TABLE 1

One hundred thirty-four GPCRs have FDA-approved drugs

Exceptions are those marked as follows: *, EMA approved; 1, approved in the United Kingdom by the The Medicines and Healthcare products Regulatory Agency (MHRA); 2, suramin is not listed in the FDA’s Orange Book, but is distributed by the Centers for Disease Control and is listed as an essential medicine by the World Health Organization; and #, GABBR1 and 2 combine to form a single active signaling complex that is activated by baclofen. Entries in bold in indicate GPCRs considered primary targets for the listed drug based on affinity and/or functional response (in the majority of cases, both). Entries not in bold indicate GPCRs targeted by approved drugs but for which such an interaction is not likely a primary aspect of the intended therapeutic use of such drugs.