Assay Detail
Binding
CHEMBL956658
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Binding affinity at human GnRH receptor
42
Total Activities
42
Compounds Tested
3
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
Non-peptide gonadotropin-releasing hormone receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 38 | 8.02 | 9.70 |
| IC50 | 3 | 9.51 | 10.00 |
| Activity | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL22055 | SUFUGOLIX | 2.0 | 1 | 10.00 |
| CHEMBL71917 | — | — | 1 | 9.70 |
| CHEMBL466731 | — | — | 1 | 9.70 |
| CHEMBL192955 | — | — | 1 | 9.35 |
| CHEMBL468551 | — | — | 1 | 9.30 |
| CHEMBL179691 | — | — | 1 | 9.25 |
| CHEMBL434936 | — | — | 1 | 9.19 |
| CHEMBL360143 | — | — | 1 | 9.15 |
| CHEMBL23969 | — | — | 1 | 8.96 |
| CHEMBL413245 | — | — | 1 | 8.82 |
| CHEMBL363759 | — | — | 1 | 8.70 |
| CHEMBL539167 | — | — | 1 | 8.64 |
| CHEMBL359894 | — | — | 1 | 8.64 |
| CHEMBL423291 | — | — | 1 | 8.43 |
| CHEMBL466730 | — | — | 1 | 8.36 |
| CHEMBL513346 | — | — | 1 | 8.35 |
| CHEMBL50546 | — | — | 1 | 8.28 |
| CHEMBL191817 | — | — | 1 | 8.28 |
| CHEMBL321376 | — | — | 1 | 8.28 |
| CHEMBL112466 | — | — | 1 | 8.26 |
| CHEMBL359810 | — | — | 1 | 8.22 |
| CHEMBL302769 | — | — | 1 | 8.12 |
| CHEMBL324912 | — | — | 1 | 8.09 |
| CHEMBL367388 | — | — | 1 | 8.05 |
| CHEMBL466736 | — | — | 1 | 7.89 |
| CHEMBL466531 | — | — | 1 | 7.85 |
| CHEMBL235269 | — | — | 1 | 7.82 |
| CHEMBL23854 | — | — | 1 | 7.82 |
| CHEMBL361798 | — | — | 1 | 7.72 |
| CHEMBL493794 | — | — | 1 | 7.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL22055 | SUFUGOLIX | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL71917 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL466731 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL192955 | — | Ki | = | 0.45 | nM | 9.35 |
| CHEMBL468551 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL179691 | — | Ki | = | 0.56 | nM | 9.25 |
| CHEMBL434936 | — | Ki | = | 0.64 | nM | 9.19 |
| CHEMBL360143 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL23969 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL413245 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL363759 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL359894 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL539167 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL423291 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL466730 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL513346 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL50546 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL191817 | — | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL321376 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL112466 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL359810 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL302769 | — | Ki | = | 7.5 | nM | 8.12 |
| CHEMBL324912 | — | Ki | = | 8.1 | nM | 8.09 |
| CHEMBL367388 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL466736 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL466531 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL235269 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL23854 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL361798 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL493794 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL60153 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL468546 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL366701 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL468552 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL494968 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL513126 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL523709 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL494621 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL179101 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL111820 | — | Ki | = | 470.0 | nM | 6.33 |
| CHEMBL466541 | — | Ki | = | 580.0 | nM | 6.24 |
| CHEMBL120432 | — | Activity | = | 0.4 | nM | - |