Antagonist activity at human mu opioid receptor expressed in CHO cells co- expressing Gqi5 assessed as decrease in DAMGO-induced intracellular calcium mobilization incubated for 15 mins followed by DAMGO addition by Fluo-AM dye based fluorescence assay
Antagonist activity at CXCR4 (unknown origin) expressed in CHO cells assessed as reduction in SDF1-induced intracellular calcium mobilization incubated for 15 mins followed by SDF1 addition by Fluo-AM dye based fluorescence assay
Potency index, ratio of N-[6-[[2-[2-[[(3R,4R,4aS,7R,7aR,12bS)-3-(cyclopropylmethyl)-4a,9-dihydroxy-1,2,4,5,6,7,7a,13-octahydro-4,12-methanobenzofuro[3,2-e]isoquinoline-7-yl]amino]-2-oxo-ethoxy]acetyl]amino]hexyl]-2-[2-[[4-[(E)-[(cyclohexylamino)-[(6,6-dimethyl-5H-imidazo[2,1-b]thiazol-3-yl)methylsulfanyl]methylene]amino]cyclohexyl]methylamino]-2-oxo-ethoxy]acetamide IC50 to test compound IC50 for Displacement of [125I]SDF-1alpha from CXCR4 in human Chem-1 cells measured after 90 mins
Inhibition of HIV1 3B reverse transcriptase infected in human GHOST CXCR4 cells assessed as reduction in viral replication incubated for 60 to 90 mins in presence of DTT and TTP by liquid scintillation counter
Therapeutic index, ratio of TC50 for human GHOST CXCR4 cells assessed as reduction in cell viability incubated for 4 hrs by XTT assay to EC50 for HIV1 3B reverse transcriptase infected in human GHOST CXCR4 cells assessed as reduction in viral replication incubated for 60 to 90 mins in presence of DTT and TTP by liquid scintillation counter
Inhibition of HIV1 3B Tat infected in human TZM-bl cells assessed as reduction in viral entry in cells when pretreated for 1 hr followed by HIV1 3B infection and further incubated for 2 days followed by luciferase substrate addition by luminescence assay
Inhibition of HIV1 3B Tat infected in human TZM-bl cells assessed as reduction in viral entry in cells at 30 uM when pretreated for 1 hr followed by HIV1 3B infection and further incubated for 2 days followed by luciferase substrate addition by luminescence assay relative to control
Antiviral activity against HIV1 3B infected in human TZM-bl cells assessed as reduction in viral entry by measuring Tat protein level at 1000 nM measured after 3 days by luciferase-based assay
Antiviral activity against HIV1 3B infected in human TZM-bl cells assessed as reduction in viral entry by measuring Tat protein level at 1000 nM measured after 3 days in presence of morphine by luciferase-based assay