Assay Detail
Binding
CHEMBL745033
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Displacement of [3H]- NKA from human NK-2 receptor expressed in MEL cells
19
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | MEL |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
4-Alkylpiperidines related to SR-48968: potent antagonists of the neurokinin-2 (NK2) receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 8.15 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL56835 | — | — | 2 | 9.22 |
| CHEMBL2115073 | — | — | 1 | 9.08 |
| CHEMBL443264 | — | — | 1 | 8.89 |
| CHEMBL2111522 | — | — | 1 | 8.68 |
| CHEMBL2115072 | — | — | 1 | 8.57 |
| CHEMBL56481 | — | — | 1 | 8.46 |
| CHEMBL56788 | — | — | 1 | 8.43 |
| CHEMBL56143 | — | — | 1 | 8.33 |
| CHEMBL58638 | — | — | 1 | 8.19 |
| CHEMBL301437 | — | — | 1 | 8.11 |
| CHEMBL417940 | — | — | 1 | 8.04 |
| CHEMBL59542 | — | — | 1 | 8.00 |
| CHEMBL56739 | — | — | 1 | 7.88 |
| CHEMBL56274 | — | — | 1 | 7.47 |
| CHEMBL57589 | — | — | 1 | 7.40 |
| CHEMBL292415 | — | — | 1 | 7.33 |
| CHEMBL58331 | — | — | 1 | 7.18 |
| CHEMBL57224 | — | — | 1 | 6.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL56835 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL2115073 | — | Ki | = | 0.84 | nM | 9.08 |
| CHEMBL443264 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL56835 | — | Ki | = | 1.75 | nM | 8.76 |
| CHEMBL2111522 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL2115072 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL56481 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL56788 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL56143 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL58638 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL301437 | — | Ki | = | 7.7 | nM | 8.11 |
| CHEMBL417940 | — | Ki | = | 9.2 | nM | 8.04 |
| CHEMBL59542 | — | Ki | = | 9.9 | nM | 8.00 |
| CHEMBL56739 | — | Ki | = | 13.1 | nM | 7.88 |
| CHEMBL56274 | — | Ki | = | 33.5 | nM | 7.47 |
| CHEMBL57589 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL292415 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL58331 | — | Ki | = | 66.0 | nM | 7.18 |
| CHEMBL57224 | — | Ki | = | 142.0 | nM | 6.85 |