Assay Detail
Binding
CHEMBL801382
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Inhibition of [3H]citalopram binding to the serotonin transporter (5-HT) in monkey caudate-putamen.
26
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cercopithecidae |
| Tissue | Caudate-putamen |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sodium-dependent serotonin transporter (CHEMBL228) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
2-Carbomethoxy-3-aryl-8-oxabicyclo[3.2.1]octanes: potent non-nitrogen inhibitors of monoamine transporters.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 7.01 | 8.61 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL87031 | — | — | 2 | 8.61 |
| CHEMBL14391 | — | — | 2 | 8.38 |
| CHEMBL316342 | — | — | 6 | 8.33 |
| CHEMBL306208 | — | — | 2 | 8.23 |
| CHEMBL313664 | — | — | 2 | 7.92 |
| CHEMBL1790051 | — | — | 2 | 7.68 |
| CHEMBL88792 | — | — | 2 | 7.52 |
| CHEMBL90903 | — | — | 2 | 6.97 |
| CHEMBL2079586 | — | — | 2 | 6.80 |
| CHEMBL329454 | — | — | 2 | 5.59 |
| CHEMBL314402 | — | — | 2 | 4.94 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL87031 | — | IC50 | = | 2.47 | nM | 8.61 |
| CHEMBL14391 | — | IC50 | = | 4.21 | nM | 8.38 |
| CHEMBL316342 | — | IC50 | = | 4.67 | nM | 8.33 |
| CHEMBL306208 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL316342 | — | IC50 | = | 6.52 | nM | 8.19 |
| CHEMBL313664 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL1790051 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL87031 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL88792 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL316342 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL316342 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL14391 | — | IC50 | = | 64.9 | nM | 7.19 |
| CHEMBL316342 | — | IC50 | = | 64.5 | nM | 7.19 |
| CHEMBL313664 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL90903 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL2079586 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL88792 | — | IC50 | = | 276.0 | nM | 6.56 |
| CHEMBL90903 | — | IC50 | = | 816.0 | nM | 6.09 |
| CHEMBL306208 | — | IC50 | = | 998.0 | nM | 6.00 |
| CHEMBL1790051 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL329454 | — | IC50 | = | 2580.0 | nM | 5.59 |
| CHEMBL316342 | — | IC50 | = | 2860.0 | nM | 5.54 |
| CHEMBL2079586 | — | IC50 | = | 5060.0 | nM | 5.30 |
| CHEMBL314402 | — | IC50 | = | 11440.0 | nM | 4.94 |
| CHEMBL329454 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL314402 | — | IC50 | > | 10000.0 | nM | - |