Assay Detail
Binding
CHEMBL3995155
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human placental microsomal 17beta-HSD2 using [2,4,6,7-3H]-E2 as substrate after 20 mins in presence of NAD+ by RP-HPLC method
32
Total Activities
32
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
Treatment of estrogen-dependent diseases: Design, synthesis and profiling of a selective 17β-HSD1 inhibitor with sub-nanomolar IC50 for a proof-of-principle study.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 7.51 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4092593 | — | — | 1 | 8.85 |
| CHEMBL4063985 | — | — | 1 | 8.19 |
| CHEMBL4101264 | — | — | 1 | 8.15 |
| CHEMBL4103524 | — | — | 1 | 8.14 |
| CHEMBL4082298 | — | — | 1 | 8.05 |
| CHEMBL4080385 | — | — | 1 | 8.05 |
| CHEMBL4099360 | — | — | 1 | 8.00 |
| CHEMBL4060257 | — | — | 1 | 7.96 |
| CHEMBL4062959 | — | — | 1 | 7.96 |
| CHEMBL4077264 | — | — | 1 | 7.75 |
| CHEMBL4073469 | — | — | 1 | 7.72 |
| CHEMBL4063839 | — | — | 1 | 7.70 |
| CHEMBL4062685 | — | — | 1 | 7.68 |
| CHEMBL4077041 | — | — | 1 | 7.58 |
| CHEMBL4091053 | — | — | 1 | 7.58 |
| CHEMBL4088861 | — | — | 1 | 7.54 |
| CHEMBL4061631 | — | — | 1 | 7.54 |
| CHEMBL4083849 | — | — | 1 | 7.46 |
| CHEMBL4072426 | — | — | 1 | 7.42 |
| CHEMBL4091749 | — | — | 1 | 7.41 |
| CHEMBL4091622 | — | — | 1 | 7.41 |
| CHEMBL4079675 | — | — | 1 | 7.39 |
| CHEMBL4101849 | — | — | 1 | 7.33 |
| CHEMBL4071808 | — | — | 1 | 7.26 |
| CHEMBL4071588 | — | — | 1 | 7.15 |
| CHEMBL4067584 | — | — | 1 | 7.07 |
| CHEMBL4094112 | — | — | 1 | 7.07 |
| CHEMBL4084832 | — | — | 1 | 6.85 |
| CHEMBL4095004 | — | — | 1 | 6.75 |
| CHEMBL4089862 | — | — | 1 | 6.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4092593 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL4063985 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL4101264 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4103524 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL4082298 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4080385 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4099360 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4060257 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4062959 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4077264 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4073469 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4063839 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4062685 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4077041 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4091053 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4061631 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4088861 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4083849 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4072426 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL4091749 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4091622 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4079675 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL4101849 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL4071808 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL4071588 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL4067584 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL4094112 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL4084832 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4095004 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4089862 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4104610 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4083262 | — | IC50 | = | 540.0 | nM | 6.27 |