Assay Detail
Binding
CHEMBL4146975
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Gonadotropin-releasing hormone receptor (CHEMBL1855) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and biological evaluation of 3-(2-aminoethyl) uracil derivatives as gonadotropin-releasing hormone (GnRH) receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 8.29 | 9.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4159155 | — | — | 1 | 9.54 |
| CHEMBL4169891 | — | — | 1 | 9.48 |
| CHEMBL4165983 | — | — | 1 | 9.42 |
| CHEMBL4173065 | — | — | 1 | 9.34 |
| CHEMBL4159247 | — | — | 1 | 9.24 |
| CHEMBL179691 | — | — | 1 | 9.23 |
| CHEMBL4170478 | — | — | 1 | 9.13 |
| CHEMBL4167067 | — | — | 1 | 8.92 |
| CHEMBL4163619 | — | — | 1 | 8.64 |
| CHEMBL4173914 | — | — | 1 | 8.27 |
| CHEMBL4160683 | — | — | 1 | 8.21 |
| CHEMBL4169027 | — | — | 1 | 8.12 |
| CHEMBL4171288 | — | — | 1 | 8.05 |
| CHEMBL4175801 | — | — | 1 | 7.95 |
| CHEMBL4164508 | — | — | 1 | 7.80 |
| CHEMBL4166009 | — | — | 1 | 7.76 |
| CHEMBL4161096 | — | — | 1 | 7.72 |
| CHEMBL4162543 | — | — | 1 | 7.69 |
| CHEMBL4172391 | — | — | 1 | 7.34 |
| CHEMBL4164417 | — | — | 1 | 7.30 |
| CHEMBL4167945 | — | — | 1 | 7.21 |
| CHEMBL4170863 | — | — | 1 | 7.16 |
| CHEMBL4174298 | — | — | 1 | 7.13 |
| CHEMBL4160259 | — | — | 1 | - |
| CHEMBL4175063 | — | — | 1 | - |
| CHEMBL4172747 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4159155 | — | IC50 | = | 0.29 | nM | 9.54 |
| CHEMBL4169891 | — | IC50 | = | 0.33 | nM | 9.48 |
| CHEMBL4165983 | — | IC50 | = | 0.38 | nM | 9.42 |
| CHEMBL4173065 | — | IC50 | = | 0.46 | nM | 9.34 |
| CHEMBL4159247 | — | IC50 | = | 0.58 | nM | 9.24 |
| CHEMBL179691 | — | IC50 | = | 0.59 | nM | 9.23 |
| CHEMBL4170478 | — | IC50 | = | 0.74 | nM | 9.13 |
| CHEMBL4167067 | — | IC50 | = | 1.21 | nM | 8.92 |
| CHEMBL4163619 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL4173914 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL4160683 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL4169027 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL4171288 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4175801 | — | IC50 | = | 11.3 | nM | 7.95 |
| CHEMBL4164508 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4166009 | — | IC50 | = | 17.2 | nM | 7.76 |
| CHEMBL4161096 | — | IC50 | = | 19.1 | nM | 7.72 |
| CHEMBL4162543 | — | IC50 | = | 20.4 | nM | 7.69 |
| CHEMBL4172391 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL4164417 | — | IC50 | = | 49.5 | nM | 7.30 |
| CHEMBL4167945 | — | IC50 | = | 62.3 | nM | 7.21 |
| CHEMBL4170863 | — | IC50 | = | 69.1 | nM | 7.16 |
| CHEMBL4174298 | — | IC50 | = | 73.3 | nM | 7.13 |
| CHEMBL4160259 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4175063 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL4172747 | — | IC50 | > | 1000.0 | nM | - |