Assay Detail
Functional
CHEMBL676488
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In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Bis-sulfonamides as endothelin receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 15 | 6.38 | 7.02 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL367958 | — | — | 1 | 7.02 |
| CHEMBL177802 | — | — | 1 | 6.98 |
| CHEMBL367444 | — | — | 1 | 6.92 |
| CHEMBL177538 | — | — | 1 | 6.61 |
| CHEMBL368738 | — | — | 1 | 6.61 |
| CHEMBL171950 | — | — | 1 | 6.54 |
| CHEMBL368617 | — | — | 1 | 6.52 |
| CHEMBL367443 | — | — | 1 | 6.51 |
| CHEMBL172071 | — | — | 1 | 6.46 |
| CHEMBL172297 | — | — | 1 | 6.16 |
| CHEMBL369676 | — | — | 1 | 6.08 |
| CHEMBL172030 | — | — | 1 | 6.08 |
| CHEMBL176997 | — | — | 1 | 5.50 |
| CHEMBL368107 | — | — | 1 | 5.32 |
| CHEMBL173201 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL367958 | — | Kd | = | 95.5 | nM | 7.02 |
| CHEMBL177802 | — | Kd | = | 104.71 | nM | 6.98 |
| CHEMBL367444 | — | Kd | = | 120.23 | nM | 6.92 |
| CHEMBL177538 | — | Kd | = | 245.47 | nM | 6.61 |
| CHEMBL368738 | — | Kd | = | 245.47 | nM | 6.61 |
| CHEMBL171950 | — | Kd | = | 288.4 | nM | 6.54 |
| CHEMBL368617 | — | Kd | = | 302.0 | nM | 6.52 |
| CHEMBL367443 | — | Kd | = | 309.03 | nM | 6.51 |
| CHEMBL172071 | — | Kd | = | 346.74 | nM | 6.46 |
| CHEMBL172297 | — | Kd | = | 691.83 | nM | 6.16 |
| CHEMBL369676 | — | Kd | = | 831.76 | nM | 6.08 |
| CHEMBL172030 | — | Kd | = | 831.76 | nM | 6.08 |
| CHEMBL176997 | — | Kd | = | 3162.28 | nM | 5.50 |
| CHEMBL368107 | — | Kd | = | 4786.3 | nM | 5.32 |
| CHEMBL173201 | — | Kd | > | 10000.0 | nM | - |