Assay Detail
Binding
CHEMBL4339469
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human AKR1C3 expressed in Escherichia coli BL21 measured after 1.5 hrs by TR-FRET assay
9
Total Activities
9
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
Potent and Highly Selective Aldo-Keto Reductase 1C3 (AKR1C3) Inhibitors Act as Chemotherapeutic Potentiators in Acute Myeloid Leukemia and T-Cell Acute Lymphoblastic Leukemia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.83 | 7.18 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4470997 | — | — | 1 | 7.18 |
| CHEMBL3103346 | — | — | 1 | 7.17 |
| CHEMBL4457540 | — | — | 1 | 7.06 |
| CHEMBL2333520 | — | — | 1 | 7.03 |
| CHEMBL511708 | BACCHARIN | — | 1 | 6.96 |
| CHEMBL4513510 | ASP-9521 | 1.0 | 1 | 6.92 |
| CHEMBL4238437 | — | — | 1 | 6.58 |
| CHEMBL4441387 | — | — | 1 | 6.49 |
| CHEMBL4439327 | — | — | 1 | 6.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4470997 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL3103346 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL4457540 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL2333520 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL511708 | BACCHARIN | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4513510 | ASP-9521 | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4238437 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL4441387 | — | IC50 | = | 326.0 | nM | 6.49 |
| CHEMBL4439327 | — | IC50 | = | 770.0 | nM | 6.11 |