G protein-coupled receptors
Download the list of all GPCR targets in CSV format 
| 5-Hydroxytryptamine receptors | ||||||
| Family name | Ligand | Official IUPHAR receptor name | Human gene symbol | Rat gene symbol | Mouse gene symbol | Comment |
| 5-Hydroxytryptamine receptors |
5-hydroxytryptamine
|
5-HT1A receptor |
HTR1A |
Htr1a |
Htr1a |
|
| 5-Hydroxytryptamine receptors |
5-HT-moduline
5-hydroxytryptamine tryptamine |
5-HT1B receptor |
HTR1B |
Htr1b |
Htr1b |
Endogenous ligand tryptamine is a weak agonist |
| 5-Hydroxytryptamine receptors |
5-HT-moduline
5-hydroxytryptamine |
5-HT1D receptor |
HTR1D |
Htr1d |
Htr1d |
|
| 5-Hydroxytryptamine receptors |
5-hydroxytryptamine
tryptamine |
5-ht1e receptor |
HTR1E |
Endogenous ligand tryptamine is a weak agonist | ||
| 5-Hydroxytryptamine receptors |
5-hydroxytryptamine
|
5-HT1F receptor |
HTR1F |
Htr1f |
Htr1f |
|
| 5-Hydroxytryptamine receptors |
5-hydroxytryptamine
tryptamine |
5-HT2A receptor |
HTR2A |
Htr2a |
Htr2a |
|
| 5-Hydroxytryptamine receptors |
5-hydroxytryptamine
|
5-HT2B receptor |
HTR2B |
Htr2b |
Htr2b |
|
| 5-Hydroxytryptamine receptors |
5-hydroxytryptamine
|
5-HT2C receptor |
HTR2C |
Htr2c |
Htr2c |
|
| 5-Hydroxytryptamine receptors |
5-hydroxytryptamine
|
5-HT4 receptor |
HTR4 |
Htr4 |
Htr4 |
|
| 5-Hydroxytryptamine receptors |
5-hydroxytryptamine
|
5-HT5A receptor |
HTR5A |
Htr5a |
Htr5a |
|
| 5-Hydroxytryptamine receptors |
5-hydroxytryptamine
|
5-ht5b receptor |
HTR5BP |
Htr5b |
Htr5b |
|
| 5-Hydroxytryptamine receptors |
5-hydroxytryptamine
|
5-HT6 receptor |
HTR6 |
Htr6 |
Htr6 |
|
| 5-Hydroxytryptamine receptors |
5-hydroxytryptamine
|
5-HT7 receptor |
HTR7 |
Htr7 |
Htr7 |
|
| Acetylcholine receptors (muscarinic) | ||||||
| Family name | Ligand | Official IUPHAR receptor name | Human gene symbol | Rat gene symbol | Mouse gene symbol | Comment |
| Acetylcholine receptors (muscarinic) |
acetylcholine
|
M1 receptor |
CHRM1 |
Chrm1 |
Chrm1 |
|
| Acetylcholine receptors (muscarinic) |
acetylcholine
|
M2 receptor |
CHRM2 |
Chrm2 |
Chrm2 |
|
| Acetylcholine receptors (muscarinic) |
acetylcholine
|
M3 receptor |
CHRM3 |
Chrm3 |
Chrm3 |
|
| Acetylcholine receptors (muscarinic) |
acetylcholine
|
M4 receptor |
CHRM4 |
Chrm4 |
Chrm4 |
|
| Acetylcholine receptors (muscarinic) |
acetylcholine
|
M5 receptor |
CHRM5 |
Chrm5 |
Chrm5 |
|
| Adenosine receptors | ||||||
| Family name | Ligand | Official IUPHAR receptor name | Human gene symbol | Rat gene symbol | Mouse gene symbol | Comment |
| Adenosine receptors |
adenosine
|
A1 receptor |
ADORA1 |
Adora1 |
Adora1 |
|
| Adenosine receptors |
adenosine
|
A2A receptor |
ADORA2A |
Adora2a |
Adora2a |
|
| Adenosine receptors |
adenosine
|
A2B receptor |
ADORA2B |
Adora2b |
Adora2b |
|
| Adenosine receptors |
adenosine
|
A3 receptor |
ADORA3 |
Adora3 |
Adora3 |
|
| Adrenoceptors | ||||||
| Family name | Ligand | Official IUPHAR receptor name | Human gene symbol | Rat gene symbol | Mouse gene symbol | Comment |
| Adrenoceptors |
(-)-adrenaline
(-)-noradrenaline |
α1A-adrenoceptor |
ADRA1A |
Adra1a |
Adra1a |
|
| Adrenoceptors |
(-)-adrenaline
(-)-noradrenaline |
α1B-adrenoceptor |
ADRA1B |
Adra1b |
Adra1b |
|
| Adrenoceptors |
(-)-adrenaline
(-)-noradrenaline |
α1D-adrenoceptor |
ADRA1D |
Adra1d |
Adra1d |
|
| Adrenoceptors |
(-)-adrenaline
(-)-noradrenaline |
α2A-adrenoceptor |
ADRA2A |
Adra2a |
Adra2a |
Adrenaline exhibits similar potency, affinity and efficacy to noradrenaline. |
| Adrenoceptors |
(-)-adrenaline
(-)-noradrenaline |
α2B-adrenoceptor |
ADRA2B |
Adra2b |
Adra2b |
Adrenaline exhibits similar potency, affinity and efficacy to noradrenaline. |
| Adrenoceptors |
(-)-adrenaline
(-)-noradrenaline |
