Assay Detail
Binding
CHEMBL4430090
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant AKR1C2 (unknown origin) assessed as reduction in S-tetralol catalyzed oxidation in presence of NADPH by fluorescence assay
6
Total Activities
6
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 C2 (CHEMBL5847) ↗| 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 | 6 | 4.76 | 5.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL717 | MEDROXYPROGESTERONE ACETATE | 4.0 | 1 | 5.40 |
| CHEMBL4470997 | — | — | 1 | 5.10 |
| CHEMBL4457540 | — | — | 1 | 4.60 |
| CHEMBL4441387 | — | — | 1 | 4.40 |
| CHEMBL511708 | BACCHARIN | — | 1 | 4.30 |
| CHEMBL464997 | DRUPANIN | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL717 | MEDROXYPROGESTERONE ACETATE | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL4470997 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL4457540 | — | IC50 | = | 25118.86 | nM | 4.60 |
| CHEMBL4441387 | — | IC50 | = | 39810.72 | nM | 4.40 |
| CHEMBL511708 | BACCHARIN | IC50 | = | 50118.72 | nM | 4.30 |
| CHEMBL464997 | DRUPANIN | IC50 | = | 125892.54 | nM | - |