Assay Detail
Binding
CHEMBL4809447
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Reversal of BCRP-mediated multidrug resistance in MDCK-II cells assessed as potentiation of adriamycin-induced cytotoxicity at 5 uM by measuring adriamycin IC50 after 48 hrs by MTT assay
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Canis lupus familiaris |
| Cell Type | MDCK-II |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Structure-Based Discovery of Pyrimidine Aminobenzene Derivatives as Potent Oral Reversal Agents against P-gp- and BCRP-Mediated Multidrug Resistance.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 7.68 | 8.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4856923 | — | — | 1 | 8.28 |
| CHEMBL4856328 | — | — | 1 | 8.27 |
| CHEMBL4863127 | — | — | 1 | 8.06 |
| CHEMBL4866124 | — | — | 1 | 8.01 |
| CHEMBL4873838 | — | — | 1 | 8.00 |
| CHEMBL4863195 | — | — | 1 | 7.96 |
| CHEMBL4851447 | — | — | 1 | 7.96 |
| CHEMBL4855618 | — | — | 1 | 7.92 |
| CHEMBL4877841 | — | — | 1 | 7.92 |
| CHEMBL4858070 | — | — | 1 | 7.89 |
| CHEMBL4850619 | — | — | 1 | 7.87 |
| CHEMBL4875177 | — | — | 1 | 7.86 |
| CHEMBL4864633 | — | — | 1 | 7.85 |
| CHEMBL4856409 | — | — | 1 | 7.84 |
| CHEMBL4852415 | — | — | 1 | 7.79 |
| CHEMBL4876765 | — | — | 1 | 7.72 |
| CHEMBL4872789 | — | — | 1 | 7.72 |
| CHEMBL348475 | TARIQUIDAR | 3.0 | 1 | 7.69 |
| CHEMBL4871513 | — | — | 1 | 7.66 |
| CHEMBL4871023 | — | — | 1 | 7.64 |
| CHEMBL4863144 | — | — | 1 | 7.61 |
| CHEMBL4862676 | — | — | 1 | 7.58 |
| CHEMBL4862544 | — | — | 1 | 7.55 |
| CHEMBL488910 | — | — | 1 | 7.51 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 7.46 |
| CHEMBL4869653 | — | — | 1 | 7.42 |
| CHEMBL4864069 | — | — | 1 | 7.21 |
| CHEMBL6966 | VERAPAMIL | 4.0 | 1 | 6.69 |
| CHEMBL4852116 | — | — | 1 | 5.91 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4856923 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL4856328 | — | IC50 | = | 5.38 | nM | 8.27 |
| CHEMBL4863127 | — | IC50 | = | 8.73 | nM | 8.06 |
| CHEMBL4866124 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL4873838 | — | IC50 | = | 10.08 | nM | 8.00 |
| CHEMBL4863195 | — | IC50 | = | 11.09 | nM | 7.96 |
| CHEMBL4851447 | — | IC50 | = | 10.84 | nM | 7.96 |
| CHEMBL4855618 | — | IC50 | = | 11.93 | nM | 7.92 |
| CHEMBL4877841 | — | IC50 | = | 12.03 | nM | 7.92 |
| CHEMBL4858070 | — | IC50 | = | 13.01 | nM | 7.89 |
| CHEMBL4850619 | — | IC50 | = | 13.6 | nM | 7.87 |
| CHEMBL4875177 | — | IC50 | = | 13.89 | nM | 7.86 |
| CHEMBL4864633 | — | IC50 | = | 14.17 | nM | 7.85 |
| CHEMBL4856409 | — | IC50 | = | 14.31 | nM | 7.84 |
| CHEMBL4852415 | — | IC50 | = | 16.24 | nM | 7.79 |
| CHEMBL4876765 | — | IC50 | = | 18.83 | nM | 7.72 |
| CHEMBL4872789 | — | IC50 | = | 18.83 | nM | 7.72 |
| CHEMBL348475 | TARIQUIDAR | IC50 | = | 20.44 | nM | 7.69 |
| CHEMBL4871513 | — | IC50 | = | 22.02 | nM | 7.66 |
| CHEMBL4871023 | — | IC50 | = | 22.71 | nM | 7.64 |
| CHEMBL4863144 | — | IC50 | = | 24.67 | nM | 7.61 |
| CHEMBL4862676 | — | IC50 | = | 26.02 | nM | 7.58 |
| CHEMBL4862544 | — | IC50 | = | 28.06 | nM | 7.55 |
| CHEMBL488910 | — | IC50 | = | 31.11 | nM | 7.51 |
| CHEMBL941 | IMATINIB | IC50 | = | 34.93 | nM | 7.46 |
| CHEMBL4869653 | — | IC50 | = | 37.66 | nM | 7.42 |
| CHEMBL4864069 | — | IC50 | = | 62.22 | nM | 7.21 |
| CHEMBL6966 | VERAPAMIL | IC50 | = | 204.43 | nM | 6.69 |
| CHEMBL4852116 | — | IC50 | = | 1245.0 | nM | 5.91 |