Assay Detail
Binding
CHEMBL747209
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50% displacement of specifically bound [3H]NPY2 from rat brain membranes.
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Novel modified carboxy terminal fragments of neuropeptide Y with high affinity for Y2-type receptors and potent functional antagonism at a Y1-type receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 6.70 | 9.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL441396 | NEUROPEPTIDE Y(NPY) | — | 1 | 9.35 |
| CHEMBL269515 | — | — | 1 | 8.10 |
| CHEMBL274850 | — | — | 1 | 7.92 |
| CHEMBL383861 | — | — | 1 | 7.92 |
| CHEMBL265849 | — | — | 1 | 7.82 |
| CHEMBL409457 | — | — | 1 | 7.43 |
| CHEMBL385246 | — | — | 1 | 7.36 |
| CHEMBL439534 | NPY[TYR32,LEU34] | — | 1 | 7.08 |
| CHEMBL386823 | — | — | 1 | 6.76 |
| CHEMBL428097 | — | — | 1 | 6.51 |
| CHEMBL439356 | — | — | 1 | 6.43 |
| CHEMBL406383 | — | — | 1 | 6.40 |
| CHEMBL386822 | — | — | 1 | 5.89 |
| CHEMBL406275 | — | — | 1 | 5.68 |
| CHEMBL269544 | — | — | 1 | 5.57 |
| CHEMBL275220 | — | — | 1 | 5.53 |
| CHEMBL385245 | — | — | 1 | 4.52 |
| CHEMBL262202 | — | — | 1 | 4.40 |
| CHEMBL277607 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL441396 | NEUROPEPTIDE Y(NPY) | IC50 | = | 0.45 | nM | 9.35 |
| CHEMBL269515 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL274850 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL383861 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL265849 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL409457 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL385246 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL439534 | NPY[TYR32,LEU34] | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL386823 | — | IC50 | = | 174.0 | nM | 6.76 |
| CHEMBL428097 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL439356 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL406383 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL386822 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL406275 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL269544 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL275220 | — | IC50 | = | 2950.0 | nM | 5.53 |
| CHEMBL385245 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL262202 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL277607 | — | IC50 | > | 100000.0 | nM | - |