GPCR ranking - Number of receptor-targeted drugs- Tanso Biosciences

All GPCRs are not made equal. As illustrated in "About GPCR," some GPCRs have dozens of drugs targeting them while the majority of GPCRs have few or none in the market, clinical trials, or labs.

Based on a GPCR drug database [1,2], the figure above and the table below rank GPCRs in ascending and descending order, respectively, of the number of receptor-targeted drugs. The distribution is obviously skewed. N.B., there are also ~150 nonsensory GPCRs missing in the table since they have never been addressed as therapeutic targets.

Some drug-receptor pairs have multiple statuses/phases like Approved and Phase 3 in the database [1]. In such cases, the most advanced status was counted toward the number in this analysis. Withdrawn was treated as a status between Phase 3 and Approved because withdrawn drugs used to be approved and are thus more advanced than ones in Phase 3 while they did not stand the test of time and are thus less advanced than still-aproved ones.

Rank	Target	Total	Approved	Withdrawn	Phase 3	Phase 2	Phase 1	Preclinical
1	DRD2	85	61	1	11	7	5	0
2	HRH1	79	73	1	2	3	0	0
3	5HT2A	70	43	1	10	12	4	0
4	ACM1	63	55	1	0	3	4	0
5	ADRB2	62	43	0	1	16	2	0
6	ADA1A	60	53	1	1	5	0	0
7	OPRM	55	39	0	7	5	4	0
8	ACM3	50	40	1	2	6	1	0
9	ACM2	44	39	1	0	3	1	0
10	ADA1B	42	38	1	0	3	0	0
11	ADRB1	42	38	0	0	4	0	0
12	ADA2A	41	34	0	2	4	0	1
13	5HT1A	38	23	0	6	8	1	0
14	ADA2B	37	30	0	1	4	1	1
15	5HT2C	37	26	1	5	5	0	0
16	ADA1D	36	32	1	0	3	0	0
17	ADA2C	36	30	0	1	4	0	1
18	DRD3	35	25	0	5	2	2	1
19	DRD1	34	28	0	3	1	2	0
20	OPRK	33	19	0	5	6	3	0
21	DRD4	29	22	0	4	1	2	0
22	OPRD	29	16	0	4	7	2	0
23	GLP1R	28	6	0	3	10	9	0
24	CNR1	22	4	1	3	8	5	1
25	GNRHR	20	12	0	3	5	0	0
26	ACM4	19	16	1	0	1	1	0
27	5HT2B	19	10	0	4	4	1	0
28	5HT1B	18	13	0	0	4	1	0
29	AA2AR	18	5	0	6	7	0	0
30	ACM5	17	14	1	0	1	1	0
31	5HT6R	17	3	1	3	7	3	0
32	AGTR1	16	9	0	3	4	0	0
33	ADRB3	15	9	0	3	1	2	0
34	EDNRA	15	4	0	5	6	0	0
35	5HT1D	14	10	0	0	3	1	0
36	AA1R	14	3	0	3	6	2	0
37	DRD5	13	9	0	1	1	2	0
38	5HT4R	13	4	0	2	5	2	0
39	HRH2	12	12	0	0	0	0	0
40	CNR2	12	3	0	1	5	1	2
41	PD2R2	12	1	0	2	6	3	0
42	NK1R	11	3	0	1	6	1	0
43	CXCR4	11	1	0	2	5	3	0
44	5HT7R	10	7	0	2	1	0	0
45	P2Y12	10	6	0	0	3	1	0
46	V2R	10	5	0	2	3	0	0
47	SSR2	10	4	0	0	3	3	0
48	S1PR1	10	2	0	3	3	2	0
49	GRM5	10	1	0	1	8	0	0
50	HRH3	9	1	0	1	4	3	0
51	PI2R	8	5	0	1	2	0	0
52	V1AR	8	4	0	1	2	1	0
53	GABR1	8	4	0	1	1	1	1
54	SSR5	8	4	0	0	3	1	0
55	SMO	8	3	0	0	3	2	0
56	CCR2	8	0	0	1	4	3	0
57	LSHR	7	5	0	0	1	1	0
58	EDNRB	7	3	0	2	2	0	0
59	PTH1R	7	3	0	1	3	0	0
60	OXYR	7	2	0	3	2	0	0
61	AA3R	7	2	0	2	2	1	0
62	GLR	7	1	0	0	4	2	0
63	MSHR	7	0	0	2	2	2	1
64	CXCR2	7	0	0	1	4	2	0
65	PE2R1	6	5	0	0	0	1	0
66	FSHR	6	4	0	1	1	0	0
67	PF2R	6	4	0	1	0	1	0
68	AA2BR	6	4	0	0	1	1	0
