Assay Detail
Binding
CHEMBL4132978
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ABCG2 ATPase activity (unknown origin) expressed in baculovirus infected high5 cell membranes after 20 mins by ascorbic acid ammonia molybdate reaction based colorimetric assay
18
Total Activities
18
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 |
Target
Broad substrate specificity ATP-binding cassette transporter ABCG2 (CHEMBL5393) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and biological investigation of 2,4-substituted quinazolines as highly potent inhibitors of breast cancer resistance protein (ABCG2).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 5.88 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4170247 | — | — | 1 | 7.70 |
| CHEMBL488910 | — | — | 1 | 7.08 |
| CHEMBL4161606 | — | — | 1 | 7.08 |
| CHEMBL4169523 | — | — | 1 | 6.75 |
| CHEMBL4161193 | — | — | 1 | 6.09 |
| CHEMBL4159527 | — | — | 1 | 5.97 |
| CHEMBL4176534 | — | — | 1 | 5.88 |
| CHEMBL4172857 | — | — | 1 | 5.84 |
| CHEMBL4159635 | — | — | 1 | 5.83 |
| CHEMBL4168440 | — | — | 1 | 5.83 |
| CHEMBL4160529 | — | — | 1 | 5.61 |
| CHEMBL3092486 | — | — | 1 | 5.53 |
| CHEMBL4164537 | — | — | 1 | 5.51 |
| CHEMBL4176826 | — | — | 1 | 5.50 |
| CHEMBL4171781 | — | — | 1 | 5.42 |
| CHEMBL4171304 | — | — | 1 | 4.96 |
| CHEMBL3092485 | — | — | 1 | 4.71 |
| CHEMBL4166863 | — | — | 1 | 4.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4170247 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL488910 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL4161606 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL4169523 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4161193 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL4159527 | — | IC50 | = | 1060.0 | nM | 5.97 |
| CHEMBL4176534 | — | IC50 | = | 1310.0 | nM | 5.88 |
| CHEMBL4172857 | — | IC50 | = | 1430.0 | nM | 5.84 |
| CHEMBL4159635 | — | IC50 | = | 1490.0 | nM | 5.83 |
| CHEMBL4168440 | — | IC50 | = | 1470.0 | nM | 5.83 |
| CHEMBL4160529 | — | IC50 | = | 2460.0 | nM | 5.61 |
| CHEMBL3092486 | — | IC50 | = | 2960.0 | nM | 5.53 |
| CHEMBL4164537 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL4176826 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL4171781 | — | IC50 | = | 3820.0 | nM | 5.42 |
| CHEMBL4171304 | — | IC50 | = | 10900.0 | nM | 4.96 |
| CHEMBL3092485 | — | IC50 | = | 19400.0 | nM | 4.71 |
| CHEMBL4166863 | — | IC50 | = | 24000.0 | nM | 4.62 |