Assay Detail
Binding
CHEMBL3430271
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ABCB1 in human A2780adr cells pre-incubated for 30 mins followed by calcein AM addition and further incubated for 60 mins by calcein AM assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | A2780 ADR |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
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 | 5 | 5.00 | 6.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL160 | CYCLOSPORINE | 4.0 | 1 | 6.04 |
| CHEMBL3426400 | — | — | 1 | 5.11 |
| CHEMBL3426393 | — | — | 1 | 4.96 |
| CHEMBL3426397 | — | — | 1 | 4.48 |
| CHEMBL3426398 | — | — | 1 | 4.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL160 | CYCLOSPORINE | IC50 | = | 919.0 | nM | 6.04 |
| CHEMBL3426400 | — | IC50 | = | 7730.0 | nM | 5.11 |
| CHEMBL3426393 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL3426397 | — | IC50 | = | 32800.0 | nM | 4.48 |
| CHEMBL3426398 | — | IC50 | = | 37200.0 | nM | 4.43 |