Assay Detail
Binding
CHEMBL1909143
Review assay metadata, readout intent, target linkage, and publication context from the same page.
DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55)
1742
Total Activities
871
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO-K1 |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent dopamine transporter (CHEMBL238) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
DrugMatrix in vitro pharmacology data
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 871 | 5.67 | 7.49 |
| Ki | 871 | 5.77 | 7.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL809 | SERTRALINE | 4.0 | 2 | 7.59 |
| CHEMBL19215 | METERGOLINE | 2.0 | 2 | 7.30 |
| CHEMBL1231 | OXYBUTYNIN | 4.0 | 2 | 7.17 |
| CHEMBL305660 | EBASTINE | 4.0 | 2 | 7.11 |
| CHEMBL926 | DOBUTAMINE | 4.0 | 2 | 6.91 |
| CHEMBL707 | DOXAZOSIN | 4.0 | 2 | 6.83 |
| CHEMBL508112 | BENZOTHIAZYL DISULFIDE | — | 2 | 6.71 |
| CHEMBL1201203 | BENZTROPINE | 4.0 | 2 | 6.71 |
| CHEMBL17157 | TERFENADINE | 4.0 | 2 | 6.69 |
| CHEMBL1177 | PEMOLINE | 4.0 | 2 | 6.38 |
| CHEMBL691 | ETHINYL ESTRADIOL | 4.0 | 2 | 6.35 |
| CHEMBL30008 | FLUNARIZINE | 2.0 | 2 | 6.33 |
| CHEMBL1419 | SIBUTRAMINE | 4.0 | 2 | 6.30 |
| CHEMBL1626 | CLEMASTINE | 4.0 | 2 | 6.27 |
| CHEMBL490 | PAROXETINE | 4.0 | 2 | 6.27 |
| CHEMBL648 | CYCLIZINE | 4.0 | 2 | 6.22 |
| CHEMBL954 | ENCLOMIPHENE | 3.0 | 2 | 6.21 |
| CHEMBL808 | ECONAZOLE | 4.0 | 2 | 6.18 |
| CHEMBL723 | CARVEDILOL | 4.0 | 2 | 6.17 |
| CHEMBL511 | PYRILAMINE | 4.0 | 2 | 6.16 |
| CHEMBL1201353 | DEXCHLORPHENIRAMINE | 4.0 | 2 | 6.13 |
| CHEMBL296419 | ASTEMIZOLE | 4.0 | 2 | 6.10 |
| CHEMBL1670 | MITOTANE | 4.0 | 2 | 6.10 |
| CHEMBL894 | BUPROPION | 4.0 | 2 | 6.08 |
| CHEMBL411 | DIETHYLSTILBESTROL | 4.0 | 2 | 6.07 |
| CHEMBL221753 | BENZETHONIUM CHLORIDE | 2.0 | 2 | 5.96 |
| CHEMBL429 | LABETALOL | 4.0 | 2 | 5.89 |
| CHEMBL153062 | 4-NONYLPHENOL | — | 2 | 5.88 |
| CHEMBL43064 | CINNARIZINE | 2.0 | 2 | 5.88 |
| CHEMBL445 | NORTRIPTYLINE | 4.0 | 2 | 5.88 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL809 | SERTRALINE | Ki | = | 25.8 | nM | 7.59 |
| CHEMBL809 | SERTRALINE | IC50 | = | 32.4 | nM | 7.49 |
| CHEMBL19215 | METERGOLINE | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL19215 | METERGOLINE | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL1231 | OXYBUTYNIN | Ki | = | 67.9 | nM | 7.17 |
| CHEMBL305660 | EBASTINE | Ki | = | 78.4 | nM | 7.11 |
| CHEMBL1231 | OXYBUTYNIN | IC50 | = | 85.5 | nM | 7.07 |
| CHEMBL305660 | EBASTINE | IC50 | = | 98.7 | nM | 7.01 |
