Assay Detail
Binding
CHEMBL754774
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Concentration giving half of the maximal ATPase activity calculated for the high-affinity binding site of the CHO P-Glycoprotein (P-gp) in two-affinity model
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cricetulus griseus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 5.67 | 7.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL83 | TAMOXIFEN | 4.0 | 1 | 7.00 |
| CHEMBL772 | RESERPINE | 4.0 | 1 | 7.00 |
| CHEMBL159 | VINBLASTINE | 4.0 | 1 | 5.89 |
| CHEMBL197 | DEXVERAPAMIL | 2.0 | 1 | 5.80 |
| CHEMBL6966 | VERAPAMIL | 4.0 | 1 | 5.60 |
| CHEMBL633 | AMIODARONE | 4.0 | 1 | 5.50 |
| CHEMBL631 | PROPAFENONE | 4.0 | 1 | 5.38 |
| CHEMBL1294 | QUINIDINE | 4.0 | 1 | 5.30 |
| CHEMBL422 | TRIFLUOPERAZINE | 4.0 | 1 | 5.19 |
| CHEMBL71 | CHLORPROMAZINE | 4.0 | 1 | 4.91 |
| CHEMBL570 | TRIFLUPROMAZINE | 4.0 | 1 | 4.80 |
| CHEMBL452861 | LEVOPROPRANOLOL | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL83 | TAMOXIFEN | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL772 | RESERPINE | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL159 | VINBLASTINE | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL197 | DEXVERAPAMIL | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL6966 | VERAPAMIL | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL633 | AMIODARONE | Ki | = | 3200.0 | nM | 5.50 |
| CHEMBL631 | PROPAFENONE | Ki | = | 4200.0 | nM | 5.38 |
| CHEMBL1294 | QUINIDINE | Ki | = | 5000.0 | nM | 5.30 |
| CHEMBL422 | TRIFLUOPERAZINE | Ki | = | 6500.0 | nM | 5.19 |
| CHEMBL71 | CHLORPROMAZINE | Ki | = | 12200.0 | nM | 4.91 |
| CHEMBL570 | TRIFLUPROMAZINE | Ki | = | 15700.0 | nM | 4.80 |
| CHEMBL452861 | LEVOPROPRANOLOL | Ki | = | 170000.0 | nM | - |