Assay Detail
Binding
CHEMBL2346183
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of AKR1C1 (unknown origin)
3
Total Activities
3
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 C1 (CHEMBL5905) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and structure-activity relationships for 1-(4-(piperidin-1-ylsulfonyl)phenyl)pyrrolidin-2-ones as novel non-carboxylate inhibitors of the aldo-keto reductase enzyme AKR1C3.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 5.50 | 5.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL23588 | FLUFENAMIC ACID | 2.0 | 1 | 5.58 |
| CHEMBL509 | MECLOFENAMIC ACID | 4.0 | 1 | 5.50 |
| CHEMBL686 | MEFENAMIC ACID | 4.0 | 1 | 5.41 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL23588 | FLUFENAMIC ACID | IC50 | = | 2640.0 | nM | 5.58 |
| CHEMBL509 | MECLOFENAMIC ACID | IC50 | = | 3160.0 | nM | 5.50 |
| CHEMBL686 | MEFENAMIC ACID | IC50 | = | 3910.0 | nM | 5.41 |