α2C-adrenoceptor |
ADRA2C |
Adra2c |
Adra2c |
Adrenaline exhibits similar potency, affinity and efficacy to noradrenaline. |
| Adrenoceptors |
(-)-adrenaline
noradrenaline (-)-noradrenaline |
β1-adrenoceptor |
ADRB1 |
Adrb1 |
Adrb1 |
Noradrenaline exhibits greater potency than adrenaline |
| Adrenoceptors |
(-)-adrenaline
(-)-noradrenaline Zn2+ |
β2-adrenoceptor |
ADRB2 |
Adrb2 |
Adrb2 |
Adrenaline exhibits greater potency than noradrenaline |
| Adrenoceptors |
(-)-adrenaline
(-)-noradrenaline |
β3-adrenoceptor |
ADRB3 |
Adrb3 |
Adrb3 |
|
| Angiotensin receptors | ||||||
| Family name | Ligand | Official IUPHAR receptor name | Human gene symbol | Rat gene symbol | Mouse gene symbol | Comment |
| Angiotensin receptors |
angiotensin A
{Sp: Human}
angiotensin II {Sp: Human, Mouse, Rat} angiotensin III {Sp: Human, Mouse, Rat} angiotensin IV {Sp: Human, Mouse, Rat} |
AT1 receptor |
AGTR1 |
Agtr1a Agtr1b |
Agtr1a Agtr1b |
|
| Angiotensin receptors |
angiotensin-(1-7)
{Sp: Human, Mouse, Rat}
angiotensin II {Sp: Human, Mouse, Rat} angiotensin III {Sp: Human, Mouse, Rat} |
AT2 receptor |
AGTR2 |
Agtr2 |
Agtr2 |
|
| Apelin receptor | ||||||
| Family name | Ligand | Official IUPHAR receptor name | Human gene symbol | Rat gene symbol | Mouse gene symbol | Comment |
| Apelin receptor |
apelin-36
{Sp: Human}
apelin-13 {Sp: Human, Mouse, Rat} apelin-17 {Sp: Human, Mouse, Rat} apelin-36 {Sp: Mouse, Rat} apelin receptor early endogenous ligand {Sp: Human} , apelin receptor early endogenous ligand {Sp: Mouse} Elabela/Toddler-32 {Sp: Human} Elabela/Toddler-21 {Sp: Human} Elabela/Toddler-11 {Sp: Human} [Pyr1]apelin-13 {Sp: Human, Mouse, Rat} |
apelin receptor |
APLNR |
Aplnr |
Aplnr |
|
| Bile acid receptor | ||||||
| Family name | Ligand | Official IUPHAR receptor name | Human gene symbol | Rat gene symbol | Mouse gene symbol | Comment |
| Bile acid receptor |
chenodeoxycholic acid
cholic acid deoxycholic acid lithocholic acid |
GPBA receptor |
GPBAR1 |
Gpbar1 |
Gpbar1 |
|
| Bombesin receptors | ||||||
| Family name | Ligand | Official IUPHAR receptor name | Human gene symbol | Rat gene symbol | Mouse gene symbol | Comment |
| Bombesin receptors |
gastrin-releasing peptide
{Sp: Human}
,
gastrin-releasing peptide
{Sp: Mouse, Rat}
,
gastrin-releasing peptide
{Sp: Pig}
gastrin releasing peptide(14-27) (human) GRP-(18-27) {Sp: Human, Pig} , GRP-(18-27) {Sp: Mouse, Rat} neuromedin B {Sp: Human, Mouse, Rat, Pig} |
BB1 receptor |
NMBR |
Nmbr |
Nmbr |
Neuromedin B is the endogenous agonist with the greatest potency |
| Bombesin receptors |
gastrin releasing peptide(14-27) (human)
GRP-(18-27) {Sp: Human, Pig} , GRP-(18-27) {Sp: Mouse, Rat} neuromedin B {Sp: Human, Mouse, Rat, Pig} neuromedin C |
BB2 receptor |
GRPR |
Grpr |
Grpr |
Gastrin-releasing peptide is the endogenous agonist with the greatest potency |
| Bombesin receptors | BB3 receptor |
BRS3 |
Brs3 |
Brs3 |
||
| Bradykinin receptors | ||||||
| Family name | Ligand | Official IUPHAR receptor name | Human gene symbol | Rat gene symbol | Mouse gene symbol | Comment |
| Bradykinin receptors |
bradykinin
{Sp: Human, Mouse, Rat}
[des-Arg9]bradykinin {Sp: Human, Mouse, Rat} [des-Arg10]kallidin {Sp: Human} [Hyp3]bradykinin {Sp: Human} kallidin {Sp: Human} Lys-[Hyp3]-bradykinin {Sp: Human} T-kinin {Sp: Human, Rat} |
B1 receptor |
BDKRB1 |
Bdkrb1 |
Bdkrb1 |
[Des-Arg10]kallidin is the most potent endogenous ligand in human |
| Bradykinin receptors |
bradykinin
{Sp: Human, Mouse, Rat}
[des-Arg9]bradykinin {Sp: Human, Mouse, Rat} [des-Arg10]kallidin {Sp: Human} [Hyp3]bradykinin {Sp: Human} kallidin {Sp: Human} Lys-[Hyp3]-bradykinin {Sp: Human} T-kinin {Sp: Human, Rat} |
B2 receptor |
BDKRB2 |
Bdkrb2 |
