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Antagonist activity at CCR5 (unknown origin) expressed in HEK293 cells co-expressing Galpha16 assessed as intracellular calcium change incubated for 15 mins by Fluo-4 AM calcium flux assay
Assay data:20 Active, 19 Activity ≤ 1 µM, 23 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of CCR2 (unknown origin) at 10 uM relative to control
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of human CCR5 at 10 uM relative to control
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
Inhibition of CCR5-mediated Luc-expressing HIV1 BaL Env-pseudotype virus infection in CCR5 expressing leukocytes containing human PBMC assessed as inhibition of viral entry by measuring luminescence pretreated for 1 hr before infection measured after 2 days of infection
Inhibition of CCR5-mediated Luc-expressing HIV1 BaL Env-pseudotype virus infection in PHA-stimulated CCR5 expressing leukocytes containing human PBMC assessed as inhibition of viral entry in presence of 10 nM DMAGO by measuring luminescence at 100 nM pretreated for 1 hr before infection measured after 2 days of infection
Inhibition of CCR5-mediated Luc-expressing HIV1 BaL Env-pseudotype virus infection in PHA-stimulated CCR5 expressing leukocytes containing human PBMC assessed as inhibition of viral entry in presence of 10 nM morphine by measuring luminescence at 100 nM pretreated for 1 hr before infection measured after 2 days of infection
Inhibition of CCR5-mediated Luc-expressing HIV1 BaL Env-pseudotype virus infection in PHA-stimulated CCR5 expressing leukocytes containing human PBMC assessed as inhibition of viral entry by measuring luminescence at 100 nM pretreated for 1 hr before infection measured after 2 days of infection
Inhibition of CCR5-mediated HIV-1 Bal entry in human GHOST CCR5 cells assessed as decrease in viral reverse transcriptase activity by measuring [3H]thymidine triphosphate incorporation measured after 60 to 90 mins by scintillation counting analysis
Assay data:2 Active, 2 Activity ≤ 1 µM, 3 Tested
Agonist activity at CCR5 (unknown origin) expressed in HOS cells co-expressing Gqi-5 assessed as stimulation of Ca2+ mobilization by calcium mobilization assay
Assay data:2 Tested
Antagonist activity at CCR5 (unknown origin) expressed in HOS cells co-expressing Gqi-5 assessed as inhibition CCL5-stimulated Ca2+ mobilization by calcium mobilization assay
Assay data:5 Active, 1 Activity ≤ 1 nM, 4 Activity ≤ 1 µM, 5 Tested
Displacement of [125I]1-alpha from recombinant rhesus macaque CCR5 expressed in Chem-1 cells by competitive radioligand binding assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Displacement of [125I]1-alpha from recombinant rhesus macaque CCR5 expressed in Chem-1 cells incubated for 90 mins by competitive radioligand binding assay
Assay data:3 Active, 3 Activity ≤ 1 µM, 4 Tested
Antagonist activity against CCR5 (unknown origin) assessed as inhibition of beta-arrestin 2 recruitment at 10 microM by beta arrestin assay relative to control
Agonist activity against CCR5 (unknown origin) assessed as induction of beta-arrestin 2 recruitment at 10 microM by beta arrestin assay relative to control
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
Antagonist activity at human CCR5 receptor expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of RNATES-induced intracellular calcium flux measured after 10 mins by FLIPR calcium mobilization assay
Assay data:3 Active, 1 Activity ≤ 1 nM, 3 Activity ≤ 1 µM, 4 Tested
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