Assay Detail
Functional
CHEMBL645201
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonism of norepinephrine induced contraction of rat isolated thoracic aorta.
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Tissue | Thoracic aorta |
| 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 | 9.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL144238 | — | — | 1 | 9.39 |
| CHEMBL27013 | — | — | 1 | 9.19 |
| CHEMBL2 | PRAZOSIN | 4.0 | 1 | 8.91 |
| CHEMBL357669 | — | — | 1 | 8.69 |
| CHEMBL144677 | — | — | 1 | 8.55 |
| CHEMBL29591 | — | — | 1 | 8.54 |
| CHEMBL148061 | — | — | 1 | 8.51 |
| CHEMBL144776 | — | — | 1 | 8.50 |
| CHEMBL138681 | — | — | 1 | 8.46 |
| CHEMBL13647 | BMY-7378 | — | 1 | 8.34 |
| CHEMBL146724 | — | — | 1 | 8.26 |
| CHEMBL341665 | — | — | 1 | 8.26 |
| CHEMBL342997 | — | — | 1 | 8.23 |
| CHEMBL146601 | — | — | 1 | 8.22 |
| CHEMBL144768 | — | — | 1 | 8.17 |
| CHEMBL144224 | — | — | 1 | 8.16 |
| CHEMBL145181 | — | — | 1 | 8.03 |
| CHEMBL144263 | — | — | 1 | 7.86 |
| CHEMBL144000 | — | — | 1 | 7.84 |
| CHEMBL358060 | — | — | 1 | 7.71 |
| CHEMBL145384 | — | — | 1 | 7.29 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL144238 | — | Kd | = | 0.4074 | nM | 9.39 |
| CHEMBL27013 | — | Kd | = | 0.6457 | nM | 9.19 |
| CHEMBL2 | PRAZOSIN | Kd | = | 1.23 | nM | 8.91 |
| CHEMBL357669 | — | Kd | = | 2.042 | nM | 8.69 |
| CHEMBL144677 | — | Kd | = | 2.818 | nM | 8.55 |
| CHEMBL29591 | — | Kd | = | 2.884 | nM | 8.54 |
| CHEMBL148061 | — | Kd | = | 3.09 | nM | 8.51 |
| CHEMBL144776 | — | Kd | = | 3.162 | nM | 8.50 |
| CHEMBL138681 | — | Kd | = | 3.467 | nM | 8.46 |
| CHEMBL13647 | BMY-7378 | Kd | = | 4.571 | nM | 8.34 |
| CHEMBL146724 | — | Kd | = | 5.495 | nM | 8.26 |
| CHEMBL341665 | — | Kd | = | 5.495 | nM | 8.26 |
| CHEMBL342997 | — | Kd | = | 5.888 | nM | 8.23 |
| CHEMBL146601 | — | Kd | = | 6.026 | nM | 8.22 |
| CHEMBL144768 | — | Kd | = | 6.761 | nM | 8.17 |
| CHEMBL144224 | — | Kd | = | 6.918 | nM | 8.16 |
| CHEMBL145181 | — | Kd | = | 9.333 | nM | 8.03 |
| CHEMBL144263 | — | Kd | = | 13.8 | nM | 7.86 |
| CHEMBL144000 | — | Kd | = | 14.45 | nM | 7.84 |
| CHEMBL358060 | — | Kd | = | 19.5 | nM | 7.71 |
| CHEMBL145384 | — | Kd | = | 51.29 | nM | 7.29 |