Assay Detail
Binding
CHEMBL4200598
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Inhibition of ABCG2 in human MCF7/Topo cells after 2 hrs by Hoechst 33342 staining based fluorescence assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 Chalcones and Ketones as ABCG2 Modulators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 5.52 | 6.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL348475 | TARIQUIDAR | 3.0 | 1 | 6.28 |
| CHEMBL410316 | FUMITREMORGIN | — | 1 | 6.14 |
| CHEMBL4213215 | — | — | 1 | 6.06 |
| CHEMBL4206629 | — | — | 1 | 5.95 |
| CHEMBL4209477 | — | — | 1 | 5.81 |
| CHEMBL4206326 | — | — | 1 | 5.67 |
| CHEMBL4203520 | — | — | 1 | 5.57 |
| CHEMBL4202610 | — | — | 1 | 5.55 |
| CHEMBL4204938 | — | — | 1 | 5.39 |
| CHEMBL4208261 | — | — | 1 | 5.18 |
| CHEMBL4216382 | — | — | 1 | 5.17 |
| CHEMBL4215970 | — | — | 1 | 5.06 |
| CHEMBL4210356 | — | — | 1 | 4.84 |
| CHEMBL4204291 | — | — | 1 | 4.63 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL348475 | TARIQUIDAR | IC50 | = | 526.0 | nM | 6.28 |
| CHEMBL410316 | FUMITREMORGIN | IC50 | = | 731.0 | nM | 6.14 |
| CHEMBL4213215 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL4206629 | — | IC50 | = | 1130.0 | nM | 5.95 |
| CHEMBL4209477 | — | IC50 | = | 1550.0 | nM | 5.81 |
| CHEMBL4206326 | — | IC50 | = | 2130.0 | nM | 5.67 |
| CHEMBL4203520 | — | IC50 | = | 2720.0 | nM | 5.57 |
| CHEMBL4202610 | — | IC50 | = | 2830.0 | nM | 5.55 |
| CHEMBL4204938 | — | IC50 | = | 4080.0 | nM | 5.39 |
| CHEMBL4208261 | — | IC50 | = | 6650.0 | nM | 5.18 |
| CHEMBL4216382 | — | IC50 | = | 6730.0 | nM | 5.17 |
| CHEMBL4215970 | — | IC50 | = | 8760.0 | nM | 5.06 |
| CHEMBL4210356 | — | IC50 | = | 14390.0 | nM | 4.84 |
| CHEMBL4204291 | — | IC50 | = | 23240.0 | nM | 4.63 |