Assay Detail
Binding
CHEMBL4196462
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of C-terminal GFP-fused human ABCG2 expressed in MDCK2 cells preincubated for 30 mins followed by Hoechst 33342 addition and measured every 60 secs for 120 mins by Hoechst 33342 accumulation assay
35
Total Activities
35
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
Structure activity relationships, multidrug resistance reversal and selectivity of heteroarylphenyl ABCG2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 6.21 | 7.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4202709 | — | — | 1 | 7.21 |
| CHEMBL3884089 | — | — | 1 | 7.17 |
| CHEMBL4205898 | — | — | 1 | 7.11 |
| CHEMBL4210872 | — | — | 1 | 7.05 |
| CHEMBL4206410 | — | — | 1 | 6.99 |
| CHEMBL2170116 | — | — | 1 | 6.95 |
| CHEMBL4217602 | — | — | 1 | 6.89 |
| CHEMBL4205357 | — | — | 1 | 6.89 |
| CHEMBL4207943 | — | — | 1 | 6.75 |
| CHEMBL4204010 | — | — | 1 | 6.72 |
| CHEMBL488910 | — | — | 1 | 6.66 |
| CHEMBL4203060 | — | — | 1 | 6.64 |
| CHEMBL4203580 | — | — | 1 | 6.59 |
| CHEMBL4215260 | — | — | 1 | 6.57 |
| CHEMBL4202490 | — | — | 1 | 6.57 |
| CHEMBL4207415 | — | — | 1 | 6.54 |
| CHEMBL4214686 | — | — | 1 | 6.54 |
| CHEMBL4215789 | — | — | 1 | 6.46 |
| CHEMBL4214177 | — | — | 1 | 6.37 |
| CHEMBL4215827 | — | — | 1 | 6.36 |
| CHEMBL4212309 | — | — | 1 | 6.35 |
| CHEMBL4205396 | — | — | 1 | 6.25 |
| CHEMBL428402 | — | — | 1 | 6.15 |
| CHEMBL4210844 | — | — | 1 | 6.13 |
| CHEMBL4211389 | — | — | 1 | 6.12 |
| CHEMBL4209777 | — | — | 1 | 5.97 |
| CHEMBL4203097 | — | — | 1 | 5.63 |
| CHEMBL4217634 | — | — | 1 | 5.49 |
| CHEMBL4210290 | — | — | 1 | 5.16 |
| CHEMBL4213221 | — | — | 1 | 5.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4202709 | — | IC50 | = | 61.6 | nM | 7.21 |
| CHEMBL3884089 | — | IC50 | = | 66.9 | nM | 7.17 |
| CHEMBL4205898 | — | IC50 | = | 77.4 | nM | 7.11 |
| CHEMBL4210872 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL4206410 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL2170116 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL4217602 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4205357 | — | IC50 | = | 129.0 | nM | 6.89 |
| CHEMBL4207943 | — | IC50 | = | 176.0 | nM | 6.75 |
| CHEMBL4204010 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL488910 | — | IC50 | = | 221.0 | nM | 6.66 |
| CHEMBL4203060 | — | IC50 | = | 228.0 | nM | 6.64 |
| CHEMBL4203580 | — | IC50 | = | 259.0 | nM | 6.59 |
| CHEMBL4215260 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4202490 | — | IC50 | = | 267.0 | nM | 6.57 |
| CHEMBL4207415 | — | IC50 | = | 287.0 | nM | 6.54 |
| CHEMBL4214686 | — | IC50 | = | 287.0 | nM | 6.54 |
| CHEMBL4215789 | — | IC50 | = | 351.0 | nM | 6.46 |
| CHEMBL4214177 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL4215827 | — | IC50 | = | 438.0 | nM | 6.36 |
| CHEMBL4212309 | — | IC50 | = | 445.0 | nM | 6.35 |
| CHEMBL4205396 | — | IC50 | = | 565.0 | nM | 6.25 |
| CHEMBL428402 | — | IC50 | = | 704.0 | nM | 6.15 |
| CHEMBL4210844 | — | IC50 | = | 733.0 | nM | 6.13 |
| CHEMBL4211389 | — | IC50 | = | 766.0 | nM | 6.12 |
| CHEMBL4209777 | — | IC50 | = | 1060.0 | nM | 5.97 |
| CHEMBL4203097 | — | IC50 | = | 2360.0 | nM | 5.63 |
| CHEMBL4217634 | — | IC50 | = | 3230.0 | nM | 5.49 |
| CHEMBL4210290 | — | IC50 | = | 6910.0 | nM | 5.16 |
| CHEMBL4213221 | — | IC50 | = | 7670.0 | nM | 5.12 |
| CHEMBL4205927 | — | IC50 | = | 8340.0 | nM | 5.08 |
| CHEMBL4202725 | — | IC50 | = | 15300.0 | nM | 4.82 |
| CHEMBL4218158 | — | IC50 | = | 15800.0 | nM | 4.80 |
| CHEMBL4215290 | — | IC50 | = | 18500.0 | nM | 4.73 |
| CHEMBL4203623 | — | IC50 | = | 39800.0 | nM | 4.40 |