Assay Detail
Binding
CHEMBL749850
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Concentration required to inhibit the specific binding of [125I]NKA to Neurokinin-2 (NK-2) receptor in rat duodenum membranes
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Subcellular | Membrane |
| 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 | 25 | 6.33 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL263852 | — | — | 1 | 8.05 |
| CHEMBL2115376 | — | — | 1 | 7.54 |
| CHEMBL405209 | — | — | 1 | 7.39 |
| CHEMBL2114443 | — | — | 1 | 7.24 |
| CHEMBL405422 | — | — | 1 | 7.17 |
| CHEMBL2372521 | — | — | 1 | 6.96 |
| CHEMBL2372519 | — | — | 1 | 6.92 |
| CHEMBL276294 | — | — | 1 | 6.80 |
| CHEMBL235363 | SUBSTANCE P | 1.0 | 1 | 6.70 |
| CHEMBL2115375 | — | — | 1 | 6.42 |
| CHEMBL411230 | — | — | 1 | 6.35 |
| CHEMBL2372444 | — | — | 1 | 6.28 |
| CHEMBL2114442 | — | — | 1 | 6.28 |
| CHEMBL410808 | — | — | 1 | 6.17 |
| CHEMBL264353 | — | — | 1 | 6.16 |
| CHEMBL265573 | — | — | 1 | 6.02 |
| CHEMBL2372516 | — | — | 1 | 5.89 |
| CHEMBL406812 | — | — | 1 | 5.77 |
| CHEMBL415600 | — | — | 1 | 5.72 |
| CHEMBL406442 | — | — | 1 | 5.44 |
| CHEMBL216813 | — | — | 1 | 5.41 |
| CHEMBL264341 | — | — | 1 | 5.31 |
| CHEMBL2372517 | — | — | 1 | 5.22 |
| CHEMBL2372525 | — | — | 1 | 4.75 |
| CHEMBL2372518 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL263852 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL2115376 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL405209 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL2114443 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL405422 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL2372521 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL2372519 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL276294 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL235363 | SUBSTANCE P | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL2115375 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL411230 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL2372444 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL2114442 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL410808 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL264353 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL265573 | — | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL2372516 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL406812 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL415600 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL406442 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL216813 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL264341 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL2372517 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL2372525 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL2372518 | — | IC50 | > | 10000.0 | nM | - |