Assay Detail
Binding
CHEMBL1011807
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Displacement of [3H]UR-MK114 from neuropeptide Y1 receptor in human SK-N-MC cells
9
Total Activities
5
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | SK-N-MC |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Guanidine-acylguanidine bioisosteric approach in the design of radioligands: synthesis of a tritium-labeled N(G)-propionylargininamide ([3H]-UR-MK114) as a highly potent and selective neuropeptide Y Y1 receptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 5 | 9.42 | 10.00 |
| IC50 | 3 | 8.70 | 9.01 |
| Kd | 1 | 8.92 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL511460 | — | — | 1 | 10.00 |
| CHEMBL508974 | — | — | 1 | 10.00 |
| CHEMBL267633 | NEUROPEPTIDE-Y | — | 2 | 9.30 |
| CHEMBL470495 | — | — | 3 | 9.00 |
| CHEMBL332347 | — | — | 2 | 8.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL511460 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL508974 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL267633 | NEUROPEPTIDE-Y | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL267633 | NEUROPEPTIDE-Y | IC50 | = | 0.9772 | nM | 9.01 |
| CHEMBL470495 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL470495 | — | Kd | = | 1.2 | nM | 8.92 |
| CHEMBL332347 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL470495 | — | IC50 | = | 2.239 | nM | 8.65 |
| CHEMBL332347 | — | IC50 | = | 3.631 | nM | 8.44 |