Assay Detail
Binding
CHEMBL670643
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In vitro inhibition of endothelin binding to human Endothelin B 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 | 4.65 | 5.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL47417 | — | — | 1 | 5.36 |
| CHEMBL295697 | — | — | 1 | 5.23 |
| CHEMBL45760 | — | — | 1 | 5.21 |
| CHEMBL433074 | — | — | 1 | 5.16 |
| CHEMBL47418 | — | — | 1 | 5.13 |
| CHEMBL416086 | — | — | 1 | 5.12 |
| CHEMBL47827 | — | — | 1 | 5.08 |
| CHEMBL44321 | — | — | 1 | 5.06 |
| CHEMBL47620 | — | — | 1 | 5.04 |
| CHEMBL296326 | — | — | 1 | 5.04 |
| CHEMBL283136 | — | — | 1 | 5.00 |
| CHEMBL296456 | — | — | 1 | 4.91 |
| CHEMBL297618 | — | — | 1 | 4.86 |
| CHEMBL48134 | — | — | 1 | 4.85 |
| CHEMBL278114 | — | — | 1 | 4.85 |
| CHEMBL47604 | — | — | 1 | 4.84 |
| CHEMBL296129 | — | — | 1 | 4.80 |
| CHEMBL295588 | — | — | 1 | 4.78 |
| CHEMBL44539 | — | — | 1 | 4.71 |
| CHEMBL47828 | — | — | 1 | 4.70 |
| CHEMBL296927 | — | — | 1 | 4.59 |
| CHEMBL417719 | — | — | 1 | 4.59 |
| CHEMBL296291 | — | — | 1 | 4.52 |
| CHEMBL283535 | — | — | 1 | 4.49 |
| CHEMBL297473 | — | — | 1 | 4.45 |
| CHEMBL19808 | — | — | 1 | 4.39 |
| CHEMBL45087 | — | — | 1 | 4.35 |
| CHEMBL43788 | — | — | 1 | 4.29 |
| CHEMBL297215 | — | — | 1 | 4.21 |
| CHEMBL295207 | — | — | 1 | 4.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL47417 | — | IC50 | = | 4370.0 | nM | 5.36 |
| CHEMBL295697 | — | IC50 | = | 5890.0 | nM | 5.23 |
| CHEMBL45760 | — | IC50 | = | 6170.0 | nM | 5.21 |
| CHEMBL433074 | — | IC50 | = | 6920.0 | nM | 5.16 |
| CHEMBL47418 | — | IC50 | = | 7410.0 | nM | 5.13 |
| CHEMBL416086 | — | IC50 | = | 7590.0 | nM | 5.12 |
| CHEMBL47827 | — | IC50 | = | 8240.0 | nM | 5.08 |
| CHEMBL44321 | — | IC50 | = | 8710.0 | nM | 5.06 |
| CHEMBL47620 | — | IC50 | = | 9080.0 | nM | 5.04 |
| CHEMBL296326 | — | IC50 | = | 9120.0 | nM | 5.04 |
| CHEMBL283136 | — | IC50 | = | 10100.0 | nM | 5.00 |
| CHEMBL296456 | — | IC50 | = | 12200.0 | nM | 4.91 |
| CHEMBL297618 | — | IC50 | = | 13800.0 | nM | 4.86 |
| CHEMBL48134 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL278114 | — | IC50 | = | 14100.0 | nM | 4.85 |
| CHEMBL47604 | — | IC50 | = | 14400.0 | nM | 4.84 |
| CHEMBL296129 | — | IC50 | = | 15800.0 | nM | 4.80 |
| CHEMBL295588 | — | IC50 | = | 16800.0 | nM | 4.78 |
| CHEMBL44539 | — | IC50 | = | 19500.0 | nM | 4.71 |
| CHEMBL47828 | — | IC50 | = | 19800.0 | nM | 4.70 |
| CHEMBL296927 | — | IC50 | = | 25700.0 | nM | 4.59 |
| CHEMBL417719 | — | IC50 | = | 25700.0 | nM | 4.59 |
| CHEMBL296291 | — | IC50 | = | 30200.0 | nM | 4.52 |
| CHEMBL283535 | — | IC50 | = | 32600.0 | nM | 4.49 |
| CHEMBL297473 | — | IC50 | = | 35500.0 | nM | 4.45 |
| CHEMBL19808 | — | IC50 | = | 40400.0 | nM | 4.39 |
| CHEMBL45087 | — | IC50 | = | 44700.0 | nM | 4.35 |
| CHEMBL43788 | — | IC50 | = | 51900.0 | nM | 4.29 |
| CHEMBL297215 | — | IC50 | = | 61000.0 | nM | 4.21 |
| CHEMBL295207 | — | IC50 | = | 61700.0 | nM | 4.21 |
| CHEMBL288967 | — | IC50 | = | 63100.0 | nM | 4.20 |
| CHEMBL48024 | — | IC50 | = | 67500.0 | nM | 4.17 |
| CHEMBL45456 | — | IC50 | = | 67600.0 | nM | 4.17 |
| CHEMBL48031 | — | IC50 | = | 67400.0 | nM | 4.17 |
| CHEMBL45269 | — | IC50 | = | 77600.0 | nM | 4.11 |
| CHEMBL44615 | — | IC50 | = | 81400.0 | nM | 4.09 |
| CHEMBL48120 | — | IC50 | = | 92100.0 | nM | 4.04 |
| CHEMBL417358 | — | IC50 | = | 97700.0 | nM | 4.01 |
| CHEMBL295583 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL295632 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL47536 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL47008 | — | IC50 | = | 117000.0 | nM | - |
| CHEMBL47450 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL297107 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL296074 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL297048 | — | IC50 | > | 100000.0 | nM | - |