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Inhibition of recombinant IRAP (unknown origin) expressed in ovalbumin expressing wild type HEK293S cells assessed as decrease in antigen-mediated IL-2 production increase in B3Z T cells pretreated with compound for 1 hr followed by washout and incubated with compound for overnight prior to B3Z T cell addition and measured after 24 hrs by sandwich ELISA assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 2 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of recombinant IRAP (unknown origin) expressed in HEK293S cells using L-AMC as substrate by flourescence assay
Assay data:29 Active, 16 Activity ≤ 1 µM, 36 Tested
Inhibition of recombinant human IRAP expressed in HEK293 cells at 100 uM using L-AMC as substrate preincubated for 30 mins followed by substrate addition measured every 3 mins for 1 hr by flourescence assay relative to control
Assay data:3 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of recombinant human IRAP expressed in HEK293 cells using L-AMC as substrate preincubated for 30 mins followed by substrate addition measured every 3 mins for 1 hr by flourescence assay
Assay data:1 Tested
Binding affinity to recombinant full length human IRAP expressed in HEK293T cells assessed as binding free energy
Assay data:13 Tested
Binding affinity to recombinant full length human IRAP expressed in HEK293T cells using Leu-MCA as substrate
Assay data:6 Active, 7 Activity ≤ 1 µM, 8 Tested
Inhibition of recombinant full length human IRAP expressed in HEK293T cells assessed as substrate cleavage using Leu-MCA as substrate by fluorogenic assay
Assay data:6 Active, 3 Activity ≤ 1 µM, 8 Tested
Competitive inhibition of human IRAP soluble domain expressed in HEK293S GnTI(-) cells assessed as increase in Km with constant Vmax using Arg-AMC as substrate incubated for 2 hrs by fluorescence assay based Michaelis-Menten analysis
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Inhibition of human IRAP soluble domain expressed in HEK293S GnTI(-) cells using Leu-AMC as substrate incubated for 2 hrs by fluorescence based assay
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
Inhibition of human IRAP soluble domain expressed in HEK293S GnTI(-) cells using Arg-AMC as substrate incubated for 2 hrs by fluorescence based assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Competitive inhibition of human recombinant IRAP expressed in baculovirus infected sf9 cells assessed as substrate Kcat using varying levels of L-AMC as substrate incubated for 5 to 10 mins by Michaelis-Menten analysis (Rvb = 0.10 +/- micromol/min/nmol)
Competitive inhibition of human recombinant IRAP expressed in baculovirus infected sf9 cells assessed as substrate Km using varying levels of L-AMC as substrate incubated for 5 to 10 mins by Michaelis-Menten analysis (Rvb = 27 +/- 3 uM)
Competitive inhibition of human recombinant IRAP expressed in baculovirus infected sf9 cells using L-AMC as substrate incubated for 5 to 10 mins by Michaelis-Menten analysis
Assay data:6 Active, 8 Tested
Inhibition of human recombinant IRAP expressed in baculovirus infected Sf9 cells using omniMMP fluorogenic substrate incubated for 5 to 10 mins by fluorescence spectrophotometry analysis
Assay data:4 Active, 10 Tested
Inhibition of recombinant mouse C-terminal His6-tagged IRAP expressed in baculovirus infected BTA-TN-5B1-4 insect cells using L-AMC as substrate measured after 1 hr by fluorescence assay
Assay data:20 Tested
Inhibition of human IRAP at <200 uM preincubated for 20 mins followed by L-leucine-7-amido-4-methylcoumarin addition by fluorescence assay
Activation of IRAP (unknown origin)-mediated Leu-AMC substrate hydrolysis after 60 mins by Rapidfire-MS analysis
Inhibition of human IRAP using L-leucine 7-amido-4-methyl coumarin substrate by microplate fluorescence reader based assay
Assay data:3 Active, 3 Activity ≤ 1 µM, 3 Tested
Inhibition of IRAP in mouse BMDC assessed as blockade of cross-presentation by measuring IL-2 level incubated for 1 day followed by compound wash out and incubated for 6 hrs with yeast cells expressing surface ovalbumin measured 20 hrs post CD8+ T cell-induction by sandwich ELISA method
Inhibition of mouse recombinant IRAP using L-leucine-7-amido-4-methyl coumarin as substrate after 5 to 10 mins by fluorescence assay
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