Assay Detail
Binding
CHEMBL3610071
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Antagonist activity against human recombinant NK3R expressed in CHO cells by aequorin functional assay
14
Total Activities
14
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 | Autocuration |
Publication
Optimization of Novel Antagonists to the Neurokinin-3 Receptor for the Treatment of Sex-Hormone Disorders (Part II).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 7.11 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3422018 | — | — | 1 | 8.40 |
| CHEMBL3608688 | — | — | 1 | 8.20 |
| CHEMBL3422010 | — | — | 1 | 7.80 |
| CHEMBL3608680 | FEZOLINETANT | 4.0 | 1 | 7.70 |
| CHEMBL3422009 | — | — | 1 | 7.70 |
| CHEMBL3608687 | — | — | 1 | 7.50 |
| CHEMBL3608683 | — | — | 1 | 7.40 |
| CHEMBL3608740 | — | — | 1 | 7.20 |
| CHEMBL3608741 | — | — | 1 | 7.10 |
| CHEMBL3608684 | — | — | 1 | 6.80 |
| CHEMBL3608682 | — | — | 1 | 6.80 |
| CHEMBL3608686 | — | — | 1 | 6.20 |
| CHEMBL3608685 | — | — | 1 | 5.90 |
| CHEMBL3608681 | — | — | 1 | 4.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3422018 | — | IC50 | = | 3.981 | nM | 8.40 |
| CHEMBL3608688 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL3422010 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL3608680 | FEZOLINETANT | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL3422009 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL3608687 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL3608683 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL3608740 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL3608741 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL3608684 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL3608682 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL3608686 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL3608685 | — | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL3608681 | — | IC50 | = | 15848.93 | nM | 4.80 |