Bdkrb2 |
Bradykinin and kallidin are the most potent endogenous ligands |
| Cannabinoid receptors | ||||||
| Family name | Ligand | Official IUPHAR receptor name | Human gene symbol | Rat gene symbol | Mouse gene symbol | Comment |
| Cannabinoid receptors |
anandamide
2-arachidonoylglycerol |
CB1 receptor |
CNR1 |
Cnr1 |
Cnr1 |
Endogenous ligands include other endocannabinoids |
| Cannabinoid receptors |
anandamide
2-arachidonoylglycerol |
CB2 receptor |
CNR2 |
Cnr2 |
Cnr2 |
Endogenous ligands include other endocannabinoids |
| Chemerin receptors | ||||||
| Family name | Ligand | Official IUPHAR receptor name | Human gene symbol | Rat gene symbol | Mouse gene symbol | Comment |
| Chemerin receptors |
chemerin
{Sp: Human}
resolvin E1 |
chemerin receptor 1 |
CMKLR1 |
Cmklr1 |
Cmklr1 |
|
| Chemerin receptors |
chemerin
{Sp: Human}
|
chemerin receptor 2 |
CMKLR2 |
Cmklr2 |
Cmklr2 |
|
| Chemokine receptors | ||||||
| Family name | Ligand | Official IUPHAR receptor name | Human gene symbol | Rat gene symbol | Mouse gene symbol | Comment |
| Chemokine receptors |
CCL14
{Sp: Human}
CCL15 {Sp: Human} CCL23 {Sp: Human} CCL3 {Sp: Human} CCL5 {Sp: Human} CCL7 {Sp: Human} CCL13 {Sp: Human} CCL8 {Sp: Human} CCL16 {Sp: Human} CCL4 {Sp: Human} CCL3 {Sp: Mouse} CCL7 {Sp: Mouse} CCL8 {Sp: Mouse} CCL4 {Sp: Mouse} CCL5 {Sp: Mouse, Rat} CCL3 {Sp: Rat} CCL7 {Sp: Rat} CCL4 {Sp: Rat} |
CCR1 |
CCR1 |
Ccr1 |
Ccr1 |
CCL15 and CCL23 are the principal endogenous agonists |
| Chemokine receptors |
CCL24
{Sp: Human}
CCL7 {Sp: Human} CCL13 {Sp: Human} CCL2 {Sp: Human} CCL8 {Sp: Human} CCL16 {Sp: Human} CCL11 {Sp: Human} CCL26 {Sp: Human} CCL2 {Sp: Mouse} CCL7 {Sp: Mouse} CCL8 {Sp: Mouse} CCL11 {Sp: Mouse} CCL2 {Sp: Rat} CCL7 {Sp: Rat} CCL11 {Sp: Rat} |
CCR2 |
CCR2 |
Ccr2 |
Ccr2 |
CCL2 is the principal endogenous agonist |
| Chemokine receptors |
CCL15
{Sp: Human}
CCL5 {Sp: Human} CCL7 {Sp: Human} CCL11 {Sp: Human} CCL13 {Sp: Human} CCL8 {Sp: Human} CCL24 {Sp: Human} CCL26 {Sp: Human} CCL2 {Sp: Human} CCL28 {Sp: Human} CCL11 {Sp: Mouse} CCL7 {Sp: Mouse} CCL8 {Sp: Mouse} CCL24 {Sp: Mouse} CCL2 {Sp: Mouse} CCL28 {Sp: Mouse} CCL5 {Sp: Mouse, Rat} CCL7 {Sp: Rat} CCL11 {Sp: Rat} CCL2 {Sp: Rat} CXCL9 {Sp: Human} CXCL10 {Sp: Human} CXCL11 {Sp: Human} CXCL9 {Sp: Mouse} CXCL10 {Sp: Mouse} CXCL11 {Sp: Mouse} CXCL10 {Sp: Rat} |
CCR3 |
CCR3 |
Ccr3 |
Ccr3 |
CCL11, CCL24 and CCL26 are the principal endogenous agonists |
| Chemokine receptors |
CCL17
{Sp: Human}
CCL22 {Sp: Human} , CCL22 {Sp: Mouse} |
CCR4 |
CCR4 |
Ccr4 |
Ccr4 |
|
| Chemokine receptors |
CCL13
{Sp: Human}
CCL14 {Sp: Human} CCL3 {Sp: Human} CCL4 {Sp: Human} CCL5 {Sp: Human} CCL11 {Sp: Human} CCL8 {Sp: Human} CCL16 {Sp: Human} CCL2 {Sp: Human} CCL7 {Sp: Human} CCL11 {Sp: Mouse} CCL3 {Sp: Mouse} CCL4 {Sp: Mouse} CCL8 {Sp: Mouse} CCL2 {Sp: Mouse} CCL7 {Sp: Mouse} CCL5 {Sp: Mouse, Rat} CCL3 {Sp: Rat} CCL4 {Sp: Rat} CCL11 {Sp: Rat} CCL2 {Sp: Rat} CCL7 {Sp: Rat} |
CCR5 |
CCR5 |
Ccr5 |
Ccr5 |
|
| Chemokine receptors |
beta-defensin 4A
{Sp: Human}
CCL20 {Sp: Human} , CCL20 {Sp: Mouse} , CCL20 {Sp: Rat} de |
CCR6 |
CCR6 |
Ccr6 |
Ccr6 |
|
| Chemokine receptors |
CCL19
{Sp: Human}
CCL21 {Sp: Human} CCL19 {Sp: Mouse} Ccl21a {Sp: Mouse} Ccl21b {Sp: Mouse} |
CCR7 |
CCR7 |
Ccr7 |
Ccr7 |
|
| Chemokine receptors |
CCL1
{Sp: Human}
,
CCL1
{Sp: Mouse}
CCL8 {Sp: Mouse} |
CCR8 |
CCR8 |
Ccr8 |
Ccr8 |
CCL1 is the principal endogenous agonist |
| Chemokine receptors |
CCL25
{Sp: Human}
,
CCL25
{Sp: Mouse}
|
CCR9 |
CCR9 |
Ccr9 |
Ccr9 |
|
| Chemokine receptors |
CCL27
{Sp: Human}
CCL28 {Sp: Human} CCL27 {Sp: Mouse} CCL28 {Sp: Mouse} |
CCR10 |
CCR10 |
Ccr10 |
Ccr10 |
|
| Chemokine receptors |
CXCL6
{Sp: Human}
