Assay Detail
Binding
CHEMBL649334
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Binding affinity against alpha-1 adrenergic receptor on rat cortex using [3H]-prazosin as radioligand.
35
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Synthesis and pharmacological characterization of novel 6-fluorochroman derivatives as potential 5-HT1A receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 35 | 7.17 | 10.01 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2 | PRAZOSIN | 4.0 | 1 | 10.01 |
| CHEMBL25213 | — | — | 1 | 8.57 |
| CHEMBL96578 | — | — | 1 | 8.56 |
| CHEMBL96279 | — | — | 1 | 8.45 |
| CHEMBL96222 | — | — | 1 | 8.39 |
| CHEMBL96714 | — | — | 3 | 8.23 |
| CHEMBL419147 | — | — | 1 | 8.08 |
| CHEMBL96517 | — | — | 1 | 7.87 |
| CHEMBL95044 | — | — | 1 | 7.72 |
| CHEMBL92651 | — | — | 1 | 7.70 |
| CHEMBL96546 | — | — | 1 | 7.51 |
| CHEMBL96901 | — | — | 1 | 7.12 |
| CHEMBL330714 | — | — | 1 | 7.04 |
| CHEMBL96265 | — | — | 1 | 7.00 |
| CHEMBL319575 | — | — | 1 | 6.92 |
| CHEMBL94303 | — | — | 1 | 6.82 |
| CHEMBL318417 | — | — | 1 | 6.77 |
| CHEMBL318418 | — | — | 1 | 6.76 |
| CHEMBL317532 | — | — | 1 | 6.70 |
| CHEMBL93030 | — | — | 1 | 6.69 |
| CHEMBL94317 | — | — | 1 | 6.68 |
| CHEMBL96858 | — | — | 1 | 6.68 |
| CHEMBL94428 | — | — | 1 | 6.60 |
| CHEMBL313420 | — | — | 1 | 6.59 |
| CHEMBL93503 | — | — | 1 | 6.52 |
| CHEMBL96266 | — | — | 1 | 6.50 |
| CHEMBL96435 | — | — | 1 | 6.50 |
| CHEMBL96903 | — | — | 1 | 6.45 |
| CHEMBL94957 | — | — | 1 | 6.24 |
| CHEMBL329675 | — | — | 1 | 6.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2 | PRAZOSIN | Ki | = | 0.097 | nM | 10.01 |
| CHEMBL25213 | — | Ki | = | 2.71 | nM | 8.57 |
| CHEMBL96578 | — | Ki | = | 2.73 | nM | 8.56 |
| CHEMBL96279 | — | Ki | = | 3.57 | nM | 8.45 |
| CHEMBL96222 | — | Ki | = | 4.07 | nM | 8.39 |
| CHEMBL96714 | — | Ki | = | 5.86 | nM | 8.23 |
| CHEMBL419147 | — | Ki | = | 8.31 | nM | 8.08 |
| CHEMBL96714 | — | Ki | = | 10.4 | nM | 7.98 |
| CHEMBL96517 | — | Ki | = | 13.5 | nM | 7.87 |
| CHEMBL95044 | — | Ki | = | 19.1 | nM | 7.72 |
| CHEMBL92651 | — | Ki | = | 19.9 | nM | 7.70 |
| CHEMBL96546 | — | Ki | = | 30.8 | nM | 7.51 |
| CHEMBL96714 | — | Ki | = | 73.3 | nM | 7.13 |
| CHEMBL96901 | — | Ki | = | 75.6 | nM | 7.12 |
| CHEMBL330714 | — | Ki | = | 91.5 | nM | 7.04 |
| CHEMBL96265 | — | Ki | = | 98.9 | nM | 7.00 |
| CHEMBL319575 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL94303 | — | Ki | = | 152.0 | nM | 6.82 |
| CHEMBL318417 | — | Ki | = | 169.0 | nM | 6.77 |
| CHEMBL318418 | — | Ki | = | 175.0 | nM | 6.76 |
| CHEMBL317532 | — | Ki | = | 198.0 | nM | 6.70 |
| CHEMBL93030 | — | Ki | = | 203.0 | nM | 6.69 |
| CHEMBL94317 | — | Ki | = | 209.0 | nM | 6.68 |
| CHEMBL96858 | — | Ki | = | 207.0 | nM | 6.68 |
| CHEMBL94428 | — | Ki | = | 249.0 | nM | 6.60 |
| CHEMBL313420 | — | Ki | = | 258.0 | nM | 6.59 |
| CHEMBL93503 | — | Ki | = | 303.0 | nM | 6.52 |
| CHEMBL96266 | — | Ki | = | 315.0 | nM | 6.50 |
| CHEMBL96435 | — | Ki | = | 317.0 | nM | 6.50 |
| CHEMBL96903 | — | Ki | = | 355.0 | nM | 6.45 |
| CHEMBL94957 | — | Ki | = | 574.0 | nM | 6.24 |
| CHEMBL329675 | — | Ki | = | 663.0 | nM | 6.18 |
| CHEMBL316593 | — | Ki | = | 734.0 | nM | 6.13 |
| CHEMBL92668 | — | Ki | = | 856.0 | nM | 6.07 |
| CHEMBL95135 | — | Ki | = | 1350.0 | nM | 5.87 |