Assay Detail
Binding
CHEMBL4048736
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ABCG2 expressed in MDCK2 cells assessed as increase in accumulation of Hoechst 33342 preincubated for 30 mins followed by Hoechst 33342 addition measured every 60 secs for 120 mins by fluorescence assay
38
Total Activities
38
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
New Inhibitors of Breast Cancer Resistance Protein (ABCG2) Containing a 2,4-Disubstituted Pyridopyrimidine Scaffold.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 38 | 6.15 | 6.83 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4072482 | — | — | 1 | 6.83 |
| CHEMBL4070627 | — | — | 1 | 6.82 |
| CHEMBL4063711 | — | — | 1 | 6.79 |
| CHEMBL4077318 | — | — | 1 | 6.79 |
| CHEMBL547193 | — | — | 1 | 6.75 |
| CHEMBL4062196 | — | — | 1 | 6.69 |
| CHEMBL488910 | — | — | 1 | 6.64 |
| CHEMBL4077346 | — | — | 1 | 6.62 |
| CHEMBL4072305 | — | — | 1 | 6.58 |
| CHEMBL4081623 | — | — | 1 | 6.46 |
| CHEMBL4094899 | — | — | 1 | 6.46 |
| CHEMBL4069654 | — | — | 1 | 6.40 |
| CHEMBL4091528 | — | — | 1 | 6.37 |
| CHEMBL4060543 | — | — | 1 | 6.34 |
| CHEMBL4094267 | — | — | 1 | 6.29 |
| CHEMBL4075334 | — | — | 1 | 6.28 |
| CHEMBL4094904 | — | — | 1 | 6.27 |
| CHEMBL4073354 | — | — | 1 | 6.24 |
| CHEMBL4067469 | — | — | 1 | 6.21 |
| CHEMBL4063699 | — | — | 1 | 6.20 |
| CHEMBL4075963 | — | — | 1 | 6.13 |
| CHEMBL4073213 | — | — | 1 | 6.06 |
| CHEMBL1194993 | — | — | 1 | 6.05 |
| CHEMBL4094008 | — | — | 1 | 6.04 |
| CHEMBL4083745 | — | — | 1 | 6.02 |
| CHEMBL4066611 | — | — | 1 | 5.92 |
| CHEMBL4104361 | — | — | 1 | 5.91 |
| CHEMBL4082782 | — | — | 1 | 5.91 |
| CHEMBL4064296 | — | — | 1 | 5.90 |
| CHEMBL4101737 | — | — | 1 | 5.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4072482 | — | IC50 | = | 149.0 | nM | 6.83 |
| CHEMBL4070627 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4077318 | — | IC50 | = | 164.0 | nM | 6.79 |
| CHEMBL4063711 | — | IC50 | = | 163.0 | nM | 6.79 |
| CHEMBL547193 | — | IC50 | = | 177.0 | nM | 6.75 |
| CHEMBL4062196 | — | IC50 | = | 206.0 | nM | 6.69 |
| CHEMBL488910 | — | IC50 | = | 227.0 | nM | 6.64 |
| CHEMBL4077346 | — | IC50 | = | 238.0 | nM | 6.62 |
| CHEMBL4072305 | — | IC50 | = | 264.0 | nM | 6.58 |
| CHEMBL4081623 | — | IC50 | = | 343.0 | nM | 6.46 |
| CHEMBL4094899 | — | IC50 | = | 348.0 | nM | 6.46 |
| CHEMBL4069654 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL4091528 | — | IC50 | = | 425.0 | nM | 6.37 |
| CHEMBL4060543 | — | IC50 | = | 454.0 | nM | 6.34 |
| CHEMBL4094267 | — | IC50 | = | 519.0 | nM | 6.29 |
| CHEMBL4075334 | — | IC50 | = | 528.0 | nM | 6.28 |
| CHEMBL4094904 | — | IC50 | = | 539.0 | nM | 6.27 |
| CHEMBL4073354 | — | IC50 | = | 572.0 | nM | 6.24 |
| CHEMBL4067469 | — | IC50 | = | 621.0 | nM | 6.21 |
| CHEMBL4063699 | — | IC50 | = | 628.0 | nM | 6.20 |
| CHEMBL4075963 | — | IC50 | = | 747.0 | nM | 6.13 |
| CHEMBL4073213 | — | IC50 | = | 876.0 | nM | 6.06 |
| CHEMBL1194993 | — | IC50 | = | 882.0 | nM | 6.05 |
| CHEMBL4094008 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL4083745 | — | IC50 | = | 963.0 | nM | 6.02 |
| CHEMBL4066611 | — | IC50 | = | 1210.0 | nM | 5.92 |
| CHEMBL4104361 | — | IC50 | = | 1230.0 | nM | 5.91 |
| CHEMBL4082782 | — | IC50 | = | 1230.0 | nM | 5.91 |
| CHEMBL4064296 | — | IC50 | = | 1260.0 | nM | 5.90 |
| CHEMBL4101737 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4091514 | — | IC50 | = | 1530.0 | nM | 5.82 |
| CHEMBL4076800 | — | IC50 | = | 2040.0 | nM | 5.69 |
| CHEMBL4092472 | — | IC50 | = | 5270.0 | nM | 5.28 |
| CHEMBL4099262 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL4060914 | — | IC50 | = | 16900.0 | nM | 4.77 |
| CHEMBL4074563 | — | IC50 | = | 19500.0 | nM | 4.71 |
| CHEMBL4072298 | — | IC50 | - | — | - | |
| CHEMBL4099250 | — | IC50 | - | — | - |