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Receptor Internalization Assay from US Patent US10053457: "Hydroxyalkyl-piperazine derivatives as CXCR3 receptor modulators"
Assay data:44 Active, 34 Activity ≤ 1 µM, 44 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
FLIPR Assay from US Patent US10053457: "Hydroxyalkyl-piperazine derivatives as CXCR3 receptor modulators"
Assay data:44 Active, 5 Activity ≤ 1 nM, 44 Activity ≤ 1 µM, 44 Tested
Antagonist activity at human recombinant CXCR3 in human venous blood assessed as receptor internalization measured for 30 mins in presence of CXCL10 by flow cytometric analysis
Assay data:39 Active, 29 Activity ≤ 1 µM, 39 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Antagonist activity at human recombinant CXCR3 expressed in CHO-K1 cells measured after 10 mins in presence of CXCL10 by FLIPR analysis
Assay data:39 Active, 38 Activity ≤ 1 µM, 39 Tested
Antagonist activity at CXCR3 (unknown origin) in presence of CXCL11 by calcium FLIPR assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Antagonist activity at CXCR3 (unknown origin) in presence of CXCL10 by calcium FLIPR assay
Antagonist activity at CXCR3 (unknown origin) in presence of CXCL9 by calcium FLIPR assay
Antagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assay
Assay data:46 Active, 39 Activity ≤ 1 µM, 47 Tested
Inhibition of CXCR3 receptor internalization in human venous whole blood incubated for 30 mins by flow cytometer analysis
Assay data:48 Active, 38 Activity ≤ 1 µM, 49 Tested
Antagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assay
Assay data:57 Active, 55 Activity ≤ 1 µM, 57 Tested
Inhibition of human CXCR3 at 10 uM relative to control
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Antagonist activity against CXCR3 (unknown origin) assessed as inhibition of beta-arrestin 2 recruitment at 10 microM by beta arrestin assay relative to control
Agonist activity against CXCR3 (unknown origin) assessed as induction of beta-arrestin 2 recruitment at 10 microM by beta arrestin assay relative to control
FLIPR Assay from US Patent US9266876: "4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives"
Assay data:243 Active, 61 Activity ≤ 1 nM, 241 Activity ≤ 1 µM, 243 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
FLIPR Assay from US Patent US9090596: "Disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds for use in the treatment of chemokine-mediated pathologies"
Assay data:4 Active, 4 Activity ≤ 1 µM, 4 Tested
Competition Radioligand Binding Assay from US Patent US9073853: "Cycloalkane carboxylic acid derivatives as CXCR3 receptor antagonists"
Assay data:157 Active, 135 Activity ≤ 1 µM, 157 Tested
FLIPR Assay from US Patent US9951063: "8-(piperazin-1-yl)-1,2,3,4-tetrahydro-isoquinoline derivatives"
Assay data:147 Active, 2 Activity ≤ 1 nM, 145 Activity ≤ 1 µM, 147 Tested
In Vitro Affinity Assay from US Patent US9580412: "Disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds for use in the treatment of chemokine-mediated diseases"
Assay data:21 Active, 20 Activity ≤ 1 µM, 21 Tested
Receptor Internalization Assay (RIA) from US Patent US10047080: "(R)-2-methyl-piperazine derivatives as CXCR3 receptor modulators"
Assay data:21 Active, 19 Activity ≤ 1 µM, 21 Tested
FLIPR Assay from US Patent US10047080: "(R)-2-methyl-piperazine derivatives as CXCR3 receptor modulators"
Assay data:21 Active, 3 Activity ≤ 1 nM, 21 Activity ≤ 1 µM, 21 Tested
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