Assay Detail
Binding
CHEMBL4327486
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Inhibition of MDR1 (unknown origin) expressed in MDCK cells assessed as reduction in calcein-AM efflux preincubated for 30 mins followed by calcein-AM addition measured after 30 mins by spectrofluorimetric method
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MDCK |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
1,2,3,4-Tetrahydroisoquinoline/2H-chromen-2-one conjugates as nanomolar P-glycoprotein inhibitors: Molecular determinants for affinity and selectivity over multidrug resistance associated protein 1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 6.35 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4592250 | — | — | 1 | 7.16 |
| CHEMBL4476238 | — | — | 1 | 6.82 |
| CHEMBL4539336 | — | — | 1 | 6.80 |
| CHEMBL4473596 | — | — | 1 | 6.80 |
| CHEMBL4462737 | — | — | 1 | 6.72 |
| CHEMBL4450854 | — | — | 1 | 6.72 |
| CHEMBL4569990 | — | — | 1 | 6.72 |
| CHEMBL4571279 | — | — | 1 | 6.66 |
| CHEMBL4464239 | — | — | 1 | 6.66 |
| CHEMBL4474108 | — | — | 1 | 6.55 |
| CHEMBL4452234 | — | — | 1 | 6.48 |
| CHEMBL4436042 | — | — | 1 | 6.42 |
| CHEMBL4563027 | — | — | 1 | 6.41 |
| CHEMBL4451488 | — | — | 1 | 6.39 |
| CHEMBL4466035 | — | — | 1 | 6.34 |
| CHEMBL4514827 | — | — | 1 | 6.26 |
| CHEMBL4562150 | — | — | 1 | 6.25 |
| CHEMBL4541580 | — | — | 1 | 6.11 |
| CHEMBL4474386 | — | — | 1 | 6.04 |
| CHEMBL4553878 | — | — | 1 | 6.00 |
| CHEMBL260599 | — | — | 1 | 5.92 |
| CHEMBL6966 | VERAPAMIL | 4.0 | 1 | 5.89 |
| CHEMBL4574355 | — | — | 1 | 5.57 |
| CHEMBL4435844 | — | — | 1 | 4.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4592250 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4476238 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4539336 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4473596 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4462737 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4450854 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4569990 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4571279 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL4464239 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL4474108 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4452234 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL4436042 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL4563027 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL4451488 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL4466035 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL4514827 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL4562150 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL4541580 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL4474386 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL4553878 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL260599 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL6966 | VERAPAMIL | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4574355 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL4435844 | — | IC50 | = | 15000.0 | nM | 4.82 |