Assay Detail
Binding
CHEMBL682105
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Binding affinity against human cloned endothelin A receptor expressed in LTK-cells
76
Total Activities
76
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 in a series of orally active gamma-hydroxy butenolide endothelin antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 76 | 7.42 | 9.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL417067 | — | — | 1 | 9.92 |
| CHEMBL8981 | PD-156707 | — | 1 | 9.52 |
| CHEMBL10781 | — | — | 1 | 9.30 |
| CHEMBL11369 | — | — | 1 | 9.30 |
| CHEMBL10854 | — | — | 1 | 9.05 |
| CHEMBL10697 | — | — | 1 | 8.92 |
| CHEMBL268480 | — | — | 1 | 8.85 |
| CHEMBL274359 | — | — | 1 | 8.77 |
| CHEMBL275701 | — | — | 1 | 8.74 |
| CHEMBL11115 | — | — | 1 | 8.74 |
| CHEMBL273723 | — | — | 1 | 8.68 |
| CHEMBL10924 | — | — | 1 | 8.62 |
| CHEMBL10607 | — | — | 1 | 8.52 |
| CHEMBL10636 | — | — | 1 | 8.41 |
| CHEMBL10661 | — | — | 1 | 8.40 |
| CHEMBL10794 | — | — | 1 | 8.17 |
| CHEMBL274383 | PD-155080 | — | 1 | 8.13 |
| CHEMBL10635 | — | — | 1 | 8.12 |
| CHEMBL10744 | — | — | 1 | 8.10 |
| CHEMBL275559 | — | — | 1 | 8.09 |
| CHEMBL11176 | — | — | 1 | 8.07 |
| CHEMBL10843 | — | — | 1 | 8.00 |
| CHEMBL10860 | — | — | 1 | 8.00 |
| CHEMBL10846 | — | — | 1 | 7.96 |
| CHEMBL276252 | — | — | 1 | 7.96 |
| CHEMBL417428 | — | — | 1 | 7.96 |
| CHEMBL10588 | — | — | 1 | 7.92 |
| CHEMBL274175 | — | — | 1 | 7.92 |
| CHEMBL10834 | — | — | 1 | 7.89 |
| CHEMBL273948 | — | — | 1 | 7.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL417067 | — | IC50 | = | 0.12 | nM | 9.92 |
| CHEMBL8981 | PD-156707 | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL11369 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL10781 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL10854 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL10697 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL268480 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL274359 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL275701 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL11115 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL273723 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL10924 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL10607 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL10636 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL10661 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL10794 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL274383 | PD-155080 | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL10635 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL10744 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL275559 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL11176 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL10843 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL10860 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL417428 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL10846 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL276252 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL10588 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL274175 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL10834 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL273948 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL11106 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL269453 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL276639 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL269409 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL417978 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL10589 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL10948 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL10644 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL10919 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL10910 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL10676 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL268754 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL10915 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL10374 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL10901 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL276018 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL274307 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL10733 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL10926 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL10996 | — | IC50 | = | 170.0 | nM | 6.77 |