Assay Detail
Binding
CHEMBL831490
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Gonadotropin-releasing hormone receptor (CHEMBL1855) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Identification of neutral 4-O-alkyl quinolone nonpeptide GnRH receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 9.06 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL441676 | — | — | 1 | 10.00 |
| CHEMBL48192 | — | — | 1 | 9.52 |
| CHEMBL364167 | — | — | 1 | 9.52 |
| CHEMBL362371 | — | — | 1 | 9.49 |
| CHEMBL120432 | — | — | 1 | 9.36 |
| CHEMBL433594 | — | — | 1 | 9.26 |
| CHEMBL185986 | — | — | 1 | 9.22 |
| CHEMBL184819 | — | — | 1 | 9.22 |
| CHEMBL185785 | — | — | 1 | 9.22 |
| CHEMBL424991 | — | — | 1 | 9.15 |
| CHEMBL362544 | — | — | 1 | 9.10 |
| CHEMBL363663 | — | — | 1 | 9.05 |
| CHEMBL185738 | — | — | 1 | 8.85 |
| CHEMBL360429 | — | — | 1 | 8.70 |
| CHEMBL365366 | — | — | 1 | 8.70 |
| CHEMBL185438 | — | — | 1 | 6.61 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL441676 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL48192 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL364167 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL362371 | — | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL120432 | — | IC50 | = | 0.44 | nM | 9.36 |
| CHEMBL433594 | — | IC50 | = | 0.55 | nM | 9.26 |
| CHEMBL185986 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL184819 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL185785 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL424991 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL362544 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL363663 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL185738 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL360429 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL365366 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL185438 | — | IC50 | = | 243.0 | nM | 6.61 |