Assay Detail
Binding
CHEMBL2329815
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant AKR1C3-mediated NADP+-dependent oxidation of S-(+)-1,2,3,4-tetrahydro-1-naphthol
62
Total Activities
62
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
Development of potent and selective indomethacin analogues for the inhibition of AKR1C3 (Type 5 17β-hydroxysteroid dehydrogenase/prostaglandin F synthase) in castrate-resistant prostate cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 62 | 5.84 | 7.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2323508 | — | — | 1 | 7.05 |
| CHEMBL6 | INDOMETHACIN | 4.0 | 1 | 7.00 |
| CHEMBL2323472 | — | — | 1 | 6.92 |
| CHEMBL2323509 | — | — | 1 | 6.92 |
| CHEMBL2323507 | — | — | 1 | 6.89 |
| CHEMBL2323473 | — | — | 1 | 6.85 |
| CHEMBL2323522 | — | — | 1 | 6.80 |
| CHEMBL179587 | — | — | 1 | 6.80 |
| CHEMBL2323490 | — | — | 1 | 6.68 |
| CHEMBL178687 | — | — | 1 | 6.66 |
| CHEMBL2323476 | — | — | 1 | 6.60 |
| CHEMBL2323474 | — | — | 1 | 6.57 |
| CHEMBL2323523 | — | — | 1 | 6.55 |
| CHEMBL2323482 | — | — | 1 | 6.54 |
| CHEMBL2323510 | — | — | 1 | 6.54 |
| CHEMBL2323525 | — | — | 1 | 6.47 |
| CHEMBL2323511 | — | — | 1 | 6.47 |
| CHEMBL2323488 | — | — | 1 | 6.30 |
| CHEMBL178499 | — | — | 1 | 6.15 |
| CHEMBL2323481 | — | — | 1 | 6.13 |
| CHEMBL503179 | — | — | 1 | 6.02 |
| CHEMBL2323486 | — | — | 1 | 5.97 |
| CHEMBL2323502 | — | — | 1 | 5.96 |
| CHEMBL2323517 | — | — | 1 | 5.96 |
| CHEMBL2323492 | — | — | 1 | 5.92 |
| CHEMBL2323513 | — | — | 1 | 5.84 |
| CHEMBL2323504 | — | — | 1 | 5.71 |
| CHEMBL2323494 | — | — | 1 | 5.68 |
| CHEMBL2323497 | — | — | 1 | 5.68 |
| CHEMBL2172787 | — | — | 1 | 5.65 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2323508 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL6 | INDOMETHACIN | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL2323509 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL2323472 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL2323507 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL2323473 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL2323522 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL179587 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL2323490 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL178687 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL2323476 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL2323474 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL2323523 | — | IC50 | = | 279.0 | nM | 6.55 |
| CHEMBL2323510 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL2323482 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL2323525 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL2323511 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL2323488 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL178499 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL2323481 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL503179 | — | IC50 | = | 960.0 | nM | 6.02 |
| CHEMBL2323486 | — | IC50 | = | 1080.0 | nM | 5.97 |
| CHEMBL2323502 | — | IC50 | = | 1110.0 | nM | 5.96 |
| CHEMBL2323517 | — | IC50 | = | 1110.0 | nM | 5.96 |
| CHEMBL2323492 | — | IC50 | = | 1190.0 | nM | 5.92 |
| CHEMBL2323513 | — | IC50 | = | 1440.0 | nM | 5.84 |
| CHEMBL2323504 | — | IC50 | = | 1940.0 | nM | 5.71 |
| CHEMBL2323494 | — | IC50 | = | 2070.0 | nM | 5.68 |
| CHEMBL2323497 | — | IC50 | = | 2090.0 | nM | 5.68 |
| CHEMBL2172787 | — | IC50 | = | 2240.0 | nM | 5.65 |
| CHEMBL2323477 | — | IC50 | = | 2230.0 | nM | 5.65 |
| CHEMBL2323505 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL2323475 | — | IC50 | = | 2440.0 | nM | 5.61 |
| CHEMBL2323518 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL2323501 | — | IC50 | = | 2520.0 | nM | 5.60 |
| CHEMBL2323515 | — | IC50 | = | 2540.0 | nM | 5.59 |
| CHEMBL2323495 | — | IC50 | = | 2650.0 | nM | 5.58 |
| CHEMBL2323520 | — | IC50 | = | 2650.0 | nM | 5.58 |
| CHEMBL2323514 | — | IC50 | = | 3110.0 | nM | 5.51 |
| CHEMBL2323516 | — | IC50 | = | 3250.0 | nM | 5.49 |
| CHEMBL2323483 | — | IC50 | = | 3560.0 | nM | 5.45 |
| CHEMBL2323496 | — | IC50 | = | 3730.0 | nM | 5.43 |
| CHEMBL2323503 | — | IC50 | = | 3970.0 | nM | 5.40 |
| CHEMBL2323521 | — | IC50 | = | 4690.0 | nM | 5.33 |
| CHEMBL2323485 | — | IC50 | = | 4960.0 | nM | 5.30 |
| CHEMBL2323524 | — | IC50 | = | 5070.0 | nM | 5.29 |
| CHEMBL2323487 | — | IC50 | = | 5210.0 | nM | 5.28 |
| CHEMBL2323512 | — | IC50 | = | 5530.0 | nM | 5.26 |
| CHEMBL73572 | — | IC50 | = | 5670.0 | nM | 5.25 |
| CHEMBL2323499 | — | IC50 | = | 5800.0 | nM | 5.24 |