Assay Detail
Binding
CHEMBL3381103
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Modulation of BCRP1 mediated drug efflux in mitoxantrone-resistant human MES-SA cells assessed as accumulation of hoechst 33342 incubated for 15 mins prior to rhodamine-123 addition measured after 90 mins by fluorescence analysis
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MES-SA |
| 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
Thieno[2,3-b]pyridines--a new class of multidrug resistance (MDR) modulators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 27 | 5.82 | 6.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3342124 | — | — | 1 | 6.70 |
| CHEMBL3342113 | — | — | 1 | 6.40 |
| CHEMBL3342121 | — | — | 1 | 6.40 |
| CHEMBL3342127 | — | — | 1 | 6.22 |
| CHEMBL3344542 | — | — | 1 | 6.16 |
| CHEMBL3342117 | — | — | 1 | 6.16 |
| CHEMBL3342122 | — | — | 1 | 6.10 |
| CHEMBL3342123 | — | — | 1 | 5.89 |
| CHEMBL3342119 | — | — | 1 | 5.89 |
| CHEMBL3342116 | — | — | 1 | 5.82 |
| CHEMBL3342125 | — | — | 1 | 5.60 |
| CHEMBL3344541 | — | — | 1 | 5.58 |
| CHEMBL3342118 | — | — | 1 | 5.58 |
| CHEMBL3342128 | — | — | 1 | 5.52 |
| CHEMBL3342134 | — | — | 1 | 5.47 |
| CHEMBL3344543 | — | — | 1 | 5.44 |
| CHEMBL3342110 | — | — | 1 | 5.39 |
| CHEMBL6966 | VERAPAMIL | 4.0 | 1 | 4.43 |
| CHEMBL3342120 | — | — | 1 | - |
| CHEMBL3342112 | — | — | 1 | - |
| CHEMBL3342111 | — | — | 1 | - |
| CHEMBL3342126 | — | — | 1 | - |
| CHEMBL3342129 | — | — | 1 | - |
| CHEMBL3342130 | — | — | 1 | - |
| CHEMBL3342131 | — | — | 1 | - |
| CHEMBL3342133 | — | — | 1 | - |
| CHEMBL3342135 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3342124 | — | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3342113 | — | EC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3342121 | — | EC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3342127 | — | EC50 | = | 600.0 | nM | 6.22 |
| CHEMBL3344542 | — | EC50 | = | 700.0 | nM | 6.16 |
| CHEMBL3342117 | — | EC50 | = | 700.0 | nM | 6.16 |
| CHEMBL3342122 | — | EC50 | = | 800.0 | nM | 6.10 |
| CHEMBL3342123 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL3342119 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL3342116 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL3342125 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL3344541 | — | EC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL3342118 | — | EC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL3342128 | — | EC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL3342134 | — | EC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL3344543 | — | EC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL3342110 | — | EC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL6966 | VERAPAMIL | EC50 | = | 37300.0 | nM | 4.43 |
| CHEMBL3342120 | — | EC50 | - | — | - | |
| CHEMBL3342112 | — | EC50 | - | — | - | |
| CHEMBL3342111 | — | EC50 | - | — | - | |
| CHEMBL3342126 | — | EC50 | - | — | - | |
| CHEMBL3342129 | — | EC50 | - | — | - | |
| CHEMBL3342130 | — | EC50 | - | — | - | |
| CHEMBL3342131 | — | EC50 | - | — | - | |
| CHEMBL3342133 | — | EC50 | - | — | - | |
| CHEMBL3342135 | — | EC50 | - | — | - |