Assay Detail
Binding
CHEMBL712499
Review assay metadata, readout intent, target linkage, and publication context from the same page.
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Gonadotropin-releasing hormone receptor (CHEMBL3066) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Discovery of a novel, potent, and orally active nonpeptide antagonist of the human luteinizing hormone-releasing hormone (LHRH) receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 7.41 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1201199 | LEUPROLIDE | 4.0 | 1 | 9.30 |
| CHEMBL1007 | GONADORELIN | 4.0 | 1 | 8.15 |
| CHEMBL544440 | — | — | 1 | 7.22 |
| CHEMBL435974 | — | — | 1 | 6.30 |
| CHEMBL135103 | — | — | 1 | 6.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1201199 | LEUPROLIDE | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL1007 | GONADORELIN | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL544440 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL435974 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL135103 | — | IC50 | = | 800.0 | nM | 6.10 |