Assay Detail
Binding
CHEMBL839737
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Inhibition of [3H]5-HT binding to serotonin transporter in rat cortical synaptosomes
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium-dependent serotonin transporter (CHEMBL313) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Discovery of the first potent, selective 5-hydroxytryptamine1D receptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 6.63 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL183460 | — | — | 1 | 8.40 |
| CHEMBL192176 | — | — | 1 | 7.60 |
| CHEMBL191605 | — | — | 1 | 7.30 |
| CHEMBL364495 | — | — | 1 | 6.70 |
| CHEMBL192536 | — | — | 1 | 6.50 |
| CHEMBL425190 | — | — | 1 | 6.50 |
| CHEMBL190190 | — | — | 1 | 6.40 |
| CHEMBL191980 | — | — | 1 | 6.30 |
| CHEMBL190298 | — | — | 1 | 6.10 |
| CHEMBL365810 | — | — | 1 | 6.00 |
| CHEMBL191619 | — | — | 1 | 5.90 |
| CHEMBL363413 | — | — | 1 | 5.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL183460 | — | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL192176 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL191605 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL364495 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL192536 | — | Ki | = | 316.23 | nM | 6.50 |
| CHEMBL425190 | — | Ki | = | 316.23 | nM | 6.50 |
| CHEMBL190190 | — | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL191980 | — | Ki | = | 501.19 | nM | 6.30 |
| CHEMBL190298 | — | Ki | = | 794.33 | nM | 6.10 |
| CHEMBL365810 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL191619 | — | Ki | = | 1258.93 | nM | 5.90 |
| CHEMBL363413 | — | Ki | = | 1258.93 | nM | 5.90 |