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Agonist activity at N-terminal GST tagged human RORgamma LBD assessed as maximal efficacy using fluorescein-D22 as coactivator incubated for 60 mins by Lanthascreen TR-FRET assay relative to control
Assay data:11 Tested
SummaryPubMed CitationRelated BioAssays by Target
ThermoFluor Assay from US Patent US10975068: "6-aminopyridin-3-yl thiazoles as modulators of RORγT"
Assay data:439 Active, 105 Activity ≤ 1 nM, 438 Activity ≤ 1 µM, 440 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Inverse agonist activity at APC-labelled RORgammat (unknown origin) assessed as inhibition of biotinylated SRC recruitment measured after 1 hr by dual FRET assay
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Binding affinity to human N-terminal His6-tagged RORgamma (262 to 507 residues) expressed in Escherichia coli BL21 (DE3) by isothermal titration calorimetry
Assay data:3 Active, 3 Activity ≤ 1 µM, 3 Tested
Inverse agonist activity at GAL4-DNA binding domain-fused human RORgammat LBD expressed in pGL4.31 transfected HEK293T cells assessed as inhibition of RORGgammat driven transcriptional activity after 24 hrs by dual-luciferase reporter gene assay
Assay data:19 Active, 18 Activity ≤ 1 µM, 20 Tested
Antagonist activity at full-length RORgamma (unknown origin) expressed in 293T cells at 10 uM after 24 hrs by luciferase reporter gene assay relative to control
Assay data:66 Tested
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