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. 2016 Dec 3;13(2):191–201. doi: 10.1007/s11302-016-9549-9

Table 2.

The (apparent) association and dissociation rate constants of LUF7445, LUF6632, and ZM241385 determined in competition association assays with [3H]-ZM241385 binding to HEK293-hA2AAR membranes

Compound k on (nM−1 min−1)a k off (min−1)a RT (min)
LUF7445b (0.0059 ± 0.00049) (1.37 ± 0.68 × 10−11) (2.86 ± 0.87 × 1011)
LUF6632 1.53 ± 0.083 0.15 ± 0.021 6.80 ± 0.97
ZM241385 1.72 ± 0.36 1.04 ± 0.13 0.96 ± 0.12

aAssociation (k on) and dissociation (k off) rate constants were determined by competition association assay at 25 °C; all these values were determined by analyzing the data in the mathematical model described by Motulsky and Mahan [27]

bFor LUF7445, no equilibrium is reached between receptors and ligand; hence, the Motulsky/Mahan mathematical model [27] for the competition association assay is not valid. The values obtained are therefore considered to provide qualitative insight only, and are in brackets