CXCL8 {Sp: Human} cytokine domain of tyrosyl tRNA synthetase {Sp: Human} |
CXCR1 |
CXCR1 |
Cxcr1 |
Cxcr1 |
CXCL8 is the principal endogenous agonist |
| Chemokine receptors |
CXCL1
{Sp: Human}
CXCL6 {Sp: Human} CXCL8 {Sp: Human} CXCL2 {Sp: Human} CXCL3 {Sp: Human} CXCL5 {Sp: Human} CXCL7 {Sp: Human} CXCL1 {Sp: Mouse} CXCL2 {Sp: Mouse} CXCL3 {Sp: Mouse} CXCL5 {Sp: Mouse} CXCL1 {Sp: Rat} CXCL2 {Sp: Rat} CXCL3 {Sp: Rat} CXCL5 {Sp: Rat} |
CXCR2 |
CXCR2 |
Cxcr2 |
Cxcr2 |
macrophage derived lectin is a proposed ligand, single publication |
| Chemokine receptors |
CCL5
{Sp: Human}
CCL7 {Sp: Human} CCL11 {Sp: Human} CCL13 {Sp: Human} CCL20 {Sp: Human} CCL19 {Sp: Human} CXCL12α {Sp: Human} CXCL10 {Sp: Human} CXCL11 {Sp: Human} CXCL9 {Sp: Human} , CXCL9 {Sp: Mouse} CXCL10 {Sp: Mouse} CXCL11 {Sp: Mouse} CXCL10 {Sp: Rat} |
CXCR3 |
CXCR3 |
Cxcr3 |
Cxcr3 |
|
| Chemokine receptors |
CXCL12γ
{Sp: Human}
CXCL12δ {Sp: Human} CXCL12ε {Sp: Human} CXCL12φ {Sp: Human} CXCL12β {Sp: Human} CXCL12α {Sp: Human} CXCL12 {Sp: Mouse} |
CXCR4 |
CXCR4 |
Cxcr4 |
Cxcr4 |
SDF1α and SDF1β are the active isomers of CXCL12 |
| Chemokine receptors |
CXCL13
{Sp: Human}
,
CXCL13
{Sp: Mouse}
|
CXCR5 |
CXCR5 |
Cxcr5 |
Cxcr5 |
|
| Chemokine receptors |
CXCL16
{Sp: Human}
,
CXCL16
{Sp: Mouse}
,
CXCL16
{Sp: Rat}
|
CXCR6 |
CXCR6 |
Cxcr6 |
Cxcr6 |
|
| Chemokine receptors |
CX3CL1
{Sp: Human}
,
CX3CL1
{Sp: Mouse}
,
CX3CL1
{Sp: Rat}
|
CX3CR1 |
CX3CR1 |
Cx3cr1 |
Cx3cr1 |
|
| Chemokine receptors |
XCL1
{Sp: Human}
XCL2 {Sp: Human} XCL1 {Sp: Mouse} , XCL1 {Sp: Rat} |
XCR1 |
XCR1 |
Xcr1 |
Xcr1 |
Specificity for the endogenous peptide XCL1 at the chemokine-GPCR interface has been determined [...]. |
| Chemokine receptors | ACKR1 |
ACKR1 |
Ackr1 |
Ackr1 |
||
| Chemokine receptors | ACKR2 |
ACKR2 |
Ackr2 |
Ackr2 |
||
| Chemokine receptors |
adrenomedullin
{Sp: Rat}
CXCL11 {Sp: Human} CXCL12α {Sp: Human} |
ACKR3 |
ACKR3 |
Ackr3 |
Ackr3 |
Several lines of evidence have suggested that adrenomedullin is a ligand for ACKR3; however, classical direct binding to the receptor has not yet been convincingly demonstrated. |
| Chemokine receptors |
CCL19
{Sp: Human}
CCL21 {Sp: Human} CCL25 {Sp: Human} |
ACKR4 |
ACKR4 |
Ackr4 |
Ackr4 |
|
| Chemokine receptors |
CCL19
{Sp: Human}
,
CCL19
{Sp: Mouse}
|
CCRL2 |
CCRL2 |
Ccrl2 |
Ccrl2 |
|
| Cholecystokinin receptors | ||||||
| Family name | Ligand | Official IUPHAR receptor name | Human gene symbol | Rat gene symbol | Mouse gene symbol | Comment |
| Cholecystokinin receptors |
CCK-58
{Sp: Human}
CCK-39 {Sp: Human} CCK-4 {Sp: Human} CCK-33 {Sp: Human} CCK-8 {Sp: Human, Mouse, Rat} CCK-33 {Sp: Mouse} , CCK-33 {Sp: Rat} gastrin-17 {Sp: Human} , gastrin-17 {Sp: Mouse} , gastrin-17 {Sp: Rat} |
CCK1 receptor |
CCKAR |
Cckar |
Cckar |
CCK-58 is an endogenous peptide fragment from the cholecystokinin precursor protein, but there is no affinity data available for this ligand at cholecystokinin receptors. For the rodent homologues of this peptide please see the following ligand entries: CCK-58 (mouse) and CCK-58 (rat). |
| Cholecystokinin receptors |
CCK-4
{Sp: Human}
CCK-33 {Sp: Human} CCK-8 {Sp: Human, Mouse, Rat} CCK-33 {Sp: Mouse} , CCK-33 {Sp: Rat} desulfated cholecystokinin-8 desulfated gastrin-14 {Sp: Human} desulfated gastrin-17 {Sp: Human} desulfated gastrin-34 {Sp: Human} desulfated gastrin-71 {Sp: Human} gastrin-34 {Sp: Human} gastrin-71 {Sp: Human} gastrin-14 {Sp: Human} gastrin-17 {Sp: Human} , gastrin-17 {Sp: Mouse} , gastrin-17 {Sp: Rat} |
CCK2 receptor |
CCKBR |
Cckbr |
Cckbr |
