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Antagonist activity at human CCR2 expressed in human U2OS cell membranes as [35S]GTPgammaS binding level at 600 nM pre-incubated for 30 mins followed by drug wash out before CCL2 stimulation and followed by further incubation for 90 mins by scintillation counting method relative to control
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inverse agonist activity at human CCR2 assessed as reduction in [35S]GTPgammaS binding at 1 uM relative to control
Assay data:2 Tested
Antagonist activity at CCR2 receptor (unknown origin) by [35S]GTPgammaS binding assay
Antagonist activity at CCR2 (unknown origin) assessed as reduction of MCP1-induced calcium flux
Assay data:2 Active, 2 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Displacement of 125I-MCP1 from human CCR2 receptor expressed in human HEK cell membrane
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
Assay data:20 Active, 20 Activity ≤ 1 µM, 20 Tested
Antagonist activity at human CCR2 by whole blood assay
Assay data:22 Active, 22 Activity ≤ 1 µM, 23 Tested
Antagonist activity at CCR2 in human THP1 cells assessed as inhibition of CCL2-induced chemotaxis at 1 uM in presence of 0.1% human serum
Assay data:10 Tested
Displacement of [125]MCP1 from CCR2 in human PBMCs at 1 uM
Assay data:6 Tested
Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
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