TABLE 1.

LPA receptor-activated Ca²⁺ mobilization profiles for hit compounds

Every compound was tested on every receptor subtype for agonist activity up to 10 μM and the E_max value listed in the table is normalized to the maximal response of LPA 18:1 at 10 μM. Those compounds that failed to activate a given receptor were tested for inhibition of the LPA 18:1 response. I_max is percentage inhibition of the ∼E_max75 LPA 18:1 response for a given receptor subtype using a 10 μM concentration of the antagonist. EC₅₀ and IC₅₀ concentrations are given as micromolar concentrations for dose-response curves covering the 30 nM to 10 μM range (Fig. 1). For determination of IC₅₀ values, dose-response curves were generated using the ∼E_max 75 concentration of LPA 18:1 for a given LPA receptor subtype, and the ligand was coapplied in concentrations ranging from 30 nM to 10 μM.

LogP, log partition coefficient; N.E., no effect up to 10 μM of the ligand, the maximal concentration tested in the present experiments.