As mentioned, the two pioneer compounds (shown in Figure 1A), T-226296 from Takeda (Osaka, Japan) and SNAP-7941 from Synaptic (Gottingen, Germany), represent the starting point of small molecular MCHR1 antagonists and present the pharmacological evidence of the anti-obesity therapeutic utility of MCHR1 antagonists [22]. The gene discussed is MCHR1; the disease is obesity due to melanocortin 4 receptor deficiency.