Assay Detail
Binding
CHEMBL1285646
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human wild type AKR1C1 dehydrogenase activity by fluorometric assay
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 C1 (CHEMBL5905) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structure-based optimization and biological evaluation of human 20α-hydroxysteroid dehydrogenase (AKR1C1) salicylic acid-based inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 8.14 | 9.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1275703 | — | — | 1 | 9.07 |
| CHEMBL1275704 | — | — | 1 | 8.89 |
| CHEMBL1275725 | — | — | 1 | 8.89 |
| CHEMBL1277648 | — | — | 1 | 8.70 |
| CHEMBL1277647 | — | — | 1 | 8.68 |
| CHEMBL1275723 | — | — | 1 | 8.59 |
| CHEMBL387536 | — | — | 1 | 8.39 |
| CHEMBL449129 | — | — | 1 | 8.23 |
| CHEMBL1277741 | — | — | 1 | 7.54 |
| CHEMBL1275724 | — | — | 1 | 7.19 |
| CHEMBL1277740 | — | — | 1 | 7.02 |
| CHEMBL1277646 | — | — | 1 | 6.47 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1275703 | — | Ki | = | 0.86 | nM | 9.07 |
| CHEMBL1275704 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL1275725 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL1277648 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL1277647 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL1275723 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL387536 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL449129 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL1277741 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL1275724 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL1277740 | — | Ki | = | 96.0 | nM | 7.02 |
| CHEMBL1277646 | — | Ki | = | 340.0 | nM | 6.47 |