Assay Detail
Binding
CHEMBL4478423
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ABCB1 in human A2780/ADR cells assessed as reduction in calcein AM efflux pre-incubated for 30 mins before calcein AM addition and measured for 60 mins by microplate reader analysis relative to control
20
Total Activities
20
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 |
Publication
Synthesis and Investigation of Tetrahydro-β-carboline Derivatives as Inhibitors of the Breast Cancer Resistance Protein (ABCG2).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 5.07 | 5.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL160 | CYCLOSPORINE | 4.0 | 1 | 5.96 |
| CHEMBL4578134 | — | — | 1 | 5.54 |
| CHEMBL4592538 | — | — | 1 | 5.47 |
| CHEMBL4542075 | — | — | 1 | 5.21 |
| CHEMBL4549558 | — | — | 1 | 5.18 |
| CHEMBL4550890 | — | — | 1 | 5.13 |
| CHEMBL4576040 | — | — | 1 | 5.13 |
| CHEMBL4581843 | — | — | 1 | 5.10 |
| CHEMBL4575544 | — | — | 1 | 5.08 |
| CHEMBL4521174 | — | — | 1 | 5.06 |
| CHEMBL4549093 | — | — | 1 | 5.04 |
| CHEMBL4559337 | — | — | 1 | 5.02 |
| CHEMBL4586159 | — | — | 1 | 4.95 |
| CHEMBL4516431 | — | — | 1 | 4.92 |
| CHEMBL4593846 | — | — | 1 | 4.89 |
| CHEMBL4555019 | — | — | 1 | 4.87 |
| CHEMBL4568684 | — | — | 1 | 4.84 |
| CHEMBL4571543 | — | — | 1 | 4.72 |
| CHEMBL4549202 | — | — | 1 | 4.65 |
| CHEMBL4563533 | — | — | 1 | 4.63 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL160 | CYCLOSPORINE | IC50 | = | 1090.0 | nM | 5.96 |
| CHEMBL4578134 | — | IC50 | = | 2860.0 | nM | 5.54 |
| CHEMBL4592538 | — | IC50 | = | 3380.0 | nM | 5.47 |
| CHEMBL4542075 | — | IC50 | = | 6220.0 | nM | 5.21 |
| CHEMBL4549558 | — | IC50 | = | 6550.0 | nM | 5.18 |
| CHEMBL4550890 | — | IC50 | = | 7330.0 | nM | 5.13 |
| CHEMBL4576040 | — | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL4581843 | — | IC50 | = | 7940.0 | nM | 5.10 |
| CHEMBL4575544 | — | IC50 | = | 8240.0 | nM | 5.08 |
| CHEMBL4521174 | — | IC50 | = | 8760.0 | nM | 5.06 |
| CHEMBL4549093 | — | IC50 | = | 9230.0 | nM | 5.04 |
| CHEMBL4559337 | — | IC50 | = | 9550.0 | nM | 5.02 |
| CHEMBL4586159 | — | IC50 | = | 11300.0 | nM | 4.95 |
| CHEMBL4516431 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL4593846 | — | IC50 | = | 12900.0 | nM | 4.89 |
| CHEMBL4555019 | — | IC50 | = | 13400.0 | nM | 4.87 |
| CHEMBL4568684 | — | IC50 | = | 14300.0 | nM | 4.84 |
| CHEMBL4571543 | — | IC50 | = | 19200.0 | nM | 4.72 |
| CHEMBL4549202 | — | IC50 | = | 22500.0 | nM | 4.65 |
| CHEMBL4563533 | — | IC50 | = | 23400.0 | nM | 4.63 |