Assay Detail
Binding
CHEMBL616658
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In vitro binding affinity towards 5-hydroxytryptamine 1D receptor in guinea-pig striatum in presence of BMY-7378 and mesulergine
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Striatum |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
5-hydroxytryptamine receptor 1D (CHEMBL2304407) ↗| Type | SINGLE PROTEIN |
| Organism | Cavia porcellus |
Publication
Evolution of a novel series of [(N,N-dimethylamino)propyl]- and piperazinylbenzanilides as the first selective 5-HT1D antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 8.22 | 8.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL15928 | GR-127935 | — | 1 | 8.50 |
| CHEMBL72088 | — | — | 1 | 8.50 |
| CHEMBL73446 | — | — | 1 | 8.50 |
| CHEMBL311150 | — | — | 1 | 8.30 |
| CHEMBL72981 | — | — | 1 | 8.30 |
| CHEMBL72700 | — | — | 1 | 8.20 |
| CHEMBL306384 | — | — | 1 | 8.20 |
| CHEMBL309021 | — | — | 1 | 8.00 |
| CHEMBL72092 | — | — | 1 | 7.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL15928 | GR-127935 | Ki | = | 3.162 | nM | 8.50 |
| CHEMBL72088 | — | Ki | = | 3.162 | nM | 8.50 |
| CHEMBL73446 | — | Ki | = | 3.162 | nM | 8.50 |
| CHEMBL311150 | — | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL72981 | — | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL72700 | — | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL306384 | — | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL309021 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL72092 | — | Ki | = | 31.62 | nM | 7.50 |