Assay Detail
Binding
CHEMBL874135
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Binding affinity towards human gonadotropin-releasing hormone receptor
27
Total Activities
27
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 structure-activity relationships of thieno[2,3-d]pyrimidine-2,4-dione derivatives as potent GnRH receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 27 | 7.69 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL71917 | — | — | 1 | 9.70 |
| CHEMBL22055 | SUFUGOLIX | 2.0 | 1 | 9.70 |
| CHEMBL120432 | — | — | 1 | 9.40 |
| CHEMBL435167 | — | — | 1 | 9.40 |
| CHEMBL333518 | — | — | 1 | 9.22 |
| CHEMBL21126 | — | — | 1 | 9.10 |
| CHEMBL280213 | — | — | 1 | 8.54 |
| CHEMBL332355 | — | — | 1 | 8.39 |
| CHEMBL331762 | — | — | 1 | 8.05 |
| CHEMBL332463 | — | — | 1 | 7.96 |
| CHEMBL121441 | — | — | 1 | 7.80 |
| CHEMBL332837 | — | — | 1 | 7.77 |
| CHEMBL332138 | — | — | 1 | 7.44 |
| CHEMBL333103 | — | — | 1 | 7.37 |
| CHEMBL120149 | — | — | 1 | 7.24 |
| CHEMBL330835 | — | — | 1 | 7.21 |
| CHEMBL333213 | — | — | 1 | 7.12 |
| CHEMBL330834 | — | — | 1 | 7.06 |
| CHEMBL332570 | — | — | 1 | 6.82 |
| CHEMBL120260 | — | — | 1 | 6.77 |
| CHEMBL334110 | — | — | 1 | 6.77 |
| CHEMBL262557 | — | — | 1 | 6.75 |
| CHEMBL333233 | — | — | 1 | 6.57 |
| CHEMBL332616 | — | — | 1 | 6.52 |
| CHEMBL334148 | — | — | 1 | 6.44 |
| CHEMBL332194 | — | — | 1 | 6.34 |
| CHEMBL122064 | — | — | 1 | 6.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL71917 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL22055 | SUFUGOLIX | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL120432 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL435167 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL333518 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL21126 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL280213 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL332355 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL331762 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL332463 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL121441 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL332837 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL332138 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL333103 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL120149 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL330835 | — | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL333213 | — | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL330834 | — | Ki | = | 88.0 | nM | 7.06 |
| CHEMBL332570 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL120260 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL334110 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL262557 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL333233 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL332616 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL334148 | — | Ki | = | 360.0 | nM | 6.44 |
| CHEMBL332194 | — | Ki | = | 460.0 | nM | 6.34 |
| CHEMBL122064 | — | Ki | = | 640.0 | nM | 6.19 |