CCK-58 is an endogenous peptide fragment from the cholecystokinin precursor protein, but there is no affinity data available for this ligand at cholecystokinin receptors. For the rodent homologues of this peptide please see the following ligand entries: CCK-58 (mouse) and CCK-58 (rat). Gastrin-34 is one of the main forms of secreted gastrin present in the blood but there is no activity data for its interactions with this receptor. For the rodent homologues of this peptide please see gastrin-34 (mouse) and gastrin-34 (rat). Desulfated gastrin-14 (minigastrin) is an endogenous antagonist of cholecystokinin and radiolabelled analogues of this peptide are used as probes for this receptor. The gastrin precursor peptide is also cleaved into larger peptides gastrin-52 and gastrin-71. |
| Class A Orphans | ||||||
| Family name | Ligand | Official IUPHAR receptor name | Human gene symbol | Rat gene symbol | Mouse gene symbol | Comment |
| Class A Orphans |
sphingosine 1-phosphate
|
GPR3 |
GPR3 |
Gpr3 |
Gpr3 |
Proposed ligand, single publication |
| Class A Orphans | Protons | GPR4 |
GPR4 |
Gpr4 |
Gpr4 |
The role of GPR4 as a proton-sensing receptor is supported by several publications. |
| Class A Orphans | GPR42 |
GPR42 |
Very closely related to FFA3. Might be a pseudogene. | |||
| Class A Orphans |
sphingosine 1-phosphate
|
GPR6 |
GPR6 |
Gpr6 |
Gpr6 |
Proposed ligand, single publication |
| Class A Orphans |
sphingosine 1-phosphate
|
GPR12 |
GPR12 |
Gpr12 |
Gpr12 |
Proposed ligand, single publication |
| Class A Orphans | GPR15 |
GPR15 |
Gpr15 |
Gpr15 |
||
| Class A Orphans |
ATP
LTC4 LTD4 LTE4 UDP UDP-galactose UDP-glucose cysteinyl-leukotrienes (CysLTs), uracil nucleotides |
GPR17 |
GPR17 |
Gpr17 |
Gpr17 |
Proposed ligands, single publication |
| Class A Orphans | GPR19 |
GPR19 |
Gpr19 |
Gpr19 |
||
| Class A Orphans | GPR20 |
GPR20 |
Gpr20 |
Gpr20 |
||
| Class A Orphans | GPR21 |
GPR21 |
Gpr21 |
Gpr21 |
||
| Class A Orphans | GPR22 |
GPR22 |
Gpr22 |
Gpr22 |
||
| Class A Orphans | GPR25 |
GPR25 |
Gpr25 |
Gpr25 |
||
| Class A Orphans | GPR26 |
GPR26 |
Gpr26 |
Gpr26 |
||
| Class A Orphans | GPR27 |
GPR27 |
Gpr27 |
Gpr27 |
||
| Class A Orphans |
12S-HETE
|
GPR31 |
GPR31 |
Gpr31 |
Gpr31c |
Proposed ligand, single publication |
| Class A Orphans |
LXA4
resolvin D1 |
GPR32 |
GPR32 |
Proposed ligand, single publication | ||
| Class A Orphans | GPR33 |
GPR33 |
Gpr33-ps1 |
Gpr33 |
pseudogene in most individuals | |
| Class A Orphans |
lysophosphatidylserine
|
GPR34 |
GPR34 |
Gpr34 |
Gpr34 |
Proposed ligand in several publications but not replicated in a recent study based on β-arrestin recruitment [...]. |
| Class A Orphans |
kynurenic acid
2-oleoyl-LPA |
GPR35 |
GPR35 |
Gpr35 |
Gpr35 |
Proposed ligands, single publications |
| Class A Orphans |
prosaptide
{Sp: Human}
prosaposin |
GPR37 |
GPR37 |
Gpr37 |
Gpr37 |
Proposed ligand, single publication |
| Class A Orphans |
prosaptide
{Sp: Human}
prosaposin |
GPR37L1 |
GPR37L1 |
Gpr37l1 |
Gpr37l1 |
Proposed ligand, single publication. |
| Class A Orphans |
obestatin
{Sp: Human}
,
obestatin
{Sp: Mouse, Rat}
Zn2+ |
GPR39 |
GPR39 |
Gpr39 |
Gpr39 |
Proposed ligands, single publications, but results for obestatin could not be repeated and have since been retracted |
| Class A Orphans | GPR45 |
GPR45 |
Gpr45 |
Gpr45 |
||
| Class A Orphans | GPR50 |
GPR50 |
Gpr50 |
Gpr50 |
||
| Class A Orphans | GPR52 |
GPR52 |
Gpr52 |
Gpr52 |
||
| Class A Orphans | GPR61 |
GPR61 |
Gpr61 |
Gpr61 |
||
| Class A Orphans | GPR62 |
GPR62 |
Gpr62 |
Gpr62 |
||
| Class A Orphans |
dihydrosphingosine 1-phosphate
dioleoylphosphatidic acid sphingosine 1-phosphate |
GPR63 |
GPR63 |
Gpr63 |
Gpr63 |
Proposed ligand, single publication |
| Class A Orphans | Protons | GPR65 |
GPR65 |
Gpr65 |
Gpr65 |
|
| Class A Orphans | Protons | GPR68 |
GPR68 |
Gpr68 |
Gpr68 |
|
| Class A Orphans |
CCL5
{Sp: Human}
