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GW-856464 is a small molecule drug developed by GSK as a potent and selective antagonist of the melanin-concentrating hormone receptor 1 (MCHR1). It was investigated for the treatment of obesity and other metabolic diseases. The compound acts by inhibiting MCHR1, which is implicated in energy homeostasis and body weight regulation. Despite promising preclinical activity as an anti-obesity agent, clinical development was discontinued after phase 1 trials due to low bioavailability[2][6][7].
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