Assay Detail
Binding
CHEMBL753512
Review assay metadata, readout intent, target linkage, and publication context from the same page.
The dissociation constant was measured as binding affinity to P-Glycoprotein C-terminal cytosolic domain using the grafit program.
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Halogenated chalcones with high-affinity binding to P-glycoprotein: potential modulators of multidrug resistance.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 7 | 5.78 | 6.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL130508 | — | — | 1 | 6.60 |
| CHEMBL131703 | 4-BROMO-2',4',6'-TRIHYDROXYCHALCONE | — | 1 | 6.24 |
| CHEMBL131961 | 4-CHLORO-2',4',6'-TRIHYDROXYCHALCONE | — | 1 | 5.89 |
| CHEMBL133588 | 4-METHOXYL-2',4',6'-TRIHYDROXYCHALCONE | — | 1 | 5.64 |
| CHEMBL334384 | 4-FLUORO-2',4',6'-TRIHYDROXYCHALCONE | — | 1 | 5.44 |
| CHEMBL129371 | 2',4',6-TRIHYDROXYCHALCONE | — | 1 | 5.34 |
| CHEMBL338066 | 4,2',4',6'-TETRAHYDROXYCHALCONE | — | 1 | 5.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL130508 | — | Kd | = | 250.0 | nM | 6.60 |
| CHEMBL131703 | 4-BROMO-2',4',6'-TRIHYDROXYCHALCONE | Kd | = | 570.0 | nM | 6.24 |
| CHEMBL131961 | 4-CHLORO-2',4',6'-TRIHYDROXYCHALCONE | Kd | = | 1300.0 | nM | 5.89 |
| CHEMBL133588 | 4-METHOXYL-2',4',6'-TRIHYDROXYCHALCONE | Kd | = | 2300.0 | nM | 5.64 |
| CHEMBL334384 | 4-FLUORO-2',4',6'-TRIHYDROXYCHALCONE | Kd | = | 3600.0 | nM | 5.44 |
| CHEMBL129371 | 2',4',6-TRIHYDROXYCHALCONE | Kd | = | 4600.0 | nM | 5.34 |
| CHEMBL338066 | 4,2',4',6'-TETRAHYDROXYCHALCONE | Kd | = | 4800.0 | nM | 5.32 |