267 | — | — | 1 | 8.40 |
| CHEMBL70017 | — | — | 1 | 8.07 |
| CHEMBL65939 | — | — | 1 | 8.00 |
| CHEMBL71787 | — | — | 1 | 7.92 |
| CHEMBL305777 | — | — | 1 | 7.57 |
| CHEMBL66762 | — | — | 1 | 7.55 |
| CHEMBL303712 | — | — | 1 | 5.70 |
| CHEMBL305035 | — | — | 1 | - |
| CHEMBL69353 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL291058 | — | IC50 | = | 0.05 | nM | 10.30 |
| CHEMBL69986 | — | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL308646 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL302974 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL304762 | — | IC50 | = | 0.29 | nM | 9.54 |
| CHEMBL69832 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL8981 | PD-156707 | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL408055 | — | IC50 | = | 0.38 | nM | 9.42 |
| CHEMBL303484 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL68269 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL304802 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL302493 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL307330 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL305267 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL70017 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL65939 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL71787 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL305777 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL66762 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL303712 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL305035 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL69353 | — | IC50 | > | 10.0 | nM | - |