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Activation of recombinant human APJ receptor expressed in rat Chem-5 cells assessed as increase in Ca2+ mobilization by FLIPR Calcium 6-QF fluorescent dye based assay
Assay data:13 Active, 13 Activity ≤ 1 µM, 13 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Displacement of [125I]-pyr-1-apelin-13 from EGFP tagged rat apelin receptor expressed in CHO cell membrane incubated for 3 hrs by gamma counter analysis
Assay data:13 Active, 8 Activity ≤ 1 nM, 13 Activity ≤ 1 µM, 13 Tested
[35S]GTPγS Binding from US Patent US11807624: "Substituted pyrimidinones as agonists of the APJ receptor"
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
GPCR beta-arrestin recruitment assay with target: APLNR Assay Type: PRESTO-Tango Concentration: 0.0000004
Assay data:211 Tested
SummaryRelated BioAssays by Target
GPCR beta-arrestin recruitment assay with target: APLNR Assay Type: PRESTO-Tango Concentration: 0.000002
GPCR beta-arrestin recruitment assay with target: APLNR Assay Type: PRESTO-Tango Concentration: 0.00001
Assay data:437 Tested
Agonist activity at human AGTRL1 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment by measuring maximal efficacy incubated for 90 mins by PathHunter assay relative to control
Assay data:2 Tested
SummaryPubMed CitationRelated BioAssays by Target
Agonist activity at human AGTRL1 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assay
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
Agonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization by measuring maximal efficacy at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assay relative to control
Assay data:38 Tested
Agonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assay
Assay data:38 Active, 32 Activity ≤ 1 µM, 47 Tested
Agonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by measuring maximal efficacy after 30 mins by TR-FRET based LANCE cAMP assay relative to control
Assay data:15 Tested
Agonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by TR-FRET based LANCE cAMP assay
Assay data:15 Active, 1 Activity ≤ 1 nM, 15 Activity ≤ 1 µM, 47 Tested
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins and measured by fluorescence based assay
Assay data:15 Active, 6 Activity ≤ 1 nM, 18 Activity ≤ 1 µM, 18 Tested
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production and measured by FLIPR assay
Assay data:1 Active, 1 Activity ≤ 1 nM, 1 Activity ≤ 1 µM, 1 Tested
Binding affinity towards human APJ receptor expressed in HEK293 cell membranes and measured by radioligand binding assay
Displacement of [125I] Apelin-13 from human APJ expressed in HEK293FT cells incubated for 2 hrs by microbeta scintillation counter analysis
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis
Assay data:20 Active, 17 Activity ≤ 1 nM, 20 Activity ≤ 1 µM, 20 Tested
Agonist activity at human APJ expressed in HEK293 cell membrane assessed as maximal efficacy for recruitment of beta-arrestin2 to receptor by BRET-based beta-arrestin2 assay relative to control
Agonist activity at human APJ expressed in HEK293 cell membrane assessed as maximal efficacy for recruitment of PDZ-RhoGEF Galphai1 to cell membrane by BRET-based G protein dissociation assay relative to control
Agonist activity at human APJ expressed in HEK293 cells assessed as maximal efficacy for dissociation of G alphai1 from the G beta gamma subunit by BRET-based G protein dissociation assay relative to control
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