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Assay Detail

CHEMBL4478045

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Functional
Agonist activity at human NPY Y4 receptor expressed in CHO cells co-expressing Gqi5-mtAEQ assessed as induction of calcium mobilization by aequorin luminescence assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

High Affinity Agonists of the Neuropeptide Y (NPY) Y4 Receptor Derived from the C-Terminal Pentapeptide of Human Pancreatic Polypeptide (hPP): Synthesis, Stereochemical Discrimination, and Radiolabeling.
Kuhn KK, Ertl T, Dukorn S, Keller M, Bernhardt G, Reiser O, Buschauer A.
J Med Chem (2016) 59 : 6045 -6058
PubMed 27223253 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 13 7.59 8.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3787712 1 8.19
CHEMBL4456247 1 8.16
CHEMBL409762 1 8.07
CHEMBL4540843 PANCREATIC POLYPEPTIDE 2.0 1 8.01
CHEMBL3787713 1 7.89
CHEMBL4522438 1 7.85
CHEMBL4475071 1 7.75
CHEMBL3787766 1 7.31
CHEMBL4549208 1 7.23
CHEMBL4581256 1 6.54
CHEMBL4533775 1 6.51
CHEMBL4581302 1 -
CHEMBL4576579 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3787712 EC50 = 6.4 nM 8.19
CHEMBL4456247 EC50 = 6.9 nM 8.16
CHEMBL409762 EC50 = 8.5 nM 8.07
CHEMBL4540843 PANCREATIC POLYPEPTIDE EC50 = 9.7 nM 8.01
CHEMBL3787713 EC50 = 13.0 nM 7.89
CHEMBL4522438 EC50 = 14.0 nM 7.85
CHEMBL4475071 EC50 = 18.0 nM 7.75
CHEMBL3787766 EC50 = 49.0 nM 7.31
CHEMBL4549208 EC50 = 59.0 nM 7.23
CHEMBL4581256 EC50 = 290.0 nM 6.54
CHEMBL4533775 EC50 = 310.0 nM 6.51
CHEMBL4581302 EC50 > 3000.0 nM -
CHEMBL4576579 EC50 > 3000.0 nM -