Assay Detail
Binding
CHEMBL4025650
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of CYP17 in Sprague-Dawley rat testes microsomes using 17-alpha hydroxyprogesterone as substrate and NADPH as cofactor pretreated for 5 mins followed by substrate and cofactor addition after 60 mins by LC/Ms analysis
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Testis |
| Subcellular | Microsomes |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Steroid 17-alpha-hydroxylase/17,20 lyase (CHEMBL4430) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Discovery of novel 1,2,3,4-tetrahydrobenzo[4, 5]thieno[2, 3-c]pyridine derivatives as potent and selective CYP17 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 6.99 | 7.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4059780 | — | — | 1 | 7.80 |
| CHEMBL4064141 | — | — | 1 | 7.68 |
| CHEMBL254328 | ABIRATERONE | 3.0 | 1 | 7.61 |
| CHEMBL4083609 | — | — | 1 | 7.55 |
| CHEMBL4101612 | — | — | 1 | 7.55 |
| CHEMBL4068802 | — | — | 1 | 7.53 |
| CHEMBL4063960 | — | — | 1 | 7.47 |
| CHEMBL4091726 | — | — | 1 | 7.25 |
| CHEMBL4083029 | — | — | 1 | 7.21 |
| CHEMBL4077026 | — | — | 1 | 7.12 |
| CHEMBL4101951 | — | — | 1 | 7.09 |
| CHEMBL4085705 | — | — | 1 | 6.94 |
| CHEMBL4083961 | — | — | 1 | 6.92 |
| CHEMBL4093882 | — | — | 1 | 6.64 |
| CHEMBL4072156 | — | — | 1 | 6.59 |
| CHEMBL4077854 | — | — | 1 | 6.59 |
| CHEMBL4090236 | — | — | 1 | 6.41 |
| CHEMBL4091391 | — | — | 1 | 6.35 |
| CHEMBL4063548 | — | — | 1 | 6.29 |
| CHEMBL4072550 | — | — | 1 | 6.27 |
| CHEMBL4099464 | — | — | 1 | 6.01 |
| CHEMBL4102114 | — | — | 1 | - |
| CHEMBL4078455 | — | — | 1 | - |
| CHEMBL4099128 | — | — | 1 | - |
| CHEMBL4074529 | — | — | 1 | - |
| CHEMBL4072728 | — | — | 1 | - |
| CHEMBL4096103 | — | — | 1 | - |
| CHEMBL4061151 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4059780 | — | IC50 | = | 15.8 | nM | 7.80 |
| CHEMBL4064141 | — | IC50 | = | 20.9 | nM | 7.68 |
| CHEMBL254328 | ABIRATERONE | IC50 | = | 24.7 | nM | 7.61 |
| CHEMBL4083609 | — | IC50 | = | 28.1 | nM | 7.55 |
| CHEMBL4101612 | — | IC50 | = | 28.1 | nM | 7.55 |
| CHEMBL4068802 | — | IC50 | = | 29.8 | nM | 7.53 |
| CHEMBL4063960 | — | IC50 | = | 33.9 | nM | 7.47 |
| CHEMBL4091726 | — | IC50 | = | 56.5 | nM | 7.25 |
| CHEMBL4083029 | — | IC50 | = | 61.1 | nM | 7.21 |
| CHEMBL4077026 | — | IC50 | = | 75.8 | nM | 7.12 |
| CHEMBL4101951 | — | IC50 | = | 80.59 | nM | 7.09 |
| CHEMBL4085705 | — | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL4083961 | — | IC50 | = | 120.6 | nM | 6.92 |
| CHEMBL4093882 | — | IC50 | = | 228.5 | nM | 6.64 |
| CHEMBL4072156 | — | IC50 | = | 257.1 | nM | 6.59 |
| CHEMBL4077854 | — | IC50 | = | 257.1 | nM | 6.59 |
| CHEMBL4090236 | — | IC50 | = | 389.8 | nM | 6.41 |
| CHEMBL4091391 | — | IC50 | = | 448.6 | nM | 6.35 |
| CHEMBL4063548 | — | IC50 | = | 516.9 | nM | 6.29 |
| CHEMBL4072550 | — | IC50 | = | 535.1 | nM | 6.27 |
| CHEMBL4099464 | — | IC50 | = | 979.8 | nM | 6.01 |
| CHEMBL4102114 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4078455 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4099128 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4074529 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4072728 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4096103 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4061151 | — | IC50 | > | 1000.0 | nM | - |