Assay Detail
Binding
CHEMBL3108467
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of AKR1C3 (unknown origin) expressed in human HCT116 cells assessed as formation of PR-104H from PR-104A preincubated for 2 hrs
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HCT-116 |
| 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
Morpholylureas are a new class of potent and selective inhibitors of the type 5 17-β-hydroxysteroid dehydrogenase (AKR1C3).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.68 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3103330 | — | — | 1 | 8.52 |
| CHEMBL3103349 | — | — | 1 | 8.00 |
| CHEMBL3103348 | — | — | 1 | 7.92 |
| CHEMBL3103332 | — | — | 1 | 7.89 |
| CHEMBL3103331 | — | — | 1 | 7.89 |
| CHEMBL3103347 | — | — | 1 | 7.75 |
| CHEMBL3103346 | — | — | 1 | 7.66 |
| CHEMBL3103334 | — | — | 1 | 7.51 |
| CHEMBL3103323 | — | — | 1 | 7.23 |
| CHEMBL3103324 | — | — | 1 | 6.41 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3103330 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3103349 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3103348 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3103332 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3103331 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3103347 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3103346 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3103334 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL3103323 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL3103324 | — | IC50 | = | 390.0 | nM | 6.41 |