Assay Detail
Binding
CHEMBL680410
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Gonadotropin-releasing hormone receptor (CHEMBL3066) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Design and synthesis of potent hexapeptide and heptapeptide gonadotropin-releasing hormone antagonists by truncation of a decapeptide analogue sequence.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 7.19 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1007 | GONADORELIN | 4.0 | 1 | 8.70 |
| CHEMBL97265 | — | — | 1 | 8.15 |
| CHEMBL2370265 | — | — | 1 | 7.96 |
| CHEMBL262190 | — | — | 1 | 7.85 |
| CHEMBL97540 | — | — | 1 | 7.80 |
| CHEMBL268720 | — | — | 1 | 7.77 |
| CHEMBL96693 | — | — | 1 | 7.70 |
| CHEMBL2370263 | — | — | 1 | 7.64 |
| CHEMBL264501 | — | — | 1 | 7.60 |
| CHEMBL405176 | — | — | 1 | 7.55 |
| CHEMBL385022 | — | — | 1 | 7.55 |
| CHEMBL428186 | — | — | 1 | 7.51 |
| CHEMBL267986 | — | — | 1 | 7.42 |
| CHEMBL406243 | — | — | 1 | 7.38 |
| CHEMBL327359 | — | — | 1 | 7.35 |
| CHEMBL94842 | — | — | 1 | 7.16 |
| CHEMBL2370256 | — | — | 1 | 7.14 |
| CHEMBL428619 | — | — | 1 | 7.13 |
| CHEMBL261927 | — | — | 1 | 7.09 |
| CHEMBL2370262 | — | — | 1 | 7.06 |
| CHEMBL409218 | — | — | 1 | 6.96 |
| CHEMBL329807 | — | — | 1 | 6.89 |
| CHEMBL408737 | — | — | 1 | 6.89 |
| CHEMBL262292 | — | — | 1 | 6.85 |
| CHEMBL265010 | — | — | 1 | 6.64 |
| CHEMBL93608 | — | — | 1 | 6.55 |
| CHEMBL330173 | — | — | 1 | 6.43 |
| CHEMBL410269 | — | — | 1 | 6.35 |
| CHEMBL318127 | — | — | 1 | 6.26 |
| CHEMBL264526 | — | — | 1 | 5.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1007 | GONADORELIN | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL97265 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL2370265 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL262190 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL97540 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL268720 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL96693 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2370263 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL264501 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL405176 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL385022 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL428186 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL267986 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL406243 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL327359 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL94842 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL2370256 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL428619 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL261927 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL2370262 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL409218 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL329807 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL408737 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL262292 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL265010 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL93608 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL330173 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL410269 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL318127 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL264526 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL409979 | — | IC50 | = | 2200.0 | nM | 5.66 |