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PRESTO-Tango GPCRome screening (NPY4R)
Assay data:1 Tested
SummaryRelated BioAssays by Target
Intrinsic activity at human neuropeptide Y Y4 receptor expressed in HEK293T cells co-expressing CRE-controlled gene reporter firefly luciferase assessed as relative luminescence measured after 15 mins relative to hPP
Assay data:5 Tested
SummaryPubMed CitationRelated BioAssays by Target
Agonist activity at human neuropeptide Y Y4 receptor expressed in HEK293T cells co-expressing CRE-controlled gene reporter firefly luciferase assessed as relative luminescence measured after 15 mins
Assay data:4 Active, 1 Activity ≤ 1 nM, 4 Activity ≤ 1 µM, 5 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Intrinsic activity at human neuropeptide Y Y4 receptor expressed in CHO-mtAEQ cells co-expressing Gqi5 by calcium aequorin assay
Assay data:21 Tested
Agonist activity at human neuropeptide Y Y4 receptor expressed in CHO-mtAEQ cells co-expressing Gqi5 by calcium aequorin assay
Assay data:15 Active, 1 Activity ≤ 1 nM, 15 Activity ≤ 1 µM, 21 Tested
Intrinsic activity at human neuropeptide Y Y4 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment by multimode plate reader relative to hPP
Agonist activity at human neuropeptide Y Y4 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment by multimode plate reader
Assay data:17 Active, 17 Activity ≤ 1 µM, 21 Tested
Intrinsic activity at human neuropeptide Y Y4 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitment by multimode plate reader relative to hPP
Agonist activity at human neuropeptide Y Y4 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitment by multimode plate reader
Assay data:17 Active, 1 Activity ≤ 1 nM, 17 Activity ≤ 1 µM, 21 Tested
Displacement of [3H]UR-KK200 from human neuropeptide Y Y4 receptor expressed in CHO-mtAEQ cells co-expressing Gqi5 assessed as fold change in affinity measured after 90 mins by scintillation counting analysis relative to Ac-Arg-Tyr-Arg-Leu-Arg-Tyr-NH2
Assay data:19 Tested
Displacement of [3H]UR-KK200 from human neuropeptide Y Y4 receptor expressed in CHO-mtAEQ cells co-expressing Gqi5 measured after 90 mins by scintillation counting analysis
Assay data:21 Active, 6 Activity ≤ 1 nM, 21 Activity ≤ 1 µM, 25 Tested
Displacement of [125I]-PP from human NPY4R expressed in HEK293 cell membranes assessed as remaining radioligand binding incubated for 5 hrs using 180 pM [125I]-PP by microBeta scintillation counting assay
Displacement of [125I]-PP from human NPY4R expressed in HEK293 cell membranes assessed as remaining radioligand binding incubated for 5 hrs using 60 pM [125I]-PP by microBeta scintillation counting assay
Displacement of [125I]-PP from human NPY4R expressed in HEK293 cell membranes incubated for 5 hrs by microBeta scintillation counting assay
Inhibition of 100 nM PP-induced receptor internalization of eYFP-tagged human NPY4R expressed in HEK293 cells at 30 uM after 30 mins by fluorescence microscopy
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Inhibition of 10 nM PP-induced receptor internalization of eYFP-tagged human NPY4R expressed in HEK293 cells at 30 uM after 30 mins by fluorescence microscopy
Inhibition of receptor internalization of eYFP-tagged human NPY4R expressed in HEK293 cells at 30 uM after 30 mins by fluorescence microscopy
Allosteric antagonist activity at human NPY4R expressed in HEK293 cells assessed as reduction in rate of PP-induced arrestin-3 recruitment at 30 uM measured after 30 mins by BRET assay
Allosteric antagonist activity at human NPY4R expressed in HEK293 cells assessed as reduction in PP-induced arrestin-3 recruitment at 30 uM measured after 30 mins by BRET assay
Allosteric antagonist activity at eFYP-tagged human NPY4R expressed in COS7 cells co-expressing Gqi5-alpha assessed as inhibition of PP-induced inositol phosphate accumulation by IP-one assay
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