Assay Detail
Binding
CHEMBL680261
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of rat gonadotropin-releasing hormone receptor
24
Total Activities
24
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 (CHEMBL3066) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Heterocyclic derivatives of 2-(3,5-dimethylphenyl)tryptamine as GnRH receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 6.81 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL11149 | — | — | 1 | 8.15 |
| CHEMBL11009 | — | — | 1 | 7.80 |
| CHEMBL10931 | — | — | 1 | 7.57 |
| CHEMBL11014 | — | — | 1 | 7.44 |
| CHEMBL262715 | — | — | 1 | 7.40 |
| CHEMBL11101 | — | — | 1 | 7.39 |
| CHEMBL273625 | — | — | 1 | 7.35 |
| CHEMBL11253 | — | — | 1 | 7.30 |
| CHEMBL267558 | — | — | 1 | 7.24 |
| CHEMBL11310 | — | — | 1 | 7.05 |
| CHEMBL11263 | — | — | 1 | 6.92 |
| CHEMBL11420 | — | — | 1 | 6.82 |
| CHEMBL275287 | — | — | 1 | 6.80 |
| CHEMBL11436 | — | — | 1 | 6.70 |
| CHEMBL11021 | — | — | 1 | 6.70 |
| CHEMBL273725 | — | — | 1 | 6.68 |
| CHEMBL275920 | — | — | 1 | 6.57 |
| CHEMBL11375 | — | — | 1 | 6.35 |
| CHEMBL11087 | — | — | 1 | 6.35 |
| CHEMBL11623 | — | — | 1 | 5.90 |
| CHEMBL269636 | — | — | 1 | 5.66 |
| CHEMBL11523 | — | — | 1 | 5.35 |
| CHEMBL11134 | — | — | 1 | 5.05 |
| CHEMBL274441 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL11149 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL11009 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL10931 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL11014 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL262715 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL11101 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL273625 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL11253 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL267558 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL11310 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL11263 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL11420 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL275287 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL11436 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL11021 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL273725 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL275920 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL11375 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL11087 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL11623 | — | IC50 | = | 1260.0 | nM | 5.90 |
| CHEMBL269636 | — | IC50 | = | 2170.0 | nM | 5.66 |
| CHEMBL11523 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL11134 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL274441 | — | IC50 | > | 10000.0 | nM | - |