Assay Detail
Binding
CHEMBL2320303
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
33
Total Activities
33
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
Solute carrier family 22 member 2 (CHEMBL1743122) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 5.16 | 6.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL790 | CHLORHEXIDINE | 4.0 | 1 | 6.40 |
| CHEMBL87563 | GABEXATE | 3.0 | 1 | 6.05 |
| CHEMBL55 | PENTAMIDINE | 4.0 | 1 | 5.92 |
| CHEMBL1502 | PANTOPRAZOLE | 4.0 | 1 | 5.82 |
| CHEMBL46 | ONDANSETRON | 4.0 | 1 | 5.77 |
| CHEMBL290106 | BITHIONOL | 4.0 | 1 | 5.72 |
| CHEMBL691 | ETHINYL ESTRADIOL | 4.0 | 1 | 5.66 |
| CHEMBL364713 | NOSCAPINE | 2.0 | 1 | 5.58 |
| CHEMBL481 | IRINOTECAN | 4.0 | 1 | 5.57 |
| CHEMBL1200629 | VECURONIUM BROMIDE | 4.0 | 1 | 5.46 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 5.38 |
| CHEMBL289469 | GRANISETRON | 4.0 | 1 | 5.37 |
| CHEMBL1106 | EPINASTINE | 4.0 | 1 | 5.37 |
| CHEMBL959 | RIMANTADINE | 4.0 | 1 | 5.36 |
| CHEMBL48361 | DABIGATRAN | 3.0 | 1 | 5.33 |
| CHEMBL723 | CARVEDILOL | 4.0 | 1 | 5.12 |
| CHEMBL219916 | DOMPERIDONE | 3.0 | 1 | 5.10 |
| CHEMBL603 | ZAFIRLUKAST | 4.0 | 1 | 5.01 |
| CHEMBL360861 | NIFEKALANT | 3.0 | 1 | 4.99 |
| CHEMBL85 | RISPERIDONE | 4.0 | 1 | 4.96 |
| CHEMBL49 | BUSPIRONE | 4.0 | 1 | 4.92 |
| CHEMBL2 | PRAZOSIN | 4.0 | 1 | 4.87 |
| CHEMBL590799 | CAMOSTAT | 3.0 | 1 | 4.78 |
| CHEMBL163 | RITONAVIR | 4.0 | 1 | 4.61 |
| CHEMBL1423 | PIMOZIDE | 4.0 | 1 | 4.47 |
| CHEMBL902 | FAMOTIDINE | 4.0 | 1 | 4.44 |
| CHEMBL1732 | DIHYDROERGOTAMINE | 4.0 | 1 | 4.30 |
| CHEMBL84 | TOPOTECAN | 4.0 | 1 | 4.21 |
| CHEMBL58 | MITOXANTRONE | 4.0 | 1 | 4.13 |
| CHEMBL339427 | TUBOCURARINE | 4.0 | 1 | 4.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL790 | CHLORHEXIDINE | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL87563 | GABEXATE | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL55 | PENTAMIDINE | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL1502 | PANTOPRAZOLE | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL46 | ONDANSETRON | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL290106 | BITHIONOL | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL691 | ETHINYL ESTRADIOL | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL364713 | NOSCAPINE | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL481 | IRINOTECAN | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL1200629 | VECURONIUM BROMIDE | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL941 | IMATINIB | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL289469 | GRANISETRON | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL1106 | EPINASTINE | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL959 | RIMANTADINE | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL48361 | DABIGATRAN | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL723 | CARVEDILOL | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL219916 | DOMPERIDONE | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL603 | ZAFIRLUKAST | IC50 | = | 9700.0 | nM | 5.01 |
| CHEMBL360861 | NIFEKALANT | IC50 | = | 10300.0 | nM | 4.99 |
| CHEMBL85 | RISPERIDONE | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL49 | BUSPIRONE | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL2 | PRAZOSIN | IC50 | = | 13600.0 | nM | 4.87 |
| CHEMBL590799 | CAMOSTAT | IC50 | = | 16500.0 | nM | 4.78 |
| CHEMBL163 | RITONAVIR | IC50 | = | 24800.0 | nM | 4.61 |
| CHEMBL1423 | PIMOZIDE | IC50 | = | 34200.0 | nM | 4.47 |
| CHEMBL902 | FAMOTIDINE | IC50 | = | 36100.0 | nM | 4.44 |
| CHEMBL1732 | DIHYDROERGOTAMINE | IC50 | = | 49900.0 | nM | 4.30 |
| CHEMBL84 | TOPOTECAN | IC50 | = | 61000.0 | nM | 4.21 |
| CHEMBL58 | MITOXANTRONE | IC50 | = | 73300.0 | nM | 4.13 |
| CHEMBL339427 | TUBOCURARINE | IC50 | = | 78800.0 | nM | 4.10 |
| CHEMBL256907 | MARAVIROC | IC50 | = | 255000.0 | nM | - |
| CHEMBL1112 | ARIPIPRAZOLE | IC50 | = | 239000.0 | nM | - |
| CHEMBL5483011 | INDINAVIR | IC50 | = | 142000.0 | nM | - |