Assay Detail
Functional
CHEMBL2076233
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TP_TRANSPORTER: inhibition of TEA uptake in OCT1-expressing HeLa cells
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | HeLa |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Functional characterization of an organic cation transporter (hOCT1) in a transiently transfected human cell line (HeLa).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 5.07 | 6.26 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL134 | CLONIDINE | 4.0 | 1 | 6.26 |
| CHEMBL1197556 | — | — | 1 | 5.56 |
| CHEMBL6966 | VERAPAMIL | 4.0 | 1 | 5.54 |
| CHEMBL655 | MIDAZOLAM | 4.0 | 1 | 5.43 |
| CHEMBL72 | DESIPRAMINE | 4.0 | 1 | 5.27 |
| CHEMBL110739 | CORTICOSTERONE | 3.0 | 1 | 5.15 |
| CHEMBL2074704 | TETRAPENTYLAMMONIUM | — | 1 | 5.13 |
| CHEMBL311617 | — | — | 1 | 4.91 |
| CHEMBL1294 | QUINIDINE | 4.0 | 1 | 4.76 |
| CHEMBL170 | QUININE | 4.0 | 1 | 4.64 |
| CHEMBL640 | PROCAINAMIDE | 4.0 | 1 | 4.13 |
| CHEMBL642 | ACEBUTOLOL | 4.0 | 1 | 4.02 |
| CHEMBL9324 | TETRYLAMMONIUM | 2.0 | 1 | - |
| CHEMBL30 | CIMETIDINE | 4.0 | 1 | - |
| CHEMBL1201219 | VECURONIUM | 4.0 | 1 | - |
| CHEMBL11978 | NICOTINYL METHYLAMIDE | -1.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL134 | CLONIDINE | Ki | = | 550.0 | nM | 6.26 |
| CHEMBL1197556 | — | Ki | = | 2730.0 | nM | 5.56 |
| CHEMBL6966 | VERAPAMIL | Ki | = | 2900.0 | nM | 5.54 |
| CHEMBL655 | MIDAZOLAM | Ki | = | 3700.0 | nM | 5.43 |
| CHEMBL72 | DESIPRAMINE | Ki | = | 5360.0 | nM | 5.27 |
| CHEMBL110739 | CORTICOSTERONE | Ki | = | 7020.0 | nM | 5.15 |
| CHEMBL2074704 | TETRAPENTYLAMMONIUM | Ki | = | 7460.0 | nM | 5.13 |
| CHEMBL311617 | — | Ki | = | 12300.0 | nM | 4.91 |
| CHEMBL1294 | QUINIDINE | Ki | = | 17500.0 | nM | 4.76 |
| CHEMBL170 | QUININE | Ki | = | 22900.0 | nM | 4.64 |
| CHEMBL640 | PROCAINAMIDE | Ki | = | 73900.0 | nM | 4.13 |
| CHEMBL642 | ACEBUTOLOL | Ki | = | 95800.0 | nM | 4.02 |
| CHEMBL9324 | TETRYLAMMONIUM | Ki | = | 161000.0 | nM | - |
| CHEMBL30 | CIMETIDINE | Ki | = | 166000.0 | nM | - |
| CHEMBL1201219 | VECURONIUM | Ki | = | 232000.0 | nM | - |
| CHEMBL11978 | NICOTINYL METHYLAMIDE | Ki | = | 7700000.0 | nM | - |