Assay Detail
Functional
CHEMBL646229
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonism of phenylephrine stimulated contraction of the rat isolated spleen.
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Tissue | Spleen |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Design, synthesis, and biological activity of prazosin-related antagonists. Role of the piperazine and furan units of prazosin on the selectivity for alpha1-adrenoreceptor subtypes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 21 | 8.34 | 9.84 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL27013 | — | — | 1 | 9.84 |
| CHEMBL144224 | — | — | 1 | 9.35 |
| CHEMBL138681 | — | — | 1 | 9.21 |
| CHEMBL144776 | — | — | 1 | 9.17 |
| CHEMBL358060 | — | — | 1 | 9.15 |
| CHEMBL2 | PRAZOSIN | 4.0 | 1 | 8.99 |
| CHEMBL144238 | — | — | 1 | 8.97 |
| CHEMBL144677 | — | — | 1 | 8.73 |
| CHEMBL342997 | — | — | 1 | 8.62 |
| CHEMBL357669 | — | — | 1 | 8.61 |
| CHEMBL144263 | — | — | 1 | 8.53 |
| CHEMBL148061 | — | — | 1 | 8.03 |
| CHEMBL144768 | — | — | 1 | 8.01 |
| CHEMBL146724 | — | — | 1 | 7.88 |
| CHEMBL144000 | — | — | 1 | 7.71 |
| CHEMBL13647 | BMY-7378 | — | 1 | 7.55 |
| CHEMBL29591 | — | — | 1 | 7.49 |
| CHEMBL341665 | — | — | 1 | 7.43 |
| CHEMBL145181 | — | — | 1 | 7.37 |
| CHEMBL146601 | — | — | 1 | 7.27 |
| CHEMBL145384 | — | — | 1 | 7.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL27013 | — | Kd | = | 0.1445 | nM | 9.84 |
| CHEMBL144224 | — | Kd | = | 0.4467 | nM | 9.35 |
| CHEMBL138681 | — | Kd | = | 0.6166 | nM | 9.21 |
| CHEMBL144776 | — | Kd | = | 0.6761 | nM | 9.17 |
| CHEMBL358060 | — | Kd | = | 0.7079 | nM | 9.15 |
| CHEMBL2 | PRAZOSIN | Kd | = | 1.023 | nM | 8.99 |
| CHEMBL144238 | — | Kd | = | 1.072 | nM | 8.97 |
| CHEMBL144677 | — | Kd | = | 1.862 | nM | 8.73 |
| CHEMBL342997 | — | Kd | = | 2.399 | nM | 8.62 |
| CHEMBL357669 | — | Kd | = | 2.455 | nM | 8.61 |
| CHEMBL144263 | — | Kd | = | 2.951 | nM | 8.53 |
| CHEMBL148061 | — | Kd | = | 9.333 | nM | 8.03 |
| CHEMBL144768 | — | Kd | = | 9.772 | nM | 8.01 |
| CHEMBL146724 | — | Kd | = | 13.18 | nM | 7.88 |
| CHEMBL144000 | — | Kd | = | 19.5 | nM | 7.71 |
| CHEMBL13647 | BMY-7378 | Kd | = | 28.18 | nM | 7.55 |
| CHEMBL29591 | — | Kd | = | 32.36 | nM | 7.49 |
| CHEMBL341665 | — | Kd | = | 37.15 | nM | 7.43 |
| CHEMBL145181 | — | Kd | = | 42.66 | nM | 7.37 |
| CHEMBL146601 | — | Kd | = | 53.7 | nM | 7.27 |
| CHEMBL145384 | — | Kd | = | 66.07 | nM | 7.18 |