Assay Detail
Binding
CHEMBL2320301
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Inhibition of human OCT3-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
12
Total Activities
12
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 3 (CHEMBL2073673) ↗| 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 | 12 | 4.92 | 6.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL790 | CHLORHEXIDINE | 4.0 | 1 | 6.39 |
| CHEMBL290106 | BITHIONOL | 4.0 | 1 | 5.26 |
| CHEMBL55 | PENTAMIDINE | 4.0 | 1 | 5.02 |
| CHEMBL902 | FAMOTIDINE | 4.0 | 1 | 4.97 |
| CHEMBL46 | ONDANSETRON | 4.0 | 1 | 4.76 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 4.59 |
| CHEMBL58 | MITOXANTRONE | 4.0 | 1 | 4.22 |
| CHEMBL481 | IRINOTECAN | 4.0 | 1 | 4.13 |
| CHEMBL1502 | PANTOPRAZOLE | 4.0 | 1 | - |
| CHEMBL360861 | NIFEKALANT | 3.0 | 1 | - |
| CHEMBL5483011 | INDINAVIR | 3.0 | 1 | - |
| CHEMBL163 | RITONAVIR | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL790 | CHLORHEXIDINE | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL290106 | BITHIONOL | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL55 | PENTAMIDINE | IC50 | = | 9500.0 | nM | 5.02 |
| CHEMBL902 | FAMOTIDINE | IC50 | = | 10700.0 | nM | 4.97 |
| CHEMBL46 | ONDANSETRON | IC50 | = | 17400.0 | nM | 4.76 |
| CHEMBL941 | IMATINIB | IC50 | = | 25500.0 | nM | 4.59 |
| CHEMBL58 | MITOXANTRONE | IC50 | = | 60500.0 | nM | 4.22 |
| CHEMBL481 | IRINOTECAN | IC50 | = | 74600.0 | nM | 4.13 |
| CHEMBL1502 | PANTOPRAZOLE | IC50 | = | 137000.0 | nM | - |
| CHEMBL360861 | NIFEKALANT | IC50 | = | 146000.0 | nM | - |
| CHEMBL5483011 | INDINAVIR | IC50 | > | 500000.0 | nM | - |
| CHEMBL163 | RITONAVIR | IC50 | > | 300000.0 | nM | - |