|
GPR75 |
GPR75 |
Gpr75 |
Gpr75 |
CCL5 was reported to be an agonist of GPR75 by Ignatov et al. [...] but the pairing could not be repeated in a recent β-arrestin assay [...]. |
| Class A Orphans | GPR78 |
GPR78 |
||||
| Class A Orphans | GPR79 |
GPR79 |
||||
| Class A Orphans | GPR82 |
GPR82 |
Gpr82 |
|||
| Class A Orphans | GPR83 |
GPR83 |
Gpr83 |
Gpr83 |
||
| Class A Orphans | Medium-chain-length fatty acids | GPR84 |
GPR84 |
Gpr84 |
Gpr84 |
Medium chain free fatty acids with carbon chain lengths of 9-14 have been shown by several groups to activate GPR84 [...][...][...]. A surrogate ligand for GPR84, 6-n-octylaminouracil, has also been proposed [...]. |
| Class A Orphans | GPR85 |
GPR85 |
Gpr85 |
Gpr85 |
||
| Class A Orphans |
LPA
|
GPR87 |
GPR87 |
Gpr87 |
Gpr87 |
Proposed ligand, single publication |
| Class A Orphans | GPR88 |
GPR88 |
Gpr88 |
Gpr88 |
||
| Class A Orphans | GPR101 |
GPR101 |
Gpr101 |
Gpr101 |
||
| Class A Orphans |
9-hydroxyoctadecadienoic acid
(lyso)phospholipid mediators, protons |
GPR132 |
GPR132 |
Gpr132 |
Gpr132 |
|
| Class A Orphans | GPR135 |
GPR135 |
Gpr135 |
Gpr135 |
||
| Class A Orphans |
L-phenylalanine
L-tryptophan |
GPR139 |
GPR139 |
Gpr139 |
Gpr139 |
|
| Class A Orphans | GPR141 |
GPR141 |
Gpr141 |
Gpr141 |
||
| Class A Orphans | GPR142 |
GPR142 |
Gpr142 |
Gpr142 |
||
| Class A Orphans | GPR146 |
GPR146 |
Gpr146 |
Gpr146 |
||
| Class A Orphans | GPR148 |
GPR148 |
||||
| Class A Orphans | GPR149 |
GPR149 |
Gpr149 |
Gpr149 |
||
| Class A Orphans | GPR150 |
GPR150 |
Gpr150 |
Gpr150 |
||
| Class A Orphans | GPR151 |
GPR151 |
Gpr151 |
Gpr151 |
||
| Class A Orphans | GPR152 |
GPR152 |
Gpr152 |
Gpr152 |
||
| Class A Orphans | GPR153 |
GPR153 |
Gpr153 |
Gpr153 |
||
| Class A Orphans | GPR160 |
GPR160 |
Gpr160 |
Gpr160 |
||
| Class A Orphans | GPR161 |
GPR161 |
Gpr161 |
Gpr161 |
||
| Class A Orphans | GPR162 |
GPR162 |
Gpr162 |
Gpr162 |
||
| Class A Orphans | GPR171 |
GPR171 |
Gpr171 |
Gpr171 |
||
| Class A Orphans | GPR173 |
GPR173 |
Gpr173 |
Gpr173 |
||
| Class A Orphans |
lysophosphatidylserine
|
GPR174 |
GPR174 |
Gpr174 |
Gpr174 |
Proposed ligand, two publications |
| Class A Orphans | GPR176 |
GPR176 |
Gpr176 |
Gpr176 |
||
| Class A Orphans | GPR182 |
GPR182 |
Gpr182 |
Gpr182 |
||
| Class A Orphans |
7α,27-dihydroxycholesterol
7β, 27-dihydroxycholesterol 7β, 25-dihydroxycholesterol 7α,25-dihydroxycholesterol 27-hydroxycholesterol 25-hydroxycholesterol 7α-hydroxycholesterol 7β-hydroxycholesterol Oxysterols |
GPR183 |
GPR183 |
Gpr183 |
Gpr183 |
Proposed ligands, two independent publications |
| Class A Orphans |
R-spondin-1
{Sp: Human}
R-spondin-2 {Sp: Human} R-spondin-3 {Sp: Human} R-spondin-4 {Sp: Human} R-spondins |
LGR4 |
LGR4 |
Lgr4 |
Lgr4 |
Proposed ligands, single publication |
| Class A Orphans |
R-spondin-1
{Sp: Human}
R-spondin-2 {Sp: Human} R-spondin-3 {Sp: Human} R-spondin-4 {Sp: Human} |
LGR5 |
LGR5 |
Lgr5 |
Lgr5 |
|
| Class A Orphans |
R-spondin-1
{Sp: Human}
R-spondin-2 {Sp: Human} R-spondin-3 {Sp: Human} R-spondin-4 {Sp: Human} R-spondins |
LGR6 |
LGR6 |
Lgr6 |
Lgr6 |
Proposed ligands, single publication |
| Class A Orphans | MAS1 |
MAS1 |
Mas1 |
Mas1 |
||
| Class A Orphans | MAS1L |
MAS1L |
||||
| Class A Orphans |
β-alanine
|
MRGPRD |
MRGPRD |
Mrgprd |
Mrgprd |
Proposed ligand, two publications |
| Class A Orphans | MRGPRE |
MRGPRE |
Mrgpre |
Mrgpre |
||
| Class A Orphans | MRGPRF |
MRGPRF |
Mrgprf |
Mrgprf |
||
| Class A Orphans | MRGPRG |
MRGPRG |
Mrgprg |
Mrgprg |
||
| Class A Orphans |
bovine adrenal medulla peptide 8-22
{Sp: Human}
|
MRGPRX1 |
MRGPRX1 |
Proposed ligand, two publications | ||
| Class A Orphans |
PAMP-20
{Sp: Human}
|
MRGPRX2 |
MRGPRX2 |