69	HCAR2	6	3	0	0	2	1	0
70	SSR1	6	3	0	0	2	1	0
71	CASR	6	2	0	1	2	0	1
72	GABR2	6	2	0	1	1	1	1
73	CCR5	6	1	0	4	1	0	0
74	OX2R	6	1	0	1	4	0	0
75	OX1R	6	1	0	1	3	1	0
76	CALRL	6	0	0	3	3	0	0
77	GHSR	6	0	0	2	3	1	0
78	GRM2	6	0	0	2	2	2	0
79	5HT1F	5	4	0	1	0	0	0
80	MTR1A	5	4	0	0	1	0	0
81	MTR1B	5	4	0	0	1	0	0
82	CLTR1	5	4	0	0	0	1	0
83	PE2R3	5	3	0	0	1	1	0
84	P2RY2	5	1	0	3	1	0	0
85	CRFR1	5	1	0	2	2	0	0
86	MC4R	5	0	0	2	1	2	0
87	GRM3	5	0	0	2	1	2	0
88	TAAR1	4	3	0	0	1	0	0
89	CALCR	4	3	0	0	1	0	0
90	V1BR	4	3	0	0	1	0	0
91	PE2R2	4	3	0	0	0	1	0
92	GHRHR	4	2	0	0	2	0	0
93	PTH2R	4	1	0	1	2	0	0
94	HCAR3	4	1	0	0	2	1	0
95	CCR9	4	0	0	2	0	2	0
96	HRH4	4	0	0	1	3	0	0
97	AGTR2	4	0	0	1	2	1	0
98	CXCR1	4	0	0	1	2	1	0
99	GPR55	4	0	0	1	2	0	1
100	GP119	4	0	0	0	2	2	0
101	SSR3	3	2	0	0	0	1	0
102	PAR1	3	1	0	1	1	0	0
103	FFAR1	3	1	0	1	0	1	0
104	GLP2R	3	1	0	0	2	0	0
105	PE2R4	3	1	0	0	1	1	0
106	SSR4	3	1	0	0	1	1	0
107	MC3R	3	0	0	1	2	0	0
108	PD2R	3	0	0	1	1	1	0
109	MTLR	3	0	0	0	2	1	0
110	CCKAR	2	0	1	1	0	0	0
111	SCTR	2	1	0	1	0	0	0
112	GPR35	2	1	0	0	1	0	0
113	BKRB2	2	1	0	0	1	0	0
114	GASR	2	1	0	0	1	0	0
115	TA2R	2	1	0	0	1	0	0
116	OPRX	2	0	0	1	1	0	0
117	P2RY1	2	0	0	1	1	0	0
118	P2RY4	2	0	0	1	1	0	0
119	P2Y11	2	0	0	1	1	0	0
120	P2Y13	2	0	0	1	1	0	0
121	P2Y14	2	0	0	1	1	0	0
122	P2RY8	2	0	0	1	1	0	0
123	P2Y10	2	0	0	1	1	0	0
124	CRFR2	2	0	0	1	1	0	0
125	VIPR2	2	0	0	1	1	0	0
126	LPAR4	2	0	0	1	1	0	0
127	LPAR6	2	0	0	1	1	0	0
128	C5AR1	2	0	0	1	0	1	0
129	GRM4	2	0	0	1	0	1	0
130	LT4R1	2	0	0	0	2	0	0
131	NK3R	2	0	0	0	2	0	0
132	NPY4R	2	0	0	0	2	0	0
133	CML1	2	0	0	0	1	1	0
134	P2RY6	2	0	0	0	1	1	0
135	NPY2R	2	0	0	0	1	1	0
136	LGR5	2	0	0	0	0	2	0
137	5HT5A	1	1	0	0	0	0	0
138	ACTHR	1	1	0	0	0	0	0
139	S1PR5	1	1	0	0	0	0	0
140	NTR2	1	1	0	0	0	0	0
141	CLTR2	1	1	0	0	0	0	0
142	TRFR	1	1	0	0	0	0	0
143	PTAFR	1	1	0	0	0	0	0
144	TSHR	1	1	0	0	0	0	0
145	BKRB1	1	1	0	0	0	0	0
146	5HT1E	1	1	0	0	0	0	0
147	GRM6	1	0	0	1	0	0	0
148	GRM7	1	0	0	1	0	0	0
149	GRM8	1	0	0	1	0	0	0
150	CCR4	1	0	0	1	0	0	0
151	PAR3	1	0	0	1	0	0	0
152	PAR4	1	0	0	1	0	0	0
153	NK2R	1	0	0	1	0	0	0
154	RXFP1	1	0	0	1	0	0	0
155	RXFP2	1	0	0	1	0	0	0
156	VIPR1	1	0	0	1	0	0	0
157	GRM1	1	0	0	1	0	0	0
158	LPAR1	1	0	0	0	1	0	0
159	MC5R	1	0	0	0	1	0	0
160	CCR1	1	0	0	0	1	0	0
161	FFAR2	1	0	0	0	1	0	0
162	GPR84	1	0	0	0	1	0	0
163	MCHR1	1	0	0	0	1	0	0
164	CCR3	1	0	0	0	1	0	0
165	MAS	1	0	0	0	1	0	0
166	NPY5R	1	0	0	0	1	0	0
167	APJ	1	0	0	0	0	1	0
168	CX3C1	1	0	0	0	0	1	0
169	GPBAR	1	0	0	0	0	1	0
170	FZD8	1	0	0	0	0	1	0
171	GIPR	1	0	0	0	0	1	0
172	LGR4	1	0	0	0	0	1	0
173	FZD10	1	0	0	0	0	1	0
174	FZD7	1	0	0	0	0	1	0

References

DrugBrowser. GPCRdb. https://gpcrdb.org/drugs/drugbrowser (accessed December 6, 2019).
Hauser AS, Attwood MM, Rask-Andersen M, Schiöth HB, Gloriam DE. Trends in GPCR drug discovery: new agents, targets and indications. Nat Rev Drug Discov. 2017;16:829-842.