Assay Detail
Binding
CHEMBL754113
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Binding affinity to nucleotide-binding domain (NBD2) of P-Glycoprotein
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
B-ring substituted 5,7-dihydroxyflavonols with high-affinity binding to P-glycoprotein responsible for cell multidrug resistance.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 8 | 5.65 | 7.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL164611 | — | — | 1 | 7.24 |
| CHEMBL166368 | — | — | 1 | 5.97 |
| CHEMBL164555 | — | — | 1 | 5.70 |
| CHEMBL165607 | — | — | 1 | 5.40 |
| CHEMBL40919 | KAEMPFERIDE | — | 1 | 5.30 |
| CHEMBL309490 | GALANGIN | — | 1 | 5.23 |
| CHEMBL150 | KAEMPFEROL | 1.0 | 1 | 5.17 |
| CHEMBL165905 | — | — | 1 | 5.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL164611 | — | Kd | = | 57.0 | nM | 7.24 |
| CHEMBL166368 | — | Kd | = | 1060.0 | nM | 5.97 |
| CHEMBL164555 | — | Kd | = | 2000.0 | nM | 5.70 |
| CHEMBL165607 | — | Kd | = | 4000.0 | nM | 5.40 |
| CHEMBL40919 | KAEMPFERIDE | Kd | = | 5000.0 | nM | 5.30 |
| CHEMBL309490 | GALANGIN | Kd | = | 5900.0 | nM | 5.23 |
| CHEMBL150 | KAEMPFEROL | Kd | = | 6700.0 | nM | 5.17 |
| CHEMBL165905 | — | Kd | = | 6800.0 | nM | 5.17 |