Assay Detail
Binding
CHEMBL1909109
Review assay metadata, readout intent, target linkage, and publication context from the same page.
DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)
1742
Total Activities
871
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HEK293 |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent serotonin transporter (CHEMBL228) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
DrugMatrix in vitro pharmacology data
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 871 | 6.29 | 10.10 |
| Ki | 871 | 6.56 | 10.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL490 | PAROXETINE | 4.0 | 2 | 10.37 |
| CHEMBL415 | CLOMIPRAMINE | 4.0 | 2 | 10.33 |
| CHEMBL809 | SERTRALINE | 4.0 | 2 | 10.12 |
| CHEMBL41 | FLUOXETINE | 4.0 | 2 | 9.57 |
| CHEMBL549 | CITALOPRAM | 4.0 | 2 | 9.32 |
| CHEMBL629 | AMITRIPTYLINE | 4.0 | 2 | 9.05 |
| CHEMBL52440 | DEXTROMETHORPHAN | 4.0 | 2 | 8.84 |
| CHEMBL637 | VENLAFAXINE | 4.0 | 2 | 8.42 |
| CHEMBL445 | NORTRIPTYLINE | 4.0 | 2 | 8.16 |
| CHEMBL506 | PRIMAQUINE | 4.0 | 2 | 8.07 |
| CHEMBL1201353 | DEXCHLORPHENIRAMINE | 4.0 | 2 | 7.89 |
| CHEMBL1113 | AMOXAPINE | 4.0 | 2 | 7.75 |
| CHEMBL71 | CHLORPROMAZINE | 4.0 | 2 | 7.68 |
| CHEMBL1628227 | DOXEPIN | 4.0 | 2 | 7.66 |
| CHEMBL1201151 | MESTRANOL | 4.0 | 2 | 7.66 |
| CHEMBL511 | PYRILAMINE | 4.0 | 2 | 7.60 |
| CHEMBL691 | ETHINYL ESTRADIOL | 4.0 | 2 | 7.54 |
| CHEMBL1200623 | ETHYLESTRENOL | 4.0 | 2 | 7.37 |
| CHEMBL564 | PROMAZINE | 4.0 | 2 | 7.34 |
| CHEMBL2103774 | TIBOLONE | 3.0 | 2 | 7.32 |
| CHEMBL1221 | SULCONAZOLE | 4.0 | 2 | 7.12 |
| CHEMBL621 | TRAZODONE | 4.0 | 2 | 6.99 |
| CHEMBL1411979 | METHAPYRILENE | 4.0 | 2 | 6.97 |
| CHEMBL723 | CARVEDILOL | 4.0 | 2 | 6.93 |
| CHEMBL1172 | DESLORATADINE | 4.0 | 2 | 6.91 |
| CHEMBL6966 | VERAPAMIL | 4.0 | 2 | 6.90 |
| CHEMBL27 | PROPRANOLOL | 4.0 | 2 | 6.70 |
| CHEMBL1237044 | TRAMADOL | 4.0 | 2 | 6.70 |
| CHEMBL1729 | CISAPRIDE | 4.0 | 2 | 6.69 |
| CHEMBL808 | ECONAZOLE | 4.0 | 2 | 6.65 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL490 | PAROXETINE | Ki | = | 0.043 | nM | 10.37 |
| CHEMBL415 | CLOMIPRAMINE | Ki | = | 0.047 | nM | 10.33 |
| CHEMBL809 | SERTRALINE | Ki | = | 0.075 | nM | 10.12 |
| CHEMBL490 | PAROXETINE | IC50 | = | 0.08 | nM | 10.10 |
| CHEMBL415 | CLOMIPRAMINE | IC50 | = | 0.088 | nM | 10.06 |
| CHEMBL809 | SERTRALINE | IC50 | = | 0.141 | nM | 9.85 |
| CHEMBL41 | FLUOXETINE | Ki | = | 0.271 | nM | 9.57 |
| CHEMBL549 | CITALOPRAM | Ki | = | 0.479 | nM | 9.32 |
| CHEMBL41 | FLUOXETINE | IC50 | = | 0.51 | nM | 9.29 |
| CHEMBL629 | AMITRIPTYLINE | Ki | = | 0.882 | nM | 9.05 |
| CHEMBL549 | CITALOPRAM | IC50 | = | 0.902 | nM | 9.04 |
| CHEMBL52440 | DEXTROMETHORPHAN | Ki | = | 1.44 | nM | 8.84 |
| CHEMBL629 | AMITRIPTYLINE | IC50 | = | 1.661 | nM | 8.78 |
| CHEMBL52440 | DEXTROMETHORPHAN | IC50 | = | 2.71 | nM | 8.57 |
| CHEMBL637 | VENLAFAXINE | Ki | = | 3.814 | nM | 8.42 |
| CHEMBL445 | NORTRIPTYLINE | Ki | = | 6.977 | nM | 8.16 |
| CHEMBL637 | VENLAFAXINE | IC50 | = | 7.18 | nM | 8.14 |
| CHEMBL506 | PRIMAQUINE | Ki | = | 8.405 | nM | 8.07 |
| CHEMBL445 | NORTRIPTYLINE | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1201353 | DEXCHLORPHENIRAMINE | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL506 | PRIMAQUINE | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL1113 | AMOXAPINE | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL71 | CHLORPROMAZINE | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL1201151 | MESTRANOL | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL1628227 | DOXEPIN | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL1201353 | DEXCHLORPHENIRAMINE | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL511 | PYRILAMINE | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL691 | ETHINYL ESTRADIOL | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL1113 | AMOXAPINE | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL71 | CHLORPROMAZINE | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL1201151 | MESTRANOL | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL1628227 | DOXEPIN | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL1200623 | ETHYLESTRENOL | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL564 | PROMAZINE | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL511 | PYRILAMINE | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL2103774 | TIBOLONE | Ki | = | 48.2 | nM | 7.32 |
| CHEMBL691 | ETHINYL ESTRADIOL | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL1221 | SULCONAZOLE | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL1200623 | ETHYLESTRENOL | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL564 | PROMAZINE | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL2103774 | TIBOLONE | IC50 | = | 90.7 | nM | 7.04 |
| CHEMBL621 | TRAZODONE | Ki | = | 102.0 | nM | 6.99 |
| CHEMBL1411979 | METHAPYRILENE | Ki | = | 106.0 | nM | 6.97 |
| CHEMBL723 | CARVEDILOL | Ki | = | 118.0 | nM | 6.93 |
| CHEMBL1172 | DESLORATADINE | Ki | = | 122.0 | nM | 6.91 |
| CHEMBL6966 | VERAPAMIL | Ki | = | 127.0 | nM | 6.90 |
| CHEMBL1221 | SULCONAZOLE | IC50 | = | 141.0 | nM | 6.85 |
| CHEMBL621 | TRAZODONE | IC50 | = | 192.0 | nM | 6.72 |
| CHEMBL1411979 | METHAPYRILENE | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL1237044 | TRAMADOL | Ki | = | 198.0 | nM | 6.70 |