Assay Detail
Binding
CHEMBL4685391
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Inhibition of sulfasalazine-stimulated ABCB1 ATPase activity (unknown origin) expressed in baculovirus infected Sf9 insect cells using ATP as substrate measured after 1 hr by colorimetric assay
9
Total Activities
9
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 |
|---|---|---|---|
| IC50 | 9 | 6.55 | 7.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4790452 | — | — | 1 | 7.03 |
| CHEMBL4764773 | — | — | 1 | 7.02 |
| CHEMBL2011282 | — | — | 1 | 6.71 |
| CHEMBL4534001 | — | — | 1 | 6.65 |
| CHEMBL488910 | — | — | 1 | 6.57 |
| CHEMBL502503 | — | — | 1 | 6.53 |
| CHEMBL2011288 | — | — | 1 | 6.13 |
| CHEMBL410316 | FUMITREMORGIN | — | 1 | 5.74 |
| CHEMBL348475 | TARIQUIDAR | 3.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4790452 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL4764773 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL2011282 | — | IC50 | = | 194.0 | nM | 6.71 |
| CHEMBL4534001 | — | IC50 | = | 226.0 | nM | 6.65 |
| CHEMBL488910 | — | IC50 | = | 271.0 | nM | 6.57 |
| CHEMBL502503 | — | IC50 | = | 294.0 | nM | 6.53 |
| CHEMBL2011288 | — | IC50 | = | 745.0 | nM | 6.13 |
| CHEMBL410316 | FUMITREMORGIN | IC50 | = | 1808.0 | nM | 5.74 |
| CHEMBL348475 | TARIQUIDAR | IC50 | >= | 1180.0 | nM | - |