Assay Detail
Functional
CHEMBL670641
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity towards human recombinant Endothelin B 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 | 6.88 | 8.18 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL330104 | — | — | 1 | 8.18 |
| CHEMBL330135 | — | — | 1 | 8.15 |
| CHEMBL415010 | — | — | 1 | 7.96 |
| CHEMBL431286 | — | — | 1 | 7.96 |
| CHEMBL94580 | — | — | 1 | 7.88 |
| CHEMBL95017 | — | — | 1 | 7.88 |
| CHEMBL96303 | — | — | 1 | 7.87 |
| CHEMBL319007 | — | — | 1 | 7.81 |
| CHEMBL419136 | — | — | 1 | 7.81 |
| CHEMBL94212 | — | — | 1 | 7.78 |
| CHEMBL329251 | — | — | 1 | 7.75 |
| CHEMBL96114 | — | — | 1 | 7.74 |
| CHEMBL93820 | — | — | 1 | 7.73 |
| CHEMBL96171 | — | — | 1 | 7.67 |
| CHEMBL327976 | — | — | 1 | 7.67 |
| CHEMBL96506 | — | — | 1 | 7.65 |
| CHEMBL316878 | — | — | 1 | 7.65 |
| CHEMBL96154 | — | — | 1 | 7.62 |
| CHEMBL318086 | — | — | 1 | 7.60 |
| CHEMBL94766 | — | — | 1 | 7.60 |
| CHEMBL317589 | — | — | 1 | 7.59 |
| CHEMBL96746 | — | — | 1 | 7.57 |
| CHEMBL406551 | — | — | 1 | 7.54 |
| CHEMBL96422 | — | — | 1 | 7.51 |
| CHEMBL91873 | — | — | 1 | 7.49 |
| CHEMBL96723 | — | — | 1 | 7.48 |
| CHEMBL94934 | — | — | 1 | 7.48 |
| CHEMBL330354 | — | — | 1 | 7.48 |
| CHEMBL94438 | — | — | 1 | 7.48 |
| CHEMBL420435 | — | — | 1 | 7.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL330104 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL330135 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL431286 | — | IC50 | = | 10.9 | nM | 7.96 |
| CHEMBL415010 | — | IC50 | = | 11.1 | nM | 7.96 |
| CHEMBL95017 | — | IC50 | = | 13.1 | nM | 7.88 |
| CHEMBL94580 | — | IC50 | = | 13.2 | nM | 7.88 |
| CHEMBL96303 | — | IC50 | = | 13.6 | nM | 7.87 |
| CHEMBL419136 | — | IC50 | = | 15.5 | nM | 7.81 |
| CHEMBL319007 | — | IC50 | = | 15.6 | nM | 7.81 |
| CHEMBL94212 | — | IC50 | = | 16.7 | nM | 7.78 |
| CHEMBL329251 | — | IC50 | = | 17.7 | nM | 7.75 |
| CHEMBL96114 | — | IC50 | = | 18.3 | nM | 7.74 |
| CHEMBL93820 | — | IC50 | = | 18.5 | nM | 7.73 |
| CHEMBL327976 | — | IC50 | = | 21.4 | nM | 7.67 |
| CHEMBL96171 | — | IC50 | = | 21.5 | nM | 7.67 |
| CHEMBL316878 | — | IC50 | = | 22.4 | nM | 7.65 |
| CHEMBL96506 | — | IC50 | = | 22.5 | nM | 7.65 |
| CHEMBL96154 | — | IC50 | = | 24.1 | nM | 7.62 |
| CHEMBL318086 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL94766 | — | IC50 | = | 25.3 | nM | 7.60 |
| CHEMBL317589 | — | IC50 | = | 25.5 | nM | 7.59 |
| CHEMBL96746 | — | IC50 | = | 26.8 | nM | 7.57 |
| CHEMBL406551 | — | IC50 | = | 28.8 | nM | 7.54 |
| CHEMBL96422 | — | IC50 | = | 30.8 | nM | 7.51 |
| CHEMBL91873 | — | IC50 | = | 32.2 | nM | 7.49 |
| CHEMBL420435 | — | IC50 | = | 32.8 | nM | 7.48 |
| CHEMBL330354 | — | IC50 | = | 33.2 | nM | 7.48 |
| CHEMBL94438 | — | IC50 | = | 32.9 | nM | 7.48 |
| CHEMBL94934 | — | IC50 | = | 33.2 | nM | 7.48 |
| CHEMBL96723 | — | IC50 | = | 33.1 | nM | 7.48 |
| CHEMBL422068 | — | IC50 | = | 36.5 | nM | 7.44 |
| CHEMBL94810 | — | IC50 | = | 39.9 | nM | 7.40 |
| CHEMBL91926 | — | IC50 | = | 47.1 | nM | 7.33 |
| CHEMBL433173 | — | IC50 | = | 47.8 | nM | 7.32 |
| CHEMBL96472 | — | IC50 | = | 48.1 | nM | 7.32 |
| CHEMBL95013 | — | IC50 | = | 47.4 | nM | 7.32 |
| CHEMBL95095 | — | IC50 | = | 49.3 | nM | 7.31 |
| CHEMBL93084 | — | IC50 | = | 49.7 | nM | 7.30 |
| CHEMBL314755 | — | IC50 | = | 49.7 | nM | 7.30 |
| CHEMBL317510 | — | IC50 | = | 50.7 | nM | 7.29 |
| CHEMBL314946 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL94964 | — | IC50 | = | 65.6 | nM | 7.18 |
| CHEMBL96932 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL431087 | — | IC50 | = | 68.8 | nM | 7.16 |
| CHEMBL316301 | — | IC50 | = | 70.3 | nM | 7.15 |
| CHEMBL419879 | — | IC50 | = | 72.7 | nM | 7.14 |
| CHEMBL329744 | — | IC50 | = | 73.6 | nM | 7.13 |
| CHEMBL96387 | — | IC50 | = | 74.9 | nM | 7.13 |
| CHEMBL96313 | — | IC50 | = | 78.2 | nM | 7.11 |
| CHEMBL431460 | — | IC50 | = | 80.2 | nM | 7.10 |