G protein – coupled receptors are classic drug development targets. GPR30 was once thought to be the G protein – coupled receptor for estrogen, but it was refuted by new experiments last year. Therefore, the Phase I clinical study of its agonist (G1) also requires further observation. Searching for new GPR30 agonists will be a very promising topic. It can not only provide new ideas for the treatment of clinical diseases, but also bring economic value through drug development.