Assay Detail
Functional
CHEMBL684350
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | HEK293 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Gonadotropin-releasing hormone receptor (CHEMBL1855) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
GnRH antagonists: a new generation of long acting analogues incorporating p-ureido-phenylalanines at positions 5 and 6.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 8.19 | 8.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL269711 | — | — | 1 | 8.55 |
| CHEMBL435322 | — | — | 1 | 8.55 |
| CHEMBL444381 | — | — | 1 | 8.52 |
| CHEMBL2370890 | — | — | 1 | 8.48 |
| CHEMBL1252 | ABARELIX | 4.0 | 1 | 8.46 |
| CHEMBL5314377 | GANIRELIX ACETATE | 4.0 | 1 | 8.44 |
| CHEMBL1200490 | CETRORELIX | 4.0 | 1 | 8.38 |
| CHEMBL269516 | — | — | 1 | 8.37 |
| CHEMBL268875 | — | — | 1 | 8.30 |
| CHEMBL412749 | — | — | 1 | 8.26 |
| CHEMBL267622 | — | — | 1 | 8.25 |
| CHEMBL219461 | — | — | 1 | 8.24 |
| CHEMBL406337 | — | — | 1 | 8.21 |
| CHEMBL438018 | — | — | 1 | 8.19 |
| CHEMBL262747 | ACYLINE | 2.0 | 1 | 8.17 |
| CHEMBL2105773 | PRAZARELIX ACETATE | -1.0 | 1 | 8.16 |
| CHEMBL415573 | — | — | 1 | 8.15 |
| CHEMBL414061 | — | — | 1 | 8.14 |
| CHEMBL414266 | — | — | 1 | 8.11 |
| CHEMBL265286 | — | — | 1 | 8.11 |
| CHEMBL413698 | — | — | 1 | 8.11 |
| CHEMBL411565 | — | — | 1 | 8.10 |
| CHEMBL414249 | — | — | 1 | 8.10 |
| CHEMBL414715 | — | — | 1 | 8.09 |
| CHEMBL2370894 | — | — | 1 | 8.09 |
| CHEMBL266653 | — | — | 1 | 8.09 |
| CHEMBL266728 | — | — | 1 | 8.07 |
| CHEMBL412336 | — | — | 1 | 8.06 |
| CHEMBL415606 | DEGARELIX | 4.0 | 1 | 8.06 |
| CHEMBL219799 | — | — | 1 | 8.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL269711 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL435322 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL444381 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2370890 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL1252 | ABARELIX | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL5314377 | GANIRELIX ACETATE | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL1200490 | CETRORELIX | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL269516 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL268875 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL412749 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL267622 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL219461 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL406337 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL438018 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL262747 | ACYLINE | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL2105773 | PRAZARELIX ACETATE | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL415573 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL414061 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL414266 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL413698 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL265286 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL411565 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL414249 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL414715 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL2370894 | — | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL266653 | — | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL266728 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL412336 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL415606 | DEGARELIX | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL219799 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL268146 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL265556 | — | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL386105 | — | IC50 | = | 10.8 | nM | 7.97 |
| CHEMBL2369138 | — | IC50 | = | 10.8 | nM | 7.97 |
| CHEMBL410165 | — | IC50 | = | 10.7 | nM | 7.97 |
| CHEMBL435925 | — | IC50 | = | 13.0 | nM | 7.89 |