Assay Detail
Binding
CHEMBL685307
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Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
26
Total Activities
26
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
3-(2-aminoalkyl)-1-(2,6-difluorobenzyl)-5- (2-fluoro-3-methoxyphenyl)-6-methyl-uracils as orally bioavailable antagonists of the human gonadotropin releasing hormone receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 26 | 7.67 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL115703 | — | — | 1 | 9.22 |
| CHEMBL116071 | — | — | 1 | 8.92 |
| CHEMBL333850 | — | — | 1 | 8.62 |
| CHEMBL119774 | — | — | 1 | 8.39 |
| CHEMBL22653 | — | — | 1 | 8.35 |
| CHEMBL117670 | — | — | 1 | 8.19 |
| CHEMBL326504 | — | — | 1 | 8.19 |
| CHEMBL116074 | — | — | 1 | 8.10 |
| CHEMBL324912 | — | — | 1 | 8.09 |
| CHEMBL119808 | — | — | 1 | 8.00 |
| CHEMBL116976 | — | — | 1 | 7.92 |
| CHEMBL117504 | — | — | 1 | 7.92 |
| CHEMBL117396 | — | — | 1 | 7.80 |
| CHEMBL327076 | — | — | 1 | 7.64 |
| CHEMBL23830 | — | — | 1 | 7.47 |
| CHEMBL116259 | — | — | 1 | 7.41 |
| CHEMBL180124 | — | — | 1 | 7.34 |
| CHEMBL23729 | — | — | 1 | 7.29 |
| CHEMBL330804 | — | — | 1 | 7.29 |
| CHEMBL119149 | — | — | 1 | 7.18 |
| CHEMBL115965 | — | — | 1 | 7.15 |
| CHEMBL119185 | — | — | 1 | 7.03 |
| CHEMBL119391 | — | — | 1 | 6.22 |
| CHEMBL116576 | — | — | 1 | 6.01 |
| CHEMBL119739 | — | — | 1 | 6.01 |
| CHEMBL117637 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL115703 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL116071 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL333850 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL119774 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL22653 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL117670 | — | Ki | = | 6.4 | nM | 8.19 |
| CHEMBL326504 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL116074 | — | Ki | = | 7.9 | nM | 8.10 |
| CHEMBL324912 | — | Ki | = | 8.1 | nM | 8.09 |
| CHEMBL119808 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL116976 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL117504 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL117396 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL327076 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL23830 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL116259 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL180124 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL23729 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL330804 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL119149 | — | Ki | = | 66.0 | nM | 7.18 |
| CHEMBL115965 | — | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL119185 | — | Ki | = | 94.0 | nM | 7.03 |
| CHEMBL119391 | — | Ki | = | 595.0 | nM | 6.22 |
| CHEMBL116576 | — | Ki | = | 965.0 | nM | 6.01 |
| CHEMBL119739 | — | Ki | = | 973.0 | nM | 6.01 |
| CHEMBL117637 | — | Ki | > | 10000.0 | nM | - |