Assay Detail
Binding
CHEMBL4825989
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of P-gp (unknown origin) expressed in MCF7 cells assessed as increase in reversal of resistance to paclitaxel-induced cytotoxicity by measuring reduction in paclitaxel EC50 at 50 nM incubated for 72 hrs in presence of paclitaxel by SRB assay (Rvb = 11.5 nM)
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MCF7 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Encequidar, First-in-Class Intestine Specific P-glycoprotein Inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 18 | 8.08 | 8.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4861299 | — | — | 1 | 8.27 |
| CHEMBL4860865 | — | — | 1 | 8.19 |
| CHEMBL4878833 | — | — | 1 | 8.19 |
| CHEMBL4866156 | — | — | 1 | 8.13 |
| CHEMBL4855294 | — | — | 1 | 8.12 |
| CHEMBL4870741 | — | — | 1 | 8.11 |
| CHEMBL4594298 | ENCEQUIDAR | 3.0 | 1 | 8.10 |
| CHEMBL4873470 | — | — | 1 | 8.10 |
| CHEMBL4867678 | — | — | 1 | 8.09 |
| CHEMBL4860692 | — | — | 1 | 8.07 |
| CHEMBL4874866 | — | — | 1 | 8.05 |
| CHEMBL4869278 | — | — | 1 | 8.04 |
| CHEMBL4849203 | — | — | 1 | 8.04 |
| CHEMBL4874542 | — | — | 1 | 8.04 |
| CHEMBL4851476 | — | — | 1 | 7.99 |
| CHEMBL4852329 | — | — | 1 | 7.99 |
| CHEMBL4862931 | — | — | 1 | 7.99 |
| CHEMBL4862848 | — | — | 1 | 7.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4861299 | — | EC50 | = | 5.4 | nM | 8.27 |
| CHEMBL4860865 | — | EC50 | = | 6.5 | nM | 8.19 |
| CHEMBL4878833 | — | EC50 | = | 6.4 | nM | 8.19 |
| CHEMBL4866156 | — | EC50 | = | 7.4 | nM | 8.13 |
| CHEMBL4855294 | — | EC50 | = | 7.6 | nM | 8.12 |
| CHEMBL4870741 | — | EC50 | = | 7.7 | nM | 8.11 |
| CHEMBL4594298 | ENCEQUIDAR | EC50 | = | 7.9 | nM | 8.10 |
| CHEMBL4873470 | — | EC50 | = | 7.9 | nM | 8.10 |
| CHEMBL4867678 | — | EC50 | = | 8.1 | nM | 8.09 |
| CHEMBL4860692 | — | EC50 | = | 8.5 | nM | 8.07 |
| CHEMBL4874866 | — | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4869278 | — | EC50 | = | 9.1 | nM | 8.04 |
| CHEMBL4849203 | — | EC50 | = | 9.1 | nM | 8.04 |
| CHEMBL4874542 | — | EC50 | = | 9.1 | nM | 8.04 |
| CHEMBL4851476 | — | EC50 | = | 10.3 | nM | 7.99 |
| CHEMBL4852329 | — | EC50 | = | 10.3 | nM | 7.99 |
| CHEMBL4862931 | — | EC50 | = | 10.2 | nM | 7.99 |
| CHEMBL4862848 | — | EC50 | = | 12.1 | nM | 7.92 |