Assay Detail
Binding
CHEMBL914034
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Displacement of [3H]WIN-35428 from DAT 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 | Autocuration |
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 | 7.82 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL227773 | — | — | 1 | 9.52 |
| CHEMBL227538 | — | — | 1 | 9.40 |
| CHEMBL437874 | — | — | 1 | 9.12 |
| CHEMBL228104 | — | — | 1 | 8.96 |
| CHEMBL388633 | — | — | 1 | 8.92 |
| CHEMBL227829 | — | — | 1 | 8.70 |
| CHEMBL390712 | — | — | 1 | 8.64 |
| CHEMBL227788 | — | — | 1 | 8.60 |
| CHEMBL390392 | — | — | 1 | 8.51 |
| CHEMBL390929 | — | — | 1 | 8.48 |
| CHEMBL227526 | — | — | 1 | 8.48 |
| CHEMBL186242 | — | — | 1 | 8.35 |
| CHEMBL227654 | — | — | 1 | 8.34 |
| CHEMBL227662 | — | — | 1 | 8.31 |
| CHEMBL388300 | — | — | 1 | 8.30 |
| CHEMBL228156 | — | — | 1 | 8.28 |
| CHEMBL227757 | — | — | 1 | 8.24 |
| CHEMBL373947 | — | — | 1 | 8.22 |
| CHEMBL227720 | — | — | 1 | 8.22 |
| CHEMBL388411 | — | — | 1 | 8.22 |
| CHEMBL364146 | — | — | 1 | 8.17 |
| CHEMBL388105 | — | — | 1 | 8.17 |
| CHEMBL375262 | — | — | 1 | 8.16 |
| CHEMBL389076 | — | — | 1 | 8.15 |
| CHEMBL390286 | — | — | 1 | 8.15 |
| CHEMBL322923 | — | — | 1 | 8.15 |
| CHEMBL388608 | — | — | 1 | 8.13 |
| CHEMBL387505 | — | — | 1 | 8.12 |
| CHEMBL387716 | — | — | 1 | 8.11 |
| CHEMBL227714 | — | — | 1 | 8.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL227773 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL227538 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL437874 | — | IC50 | = | 0.76 | nM | 9.12 |
| CHEMBL228104 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL388633 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL227829 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL390712 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL227788 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL390392 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL390929 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL227526 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL186242 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL227654 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL227662 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL388300 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL228156 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL227757 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL373947 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL227720 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL388411 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL364146 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL388105 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL375262 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL322923 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL389076 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL390286 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL388608 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL387505 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL387716 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL227714 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL365092 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL227438 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL187695 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL388545 | — | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL227580 | — | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL387522 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL169429 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL376594 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL227629 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL227658 | — | IC50 | = | 11.3 | nM | 7.95 |
| CHEMBL186447 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL228096 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL227537 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL227787 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL389672 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL387983 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL388856 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL376107 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL228158 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL426752 | — | IC50 | = | 32.0 | nM | 7.50 |