Assay Detail
Binding
CHEMBL1687512
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Inhibition of AKR1C3 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 C3 (CHEMBL4681) ↗| 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 | 6.62 | 7.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1682200 | — | — | 1 | 7.44 |
| CHEMBL23588 | FLUFENAMIC ACID | 2.0 | 1 | 7.29 |
| CHEMBL1682201 | — | — | 1 | 7.27 |
| CHEMBL1682202 | — | — | 1 | 7.21 |
| CHEMBL1682204 | — | — | 1 | 6.92 |
| CHEMBL1682203 | — | — | 1 | 6.89 |
| CHEMBL1682205 | — | — | 1 | 6.55 |
| CHEMBL1682206 | — | — | 1 | 6.31 |
| CHEMBL1682207 | — | — | 1 | 6.16 |
| CHEMBL1682198 | 3-PHENYLAMINO BENZOIC ACID | — | 1 | 6.03 |
| CHEMBL23832 | FENAMIC ACID | 1.0 | 1 | 5.82 |
| CHEMBL1682199 | 4-PHENYLAMINO BENZOIC ACID | — | 1 | 5.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1682200 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL23588 | FLUFENAMIC ACID | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL1682201 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL1682202 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL1682204 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL1682203 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL1682205 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL1682206 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL1682207 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL1682198 | 3-PHENYLAMINO BENZOIC ACID | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL23832 | FENAMIC ACID | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL1682199 | 4-PHENYLAMINO BENZOIC ACID | IC50 | = | 2800.0 | nM | 5.55 |