Figure 1

Screening for selectivity of G9a-inhibitors at 1 µM among dopamine D₁, D₅, D₂ and D₃ receptors (D₁R, D₅R, D₂R, D₃R, respectively) and at the histamine H₄ receptor (H₄R). For comparison, the figure depicts the inhibition of specific binding to H₃R that was extracted from affinity screening data. Bars represent means ± s.d. of the inhibition of radioligand binding to the respective receptor by either A-366, UNC-0642 or control compound (100 µM fluphenazine for D₁R and D₅R, 10 µM haloperidol for D₂R and D₃R, 100 µM JNJ-7777120 for H₄R or 10 µM pitolisant for H₃R).[³H]-SCH23390, [³H]-spiperone, [³H]-histamine and [³H]N^α-methylhistamine were used as radiolabelled tracers at D₁R/D₅R, D₂R/D₃R, H₄R and H₃R, respectively, each at approx. 1 × K_D.