Assay Detail
Binding
CHEMBL670651
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Inhibitory activity against [125I]ET1 binding to human endothelin B receptor
25
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Structure-activity relationships of a novel class of endothelin receptor selective antagonists; 6-carboxy-2-isopropylamino-5,7-diarylcyclopenteno[1,2-b]pyridines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 7.41 | 8.25 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL286621 | — | — | 2 | 8.25 |
| CHEMBL287683 | — | — | 2 | 8.02 |
| CHEMBL411925 | — | — | 2 | 7.96 |
| CHEMBL432856 | — | — | 1 | 7.85 |
| CHEMBL287622 | — | — | 1 | 7.72 |
| CHEMBL35984 | — | — | 1 | 7.70 |
| CHEMBL37920 | — | — | 1 | 7.64 |
| CHEMBL289634 | — | — | 2 | 7.60 |
| CHEMBL36627 | — | — | 1 | 7.60 |
| CHEMBL37427 | — | — | 1 | 7.37 |
| CHEMBL38000 | — | — | 1 | 7.35 |
| CHEMBL288247 | — | — | 2 | 7.29 |
| CHEMBL289216 | — | — | 2 | 7.21 |
| CHEMBL287711 | — | — | 1 | 7.21 |
| CHEMBL290181 | — | — | 1 | 7.06 |
| CHEMBL291247 | — | — | 1 | 7.00 |
| CHEMBL36671 | — | — | 1 | 6.54 |
| CHEMBL37973 | — | — | 1 | 6.38 |
| CHEMBL287517 | — | — | 1 | 6.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL286621 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL286621 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL287683 | — | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL411925 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL432856 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL411925 | — | IC50 | = | 15.7 | nM | 7.80 |
| CHEMBL287622 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL35984 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL37920 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL289634 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL36627 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL287683 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL37427 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL38000 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL289634 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL288247 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL288247 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL289216 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL287711 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL289216 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL290181 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL291247 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL36671 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL37973 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL287517 | — | IC50 | = | 480.0 | nM | 6.32 |