Assay Detail
Binding
CHEMBL747339
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Concentration required to inhibit the specific binding of [125I]BH-ELE to Neurokinin-3 (NK-3) 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 | 5.94 | 7.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL263852 | — | — | 1 | 7.19 |
| CHEMBL405209 | — | — | 1 | 7.04 |
| CHEMBL2115376 | — | — | 1 | 6.96 |
| CHEMBL235363 | SUBSTANCE P | 1.0 | 1 | 6.89 |
| CHEMBL405422 | — | — | 1 | 6.77 |
| CHEMBL2114443 | — | — | 1 | 6.75 |
| CHEMBL276294 | — | — | 1 | 6.72 |
| CHEMBL2372521 | — | — | 1 | 6.35 |
| CHEMBL265155 | — | — | 1 | 5.92 |
| CHEMBL2372519 | — | — | 1 | 5.80 |
| CHEMBL411230 | — | — | 1 | 5.72 |
| CHEMBL2372444 | — | — | 1 | 5.72 |
| CHEMBL2114442 | — | — | 1 | 5.68 |
| CHEMBL410808 | — | — | 1 | 5.66 |
| CHEMBL2115375 | — | — | 1 | 5.66 |
| CHEMBL264353 | — | — | 1 | 5.51 |
| CHEMBL269584 | — | — | 1 | 5.13 |
| CHEMBL265573 | — | — | 1 | 4.93 |
| CHEMBL2372516 | — | — | 1 | 4.82 |
| CHEMBL406442 | — | — | 1 | 4.77 |
| CHEMBL2372525 | — | — | 1 | 4.70 |
| CHEMBL415600 | — | — | 1 | - |
| CHEMBL2372518 | — | — | 1 | - |
| CHEMBL216813 | — | — | 1 | - |
| CHEMBL2372517 | — | — | 1 | - |
| CHEMBL406812 | — | — | 1 | - |
| CHEMBL264341 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL263852 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL405209 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL2115376 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL235363 | SUBSTANCE P | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL405422 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL2114443 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL276294 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL2372521 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL265155 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL2372519 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL411230 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL2372444 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL2114442 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL410808 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL2115375 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL264353 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL269584 | — | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL265573 | — | IC50 | = | 11700.0 | nM | 4.93 |
| CHEMBL2372516 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL406442 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL2372525 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL415600 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2372518 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL216813 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2372517 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL406812 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL264341 | — | IC50 | > | 10000.0 | nM | - |