Assay Detail
Binding
CHEMBL709251
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 the cloned human Leutinizing releasing hormone receptor
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 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 | 6 | 8.05 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL544440 | — | — | 1 | 9.70 |
| CHEMBL1201199 | LEUPROLIDE | 4.0 | 1 | 9.52 |
| CHEMBL135103 | — | — | 1 | 8.22 |
| CHEMBL1007 | GONADORELIN | 4.0 | 1 | 8.00 |
| CHEMBL336319 | — | — | 1 | 7.16 |
| CHEMBL131751 | — | — | 1 | 5.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL544440 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL1201199 | LEUPROLIDE | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL135103 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1007 | GONADORELIN | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL336319 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL131751 | — | IC50 | = | 2000.0 | nM | 5.70 |