Assay Detail
Binding
CHEMBL680276
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Inhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranes
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Gonadotropin-releasing hormone receptor (CHEMBL3066) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Structure-activity studies of reduced-size gonadotropin-releasing hormone agonists derived from the sequence of an endothelin antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 5.88 | 6.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL327528 | — | — | 1 | 6.64 |
| CHEMBL327529 | — | — | 1 | 6.50 |
| CHEMBL2370249 | — | — | 1 | 6.30 |
| CHEMBL2370251 | — | — | 1 | 6.16 |
| CHEMBL329695 | — | — | 1 | 6.16 |
| CHEMBL317064 | — | — | 1 | 5.72 |
| CHEMBL317341 | — | — | 1 | 5.70 |
| CHEMBL2370259 | — | — | 1 | 5.40 |
| CHEMBL329946 | — | — | 1 | 5.10 |
| CHEMBL2370261 | — | — | 1 | 5.10 |
| CHEMBL2370260 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL327528 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL327529 | — | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL2370249 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL2370251 | — | Ki | = | 700.0 | nM | 6.16 |
| CHEMBL329695 | — | Ki | = | 700.0 | nM | 6.16 |
| CHEMBL317064 | — | Ki | = | 1900.0 | nM | 5.72 |
| CHEMBL317341 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL2370259 | — | Ki | = | 4000.0 | nM | 5.40 |
| CHEMBL329946 | — | Ki | = | 8000.0 | nM | 5.10 |
| CHEMBL2370261 | — | Ki | = | 8000.0 | nM | 5.10 |
| CHEMBL2370260 | — | Ki | > | 10000.0 | nM | - |