Assay Detail
Binding
CHEMBL4046325
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Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of substrate [3H]MPP+ after 1 min by liquid scintillation counting method
9
Total Activities
9
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 |
Publication
A new chemotype inhibitor for the human organic cation transporter 3 (hOCT3).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 5.10 | 6.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4062501 | — | — | 1 | 6.05 |
| CHEMBL4100146 | — | — | 1 | 5.62 |
| CHEMBL1160763 | — | — | 1 | 5.20 |
| CHEMBL43415 | — | — | 1 | 5.00 |
| CHEMBL41040 | — | — | 1 | 5.00 |
| CHEMBL13823 | — | — | 1 | 4.86 |
| CHEMBL1160766 | — | — | 1 | 4.65 |
| CHEMBL14047 | PHENYLGUANIDINE | — | 1 | 4.39 |
| CHEMBL272259 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4062501 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL4100146 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL1160763 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL43415 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL41040 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL13823 | — | IC50 | = | 13700.0 | nM | 4.86 |
| CHEMBL1160766 | — | IC50 | = | 22600.0 | nM | 4.65 |
| CHEMBL14047 | PHENYLGUANIDINE | IC50 | = | 41100.0 | nM | 4.39 |
| CHEMBL272259 | — | IC50 | = | 761900.0 | nM | - |