Assay Detail
Binding
CHEMBL832980
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Inhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYY
13
Total Activities
13
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
Discovery of 4-(dimethylamino)quinazolines as potent and selective antagonists for the melanin-concentrating hormone receptor 1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 7.35 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL17645 | CGP-71683A | — | 1 | 8.89 |
| CHEMBL192266 | — | — | 1 | 8.80 |
| CHEMBL193970 | — | — | 1 | 8.60 |
| CHEMBL193438 | — | — | 1 | 8.57 |
| CHEMBL193666 | — | — | 1 | 8.31 |
| CHEMBL193771 | — | — | 1 | 7.51 |
| CHEMBL195123 | — | — | 1 | 7.39 |
| CHEMBL425012 | — | — | 1 | 7.11 |
| CHEMBL195810 | — | — | 1 | 6.92 |
| CHEMBL194602 | — | — | 1 | 6.82 |
| CHEMBL195346 | — | — | 1 | 6.06 |
| CHEMBL194173 | — | — | 1 | 5.52 |
| CHEMBL360671 | — | — | 1 | 5.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL17645 | CGP-71683A | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL192266 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL193970 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL193438 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL193666 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL193771 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL195123 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL425012 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL195810 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL194602 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL195346 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL194173 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL360671 | — | IC50 | = | 8900.0 | nM | 5.05 |