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Class
Ligand Type
GPCR Family
GPCR Target
(Human unless noted)
NEW
Anon-peptide
Acetylcholine (muscarinic)
M1
Anon-peptide
Acetylcholine (muscarinic)
M2
Anon-peptide
Acetylcholine (muscarinic)
M3
Anon-peptide
Acetylcholine (muscarinic)
M4
Anon-peptide
Acetylcholine (muscarinic)
M5
Anon-peptide
Adenosine
A1
Anon-peptide
Adenosine
A2B
Anon-peptide
Adenosine
A3
Anon-peptide
Adrenergic
alpha1A
Anon-peptide
Adrenergic
alpha1B
Anon-peptide
Adrenergic
alpha1D
Anon-peptide
Adrenergic
alpha2A
Anon-peptide
Adrenergic
beta 1
Anon-peptide
Adrenergic
beta 2
Anon-peptide
Adrenergic
beta 3
Anon-peptide
alpha-Ketoglutarate
OXGR1 , GPR99 , GPR80
Apeptide
Anaphylotoxin
C3aR
Apeptide
Anaphylotoxin
C5aR
Apeptide
Angiotensin
AT1
Apeptide
Apelin
APJ
Apeptide
Bombesin
BB1
Apeptide
Bombesin
BB2
Apeptide
Bombesin
BB3
Apeptide
Bradykinin
B2
Bpeptide
Calcitonin
CGRP1
Cnon-peptide
Calcium sensor
CaS
Anon-peptide
Cannabinoid
CB1
Anon-peptide
Cannabinoid
CB2
Apeptide
Chemoattractant
ChemR23 / CMKLR1
Apeptide
Chemokine
CCR1
Apeptide
Chemokine
CCR10
Apeptide
Chemokine
CCR2B
Apeptide
Chemokine
CCR3
Apeptide
Chemokine
CCR4
Apeptide
Chemokine
CCR5, rhesus macaque
Apeptide
Chemokine
CCR6
Apeptide
Chemokine
CCR7
Apeptide
Chemokine
CCR8
Apeptide
Chemokine
CCR9
Apeptide
Chemokine
CX3CR1
Apeptide
Chemokine
CXCR1 / IL-8a
Apeptide
Chemokine
CXCR2 / IL-8b
Apeptide
Chemokine
CXCR3
Apeptide
Chemokine
CXCR4
Apeptide
Chemokine
CXCR5
New
Apeptide
Chemokine
CXCR6
Apeptide
Chemokine
XCR1 / GPR5
Apeptide
Cholecystokinin
CCK1 / CCKa
Apeptide
Cholecystokinin
CCK2 / CCKb
Bpeptide
CRF Receptor
CRF1
Bpeptide
CRF Receptor
CRF2
Anon-peptide
Dopamine
D1
Anon-peptide
Dopamine
D2L
Anon-peptide
Dopamine
D4
New
Anon-peptide
Dopamine
D5
Apeptide
Endothelin
ETA
Apeptide
Endothelin
ETB
Anon-peptide
Free Fatty Acid
FFA3 / GPR41
Anon-peptide
Free Fatty Acid
FFA2 / GPR43
Cnon-peptide
GABAB
GABAB1b
Apeptide
Galanin
GAL1
Apeptide
Galanin
GAL2
Apeptide
Ghrelin
Ghrelin / GHSR-1a / growth hormone secretagogue receptor
Bpeptide
Glucagon
GIP
Bpeptide
Glucagon
GLP-1
B
peptide
Glucagon
GLP-2
New
Bpeptide
Glucagon
glucagon / GCG
Bpeptide
Glucagon
secretin receptor / SEC
C
non-peptide
Glutamate (metabotropic)
mGlu1
New
Cnon-peptide
Glutamate (metabotropic)
mGlu2
Apeptide
Glycoprotein hormone
TSH / TSHR
Apeptide
GnRH
GnRH / LHRH
Anon-peptide
Histamine
H1
Anon-peptide
Histamine
H2
Anon-peptide
Histamine
H3
Apeptide
KiSS1-derived peptide
KiSS1 / GPR54
Anon-peptide
Leukotriene
BLT1
Anon-peptide
Leukotriene
CysLT1
Anon-peptide
Leukotriene
CysLT2
Anon-peptide
Lysophospholipid
LPA1 / EDG2
Anon-peptide
Lysophospholipid
LPA3 / EDG7
Anon-peptide
Lysophospholipid
LPA5 / GPR92
Anon-peptide
