Assay Detail
Binding
CHEMBL896502
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| 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 |
|---|---|---|---|
| Ki | 26 | 8.45 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL413245 | — | — | 1 | 9.70 |
| CHEMBL395225 | — | — | 1 | 9.52 |
| CHEMBL231954 | — | — | 1 | 9.40 |
| CHEMBL231760 | — | — | 1 | 9.30 |
| CHEMBL392446 | — | — | 1 | 9.30 |
| CHEMBL410547 | — | — | 1 | 9.22 |
| CHEMBL267838 | — | — | 1 | 9.22 |
| CHEMBL231761 | — | — | 1 | 9.15 |
| CHEMBL231739 | — | — | 1 | 9.00 |
| CHEMBL232150 | — | — | 1 | 8.89 |
| CHEMBL398060 | — | — | 1 | 8.82 |
| CHEMBL233341 | — | — | 1 | 8.82 |
| CHEMBL401226 | — | — | 1 | 8.74 |
| CHEMBL232097 | — | — | 1 | 8.74 |
| CHEMBL394613 | — | — | 1 | 8.70 |
| CHEMBL429976 | — | — | 1 | 8.59 |
| CHEMBL232151 | — | — | 1 | 8.35 |
| CHEMBL392843 | — | — | 1 | 8.33 |
| CHEMBL232356 | — | — | 1 | 8.25 |
| CHEMBL394634 | — | — | 1 | 8.21 |
| CHEMBL233762 | — | — | 1 | 7.75 |
| CHEMBL393540 | — | — | 1 | 6.92 |
| CHEMBL232752 | — | — | 1 | 6.33 |
| CHEMBL401225 | — | — | 1 | 6.18 |
| CHEMBL409825 | — | — | 1 | 5.80 |
| CHEMBL233761 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL413245 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL395225 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL231954 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL231760 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL392446 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL410547 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL267838 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL231761 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL231739 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL232150 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL398060 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL233341 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL401226 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL232097 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL394613 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL429976 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL232151 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL392843 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL232356 | — | Ki | = | 5.6 | nM | 8.25 |
| CHEMBL394634 | — | Ki | = | 6.2 | nM | 8.21 |
| CHEMBL233762 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL393540 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL232752 | — | Ki | = | 470.0 | nM | 6.33 |
| CHEMBL401225 | — | Ki | = | 660.0 | nM | 6.18 |
| CHEMBL409825 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL233761 | — | Ki | > | 10000.0 | nM | - |