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Assay Detail

CHEMBL4621614

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Binding
Agonist activity at human Y4R expressed in HEK293T cells co-expressing ARRB1 assessed as induction of beta-arrestin1 recruitment measured for 40 mins by D-luciferin based luminescence assay
ChEMBL ↗
50
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK-293T
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 50 6.64 8.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4540843 PANCREATIC POLYPEPTIDE 2.0 2 8.66
CHEMBL4649711 — — 2 7.29
CHEMBL4646391 — — 2 7.17
CHEMBL4645738 — — 2 7.00
CHEMBL4633774 — — 2 6.80
CHEMBL4641831 — — 2 6.80
CHEMBL4633593 — — 2 6.79
CHEMBL4643458 — — 2 6.77
CHEMBL4645462 — — 2 6.75
CHEMBL4639709 — — 2 6.56
CHEMBL4637617 — — 2 6.34
CHEMBL4643341 — — 2 6.28
CHEMBL4646733 — — 2 6.26
CHEMBL4642752 — — 2 6.22
CHEMBL4641659 — — 2 5.97
CHEMBL4649438 — — 2 5.62
CHEMBL4642345 — — 2 5.61
CHEMBL4640794 — — 2 -
CHEMBL4639421 — — 2 -
CHEMBL4643522 — — 2 -
CHEMBL4643863 — — 2 -
CHEMBL4646230 — — 2 -
CHEMBL4637810 — — 2 -
CHEMBL4643497 — — 2 -
CHEMBL4643154 — — 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4540843 PANCREATIC POLYPEPTIDE EC50 = 2.188 nM 8.66
CHEMBL4540843 PANCREATIC POLYPEPTIDE EC50 = 2.4 nM 8.62
CHEMBL4649711 — EC50 = 51.0 nM 7.29
CHEMBL4649711 — EC50 = 51.29 nM 7.29
CHEMBL4646391 — EC50 = 67.0 nM 7.17
CHEMBL4646391 — EC50 = 67.61 nM 7.17
CHEMBL4645738 — EC50 = 100.0 nM 7.00
CHEMBL4645738 — EC50 = 100.0 nM 7.00
CHEMBL4633774 — EC50 = 160.0 nM 6.80
CHEMBL4641831 — EC50 = 160.0 nM 6.80
CHEMBL4633593 — EC50 = 162.18 nM 6.79
CHEMBL4633774 — EC50 = 162.18 nM 6.79
CHEMBL4641831 — EC50 = 165.96 nM 6.78
CHEMBL4643458 — EC50 = 169.82 nM 6.77
CHEMBL4643458 — EC50 = 170.0 nM 6.77
CHEMBL4633593 — EC50 = 170.0 nM 6.77
CHEMBL4645462 — EC50 = 180.0 nM 6.75
CHEMBL4645462 — EC50 = 181.97 nM 6.74
CHEMBL4639709 — EC50 = 275.42 nM 6.56
CHEMBL4639709 — EC50 = 280.0 nM 6.55
CHEMBL4637617 — EC50 = 457.09 nM 6.34
CHEMBL4637617 — EC50 = 460.0 nM 6.34
CHEMBL4643341 — EC50 = 524.81 nM 6.28
CHEMBL4643341 — EC50 = 520.0 nM 6.28
CHEMBL4646733 — EC50 = 549.54 nM 6.26
CHEMBL4646733 — EC50 = 550.0 nM 6.26
CHEMBL4642752 — EC50 = 602.56 nM 6.22
CHEMBL4642752 — EC50 = 600.0 nM 6.22
CHEMBL4641659 — EC50 = 1071.52 nM 5.97
CHEMBL4641659 — EC50 = 1070.0 nM 5.97
CHEMBL4649438 — EC50 = 2400.0 nM 5.62
CHEMBL4649438 — EC50 = 2398.83 nM 5.62
CHEMBL4642345 — EC50 = 2454.71 nM 5.61
CHEMBL4642345 — EC50 = 2500.0 nM 5.60
CHEMBL4646230 — EC50 > 31622.78 nM -
CHEMBL4643154 — EC50 > 30000.0 nM -
CHEMBL4643497 — EC50 > 30000.0 nM -
CHEMBL4637810 — EC50 > 30000.0 nM -
CHEMBL4637810 — EC50 > 31622.78 nM -
CHEMBL4646230 — EC50 > 30000.0 nM -
CHEMBL4643497 — EC50 > 31622.78 nM -
CHEMBL4643154 — EC50 > 31622.78 nM -
CHEMBL4643863 — EC50 > 30000.0 nM -
CHEMBL4643863 — EC50 > 31622.78 nM -
CHEMBL4643522 — EC50 > 31622.78 nM -
CHEMBL4643522 — EC50 > 30000.0 nM -
CHEMBL4639421 — EC50 > 30000.0 nM -
CHEMBL4640794 — EC50 > 31622.78 nM -
CHEMBL4640794 — EC50 > 30000.0 nM -
CHEMBL4639421 — EC50 > 31622.78 nM -