Table 1. Biological and ADME Assay Data for 2-Aminoheterocyclic Tetrahydroisoquinoline CXCR4 Antagonists.

^aConcentration of compound inhibiting the Ca²⁺ flux (release) by 50%, reported as a single experiment (n = 1) or the mean of several experiments (n > 1).

^bMetabolic stability was determined as the percentage of test compound remaining after incubation for 10 min at 37 °C in liver microsome preparations (CYP450 and other NADP-dependent enzymes).

^cn = 1.

^dReported error represents the standard deviation of multiple experiments (n = 2).

^eReported error represents the standard deviation of multiple experiments (n = 3).

^fReported error represents the standard deviation of multiple experiments (n = 4).

^gReported error represents the standard deviation of multiple experiments (n = 5).

^hLower limit (<20 μM) in the CYP450 2D6 assay is shown; all compounds had >20 μM activity against CYP450 3A4.

ⁱCYP 2C9 IC₅₀ = 6.67 μM.

^jValue not determined (n.d.).