Assay Detail
Binding
CHEMBL3631241
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human placental microsomal 17beta HSD2 using unlabeled- and labelled [2,4,6,7-3H]-E2 as substrate incubated for 20 mins by HPLC analysis
37
Total Activities
37
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
17-beta-hydroxysteroid dehydrogenase type 2 (CHEMBL2789) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Towards the evaluation in an animal disease model: Fluorinated 17β-HSD1 inhibitors showing strong activity towards both the human and the rat enzyme.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 37 | 7.06 | 8.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3629589 | — | — | 1 | 8.57 |
| CHEMBL3629588 | — | — | 1 | 8.43 |
| CHEMBL3629587 | — | — | 1 | 8.22 |
| CHEMBL3629590 | — | — | 1 | 8.19 |
| CHEMBL3629591 | — | — | 1 | 8.10 |
| CHEMBL3629586 | — | — | 1 | 7.89 |
| CHEMBL3629585 | — | — | 1 | 7.77 |
| CHEMBL3629592 | — | — | 1 | 7.70 |
| CHEMBL3629584 | — | — | 1 | 7.60 |
| CHEMBL3629452 | — | — | 1 | 7.08 |
| CHEMBL3629442 | — | — | 1 | 7.06 |
| CHEMBL3629581 | — | — | 1 | 7.00 |
| CHEMBL3629458 | — | — | 1 | 6.98 |
| CHEMBL3629438 | — | — | 1 | 6.95 |
| CHEMBL3629582 | — | — | 1 | 6.95 |
| CHEMBL3629441 | — | — | 1 | 6.94 |
| CHEMBL3629450 | — | — | 1 | 6.94 |
| CHEMBL3629435 | — | — | 1 | 6.92 |
| CHEMBL3629455 | — | — | 1 | 6.90 |
| CHEMBL3629456 | — | — | 1 | 6.89 |
| CHEMBL3629447 | — | — | 1 | 6.89 |
| CHEMBL3629454 | — | — | 1 | 6.84 |
| CHEMBL3629446 | — | — | 1 | 6.83 |
| CHEMBL3629443 | — | — | 1 | 6.80 |
| CHEMBL3629453 | — | — | 1 | 6.79 |
| CHEMBL3629440 | — | — | 1 | 6.77 |
| CHEMBL3629451 | — | — | 1 | 6.73 |
| CHEMBL3629439 | — | — | 1 | 6.70 |
| CHEMBL3629583 | — | — | 1 | 6.67 |
| CHEMBL3629444 | — | — | 1 | 6.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3629589 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL3629588 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL3629587 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3629590 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL3629591 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3629586 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3629585 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3629592 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3629584 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3629452 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL3629442 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL3629581 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL3629458 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL3629438 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL3629582 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL3629441 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL3629450 | — | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL3629435 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3629455 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL3629447 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3629456 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3629454 | — | IC50 | = | 144.0 | nM | 6.84 |
| CHEMBL3629446 | — | IC50 | = | 148.0 | nM | 6.83 |
| CHEMBL3629443 | — | IC50 | = | 159.0 | nM | 6.80 |
| CHEMBL3629453 | — | IC50 | = | 162.0 | nM | 6.79 |
| CHEMBL3629440 | — | IC50 | = | 171.0 | nM | 6.77 |
| CHEMBL3629451 | — | IC50 | = | 185.0 | nM | 6.73 |
| CHEMBL3629439 | — | IC50 | = | 199.0 | nM | 6.70 |
| CHEMBL3629583 | — | IC50 | = | 215.0 | nM | 6.67 |
| CHEMBL3629444 | — | IC50 | = | 218.0 | nM | 6.66 |
| CHEMBL3629457 | — | IC50 | = | 282.0 | nM | 6.55 |
| CHEMBL3629448 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL3629449 | — | IC50 | = | 322.0 | nM | 6.49 |
| CHEMBL3629445 | — | IC50 | = | 392.0 | nM | 6.41 |
| CHEMBL3629436 | — | IC50 | = | 459.0 | nM | 6.34 |
| CHEMBL3627738 | — | IC50 | = | 716.0 | nM | 6.14 |
| CHEMBL3629437 | — | IC50 | = | 763.0 | nM | 6.12 |