Assay Detail
Binding
CHEMBL681515
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Amide bond surrogates: A study in thiophenesulfonamide based endothelin receptor antagonists
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 6.81 | 7.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL173761 | — | — | 1 | 7.36 |
| CHEMBL171972 | — | — | 1 | 7.34 |
| CHEMBL172248 | — | — | 1 | 7.28 |
| CHEMBL175045 | — | — | 1 | 7.26 |
| CHEMBL173977 | — | — | 1 | 7.24 |
| CHEMBL368780 | — | — | 1 | 7.21 |
| CHEMBL176675 | — | — | 1 | 7.14 |
| CHEMBL366680 | — | — | 1 | 7.10 |
| CHEMBL426218 | — | — | 1 | 7.09 |
| CHEMBL366378 | — | — | 1 | 7.04 |
| CHEMBL173189 | — | — | 1 | 6.99 |
| CHEMBL174086 | — | — | 1 | 6.97 |
| CHEMBL367763 | — | — | 1 | 6.85 |
| CHEMBL172987 | — | — | 1 | 6.78 |
| CHEMBL435346 | — | — | 1 | 6.75 |
| CHEMBL173982 | — | — | 1 | 6.69 |
| CHEMBL174363 | — | — | 1 | 6.66 |
| CHEMBL176422 | — | — | 1 | 6.64 |
| CHEMBL177070 | — | — | 1 | 6.62 |
| CHEMBL366364 | — | — | 1 | 6.46 |
| CHEMBL277595 | — | — | 1 | 6.20 |
| CHEMBL367024 | — | — | 1 | 4.21 |
| CHEMBL292802 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL173761 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL171972 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL172248 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL175045 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL173977 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL368780 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL176675 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL366680 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL426218 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL366378 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL173189 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL174086 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL367763 | — | IC50 | = | 141.0 | nM | 6.85 |
| CHEMBL172987 | — | IC50 | = | 166.0 | nM | 6.78 |
| CHEMBL435346 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL173982 | — | IC50 | = | 205.0 | nM | 6.69 |
| CHEMBL174363 | — | IC50 | = | 218.0 | nM | 6.66 |
| CHEMBL176422 | — | IC50 | = | 231.0 | nM | 6.64 |
| CHEMBL177070 | — | IC50 | = | 237.0 | nM | 6.62 |
| CHEMBL366364 | — | IC50 | = | 347.0 | nM | 6.46 |
| CHEMBL277595 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL367024 | — | IC50 | = | 62000.0 | nM | 4.21 |
| CHEMBL292802 | — | IC50 | = | 8900.0 | nM | - |