Proposed ligand, two publications | ||
| Class A Orphans | MRGPRX3 |
MRGPRX3 |
||||
| Class A Orphans | MRGPRX4 |
MRGPRX4 |
||||
| Class A Orphans | P2RY8 |
P2RY8 |
||||
| Class A Orphans |
LPA
sphingosine 1-phosphate |
P2RY10 |
P2RY10 |
P2ry10 |
P2ry10 |
Proposed ligands, single publication |
| Class A Orphans | TAAR2 |
TAAR2 |
Taar2 |
Taar2 |
||
| Class A Orphans |
isoamylamine
|
TAAR3 |
TAAR3P |
Taar3 |
Taar3 |
probable pseudogene. |
| Class A Orphans | TAAR4P |
TAAR4P |
Taar4 |
Taar4 |
||
| Class A Orphans | TAAR5 |
TAAR5 |
Taar5 |
Taar5 |
||
| Class A Orphans | TAAR6 |
TAAR6 |
Taar6 |
Taar6 |
||
| Class A Orphans | TAAR8 |
TAAR8 |
Taar8a |
Taar8b |
||
| Class A Orphans | TAAR9 |
TAAR9 |
Taar9 |
Taar9 |
||
| Complement peptide receptors | ||||||
| Family name | Ligand | Official IUPHAR receptor name | Human gene symbol | Rat gene symbol | Mouse gene symbol | Comment |
| Complement peptide receptors |
C5a
{Sp: Human}
C3a {Sp: Human} C5a {Sp: Mouse} C3a {Sp: Mouse} C5a {Sp: Rat} C3a {Sp: Rat} |
C3a receptor |
C3AR1 |
C3ar1 |
C3ar1 |
C3a anaphylatoxin has a higher potency than C5a anaphylatoxin |
| Complement peptide receptors |
C5a
{Sp: Human}
C3a {Sp: Human} C5a {Sp: Mouse} C3a {Sp: Mouse} C5a {Sp: Rat} C3a {Sp: Rat} C5a des-Arg {Sp: Human} ribosomal protein S19 {Sp: Human} |
C5a1 receptor |
C5AR1 |
C5ar1 |
C5ar1 |
C5a anaphylatoxin has a higher potency than C3a anaphylatoxin |
| Complement peptide receptors |
C5a
{Sp: Human}
C5a des-Arg {Sp: Human} |
C5a2 receptor |
C5AR2 |
C5ar2 |
C5ar2 |
|
| Dopamine receptors | ||||||
| Family name | Ligand | Official IUPHAR receptor name | Human gene symbol | Rat gene symbol | Mouse gene symbol | Comment |
| Dopamine receptors |
dopamine
5-hydroxytryptamine noradrenaline |
D1 receptor |
DRD1 |
Drd1 |
Drd1 |
|
| Dopamine receptors |
dopamine
|
D2 receptor |
DRD2 |
Drd2 |
Drd2 |
|
| Dopamine receptors |
dopamine
|
D3 receptor |
DRD3 |
Drd3 |
Drd3 |
|
| Dopamine receptors |
dopamine
|
D4 receptor |
DRD4 |
Drd4 |
Drd4 |
|
| Dopamine receptors |
dopamine
5-hydroxytryptamine noradrenaline |
D5 receptor |
DRD5 |
Drd5 |
Drd5 |
|
| Endothelin receptors | ||||||
| Family name | Ligand | Official IUPHAR receptor name | Human gene symbol | Rat gene symbol | Mouse gene symbol | Comment |
| Endothelin receptors |
endothelin-2
{Sp: Human}
endothelin-1 {Sp: Human, Mouse, Rat} endothelin-2 {Sp: Mouse, Rat} |
ETA receptor |
EDNRA |
Ednra |
Ednra |
Endothelin-3 is a low potency endogenous agonist |
| Endothelin receptors |
endothelin-2
{Sp: Human}
endothelin-1 {Sp: Human, Mouse, Rat} endothelin-3 {Sp: Human, Mouse, Rat} endothelin-2 {Sp: Mouse, Rat} |
ETB receptor |
EDNRB |
Ednrb |
Ednrb |
|
| Formylpeptide receptors | ||||||
| Family name | Ligand | Official IUPHAR receptor name | Human gene symbol | Rat gene symbol | Mouse gene symbol | Comment |
| Formylpeptide receptors |
annexin I
{Sp: Human}
,
annexin I
{Sp: Mouse}
,
annexin I
{Sp: Rat}
cathepsin G {Sp: Human} , cathepsin G {Sp: Mouse} , cathepsin G {Sp: Rat} spinorphin |
FPR1 |
FPR1 |
Fpr1 |
Fpr1 |
|
| Formylpeptide receptors |
annexin I
{Sp: Human}
,
annexin I
{Sp: Mouse}
,
annexin I
{Sp: Rat}
aspirin triggered lipoxin A4 aspirin-triggered resolvin D1 CRAMP {Sp: Mouse} humanin {Sp: Human} LL-37 {Sp: Human} LXA4 PrP106-126 resolvin D1 serum amyloid A {Sp: Human} |
FPR2 |
FPR2 |
Fpr2 |
Fpr2 |
|
| Formylpeptide receptors |
annexin I-(2-26)
{Sp: Human}
F2L {Sp: Human} , F2L {Sp: Mouse, Rat} humanin {Sp: Human} |
FPR3 |
FPR3 |
Fpr3 |
Fpr3 |
|
| Free fatty acid receptors | ||||||
| Family name | Ligand | Official IUPHAR receptor name | Human gene symbol | Rat gene symbol | Mouse gene symbol | Comment |
| Free fatty acid receptors |
docosahexaenoic acid
