Assay Detail
Binding
CHEMBL3096293
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human BCRP expressed in MDCK2 cells assessed as Hoechst 33342 accumulation treated 30 mins before Hoechst 33342 addition measured up to 120 mins by fluorescence assay
31
Total Activities
31
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
Investigation of quinazolines as inhibitors of breast cancer resistance protein (ABCG2).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 6.13 | 7.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3092485 | — | — | 1 | 7.12 |
| CHEMBL3092490 | — | — | 1 | 6.85 |
| CHEMBL1360562 | — | — | 1 | 6.82 |
| CHEMBL3092488 | — | — | 1 | 6.72 |
| CHEMBL488910 | — | — | 1 | 6.60 |
| CHEMBL3092489 | — | — | 1 | 6.58 |
| CHEMBL3092482 | — | — | 1 | 6.54 |
| CHEMBL3092486 | — | — | 1 | 6.52 |
| CHEMBL3092487 | — | — | 1 | 6.52 |
| CHEMBL3092500 | — | — | 1 | 6.48 |
| CHEMBL3092483 | — | — | 1 | 6.38 |
| CHEMBL3092491 | — | — | 1 | 6.33 |
| CHEMBL3092499 | — | — | 1 | 6.32 |
| CHEMBL3092484 | — | — | 1 | 6.19 |
| CHEMBL1999832 | — | — | 1 | 6.17 |
| CHEMBL3092498 | — | — | 1 | 6.10 |
| CHEMBL3092496 | — | — | 1 | 6.09 |
| CHEMBL92824 | — | — | 1 | 6.03 |
| CHEMBL2333998 | — | — | 1 | 5.97 |
| CHEMBL290096 | — | — | 1 | 5.97 |
| CHEMBL3092493 | — | — | 1 | 5.95 |
| CHEMBL3092492 | — | — | 1 | 5.93 |
| CHEMBL29197 | — | — | 1 | 5.76 |
| CHEMBL3092501 | — | — | 1 | 5.76 |
| CHEMBL3092481 | — | — | 1 | 5.70 |
| CHEMBL316064 | — | — | 1 | 5.62 |
| CHEMBL3092497 | — | — | 1 | 5.54 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 5.50 |
| CHEMBL3092495 | — | — | 1 | 5.42 |
| CHEMBL3092494 | — | — | 1 | 5.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3092485 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL3092490 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL1360562 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3092488 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL488910 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL3092489 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL3092482 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL3092486 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL3092487 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL3092500 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL3092483 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL3092491 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL3092499 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL3092484 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL1999832 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL3092498 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL3092496 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL92824 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL2333998 | — | IC50 | = | 1060.0 | nM | 5.97 |
| CHEMBL290096 | — | IC50 | = | 1080.0 | nM | 5.97 |
| CHEMBL3092493 | — | IC50 | = | 1130.0 | nM | 5.95 |
| CHEMBL3092492 | — | IC50 | = | 1180.0 | nM | 5.93 |
| CHEMBL29197 | — | IC50 | = | 1730.0 | nM | 5.76 |
| CHEMBL3092501 | — | IC50 | = | 1740.0 | nM | 5.76 |
| CHEMBL3092481 | — | IC50 | = | 1990.0 | nM | 5.70 |
| CHEMBL316064 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL3092497 | — | IC50 | = | 2920.0 | nM | 5.54 |
| CHEMBL939 | GEFITINIB | IC50 | = | 3190.0 | nM | 5.50 |
| CHEMBL3092495 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL3092494 | — | IC50 | = | 4790.0 | nM | 5.32 |
| CHEMBL100714 | — | IC50 | = | 7380.0 | nM | 5.13 |