Assay Detail
Binding
CHEMBL4685389
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Activation of ABCB1 ATPase activity (unknown origin) expressed in baculovirus infected Sf9 insect cells using ATP as substrate measured after 1 hr by colorimetric assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Tariquidar-related triazoles as potent, selective and stable inhibitors of ABCG2 (BCRP).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 10 | 6.76 | 7.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4790452 | — | — | 1 | 7.28 |
| CHEMBL488910 | — | — | 1 | 7.16 |
| CHEMBL4764773 | — | — | 1 | 7.16 |
| CHEMBL502503 | — | — | 1 | 6.98 |
| CHEMBL4534001 | — | — | 1 | 6.87 |
| CHEMBL348475 | TARIQUIDAR | 3.0 | 1 | 6.68 |
| CHEMBL2011282 | — | — | 1 | 6.56 |
| CHEMBL4786467 | — | — | 1 | 6.49 |
| CHEMBL410316 | FUMITREMORGIN | — | 1 | 6.38 |
| CHEMBL421 | SULFASALAZINE | 4.0 | 1 | 6.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4790452 | — | EC50 | = | 52.0 | nM | 7.28 |
| CHEMBL488910 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4764773 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL502503 | — | EC50 | = | 105.0 | nM | 6.98 |
| CHEMBL4534001 | — | EC50 | = | 134.0 | nM | 6.87 |
| CHEMBL348475 | TARIQUIDAR | EC50 | = | 211.0 | nM | 6.68 |
| CHEMBL2011282 | — | EC50 | = | 274.0 | nM | 6.56 |
| CHEMBL4786467 | — | EC50 | = | 327.0 | nM | 6.49 |
| CHEMBL410316 | FUMITREMORGIN | EC50 | = | 412.0 | nM | 6.38 |
| CHEMBL421 | SULFASALAZINE | EC50 | = | 916.0 | nM | 6.04 |