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Cell-Based Luminescent Assay from US Patent US10196369: "Spirocyclic EBI2 modulators"
Assay data:102 Active, 102 Activity ≤ 1 µM, 102 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
PRESTO-Tango GPCRome screening (GPR183)
Assay data:1 Tested
SummaryRelated BioAssays by Target
Agonist activity at Go2-q-coupled EBI2 (unknown origin) expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysis
Assay data:4 Active, 1 Activity ≤ 1 nM, 4 Activity ≤ 1 µM, 4 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Agonist activity at Go2-q-coupled mouse EBI2 expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding at 1 uM preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysis relative to control
Assay data:3 Tested
SummaryPubMed CitationRelated BioAssays by Target
Agonist activity at Go2-q-coupled rat EBI2 expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding at 1 uM preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysis relative to control
Agonist activity at Go2-q-coupled human EBI2 expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding at 1 uM preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysis relative to control
Agonist activity at Go2-q-coupled mouse EBI2 expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysis
Assay data:3 Active, 1 Activity ≤ 1 nM, 3 Activity ≤ 1 µM, 3 Tested
Agonist activity at Go2-q-coupled rat EBI2 expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysis
Assay data:3 Active, 3 Activity ≤ 1 µM, 3 Tested
Agonist activity at Go2-q-coupled human EBI2 expressed in COS7 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 1 hr by scintillation counting analysis
Assay data:3 Active, 2 Activity ≤ 1 nM, 3 Activity ≤ 1 µM, 3 Tested
Antagonist activity at human Gi/o-coupled EBI2 expressed in CHOK1 cells assessed as inhibition of 7alpha,25-ihydroxycholesterol-induced beta-arrestin recruitment at 10 uM measured after 120 mins by beta-galactosidase based PathHunter assay relative to control
Human GPR183 (Class A Orphans)
Assay data:8 Active, 8 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Antagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of oxysterol-induced cell migration after 3 hrs by flow cytometric analysis
Assay data:1 Active, 1 Tested
Antagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of 7-alpha,25-OHC-induced cell migration after 3 hrs by flow cytometric analysis
Assay data:2 Active, 1 Activity ≤ 1 nM, 2 Activity ≤ 1 µM, 2 Tested
Antagonist activity at EBI2 receptor in human U937 cells assessed as inhibition of oxysterol-induced calcium release measured for 3 mins by FLIPR assay
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of 0.1 nM oxysterol-induced [35S]GTPgammaS binding after 1 hr by scintillation counting analysis
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of 0.33 nM oxysterol-induced [35S]GTPgammaS binding after 1 hr by scintillation counting analysis
Inverse agonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of [35S]GTPgammaS binding after 1 hr by scintillation counting analysis
Competitive antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of 7-alpha,25-OHC-induced [35S]GTPgammaS binding after 1 hr by schild plot analysis
Antagonist activity at recombinant mouse EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
Assay data:22 Active, 21 Activity ≤ 1 µM, 22 Tested
Antagonist activity at recombinant human EBI2 receptor expressed in CHO cells assessed as inhibition of NIBR51-induced intracellular calcium release measured for 3 mins by FLIPR assay
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