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Displacement of [125I]-CX3CL1 from human CX3CR1 transfected in HEK293 cells after 24 hrs by scintillation counting analysis
Assay data:50 Active, 47 Activity ≤ 1 µM, 51 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Displacement of [125I]-IL8 from human CXCR2 transfected in HEK293 cells after 4 hrs by microbeta counting analysis
Assay data:45 Active, 26 Activity ≤ 1 µM, 51 Tested
Selectivity ratio of Ki for human CXCR2 to Ki for human CX3CR1
Assay data:47 Tested
SummaryPubMed Citation
Solubility of the compound in phosphate buffer at pH 7.4 after 24 hrs by HPLC analysis
Assay data:8 Active, 5 Activity ≤ 1 µM, 19 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed Citation
Metabolic stability in human liver microsomes assessed as intrinsic clearance by LC-MS/MS analysis
Assay data:19 Tested
Apparent permeability from apical to basolateral side in human Caco2 cells at pH 6.5 after 90 mins by LC-MS analysis
Clearance in Sprague-Dawley rat at 3 umol/kg, iv or 10 umol/kg, po by LC-MS analysis
Assay data:2 Tested
Half life in Sprague-Dawley rat at 3 umol/kg, iv by LC-MS analysis
Half life in Sprague-Dawley rat at 10 umol/kg, po by LC-MS analysis
Volume of distribution at steady state in Sprague-Dawley rat at 3 umol/kg, iv or 10 umol/kg, po by LC-MS analysis
Oral bioavailability in Sprague-Dawley rat at 3 umol/kg by LC-MS analysis
Selectivity for human CX3CR1 over human CCR1
Assay data:1 Tested
Antagonist activity at CCR4 (unknown origin)
SummaryPubMed CitationRelated BioAssays by Target
Selectivity for human CX3CR1 over human CCR2
Antagonist activity at CCR5 (unknown origin)
Antagonist activity at CCR3 (unknown origin)
Antagonist activity at CCR6 (unknown origin)
Binding affinity to adenosine A1 receptor (unknown origin)
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Binding affinity to adenosine A1 receptor (unknown origin) at 10 uM
Binding affinity to dopamine transporter (unknown origin)
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
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