Assay Detail
Binding
CHEMBL616211
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In vitro inhibition of [3H]spiperone binding to 5-hydroxytryptamine 1A receptor from rat hippocampal tissue.
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Hippocampus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Polycyclic aryl- and heteroarylpiperazinyl imides as 5-HT1A receptor ligands and potential anxiolytic agents: synthesis and structure-activity relationship studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 33 | 7.70 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1202512 | — | — | 1 | 9.00 |
| CHEMBL1202513 | — | — | 1 | 8.89 |
| CHEMBL1202507 | — | — | 1 | 8.89 |
| CHEMBL1204093 | — | — | 1 | 8.89 |
| CHEMBL1202527 | — | — | 1 | 8.30 |
| CHEMBL1202530 | — | — | 1 | 8.15 |
| CHEMBL274047 | TANDOSPIRONE | 2.0 | 1 | 8.05 |
| CHEMBL8412 | IPSAPIRONE | 2.0 | 1 | 8.00 |
| CHEMBL49 | BUSPIRONE | 4.0 | 1 | 8.00 |
| CHEMBL1202506 | — | — | 1 | 7.92 |
| CHEMBL1202520 | — | — | 1 | 7.85 |
| CHEMBL29326 | — | — | 1 | 7.85 |
| CHEMBL1202494 | — | — | 1 | 7.85 |
| CHEMBL1202523 | — | — | 1 | 7.77 |
| CHEMBL1204094 | — | — | 1 | 7.77 |
| CHEMBL418762 | — | — | 1 | 7.72 |
| CHEMBL1202493 | — | — | 1 | 7.70 |
| CHEMBL1202515 | — | — | 1 | 7.60 |
| CHEMBL1202508 | — | — | 1 | 7.58 |
| CHEMBL286242 | — | — | 1 | 7.58 |
| CHEMBL431295 | — | — | 1 | 7.43 |
| CHEMBL1202504 | — | — | 1 | 7.42 |
| CHEMBL31197 | — | — | 1 | 7.39 |
| CHEMBL1202511 | — | — | 1 | 7.39 |
| CHEMBL28352 | — | — | 1 | 7.38 |
| CHEMBL28406 | — | — | 1 | 7.29 |
| CHEMBL1202516 | — | — | 1 | 7.24 |
| CHEMBL29278 | — | — | 1 | 6.97 |
| CHEMBL412258 | — | — | 1 | 6.91 |
| CHEMBL1202502 | — | — | 1 | 6.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1202512 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL1202513 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL1204093 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL1202507 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL1202527 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL1202530 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL274047 | TANDOSPIRONE | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL8412 | IPSAPIRONE | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL49 | BUSPIRONE | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL1202506 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL1202520 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL29326 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL1202494 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL1202523 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL1204094 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL418762 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL1202493 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL1202515 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL1202508 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL286242 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL431295 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL1202504 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL31197 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL1202511 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL28352 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL28406 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL1202516 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL29278 | — | Ki | = | 107.0 | nM | 6.97 |
| CHEMBL412258 | — | Ki | = | 122.0 | nM | 6.91 |
| CHEMBL1202502 | — | Ki | = | 129.0 | nM | 6.89 |
| CHEMBL29155 | — | Ki | = | 162.0 | nM | 6.79 |
| CHEMBL28026 | — | Ki | = | 162.0 | nM | 6.79 |
| CHEMBL284203 | — | Ki | = | 190.0 | nM | 6.72 |