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Assay Detail

CHEMBL5042867

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [125I]-1DMeNPFF from mouse NPFF2R receptor by TopCount scintillation counting method
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Neuropeptide FF receptor 2 (CHEMBL4523416)
Type SINGLE PROTEIN
Organism Mus musculus

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.
Quillet R, Schneider S, Utard V, Drieu la Rochelle A, Elhabazi K, Henningsen JB, Gizzi P, Schmitt M, Kugler V, Simonneaux V, Ilien B, Simonin F, Bihel F.
J Med Chem (2021) 64 : 7555 -7564
PubMed 34008968 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 6.36 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL429731 1 8.96
CHEMBL4776204 1 6.08
CHEMBL5074999 1 5.84
CHEMBL5091013 1 5.56
CHEMBL5085324 1 5.37
CHEMBL2165920 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL429731 Ki = 1.1 nM 8.96
CHEMBL4776204 Ki = 824.0 nM 6.08
CHEMBL5074999 Ki = 1450.0 nM 5.84
CHEMBL5091013 Ki = 2750.0 nM 5.56
CHEMBL5085324 Ki = 4300.0 nM 5.37
CHEMBL2165920 Ki - -