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Assay Detail

CHEMBL4265253

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Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y1R expressed in BHK-21 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 BHK-21
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Neuropeptide Y receptor type 1 (CHEMBL4777) ↗
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 6.47 9.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4281479 — — 2 9.90
CHEMBL4284905 — — 2 9.60
CHEMBL4279973 — — 2 9.40
CHEMBL4286615 — — 2 9.10
CHEMBL4290048 — — 2 8.40
CHEMBL4287140 — — 2 7.90
CHEMBL4292105 — — 2 7.40
CHEMBL4278700 — — 2 7.40
CHEMBL4276961 — — 2 7.30
CHEMBL4294277 — — 2 6.80
CHEMBL4283705 — — 2 6.70
CHEMBL439122 — — 2 6.40
CHEMBL4279794 — — 2 6.40
CHEMBL4280392 — — 2 6.30
CHEMBL4281010 — — 2 6.30
CHEMBL4277590 — — 2 6.20
CHEMBL4277676 — — 2 6.20
CHEMBL4277697 — — 2 6.00
CHEMBL4294418 — — 2 5.90
CHEMBL4289021 — — 2 5.90
CHEMBL4283846 — — 2 5.80
CHEMBL4282216 — — 2 5.70
CHEMBL4290615 — — 2 5.60
CHEMBL4290445 — — 2 5.60
CHEMBL4288294 — — 2 5.40
CHEMBL4279133 — — 2 5.40
CHEMBL4282616 — — 2 5.30
CHEMBL4291016 — — 2 5.30
CHEMBL4287058 — — 2 5.20
CHEMBL4290891 — — 2 5.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4281479 — Ki = 0.1259 nM 9.90
CHEMBL4281479 — Ki = 0.13 nM 9.89
CHEMBL4284905 — Ki = 0.2512 nM 9.60
CHEMBL4284905 — Ki = 0.25 nM 9.60
CHEMBL4279973 — Ki = 0.3981 nM 9.40
CHEMBL4279973 — Ki = 0.4 nM 9.40
CHEMBL4286615 — Ki = 0.79 nM 9.10
CHEMBL4286615 — Ki = 0.7943 nM 9.10
CHEMBL4290048 — Ki = 4.0 nM 8.40
CHEMBL4290048 — Ki = 3.981 nM 8.40
CHEMBL4287140 — Ki = 12.59 nM 7.90
CHEMBL4287140 — Ki = 13.0 nM 7.89
CHEMBL4292105 — Ki = 39.81 nM 7.40
CHEMBL4292105 — Ki = 40.0 nM 7.40
CHEMBL4278700 — Ki = 39.81 nM 7.40
CHEMBL4278700 — Ki = 40.0 nM 7.40
CHEMBL4276961 — Ki = 50.0 nM 7.30
CHEMBL4276961 — Ki = 50.12 nM 7.30
CHEMBL4294277 — Ki = 160.0 nM 6.80
CHEMBL4294277 — Ki = 158.49 nM 6.80
CHEMBL4283705 — Ki = 200.0 nM 6.70
CHEMBL4283705 — Ki = 199.53 nM 6.70
CHEMBL4279794 — Ki = 400.0 nM 6.40
CHEMBL4279794 — Ki = 398.11 nM 6.40
CHEMBL439122 — Ki = 400.0 nM 6.40
CHEMBL439122 — Ki = 398.11 nM 6.40
CHEMBL4280392 — Ki = 500.0 nM 6.30
CHEMBL4281010 — Ki = 500.0 nM 6.30
CHEMBL4281010 — Ki = 501.19 nM 6.30
CHEMBL4280392 — Ki = 501.19 nM 6.30
CHEMBL4277590 — Ki = 630.0 nM 6.20
CHEMBL4277590 — Ki = 630.96 nM 6.20
CHEMBL4277676 — Ki = 630.96 nM 6.20
CHEMBL4277676 — Ki = 630.0 nM 6.20
CHEMBL4277697 — Ki = 1000.0 nM 6.00
CHEMBL4277697 — Ki = 1000.0 nM 6.00
CHEMBL4289021 — Ki = 1258.93 nM 5.90
CHEMBL4294418 — Ki = 1258.93 nM 5.90
CHEMBL4294418 — Ki = 1300.0 nM 5.89
CHEMBL4289021 — Ki = 1300.0 nM 5.89
CHEMBL4283846 — Ki = 1600.0 nM 5.80
CHEMBL4283846 — Ki = 1584.89 nM 5.80
CHEMBL4282216 — Ki = 1995.26 nM 5.70
CHEMBL4282216 — Ki = 2000.0 nM 5.70
CHEMBL4290615 — Ki = 2511.89 nM 5.60
CHEMBL4290615 — Ki = 2500.0 nM 5.60
CHEMBL4290445 — Ki = 2511.89 nM 5.60
CHEMBL4290445 — Ki = 2500.0 nM 5.60
CHEMBL4288294 — Ki = 4000.0 nM 5.40
CHEMBL4279133 — Ki = 4000.0 nM 5.40