Assay Detail
Binding
CHEMBL677402
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In vitro binding affinity to endothelin B receptor in rat cerebellum
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Cerebellum |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Potent nonpeptide endothelin antagonists: synthesis and structure-activity relationships of pyrazole-5-carboxylic acids.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 7.62 | 8.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL313153 | — | — | 1 | 8.77 |
| CHEMBL87070 | — | — | 1 | 8.59 |
| CHEMBL313044 | — | — | 1 | 8.49 |
| CHEMBL314973 | — | — | 1 | 8.49 |
| CHEMBL315280 | — | — | 1 | 8.48 |
| CHEMBL314454 | — | — | 1 | 8.47 |
| CHEMBL86505 | — | — | 1 | 8.40 |
| CHEMBL87801 | — | — | 1 | 8.34 |
| CHEMBL314974 | — | — | 1 | 8.31 |
| CHEMBL314357 | — | — | 1 | 8.20 |
| CHEMBL314206 | — | — | 1 | 8.07 |
| CHEMBL312979 | — | — | 1 | 8.01 |
| CHEMBL316187 | — | — | 1 | 8.01 |
| CHEMBL88011 | — | — | 1 | 8.00 |
| CHEMBL315622 | — | — | 1 | 7.96 |
| CHEMBL315936 | — | — | 1 | 7.83 |
| CHEMBL313920 | — | — | 1 | 7.58 |
| CHEMBL315752 | — | — | 1 | 7.51 |
| CHEMBL26474 | — | — | 1 | 7.47 |
| CHEMBL312854 | — | — | 1 | 7.36 |
| CHEMBL315638 | — | — | 1 | 7.05 |
| CHEMBL315175 | — | — | 1 | 6.88 |
| CHEMBL315788 | — | — | 1 | 6.75 |
| CHEMBL88019 | — | — | 1 | 6.36 |
| CHEMBL315805 | — | — | 1 | 6.09 |
| CHEMBL86965 | — | — | 1 | 6.08 |
| CHEMBL86821 | — | — | 1 | 6.02 |
| CHEMBL315087 | — | — | 1 | 5.69 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL313153 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL87070 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL313044 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL314973 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL315280 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL314454 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL86505 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL87801 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL314974 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL314357 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL314206 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL312979 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL316187 | — | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL88011 | — | IC50 | = | 9.9 | nM | 8.00 |
| CHEMBL315622 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL315936 | — | IC50 | = | 14.8 | nM | 7.83 |
| CHEMBL313920 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL315752 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL26474 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL312854 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL315638 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL315175 | — | IC50 | = | 131.0 | nM | 6.88 |
| CHEMBL315788 | — | IC50 | = | 178.0 | nM | 6.75 |
| CHEMBL88019 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL315805 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL86965 | — | IC50 | = | 825.0 | nM | 6.08 |
| CHEMBL86821 | — | IC50 | = | 953.0 | nM | 6.02 |
| CHEMBL315087 | — | IC50 | = | 2045.0 | nM | 5.69 |