Assay Detail
Functional
CHEMBL2078481
Review assay metadata, readout intent, target linkage, and publication context from the same page.
TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 0.25 uM) in OCT1-expressing HEK293 cells
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | HEK293 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Expression and pharmacological profile of the human organic cation transporters hOCT1, hOCT2 and hOCT3.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 5.46 | 6.01 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1197556 | — | — | 1 | 6.01 |
| CHEMBL2 | PRAZOSIN | 4.0 | 1 | 5.74 |
| CHEMBL753 | PHENOXYBENZAMINE | 4.0 | 1 | 5.57 |
| CHEMBL103 | PROGESTERONE | 4.0 | 1 | 5.52 |
| CHEMBL135 | ESTRADIOL | 4.0 | 1 | 5.24 |
| CHEMBL110739 | CORTICOSTERONE | 3.0 | 1 | 4.66 |
| CHEMBL2074900 | — | — | 1 | - |
| CHEMBL2074647 | METIPRENALINE | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1197556 | — | IC50 | = | 980.0 | nM | 6.01 |
| CHEMBL2 | PRAZOSIN | IC50 | = | 1840.0 | nM | 5.74 |
| CHEMBL753 | PHENOXYBENZAMINE | IC50 | = | 2720.0 | nM | 5.57 |
| CHEMBL103 | PROGESTERONE | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL135 | ESTRADIOL | IC50 | = | 5730.0 | nM | 5.24 |
| CHEMBL110739 | CORTICOSTERONE | IC50 | = | 21700.0 | nM | 4.66 |
| CHEMBL2074900 | — | IC50 | > | 300.0 | nM | - |
| CHEMBL2074647 | METIPRENALINE | IC50 | > | 100000.0 | nM | - |