Assay Detail
Functional
CHEMBL5209618
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of the Organic Cation Transporter 3 (OCT3, SLC22A3) as assessed by a phenotypic impedance-based assay detecting changes in cell morphology by MPP+ uptake in HEK-293 JumpIN-SLC22A3 cells (PubChem AID: 1745861)
5
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Solute carrier family 22 member 3 (CHEMBL2073673) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
MPP+-Induced Changes in Cellular Impedance as a Measure for Organic Cation Transporter (SLC22A1-3) Activity and Inhibition
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 5.90 | 6.40 |
| EC50 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4129927 | — | — | 1 | 6.40 |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | 6.30 |
| CHEMBL110739 | CORTICOSTERONE | 3.0 | 1 | 5.80 |
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 5.10 |
| CHEMBL271379 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4129927 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL255863 | NILOTINIB | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL110739 | CORTICOSTERONE | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL271379 | — | EC50 | = | 199000.0 | nM | - |