Assay Detail
Binding
CHEMBL616102
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Binding affinity at 5-hydroxytryptamine 1A receptor in rat cerebral cortex membranes by [3H]8-OH-DPAT displacement.
18
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Cerebral cortex |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
2-[4-(o-methoxyphenyl)piperazin-1-ylmethyl]-1,3-dioxoperhydroimidazo[1,5-a]pyridine as a new selective 5-HT1A receptor ligand
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 7.69 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL8618 | NAN-190 | — | 2 | 9.22 |
| CHEMBL43992 | — | — | 1 | 8.39 |
| CHEMBL45253 | — | — | 1 | 8.24 |
| CHEMBL42644 | — | — | 1 | 8.14 |
| CHEMBL46881 | — | — | 1 | 8.06 |
| CHEMBL417709 | — | — | 1 | 8.00 |
| CHEMBL26853 | — | — | 1 | 7.70 |
| CHEMBL49 | BUSPIRONE | 4.0 | 1 | 7.69 |
| CHEMBL295168 | — | — | 1 | 7.50 |
| CHEMBL296713 | — | — | 1 | 7.34 |
| CHEMBL44786 | — | — | 1 | 7.27 |
| CHEMBL42396 | — | — | 1 | 7.18 |
| CHEMBL42404 | — | — | 1 | 7.11 |
| CHEMBL46525 | — | — | 1 | 6.89 |
| CHEMBL41978 | — | — | 1 | 6.81 |
| CHEMBL265494 | — | — | 1 | 6.00 |
| CHEMBL291165 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL8618 | NAN-190 | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL8618 | NAN-190 | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL43992 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL45253 | — | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL42644 | — | Ki | = | 7.2 | nM | 8.14 |
| CHEMBL46881 | — | Ki | = | 8.8 | nM | 8.06 |
| CHEMBL417709 | — | Ki | = | 9.9 | nM | 8.00 |
| CHEMBL26853 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL49 | BUSPIRONE | Ki | = | 20.5 | nM | 7.69 |
| CHEMBL295168 | — | Ki | = | 31.7 | nM | 7.50 |
| CHEMBL296713 | — | Ki | = | 45.5 | nM | 7.34 |
| CHEMBL44786 | — | Ki | = | 53.6 | nM | 7.27 |
| CHEMBL42396 | — | Ki | = | 65.8 | nM | 7.18 |
| CHEMBL42404 | — | Ki | = | 78.5 | nM | 7.11 |
| CHEMBL46525 | — | Ki | = | 128.0 | nM | 6.89 |
| CHEMBL41978 | — | Ki | = | 154.0 | nM | 6.81 |
| CHEMBL265494 | — | Ki | = | 990.0 | nM | 6.00 |
| CHEMBL291165 | — | Ki | > | 1000.0 | nM | - |