Assay Detail
Binding
CHEMBL682104
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Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
64
Total Activities
64
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HTB 139) |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Halogen substitution at the isoxazole ring enhances the activity of N-(isoxazolyl)sulfonamide endothelin antagonists
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 64 | 6.39 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL80857 | — | — | 1 | 8.85 |
| CHEMBL309692 | — | — | 1 | 8.55 |
| CHEMBL310739 | — | — | 1 | 8.42 |
| CHEMBL311138 | — | — | 1 | 8.21 |
| CHEMBL78563 | — | — | 1 | 8.09 |
| CHEMBL311781 | — | — | 1 | 7.81 |
| CHEMBL79066 | — | — | 1 | 7.57 |
| CHEMBL311742 | — | — | 1 | 7.54 |
| CHEMBL312266 | — | — | 1 | 7.40 |
| CHEMBL80484 | — | — | 1 | 7.36 |
| CHEMBL78830 | — | — | 1 | 7.28 |
| CHEMBL311461 | — | — | 1 | 7.21 |
| CHEMBL80438 | — | — | 1 | 7.15 |
| CHEMBL312187 | — | — | 1 | 7.14 |
| CHEMBL78080 | — | — | 1 | 7.10 |
| CHEMBL80342 | — | — | 1 | 6.96 |
| CHEMBL309397 | — | — | 1 | 6.96 |
| CHEMBL80538 | — | — | 1 | 6.92 |
| CHEMBL312685 | — | — | 1 | 6.92 |
| CHEMBL311216 | — | — | 1 | 6.85 |
| CHEMBL78929 | — | — | 1 | 6.85 |
| CHEMBL310361 | — | — | 1 | 6.80 |
| CHEMBL311510 | — | — | 1 | 6.80 |
| CHEMBL78669 | — | — | 1 | 6.77 |
| CHEMBL79031 | — | — | 1 | 6.64 |
| CHEMBL80808 | — | — | 1 | 6.64 |
| CHEMBL420029 | — | — | 1 | 6.62 |
| CHEMBL80532 | — | — | 1 | 6.57 |
| CHEMBL80807 | — | — | 1 | 6.57 |
| CHEMBL311455 | — | — | 1 | 6.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL80857 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL309692 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL310739 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL311138 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL78563 | — | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL311781 | — | IC50 | = | 15.6 | nM | 7.81 |
| CHEMBL79066 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL311742 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL312266 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL80484 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL78830 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL311461 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL80438 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL312187 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL78080 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL80342 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL309397 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL80538 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL312685 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL311216 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL78929 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL310361 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL311510 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL78669 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL80808 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL79031 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL420029 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL80532 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL80807 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL311455 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL76949 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL76779 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL80317 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL78853 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL312670 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL80507 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL417651 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL80506 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL76420 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL78499 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL80180 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL453 | SULFISOXAZOLE | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL308521 | — | IC50 | = | 980.0 | nM | 6.01 |
| CHEMBL77090 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL312551 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL76438 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL76360 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL81593 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL310944 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL78552 | — | IC50 | = | 2000.0 | nM | 5.70 |