Assay Detail
Functional
CHEMBL896503
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Cell Type | Pituitary gland cell |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Gonadotropin-releasing hormone receptor (CHEMBL3066) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Identification of 2-(4,5,6,7-tetrahydro-1H-pyrrolo[3,2-c]pyridin-3-yl)-ethylamine derivatives as novel GnRH receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 7.40 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL413245 | — | — | 1 | 9.22 |
| CHEMBL231760 | — | — | 1 | 8.92 |
| CHEMBL267838 | — | — | 1 | 8.19 |
| CHEMBL231761 | — | — | 1 | 7.55 |
| CHEMBL410547 | — | — | 1 | 7.36 |
| CHEMBL398060 | — | — | 1 | 7.33 |
| CHEMBL392446 | — | — | 1 | 7.24 |
| CHEMBL233341 | — | — | 1 | 7.20 |
| CHEMBL395225 | — | — | 1 | 7.17 |
| CHEMBL232150 | — | — | 1 | 7.02 |
| CHEMBL232151 | — | — | 1 | 6.96 |
| CHEMBL233762 | — | — | 1 | 6.60 |
| CHEMBL401226 | — | — | 1 | 6.55 |
| CHEMBL392843 | — | — | 1 | 6.32 |
| CHEMBL232356 | — | — | 1 | - |
| CHEMBL401225 | — | — | 1 | - |
| CHEMBL393540 | — | — | 1 | - |
| CHEMBL429976 | — | — | 1 | - |
| CHEMBL232752 | — | — | 1 | - |
| CHEMBL231954 | — | — | 1 | - |
| CHEMBL231739 | — | — | 1 | - |
| CHEMBL232097 | — | — | 1 | - |
| CHEMBL394634 | — | — | 1 | - |
| CHEMBL409825 | — | — | 1 | - |
| CHEMBL394613 | — | — | 1 | - |
| CHEMBL233761 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL413245 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL231760 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL267838 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL231761 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL410547 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL398060 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL392446 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL233341 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL395225 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL232150 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL232151 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL233762 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL401226 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL392843 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL232356 | — | IC50 | - | — | - | |
| CHEMBL401225 | — | IC50 | - | — | - | |
| CHEMBL393540 | — | IC50 | - | — | - | |
| CHEMBL429976 | — | IC50 | - | — | - | |
| CHEMBL232752 | — | IC50 | - | — | - | |
| CHEMBL231954 | — | IC50 | - | — | - | |
| CHEMBL231739 | — | IC50 | - | — | - | |
| CHEMBL232097 | — | IC50 | - | — | - | |
| CHEMBL394634 | — | IC50 | - | — | - | |
| CHEMBL409825 | — | IC50 | - | — | - | |
| CHEMBL394613 | — | IC50 | - | — | - | |
| CHEMBL233761 | — | IC50 | - | — | - |