Assay Detail
Binding
CHEMBL684199
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Gonadotropin-releasing hormone receptor (CHEMBL1855) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and initial structure-activity relationships of a novel series of imidazolo[1,2-a]pyrimid-5-ones as potent GnRH receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 6.85 | 8.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL419998 | — | — | 1 | 8.57 |
| CHEMBL302769 | — | — | 1 | 8.12 |
| CHEMBL71141 | — | — | 1 | 7.92 |
| CHEMBL306684 | — | — | 1 | 7.85 |
| CHEMBL71793 | — | — | 1 | 7.54 |
| CHEMBL303260 | — | — | 1 | 7.44 |
| CHEMBL273358 | — | — | 1 | 7.39 |
| CHEMBL304156 | — | — | 1 | 7.28 |
| CHEMBL67638 | — | — | 1 | 7.10 |
| CHEMBL70851 | — | — | 1 | 6.64 |
| CHEMBL308696 | — | — | 1 | 6.54 |
| CHEMBL70276 | — | — | 1 | 6.52 |
| CHEMBL68664 | — | — | 1 | 6.02 |
| CHEMBL69914 | — | — | 1 | 5.66 |
| CHEMBL68964 | — | — | 1 | 4.55 |
| CHEMBL262787 | — | — | 1 | 4.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL419998 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL302769 | — | Ki | = | 7.5 | nM | 8.12 |
| CHEMBL71141 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL306684 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL71793 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL303260 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL273358 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL304156 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL67638 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL70851 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL308696 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL70276 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL68664 | — | Ki | = | 950.0 | nM | 6.02 |
| CHEMBL69914 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL68964 | — | Ki | = | 28000.0 | nM | 4.55 |
| CHEMBL262787 | — | Ki | = | 30000.0 | nM | 4.52 |