Assay Detail
Binding
CHEMBL689128
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
23
Total Activities
23
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
Design, synthesis and structure-activity relationships of novel imidazolo[1,2-a]pyrimid-5-ones as potent GnRH receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 6.84 | 8.34 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL297491 | — | — | 1 | 8.34 |
| CHEMBL302769 | — | — | 1 | 8.12 |
| CHEMBL304308 | — | — | 1 | 7.96 |
| CHEMBL432922 | — | — | 1 | 7.75 |
| CHEMBL306431 | — | — | 1 | 7.33 |
| CHEMBL303621 | — | — | 1 | 7.25 |
| CHEMBL71400 | — | — | 1 | 7.19 |
| CHEMBL305034 | — | — | 1 | 7.17 |
| CHEMBL69361 | — | — | 1 | 7.10 |
| CHEMBL304548 | — | — | 1 | 7.00 |
| CHEMBL68753 | — | — | 1 | 6.96 |
| CHEMBL68988 | — | — | 1 | 6.96 |
| CHEMBL67370 | — | — | 1 | 6.89 |
| CHEMBL67820 | — | — | 1 | 6.85 |
| CHEMBL66808 | — | — | 1 | 6.82 |
| CHEMBL68625 | — | — | 1 | 6.66 |
| CHEMBL308446 | — | — | 1 | 6.64 |
| CHEMBL68698 | — | — | 1 | 6.43 |
| CHEMBL68985 | — | — | 1 | 5.85 |
| CHEMBL68537 | — | — | 1 | 5.60 |
| CHEMBL304067 | — | — | 1 | 5.02 |
| CHEMBL304950 | — | — | 1 | 4.55 |
| CHEMBL20596 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL297491 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL302769 | — | Ki | = | 7.5 | nM | 8.12 |
| CHEMBL304308 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL432922 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL306431 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL303621 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL71400 | — | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL305034 | — | Ki | = | 67.0 | nM | 7.17 |
| CHEMBL69361 | — | Ki | = | 79.0 | nM | 7.10 |
| CHEMBL304548 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL68753 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL68988 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL67370 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL67820 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL66808 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL68625 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL308446 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL68698 | — | Ki | = | 370.0 | nM | 6.43 |
| CHEMBL68985 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL68537 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL304067 | — | Ki | = | 9500.0 | nM | 5.02 |
| CHEMBL304950 | — | Ki | = | 28000.0 | nM | 4.55 |
| CHEMBL20596 | — | Ki | - | nM | - |