Assay Detail
Binding
CHEMBL808140
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Binding affinity at serotonin transporter from rat cerebral cortex by [3H]-paroxetine displacement.
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Cerebral cortex |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sodium-dependent serotonin transporter (CHEMBL313) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
First dual NK(1) antagonists-serotonin reuptake inhibitors: synthesis and SAR of a new class of potential antidepressants.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 7.04 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL329402 | — | — | 1 | 7.70 |
| CHEMBL88998 | — | — | 1 | 7.60 |
| CHEMBL88731 | — | — | 1 | 7.60 |
| CHEMBL87194 | — | — | 1 | 7.60 |
| CHEMBL91418 | — | — | 1 | 7.50 |
| CHEMBL89385 | — | — | 1 | 7.50 |
| CHEMBL89230 | — | — | 1 | 7.40 |
| CHEMBL91436 | — | — | 1 | 7.40 |
| CHEMBL89847 | — | — | 1 | 7.30 |
| CHEMBL315939 | — | — | 1 | 7.00 |
| CHEMBL89425 | — | — | 1 | 6.80 |
| CHEMBL419312 | — | — | 1 | 6.80 |
| CHEMBL89640 | — | — | 1 | 6.80 |
| CHEMBL422773 | — | — | 1 | 6.80 |
| CHEMBL86890 | — | — | 1 | 6.80 |
| CHEMBL313070 | — | — | 1 | 6.70 |
| CHEMBL88810 | — | — | 1 | 6.70 |
| CHEMBL87066 | — | — | 1 | 6.60 |
| CHEMBL89245 | — | — | 1 | 6.60 |
| CHEMBL89818 | — | — | 1 | 6.50 |
| CHEMBL315937 | — | — | 1 | 6.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL329402 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL88998 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL88731 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL87194 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL91418 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL89385 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL89230 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL91436 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL89847 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL315939 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL89425 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL419312 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL89640 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL422773 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL86890 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL313070 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL88810 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL87066 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL89245 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL89818 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL315937 | — | IC50 | = | 630.96 | nM | 6.20 |