Assay Detail
Binding
CHEMBL677977
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Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
50
Total Activities
50
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Synthesis and structure-activity relationships of 2-substituted D-tryptophan-containing peptidic endothelin receptor antagonists: importance of the C-2 substituent of the D-tryptophan residue for endothelin A and B receptor subtype selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 50 | 7.62 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL307936 | — | — | 1 | 9.00 |
| CHEMBL2304015 | — | — | 1 | 8.74 |
| CHEMBL305524 | — | — | 1 | 8.72 |
| CHEMBL308403 | — | — | 1 | 8.70 |
| CHEMBL72891 | — | — | 1 | 8.62 |
| CHEMBL2304007 | — | — | 1 | 8.57 |
| CHEMBL308621 | — | — | 1 | 8.55 |
| CHEMBL305650 | — | — | 1 | 8.42 |
| CHEMBL73925 | — | — | 1 | 8.42 |
| CHEMBL311134 | — | — | 1 | 8.32 |
| CHEMBL2304006 | — | — | 1 | 8.31 |
| CHEMBL424422 | — | — | 1 | 8.25 |
| CHEMBL77083 | — | — | 1 | 8.24 |
| CHEMBL74471 | — | — | 1 | 8.17 |
| CHEMBL308584 | — | — | 1 | 8.10 |
| CHEMBL310111 | — | — | 1 | 8.09 |
| CHEMBL2304011 | — | — | 1 | 8.09 |
| CHEMBL306977 | — | — | 1 | 8.05 |
| CHEMBL308815 | — | — | 1 | 8.04 |
| CHEMBL77033 | — | — | 1 | 8.04 |
| CHEMBL307903 | — | — | 1 | 8.03 |
| CHEMBL76735 | — | — | 1 | 8.02 |
| CHEMBL77853 | — | — | 1 | 8.01 |
| CHEMBL449962 | — | — | 1 | 7.85 |
| CHEMBL412602 | — | — | 1 | 7.82 |
| CHEMBL2304012 | — | — | 1 | 7.72 |
| CHEMBL78230 | — | — | 1 | 7.70 |
| CHEMBL311384 | — | — | 1 | 7.68 |
| CHEMBL303185 | — | — | 1 | 7.66 |
| CHEMBL308383 | — | — | 1 | 7.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL307936 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL2304015 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL305524 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL308403 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL72891 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL2304007 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL308621 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL305650 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL73925 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL311134 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL2304006 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL424422 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL77083 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL74471 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL308584 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL310111 | — | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL2304011 | — | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL306977 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL308815 | — | IC50 | = | 9.2 | nM | 8.04 |
| CHEMBL77033 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL307903 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL76735 | — | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL77853 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL449962 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL412602 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2304012 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL78230 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL311384 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL303185 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL308383 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL77468 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL2304016 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL2304013 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL306171 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL2304009 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL2304018 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL74000 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL273583 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL2304005 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL2304008 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL2304010 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL1744023 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL74837 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL405724 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL309003 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL78023 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL306123 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL2304014 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL307077 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL2304017 | — | IC50 | = | 23000.0 | nM | 4.64 |