Assay Detail
Functional
CHEMBL2077839
Review assay metadata, readout intent, target linkage, and publication context from the same page.
TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 1 uM) in OCT3-expressing HRPE cells
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | HRPE |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Solute carrier family 22 member 3 (CHEMBL1770033) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Identity of the organic cation transporter OCT3 as the extraneuronal monoamine transporter (uptake2) and evidence for the expression of the transporter in the brain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 4.19 | 4.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL405 | AMPHETAMINE | 4.0 | 1 | 4.38 |
| CHEMBL59 | DOPAMINE | 4.0 | 1 | 4.21 |
| CHEMBL72 | DESIPRAMINE | 4.0 | 1 | 4.17 |
| CHEMBL39 | SEROTONIN | 3.0 | 1 | 4.01 |
| CHEMBL1201201 | METHAMPHETAMINE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL405 | AMPHETAMINE | IC50 | = | 42000.0 | nM | 4.38 |
| CHEMBL59 | DOPAMINE | IC50 | = | 62000.0 | nM | 4.21 |
| CHEMBL72 | DESIPRAMINE | IC50 | = | 68000.0 | nM | 4.17 |
| CHEMBL39 | SEROTONIN | IC50 | = | 97000.0 | nM | 4.01 |
| CHEMBL1201201 | METHAMPHETAMINE | IC50 | = | 248000.0 | nM | - |