Assay Detail
Binding
CHEMBL4151582
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Inhibition of c-terminal GFP-tagged human ABCG2 expressed in MDCK2 cells preincubated for 30 mins before Hoechst 33342 addition by Hoechst 33342 accumulation assay
41
Total Activities
41
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
2,4,6-Substituted Quinazolines with Extraordinary Inhibitory Potency toward ABCG2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 41 | 6.92 | 7.63 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4172752 | — | — | 1 | 7.63 |
| CHEMBL4168022 | — | — | 1 | 7.56 |
| CHEMBL4163310 | — | — | 1 | 7.56 |
| CHEMBL4167856 | — | — | 1 | 7.52 |
| CHEMBL4160408 | — | — | 1 | 7.48 |
| CHEMBL4166754 | — | — | 1 | 7.48 |
| CHEMBL4163063 | — | — | 1 | 7.43 |
| CHEMBL4171017 | — | — | 1 | 7.43 |
| CHEMBL4164420 | — | — | 1 | 7.35 |
| CHEMBL4171213 | — | — | 1 | 7.35 |
| CHEMBL4174412 | — | — | 1 | 7.33 |
| CHEMBL4163784 | — | — | 1 | 7.32 |
| CHEMBL4174458 | — | — | 1 | 7.32 |
| CHEMBL4164189 | — | — | 1 | 7.31 |
| CHEMBL4172063 | — | — | 1 | 7.29 |
| CHEMBL4164845 | — | — | 1 | 7.24 |
| CHEMBL4174809 | — | — | 1 | 7.24 |
| CHEMBL4175885 | — | — | 1 | 7.23 |
| CHEMBL4167604 | — | — | 1 | 7.22 |
| CHEMBL4174654 | — | — | 1 | 7.21 |
| CHEMBL4159686 | — | — | 1 | 7.20 |
| CHEMBL4170623 | — | — | 1 | 7.18 |
| CHEMBL4175064 | — | — | 1 | 7.18 |
| CHEMBL4164155 | — | — | 1 | 7.12 |
| CHEMBL4170981 | — | — | 1 | 7.10 |
| CHEMBL4159937 | — | — | 1 | 7.00 |
| CHEMBL4159327 | — | — | 1 | 6.97 |
| CHEMBL4162699 | — | — | 1 | 6.92 |
| CHEMBL2158554 | — | — | 1 | 6.82 |
| CHEMBL488910 | — | — | 1 | 6.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4172752 | — | IC50 | = | 23.4 | nM | 7.63 |
| CHEMBL4168022 | — | IC50 | = | 27.6 | nM | 7.56 |
| CHEMBL4163310 | — | IC50 | = | 27.8 | nM | 7.56 |
| CHEMBL4167856 | — | IC50 | = | 30.2 | nM | 7.52 |
| CHEMBL4160408 | — | IC50 | = | 33.1 | nM | 7.48 |
| CHEMBL4166754 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4163063 | — | IC50 | = | 37.4 | nM | 7.43 |
| CHEMBL4171017 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL4164420 | — | IC50 | = | 44.8 | nM | 7.35 |
| CHEMBL4171213 | — | IC50 | = | 44.8 | nM | 7.35 |
| CHEMBL4174412 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL4163784 | — | IC50 | = | 48.2 | nM | 7.32 |
| CHEMBL4174458 | — | IC50 | = | 48.1 | nM | 7.32 |
| CHEMBL4164189 | — | IC50 | = | 49.1 | nM | 7.31 |
| CHEMBL4172063 | — | IC50 | = | 51.5 | nM | 7.29 |
| CHEMBL4164845 | — | IC50 | = | 57.2 | nM | 7.24 |
| CHEMBL4174809 | — | IC50 | = | 57.7 | nM | 7.24 |
| CHEMBL4175885 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL4167604 | — | IC50 | = | 59.6 | nM | 7.22 |
| CHEMBL4174654 | — | IC50 | = | 61.4 | nM | 7.21 |
| CHEMBL4159686 | — | IC50 | = | 63.8 | nM | 7.20 |
| CHEMBL4175064 | — | IC50 | = | 66.3 | nM | 7.18 |
| CHEMBL4170623 | — | IC50 | = | 65.3 | nM | 7.18 |
| CHEMBL4164155 | — | IC50 | = | 75.5 | nM | 7.12 |
| CHEMBL4170981 | — | IC50 | = | 78.7 | nM | 7.10 |
| CHEMBL4159937 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL4159327 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL4162699 | — | IC50 | = | 119.0 | nM | 6.92 |
| CHEMBL2158554 | — | IC50 | = | 152.0 | nM | 6.82 |
| CHEMBL488910 | — | IC50 | = | 227.0 | nM | 6.64 |
| CHEMBL4169043 | — | IC50 | = | 369.0 | nM | 6.43 |
| CHEMBL4176905 | — | IC50 | = | 646.0 | nM | 6.19 |
| CHEMBL4165609 | — | IC50 | = | 726.0 | nM | 6.14 |
| CHEMBL4173540 | — | IC50 | = | 799.0 | nM | 6.10 |
| CHEMBL4167361 | — | IC50 | = | 835.0 | nM | 6.08 |
| CHEMBL1194993 | — | IC50 | = | 882.0 | nM | 6.05 |
| CHEMBL4166495 | — | IC50 | = | 904.0 | nM | 6.04 |
| CHEMBL4171155 | — | IC50 | = | 1040.0 | nM | 5.98 |
| CHEMBL4172412 | — | IC50 | = | 1150.0 | nM | 5.94 |
| CHEMBL4161772 | — | IC50 | = | 1620.0 | nM | 5.79 |
| CHEMBL4165209 | — | IC50 | = | 5310.0 | nM | 5.28 |