Assay Detail
Functional
CHEMBL870204
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 9 | 7.49 | 8.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL207220 | — | — | 1 | 8.44 |
| CHEMBL210537 | — | — | 1 | 7.70 |
| CHEMBL209821 | NALUZOTAN | 3.0 | 1 | 7.70 |
| CHEMBL209324 | — | — | 1 | 7.68 |
| CHEMBL207478 | — | — | 1 | 7.50 |
| CHEMBL379984 | — | — | 1 | 7.22 |
| CHEMBL49 | BUSPIRONE | 4.0 | 1 | 7.10 |
| CHEMBL284092 | GEPIRONE | 4.0 | 1 | 6.54 |
| CHEMBL411941 | CYCLORGDFV | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL207220 | — | EC50 | = | 3.6 | nM | 8.44 |
| CHEMBL210537 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL209821 | NALUZOTAN | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL209324 | — | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL207478 | — | EC50 | = | 32.0 | nM | 7.50 |
| CHEMBL379984 | — | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL49 | BUSPIRONE | EC50 | = | 80.0 | nM | 7.10 |
| CHEMBL284092 | GEPIRONE | EC50 | = | 288.0 | nM | 6.54 |
| CHEMBL411941 | CYCLORGDFV | EC50 | - | — | - |