Assay Detail
Binding
CHEMBL4430599
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity against human GnRH receptor expressed in HEK293 cells assessed as reduction in ERK1/2 phosphorylation pre-incubated for 5 mins before LHRH stimulation for 5 mins by chemiluminescence based assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Gonadotropin-releasing hormone receptor (CHEMBL1855) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of an Orally Bioavailable Gonadotropin-Releasing Hormone Receptor Antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 2 | 8.54 | 8.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4449332 | — | — | 1 | 8.54 |
| CHEMBL4593521 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4449332 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL4593521 | — | IC50 | - | — | - |