Assay Detail
Binding
CHEMBL4328822
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GFP-fused human ABCG2 expressed in MDCK2 cells assessed as Hoechst 33342 accumulation preincubated for 30 mins followed by Hoechst 33342 addition by fluorescence assay
40
Total Activities
40
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 evaluation of quinazoline derivatives - A SAR study of novel inhibitors of ABCG2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 40 | 5.88 | 7.26 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4456005 | — | — | 1 | 7.26 |
| CHEMBL2158556 | — | — | 1 | 7.16 |
| CHEMBL4582715 | — | — | 1 | 7.03 |
| CHEMBL2158554 | — | — | 1 | 6.82 |
| CHEMBL4469532 | — | — | 1 | 6.81 |
| CHEMBL4470633 | — | — | 1 | 6.75 |
| CHEMBL4446794 | — | — | 1 | 6.70 |
| CHEMBL488910 | — | — | 1 | 6.64 |
| CHEMBL4579169 | — | — | 1 | 6.52 |
| CHEMBL4483754 | — | — | 1 | 6.47 |
| CHEMBL1307612 | — | — | 1 | 6.44 |
| CHEMBL435866 | — | — | 1 | 6.37 |
| CHEMBL117697 | — | — | 1 | 6.19 |
| CHEMBL4475108 | — | — | 1 | 6.19 |
| CHEMBL1194993 | — | — | 1 | 6.05 |
| CHEMBL4450363 | — | — | 1 | 6.02 |
| CHEMBL4442077 | — | — | 1 | 6.00 |
| CHEMBL4554634 | — | — | 1 | 6.00 |
| CHEMBL4561833 | — | — | 1 | 5.90 |
| CHEMBL4560864 | — | — | 1 | 5.87 |
| CHEMBL4464779 | — | — | 1 | 5.69 |
| CHEMBL4448170 | — | — | 1 | 5.59 |
| CHEMBL166336 | — | — | 1 | 5.58 |
| CHEMBL4533300 | — | — | 1 | 5.54 |
| CHEMBL4464445 | — | — | 1 | 5.43 |
| CHEMBL4454183 | — | — | 1 | 5.41 |
| CHEMBL4465018 | — | — | 1 | 5.40 |
| CHEMBL4588846 | — | — | 1 | 5.32 |
| CHEMBL4451576 | — | — | 1 | 5.14 |
| CHEMBL4446484 | — | — | 1 | 5.13 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4456005 | — | IC50 | = | 54.5 | nM | 7.26 |
| CHEMBL2158556 | — | IC50 | = | 69.6 | nM | 7.16 |
| CHEMBL4582715 | — | IC50 | = | 93.1 | nM | 7.03 |
| CHEMBL2158554 | — | IC50 | = | 152.0 | nM | 6.82 |
| CHEMBL4469532 | — | IC50 | = | 156.0 | nM | 6.81 |
| CHEMBL4470633 | — | IC50 | = | 178.0 | nM | 6.75 |
| CHEMBL4446794 | — | IC50 | = | 202.0 | nM | 6.70 |
| CHEMBL488910 | — | IC50 | = | 227.0 | nM | 6.64 |
| CHEMBL4579169 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4483754 | — | IC50 | = | 335.0 | nM | 6.47 |
| CHEMBL1307612 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL435866 | — | IC50 | = | 424.0 | nM | 6.37 |
| CHEMBL117697 | — | IC50 | = | 645.0 | nM | 6.19 |
| CHEMBL4475108 | — | IC50 | = | 652.0 | nM | 6.19 |
| CHEMBL1194993 | — | IC50 | = | 882.0 | nM | 6.05 |
| CHEMBL4450363 | — | IC50 | = | 953.0 | nM | 6.02 |
| CHEMBL4442077 | — | IC50 | = | 994.0 | nM | 6.00 |
| CHEMBL4554634 | — | IC50 | = | 989.0 | nM | 6.00 |
| CHEMBL4561833 | — | IC50 | = | 1270.0 | nM | 5.90 |
| CHEMBL4560864 | — | IC50 | = | 1350.0 | nM | 5.87 |
| CHEMBL4464779 | — | IC50 | = | 2025.0 | nM | 5.69 |
| CHEMBL4448170 | — | IC50 | = | 2570.0 | nM | 5.59 |
| CHEMBL166336 | — | IC50 | = | 2630.0 | nM | 5.58 |
| CHEMBL4533300 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL4464445 | — | IC50 | = | 3669.0 | nM | 5.43 |
| CHEMBL4454183 | — | IC50 | = | 3860.0 | nM | 5.41 |
| CHEMBL4465018 | — | IC50 | = | 3948.0 | nM | 5.40 |
| CHEMBL4588846 | — | IC50 | = | 4780.0 | nM | 5.32 |
| CHEMBL4451576 | — | IC50 | = | 7270.0 | nM | 5.14 |
| CHEMBL4446484 | — | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL92985 | — | IC50 | = | 8120.0 | nM | 5.09 |
| CHEMBL4526091 | — | IC50 | = | 10080.0 | nM | 5.00 |
| CHEMBL4529348 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL289959 | — | IC50 | = | 10700.0 | nM | 4.97 |
| CHEMBL4449051 | — | IC50 | = | 14500.0 | nM | 4.84 |
| CHEMBL4588052 | — | IC50 | = | 14800.0 | nM | 4.83 |
| CHEMBL4524796 | — | IC50 | = | 28900.0 | nM | 4.54 |
| CHEMBL4452211 | — | IC50 | - | — | - | |
| CHEMBL4587670 | — | IC50 | - | — | - | |
| CHEMBL4550398 | — | IC50 | - | — | - |