Assay Detail
Binding
CHEMBL750292
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Concentration required to inhibit the specific binding of [125I]BH-SP to Neurokinin-1 (NK-1) receptor in rat brain synaptosomes
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Synaptosomes |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Design and synthesis of side-chain conformationally restricted phenylalanines and their use for structure-activity studies on tachykinin NK-1 receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 7.20 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2115376 | — | — | 1 | 9.22 |
| CHEMBL235363 | SUBSTANCE P | 1.0 | 1 | 9.19 |
| CHEMBL405422 | — | — | 1 | 8.62 |
| CHEMBL405209 | — | — | 1 | 8.60 |
| CHEMBL263852 | — | — | 1 | 8.59 |
| CHEMBL2372518 | — | — | 1 | 8.54 |
| CHEMBL2115375 | — | — | 1 | 8.51 |
| CHEMBL2372516 | — | — | 1 | 8.48 |
| CHEMBL276294 | — | — | 1 | 8.11 |
| CHEMBL265155 | — | — | 1 | 7.75 |
| CHEMBL2114443 | — | — | 1 | 7.55 |
| CHEMBL2372521 | — | — | 1 | 7.54 |
| CHEMBL2372519 | — | — | 1 | 7.32 |
| CHEMBL2114442 | — | — | 1 | 7.27 |
| CHEMBL411230 | — | — | 1 | 7.21 |
| CHEMBL265573 | — | — | 1 | 7.20 |
| CHEMBL415600 | — | — | 1 | 7.11 |
| CHEMBL410808 | — | — | 1 | 6.30 |
| CHEMBL2372525 | — | — | 1 | 5.92 |
| CHEMBL406442 | — | — | 1 | 5.89 |
| CHEMBL264353 | — | — | 1 | 5.85 |
| CHEMBL406812 | — | — | 1 | 5.64 |
| CHEMBL2372444 | — | — | 1 | 5.62 |
| CHEMBL2372517 | — | — | 1 | 5.60 |
| CHEMBL269584 | — | — | 1 | 5.57 |
| CHEMBL264341 | — | — | 1 | 5.57 |
| CHEMBL216813 | — | — | 1 | 5.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2115376 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL235363 | SUBSTANCE P | IC50 | = | 0.64 | nM | 9.19 |
| CHEMBL405422 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL405209 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL263852 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL2372518 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL2115375 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL2372516 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL276294 | — | IC50 | = | 7.84 | nM | 8.11 |
| CHEMBL265155 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL2114443 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL2372521 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL2372519 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL2114442 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL411230 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL265573 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL415600 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL410808 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL2372525 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL406442 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL264353 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL406812 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL2372444 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL2372517 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL269584 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL264341 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL216813 | — | IC50 | = | 2800.0 | nM | 5.55 |