Assay Detail
Binding
CHEMBL4428989
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant AKR1C2 using S-tetralol as substrate assessed as reduction in NADP+-dependent S-tetralol oxidation preincubated for 10 mins followed by protein addition by fluorometric assay
14
Total Activities
14
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
Discovery of (R)-2-(6-Methoxynaphthalen-2-yl)butanoic Acid as a Potent and Selective Aldo-keto Reductase 1C3 Inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 5.35 | 5.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL154 | NAPROXEN | 4.0 | 1 | 5.90 |
| CHEMBL1236131 | — | — | 1 | 5.87 |
| CHEMBL4551048 | — | — | 1 | 5.82 |
| CHEMBL4466610 | — | — | 1 | 5.76 |
| CHEMBL4446810 | — | — | 1 | 5.72 |
| CHEMBL4457933 | — | — | 1 | 5.62 |
| CHEMBL1618254 | — | — | 1 | 5.56 |
| CHEMBL4459662 | — | — | 1 | 5.52 |
| CHEMBL4437291 | — | — | 1 | 5.36 |
| CHEMBL4473378 | — | — | 1 | 5.20 |
| CHEMBL4437071 | — | — | 1 | 5.12 |
| CHEMBL1105 | 6-METHOXY-2-NAPHTHYLACETIC ACID | -1.0 | 1 | 4.72 |
| CHEMBL4447175 | — | — | 1 | 4.47 |
| CHEMBL4435662 | — | — | 1 | 4.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL154 | NAPROXEN | IC50 | = | 1260.0 | nM | 5.90 |
| CHEMBL1236131 | — | IC50 | = | 1350.0 | nM | 5.87 |
| CHEMBL4551048 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4466610 | — | IC50 | = | 1720.0 | nM | 5.76 |
| CHEMBL4446810 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL4457933 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL1618254 | — | IC50 | = | 2750.0 | nM | 5.56 |
| CHEMBL4459662 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL4437291 | — | IC50 | = | 4350.0 | nM | 5.36 |
| CHEMBL4473378 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL4437071 | — | IC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL1105 | 6-METHOXY-2-NAPHTHYLACETIC ACID | IC50 | = | 19040.0 | nM | 4.72 |
| CHEMBL4447175 | — | IC50 | = | 34000.0 | nM | 4.47 |
| CHEMBL4435662 | — | IC50 | = | 48100.0 | nM | 4.32 |