| CHEMBL926 | DOBUTAMINE | Ki | = | 123.0 | nM | 6.91 |
| CHEMBL707 | DOXAZOSIN | Ki | = | 149.0 | nM | 6.83 |
| CHEMBL926 | DOBUTAMINE | IC50 | = | 155.0 | nM | 6.81 |
| CHEMBL707 | DOXAZOSIN | IC50 | = | 188.0 | nM | 6.73 |
| CHEMBL1201203 | BENZTROPINE | Ki | = | 193.0 | nM | 6.71 |
| CHEMBL508112 | BENZOTHIAZYL DISULFIDE | Ki | = | 194.0 | nM | 6.71 |
| CHEMBL17157 | TERFENADINE | Ki | = | 203.0 | nM | 6.69 |
| CHEMBL1201203 | BENZTROPINE | IC50 | = | 243.0 | nM | 6.61 |
| CHEMBL508112 | BENZOTHIAZYL DISULFIDE | IC50 | = | 245.0 | nM | 6.61 |
| CHEMBL17157 | TERFENADINE | IC50 | = | 255.0 | nM | 6.59 |
| CHEMBL1177 | PEMOLINE | Ki | = | 414.2 | nM | 6.38 |
| CHEMBL691 | ETHINYL ESTRADIOL | Ki | = | 444.0 | nM | 6.35 |
| CHEMBL30008 | FLUNARIZINE | Ki | = | 464.0 | nM | 6.33 |
| CHEMBL1419 | SIBUTRAMINE | Ki | = | 502.0 | nM | 6.30 |
| CHEMBL1177 | PEMOLINE | IC50 | = | 521.3 | nM | 6.28 |
| CHEMBL490 | PAROXETINE | Ki | = | 534.0 | nM | 6.27 |
| CHEMBL1626 | CLEMASTINE | Ki | = | 538.0 | nM | 6.27 |
| CHEMBL691 | ETHINYL ESTRADIOL | IC50 | = | 559.0 | nM | 6.25 |
| CHEMBL30008 | FLUNARIZINE | IC50 | = | 584.0 | nM | 6.23 |
| CHEMBL648 | CYCLIZINE | Ki | = | 606.0 | nM | 6.22 |
| CHEMBL954 | ENCLOMIPHENE | Ki | = | 623.0 | nM | 6.21 |
| CHEMBL1419 | SIBUTRAMINE | IC50 | = | 632.0 | nM | 6.20 |
| CHEMBL808 | ECONAZOLE | Ki | = | 663.0 | nM | 6.18 |
| CHEMBL490 | PAROXETINE | IC50 | = | 672.0 | nM | 6.17 |
| CHEMBL723 | CARVEDILOL | Ki | = | 671.0 | nM | 6.17 |
| CHEMBL1626 | CLEMASTINE | IC50 | = | 678.0 | nM | 6.17 |
| CHEMBL511 | PYRILAMINE | Ki | = | 699.0 | nM | 6.16 |
| CHEMBL1201353 | DEXCHLORPHENIRAMINE | Ki | = | 739.0 | nM | 6.13 |
| CHEMBL648 | CYCLIZINE | IC50 | = | 763.0 | nM | 6.12 |
| CHEMBL954 | ENCLOMIPHENE | IC50 | = | 784.0 | nM | 6.11 |
| CHEMBL296419 | ASTEMIZOLE | Ki | = | 793.0 | nM | 6.10 |
| CHEMBL1670 | MITOTANE | Ki | = | 795.0 | nM | 6.10 |
| CHEMBL808 | ECONAZOLE | IC50 | = | 835.0 | nM | 6.08 |
| CHEMBL894 | BUPROPION | Ki | = | 821.4 | nM | 6.08 |
| CHEMBL723 | CARVEDILOL | IC50 | = | 845.0 | nM | 6.07 |
| CHEMBL411 | DIETHYLSTILBESTROL | Ki | = | 851.0 | nM | 6.07 |
| CHEMBL511 | PYRILAMINE | IC50 | = | 879.0 | nM | 6.06 |
| CHEMBL1201353 | DEXCHLORPHENIRAMINE | IC50 | = | 931.0 | nM | 6.03 |
| CHEMBL1670 | MITOTANE | IC50 | = | 1001.0 | nM | 6.00 |
| CHEMBL296419 | ASTEMIZOLE | IC50 | = | 998.0 | nM | 6.00 |
| CHEMBL894 | BUPROPION | IC50 | = | 1033.8 | nM | 5.99 |
| CHEMBL411 | DIETHYLSTILBESTROL | IC50 | = | 1071.0 | nM | 5.97 |