Assay Detail
Binding
CHEMBL682358
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
46
Total Activities
46
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 N2-aryl-3-(isoxazolylsulfamoyl)-2-thiophenecarboxamides as selective endothelin receptor-A antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 46 | 7.43 | 8.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL48134 | — | — | 1 | 8.59 |
| CHEMBL297473 | — | — | 1 | 8.52 |
| CHEMBL19808 | — | — | 1 | 8.47 |
| CHEMBL417719 | — | — | 1 | 8.42 |
| CHEMBL296456 | — | — | 1 | 8.41 |
| CHEMBL296927 | — | — | 1 | 8.35 |
| CHEMBL47604 | — | — | 1 | 8.29 |
| CHEMBL295588 | — | — | 1 | 8.25 |
| CHEMBL47620 | — | — | 1 | 8.22 |
| CHEMBL296129 | — | — | 1 | 8.21 |
| CHEMBL47827 | — | — | 1 | 8.18 |
| CHEMBL47828 | — | — | 1 | 8.17 |
| CHEMBL297618 | — | — | 1 | 8.03 |
| CHEMBL283535 | — | — | 1 | 8.00 |
| CHEMBL297215 | — | — | 1 | 7.97 |
| CHEMBL296326 | — | — | 1 | 7.92 |
| CHEMBL45087 | — | — | 1 | 7.89 |
| CHEMBL278114 | — | — | 1 | 7.82 |
| CHEMBL43788 | — | — | 1 | 7.82 |
| CHEMBL47418 | — | — | 1 | 7.77 |
| CHEMBL283136 | — | — | 1 | 7.72 |
| CHEMBL47417 | — | — | 1 | 7.70 |
| CHEMBL296291 | — | — | 1 | 7.62 |
| CHEMBL47450 | — | — | 1 | 7.57 |
| CHEMBL295583 | — | — | 1 | 7.51 |
| CHEMBL45456 | — | — | 1 | 7.50 |
| CHEMBL433074 | — | — | 1 | 7.33 |
| CHEMBL295697 | — | — | 1 | 7.27 |
| CHEMBL48120 | — | — | 1 | 7.24 |
| CHEMBL47008 | — | — | 1 | 7.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL48134 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL297473 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL19808 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL417719 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL296456 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL296927 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL47604 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL295588 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL47620 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL296129 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL47827 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL47828 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL297618 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL283535 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL297215 | — | IC50 | = | 10.8 | nM | 7.97 |
| CHEMBL296326 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL45087 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL278114 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL43788 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL47418 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL283136 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL47417 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL296291 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL47450 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL295583 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL45456 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL433074 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL295697 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL48120 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL47008 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL44615 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL288967 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL48031 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL295207 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL48024 | — | IC50 | = | 146.0 | nM | 6.84 |
| CHEMBL45269 | — | IC50 | = | 166.0 | nM | 6.78 |
| CHEMBL45760 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL44539 | — | IC50 | = | 214.0 | nM | 6.67 |
| CHEMBL417358 | — | IC50 | = | 229.0 | nM | 6.64 |
| CHEMBL295632 | — | IC50 | = | 549.0 | nM | 6.26 |
| CHEMBL297107 | — | IC50 | = | 838.0 | nM | 6.08 |
| CHEMBL416086 | — | IC50 | = | 933.0 | nM | 6.03 |
| CHEMBL44321 | — | IC50 | = | 977.0 | nM | 6.01 |
| CHEMBL297048 | — | IC50 | = | 1290.0 | nM | 5.89 |
| CHEMBL296074 | — | IC50 | = | 1430.0 | nM | 5.84 |
| CHEMBL47536 | — | IC50 | = | 1910.0 | nM | 5.72 |