Assay Detail
Functional
CHEMBL689133
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Competitive antagonism of GnRH-induced response in the reporter gene assay
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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 |
|---|---|---|---|
| Kd | 28 | 9.03 | 9.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL411565 | — | — | 1 | 9.50 |
| CHEMBL5314377 | GANIRELIX ACETATE | 4.0 | 1 | 9.30 |
| CHEMBL406337 | — | — | 1 | 9.30 |
| CHEMBL2370890 | — | — | 1 | 9.30 |
| CHEMBL412749 | — | — | 1 | 9.20 |
| CHEMBL268146 | — | — | 1 | 9.20 |
| CHEMBL415606 | DEGARELIX | 4.0 | 1 | 9.20 |
| CHEMBL412336 | — | — | 1 | 9.20 |
| CHEMBL438018 | — | — | 1 | 9.20 |
| CHEMBL266653 | — | — | 1 | 9.10 |
| CHEMBL414249 | — | — | 1 | 9.10 |
| CHEMBL219461 | — | — | 1 | 9.10 |
| CHEMBL1252 | ABARELIX | 4.0 | 1 | 9.10 |
| CHEMBL265286 | — | — | 1 | 9.00 |
| CHEMBL413698 | — | — | 1 | 9.00 |
| CHEMBL265556 | — | — | 1 | 9.00 |
| CHEMBL386105 | — | — | 1 | 9.00 |
| CHEMBL266728 | — | — | 1 | 9.00 |
| CHEMBL1200490 | CETRORELIX | 4.0 | 1 | 8.90 |
| CHEMBL267622 | — | — | 1 | 8.90 |
| CHEMBL269516 | — | — | 1 | 8.90 |
| CHEMBL268875 | — | — | 1 | 8.90 |
| CHEMBL444381 | — | — | 1 | 8.80 |
| CHEMBL2105773 | PRAZARELIX ACETATE | -1.0 | 1 | 8.80 |
| CHEMBL269711 | — | — | 1 | 8.80 |
| CHEMBL415573 | — | — | 1 | 8.80 |
| CHEMBL435322 | — | — | 1 | 8.70 |
| CHEMBL262747 | ACYLINE | 2.0 | 1 | 8.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL411565 | — | Kd | = | 0.3162 | nM | 9.50 |
| CHEMBL5314377 | GANIRELIX ACETATE | Kd | = | 0.5012 | nM | 9.30 |
| CHEMBL406337 | — | Kd | = | 0.5012 | nM | 9.30 |
| CHEMBL2370890 | — | Kd | = | 0.5012 | nM | 9.30 |
| CHEMBL412749 | — | Kd | = | 0.631 | nM | 9.20 |
| CHEMBL268146 | — | Kd | = | 0.631 | nM | 9.20 |
| CHEMBL415606 | DEGARELIX | Kd | = | 0.631 | nM | 9.20 |
| CHEMBL412336 | — | Kd | = | 0.631 | nM | 9.20 |
| CHEMBL438018 | — | Kd | = | 0.631 | nM | 9.20 |
| CHEMBL266653 | — | Kd | = | 0.7943 | nM | 9.10 |
| CHEMBL414249 | — | Kd | = | 0.7943 | nM | 9.10 |
| CHEMBL219461 | — | Kd | = | 0.7943 | nM | 9.10 |
| CHEMBL1252 | ABARELIX | Kd | = | 0.7943 | nM | 9.10 |
| CHEMBL265286 | — | Kd | = | 1.0 | nM | 9.00 |
| CHEMBL413698 | — | Kd | = | 1.0 | nM | 9.00 |
| CHEMBL265556 | — | Kd | = | 1.0 | nM | 9.00 |
| CHEMBL386105 | — | Kd | = | 1.0 | nM | 9.00 |
| CHEMBL266728 | — | Kd | = | 1.0 | nM | 9.00 |
| CHEMBL1200490 | CETRORELIX | Kd | = | 1.259 | nM | 8.90 |
| CHEMBL267622 | — | Kd | = | 1.259 | nM | 8.90 |
| CHEMBL269516 | — | Kd | = | 1.259 | nM | 8.90 |
| CHEMBL268875 | — | Kd | = | 1.259 | nM | 8.90 |
| CHEMBL444381 | — | Kd | = | 1.585 | nM | 8.80 |
| CHEMBL2105773 | PRAZARELIX ACETATE | Kd | = | 1.585 | nM | 8.80 |
| CHEMBL269711 | — | Kd | = | 1.585 | nM | 8.80 |
| CHEMBL415573 | — | Kd | = | 1.585 | nM | 8.80 |
| CHEMBL435322 | — | Kd | = | 1.995 | nM | 8.70 |
| CHEMBL262747 | ACYLINE | Kd | = | 2.512 | nM | 8.60 |