Assay Detail
Binding
CHEMBL4380184
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of wild type human dopamine transporter expressed in HEK293 cells assessed as inhibition of [3H]dopamine reuptake preincubated for 5 mins followed by [3H]dopamine addition and measured after 1 min by liquid scintillation analysis
72
Total Activities
70
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
Structure-Activity Relationships of Novel Thiazole-Based Modafinil Analogues Acting at Monoamine Transporters.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 72 | 4.93 | 6.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4465494 | — | — | 1 | 6.19 |
| CHEMBL4473574 | — | — | 1 | 5.96 |
| CHEMBL4567505 | — | — | 1 | 5.80 |
| CHEMBL4593487 | — | — | 1 | 5.73 |
| CHEMBL4522454 | — | — | 1 | 5.70 |
| CHEMBL4469951 | — | — | 1 | 5.64 |
| CHEMBL4552477 | — | — | 1 | 5.52 |
| CHEMBL4437004 | — | — | 1 | 5.52 |
| CHEMBL4459152 | — | — | 1 | 5.49 |
| CHEMBL4552525 | — | — | 1 | 5.48 |
| CHEMBL4459947 | — | — | 1 | 5.44 |
| CHEMBL4445285 | — | — | 1 | 5.42 |
| CHEMBL4455184 | — | — | 1 | 5.39 |
| CHEMBL4439598 | — | — | 1 | 5.39 |
| CHEMBL4568351 | — | — | 1 | 5.38 |
| CHEMBL4543324 | — | — | 1 | 5.38 |
| CHEMBL4456176 | — | — | 1 | 5.34 |
| CHEMBL4438894 | — | — | 1 | 5.33 |
| CHEMBL4583781 | — | — | 1 | 5.30 |
| CHEMBL4473522 | — | — | 1 | 5.28 |
| CHEMBL4453763 | — | — | 1 | 5.22 |
| CHEMBL4470394 | — | — | 1 | 5.21 |
| CHEMBL1201192 | ARMODAFINIL | 4.0 | 1 | 5.18 |
| CHEMBL4576306 | — | — | 1 | 5.18 |
| CHEMBL4441345 | — | — | 1 | 5.17 |
| CHEMBL4444833 | — | — | 3 | 5.17 |
| CHEMBL4569016 | — | — | 1 | 5.16 |
| CHEMBL4436791 | — | — | 1 | 5.13 |
| CHEMBL4464187 | — | — | 1 | 5.13 |
| CHEMBL4532133 | — | — | 1 | 5.13 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4465494 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL4473574 | — | IC50 | = | 1090.0 | nM | 5.96 |
| CHEMBL4567505 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4593487 | — | IC50 | = | 1850.0 | nM | 5.73 |
| CHEMBL4522454 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL4469951 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL4552477 | — | IC50 | = | 2990.0 | nM | 5.52 |
| CHEMBL4437004 | — | IC50 | = | 3020.0 | nM | 5.52 |
| CHEMBL4459152 | — | IC50 | = | 3250.0 | nM | 5.49 |
| CHEMBL4552525 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL4459947 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL4445285 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL4439598 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL4455184 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL4543324 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL4568351 | — | IC50 | = | 4170.0 | nM | 5.38 |
| CHEMBL4456176 | — | IC50 | = | 4610.0 | nM | 5.34 |
| CHEMBL4438894 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL4583781 | — | IC50 | = | 5040.0 | nM | 5.30 |
| CHEMBL4473522 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL4453763 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL4470394 | — | IC50 | = | 6210.0 | nM | 5.21 |
| CHEMBL1201192 | ARMODAFINIL | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL4576306 | — | IC50 | = | 6660.0 | nM | 5.18 |
| CHEMBL4441345 | — | IC50 | = | 6760.0 | nM | 5.17 |
| CHEMBL4444833 | — | IC50 | = | 6800.0 | nM | 5.17 |
| CHEMBL4569016 | — | IC50 | = | 6970.0 | nM | 5.16 |
| CHEMBL4532133 | — | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL4436791 | — | IC50 | = | 7320.0 | nM | 5.13 |
| CHEMBL4464187 | — | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL4441307 | — | IC50 | = | 8300.0 | nM | 5.08 |
| CHEMBL4453638 | — | IC50 | = | 9580.0 | nM | 5.02 |
| CHEMBL4444833 | — | IC50 | = | 10570.0 | nM | 4.98 |
| CHEMBL4568024 | — | IC50 | = | 12200.0 | nM | 4.91 |
| CHEMBL4470744 | — | IC50 | = | 13500.0 | nM | 4.87 |
| CHEMBL4443822 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL4461921 | — | IC50 | = | 14640.0 | nM | 4.83 |
| CHEMBL4453674 | — | IC50 | = | 14730.0 | nM | 4.83 |
| CHEMBL4456526 | — | IC50 | = | 19600.0 | nM | 4.71 |
| CHEMBL4441995 | — | IC50 | = | 22400.0 | nM | 4.65 |
| CHEMBL4461901 | — | IC50 | = | 22500.0 | nM | 4.65 |
| CHEMBL4466223 | — | IC50 | = | 24300.0 | nM | 4.61 |
| CHEMBL4517473 | — | IC50 | = | 24320.0 | nM | 4.61 |
| CHEMBL4558014 | — | IC50 | = | 27800.0 | nM | 4.56 |
| CHEMBL4451429 | — | IC50 | = | 28430.0 | nM | 4.55 |
| CHEMBL4466697 | — | IC50 | = | 29390.0 | nM | 4.53 |
| CHEMBL4541596 | — | IC50 | = | 33270.0 | nM | 4.48 |
| CHEMBL4587340 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL4461596 | — | IC50 | = | 36300.0 | nM | 4.44 |
| CHEMBL4439670 | — | IC50 | = | 37800.0 | nM | 4.42 |