Assay Detail
Binding
CHEMBL5520730
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of P-gp efflux in MDCKII-MDR1 cells using calcein-AM as substrate assessed as intracellular calcein fluorescence preincubated for 15 mins followed by substrate addition and measured by fluorescence based assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Canis lupus familiaris |
| Cell Type | MDCKII-MDR1 |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Hit-to-Lead Identification and Validation of a Triaromatic Pleuromutilin Antibiotic Candidate.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 4.57 | 5.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4744370 | — | — | 1 | 5.70 |
| CHEMBL5523552 | — | — | 1 | 5.16 |
| CHEMBL5560546 | — | — | 1 | 5.00 |
| CHEMBL4746064 | — | — | 1 | 4.44 |
| CHEMBL3291398 | LEFAMULIN | 4.0 | 1 | 4.37 |
| CHEMBL5559113 | — | — | 1 | 4.34 |
| CHEMBL5561773 | — | — | 1 | 4.33 |
| CHEMBL5560022 | — | — | 1 | 4.30 |
| CHEMBL5565180 | — | — | 1 | 4.09 |
| CHEMBL5559456 | — | — | 1 | 4.01 |
| CHEMBL5563824 | — | — | 1 | - |
| CHEMBL5555635 | — | — | 1 | - |
| CHEMBL5557915 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4744370 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5523552 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL5560546 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4746064 | — | IC50 | = | 36000.0 | nM | 4.44 |
| CHEMBL3291398 | LEFAMULIN | IC50 | = | 43000.0 | nM | 4.37 |
| CHEMBL5559113 | — | IC50 | = | 46000.0 | nM | 4.34 |
| CHEMBL5561773 | — | IC50 | = | 47000.0 | nM | 4.33 |
| CHEMBL5560022 | — | IC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL5565180 | — | IC50 | = | 81000.0 | nM | 4.09 |
| CHEMBL5559456 | — | IC50 | = | 98000.0 | nM | 4.01 |
| CHEMBL5563824 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5555635 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5557915 | — | IC50 | - | — | - |