Assay Detail
Binding
CHEMBL3705601
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
5-membered ring heteroaromatic derivatives having NPY Y5 receptor antagonistic activity
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 9.16 | 9.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3666784 | — | — | 1 | 9.89 |
| CHEMBL3666787 | — | — | 1 | 9.74 |
| CHEMBL3666782 | — | — | 1 | 9.70 |
| CHEMBL3666781 | — | — | 1 | 9.66 |
| CHEMBL3666786 | — | — | 1 | 9.66 |
| CHEMBL3666788 | — | — | 1 | 9.64 |
| CHEMBL3666779 | — | — | 1 | 9.49 |
| CHEMBL3666780 | — | — | 1 | 9.47 |
| CHEMBL3666794 | — | — | 1 | 9.30 |
| CHEMBL3666798 | — | — | 1 | 9.21 |
| CHEMBL3666801 | — | — | 1 | 9.19 |
| CHEMBL3666792 | — | — | 1 | 9.15 |
| CHEMBL3666790 | — | — | 1 | 9.10 |
| CHEMBL3666795 | — | — | 1 | 9.10 |
| CHEMBL3666785 | — | — | 1 | 9.07 |
| CHEMBL3666791 | — | — | 1 | 9.05 |
| CHEMBL3666789 | — | — | 1 | 9.05 |
| CHEMBL3666799 | — | — | 1 | 8.98 |
| CHEMBL3666783 | — | — | 1 | 8.85 |
| CHEMBL3666793 | — | — | 1 | 8.82 |
| CHEMBL3666802 | — | — | 1 | 8.78 |
| CHEMBL3666803 | — | — | 1 | 8.72 |
| CHEMBL3666796 | — | — | 1 | 8.51 |
| CHEMBL3666800 | — | — | 1 | 8.44 |
| CHEMBL3666797 | — | — | 1 | 8.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3666784 | — | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL3666787 | — | IC50 | = | 0.18 | nM | 9.74 |
| CHEMBL3666782 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3666781 | — | IC50 | = | 0.22 | nM | 9.66 |
| CHEMBL3666786 | — | IC50 | = | 0.22 | nM | 9.66 |
| CHEMBL3666788 | — | IC50 | = | 0.23 | nM | 9.64 |
| CHEMBL3666779 | — | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL3666780 | — | IC50 | = | 0.34 | nM | 9.47 |
| CHEMBL3666794 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3666798 | — | IC50 | = | 0.61 | nM | 9.21 |
| CHEMBL3666801 | — | IC50 | = | 0.65 | nM | 9.19 |
| CHEMBL3666792 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL3666790 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL3666795 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL3666785 | — | IC50 | = | 0.86 | nM | 9.07 |
| CHEMBL3666791 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3666789 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3666799 | — | IC50 | = | 1.04 | nM | 8.98 |
| CHEMBL3666783 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3666793 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3666802 | — | IC50 | = | 1.67 | nM | 8.78 |
| CHEMBL3666803 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3666796 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL3666800 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL3666797 | — | IC50 | = | 4.21 | nM | 8.38 |