Assay Detail
Binding
CHEMBL847531
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Ability to inhibit [3H]citalopram binding to serotonin transporter in cynomolgus monkey striatum
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cercopithecidae |
| Tissue | Striatum |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent serotonin transporter (CHEMBL228) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Substituted 3-phenyltropane analogs of cocaine: synthesis, inhibition of binding at cocaine recognition sites, and positron emission tomography imaging.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 7.91 | 8.79 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL81525 | — | — | 1 | 8.79 |
| CHEMBL87031 | — | — | 1 | 8.61 |
| CHEMBL14391 | — | — | 1 | 8.60 |
| CHEMBL306208 | — | — | 1 | 8.23 |
| CHEMBL67387 | — | — | 1 | 8.01 |
| CHEMBL171106 | — | — | 1 | 7.69 |
| CHEMBL2079586 | — | — | 1 | 6.80 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL81525 | — | IC50 | = | 1.63 | nM | 8.79 |
| CHEMBL87031 | — | IC50 | = | 2.47 | nM | 8.61 |
| CHEMBL14391 | — | IC50 | = | 2.53 | nM | 8.60 |
| CHEMBL306208 | — | IC50 | = | 5.87 | nM | 8.23 |
| CHEMBL67387 | — | IC50 | = | 9.88 | nM | 8.01 |
| CHEMBL171106 | — | IC50 | = | 20.4 | nM | 7.69 |
| CHEMBL2079586 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL370805 | COCAINE | IC50 | = | 270.0 | nM | 6.57 |