Assay Detail
Binding
CHEMBL870197
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Displacement of [3H]8-OH-DPAT from human 5HT1A receptor in HEK293 cells
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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 |
|---|---|---|---|
| Ki | 27 | 7.62 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL209324 | — | — | 1 | 9.00 |
| CHEMBL207220 | — | — | 1 | 8.89 |
| CHEMBL209821 | NALUZOTAN | 3.0 | 1 | 8.29 |
| CHEMBL8412 | IPSAPIRONE | 2.0 | 1 | 8.22 |
| CHEMBL210537 | — | — | 1 | 8.17 |
| CHEMBL377697 | — | — | 1 | 8.05 |
| CHEMBL379984 | — | — | 1 | 8.04 |
| CHEMBL207478 | — | — | 1 | 8.01 |
| CHEMBL211012 | — | — | 1 | 8.00 |
| CHEMBL210874 | — | — | 1 | 7.89 |
| CHEMBL284092 | GEPIRONE | 4.0 | 1 | 7.89 |
| CHEMBL210795 | — | — | 1 | 7.75 |
| CHEMBL49 | BUSPIRONE | 4.0 | 1 | 7.70 |
| CHEMBL209459 | — | — | 1 | 7.66 |
| CHEMBL209985 | — | — | 1 | 7.62 |
| CHEMBL209176 | — | — | 1 | 7.40 |
| CHEMBL266832 | — | — | 1 | 7.40 |
| CHEMBL205550 | — | — | 1 | 7.34 |
| CHEMBL207553 | — | — | 1 | 7.33 |
| CHEMBL445928 | — | — | 1 | 7.25 |
| CHEMBL379364 | — | — | 1 | 7.11 |
| CHEMBL2111058 | SUNEPITRON | 2.0 | 1 | 7.04 |
| CHEMBL384677 | — | — | 1 | 6.95 |
| CHEMBL426318 | — | — | 1 | 6.85 |
| CHEMBL209072 | — | — | 1 | 6.37 |
| CHEMBL210498 | — | — | 1 | 5.87 |
| CHEMBL411941 | CYCLORGDFV | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL209324 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL207220 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL209821 | NALUZOTAN | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL8412 | IPSAPIRONE | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL210537 | — | Ki | = | 6.8 | nM | 8.17 |
| CHEMBL377697 | — | Ki | = | 8.9 | nM | 8.05 |
| CHEMBL379984 | — | Ki | = | 9.2 | nM | 8.04 |
| CHEMBL207478 | — | Ki | = | 9.7 | nM | 8.01 |
| CHEMBL211012 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL210874 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL284092 | GEPIRONE | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL210795 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL49 | BUSPIRONE | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL209459 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL209985 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL209176 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL266832 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL205550 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL207553 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL445928 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL379364 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL2111058 | SUNEPITRON | Ki | = | 92.0 | nM | 7.04 |
| CHEMBL384677 | — | Ki | = | 112.0 | nM | 6.95 |
| CHEMBL426318 | — | Ki | = | 141.0 | nM | 6.85 |
| CHEMBL209072 | — | Ki | = | 426.0 | nM | 6.37 |
| CHEMBL210498 | — | Ki | = | 1360.0 | nM | 5.87 |
| CHEMBL411941 | CYCLORGDFV | Ki | - | — | - |