Assay Detail
Binding
CHEMBL5347181
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [1251][D-Trp6]-LH-RH from human GnRH-R expressed in Chem-1 cells incubated for 60 mins by liquid scintillation counting analysis
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Chem-1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Gonadotropin-releasing hormone receptor (CHEMBL1855) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of the thieno[2,3-d]pyrimidine-2,4-dione derivative 21a: A potent and orally bioavailable gonadotropin-releasing hormone receptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 9.50 | 9.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5419365 | — | — | 1 | 9.66 |
| CHEMBL5398152 | — | — | 1 | 9.64 |
| CHEMBL1800159 | RELUGOLIX | 4.0 | 1 | 9.60 |
| CHEMBL5434324 | — | — | 1 | 9.59 |
| CHEMBL5400302 | — | — | 1 | 9.59 |
| CHEMBL5433025 | — | — | 1 | 9.55 |
| CHEMBL5419489 | — | — | 1 | 9.49 |
| CHEMBL5425604 | — | — | 1 | 9.46 |
| CHEMBL5427278 | — | — | 1 | 9.42 |
| CHEMBL5413078 | — | — | 1 | 9.26 |
| CHEMBL5420128 | — | — | 1 | 9.24 |
| CHEMBL5407004 | — | — | 1 | - |
| CHEMBL5395542 | — | — | 1 | - |
| CHEMBL5409192 | — | — | 1 | - |
| CHEMBL5422863 | — | — | 1 | - |
| CHEMBL5403996 | — | — | 1 | - |
| CHEMBL5432553 | — | — | 1 | - |
| CHEMBL5404509 | — | — | 1 | - |
| CHEMBL5424526 | — | — | 1 | - |
| CHEMBL5414381 | — | — | 1 | - |
| CHEMBL5429424 | — | — | 1 | - |
| CHEMBL5416399 | — | — | 1 | - |
| CHEMBL5441000 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5419365 | — | IC50 | = | 0.22 | nM | 9.66 |
| CHEMBL5398152 | — | IC50 | = | 0.23 | nM | 9.64 |
| CHEMBL1800159 | RELUGOLIX | IC50 | = | 0.25 | nM | 9.60 |
| CHEMBL5434324 | — | IC50 | = | 0.26 | nM | 9.59 |
| CHEMBL5400302 | — | IC50 | = | 0.26 | nM | 9.59 |
| CHEMBL5433025 | — | IC50 | = | 0.28 | nM | 9.55 |
| CHEMBL5419489 | — | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL5425604 | — | IC50 | = | 0.35 | nM | 9.46 |
| CHEMBL5427278 | — | IC50 | = | 0.38 | nM | 9.42 |
| CHEMBL5413078 | — | IC50 | = | 0.55 | nM | 9.26 |
| CHEMBL5420128 | — | IC50 | = | 0.57 | nM | 9.24 |
| CHEMBL5407004 | — | IC50 | - | — | - | |
| CHEMBL5395542 | — | IC50 | - | — | - | |
| CHEMBL5409192 | — | IC50 | - | — | - | |
| CHEMBL5422863 | — | IC50 | - | — | - | |
| CHEMBL5403996 | — | IC50 | - | — | - | |
| CHEMBL5432553 | — | IC50 | - | — | - | |
| CHEMBL5404509 | — | IC50 | - | — | - | |
| CHEMBL5424526 | — | IC50 | - | — | - | |
| CHEMBL5414381 | — | IC50 | - | — | - | |
| CHEMBL5429424 | — | IC50 | - | — | - | |
| CHEMBL5416399 | — | IC50 | - | — | - | |
| CHEMBL5441000 | — | IC50 | - | — | - |