Assay Detail
Functional
CHEMBL784303
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
33
Total Activities
33
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
Substituted indole-5-carboxamides and -acetamides as potent nonpeptide GnRH receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 6.66 | 7.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL297151 | — | — | 1 | 7.50 |
| CHEMBL47761 | — | — | 1 | 7.40 |
| CHEMBL265774 | — | — | 1 | 7.38 |
| CHEMBL295152 | — | — | 1 | 7.19 |
| CHEMBL297430 | — | — | 1 | 7.16 |
| CHEMBL45489 | — | — | 1 | 7.14 |
| CHEMBL45597 | — | — | 1 | 7.09 |
| CHEMBL49891 | — | — | 1 | 7.02 |
| CHEMBL239108 | — | — | 1 | 7.02 |
| CHEMBL48763 | — | — | 1 | 6.92 |
| CHEMBL42592 | — | — | 1 | 6.89 |
| CHEMBL49542 | — | — | 1 | 6.89 |
| CHEMBL295731 | — | — | 1 | 6.85 |
| CHEMBL297927 | — | — | 1 | 6.82 |
| CHEMBL297918 | — | — | 1 | 6.80 |
| CHEMBL49578 | — | — | 1 | 6.68 |
| CHEMBL300268 | — | — | 1 | 6.66 |
| CHEMBL445848 | — | — | 1 | 6.62 |
| CHEMBL443768 | — | — | 1 | 6.57 |
| CHEMBL298074 | — | — | 1 | 6.50 |
| CHEMBL45614 | — | — | 1 | 6.42 |
| CHEMBL300045 | — | — | 1 | 6.40 |
| CHEMBL47862 | — | — | 1 | 6.29 |
| CHEMBL416285 | — | — | 1 | 6.27 |
| CHEMBL298748 | — | — | 1 | 6.21 |
| CHEMBL48069 | — | — | 1 | 6.18 |
| CHEMBL295908 | — | — | 1 | 6.16 |
| CHEMBL291201 | — | — | 1 | 6.10 |
| CHEMBL49893 | — | — | 1 | 6.09 |
| CHEMBL296644 | — | — | 1 | 5.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL297151 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL47761 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL265774 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL295152 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL297430 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL45489 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL45597 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL49891 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL239108 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL48763 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL42592 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL49542 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL295731 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL297927 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL297918 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL49578 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL300268 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL445848 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL443768 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL298074 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL45614 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL300045 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL47862 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL416285 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL298748 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL48069 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL295908 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL291201 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL49893 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL296644 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL45639 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL47227 | — | IC50 | > | 6200.0 | nM | - |
| CHEMBL10931 | — | IC50 | > | 6200.0 | nM | - |