Assay Detail
Binding
CHEMBL2320300
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Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells up to 500 uM after 1.5 mins by fluorescence assay
11
Total Activities
11
Compounds Tested
2
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
Multidrug and toxin extrusion protein 2 (CHEMBL1743127) ↗| 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 | 9 | 5.58 | 6.80 |
| Inhibition | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL46 | ONDANSETRON | 4.0 | 1 | 6.80 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 6.46 |
| CHEMBL58 | MITOXANTRONE | 4.0 | 1 | 6.28 |
| CHEMBL55 | PENTAMIDINE | 4.0 | 1 | 5.57 |
| CHEMBL163 | RITONAVIR | 4.0 | 1 | 5.36 |
| CHEMBL360861 | NIFEKALANT | 3.0 | 1 | 5.19 |
| CHEMBL5483011 | INDINAVIR | 3.0 | 1 | 5.11 |
| CHEMBL481 | IRINOTECAN | 4.0 | 1 | 5.10 |
| CHEMBL1502 | PANTOPRAZOLE | 4.0 | 1 | 4.37 |
| CHEMBL364713 | NOSCAPINE | 2.0 | 1 | - |
| CHEMBL723 | CARVEDILOL | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL46 | ONDANSETRON | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL941 | IMATINIB | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL58 | MITOXANTRONE | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL55 | PENTAMIDINE | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL163 | RITONAVIR | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL360861 | NIFEKALANT | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL5483011 | INDINAVIR | IC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL481 | IRINOTECAN | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL1502 | PANTOPRAZOLE | IC50 | = | 43200.0 | nM | 4.37 |
| CHEMBL364713 | NOSCAPINE | Inhibition | - | % | - | |
| CHEMBL723 | CARVEDILOL | Inhibition | - | % | - |