Assay Detail
Binding
CHEMBL670645
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor
57
Total Activities
57
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
The use of sulfonylamido pyrimidines incorporating an unsaturated side chain as endothelin receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 57 | 6.36 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL368996 | — | — | 1 | 7.89 |
| CHEMBL368383 | — | — | 1 | 7.75 |
| CHEMBL264035 | — | — | 1 | 7.55 |
| CHEMBL367036 | — | — | 1 | 7.50 |
| CHEMBL94786 | — | — | 1 | 7.38 |
| CHEMBL173358 | — | — | 1 | 7.36 |
| CHEMBL368828 | — | — | 1 | 7.31 |
| CHEMBL177203 | — | — | 1 | 7.30 |
| CHEMBL368211 | — | — | 1 | 7.11 |
| CHEMBL368829 | — | — | 1 | 7.00 |
| CHEMBL368386 | — | — | 1 | 6.91 |
| CHEMBL170342 | — | — | 1 | 6.74 |
| CHEMBL367453 | — | — | 1 | 6.71 |
| CHEMBL139734 | — | — | 1 | 6.70 |
| CHEMBL176482 | — | — | 1 | 6.69 |
| CHEMBL368989 | — | — | 1 | 6.68 |
| CHEMBL175057 | — | — | 1 | 6.66 |
| CHEMBL275897 | — | — | 1 | 6.63 |
| CHEMBL368117 | — | — | 1 | 6.62 |
| CHEMBL175058 | — | — | 1 | 6.62 |
| CHEMBL366797 | — | — | 1 | 6.59 |
| CHEMBL957 | BOSENTAN | 4.0 | 1 | 6.55 |
| CHEMBL174094 | — | — | 1 | 6.53 |
| CHEMBL366652 | — | — | 1 | 6.53 |
| CHEMBL176999 | — | — | 1 | 6.44 |
| CHEMBL163638 | — | — | 1 | 6.23 |
| CHEMBL175278 | — | — | 1 | 6.22 |
| CHEMBL369362 | — | — | 1 | 6.21 |
| CHEMBL366885 | — | — | 1 | 6.18 |
| CHEMBL173721 | — | — | 1 | 6.13 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL368996 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL368383 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL264035 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL367036 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL94786 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL173358 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL368828 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL177203 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL368211 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL368829 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL368386 | — | IC50 | = | 123.0 | nM | 6.91 |
| CHEMBL170342 | — | IC50 | = | 183.0 | nM | 6.74 |
| CHEMBL367453 | — | IC50 | = | 197.0 | nM | 6.71 |
| CHEMBL139734 | — | IC50 | = | 199.0 | nM | 6.70 |
| CHEMBL176482 | — | IC50 | = | 205.0 | nM | 6.69 |
| CHEMBL368989 | — | IC50 | = | 207.0 | nM | 6.68 |
| CHEMBL175057 | — | IC50 | = | 221.0 | nM | 6.66 |
| CHEMBL275897 | — | IC50 | = | 236.0 | nM | 6.63 |
| CHEMBL368117 | — | IC50 | = | 238.0 | nM | 6.62 |
| CHEMBL175058 | — | IC50 | = | 241.0 | nM | 6.62 |
| CHEMBL366797 | — | IC50 | = | 258.0 | nM | 6.59 |
| CHEMBL957 | BOSENTAN | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL174094 | — | IC50 | = | 295.0 | nM | 6.53 |
| CHEMBL366652 | — | IC50 | = | 294.0 | nM | 6.53 |
| CHEMBL176999 | — | IC50 | = | 366.0 | nM | 6.44 |
| CHEMBL163638 | — | IC50 | = | 589.0 | nM | 6.23 |
| CHEMBL175278 | — | IC50 | = | 603.0 | nM | 6.22 |
| CHEMBL369362 | — | IC50 | = | 612.0 | nM | 6.21 |
| CHEMBL366885 | — | IC50 | = | 656.0 | nM | 6.18 |
| CHEMBL173721 | — | IC50 | = | 744.0 | nM | 6.13 |
| CHEMBL368929 | — | IC50 | = | 746.0 | nM | 6.13 |
| CHEMBL177143 | — | IC50 | = | 823.0 | nM | 6.08 |
| CHEMBL367382 | — | IC50 | = | 832.0 | nM | 6.08 |
| CHEMBL176741 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL173465 | — | IC50 | = | 903.0 | nM | 6.04 |
| CHEMBL173689 | — | IC50 | = | 973.0 | nM | 6.01 |
| CHEMBL176664 | — | IC50 | = | 1030.0 | nM | 5.99 |
| CHEMBL368860 | — | IC50 | = | 1060.0 | nM | 5.97 |
| CHEMBL173743 | — | IC50 | = | 1140.0 | nM | 5.94 |
| CHEMBL175435 | — | IC50 | = | 1190.0 | nM | 5.92 |
| CHEMBL367767 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL175111 | — | IC50 | = | 1520.0 | nM | 5.82 |
| CHEMBL367686 | — | IC50 | = | 1670.0 | nM | 5.78 |
| CHEMBL172184 | — | IC50 | = | 1950.0 | nM | 5.71 |
| CHEMBL425682 | — | IC50 | = | 2030.0 | nM | 5.69 |
| CHEMBL367339 | — | IC50 | = | 2085.0 | nM | 5.68 |
| CHEMBL176650 | — | IC50 | = | 2280.0 | nM | 5.64 |
| CHEMBL170401 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL176698 | — | IC50 | = | 2620.0 | nM | 5.58 |
| CHEMBL177111 | — | IC50 | = | 2880.0 | nM | 5.54 |