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Binding affinity to wild type human CXCR2 assessed as dissociation constant
Assay data:2 Active, 2 Activity ≤ 1 µM, 3 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of wild type CXCR2 (unknown origin)
Assay data:1 Active, 1 Activity ≤ 1 µM, 2 Tested
Antagonist activity at CXCR2 (unknown origin)
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
Inhibition of human CXCR2-mediated chemotaxis expressed in mouse BaF3 cells
Binding affinity to human CXCR2 assessed as dissociation constant incubated for 6 to 24 hrs by radioligand binding assay
Assay data:1 Active, 1 Activity ≤ 1 nM, 1 Activity ≤ 1 µM, 1 Tested
Binding affinity to human CXCR2 expressed in human U87 cells assessed as inhibition of CXCL8 AF647-induced calcium response incubated for 10 mins followed by addition of CXCL8 AF647 measured by FLIPR Tetra system method
Assay data:7 Active, 5 Activity ≤ 1 µM, 16 Tested
Binding affinity to human CXCR2 expressed in human U87 cells assessed as inhibition of CXCL8 AF647-binding incubated for 15 mins followed by addition of CXCL8 AF647 measured after 30 mins by flow cytometry analysis
Assay data:9 Active, 6 Activity ≤ 1 µM, 16 Tested
Chemokine CXCR2 (IL-8RB) Eurofins-Panlabs radioligand binding assay
Assay data:1 Tested
SummaryRelated BioAssays by Target
IL-8B (h) (CXCR2) CEREP panel
Inhibition of human CXCR2 at 10 uM relative to control
SummaryPubMed CitationRelated BioAssays by Target
Antagonist activity against CXCR2 (unknown origin) assessed as inhibition of beta-arrestin 2 recruitment at 10 microM by beta arrestin assay relative to control
Agonist activity against CXCR2 (unknown origin) assessed as induction of beta-arrestin 2 recruitment at 10 microM by beta arrestin assay relative to control
Displacement of [I-125]-interleukin-8 against human recombinant CXCR2 expressed in CHO-K1 cells incubated for 60 mins by radio ligand binding assay
Assay data:2 Active, 1 Activity ≤ 1 µM, 2 Tested
Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assay
Assay data:32 Active, 19 Activity ≤ 1 µM, 35 Tested
Antagonist activity against CXCR2 (unknown origin) by calcium flux assay
Antagonist activity at CXCR2 (unknown origin) at 10 uM by calcium flux assay relative to control
Assay data:22 Tested
Inhibition Assay from US Patent US11136315: "CXCR2 antagonist"
Assay data:35 Active, 35 Activity ≤ 1 µM, 35 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
In Vitro Assay from US Patent USRE48547: "Aminopyrimidinecarboxamides as CXCR2 modulators"
Assay data:6 Active, 4 Activity ≤ 1 µM, 6 Tested
In Vitro Affinity Assay from US Patent US10647706: "Chemokine CXCR1 and CXCR2 receptor antagonist compounds, and use thereof in the treatment of chemokine-mediated pathologies"
Assay data:6 Active, 14 Activity ≤ 1 µM, 14 Tested
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