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Assay Detail

CHEMBL4621607

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Binding
Displacement of [3H]UR-KK200 from human Y4 receptor expressed in CHO cells co-expressing Gqi5-mtAEQ measured after 90 mins by scintillation counting analysis
ChEMBL ↗
62
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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
Ki 62 7.61 9.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4648150 — — 1 9.44
CHEMBL4540843 PANCREATIC POLYPEPTIDE 2.0 2 9.17
CHEMBL4646391 — — 2 8.86
CHEMBL4641831 — — 2 8.79
CHEMBL4649711 — — 2 8.70
CHEMBL4633774 — — 2 8.60
CHEMBL4633593 — — 2 8.47
CHEMBL4639709 — — 2 8.47
CHEMBL4642345 — — 2 8.41
CHEMBL4637617 — — 2 8.40
CHEMBL4643458 — — 2 8.40
CHEMBL4645738 — — 2 8.35
CHEMBL4649438 — — 2 8.13
CHEMBL4645462 — — 2 8.12
CHEMBL4646733 — — 2 8.06
CHEMBL4642752 — — 2 7.85
CHEMBL4632871 — — 2 7.57
CHEMBL4634913 — — 2 7.55
CHEMBL4643341 — — 2 7.51
CHEMBL4641659 — — 2 7.25
CHEMBL4633581 — — 2 7.05
CHEMBL4637810 — — 2 7.03
CHEMBL4640794 — — 2 6.93
CHEMBL4641329 — — 2 6.81
CHEMBL4643522 — — 2 6.73
CHEMBL4639421 — — 2 6.64
CHEMBL4636233 — — 2 6.62
CHEMBL2440199 — — 1 6.47
CHEMBL4646230 — — 2 6.46
CHEMBL4643497 — — 2 5.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4648150 — Ki = 0.36 nM 9.44
CHEMBL4540843 PANCREATIC POLYPEPTIDE Ki = 0.68 nM 9.17
CHEMBL4540843 PANCREATIC POLYPEPTIDE Ki = 0.6918 nM 9.16
CHEMBL4646391 — Ki = 1.38 nM 8.86
CHEMBL4646391 — Ki = 1.4 nM 8.85
CHEMBL4641831 — Ki = 1.622 nM 8.79
CHEMBL4641831 — Ki = 1.7 nM 8.77
CHEMBL4649711 — Ki = 2.0 nM 8.70
CHEMBL4649711 — Ki = 2.042 nM 8.69
CHEMBL4633774 — Ki = 2.512 nM 8.60
CHEMBL4633774 — Ki = 2.8 nM 8.55
CHEMBL4639709 — Ki = 3.4 nM 8.47
CHEMBL4633593 — Ki = 3.4 nM 8.47
CHEMBL4639709 — Ki = 3.388 nM 8.47
CHEMBL4633593 — Ki = 3.715 nM 8.43
CHEMBL4642345 — Ki = 3.9 nM 8.41
CHEMBL4642345 — Ki = 3.89 nM 8.41
CHEMBL4637617 — Ki = 3.981 nM 8.40
CHEMBL4643458 — Ki = 3.981 nM 8.40
CHEMBL4637617 — Ki = 4.0 nM 8.40
CHEMBL4643458 — Ki = 4.3 nM 8.37
CHEMBL4645738 — Ki = 4.467 nM 8.35
CHEMBL4645738 — Ki = 4.8 nM 8.32
CHEMBL4649438 — Ki = 7.4 nM 8.13
CHEMBL4649438 — Ki = 7.413 nM 8.13
CHEMBL4645462 — Ki = 7.586 nM 8.12
CHEMBL4645462 — Ki = 7.9 nM 8.10
CHEMBL4646733 — Ki = 8.71 nM 8.06
CHEMBL4646733 — Ki = 8.9 nM 8.05
CHEMBL4642752 — Ki = 14.13 nM 7.85
CHEMBL4642752 — Ki = 17.0 nM 7.77
CHEMBL4632871 — Ki = 26.92 nM 7.57
CHEMBL4632871 — Ki = 28.0 nM 7.55
CHEMBL4634913 — Ki = 28.18 nM 7.55
CHEMBL4634913 — Ki = 29.0 nM 7.54
CHEMBL4643341 — Ki = 30.9 nM 7.51
CHEMBL4643341 — Ki = 38.0 nM 7.42
CHEMBL4641659 — Ki = 56.23 nM 7.25
CHEMBL4641659 — Ki = 63.0 nM 7.20
CHEMBL4633581 — Ki = 89.13 nM 7.05
CHEMBL4637810 — Ki = 93.0 nM 7.03
CHEMBL4637810 — Ki = 93.33 nM 7.03
CHEMBL4633581 — Ki = 97.0 nM 7.01
CHEMBL4640794 — Ki = 117.49 nM 6.93
CHEMBL4640794 — Ki = 120.0 nM 6.92
CHEMBL4641329 — Ki = 154.88 nM 6.81
CHEMBL4641329 — Ki = 160.0 nM 6.80
CHEMBL4643522 — Ki = 186.21 nM 6.73
CHEMBL4643522 — Ki = 190.0 nM 6.72
CHEMBL4639421 — Ki = 229.09 nM 6.64