Assay Detail
Binding
CHEMBL2175577
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant AKR1C2 assessed as 1-acenaphthenol oxidation by spectrophotometry
11
Total Activities
11
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 inhibitors of aldo-keto reductases AKR1C1 and AKR1C3 discovered by virtual screening of a fragment library.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 4.47 | 6.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL686 | MEFENAMIC ACID | 4.0 | 1 | 6.66 |
| CHEMBL2172255 | — | — | 1 | 4.74 |
| CHEMBL2172254 | — | — | 1 | 4.67 |
| CHEMBL1527416 | — | — | 1 | 4.48 |
| CHEMBL2172251 | — | — | 1 | 4.40 |
| CHEMBL1328030 | — | — | 1 | 4.24 |
| CHEMBL2172243 | — | — | 1 | 4.24 |
| CHEMBL1373742 | — | — | 1 | 4.05 |
| CHEMBL2172252 | — | — | 1 | 3.92 |
| CHEMBL1896308 | — | — | 1 | 3.92 |
| CHEMBL1414132 | — | — | 1 | 3.86 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL686 | MEFENAMIC ACID | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL2172255 | — | Ki | = | 18200.0 | nM | 4.74 |
| CHEMBL2172254 | — | Ki | = | 21300.0 | nM | 4.67 |
| CHEMBL1527416 | — | Ki | = | 33000.0 | nM | 4.48 |
| CHEMBL2172251 | — | Ki | = | 40000.0 | nM | 4.40 |
| CHEMBL1328030 | — | Ki | = | 57300.0 | nM | 4.24 |
| CHEMBL2172243 | — | Ki | = | 58000.0 | nM | 4.24 |
| CHEMBL1373742 | — | Ki | = | 90000.0 | nM | 4.05 |
| CHEMBL2172252 | — | Ki | = | 121000.0 | nM | 3.92 |
| CHEMBL1896308 | — | Ki | = | 119000.0 | nM | 3.92 |
| CHEMBL1414132 | — | Ki | = | 137000.0 | nM | 3.86 |