Assay Detail
Binding
CHEMBL685310
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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
A novel synthesis of 2-arylpyrrolo[1,2-a]pyrimid-7-ones and their structure-activity relationships as potent GnRH receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 30 | 7.59 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL130558 | — | — | 1 | 8.96 |
| CHEMBL130126 | — | — | 1 | 8.92 |
| CHEMBL337919 | — | — | 1 | 8.68 |
| CHEMBL419998 | — | — | 1 | 8.57 |
| CHEMBL308910 | — | — | 1 | 8.55 |
| CHEMBL340156 | — | — | 1 | 8.48 |
| CHEMBL335647 | — | — | 1 | 8.42 |
| CHEMBL130400 | — | — | 1 | 8.40 |
| CHEMBL434995 | — | — | 1 | 8.24 |
| CHEMBL434423 | — | — | 1 | 8.04 |
| CHEMBL131182 | — | — | 1 | 8.00 |
| CHEMBL337748 | — | — | 1 | 7.85 |
| CHEMBL334537 | — | — | 1 | 7.85 |
| CHEMBL339468 | — | — | 1 | 7.77 |
| CHEMBL128810 | — | — | 1 | 7.68 |
| CHEMBL131127 | — | — | 1 | 7.50 |
| CHEMBL132616 | — | — | 1 | 7.38 |
| CHEMBL335610 | — | — | 1 | 7.36 |
| CHEMBL324375 | — | — | 1 | 7.26 |
| CHEMBL337865 | — | — | 1 | 7.21 |
| CHEMBL132338 | — | — | 1 | 7.19 |
| CHEMBL130487 | — | — | 1 | 7.00 |
| CHEMBL131942 | — | — | 1 | 6.89 |
| CHEMBL339273 | — | — | 1 | 6.81 |
| CHEMBL130513 | — | — | 1 | 6.72 |
| CHEMBL132339 | — | — | 1 | 6.57 |
| CHEMBL127502 | — | — | 1 | 6.40 |
| CHEMBL132392 | — | — | 1 | 6.36 |
| CHEMBL130195 | — | — | 1 | 6.35 |
| CHEMBL434621 | — | — | 1 | 6.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL130558 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL130126 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL337919 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL419998 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL308910 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL340156 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL335647 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL130400 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL434995 | — | Ki | = | 5.8 | nM | 8.24 |
| CHEMBL434423 | — | Ki | = | 9.2 | nM | 8.04 |
| CHEMBL131182 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL337748 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL334537 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL339468 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL128810 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL131127 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL132616 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL335610 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL324375 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL337865 | — | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL132338 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL130487 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL131942 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL339273 | — | Ki | = | 154.0 | nM | 6.81 |
| CHEMBL130513 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL132339 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL127502 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL132392 | — | Ki | = | 440.0 | nM | 6.36 |
| CHEMBL130195 | — | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL434621 | — | Ki | = | 630.0 | nM | 6.20 |