Assay Detail
Functional
CHEMBL5362786
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Agonist activity at human 5HT1A expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP production preincubated for 10 mins followed by forskolin addition for 5 mins
12
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of novel arylpiperazine-based DA/5-HT modulators as potential antipsychotic agents - Design, synthesis, structural studies and pharmacological profiling.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 9 | 7.97 | 9.57 |
| pEC50 | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL18840 | — | — | 2 | 9.57 |
| CHEMBL5409227 | — | — | 2 | 7.55 |
| CHEMBL5431642 | — | — | 2 | 6.80 |
| CHEMBL5418283 | — | — | 2 | - |
| CHEMBL54 | HALOPERIDOL | 4.0 | 2 | - |
| CHEMBL85 | RISPERIDONE | 4.0 | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL18840 | — | EC50 | = | 0.2692 | nM | 9.57 |
| CHEMBL18840 | — | EC50 | = | 0.27 | nM | 9.57 |
| CHEMBL5409227 | — | EC50 | = | 28.18 | nM | 7.55 |
| CHEMBL5409227 | — | EC50 | = | 28.4 | nM | 7.55 |
| CHEMBL5431642 | — | EC50 | = | 158.49 | nM | 6.80 |
| CHEMBL5431642 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL5418283 | — | pEC50 | - | — | - | |
| CHEMBL5418283 | — | EC50 | - | — | - | |
| CHEMBL54 | HALOPERIDOL | pEC50 | - | — | - | |
| CHEMBL54 | HALOPERIDOL | EC50 | - | — | - | |
| CHEMBL85 | RISPERIDONE | pEC50 | - | — | - | |
| CHEMBL85 | RISPERIDONE | EC50 | - | — | - |