Assay Detail
Binding
CHEMBL652738
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Ability to bind to alpha-1 adrenergic receptor in vitro in cortex of the rat brain using [3H]prazosin radioligand
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
New arylpiperazine 5-HT(1A) receptor ligands containing the pyrimido[2,1-f]purine fragment: synthesis, in vitro, and in vivo pharmacological evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 7.50 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL195047 | — | — | 1 | 7.96 |
| CHEMBL191907 | — | — | 1 | 7.68 |
| CHEMBL193595 | — | — | 1 | 7.60 |
| CHEMBL2112351 | — | — | 1 | 7.54 |
| CHEMBL425567 | — | — | 1 | 7.48 |
| CHEMBL193867 | — | — | 1 | 7.42 |
| CHEMBL195849 | — | — | 1 | 7.34 |
| CHEMBL2112360 | — | — | 1 | 7.24 |
| CHEMBL2112361 | — | — | 1 | 7.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL195047 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL191907 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL193595 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL2112351 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL425567 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL193867 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL195849 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL2112360 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL2112361 | — | Ki | = | 62.0 | nM | 7.21 |