Assay Detail
Binding
CHEMBL4133560
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of AKR1C2 (unknown origin) using S-tetralol as substrate by by fluorimtery
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 C2 (CHEMBL5847) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Hydroxytriazole derivatives as potent and selective aldo-keto reductase 1C3 (AKR1C3) inhibitors discovered by bioisosteric scaffold hopping approach.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 4.69 | 6.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL23588 | FLUFENAMIC ACID | 2.0 | 1 | 6.28 |
| CHEMBL4166887 | — | — | 1 | 4.20 |
| CHEMBL4159654 | — | — | 1 | 4.15 |
| CHEMBL4174786 | — | — | 1 | 4.13 |
| CHEMBL4170286 | — | — | 1 | - |
| CHEMBL4163031 | — | — | 1 | - |
| CHEMBL4173733 | — | — | 1 | - |
| CHEMBL4166474 | — | — | 1 | - |
| CHEMBL4177097 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL23588 | FLUFENAMIC ACID | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL4166887 | — | IC50 | = | 62940.0 | nM | 4.20 |
| CHEMBL4159654 | — | IC50 | = | 70630.0 | nM | 4.15 |
| CHEMBL4174786 | — | IC50 | = | 73230.0 | nM | 4.13 |
| CHEMBL4170286 | — | IC50 | - | — | - | |
| CHEMBL4163031 | — | IC50 | - | — | - | |
| CHEMBL4173733 | — | IC50 | - | — | - | |
| CHEMBL4166474 | — | IC50 | - | — | - | |
| CHEMBL4177097 | — | IC50 | - | — | - |