Assay Detail
Binding
CHEMBL4430166
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of AKR1C3 in human HL60 cells assessed as potentiation of etoposide-induced cytotoxicity by measuring etoposide IC50 pre-treated with compound for 24 hrs followed by etoposide exposure for additional 72 hrs by MTS assay (Rvb = 1.16 uM)
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Aldo-keto reductase family 1 member C3 (CHEMBL4681) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Selective AKR1C3 Inhibitors Potentiate Chemotherapeutic Activity in Multiple Acute Myeloid Leukemia (AML) Cell Lines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 6.63 | 6.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4441387 | — | — | 1 | 6.70 |
| CHEMBL4457540 | — | — | 1 | 6.68 |
| CHEMBL4470997 | — | — | 1 | 6.57 |
| CHEMBL511708 | BACCHARIN | — | 1 | 6.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4441387 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4457540 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4470997 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL511708 | BACCHARIN | IC50 | = | 280.0 | nM | 6.55 |