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Assay Detail

CHEMBL4265258

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

Functional
Activation of human Y2R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL ↗
40
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Neuropeptide Y receptor type 2 (CHEMBL4018) ↗
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
EC50 40 8.38 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4281479 — — 2 9.10
CHEMBL4292105 — — 2 9.00
CHEMBL4279794 — — 2 9.00
CHEMBL4277590 — — 2 8.80
CHEMBL4290445 — — 2 8.80
CHEMBL4294418 — — 2 8.70
CHEMBL4284905 — — 2 8.70
CHEMBL4279973 — — 2 8.60
CHEMBL4277676 — — 2 8.30
CHEMBL4283257 — — 2 8.30
CHEMBL4282168 — — 2 8.30
CHEMBL4285633 — — 2 8.10
CHEMBL4281010 — — 2 8.10
CHEMBL4280392 — — 2 8.10
CHEMBL4294277 — — 2 8.00
CHEMBL4287058 — — 2 8.00
CHEMBL4286615 — — 2 7.90
CHEMBL4278700 — — 2 7.80
CHEMBL4288294 — — 2 7.60
CHEMBL4276961 — — 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4281479 — EC50 = 0.7943 nM 9.10
CHEMBL4281479 — EC50 = 0.79 nM 9.10
CHEMBL4292105 — EC50 = 1.0 nM 9.00
CHEMBL4292105 — EC50 = 1.0 nM 9.00
CHEMBL4279794 — EC50 = 1.0 nM 9.00
CHEMBL4279794 — EC50 = 1.0 nM 9.00
CHEMBL4290445 — EC50 = 1.6 nM 8.80
CHEMBL4290445 — EC50 = 1.585 nM 8.80
CHEMBL4277590 — EC50 = 1.6 nM 8.80
CHEMBL4277590 — EC50 = 1.585 nM 8.80
CHEMBL4284905 — EC50 = 1.995 nM 8.70
CHEMBL4294418 — EC50 = 1.995 nM 8.70
CHEMBL4294418 — EC50 = 2.0 nM 8.70
CHEMBL4284905 — EC50 = 2.0 nM 8.70
CHEMBL4279973 — EC50 = 2.512 nM 8.60
CHEMBL4279973 — EC50 = 2.5 nM 8.60
CHEMBL4277676 — EC50 = 5.012 nM 8.30
CHEMBL4277676 — EC50 = 5.0 nM 8.30
CHEMBL4283257 — EC50 = 5.012 nM 8.30
CHEMBL4282168 — EC50 = 5.012 nM 8.30
CHEMBL4283257 — EC50 = 5.0 nM 8.30
CHEMBL4282168 — EC50 = 5.0 nM 8.30
CHEMBL4285633 — EC50 = 7.943 nM 8.10
CHEMBL4280392 — EC50 = 7.943 nM 8.10
CHEMBL4280392 — EC50 = 7.9 nM 8.10
CHEMBL4285633 — EC50 = 7.9 nM 8.10
CHEMBL4281010 — EC50 = 7.943 nM 8.10
CHEMBL4281010 — EC50 = 7.9 nM 8.10
CHEMBL4287058 — EC50 = 10.0 nM 8.00
CHEMBL4294277 — EC50 = 10.0 nM 8.00
CHEMBL4294277 — EC50 = 10.0 nM 8.00
CHEMBL4287058 — EC50 = 10.0 nM 8.00
CHEMBL4286615 — EC50 = 12.59 nM 7.90
CHEMBL4286615 — EC50 = 13.0 nM 7.89
CHEMBL4278700 — EC50 = 15.85 nM 7.80
CHEMBL4278700 — EC50 = 16.0 nM 7.80
CHEMBL4288294 — EC50 = 25.0 nM 7.60
CHEMBL4288294 — EC50 = 25.12 nM 7.60
CHEMBL4276961 — EC50 > 31.62 nM -
CHEMBL4276961 — EC50 > 30.0 nM -