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Assay Detail

CHEMBL4265255

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [125I]-PP from human Y4R expressed in CHO-K1 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 CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Neuropeptide Y receptor type 4 (CHEMBL4877) ↗
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 7.01 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4286615 — — 2 11.00
CHEMBL4276961 — — 2 11.00
CHEMBL4278700 — — 2 10.00
CHEMBL4290048 — — 2 9.80
CHEMBL4279973 — — 2 9.80
CHEMBL4281479 — — 2 9.10
CHEMBL4287140 — — 2 8.80
CHEMBL4284905 — — 2 8.60
CHEMBL4282216 — — 2 8.20
CHEMBL4292105 — — 2 7.90
CHEMBL4279794 — — 2 7.80
CHEMBL4281010 — — 2 7.60
CHEMBL4294418 — — 2 7.30
CHEMBL4289021 — — 2 7.30
CHEMBL4277697 — — 2 7.20
CHEMBL4291016 — — 2 7.00
CHEMBL4294277 — — 2 7.00
CHEMBL4283705 — — 2 6.90
CHEMBL4287469 — — 2 6.90
CHEMBL439122 — — 2 6.70
CHEMBL4282616 — — 2 6.70
CHEMBL4277590 — — 2 6.50
CHEMBL4290615 — — 2 6.50
CHEMBL4290488 — — 2 6.30
CHEMBL4280898 — — 2 6.20
CHEMBL4282168 — — 2 6.20
CHEMBL4280392 — — 2 6.20
CHEMBL4290445 — — 2 6.10
CHEMBL4277676 — — 2 6.10
CHEMBL4281120 — — 2 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4276961 — Ki = 0.01 nM 11.00
CHEMBL4276961 — Ki = 0.01 nM 11.00
CHEMBL4286615 — Ki = 0.01 nM 11.00
CHEMBL4286615 — Ki = 0.01 nM 11.00
CHEMBL4278700 — Ki = 0.1 nM 10.00
CHEMBL4278700 — Ki = 0.1 nM 10.00
CHEMBL4279973 — Ki = 0.1585 nM 9.80
CHEMBL4279973 — Ki = 0.16 nM 9.80
CHEMBL4290048 — Ki = 0.1585 nM 9.80
CHEMBL4290048 — Ki = 0.16 nM 9.80
CHEMBL4281479 — Ki = 0.79 nM 9.10
CHEMBL4281479 — Ki = 0.7943 nM 9.10
CHEMBL4287140 — Ki = 1.6 nM 8.80
CHEMBL4287140 — Ki = 1.585 nM 8.80
CHEMBL4284905 — Ki = 2.512 nM 8.60
CHEMBL4284905 — Ki = 2.5 nM 8.60
CHEMBL4282216 — Ki = 6.31 nM 8.20
CHEMBL4282216 — Ki = 6.3 nM 8.20
CHEMBL4292105 — Ki = 12.59 nM 7.90
CHEMBL4292105 — Ki = 13.0 nM 7.89
CHEMBL4279794 — Ki = 15.85 nM 7.80
CHEMBL4279794 — Ki = 16.0 nM 7.80
CHEMBL4281010 — Ki = 25.0 nM 7.60
CHEMBL4281010 — Ki = 25.12 nM 7.60
CHEMBL4289021 — Ki = 50.0 nM 7.30
CHEMBL4294418 — Ki = 50.12 nM 7.30
CHEMBL4294418 — Ki = 50.0 nM 7.30
CHEMBL4289021 — Ki = 50.12 nM 7.30
CHEMBL4277697 — Ki = 63.1 nM 7.20
CHEMBL4277697 — Ki = 63.0 nM 7.20
CHEMBL4291016 — Ki = 100.0 nM 7.00
CHEMBL4291016 — Ki = 100.0 nM 7.00
CHEMBL4294277 — Ki = 100.0 nM 7.00
CHEMBL4294277 — Ki = 100.0 nM 7.00
CHEMBL4283705 — Ki = 125.89 nM 6.90
CHEMBL4287469 — Ki = 125.89 nM 6.90
CHEMBL4287469 — Ki = 130.0 nM 6.89
CHEMBL4283705 — Ki = 130.0 nM 6.89
CHEMBL4282616 — Ki = 200.0 nM 6.70
CHEMBL4282616 — Ki = 199.53 nM 6.70
CHEMBL439122 — Ki = 200.0 nM 6.70
CHEMBL439122 — Ki = 199.53 nM 6.70
CHEMBL4277590 — Ki = 316.23 nM 6.50
CHEMBL4277590 — Ki = 320.0 nM 6.50
CHEMBL4290615 — Ki = 320.0 nM 6.50
CHEMBL4290615 — Ki = 316.23 nM 6.50
CHEMBL4290488 — Ki = 501.19 nM 6.30
CHEMBL4290488 — Ki = 500.0 nM 6.30
CHEMBL4280392 — Ki = 630.0 nM 6.20
CHEMBL4280392 — Ki = 630.96 nM 6.20