Assay Detail
Binding
CHEMBL874561
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Inhibitory activity against neuropeptide Y receptor type 5 by using [125I]PYY as radioligand expressed in COS-1 cells
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | COS-1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Lead optimization of 4-(dimethylamino)quinazolines, potent and selective antagonists for the melanin-concentrating hormone receptor 1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 6.25 | 8.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL537846 | — | — | 1 | 8.57 |
| CHEMBL181217 | — | — | 1 | 6.92 |
| CHEMBL181727 | — | — | 1 | 6.34 |
| CHEMBL367355 | — | — | 1 | 6.33 |
| CHEMBL360117 | — | — | 1 | 6.25 |
| CHEMBL180003 | — | — | 1 | 6.06 |
| CHEMBL181393 | — | — | 1 | 5.75 |
| CHEMBL181466 | — | — | 1 | 5.62 |
| CHEMBL182150 | — | — | 1 | 5.57 |
| CHEMBL360671 | — | — | 1 | 5.05 |
| CHEMBL181184 | — | — | 1 | - |
| CHEMBL178084 | — | — | 1 | - |
| CHEMBL182235 | — | — | 1 | - |
| CHEMBL360876 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL537846 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL181217 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL181727 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL367355 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL360117 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL180003 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL181393 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL181466 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL182150 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL360671 | — | IC50 | = | 8900.0 | nM | 5.05 |
| CHEMBL181184 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL178084 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL182235 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL360876 | — | IC50 | > | 1000.0 | nM | - |