Assay Detail
Binding
CHEMBL677440
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Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells
76
Total Activities
76
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO-K1 |
| 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 | 5.61 | 6.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL10854 | — | — | 1 | 6.75 |
| CHEMBL273948 | — | — | 1 | 6.65 |
| CHEMBL11369 | — | — | 1 | 6.62 |
| CHEMBL10781 | — | — | 1 | 6.58 |
| CHEMBL10607 | — | — | 1 | 6.58 |
| CHEMBL417067 | — | — | 1 | 6.35 |
| CHEMBL10843 | — | — | 1 | 6.20 |
| CHEMBL10794 | — | — | 1 | 6.19 |
| CHEMBL274359 | — | — | 1 | 6.12 |
| CHEMBL8981 | PD-156707 | — | 1 | 6.11 |
| CHEMBL275701 | — | — | 1 | 6.07 |
| CHEMBL10697 | — | — | 1 | 6.06 |
| CHEMBL268480 | — | — | 1 | 6.02 |
| CHEMBL273723 | — | — | 1 | 6.00 |
| CHEMBL10919 | — | — | 1 | 5.89 |
| CHEMBL275559 | — | — | 1 | 5.85 |
| CHEMBL276639 | — | — | 1 | 5.82 |
| CHEMBL11115 | — | — | 1 | 5.81 |
| CHEMBL10635 | — | — | 1 | 5.80 |
| CHEMBL10819 | — | — | 1 | 5.80 |
| CHEMBL10588 | — | — | 1 | 5.76 |
| CHEMBL10948 | — | — | 1 | 5.75 |
| CHEMBL11345 | — | — | 1 | 5.72 |
| CHEMBL417978 | — | — | 1 | 5.70 |
| CHEMBL417428 | — | — | 1 | 5.70 |
| CHEMBL274175 | — | — | 1 | 5.70 |
| CHEMBL276252 | — | — | 1 | 5.66 |
| CHEMBL10996 | — | — | 1 | 5.57 |
| CHEMBL10661 | — | — | 1 | 5.52 |
| CHEMBL10860 | — | — | 1 | 5.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL10854 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL273948 | — | IC50 | = | 225.0 | nM | 6.65 |
| CHEMBL11369 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL10781 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL10607 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL417067 | — | IC50 | = | 445.0 | nM | 6.35 |
| CHEMBL10843 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL10794 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL274359 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL8981 | PD-156707 | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL275701 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL10697 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL268480 | — | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL273723 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL10919 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL275559 | — | IC50 | = | 1410.0 | nM | 5.85 |
| CHEMBL276639 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL11115 | — | IC50 | = | 1550.0 | nM | 5.81 |
| CHEMBL10635 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL10819 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL10588 | — | IC50 | = | 1750.0 | nM | 5.76 |
| CHEMBL10948 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL11345 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL274175 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL417978 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL417428 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL276252 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL10996 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL10661 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL10860 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL10901 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL10589 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL274383 | PD-155080 | IC50 | = | 4550.0 | nM | 5.34 |
| CHEMBL268754 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL11341 | — | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL11176 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL11162 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL276601 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL11064 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL274307 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL273951 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL11106 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL10940 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL10846 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL274857 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL10808 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL267094 | — | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL11131 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL274805 | — | IC50 | > | 2500.0 | nM | - |
| CHEMBL10733 | — | IC50 | > | 2500.0 | nM | - |