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Assay Detail

CHEMBL5335577

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Binding
Agonist potency at human Y4 receptor expressed in HEK293T-NlucN-mGSi/Y4R-NlucC cells by miniGsi protein recruitment assay
11
Total Activities
8
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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

Stereochemistry-Driven Interactions of α,γ-Peptide Ligands with the Neuropeptide Y Y<sub>4</sub>-Receptor.
Plut E, Calderón JC, Stanojlović V, Gattor AO, Höring C, Humphrys LJ, Konieczny A, Kerres S, Schubert M, Keller M, Cabrele C, Clark T, Reiser O.
J Med Chem (2023) 66 : 9642 -9657
PubMed 37440703 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 7.38 9.00
pEC50 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4856311 1 9.00
CHEMBL4873376 1 8.77
CHEMBL5426658 2 7.73
CHEMBL4633593 2 6.98
CHEMBL4639709 1 6.77
CHEMBL5418083 2 6.33
CHEMBL5431678 1 -
CHEMBL5434829 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4856311 EC50 = 1.0 nM 9.00
CHEMBL4873376 EC50 = 1.7 nM 8.77
CHEMBL5426658 EC50 = 18.62 nM 7.73
CHEMBL5426658 EC50 = 20.0 nM 7.70
CHEMBL4633593 EC50 = 104.71 nM 6.98
CHEMBL4633593 EC50 = 110.0 nM 6.96
CHEMBL4639709 EC50 = 170.0 nM 6.77
CHEMBL5418083 EC50 = 467.74 nM 6.33
CHEMBL5418083 EC50 = 610.0 nM 6.21
CHEMBL5431678 pEC50 - -
CHEMBL5434829 pEC50 - -