Assay Detail
Binding
CHEMBL4339431
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human AKR1C3 expressed in Escherichia coli BL21 (D3) using S-tetralol as substrate in presence of NADP+ by UV-spectrophotometric method
56
Total Activities
56
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 | 56 | 6.53 | 7.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4467043 | — | — | 1 | 7.22 |
| CHEMBL4470997 | — | — | 1 | 7.18 |
| CHEMBL4592947 | — | — | 1 | 7.16 |
| CHEMBL4473138 | — | — | 1 | 7.16 |
| CHEMBL4467986 | — | — | 1 | 7.16 |
| CHEMBL4459691 | — | — | 1 | 7.12 |
| CHEMBL4457830 | — | — | 1 | 7.09 |
| CHEMBL4457540 | — | — | 1 | 7.06 |
| CHEMBL4561928 | — | — | 1 | 7.05 |
| CHEMBL4581405 | — | — | 1 | 7.04 |
| CHEMBL4543354 | — | — | 1 | 7.03 |
| CHEMBL4442981 | — | — | 1 | 7.01 |
| CHEMBL4453512 | — | — | 1 | 7.01 |
| CHEMBL4538670 | — | — | 1 | 7.00 |
| CHEMBL511708 | BACCHARIN | — | 1 | 7.00 |
| CHEMBL4532211 | — | — | 1 | 6.96 |
| CHEMBL4547181 | — | — | 1 | 6.96 |
| CHEMBL4441187 | — | — | 1 | 6.96 |
| CHEMBL4545749 | — | — | 1 | 6.92 |
| CHEMBL4543333 | — | — | 1 | 6.90 |
| CHEMBL4467992 | — | — | 1 | 6.90 |
| CHEMBL4587755 | — | — | 1 | 6.89 |
| CHEMBL4460107 | — | — | 1 | 6.89 |
| CHEMBL4582279 | — | — | 1 | 6.88 |
| CHEMBL4574718 | — | — | 1 | 6.87 |
| CHEMBL4580471 | — | — | 1 | 6.87 |
| CHEMBL4526918 | — | — | 1 | 6.85 |
| CHEMBL4590593 | — | — | 1 | 6.81 |
| CHEMBL4568995 | — | — | 1 | 6.80 |
| CHEMBL4452028 | — | — | 1 | 6.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4467043 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4470997 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL4473138 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4467986 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4592947 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4459691 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL4457830 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL4457540 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL4561928 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL4581405 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL4543354 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL4442981 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL4453512 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL4538670 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL511708 | BACCHARIN | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4532211 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4441187 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4547181 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4545749 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4543333 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL4467992 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL4587755 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4460107 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4582279 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL4580471 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL4574718 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL4526918 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4590593 | — | IC50 | = | 156.0 | nM | 6.81 |
| CHEMBL4568995 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4452028 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4591479 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4516371 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4587420 | — | IC50 | = | 233.0 | nM | 6.63 |
| CHEMBL4577172 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL4579768 | — | IC50 | = | 273.0 | nM | 6.56 |
| CHEMBL4442107 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL4454121 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4547925 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL4472272 | — | IC50 | = | 348.0 | nM | 6.46 |
| CHEMBL4470281 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL4441387 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL2269701 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL4537068 | — | IC50 | = | 453.0 | nM | 6.34 |
| CHEMBL4581432 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL4468606 | — | IC50 | = | 866.0 | nM | 6.06 |
| CHEMBL4458176 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4551043 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4532171 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4551710 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4439627 | — | IC50 | = | 2300.0 | nM | 5.64 |