Assay Detail
Binding
CHEMBL2433692
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Displacement of [3H]Win35428 from human recombinant DAT over-expressed in CHOK1 cells
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent dopamine transporter (CHEMBL238) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and biological evaluation of novel 3,4-diaryl lactam derivatives as triple reuptake inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 7.02 | 8.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2430688 | — | — | 1 | 8.09 |
| CHEMBL543876 | — | — | 1 | 7.85 |
| CHEMBL2430690 | — | — | 1 | 7.76 |
| CHEMBL2430697 | — | — | 1 | 7.64 |
| CHEMBL2430696 | — | — | 1 | 7.49 |
| CHEMBL2430682 | — | — | 1 | 7.48 |
| CHEMBL2430695 | — | — | 1 | 7.44 |
| CHEMBL2430693 | — | — | 1 | 7.44 |
| CHEMBL2430694 | — | — | 1 | 7.41 |
| CHEMBL2430692 | — | — | 1 | 7.38 |
| CHEMBL2430689 | — | — | 1 | 7.09 |
| CHEMBL2430680 | — | — | 1 | 7.00 |
| CHEMBL2430699 | — | — | 1 | 6.92 |
| CHEMBL2430700 | — | — | 1 | 6.80 |
| CHEMBL2430686 | — | — | 1 | 6.76 |
| CHEMBL2430681 | — | — | 1 | 6.75 |
| CHEMBL2430685 | — | — | 1 | 6.55 |
| CHEMBL2430684 | — | — | 1 | 6.55 |
| CHEMBL2430687 | — | — | 1 | 5.76 |
| CHEMBL2430698 | — | — | 1 | 5.67 |
| CHEMBL415 | CLOMIPRAMINE | 4.0 | 1 | 5.56 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2430688 | — | IC50 | = | 8.14 | nM | 8.09 |
| CHEMBL543876 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2430690 | — | IC50 | = | 17.3 | nM | 7.76 |
| CHEMBL2430697 | — | IC50 | = | 22.7 | nM | 7.64 |
| CHEMBL2430696 | — | IC50 | = | 32.7 | nM | 7.49 |
| CHEMBL2430682 | — | IC50 | = | 33.1 | nM | 7.48 |
| CHEMBL2430695 | — | IC50 | = | 36.6 | nM | 7.44 |
| CHEMBL2430693 | — | IC50 | = | 36.3 | nM | 7.44 |
| CHEMBL2430694 | — | IC50 | = | 38.7 | nM | 7.41 |
| CHEMBL2430692 | — | IC50 | = | 41.7 | nM | 7.38 |
| CHEMBL2430689 | — | IC50 | = | 81.5 | nM | 7.09 |
| CHEMBL2430680 | — | IC50 | = | 99.6 | nM | 7.00 |
| CHEMBL2430699 | — | IC50 | = | 120.9 | nM | 6.92 |
| CHEMBL2430700 | — | IC50 | = | 159.7 | nM | 6.80 |
| CHEMBL2430686 | — | IC50 | = | 171.9 | nM | 6.76 |
| CHEMBL2430681 | — | IC50 | = | 179.3 | nM | 6.75 |
| CHEMBL2430685 | — | IC50 | = | 280.6 | nM | 6.55 |
| CHEMBL2430684 | — | IC50 | = | 284.7 | nM | 6.55 |
| CHEMBL2430687 | — | IC50 | = | 1731.0 | nM | 5.76 |
| CHEMBL2430698 | — | IC50 | = | 2143.0 | nM | 5.67 |
| CHEMBL415 | CLOMIPRAMINE | IC50 | = | 2777.0 | nM | 5.56 |