Assay Detail
Binding
CHEMBL4685382
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ABCG2 in topotecan-cultured human MCF7 cells using Hoechst 33342 as substrate measured after 2 hrs 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 | MCF7 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Broad substrate specificity ATP-binding cassette transporter ABCG2 (CHEMBL5393) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Tariquidar-related triazoles as potent, selective and stable inhibitors of ABCG2 (BCRP).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 6.39 | 7.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4764773 | — | — | 1 | 7.10 |
| CHEMBL4790452 | — | — | 1 | 7.09 |
| CHEMBL488910 | — | — | 1 | 7.04 |
| CHEMBL502503 | — | — | 1 | 7.00 |
| CHEMBL4743830 | — | — | 1 | 6.85 |
| CHEMBL4753800 | — | — | 1 | 6.84 |
| CHEMBL4744075 | — | — | 1 | 6.82 |
| CHEMBL4748169 | — | — | 1 | 6.53 |
| CHEMBL4788617 | — | — | 1 | 6.46 |
| CHEMBL4783985 | — | — | 1 | 6.31 |
| CHEMBL4747726 | — | — | 1 | 6.21 |
| CHEMBL2011288 | — | — | 1 | 6.15 |
| CHEMBL4534001 | — | — | 1 | 5.95 |
| CHEMBL410316 | FUMITREMORGIN | — | 1 | 5.83 |
| CHEMBL2011282 | — | — | 1 | 5.75 |
| CHEMBL4786467 | — | — | 1 | 5.48 |
| CHEMBL348475 | TARIQUIDAR | 3.0 | 1 | 5.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4764773 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL4790452 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL488910 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL502503 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL4743830 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4753800 | — | IC50 | = | 144.0 | nM | 6.84 |
| CHEMBL4744075 | — | IC50 | = | 153.0 | nM | 6.82 |
| CHEMBL4748169 | — | IC50 | = | 295.0 | nM | 6.53 |
| CHEMBL4788617 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL4783985 | — | IC50 | = | 486.0 | nM | 6.31 |
| CHEMBL4747726 | — | IC50 | = | 617.0 | nM | 6.21 |
| CHEMBL2011288 | — | IC50 | = | 707.0 | nM | 6.15 |
| CHEMBL4534001 | — | IC50 | = | 1115.0 | nM | 5.95 |
| CHEMBL410316 | FUMITREMORGIN | IC50 | = | 1483.0 | nM | 5.83 |
| CHEMBL2011282 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4786467 | — | IC50 | = | 3345.0 | nM | 5.48 |
| CHEMBL348475 | TARIQUIDAR | IC50 | = | 6223.0 | nM | 5.21 |