Assay Detail
Binding
CHEMBL4668531
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human AKR1C3 expressed in Escherichia coli incubated for 30 mins in presence of NADPH regeneration system by UHPLC analysis
6
Total Activities
4
Compounds Tested
2
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
Overview of AKR1C3: Inhibitor Achievements and Disease Insights.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 5.29 | 5.67 |
| Ki | 3 | 6.09 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2103840 | DINACICLIB | 3.0 | 1 | 7.16 |
| CHEMBL52387 | (RS)-ROSCOVITINE | — | 2 | 5.85 |
| CHEMBL103579 | — | — | 2 | 5.26 |
| CHEMBL2017974 | BUPARLISIB | 3.0 | 1 | 5.02 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2103840 | DINACICLIB | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL52387 | (RS)-ROSCOVITINE | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL52387 | (RS)-ROSCOVITINE | IC50 | = | 2150.0 | nM | 5.67 |
| CHEMBL103579 | — | Ki | = | 5500.0 | nM | 5.26 |
| CHEMBL103579 | — | IC50 | = | 6580.0 | nM | 5.18 |
| CHEMBL2017974 | BUPARLISIB | IC50 | = | 9500.0 | nM | 5.02 |