Assay Detail
Binding
CHEMBL4406743
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of (sCy5)-[Lys2 Arg4]-BVD15 from GFP-tagged Y1R in human HEK293T cells assessed as inhibitory constant incubated for 5 mins followed by (sCy5)-[Lys2 Arg4]-BVD15 addition and measured after 30 mins by fluorescence based assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Heterodimeric Analogues of the Potent Y1R Antagonist 1229U91, Lacking One of the Pharmacophoric C-Terminal Structures, Retain Potent Y1R Affinity and Show Improved Selectivity over Y4R.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 8.57 | 9.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4454036 | — | — | 1 | 9.59 |
| CHEMBL4476074 | — | — | 1 | 9.56 |
| CHEMBL4445317 | — | — | 1 | 9.44 |
| CHEMBL4519035 | — | — | 1 | 9.24 |
| CHEMBL2110365 | — | — | 1 | 8.99 |
| CHEMBL4573545 | — | — | 1 | 8.63 |
| CHEMBL4534028 | — | — | 1 | 8.09 |
| CHEMBL4578617 | — | — | 1 | 7.89 |
| CHEMBL267633 | NEUROPEPTIDE-Y | — | 1 | 7.78 |
| CHEMBL4468261 | — | — | 1 | 7.60 |
| CHEMBL4572358 | — | — | 1 | 7.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4454036 | — | Ki | = | 0.257 | nM | 9.59 |
| CHEMBL4476074 | — | Ki | = | 0.2754 | nM | 9.56 |
| CHEMBL4445317 | — | Ki | = | 0.3631 | nM | 9.44 |
| CHEMBL4519035 | — | Ki | = | 0.5754 | nM | 9.24 |
| CHEMBL2110365 | — | Ki | = | 1.023 | nM | 8.99 |
| CHEMBL4573545 | — | Ki | = | 2.344 | nM | 8.63 |
| CHEMBL4534028 | — | Ki | = | 8.128 | nM | 8.09 |
| CHEMBL4578617 | — | Ki | = | 12.88 | nM | 7.89 |
| CHEMBL267633 | NEUROPEPTIDE-Y | Ki | = | 16.6 | nM | 7.78 |
| CHEMBL4468261 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL4572358 | — | Ki | = | 31.62 | nM | 7.50 |