Assay Detail
Binding
CHEMBL829039
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | RBL |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Gonadotropin-releasing hormone receptor (CHEMBL1855) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and structure-activity relationships of uracil derived human GnRH receptor antagonists: (R)-3-[2-(2-amino)phenethyl]-1-(2,6-difluorobenzyl)-6-methyluracils containing a substituted thiophene or thiazole at C-5.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 31 | 7.34 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL363759 | — | — | 1 | 8.70 |
| CHEMBL365012 | — | — | 1 | 8.52 |
| CHEMBL112466 | — | — | 1 | 8.30 |
| CHEMBL185143 | — | — | 1 | 8.15 |
| CHEMBL364842 | — | — | 1 | 8.05 |
| CHEMBL186563 | — | — | 1 | 8.00 |
| CHEMBL184345 | — | — | 1 | 7.85 |
| CHEMBL183938 | — | — | 1 | 7.82 |
| CHEMBL363731 | — | — | 1 | 7.75 |
| CHEMBL364840 | — | — | 1 | 7.70 |
| CHEMBL426058 | — | — | 1 | 7.58 |
| CHEMBL185154 | — | — | 1 | 7.52 |
| CHEMBL363900 | — | — | 1 | 7.48 |
| CHEMBL367812 | — | — | 1 | 7.47 |
| CHEMBL186646 | — | — | 1 | 7.46 |
| CHEMBL438201 | — | — | 1 | 7.38 |
| CHEMBL365001 | — | — | 1 | 7.38 |
| CHEMBL187243 | — | — | 1 | 7.33 |
| CHEMBL425178 | — | — | 1 | 7.31 |
| CHEMBL187217 | — | — | 1 | 7.31 |
| CHEMBL184855 | — | — | 1 | 7.16 |
| CHEMBL363659 | — | — | 1 | 6.92 |
| CHEMBL366127 | — | — | 1 | 6.89 |
| CHEMBL360625 | — | — | 1 | 6.89 |
| CHEMBL361513 | — | — | 1 | 6.82 |
| CHEMBL360363 | — | — | 1 | 6.80 |
| CHEMBL361313 | — | — | 1 | 6.68 |
| CHEMBL365695 | — | — | 1 | 6.57 |
| CHEMBL367806 | — | — | 1 | 6.30 |
| CHEMBL360384 | — | — | 1 | 5.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL363759 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL365012 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL112466 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL185143 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL364842 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL186563 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL184345 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL183938 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL363731 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL364840 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL426058 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL185154 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL363900 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL367812 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL186646 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL438201 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL365001 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL187243 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL425178 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL187217 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL184855 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL363659 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL366127 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL360625 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL361513 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL360363 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL361313 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL365695 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL367806 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL360384 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL367369 | — | Ki | = | 3000.0 | nM | 5.52 |