Assay Detail
Binding
CHEMBL914035
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Displacement of [3H]citalopram from SERT in rhesus monkey caudate-putamen
67
Total Activities
67
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Macaca mulatta |
| Tissue | Caudate-putamen |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Sodium-dependent serotonin transporter (CHEMBL5453) ↗| Type | SINGLE PROTEIN |
| Organism | Macaca mulatta |
Publication
Synthesis of 8-thiabicyclo[3.2.1]octanes and their binding affinity for the dopamine and serotonin transporters.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 67 | 6.69 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL228104 | — | — | 1 | 8.60 |
| CHEMBL227829 | — | — | 1 | 8.52 |
| CHEMBL227526 | — | — | 1 | 8.33 |
| CHEMBL390929 | — | — | 1 | 8.19 |
| CHEMBL227757 | — | — | 1 | 8.10 |
| CHEMBL389672 | — | — | 1 | 8.00 |
| CHEMBL387983 | — | — | 1 | 7.89 |
| CHEMBL388411 | — | — | 1 | 7.85 |
| CHEMBL227773 | — | — | 1 | 7.82 |
| CHEMBL227720 | — | — | 1 | 7.77 |
| CHEMBL227538 | — | — | 1 | 7.57 |
| CHEMBL390712 | — | — | 1 | 7.51 |
| CHEMBL388545 | — | — | 1 | 7.48 |
| CHEMBL227580 | — | — | 1 | 7.48 |
| CHEMBL227714 | — | — | 1 | 7.44 |
| CHEMBL227662 | — | — | 1 | 7.41 |
| CHEMBL390764 | — | — | 1 | 7.24 |
| CHEMBL390392 | — | — | 1 | 7.19 |
| CHEMBL227438 | — | — | 1 | 7.16 |
| CHEMBL376107 | — | — | 1 | 7.05 |
| CHEMBL375262 | — | — | 1 | 7.00 |
| CHEMBL228156 | — | — | 1 | 6.92 |
| CHEMBL388412 | — | — | 1 | 6.86 |
| CHEMBL387522 | — | — | 1 | 6.86 |
| CHEMBL228096 | — | — | 1 | 6.78 |
| CHEMBL426752 | — | — | 1 | 6.63 |
| CHEMBL373947 | — | — | 1 | 6.47 |
| CHEMBL388105 | — | — | 1 | 6.43 |
| CHEMBL389076 | — | — | 1 | 6.32 |
| CHEMBL390492 | — | — | 1 | 6.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL228104 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL227829 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL227526 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL390929 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL227757 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL389672 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL387983 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL388411 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL227773 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL227720 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL227538 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL390712 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL388545 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL227580 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL227714 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL227662 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL390764 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL390392 | — | IC50 | = | 64.5 | nM | 7.19 |
| CHEMBL227438 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL376107 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL375262 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL228156 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL388412 | — | IC50 | = | 139.0 | nM | 6.86 |
| CHEMBL387522 | — | IC50 | = | 139.0 | nM | 6.86 |
| CHEMBL228096 | — | IC50 | = | 166.0 | nM | 6.78 |
| CHEMBL426752 | — | IC50 | = | 235.0 | nM | 6.63 |
| CHEMBL373947 | — | IC50 | = | 342.0 | nM | 6.47 |
| CHEMBL388105 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL389076 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL390492 | — | IC50 | = | 494.0 | nM | 6.31 |
| CHEMBL390286 | — | IC50 | = | 702.0 | nM | 6.15 |
| CHEMBL388633 | — | IC50 | = | 867.0 | nM | 6.06 |
| CHEMBL227658 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL227629 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL437874 | — | IC50 | = | 1220.0 | nM | 5.91 |
| CHEMBL227578 | — | IC50 | = | 1590.0 | nM | 5.80 |
| CHEMBL375908 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL227654 | — | IC50 | = | 2120.0 | nM | 5.67 |
| CHEMBL227788 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL226974 | — | IC50 | = | 2860.0 | nM | 5.54 |
| CHEMBL388300 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL322923 | — | IC50 | = | 5160.0 | nM | 5.29 |
| CHEMBL227632 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL388608 | — | IC50 | = | 5370.0 | nM | 5.27 |
| CHEMBL169429 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL449654 | — | IC50 | = | 46700.0 | nM | 4.33 |
| CHEMBL227878 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL228092 | — | IC50 | > | 8000.0 | nM | - |
| CHEMBL186501 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL389159 | — | IC50 | > | 11000.0 | nM | - |