Assay Detail
Binding
CHEMBL4433104
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Inhibition of [3H]-5-dopamine reuptake in human DAT expressed in HEK293 cells by liquid scintillation counting method
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent dopamine transporter (CHEMBL238) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Exploration of substituted arylpiperazine-tetrazoles as promising dual norepinephrine and dopamine reuptake inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 5.70 | 6.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4288240 | — | — | 1 | 6.09 |
| CHEMBL4442592 | — | — | 1 | 6.04 |
| CHEMBL4522348 | — | — | 1 | 6.00 |
| CHEMBL4579759 | — | — | 1 | 5.98 |
| CHEMBL4452761 | — | — | 1 | 5.94 |
| CHEMBL4435098 | — | — | 1 | 5.92 |
| CHEMBL894 | BUPROPION | 4.0 | 1 | 5.92 |
| CHEMBL4463452 | — | — | 1 | 5.88 |
| CHEMBL4529583 | — | — | 1 | 5.85 |
| CHEMBL4456619 | — | — | 1 | 5.84 |
| CHEMBL4558778 | — | — | 1 | 5.83 |
| CHEMBL4534817 | — | — | 1 | 5.79 |
| CHEMBL4455262 | — | — | 1 | 5.65 |
| CHEMBL4547192 | — | — | 1 | 5.65 |
| CHEMBL4593696 | — | — | 1 | 5.61 |
| CHEMBL1201066 | VENLAFAXINE HYDROCHLORIDE | 4.0 | 1 | 5.59 |
| CHEMBL4462562 | — | — | 1 | 5.54 |
| CHEMBL4469505 | — | — | 1 | 5.52 |
| CHEMBL4450647 | — | — | 1 | 5.45 |
| CHEMBL4559266 | — | — | 1 | 5.43 |
| CHEMBL4532628 | — | — | 1 | 5.42 |
| CHEMBL4435085 | — | — | 1 | 5.38 |
| CHEMBL4532284 | — | — | 1 | 5.32 |
| CHEMBL4532229 | — | — | 1 | 5.25 |
| CHEMBL4441014 | — | — | 1 | - |
| CHEMBL4563389 | — | — | 1 | - |
| CHEMBL4530231 | — | — | 1 | - |
| CHEMBL4455798 | — | — | 1 | - |
| CHEMBL4449806 | — | — | 1 | - |
| CHEMBL4557158 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4288240 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL4442592 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL4522348 | — | IC50 | = | 1010.0 | nM | 6.00 |
| CHEMBL4579759 | — | IC50 | = | 1040.0 | nM | 5.98 |
| CHEMBL4452761 | — | IC50 | = | 1140.0 | nM | 5.94 |
| CHEMBL4435098 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL894 | BUPROPION | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4463452 | — | IC50 | = | 1330.0 | nM | 5.88 |
| CHEMBL4529583 | — | IC50 | = | 1420.0 | nM | 5.85 |
| CHEMBL4456619 | — | IC50 | = | 1430.0 | nM | 5.84 |
| CHEMBL4558778 | — | IC50 | = | 1470.0 | nM | 5.83 |
| CHEMBL4534817 | — | IC50 | = | 1640.0 | nM | 5.79 |
| CHEMBL4455262 | — | IC50 | = | 2250.0 | nM | 5.65 |
| CHEMBL4547192 | — | IC50 | = | 2250.0 | nM | 5.65 |
| CHEMBL4593696 | — | IC50 | = | 2480.0 | nM | 5.61 |
| CHEMBL1201066 | VENLAFAXINE HYDROCHLORIDE | IC50 | = | 2550.0 | nM | 5.59 |
| CHEMBL4462562 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL4469505 | — | IC50 | = | 3040.0 | nM | 5.52 |
| CHEMBL4450647 | — | IC50 | = | 3590.0 | nM | 5.45 |
| CHEMBL4559266 | — | IC50 | = | 3720.0 | nM | 5.43 |
| CHEMBL4532628 | — | IC50 | = | 3850.0 | nM | 5.42 |
| CHEMBL4435085 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL4532284 | — | IC50 | = | 4740.0 | nM | 5.32 |
| CHEMBL4532229 | — | IC50 | = | 5580.0 | nM | 5.25 |
| CHEMBL4472139 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4539630 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4452169 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4554733 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4438467 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4557158 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4449806 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4455798 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4530231 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4563389 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4441014 | — | IC50 | > | 10000.0 | nM | - |