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Assay Detail

CHEMBL4265256

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Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL ↗
86
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Neuropeptide Y receptor type 5 (CHEMBL4561) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design of Y2 Receptor Selective and Proteolytically Stable PYY3-36 Analogues.
Østergaard S, Kofoed J, Paulsson JF, Madsen KG, Jorgensen R, Wulff BS.
J Med Chem (2018) 61 : 10519 -10530
PubMed 30399314 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 86 6.97 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4284905 — — 2 9.40
CHEMBL4281479 — — 2 9.30
CHEMBL4277590 — — 2 9.20
CHEMBL4286615 — — 2 9.20
CHEMBL4278700 — — 2 8.90
CHEMBL4279973 — — 2 8.80
CHEMBL4292105 — — 2 8.50
CHEMBL4290048 — — 2 8.40
CHEMBL4276961 — — 2 8.00
CHEMBL4287140 — — 2 7.80
CHEMBL4279794 — — 2 7.80
CHEMBL4294277 — — 2 7.60
CHEMBL4290891 — — 2 7.50
CHEMBL4280250 — — 2 7.40
CHEMBL4282616 — — 2 7.30
CHEMBL4277676 — — 2 7.10
CHEMBL4288294 — — 2 7.00
CHEMBL4287469 — — 2 7.00
CHEMBL4285633 — — 2 7.00
CHEMBL4280392 — — 2 6.90
CHEMBL4283846 — — 2 6.80
CHEMBL4289021 — — 2 6.70
CHEMBL4290615 — — 2 6.70
CHEMBL4282216 — — 2 6.60
CHEMBL4283705 — — 2 6.40
CHEMBL4290445 — — 2 6.40
CHEMBL4281010 — — 2 6.20
CHEMBL4279133 — — 2 6.20
CHEMBL4294418 — — 2 6.10
CHEMBL4287058 — — 2 6.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4284905 — Ki = 0.4 nM 9.40
CHEMBL4284905 — Ki = 0.3981 nM 9.40
CHEMBL4281479 — Ki = 0.5012 nM 9.30
CHEMBL4281479 — Ki = 0.5 nM 9.30
CHEMBL4277590 — Ki = 0.631 nM 9.20
CHEMBL4277590 — Ki = 0.63 nM 9.20
CHEMBL4286615 — Ki = 0.631 nM 9.20
CHEMBL4286615 — Ki = 0.63 nM 9.20
CHEMBL4278700 — Ki = 1.259 nM 8.90
CHEMBL4278700 — Ki = 1.3 nM 8.89
CHEMBL4279973 — Ki = 1.6 nM 8.80
CHEMBL4279973 — Ki = 1.585 nM 8.80
CHEMBL4292105 — Ki = 3.162 nM 8.50
CHEMBL4292105 — Ki = 3.2 nM 8.49
CHEMBL4290048 — Ki = 3.981 nM 8.40
CHEMBL4290048 — Ki = 4.0 nM 8.40
CHEMBL4276961 — Ki = 10.0 nM 8.00
CHEMBL4276961 — Ki = 10.0 nM 8.00
CHEMBL4287140 — Ki = 15.85 nM 7.80
CHEMBL4287140 — Ki = 16.0 nM 7.80
CHEMBL4279794 — Ki = 16.0 nM 7.80
CHEMBL4279794 — Ki = 15.85 nM 7.80
CHEMBL4294277 — Ki = 25.12 nM 7.60
CHEMBL4294277 — Ki = 25.0 nM 7.60
CHEMBL4290891 — Ki = 32.0 nM 7.50
CHEMBL4290891 — Ki = 31.62 nM 7.50
CHEMBL4280250 — Ki = 39.81 nM 7.40
CHEMBL4280250 — Ki = 40.0 nM 7.40
CHEMBL4282616 — Ki = 50.12 nM 7.30
CHEMBL4282616 — Ki = 50.0 nM 7.30
CHEMBL4277676 — Ki = 79.0 nM 7.10
CHEMBL4277676 — Ki = 79.43 nM 7.10
CHEMBL4285633 — Ki = 100.0 nM 7.00
CHEMBL4287469 — Ki = 100.0 nM 7.00
CHEMBL4287469 — Ki = 100.0 nM 7.00
CHEMBL4288294 — Ki = 100.0 nM 7.00
CHEMBL4288294 — Ki = 100.0 nM 7.00
CHEMBL4285633 — Ki = 100.0 nM 7.00
CHEMBL4280392 — Ki = 125.89 nM 6.90
CHEMBL4280392 — Ki = 130.0 nM 6.89
CHEMBL4283846 — Ki = 160.0 nM 6.80
CHEMBL4283846 — Ki = 158.49 nM 6.80
CHEMBL4289021 — Ki = 200.0 nM 6.70
CHEMBL4289021 — Ki = 199.53 nM 6.70
CHEMBL4290615 — Ki = 200.0 nM 6.70
CHEMBL4290615 — Ki = 199.53 nM 6.70
CHEMBL4282216 — Ki = 251.19 nM 6.60
CHEMBL4282216 — Ki = 250.0 nM 6.60
CHEMBL4290445 — Ki = 398.11 nM 6.40
CHEMBL4290445 — Ki = 400.0 nM 6.40