Assay Detail
Binding
CHEMBL5350504
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant AKR1C1 transfected in Escherichia coli BL21 (DE3) pLysS competent cells using S-tetralol as substrate assessed as inhibition of NADP+ dependent substrate oxidation incubated for 10 mins by fluorescence microplate reader assay
8
Total Activities
8
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
Development of Biaryl-Containing Aldo-Keto Reductase 1C3 (AKR1C3) Inhibitors for Reversing AKR1C3-Mediated Drug Resistance in Cancer Treatment.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 5.45 | 5.94 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5412756 | — | — | 1 | 5.94 |
| CHEMBL563 | FLURBIPROFEN | 4.0 | 1 | 5.69 |
| CHEMBL5421222 | — | — | 1 | 5.69 |
| CHEMBL5438441 | — | — | 1 | 5.53 |
| CHEMBL5436517 | — | — | 1 | 5.42 |
| CHEMBL5422070 | — | — | 1 | 5.36 |
| CHEMBL5398653 | — | — | 1 | 5.08 |
| CHEMBL5398973 | — | — | 1 | 4.87 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5412756 | — | IC50 | = | 1150.0 | nM | 5.94 |
| CHEMBL563 | FLURBIPROFEN | IC50 | = | 2050.0 | nM | 5.69 |
| CHEMBL5421222 | — | IC50 | = | 2060.0 | nM | 5.69 |
| CHEMBL5438441 | — | IC50 | = | 2930.0 | nM | 5.53 |
| CHEMBL5436517 | — | IC50 | = | 3840.0 | nM | 5.42 |
| CHEMBL5422070 | — | IC50 | = | 4360.0 | nM | 5.36 |
| CHEMBL5398653 | — | IC50 | = | 8320.0 | nM | 5.08 |
| CHEMBL5398973 | — | IC50 | = | 13460.0 | nM | 4.87 |