Assay Detail
Functional
CHEMBL682357
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
104
Total Activities
104
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Novel benzo[1,4]diazepin-2-one derivatives as endothelin receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 104 | 7.58 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL329251 | — | — | 1 | 8.96 |
| CHEMBL431286 | — | — | 1 | 8.85 |
| CHEMBL330104 | — | — | 1 | 8.74 |
| CHEMBL94580 | — | — | 1 | 8.62 |
| CHEMBL91873 | — | — | 1 | 8.60 |
| CHEMBL329477 | — | — | 1 | 8.60 |
| CHEMBL316453 | — | — | 1 | 8.52 |
| CHEMBL96932 | — | — | 1 | 8.51 |
| CHEMBL96723 | — | — | 1 | 8.46 |
| CHEMBL415010 | — | — | 1 | 8.46 |
| CHEMBL93820 | — | — | 1 | 8.43 |
| CHEMBL96171 | — | — | 1 | 8.41 |
| CHEMBL316878 | — | — | 1 | 8.34 |
| CHEMBL94212 | — | — | 1 | 8.30 |
| CHEMBL327976 | — | — | 1 | 8.24 |
| CHEMBL314755 | — | — | 1 | 8.23 |
| CHEMBL318247 | — | — | 1 | 8.22 |
| CHEMBL317510 | — | — | 1 | 8.20 |
| CHEMBL317589 | — | — | 1 | 8.19 |
| CHEMBL95013 | — | — | 1 | 8.19 |
| CHEMBL93084 | — | — | 1 | 8.19 |
| CHEMBL420435 | — | — | 1 | 8.19 |
| CHEMBL94964 | — | — | 1 | 8.18 |
| CHEMBL96746 | — | — | 1 | 8.17 |
| CHEMBL94438 | — | — | 1 | 8.17 |
| CHEMBL419136 | — | — | 1 | 8.17 |
| CHEMBL406551 | — | — | 1 | 8.17 |
| CHEMBL328878 | — | — | 1 | 8.16 |
| CHEMBL94934 | — | — | 1 | 8.14 |
| CHEMBL96318 | — | — | 1 | 8.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL329251 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL431286 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL330104 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL94580 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL329477 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL91873 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL316453 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL96932 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL96723 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL415010 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL93820 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL96171 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL316878 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL94212 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL327976 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL314755 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL318247 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL317510 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL420435 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL93084 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL317589 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL95013 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL94964 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL419136 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL96746 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL406551 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL94438 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL328878 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL94934 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL419879 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL96318 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL316301 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL330135 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL433173 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL95017 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL319754 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL422068 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL314946 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL319007 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL95095 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL96472 | — | IC50 | = | 10.2 | nM | 7.99 |
| CHEMBL316629 | — | IC50 | = | 10.2 | nM | 7.99 |
| CHEMBL96422 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL94766 | — | IC50 | = | 11.8 | nM | 7.93 |
| CHEMBL330425 | — | IC50 | = | 12.3 | nM | 7.91 |
| CHEMBL313867 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL330354 | — | IC50 | = | 13.9 | nM | 7.86 |
| CHEMBL96114 | — | IC50 | = | 17.1 | nM | 7.77 |
| CHEMBL318086 | — | IC50 | = | 16.9 | nM | 7.77 |
| CHEMBL96154 | — | IC50 | = | 17.1 | nM | 7.77 |