Assay Detail
Binding
CHEMBL995612
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Binding affinity to human GnRHR
27
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Gonadotropin-releasing hormone receptor (CHEMBL1855) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Potent and orally bioavailable zwitterion GnRH antagonists with low CYP3A4 inhibitory activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 27 | 7.85 | 9.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL434936 | — | — | 1 | 9.19 |
| CHEMBL364914 | — | — | 1 | 9.05 |
| CHEMBL189164 | — | — | 1 | 8.96 |
| CHEMBL371613 | — | — | 1 | 8.89 |
| CHEMBL509075 | — | — | 2 | 8.70 |
| CHEMBL450471 | — | — | 2 | 8.50 |
| CHEMBL508435 | — | — | 1 | 8.48 |
| CHEMBL453167 | — | — | 1 | 8.47 |
| CHEMBL508020 | — | — | 1 | 8.44 |
| CHEMBL191817 | — | — | 1 | 8.28 |
| CHEMBL192172 | — | — | 1 | 8.22 |
| CHEMBL365985 | — | — | 1 | 8.11 |
| CHEMBL499026 | — | — | 1 | 8.00 |
| CHEMBL526327 | — | — | 1 | 7.66 |
| CHEMBL455769 | — | — | 1 | 7.50 |
| CHEMBL526887 | — | — | 1 | 7.38 |
| CHEMBL445691 | — | — | 1 | 7.18 |
| CHEMBL495882 | — | — | 1 | 7.16 |
| CHEMBL499307 | — | — | 1 | 7.11 |
| CHEMBL503624 | — | — | 1 | 6.96 |
| CHEMBL497747 | — | — | 1 | 5.96 |
| CHEMBL499589 | — | — | 1 | 5.43 |
| CHEMBL499849 | — | — | 1 | 5.41 |
| CHEMBL499588 | — | — | 1 | - |
| CHEMBL456279 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL434936 | — | Ki | = | 0.64 | nM | 9.19 |
| CHEMBL364914 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL189164 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL371613 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL509075 | — | Ki | = | 1.995 | nM | 8.70 |
| CHEMBL509075 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL450471 | — | Ki | = | 3.162 | nM | 8.50 |
| CHEMBL508435 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL450471 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL453167 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL508020 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL191817 | — | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL192172 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL365985 | — | Ki | = | 7.8 | nM | 8.11 |
| CHEMBL499026 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL526327 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL455769 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL526887 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL445691 | — | Ki | = | 66.0 | nM | 7.18 |
| CHEMBL495882 | — | Ki | = | 69.0 | nM | 7.16 |
| CHEMBL499307 | — | Ki | = | 77.0 | nM | 7.11 |
| CHEMBL503624 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL497747 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL499589 | — | Ki | = | 3700.0 | nM | 5.43 |
| CHEMBL499849 | — | Ki | = | 3900.0 | nM | 5.41 |
| CHEMBL499588 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL456279 | — | Ki | > | 10000.0 | nM | - |