Assay Detail
Binding
CHEMBL3758022
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
13
Total Activities
7
Compounds Tested
2
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
Novel peptidomimetics related to gonadotropin-releasing hormone (GnRH)
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 6.83 | 9.54 |
| Activity | 6 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1201199 | LEUPROLIDE | 4.0 | 1 | 9.54 |
| CHEMBL4299455 | — | — | 2 | 6.72 |
| CHEMBL4299432 | — | — | 2 | 6.55 |
| CHEMBL4299453 | — | — | 2 | 6.39 |
| CHEMBL3753755 | — | — | 2 | 6.26 |
| CHEMBL3754384 | — | — | 2 | 6.23 |
| CHEMBL3754120 | — | — | 2 | 6.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1201199 | LEUPROLIDE | IC50 | = | 0.2884 | nM | 9.54 |
| CHEMBL4299455 | — | IC50 | = | 190.55 | nM | 6.72 |
| CHEMBL4299432 | — | IC50 | = | 281.84 | nM | 6.55 |
| CHEMBL4299453 | — | IC50 | = | 407.38 | nM | 6.39 |
| CHEMBL3753755 | — | IC50 | = | 549.54 | nM | 6.26 |
| CHEMBL3754384 | — | IC50 | = | 588.84 | nM | 6.23 |
| CHEMBL3754120 | — | IC50 | = | 724.44 | nM | 6.14 |
| CHEMBL3754384 | — | Activity | - | — | - | |
| CHEMBL3753755 | — | Activity | - | — | - | |
| CHEMBL3754120 | — | Activity | - | — | - | |
| CHEMBL4299455 | — | Activity | - | — | - | |
| CHEMBL4299432 | — | Activity | - | — | - | |
| CHEMBL4299453 | — | Activity | - | — | - |