Assay Detail
Binding
CHEMBL3875847
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human GFP-fused ABCG2 expressed in MDCK2 cells assessed as reduction in pheophorbide A efflux preincubated for 30 mins followed by pheophorbide A addition measured after 2 hrs by flow cytometry
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MDCK-II |
| 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
Phenyltetrazolyl-phenylamides: Substituent impact on modulation capability and selectivity toward the efflux protein ABCG2 and investigation of interaction with the transporter.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 6.57 | 7.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3884089 | — | — | 1 | 7.19 |
| CHEMBL3883513 | — | — | 1 | 7.01 |
| CHEMBL3885113 | — | — | 1 | 6.93 |
| CHEMBL3884853 | — | — | 1 | 6.91 |
| CHEMBL3883590 | — | — | 1 | 6.89 |
| CHEMBL3885031 | — | — | 1 | 6.88 |
| CHEMBL3883987 | — | — | 1 | 6.68 |
| CHEMBL3885018 | — | — | 1 | 6.67 |
| CHEMBL3884824 | — | — | 1 | 6.61 |
| CHEMBL3885364 | — | — | 1 | 6.60 |
| CHEMBL488910 | — | — | 1 | 6.56 |
| CHEMBL3885456 | — | — | 1 | 6.52 |
| CHEMBL3883387 | — | — | 1 | 6.51 |
| CHEMBL3885022 | — | — | 1 | 6.49 |
| CHEMBL3883389 | — | — | 1 | 6.34 |
| CHEMBL3885212 | — | — | 1 | 6.29 |
| CHEMBL3883929 | — | — | 1 | 6.17 |
| CHEMBL428402 | — | — | 1 | 6.13 |
| CHEMBL3884050 | — | — | 1 | 5.44 |
| CHEMBL3884305 | — | — | 1 | - |
| CHEMBL3884145 | — | — | 1 | - |
| CHEMBL3885424 | — | — | 1 | - |
| CHEMBL3884164 | — | — | 1 | - |
| CHEMBL3883933 | — | — | 1 | - |
| CHEMBL3885414 | — | — | 1 | - |
| CHEMBL3883221 | — | — | 1 | - |
| CHEMBL3885158 | — | — | 1 | - |
| CHEMBL3884827 | — | — | 1 | - |
| CHEMBL3883362 | — | — | 1 | - |
| CHEMBL3884587 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3884089 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL3883513 | — | IC50 | = | 96.6 | nM | 7.01 |
| CHEMBL3885113 | — | IC50 | = | 117.0 | nM | 6.93 |
| CHEMBL3884853 | — | IC50 | = | 123.0 | nM | 6.91 |
| CHEMBL3883590 | — | IC50 | = | 129.0 | nM | 6.89 |
| CHEMBL3885031 | — | IC50 | = | 131.0 | nM | 6.88 |
| CHEMBL3883987 | — | IC50 | = | 208.0 | nM | 6.68 |
| CHEMBL3885018 | — | IC50 | = | 212.0 | nM | 6.67 |
| CHEMBL3884824 | — | IC50 | = | 247.0 | nM | 6.61 |
| CHEMBL3885364 | — | IC50 | = | 251.0 | nM | 6.60 |
| CHEMBL488910 | — | IC50 | = | 276.0 | nM | 6.56 |
| CHEMBL3885456 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL3883387 | — | IC50 | = | 311.0 | nM | 6.51 |
| CHEMBL3885022 | — | IC50 | = | 321.0 | nM | 6.49 |
| CHEMBL3883389 | — | IC50 | = | 458.0 | nM | 6.34 |
| CHEMBL3885212 | — | IC50 | = | 511.0 | nM | 6.29 |
| CHEMBL3883929 | — | IC50 | = | 679.0 | nM | 6.17 |
| CHEMBL428402 | — | IC50 | = | 741.0 | nM | 6.13 |
| CHEMBL3884050 | — | IC50 | = | 3630.0 | nM | 5.44 |
| CHEMBL3884305 | — | IC50 | - | — | - | |
| CHEMBL3884145 | — | IC50 | - | — | - | |
| CHEMBL3885424 | — | IC50 | - | — | - | |
| CHEMBL3884164 | — | IC50 | - | — | - | |
| CHEMBL3883933 | — | IC50 | - | — | - | |
| CHEMBL3885414 | — | IC50 | - | — | - | |
| CHEMBL3883221 | — | IC50 | - | — | - | |
| CHEMBL3885158 | — | IC50 | - | — | - | |
| CHEMBL3884827 | — | IC50 | - | — | - | |
| CHEMBL3883362 | — | IC50 | - | — | - | |
| CHEMBL3884587 | — | IC50 | - | — | - | |
| CHEMBL3885198 | — | IC50 | - | — | - | |
| CHEMBL3885165 | — | IC50 | - | — | - |