TABLE 3.

Representative triazole and isoquinolinone compounds in whole cell G protein signaling assays

EC₅₀ and E_max values were calculated as described in Table 1. Bias factors (ΔΔlog(τ/K_a)_{assay1 − assay2}) were calculated as described under “Experimental Procedures.” βArrestin2 EFC and βarrestin2 imaging transduction coefficients are found in Table 2. The asterisk indicates that log K_a values were constrained to <0 (less than 1 m relative affinity) to permit convergence to the operational model. n ≥ 5 individual assays; means are presented ± S.E. Maximal stimulation over vehicle treatment with U69,593 was ∼2-fold for whole cell [³⁵S]GTPγS binding (wcG) and ∼8-fold for the cellular impedance assay.