Assay Detail
Functional
CHEMBL907461
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Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
22
Total Activities
22
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 | Expert |
Publication
Towards a new generation of potential antipsychotic agents combining D2 and 5-HT1A receptor activities.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 22 | 7.32 | 8.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL221920 | — | — | 1 | 8.58 |
| CHEMBL384657 | — | — | 1 | 8.54 |
| CHEMBL221692 | ADOPRAZINE | 2.0 | 1 | 8.23 |
| CHEMBL375297 | — | — | 1 | 8.19 |
| CHEMBL218261 | — | — | 1 | 8.00 |
| CHEMBL219486 | — | — | 1 | 7.61 |
| CHEMBL56 | 8-OH-DPAT | — | 1 | 7.55 |
| CHEMBL221131 | — | — | 1 | 7.49 |
| CHEMBL218313 | — | — | 1 | 7.47 |
| CHEMBL221743 | — | — | 1 | 7.33 |
| CHEMBL386988 | — | — | 1 | 7.17 |
| CHEMBL220809 | — | — | 1 | 7.16 |
| CHEMBL220808 | SARIZOTAN | 3.0 | 1 | 7.11 |
| CHEMBL221183 | — | — | 1 | 6.95 |
| CHEMBL441546 | — | — | 1 | 6.87 |
| CHEMBL413777 | — | — | 1 | 6.71 |
| CHEMBL218166 | BIFEPRUNOX | 3.0 | 1 | 6.49 |
| CHEMBL218217 | — | — | 1 | 5.85 |
| CHEMBL221957 | — | — | 1 | 5.81 |
| CHEMBL219111 | — | — | 1 | - |
| CHEMBL376634 | — | — | 1 | - |
| CHEMBL425810 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL221920 | — | EC50 | = | 2.63 | nM | 8.58 |
| CHEMBL384657 | — | EC50 | = | 2.884 | nM | 8.54 |
| CHEMBL221692 | ADOPRAZINE | EC50 | = | 5.888 | nM | 8.23 |
| CHEMBL375297 | — | EC50 | = | 6.457 | nM | 8.19 |
| CHEMBL218261 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL219486 | — | EC50 | = | 24.55 | nM | 7.61 |
| CHEMBL56 | 8-OH-DPAT | EC50 | = | 28.18 | nM | 7.55 |
| CHEMBL221131 | — | EC50 | = | 32.36 | nM | 7.49 |
| CHEMBL218313 | — | EC50 | = | 33.88 | nM | 7.47 |
| CHEMBL221743 | — | EC50 | = | 46.77 | nM | 7.33 |
| CHEMBL386988 | — | EC50 | = | 67.61 | nM | 7.17 |
| CHEMBL220809 | — | EC50 | = | 69.18 | nM | 7.16 |
| CHEMBL220808 | SARIZOTAN | EC50 | = | 77.62 | nM | 7.11 |
| CHEMBL221183 | — | EC50 | = | 112.2 | nM | 6.95 |
| CHEMBL441546 | — | EC50 | = | 134.9 | nM | 6.87 |
| CHEMBL413777 | — | EC50 | = | 194.98 | nM | 6.71 |
| CHEMBL218166 | BIFEPRUNOX | EC50 | = | 323.59 | nM | 6.49 |
| CHEMBL218217 | — | EC50 | = | 1412.54 | nM | 5.85 |
| CHEMBL221957 | — | EC50 | = | 1548.82 | nM | 5.81 |
| CHEMBL219111 | — | EC50 | < | 10000.0 | nM | - |
| CHEMBL376634 | — | EC50 | < | 10000.0 | nM | - |
| CHEMBL425810 | — | EC50 | < | 10000.0 | nM | - |