Assay Detail
Binding
CHEMBL1687513
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Inhibition of AKR1C2 by fluorimetric method
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Aldo-keto reductase family 1 member C2 (CHEMBL5847) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of substituted 3-(phenylamino)benzoic acids as potent and selective inhibitors of type 5 17β-hydroxysteroid dehydrogenase (AKR1C3).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 5.12 | 6.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL23588 | FLUFENAMIC ACID | 2.0 | 1 | 6.43 |
| CHEMBL23832 | FENAMIC ACID | 1.0 | 1 | 6.36 |
| CHEMBL1682199 | 4-PHENYLAMINO BENZOIC ACID | — | 1 | 5.52 |
| CHEMBL1682200 | — | — | 1 | 5.47 |
| CHEMBL1682206 | — | — | 1 | 4.96 |
| CHEMBL1682198 | 3-PHENYLAMINO BENZOIC ACID | — | 1 | 4.89 |
| CHEMBL1682202 | — | — | 1 | 4.82 |
| CHEMBL1682204 | — | — | 1 | 4.75 |
| CHEMBL1682201 | — | — | 1 | 4.72 |
| CHEMBL1682203 | — | — | 1 | 4.72 |
| CHEMBL1682205 | — | — | 1 | 4.51 |
| CHEMBL1682207 | — | — | 1 | 4.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL23588 | FLUFENAMIC ACID | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL23832 | FENAMIC ACID | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL1682199 | 4-PHENYLAMINO BENZOIC ACID | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL1682200 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL1682206 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL1682198 | 3-PHENYLAMINO BENZOIC ACID | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL1682202 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL1682204 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL1682201 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL1682203 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL1682205 | — | IC50 | = | 31000.0 | nM | 4.51 |
| CHEMBL1682207 | — | IC50 | = | 56000.0 | nM | 4.25 |