Assay Detail
Functional
CHEMBL5042877
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human NPFF1 receptor expressed in HEK293 cells assessed as rightward shift of the dose dependent curve of (S)-N1-((S)-1-((S)-1-amino-1-oxo-3-phenylpropan-2-ylamino)-5-guanidino-1-oxopentan-2-yl)-2-((S)-1-((S)-2-((S)-4-amino-2-((S)-1-((S)-2-amino-3-methylbutanoyl)pyrrolidine-2-carboxamido)-4-oxobutanamido)-4-methylpentanoyl)pyrrolidine-2-carboxamido)pentanediamide
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Identification of an <i>N</i>-acylated-<sup>D</sup>Arg-Leu-NH<sub>2</sub> Dipeptide as a Highly Selective Neuropeptide FF1 Receptor Antagonist That Potently Prevents Opioid-Induced Hyperalgesia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 2 | 7.75 | 7.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5085324 | — | — | 1 | 7.80 |
| CHEMBL5091013 | — | — | 1 | 7.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5085324 | — | Kd | = | 15.85 | nM | 7.80 |
| CHEMBL5091013 | — | Kd | = | 19.95 | nM | 7.70 |