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