Assay Detail
Functional
CHEMBL896501
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | RBL |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Gonadotropin-releasing hormone receptor (CHEMBL1855) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 6.87 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL413245 | — | — | 1 | 8.82 |
| CHEMBL410547 | — | — | 1 | 8.15 |
| CHEMBL267838 | — | — | 1 | 8.05 |
| CHEMBL231761 | — | — | 1 | 7.80 |
| CHEMBL394613 | — | — | 1 | 7.66 |
| CHEMBL231760 | — | — | 1 | 7.58 |
| CHEMBL231954 | — | — | 1 | 7.50 |
| CHEMBL395225 | — | — | 1 | 7.22 |
| CHEMBL392446 | — | — | 1 | 7.21 |
| CHEMBL394634 | — | — | 1 | 7.20 |
| CHEMBL398060 | — | — | 1 | 7.07 |
| CHEMBL231739 | — | — | 1 | 7.06 |
| CHEMBL232097 | — | — | 1 | 7.04 |
| CHEMBL392843 | — | — | 1 | 6.69 |
| CHEMBL429976 | — | — | 1 | 6.57 |
| CHEMBL401226 | — | — | 1 | 6.57 |
| CHEMBL232356 | — | — | 1 | 6.33 |
| CHEMBL232150 | — | — | 1 | 6.32 |
| CHEMBL233341 | — | — | 1 | 6.26 |
| CHEMBL232151 | — | — | 1 | 5.96 |
| CHEMBL409825 | — | — | 1 | 5.80 |
| CHEMBL233762 | — | — | 1 | 5.46 |
| CHEMBL232752 | — | — | 1 | 5.38 |
| CHEMBL393540 | — | — | 1 | 5.09 |
| CHEMBL233761 | — | — | 1 | - |
| CHEMBL401225 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL413245 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL410547 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL267838 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL231761 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL394613 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL231760 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL231954 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL395225 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL392446 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL394634 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL398060 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL231739 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL232097 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL392843 | — | IC50 | = | 205.0 | nM | 6.69 |
| CHEMBL429976 | — | IC50 | = | 267.0 | nM | 6.57 |
| CHEMBL401226 | — | IC50 | = | 271.0 | nM | 6.57 |
| CHEMBL232356 | — | IC50 | = | 462.0 | nM | 6.33 |
| CHEMBL232150 | — | IC50 | = | 475.0 | nM | 6.32 |
| CHEMBL233341 | — | IC50 | = | 546.0 | nM | 6.26 |
| CHEMBL232151 | — | IC50 | = | 1110.0 | nM | 5.96 |
| CHEMBL409825 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL233762 | — | IC50 | = | 3480.0 | nM | 5.46 |
| CHEMBL232752 | — | IC50 | = | 4180.0 | nM | 5.38 |
| CHEMBL393540 | — | IC50 | = | 8090.0 | nM | 5.09 |
| CHEMBL233761 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL401225 | — | IC50 | > | 10000.0 | nM | - |