Assay Detail
Binding
CHEMBL617466
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Ability to bind to central serotonin 5-hydroxytryptamine 2A receptor in vitro in cortex of the rat brain using [3H]ketanserin radioligand
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
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 | 16 | 6.47 | 7.25 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL191907 | — | — | 1 | 7.25 |
| CHEMBL2112359 | — | — | 1 | 7.19 |
| CHEMBL193595 | — | — | 1 | 7.14 |
| CHEMBL2112361 | — | — | 1 | 7.07 |
| CHEMBL195849 | — | — | 1 | 7.07 |
| CHEMBL2112351 | — | — | 1 | 6.63 |
| CHEMBL86719 | — | — | 1 | 6.61 |
| CHEMBL2112360 | — | — | 1 | 6.61 |
| CHEMBL2112363 | — | — | 1 | 6.49 |
| CHEMBL2112362 | — | — | 1 | 6.36 |
| CHEMBL328292 | — | — | 1 | 6.25 |
| CHEMBL425567 | — | — | 1 | 6.08 |
| CHEMBL193867 | — | — | 1 | 6.06 |
| CHEMBL195047 | — | — | 1 | 6.00 |
| CHEMBL91588 | — | — | 1 | 5.41 |
| CHEMBL91021 | — | — | 1 | 5.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL191907 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL2112359 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL193595 | — | Ki | = | 72.0 | nM | 7.14 |
| CHEMBL2112361 | — | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL195849 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL2112351 | — | Ki | = | 234.0 | nM | 6.63 |
| CHEMBL86719 | — | Ki | = | 243.0 | nM | 6.61 |
| CHEMBL2112360 | — | Ki | = | 246.0 | nM | 6.61 |
| CHEMBL2112363 | — | Ki | = | 326.0 | nM | 6.49 |
| CHEMBL2112362 | — | Ki | = | 440.0 | nM | 6.36 |
| CHEMBL328292 | — | Ki | = | 562.0 | nM | 6.25 |
| CHEMBL425567 | — | Ki | = | 835.0 | nM | 6.08 |
| CHEMBL193867 | — | Ki | = | 880.0 | nM | 6.06 |
| CHEMBL195047 | — | Ki | = | 997.0 | nM | 6.00 |
| CHEMBL91588 | — | Ki | = | 3882.0 | nM | 5.41 |
| CHEMBL91021 | — | Ki | = | 4680.0 | nM | 5.33 |