Assay Detail
Functional
CHEMBL3594589
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Agonist activity at human 5-HT1A receptor expressed in human HeLa cell membranes assessed as stimulation of [35S]GTPgammaS binding after 20 mins by liquid scintillation counting analysis
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HeLa |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Arylpiperazine agonists of the serotonin 5-HT1A receptor preferentially activate cAMP signaling versus recruitment of β-arrestin-2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 9.37 | 10.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL511857 | — | — | 1 | 10.55 |
| CHEMBL423181 | — | — | 1 | 9.80 |
| CHEMBL140406 | — | — | 1 | 9.51 |
| CHEMBL139505 | — | — | 1 | 9.42 |
| CHEMBL444590 | — | — | 1 | 9.32 |
| CHEMBL344146 | — | — | 1 | 7.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL511857 | — | Ki | = | 0.028 | nM | 10.55 |
| CHEMBL423181 | — | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL140406 | — | Ki | = | 0.31 | nM | 9.51 |
| CHEMBL139505 | — | Ki | = | 0.38 | nM | 9.42 |
| CHEMBL444590 | — | Ki | = | 0.48 | nM | 9.32 |
| CHEMBL344146 | — | Ki | = | 23.0 | nM | 7.64 |