Assay Detail
Functional
CHEMBL831116
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptor
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Gonadotropin-releasing hormone receptor (CHEMBL1855) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Iterative approach to the discovery of novel degarelix analogues: substitutions at positions 3, 7, and 8. Part II.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 8.40 | 8.86 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL410967 | — | — | 1 | 8.86 |
| CHEMBL2105773 | PRAZARELIX ACETATE | -1.0 | 1 | 8.85 |
| CHEMBL265879 | — | — | 1 | 8.83 |
| CHEMBL405273 | — | — | 1 | 8.82 |
| CHEMBL428825 | — | — | 1 | 8.81 |
| CHEMBL414347 | — | — | 1 | 8.81 |
| CHEMBL413450 | — | — | 1 | 8.79 |
| CHEMBL415606 | DEGARELIX | 4.0 | 1 | 8.79 |
| CHEMBL264090 | — | — | 1 | 8.76 |
| CHEMBL415820 | — | — | 1 | 8.75 |
| CHEMBL267873 | — | — | 1 | 8.75 |
| CHEMBL415595 | — | — | 1 | 8.74 |
| CHEMBL412500 | — | — | 1 | 8.73 |
| CHEMBL265020 | — | — | 1 | 8.71 |
| CHEMBL2371821 | — | — | 1 | 8.70 |
| CHEMBL438905 | — | — | 1 | 8.70 |
| CHEMBL2371822 | — | — | 1 | 8.68 |
| CHEMBL402683 | — | — | 1 | 8.65 |
| CHEMBL414507 | — | — | 1 | 8.57 |
| CHEMBL437672 | — | — | 1 | 8.54 |
| CHEMBL415549 | — | — | 1 | 8.46 |
| CHEMBL414346 | — | — | 1 | 8.42 |
| CHEMBL406225 | — | — | 1 | 8.37 |
| CHEMBL266444 | — | — | 1 | 8.28 |
| CHEMBL404973 | — | — | 1 | 8.26 |
| CHEMBL429378 | — | — | 1 | 8.04 |
| CHEMBL263507 | — | — | 1 | 7.97 |
| CHEMBL415813 | — | — | 1 | 7.87 |
| CHEMBL415328 | — | — | 1 | 7.65 |
| CHEMBL268829 | — | — | 1 | 7.59 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL410967 | — | IC50 | = | 1.38 | nM | 8.86 |
| CHEMBL2105773 | PRAZARELIX ACETATE | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL265879 | — | IC50 | = | 1.47 | nM | 8.83 |
| CHEMBL405273 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL428825 | — | IC50 | = | 1.54 | nM | 8.81 |
| CHEMBL414347 | — | IC50 | = | 1.56 | nM | 8.81 |
| CHEMBL413450 | — | IC50 | = | 1.62 | nM | 8.79 |
| CHEMBL415606 | DEGARELIX | IC50 | = | 1.64 | nM | 8.79 |
| CHEMBL264090 | — | IC50 | = | 1.72 | nM | 8.76 |
| CHEMBL415820 | — | IC50 | = | 1.77 | nM | 8.75 |
| CHEMBL267873 | — | IC50 | = | 1.77 | nM | 8.75 |
| CHEMBL415595 | — | IC50 | = | 1.83 | nM | 8.74 |
| CHEMBL412500 | — | IC50 | = | 1.85 | nM | 8.73 |
| CHEMBL265020 | — | IC50 | = | 1.97 | nM | 8.71 |
| CHEMBL438905 | — | IC50 | = | 1.98 | nM | 8.70 |
| CHEMBL2371821 | — | IC50 | = | 2.01 | nM | 8.70 |
| CHEMBL2371822 | — | IC50 | = | 2.11 | nM | 8.68 |
| CHEMBL402683 | — | IC50 | = | 2.24 | nM | 8.65 |
| CHEMBL414507 | — | IC50 | = | 2.71 | nM | 8.57 |
| CHEMBL437672 | — | IC50 | = | 2.85 | nM | 8.54 |
| CHEMBL415549 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL414346 | — | IC50 | = | 3.79 | nM | 8.42 |
| CHEMBL406225 | — | IC50 | = | 4.25 | nM | 8.37 |
| CHEMBL266444 | — | IC50 | = | 5.31 | nM | 8.28 |
| CHEMBL404973 | — | IC50 | = | 5.52 | nM | 8.26 |
| CHEMBL429378 | — | IC50 | = | 9.18 | nM | 8.04 |
| CHEMBL263507 | — | IC50 | = | 10.64 | nM | 7.97 |
| CHEMBL415813 | — | IC50 | = | 13.47 | nM | 7.87 |
| CHEMBL415328 | — | IC50 | = | 22.58 | nM | 7.65 |
| CHEMBL268829 | — | IC50 | = | 25.79 | nM | 7.59 |
| CHEMBL406535 | — | IC50 | = | 48.91 | nM | 7.31 |
| CHEMBL266893 | — | IC50 | = | 52.24 | nM | 7.28 |
| CHEMBL412212 | — | IC50 | = | 178.19 | nM | 6.75 |