Assay Detail
Functional
CHEMBL918449
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
22
Total Activities
22
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
Structure-activity relationship studies of gonadotropin-releasing hormone antagonists containing S-aryl/alkyl norcysteines and their oxidized derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 8.33 | 9.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL415659 | — | — | 1 | 9.51 |
| CHEMBL262747 | ACYLINE | 2.0 | 1 | 9.28 |
| CHEMBL387499 | — | — | 1 | 9.22 |
| CHEMBL227861 | — | — | 1 | 9.14 |
| CHEMBL427438 | — | — | 1 | 9.10 |
| CHEMBL227451 | — | — | 1 | 9.09 |
| CHEMBL434371 | — | — | 1 | 9.08 |
| CHEMBL389248 | — | — | 1 | 9.06 |
| CHEMBL388369 | — | — | 1 | 8.92 |
| CHEMBL441211 | — | — | 1 | 8.92 |
| CHEMBL2105773 | PRAZARELIX ACETATE | -1.0 | 1 | 8.87 |
| CHEMBL414344 | — | — | 1 | 8.66 |
| CHEMBL427269 | — | — | 1 | 8.52 |
| CHEMBL415432 | — | — | 1 | 8.34 |
| CHEMBL228197 | — | — | 1 | 8.21 |
| CHEMBL389945 | — | — | 1 | 8.16 |
| CHEMBL425486 | — | — | 1 | 7.89 |
| CHEMBL268297 | — | — | 1 | 7.60 |
| CHEMBL428795 | — | — | 1 | 7.41 |
| CHEMBL415380 | — | — | 1 | 7.07 |
| CHEMBL373725 | — | — | 1 | 5.70 |
| CHEMBL373724 | — | — | 1 | 5.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL415659 | — | IC50 | = | 0.31 | nM | 9.51 |
| CHEMBL262747 | ACYLINE | IC50 | = | 0.52 | nM | 9.28 |
| CHEMBL387499 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL227861 | — | IC50 | = | 0.73 | nM | 9.14 |
| CHEMBL427438 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL227451 | — | IC50 | = | 0.81 | nM | 9.09 |
| CHEMBL434371 | — | IC50 | = | 0.83 | nM | 9.08 |
| CHEMBL389248 | — | IC50 | = | 0.87 | nM | 9.06 |
| CHEMBL388369 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL441211 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL2105773 | PRAZARELIX ACETATE | IC50 | = | 1.36 | nM | 8.87 |
| CHEMBL414344 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL427269 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL415432 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL228197 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL389945 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL425486 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL268297 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL428795 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL415380 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL373725 | — | IC50 | = | 2004.0 | nM | 5.70 |
| CHEMBL373724 | — | IC50 | = | 3815.0 | nM | 5.42 |