Assay Detail
Binding
CHEMBL4685384
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ABCB1 in human KB-V1 cells using calcein-AM as substrate measured after 10 mins by fluorescence assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | KB-V1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Tariquidar-related triazoles as potent, selective and stable inhibitors of ABCG2 (BCRP).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 5.80 | 6.45 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL348475 | TARIQUIDAR | 3.0 | 1 | 6.45 |
| CHEMBL4753800 | — | — | 1 | 5.79 |
| CHEMBL2011288 | — | — | 1 | 5.17 |
| CHEMBL410316 | FUMITREMORGIN | — | 1 | - |
| CHEMBL488910 | — | — | 1 | - |
| CHEMBL4534001 | — | — | 1 | - |
| CHEMBL2011282 | — | — | 1 | - |
| CHEMBL4786467 | — | — | 1 | - |
| CHEMBL502503 | — | — | 1 | - |
| CHEMBL4744075 | — | — | 1 | - |
| CHEMBL4783985 | — | — | 1 | - |
| CHEMBL4747726 | — | — | 1 | - |
| CHEMBL4743830 | — | — | 1 | - |
| CHEMBL4764773 | — | — | 1 | - |
| CHEMBL4748169 | — | — | 1 | - |
| CHEMBL4790452 | — | — | 1 | - |
| CHEMBL4788617 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL348475 | TARIQUIDAR | IC50 | = | 356.0 | nM | 6.45 |
| CHEMBL4753800 | — | IC50 | = | 1623.0 | nM | 5.79 |
| CHEMBL2011288 | — | IC50 | = | 6756.0 | nM | 5.17 |
| CHEMBL410316 | FUMITREMORGIN | IC50 | - | — | - | |
| CHEMBL488910 | — | IC50 | >= | 25520.0 | nM | - |
| CHEMBL4534001 | — | IC50 | - | — | - | |
| CHEMBL2011282 | — | IC50 | - | — | - | |
| CHEMBL4786467 | — | IC50 | >= | 65480.0 | nM | - |
| CHEMBL502503 | — | IC50 | >= | 12080.0 | nM | - |
| CHEMBL4744075 | — | IC50 | >= | 25030.0 | nM | - |
| CHEMBL4783985 | — | IC50 | >= | 38270.0 | nM | - |
| CHEMBL4747726 | — | IC50 | - | — | - | |
| CHEMBL4743830 | — | IC50 | - | — | - | |
| CHEMBL4764773 | — | IC50 | - | — | - | |
| CHEMBL4748169 | — | IC50 | >= | 21830.0 | nM | - |
| CHEMBL4790452 | — | IC50 | >= | 44460.0 | nM | - |
| CHEMBL4788617 | — | IC50 | >= | 10730.0 | nM | - |