Assay Detail
Binding
CHEMBL3108471
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Inhibition of recombinant AKR1C3 (unknown origin) after 1 hr by competitive fluorescence assay
53
Total Activities
53
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
Morpholylureas are a new class of potent and selective inhibitors of the type 5 17-β-hydroxysteroid dehydrogenase (AKR1C3).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 53 | 6.00 | 7.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3103330 | — | — | 1 | 7.60 |
| CHEMBL3103349 | — | — | 1 | 7.17 |
| CHEMBL3103346 | — | — | 1 | 7.17 |
| CHEMBL3103334 | — | — | 1 | 7.00 |
| CHEMBL3103331 | — | — | 1 | 6.96 |
| CHEMBL3103347 | — | — | 1 | 6.96 |
| CHEMBL3103348 | — | — | 1 | 6.85 |
| CHEMBL3103332 | — | — | 1 | 6.80 |
| CHEMBL3103363 | — | — | 1 | 6.46 |
| CHEMBL3103335 | — | — | 1 | 6.46 |
| CHEMBL3103324 | — | — | 1 | 6.46 |
| CHEMBL3103362 | — | — | 1 | 6.44 |
| CHEMBL3103323 | — | — | 1 | 6.34 |
| CHEMBL3103336 | — | — | 1 | 6.32 |
| CHEMBL1418164 | — | — | 1 | 6.30 |
| CHEMBL3103333 | — | — | 1 | 6.28 |
| CHEMBL3103356 | — | — | 1 | 6.24 |
| CHEMBL3103345 | — | — | 1 | 6.18 |
| CHEMBL3103359 | — | — | 1 | 6.16 |
| CHEMBL3103358 | — | — | 1 | 5.64 |
| CHEMBL3103344 | — | — | 1 | 5.54 |
| CHEMBL3103328 | — | — | 1 | 5.43 |
| CHEMBL1545268 | — | — | 1 | 5.42 |
| CHEMBL3103365 | — | — | 1 | 5.31 |
| CHEMBL3103360 | — | — | 1 | 5.28 |
| CHEMBL3103355 | — | — | 1 | 5.26 |
| CHEMBL1447127 | — | — | 1 | 5.21 |
| CHEMBL3103341 | — | — | 1 | 5.04 |
| CHEMBL3103357 | — | — | 1 | 4.92 |
| CHEMBL3103340 | — | — | 1 | 4.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3103330 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3103349 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL3103346 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL3103334 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3103331 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3103347 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3103348 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3103332 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3103363 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL3103335 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL3103324 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL3103362 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL3103323 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL3103336 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL1418164 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL3103333 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL3103356 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL3103345 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL3103359 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL3103358 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL3103344 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL3103328 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL1545268 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL3103365 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL3103360 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL3103355 | — | IC50 | = | 5520.0 | nM | 5.26 |
| CHEMBL1447127 | — | IC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL3103341 | — | IC50 | = | 9100.0 | nM | 5.04 |
| CHEMBL3103357 | — | IC50 | = | 12100.0 | nM | 4.92 |
| CHEMBL3103340 | — | IC50 | = | 12600.0 | nM | 4.90 |
| CHEMBL1865699 | — | IC50 | = | 20300.0 | nM | 4.69 |
| CHEMBL3103322 | — | IC50 | = | 21900.0 | nM | 4.66 |
| CHEMBL3103327 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL3103354 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3103329 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3102863 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3103337 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3103338 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL1608134 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3103351 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3103339 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL1499626 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3103361 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3103342 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3103343 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3103320 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3103321 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3103325 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3103326 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3103364 | — | IC50 | > | 30000.0 | nM | - |