Assay Detail
Binding
CHEMBL870200
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Binding affinity to D2 receptor by radioligand binding assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 |
|---|---|---|---|
| Ki | 6 | 7.36 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL49 | BUSPIRONE | 4.0 | 1 | 7.89 |
| CHEMBL284092 | GEPIRONE | 4.0 | 1 | 7.24 |
| CHEMBL8412 | IPSAPIRONE | 2.0 | 1 | 6.96 |
| CHEMBL209821 | NALUZOTAN | 3.0 | 1 | - |
| CHEMBL379984 | — | — | 1 | - |
| CHEMBL411941 | CYCLORGDFV | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL49 | BUSPIRONE | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL284092 | GEPIRONE | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL8412 | IPSAPIRONE | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL209821 | NALUZOTAN | Ki | > | 2000.0 | nM | - |
| CHEMBL379984 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL411941 | CYCLORGDFV | Ki | - | — | - |