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Assay Detail

CHEMBL4621618

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Functional
Agonist activity at human Y4 receptor expressed in CHO cells co-expressing Gqi5-mtAEQ assessed as intracellular calcium mobilization measured for 43 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL ↗
50
Total Activities
25
Compounds Tested
2
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

Oligopeptides as Neuropeptide Y Y4 Receptor Ligands: Identification of a High-Affinity Tetrapeptide Agonist and a Hexapeptide Antagonist.
Konieczny A, Braun D, Wifling D, Bernhardt G, Keller M.
J Med Chem (2020) 63 : 8198 -8215
PubMed 32614182 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 43 6.58 7.97
pEC50 7 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4540843 PANCREATIC POLYPEPTIDE 2.0 2 7.97
CHEMBL4649711 — — 2 7.00
CHEMBL4633774 — — 2 6.97
CHEMBL4646391 — — 2 6.93
CHEMBL4633593 — — 2 6.74
CHEMBL4643458 — — 2 6.64
CHEMBL4641831 — — 2 6.61
CHEMBL4643341 — — 2 6.42
CHEMBL4639709 — — 2 6.36
CHEMBL4646733 — — 2 6.26
CHEMBL4637617 — — 2 6.21
CHEMBL4645462 — — 2 5.92
CHEMBL4642752 — — 2 5.60
CHEMBL4641659 — — 2 -
CHEMBL4640794 — — 2 -
CHEMBL4645738 — — 2 -
CHEMBL4639421 — — 2 -
CHEMBL4643522 — — 2 -
CHEMBL4643863 — — 2 -
CHEMBL4646230 — — 2 -
CHEMBL4649438 — — 2 -
CHEMBL4637810 — — 2 -
CHEMBL4643497 — — 2 -
CHEMBL4643154 — — 2 -
CHEMBL4642345 — — 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4540843 PANCREATIC POLYPEPTIDE EC50 = 10.6 nM 7.97
CHEMBL4540843 PANCREATIC POLYPEPTIDE EC50 = 10.96 nM 7.96
CHEMBL4649711 — EC50 = 100.0 nM 7.00
CHEMBL4649711 — EC50 = 102.33 nM 6.99
CHEMBL4633774 — EC50 = 107.15 nM 6.97
CHEMBL4633774 — EC50 = 110.0 nM 6.96
CHEMBL4646391 — EC50 = 117.49 nM 6.93
CHEMBL4646391 — EC50 = 120.0 nM 6.92
CHEMBL4633593 — EC50 = 181.97 nM 6.74
CHEMBL4633593 — EC50 = 190.0 nM 6.72
CHEMBL4643458 — EC50 = 230.0 nM 6.64
CHEMBL4643458 — EC50 = 234.42 nM 6.63
CHEMBL4641831 — EC50 = 245.47 nM 6.61
CHEMBL4641831 — EC50 = 250.0 nM 6.60
CHEMBL4643341 — EC50 = 380.0 nM 6.42
CHEMBL4643341 — EC50 = 380.19 nM 6.42
CHEMBL4639709 — EC50 = 436.52 nM 6.36
CHEMBL4639709 — EC50 = 440.0 nM 6.36
CHEMBL4646733 — EC50 = 549.54 nM 6.26
CHEMBL4646733 — EC50 = 550.0 nM 6.26
CHEMBL4637617 — EC50 = 616.6 nM 6.21
CHEMBL4637617 — EC50 = 620.0 nM 6.21
CHEMBL4645462 — EC50 = 1202.26 nM 5.92
CHEMBL4645462 — EC50 = 1200.0 nM 5.92
CHEMBL4642752 — EC50 = 2500.0 nM 5.60
CHEMBL4642752 — EC50 = 2511.89 nM 5.60
CHEMBL4645738 — EC50 - — -
CHEMBL4640794 — EC50 > 31622.78 nM -
CHEMBL4646230 — EC50 > 31622.78 nM -
CHEMBL4649438 — pEC50 - — -
CHEMBL4637810 — pEC50 - — -
CHEMBL4643497 — pEC50 - — -
CHEMBL4643154 — pEC50 - — -
CHEMBL4642345 — pEC50 - — -
CHEMBL4645738 — pEC50 - — -
CHEMBL4639421 — EC50 > 31622.78 nM -
CHEMBL4643863 — EC50 > 30000.0 nM -
CHEMBL4643522 — EC50 > 30000.0 nM -
CHEMBL4639421 — EC50 > 30000.0 nM -
CHEMBL4640794 — EC50 > 30000.0 nM -
CHEMBL4641659 — EC50 - — -
CHEMBL4643522 — EC50 > 31622.78 nM -
CHEMBL4642345 — EC50 - — -
CHEMBL4643863 — EC50 > 31622.78 nM -
CHEMBL4641659 — pEC50 - — -
CHEMBL4643154 — EC50 - — -
CHEMBL4646230 — EC50 > 30000.0 nM -
CHEMBL4649438 — EC50 - — -
CHEMBL4637810 — EC50 - — -
CHEMBL4643497 — EC50 - — -