Lysophospholipid
S1P1 / EDG1
Anon-peptide
Lysophospholipid
S1P2 / EDG5
Anon-peptide
Lysophospholipid
S1P3 / EDG3
Anon-peptide
Lysophospholipid
S1P4 / EDG6
Anon-peptide
Lysophospholipid
S1P5 / EDG8
Apeptide
Mas-related gene
MRGX1 / MRGPRX1
Apeptide
Mas-related gene
MRGX2 / MRGPRX2
Apeptide
Mas-related gene
MRGPRD / MrgD
Apeptide
Melanin-concentrating hormone
MCHR1 / GPR24
Apeptide
Melanin-concentrating hormone
MCHR2
Apeptide
Melanocortin
MC2
Apeptide
Melanocortin
MC4
Apeptide
Melanocortin
MC5
Apeptide
Motilin
motilin receptor / MTLR / GPR38
Apeptide
Neuromedin U
NMU1
Apeptide
Neuromedin U
NMU2
Apeptide
Neuropeptide B/W
NPBW1 / GPR7
Apeptide
Neuropeptide Y
Y2
Apeptide
Neuropeptide Y
Y4
Apeptide
Neurotensin
NTR1 / NTS1
Apeptide
N-formylpeptide
FPR1
Apeptide
N-formylpeptide
FPRL1 / AXL / HM63
Anon-peptide
Nicotinic Acid
GPR109A
Apeptide
Opioid
Delta / OP1 / DOP / DOR
Apeptide
Opioid
Kappa / OP2 / KOP / KOR
Apeptide
Opioid
Mu / OP3 / MOP / MOR
Apeptide
Opioid
NOP / ORL1 / OP4
Apeptide
Orexin
OX1
Apeptide
Orexin
OX2
Apeptide
Oxytocin
OT
Anon-peptide
P2 / Purinergic (metabotropic)
P2Y1
Anon-peptide
P2 / Purinergic (metabotropic)
P2Y2
Anon-peptide
P2 / Purinergic (metabotropic)
P2Y4
Anon-peptide
P2 / Purinergic (metabotropic)
P2Y11
Anon-peptide
P2Y / Purinergic (metabotropic)
P2Y12
New
Apeptide
Peptide P518
GPR103 / QRFP
Anon-peptide
Platelet Activating Factor
PAF
Apeptide
Prokineticin
PK1 / PKR1
Apeptide
Prokineticin
PK2 / PKR2
Apeptide
Prolactin-releasing peptide
PRP / PrRP / GPR10
Anon-peptide
Prostanoid
DP
Anon-peptide
Prostanoid
EP1
Anon-peptide
Prostanoid
EP2
Anon-peptide
Prostanoid
EP3
Anon-peptide
Prostanoid
EP4
Anon-peptide
Prostanoid
FP
Anon-peptide
Prostanoid
IP1 / PGI2
Anon-peptide
Prostanoid
TP / TXA2 / PGH2
Apeptide
Protease-activated
Thrombin-activated PARs
Apeptide
Protease-activated
Trypsin-activated PARs
Bpeptide
PTH receptor
PTH1
Bpeptide
PTH receptor
PTH2
Anon-peptide
Serotonin
5-HT1A
Anon-peptide
Serotonin
5-HT2A
Anon-peptide
Serotonin
5-HT2B
Anon-peptide
Serotonin
5-HT2C
Anon-peptide
Serotonin
5-HT4
New
Anon-peptide
Serotonin
5-HT6
Apeptide
Somatostatin
sst2
Apeptide
Somatostatin
sst3
Apeptide
Somatostatin
sst4
Apeptide
Somatostatin
sst5
Anon-peptide
SPC/LPC /proton-sensor
GPR68/OGR1
A
non-peptide
Succinate
SUCNRI/GPR91
New
Apeptide
Tackykinin /neurokinin
NK1
Apeptide
Tackykinin /neurokinin
NK2
Apeptide
Tackykinin /neurokinin
NK3
Apeptide
TRH
TRH
Apeptide
Urotensin II
UT / UT1 / GPR14
Apeptide
Vasopressin
V1A
Apeptide
Vasopressin
V1B
Apeptide
Vasopressin
V2
Bpeptide
VIP/PACAP
PAC1 long isoform / PACAP
Bpeptide
VIP/PACAP
VPAC1 / VIP1
B
peptide
VIP/PACAP
VPAC2 / VIP2
Anon-peptide
Orphan
GPR39
New

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