Assay Detail
Binding
CHEMBL5122827
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human AKR1C3 transfected in Escherichia coli BL21 (DE) assessed as reduction in NADPH production using S-tetralol as substrate by fluorescence based analysis
12
Total Activities
12
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 C3 (CHEMBL4681) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
New aldo-keto reductase 1C3 (AKR1C3) inhibitors based on the hydroxytriazole scaffold.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 6.57 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5194388 | — | — | 1 | 7.16 |
| CHEMBL5172658 | — | — | 1 | 6.96 |
| CHEMBL5174744 | — | — | 1 | 6.72 |
| CHEMBL5204156 | — | — | 1 | 6.68 |
| CHEMBL5170149 | — | — | 1 | 6.66 |
| CHEMBL5170401 | — | — | 1 | 6.58 |
| CHEMBL5175151 | — | — | 1 | 6.57 |
| CHEMBL4174786 | — | — | 1 | 6.51 |
| CHEMBL5206583 | — | — | 1 | 6.51 |
| CHEMBL5191752 | — | — | 1 | 6.40 |
| CHEMBL5187723 | — | — | 1 | 6.33 |
| CHEMBL5183881 | — | — | 1 | 5.79 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5194388 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL5172658 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL5174744 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL5204156 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL5170149 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL5170401 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL5175151 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4174786 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL5206583 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL5191752 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL5187723 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL5183881 | — | IC50 | = | 1630.0 | nM | 5.79 |