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Antagonist activity at CCR2 (unknown origin)
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of wild type CCR2 mutant (unknown origin)
Assay data:4 Active, 4 Activity ≤ 1 µM, 6 Tested
Binding affinity to CCR2 (unknown origin) assessed as dissociation constant
Assay data:1 Active, 1 Activity ≤ 1 nM, 1 Activity ≤ 1 µM, 1 Tested
Binding affinity to CCR2 (unknown origin) assessed as inhibition constant
Assay data:6 Active, 6 Activity ≤ 1 µM, 6 Tested
Inhibition of CCR2 (unknown origin) at 10 uM relative to control
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Antagonist activity at CCR2b in human Tango CCR2-bla U2OS cells using FRET B/G as substrate assessed as inhibition of CCL2- induced beta-arrestin recruitment at 1 uM incubated for 30 mins followed by CCL2 addition and measured after 16 hrs by fluorescence based analysis relative to control
Assay data:4 Tested
Displacement of [3H]-CCR2-RA-[R] from CCR2b in human Tango CCR2-bla U2OS cell membranes at 1 uM by scintillation spectrometry analysis
Antagonist activity against CCR2 (unknown origin) assessed as inhibition of beta-arrestin 2 recruitment at 10 microM by beta arrestin assay relative to control
Agonist activity against CCR2 (unknown origin) assessed as induction of beta-arrestin 2 recruitment at 10 microM by beta arrestin assay relative to control
Binding Assay from US Patent US8921559: "4-substituted-cyclohexylamino-4-piperidinyl-acetamide antagonists of CCR2"
Assay data:53 Active, 52 Activity ≤ 1 µM, 53 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Radioligand Binding Assay from US Patent US8906911: "Chemokine receptor antagonists"
Assay data:62 Active, 43 Activity ≤ 1 µM, 68 Tested
Binding Assay from US Patent US8822460: "Fused cyclopentyl antagonists of CCR2"
Assay data:10 Active, 10 Activity ≤ 1 µM, 10 Tested
Biological Assay from US Patent US9663460: "Sulfur derivatives as chemokine receptor modulators"
Assay data:209 Active, 159 Activity ≤ 1 µM, 209 Tested
FLIPR Assay from US Patent US9603834: "1,2- bis-sulfonamide derivatives as chemokine receptor modulators"
Assay data:26 Active, 26 Activity ≤ 1 µM, 26 Tested
Chemokine CCR2B Eurofins-Panlabs radioligand binding assay
SummaryRelated BioAssays by Target
PRESTO-Tango GPCRome screening (CCR2)
CCR2/H AG Cerep selectivity data (BI)
Antagonist activity at CCR2 in human whole blood assessed as inhibition of CCL2-induced CD11b upregulation
Assay data:2 Active, 2 Activity ≤ 1 µM, 3 Tested
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