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Assay Detail

CHEMBL4841978

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Functional
Agonist activity at human neuropeptide Y Y4 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment by multimode plate reader
21
Total Activities
21
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 21 7.26 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4873376 1 8.80
CHEMBL4856311 1 8.78
CHEMBL4540843 PANCREATIC POLYPEPTIDE 2.0 1 8.37
CHEMBL4857577 1 8.27
CHEMBL4848958 1 7.89
CHEMBL4874850 1 7.05
CHEMBL4866086 1 7.03
CHEMBL4852799 1 7.02
CHEMBL4633593 1 6.95
CHEMBL4860290 1 6.89
CHEMBL4865048 1 6.85
CHEMBL4863955 1 6.84
CHEMBL4870168 1 6.79
CHEMBL4858915 1 6.75
CHEMBL4862140 1 6.53
CHEMBL4874445 1 6.45
CHEMBL4877802 1 6.12
CHEMBL4866955 1 -
CHEMBL4852354 1 -
CHEMBL4868787 1 -
CHEMBL4861544 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4873376 EC50 = 1.585 nM 8.80
CHEMBL4856311 EC50 = 1.66 nM 8.78
CHEMBL4540843 PANCREATIC POLYPEPTIDE EC50 = 4.266 nM 8.37
CHEMBL4857577 EC50 = 5.37 nM 8.27
CHEMBL4848958 EC50 = 12.88 nM 7.89
CHEMBL4874850 EC50 = 89.13 nM 7.05
CHEMBL4866086 EC50 = 93.33 nM 7.03
CHEMBL4852799 EC50 = 95.5 nM 7.02
CHEMBL4633593 EC50 = 112.2 nM 6.95
CHEMBL4860290 EC50 = 128.82 nM 6.89
CHEMBL4865048 EC50 = 141.25 nM 6.85
CHEMBL4863955 EC50 = 144.54 nM 6.84
CHEMBL4870168 EC50 = 162.18 nM 6.79
CHEMBL4858915 EC50 = 177.83 nM 6.75
CHEMBL4862140 EC50 = 295.12 nM 6.53
CHEMBL4874445 EC50 = 354.81 nM 6.45
CHEMBL4877802 EC50 = 758.58 nM 6.12
CHEMBL4866955 EC50 > 10000.0 nM -
CHEMBL4852354 EC50 > 10000.0 nM -
CHEMBL4868787 EC50 > 10000.0 nM -
CHEMBL4861544 EC50 > 10000.0 nM -