Assay Detail
Binding
CHEMBL2320298
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human MATE1-mediated [14]-metformin uptake expressed in polarized MDCK2 cells after 5 mins by liquid scintillation counting analysis
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MDCK-II |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Multidrug and toxin extrusion protein 1 (CHEMBL1743126) ↗| 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 | 6.13 | 7.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL941 | IMATINIB | 4.0 | 1 | 7.40 |
| CHEMBL58 | MITOXANTRONE | 4.0 | 1 | 6.72 |
| CHEMBL55 | PENTAMIDINE | 4.0 | 1 | 6.39 |
| CHEMBL360861 | NIFEKALANT | 3.0 | 1 | 6.19 |
| CHEMBL5483011 | INDINAVIR | 3.0 | 1 | 5.72 |
| CHEMBL163 | RITONAVIR | 4.0 | 1 | 5.68 |
| CHEMBL1502 | PANTOPRAZOLE | 4.0 | 1 | 5.55 |
| CHEMBL481 | IRINOTECAN | 4.0 | 1 | 5.37 |
| CHEMBL46 | ONDANSETRON | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL941 | IMATINIB | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL58 | MITOXANTRONE | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL55 | PENTAMIDINE | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL360861 | NIFEKALANT | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL5483011 | INDINAVIR | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL163 | RITONAVIR | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL1502 | PANTOPRAZOLE | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL481 | IRINOTECAN | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL46 | ONDANSETRON | IC50 | < | 10.0 | nM | - |