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Assay Detail

CHEMBL4841982

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Functional
Agonist activity at human neuropeptide Y Y4 receptor expressed in HEK293T cells co-expressing CRE-controlled gene reporter firefly luciferase assessed as relative luminescence measured after 15 mins
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Neuropeptide Y receptor type 4 (CHEMBL4877)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

N-Terminus to Arginine Side-Chain Cyclization of Linear Peptidic Neuropeptide Y Y<sub>4</sub> Receptor Ligands Results in Picomolar Binding Constants.
Konieczny A, Conrad M, Ertl FJ, Gleixner J, Gattor AO, Grätz L, Schmidt MF, Neu E, Horn AHC, Wifling D, Gmeiner P, Clark T, Sticht H, Keller M.
J Med Chem (2021) 64 : 16746 -16769
PubMed 34748345 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 8.52 9.53

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4540843 PANCREATIC POLYPEPTIDE 2.0 1 9.53
CHEMBL4856311 1 8.85
CHEMBL4870168 1 7.92
CHEMBL4865048 1 7.77
CHEMBL4873376 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4540843 PANCREATIC POLYPEPTIDE EC50 = 0.2951 nM 9.53
CHEMBL4856311 EC50 = 1.413 nM 8.85
CHEMBL4870168 EC50 = 12.02 nM 7.92
CHEMBL4865048 EC50 = 16.98 nM 7.77
CHEMBL4873376 EC50 = 588843655.36 nM -