Assay Detail
Binding
CHEMBL994103
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
45
Total Activities
44
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
Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 45 | 4.58 | 5.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1626 | CLEMASTINE | 4.0 | 1 | 5.31 |
| CHEMBL43 | AMSACRINE | 4.0 | 1 | 5.30 |
| CHEMBL6966 | VERAPAMIL | 4.0 | 1 | 5.17 |
| CHEMBL1272 | REPAGLINIDE | 4.0 | 1 | 5.04 |
| CHEMBL2 | PRAZOSIN | 4.0 | 1 | 5.00 |
| CHEMBL631 | PROPAFENONE | 4.0 | 1 | 4.96 |
| CHEMBL23 | DILTIAZEM | 4.0 | 1 | 4.91 |
| CHEMBL517712 | ATROPINE | 4.0 | 1 | 4.91 |
| CHEMBL900 | ORPHENADRINE | 4.0 | 1 | 4.90 |
| CHEMBL753 | PHENOXYBENZAMINE | 4.0 | 1 | 4.82 |
| CHEMBL11 | IMIPRAMINE | 4.0 | 1 | 4.77 |
| CHEMBL629 | AMITRIPTYLINE | 4.0 | 1 | 4.77 |
| CHEMBL564 | PROMAZINE | 4.0 | 1 | 4.76 |
| CHEMBL549 | CITALOPRAM | 4.0 | 1 | 4.73 |
| CHEMBL415 | CLOMIPRAMINE | 4.0 | 1 | 4.71 |
| CHEMBL46 | ONDANSETRON | 4.0 | 1 | 4.69 |
| CHEMBL53 | APOMORPHINE | 4.0 | 1 | 4.68 |
| CHEMBL134 | CLONIDINE | 4.0 | 1 | 4.65 |
| CHEMBL611 | TERAZOSIN | 4.0 | 1 | 4.62 |
| CHEMBL841 | LOPERAMIDE | 4.0 | 1 | 4.62 |
| CHEMBL71 | CHLORPROMAZINE | 4.0 | 1 | 4.57 |
| CHEMBL321582 | BUCINDOLOL | 2.0 | 1 | 4.57 |
| CHEMBL807 | MEMANTINE | 4.0 | 1 | 4.57 |
| CHEMBL644 | TRIMIPRAMINE | 4.0 | 1 | 4.56 |
| CHEMBL70 | MORPHINE | 4.0 | 1 | 4.55 |
| CHEMBL546 | OXPRENOLOL | 4.0 | 1 | 4.54 |
| CHEMBL757 | NANDROLONE | 3.0 | 1 | 4.46 |
| CHEMBL643 | PROMETHAZINE | 4.0 | 1 | 4.46 |
| CHEMBL493682 | DENOPAMINE | 2.0 | 1 | 4.33 |
| CHEMBL728 | PROCHLORPERAZINE | 4.0 | 1 | 4.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1626 | CLEMASTINE | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL43 | AMSACRINE | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL6966 | VERAPAMIL | IC50 | = | 6800.0 | nM | 5.17 |
| CHEMBL1272 | REPAGLINIDE | IC50 | = | 9200.0 | nM | 5.04 |
| CHEMBL2 | PRAZOSIN | IC50 | = | 9900.0 | nM | 5.00 |
| CHEMBL631 | PROPAFENONE | IC50 | = | 11100.0 | nM | 4.96 |
| CHEMBL23 | DILTIAZEM | IC50 | = | 12400.0 | nM | 4.91 |
| CHEMBL517712 | ATROPINE | IC50 | = | 12200.0 | nM | 4.91 |
| CHEMBL900 | ORPHENADRINE | IC50 | = | 12600.0 | nM | 4.90 |
| CHEMBL753 | PHENOXYBENZAMINE | IC50 | = | 15100.0 | nM | 4.82 |
| CHEMBL629 | AMITRIPTYLINE | IC50 | = | 16900.0 | nM | 4.77 |
| CHEMBL11 | IMIPRAMINE | IC50 | = | 17100.0 | nM | 4.77 |
| CHEMBL564 | PROMAZINE | IC50 | = | 17200.0 | nM | 4.76 |
| CHEMBL549 | CITALOPRAM | IC50 | = | 18800.0 | nM | 4.73 |
| CHEMBL415 | CLOMIPRAMINE | IC50 | = | 19300.0 | nM | 4.71 |
| CHEMBL46 | ONDANSETRON | IC50 | = | 20400.0 | nM | 4.69 |
| CHEMBL53 | APOMORPHINE | IC50 | = | 20800.0 | nM | 4.68 |
| CHEMBL134 | CLONIDINE | IC50 | = | 22600.0 | nM | 4.65 |
| CHEMBL611 | TERAZOSIN | IC50 | = | 23700.0 | nM | 4.62 |
| CHEMBL841 | LOPERAMIDE | IC50 | = | 23700.0 | nM | 4.62 |
| CHEMBL807 | MEMANTINE | IC50 | = | 27200.0 | nM | 4.57 |
| CHEMBL71 | CHLORPROMAZINE | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL321582 | BUCINDOLOL | IC50 | = | 27200.0 | nM | 4.57 |
| CHEMBL644 | TRIMIPRAMINE | IC50 | = | 27700.0 | nM | 4.56 |
| CHEMBL70 | MORPHINE | IC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL546 | OXPRENOLOL | IC50 | = | 28600.0 | nM | 4.54 |
| CHEMBL757 | NANDROLONE | IC50 | = | 35100.0 | nM | 4.46 |
| CHEMBL643 | PROMETHAZINE | IC50 | = | 35100.0 | nM | 4.46 |
| CHEMBL493682 | DENOPAMINE | IC50 | = | 46900.0 | nM | 4.33 |
| CHEMBL728 | PROCHLORPERAZINE | IC50 | = | 49600.0 | nM | 4.30 |
| CHEMBL170 | QUININE | IC50 | = | 51600.0 | nM | 4.29 |
| CHEMBL1237044 | TRAMADOL | IC50 | = | 52500.0 | nM | 4.28 |
| CHEMBL72 | DESIPRAMINE | IC50 | = | 56800.0 | nM | 4.25 |
| CHEMBL22 | TRIMETHOPRIM | IC50 | = | 56800.0 | nM | 4.25 |
| CHEMBL945 | AMILORIDE | IC50 | = | 57000.0 | nM | 4.24 |
| CHEMBL27 | PROPRANOLOL | IC50 | = | 63200.0 | nM | 4.20 |
| CHEMBL1724 | MEPENZOLATE BROMIDE | IC50 | = | 64900.0 | nM | 4.19 |
| CHEMBL908 | CHLORPROTHIXENE | IC50 | = | 77800.0 | nM | 4.11 |
| CHEMBL517 | DISOPYRAMIDE | IC50 | = | 81700.0 | nM | 4.09 |
| CHEMBL6066864 | FLUPENTIXOL | IC50 | = | 89500.0 | nM | 4.05 |
| CHEMBL6066864 | FLUPENTIXOL | IC50 | = | 89500.0 | nM | 4.05 |
| CHEMBL86 | METOCLOPRAMIDE | IC50 | = | 94800.0 | nM | 4.02 |
| CHEMBL54 | HALOPERIDOL | IC50 | = | 141900.0 | nM | - |
| CHEMBL1294 | QUINIDINE | IC50 | = | 113800.0 | nM | - |
| CHEMBL726 | FLUPHENAZINE | IC50 | = | 110000.0 | nM | - |