Assay Detail
Binding
CHEMBL1804384
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]leuprorelin from monkey GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Macaca mulatta |
| Cell Type | CHO |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Discovery of 1-{4-[1-(2,6-difluorobenzyl)-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl]phenyl}-3-methoxyurea (TAK-385) as a potent, orally active, non-peptide antagonist of the human gonadotropin-releasing hormone receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 2 | 9.14 | 9.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1800159 | RELUGOLIX | 4.0 | 1 | 9.48 |
| CHEMBL22055 | SUFUGOLIX | 2.0 | 1 | 8.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1800159 | RELUGOLIX | IC50 | = | 0.33 | nM | 9.48 |
| CHEMBL22055 | SUFUGOLIX | IC50 | = | 1.6 | nM | 8.80 |