Assay Detail
Binding
CHEMBL710690
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Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in monkey (chinese hamster ovary (CHO) cells)
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cercopithecidae |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Gonadotropin-releasing hormone receptor (CHEMBL1855) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of a thieno[2,3-d]pyrimidine-2,4-dione bearing a p-methoxyureidophenyl moiety at the 6-position: a highly potent and orally bioavailable non-peptide antagonist for the human luteinizing hormone-releasing hormone receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 2 | 8.79 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL435167 | — | — | 1 | 9.52 |
| CHEMBL21126 | — | — | 1 | 8.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL435167 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL21126 | — | IC50 | = | 9.0 | nM | 8.05 |