Assay Detail
Binding
CHEMBL3430265
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GFP-tagged human BCRP expressed in MDCK2 cells pre-incubated for 30 mins followed by Hoechst 33342 addition and further incubated for 120 mins by Hoechst 33342 accumulation assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MDCK-II |
| 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
HM30181 Derivatives as Novel Potent and Selective Inhibitors of the Breast Cancer Resistance Protein (BCRP/ABCG2).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.72 | 7.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3426401 | — | — | 1 | 7.19 |
| CHEMBL3426399 | — | — | 1 | 7.14 |
| CHEMBL3426402 | — | — | 1 | 7.10 |
| CHEMBL3426387 | — | — | 1 | 7.10 |
| CHEMBL3426384 | — | — | 1 | 7.00 |
| CHEMBL3426395 | — | — | 1 | 6.97 |
| CHEMBL3426388 | — | — | 1 | 6.93 |
| CHEMBL3426398 | — | — | 1 | 6.93 |
| CHEMBL488910 | — | — | 1 | 6.89 |
| CHEMBL3426391 | — | — | 1 | 6.86 |
| CHEMBL3426400 | — | — | 1 | 6.75 |
| CHEMBL3426382 | — | — | 1 | 6.74 |
| CHEMBL3426397 | — | — | 1 | 6.70 |
| CHEMBL3426386 | — | — | 1 | 6.58 |
| CHEMBL3426396 | — | — | 1 | 6.57 |
| CHEMBL3426393 | — | — | 1 | 6.35 |
| CHEMBL428402 | — | — | 1 | 6.14 |
| CHEMBL3426394 | — | — | 1 | 4.95 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3426401 | — | IC50 | = | 64.2 | nM | 7.19 |
| CHEMBL3426399 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL3426402 | — | IC50 | = | 79.4 | nM | 7.10 |
| CHEMBL3426387 | — | IC50 | = | 78.9 | nM | 7.10 |
| CHEMBL3426384 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3426395 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL3426388 | — | IC50 | = | 118.0 | nM | 6.93 |
| CHEMBL3426398 | — | IC50 | = | 117.0 | nM | 6.93 |
| CHEMBL488910 | — | IC50 | = | 128.0 | nM | 6.89 |
| CHEMBL3426391 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL3426400 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL3426382 | — | IC50 | = | 184.0 | nM | 6.74 |
| CHEMBL3426397 | — | IC50 | = | 201.0 | nM | 6.70 |
| CHEMBL3426386 | — | IC50 | = | 261.0 | nM | 6.58 |
| CHEMBL3426396 | — | IC50 | = | 269.0 | nM | 6.57 |
| CHEMBL3426393 | — | IC50 | = | 451.0 | nM | 6.35 |
| CHEMBL428402 | — | IC50 | = | 721.0 | nM | 6.14 |
| CHEMBL3426394 | — | IC50 | = | 11200.0 | nM | 4.95 |