Assay Detail
Functional
CHEMBL796076
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibitory potency at native endothelin A and endothelin B receptors by inhibiting endothelin-1 contractions of rat aortic rings
48
Total Activities
48
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Expert |
Publication
Novel benzo[1,4]diazepin-2-one derivatives as endothelin receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| pA2 | 41 | - | - |
| Kd | 7 | 7.77 | 8.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL330104 | — | — | 1 | 8.55 |
| CHEMBL329477 | — | — | 1 | 8.18 |
| CHEMBL329251 | — | — | 1 | 7.83 |
| CHEMBL431286 | — | — | 1 | 7.80 |
| CHEMBL91873 | — | — | 1 | 7.59 |
| CHEMBL313867 | — | — | 1 | 7.35 |
| CHEMBL316878 | — | — | 1 | 7.08 |
| CHEMBL96193 | — | — | 1 | - |
| CHEMBL431087 | — | — | 1 | - |
| CHEMBL420435 | — | — | 1 | - |
| CHEMBL327976 | — | — | 1 | - |
| CHEMBL91926 | — | — | 1 | - |
| CHEMBL94766 | — | — | 1 | - |
| CHEMBL419879 | — | — | 1 | - |
| CHEMBL328073 | — | — | 1 | - |
| CHEMBL95095 | — | — | 1 | - |
| CHEMBL96154 | — | — | 1 | - |
| CHEMBL313870 | — | — | 1 | - |
| CHEMBL94752 | — | — | 1 | - |
| CHEMBL96313 | — | — | 1 | - |
| CHEMBL96472 | — | — | 1 | - |
| CHEMBL431460 | — | — | 1 | - |
| CHEMBL94446 | — | — | 1 | - |
| CHEMBL316629 | — | — | 1 | - |
| CHEMBL96387 | — | — | 1 | - |
| CHEMBL329744 | — | — | 1 | - |
| CHEMBL330359 | — | — | 1 | - |
| CHEMBL94438 | — | — | 1 | - |
| CHEMBL96422 | — | — | 1 | - |
| CHEMBL94091 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL330104 | — | Kd | = | 2.818 | nM | 8.55 |
| CHEMBL329477 | — | Kd | = | 6.607 | nM | 8.18 |
| CHEMBL329251 | — | Kd | = | 14.79 | nM | 7.83 |
| CHEMBL431286 | — | Kd | = | 15.85 | nM | 7.80 |
| CHEMBL91873 | — | Kd | = | 25.7 | nM | 7.59 |
| CHEMBL313867 | — | Kd | = | 44.67 | nM | 7.35 |
| CHEMBL316878 | — | Kd | = | 83.18 | nM | 7.08 |
| CHEMBL316851 | — | pA2 | - | — | - | |
| CHEMBL313870 | — | pA2 | - | — | - | |
| CHEMBL96318 | — | pA2 | - | — | - | |
| CHEMBL318247 | — | pA2 | - | — | - | |
| CHEMBL96506 | — | pA2 | - | — | - | |
| CHEMBL319007 | — | pA2 | - | — | - | |
| CHEMBL317589 | — | pA2 | - | — | - | |
| CHEMBL314946 | — | pA2 | - | — | - | |
| CHEMBL431087 | — | pA2 | - | — | - | |
| CHEMBL96114 | — | pA2 | - | — | - | |
| CHEMBL94212 | — | pA2 | - | — | - | |
| CHEMBL450628 | — | pA2 | - | — | - | |
| CHEMBL96746 | — | pA2 | - | — | - | |
| CHEMBL94962 | — | pA2 | - | — | - | |
| CHEMBL96463 | — | pA2 | - | — | - | |
| CHEMBL93820 | — | pA2 | - | — | - | |
| CHEMBL95017 | — | pA2 | - | — | - | |
| CHEMBL329943 | — | pA2 | - | — | - | |
| CHEMBL433173 | — | pA2 | - | — | - | |
| CHEMBL93612 | — | pA2 | - | — | - | |
| CHEMBL96313 | — | pA2 | - | — | - | |
| CHEMBL94091 | — | pA2 | - | — | - | |
| CHEMBL96422 | — | pA2 | - | — | - | |
| CHEMBL94438 | — | pA2 | - | — | - | |
| CHEMBL330359 | — | pA2 | - | — | - | |
| CHEMBL329744 | — | pA2 | - | — | - | |
| CHEMBL96387 | — | pA2 | - | — | - | |
| CHEMBL316629 | — | pA2 | - | — | - | |
| CHEMBL94446 | — | pA2 | - | — | - | |
| CHEMBL431460 | — | pA2 | - | — | - | |
| CHEMBL96472 | — | pA2 | - | — | - | |
| CHEMBL96154 | — | pA2 | - | — | - | |
| CHEMBL94752 | — | pA2 | - | — | - | |
| CHEMBL96193 | — | pA2 | - | — | - | |
| CHEMBL420435 | — | pA2 | - | — | - | |
| CHEMBL327976 | — | pA2 | - | — | - | |
| CHEMBL91926 | — | pA2 | - | — | - | |
| CHEMBL94766 | — | pA2 | - | — | - | |
| CHEMBL419879 | — | pA2 | - | — | - | |
| CHEMBL328073 | — | pA2 | - | — | - | |
| CHEMBL95095 | — | pA2 | - | — | - |