Assay Detail
Binding
CHEMBL1780905
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ABCG2 expressed in human MCF7/Topo cells by Hoechst microplate assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | MCF7/Topo |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Broad substrate specificity ATP-binding cassette transporter ABCG2 (CHEMBL5393) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Solid phase synthesis of tariquidar-related modulators of ABC transporters preferring breast cancer resistance protein (ABCG2).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 6.69 | 7.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL502503 | — | — | 1 | 7.23 |
| CHEMBL396298 | ELACRIDAR | 2.0 | 1 | 6.90 |
| CHEMBL1779526 | — | — | 1 | 6.89 |
| CHEMBL455275 | — | — | 1 | 6.76 |
| CHEMBL1779524 | — | — | 1 | 6.74 |
| CHEMBL1779525 | — | — | 1 | 6.41 |
| CHEMBL1777831 | — | — | 1 | 6.29 |
| CHEMBL348475 | TARIQUIDAR | 3.0 | 1 | 6.28 |
| CHEMBL1779523 | — | — | 1 | - |
| CHEMBL1779522 | — | — | 1 | - |
| CHEMBL1779521 | — | — | 1 | - |
| CHEMBL1779520 | — | — | 1 | - |
| CHEMBL1779519 | — | — | 1 | - |
| CHEMBL1779518 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL502503 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL396298 | ELACRIDAR | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL1779526 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL455275 | — | IC50 | = | 172.0 | nM | 6.76 |
| CHEMBL1779524 | — | IC50 | = | 183.0 | nM | 6.74 |
| CHEMBL1779525 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL1777831 | — | IC50 | = | 508.0 | nM | 6.29 |
| CHEMBL348475 | TARIQUIDAR | IC50 | = | 526.0 | nM | 6.28 |
| CHEMBL1779523 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL1779522 | — | IC50 | > | 6200.0 | nM | - |
| CHEMBL1779521 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL1779520 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL1779519 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1779518 | — | IC50 | > | 5000.0 | nM | - |