Assay Detail
Functional
CHEMBL692301
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NPY Y1-antagonistic activity in HEL cells by measuring the inhibition of porcine NPY (10 nM) stimulated increase in the intracellular [Ca2+] concentration in a FURA-assay.
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | HEL |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Structure-activity relationships of neuropeptide Y Y1 receptor antagonists related to BIBP 3226.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 5.70 | 7.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL44246 | — | — | 1 | 7.77 |
| CHEMBL288355 | — | — | 1 | 7.22 |
| CHEMBL41457 | — | — | 1 | 7.09 |
| CHEMBL417711 | — | — | 1 | 7.00 |
| CHEMBL289620 | — | — | 1 | 6.96 |
| CHEMBL41673 | — | — | 1 | 6.70 |
| CHEMBL42747 | — | — | 1 | 6.55 |
| CHEMBL41981 | — | — | 1 | 6.05 |
| CHEMBL42793 | — | — | 1 | 6.00 |
| CHEMBL43627 | — | — | 1 | 5.96 |
| CHEMBL40430 | — | — | 1 | 5.85 |
| CHEMBL43710 | — | — | 1 | 5.66 |
| CHEMBL433627 | — | — | 1 | 5.60 |
| CHEMBL41686 | — | — | 1 | 5.52 |
| CHEMBL43628 | — | — | 1 | 5.43 |
| CHEMBL42686 | — | — | 1 | 5.34 |
| CHEMBL43523 | — | — | 1 | 5.12 |
| CHEMBL38531 | — | — | 1 | 5.09 |
| CHEMBL41392 | — | — | 1 | 4.94 |
| CHEMBL40475 | — | — | 1 | 4.92 |
| CHEMBL290175 | — | — | 1 | 4.92 |
| CHEMBL296523 | — | — | 1 | 4.68 |
| CHEMBL41166 | — | — | 1 | 4.66 |
| CHEMBL43753 | — | — | 1 | 4.65 |
| CHEMBL42861 | — | — | 1 | 4.29 |
| CHEMBL42625 | — | — | 1 | 4.12 |
| CHEMBL435169 | — | — | 1 | - |
| CHEMBL40458 | — | — | 1 | - |
| CHEMBL290261 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL44246 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL288355 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL41457 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL417711 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL289620 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL41673 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL42747 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL41981 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL42793 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL43627 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL40430 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL43710 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL433627 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL41686 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL43628 | — | IC50 | = | 3750.0 | nM | 5.43 |
| CHEMBL42686 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL43523 | — | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL38531 | — | IC50 | = | 8100.0 | nM | 5.09 |
| CHEMBL41392 | — | IC50 | = | 11500.0 | nM | 4.94 |
| CHEMBL40475 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL290175 | — | IC50 | = | 11900.0 | nM | 4.92 |
| CHEMBL296523 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL41166 | — | IC50 | = | 21800.0 | nM | 4.66 |
| CHEMBL43753 | — | IC50 | = | 22300.0 | nM | 4.65 |
| CHEMBL42861 | — | IC50 | = | 51000.0 | nM | 4.29 |
| CHEMBL42625 | — | IC50 | = | 76000.0 | nM | 4.12 |
| CHEMBL435169 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL40458 | — | IC50 | - | nM | - | |
| CHEMBL290261 | — | IC50 | - | nM | - |