α-linolenic acid myristic acid oleic acid long chain carboxylic acids |
FFA1 receptor |
FFAR1 |
Ffar1 |
Ffar1 |
|
| Free fatty acid receptors |
acetic acid
butyric acid 1-methylcyclopropanecarboxylic acid propanoic acid trans-2-methylcrotonic acid |
FFA2 receptor |
FFAR2 |
Ffar2 |
Ffar2 |
|
| Free fatty acid receptors |
butyric acid
1-methylcyclopropanecarboxylic acid propanoic acid |
FFA3 receptor |
FFAR3 |
Ffar3 |
Ffar3 |
|
| Free fatty acid receptors |
linoleic acid
α-linolenic acid myristic acid oleic acid Free fatty acids |
FFA4 receptor |
FFAR4 |
Ffar4 |
Ffar4 |
|
| Free fatty acid receptors | GPR42 |
GPR42 |
Very closely related to FFA3. Might be a pseudogene. | |||
| Galanin receptors | ||||||
| Family name | Ligand | Official IUPHAR receptor name | Human gene symbol | Rat gene symbol | Mouse gene symbol | Comment |
| Galanin receptors |
galanin
{Sp: Human}
,
galanin
{Sp: Mouse, Rat}
galanin-like peptide {Sp: Human} , galanin-like peptide {Sp: Mouse} , galanin-like peptide {Sp: Rat} |
GAL1 receptor |
GALR1 |
Galr1 |
Galr1 |
Galanin is more potent than galanin-like peptide |
| Galanin receptors |
galanin
{Sp: Human}
,
galanin
{Sp: Mouse, Rat}
galanin-like peptide {Sp: Human} , galanin-like peptide {Sp: Mouse} , galanin-like peptide {Sp: Rat} spexin-1 {Sp: Human} |
GAL2 receptor |
GALR2 |
Galr2 |
Galr2 |
|
| Galanin receptors |
galanin
{Sp: Human}
,
galanin
{Sp: Mouse, Rat}
galanin-like peptide {Sp: Human} , galanin-like peptide {Sp: Mouse} , galanin-like peptide {Sp: Rat} spexin-1 {Sp: Human} |
GAL3 receptor |
GALR3 |
Galr3 |
Galr3 |
Galanin-like peptide is more potent than galanin |
| Ghrelin receptor | ||||||
| Family name | Ligand | Official IUPHAR receptor name | Human gene symbol | Rat gene symbol | Mouse gene symbol | Comment |
| Ghrelin receptor |
[des-Gln14]ghrelin
{Sp: Human}
,
[des-Gln14]ghrelin
{Sp: Mouse, Rat}
ghrelin {Sp: Human} , ghrelin {Sp: Mouse, Rat} |
ghrelin receptor |
GHSR |
Ghsr |
Ghsr |
The major circulating form of ghrelin is [des-octanoyl]ghrelin (human)/[des-octanoyl]ghrelin (mouse/rat). |
| Glycoprotein hormone receptors | ||||||
| Family name | Ligand | Official IUPHAR receptor name | Human gene symbol | Rat gene symbol | Mouse gene symbol | Comment |
| Glycoprotein hormone receptors |
FSH
{Sp: Human}
,
FSH
{Sp: Mouse}
,
FSH
{Sp: Rat}
|
FSH receptor |
FSHR |
Fshr |
Fshr |
|
| Glycoprotein hormone receptors |
hCG
{Sp: Human}
LH {Sp: Human} , LH {Sp: Mouse} , LH {Sp: Rat} |
LH receptor |
LHCGR |
Lhcgr |
Lhcgr |
|
| Glycoprotein hormone receptors |
TSH
{Sp: Human}
,
TSH
{Sp: Mouse}
,
TSH
{Sp: Rat}
|
TSH receptor |
TSHR |
Tshr |
Tshr |
|
| Gonadotrophin-releasing hormone receptors | ||||||
| Family name | Ligand | Official IUPHAR receptor name | Human gene symbol | Rat gene symbol | Mouse gene symbol | Comment |
| Gonadotrophin-releasing hormone receptors |
GnRH I
{Sp: Human, Mouse, Rat}
GnRH II {Sp: Human} |
GnRH1 receptor |
GNRHR |
Gnrhr |
Gnrhr |
GnRH I is the more potent agonist |
| Gonadotrophin-releasing hormone receptors |
GnRH I
{Sp: Human, Mouse, Rat}
GnRH II {Sp: Human} |
GnRH2 receptor |
GNRHR2 |
Probable transcribed pseudogene in man [...]. Natural/endogenous ligands refer to non-human mammalian species. | ||
| GPR18, GPR55 and GPR119 | ||||||
| Family name | Ligand | Official IUPHAR receptor name | Human gene symbol | Rat gene symbol | Mouse gene symbol | Comment |
| GPR18, GPR55 and GPR119 |
N-arachidonoylglycine
|
GPR18 |
GPR18 |
Gpr18 |
Gpr18 |
|
| GPR18, GPR55 and GPR119 |
anandamide
2-arachidonoylglycerol 2-arachidonoylglycerolphosphoinositol lysophosphatidylinositol N-palmitoylethanolamine |
GPR55 |
GPR55 |
Gpr55 |
Gpr55 |
Proposed ligand, several publications |
| GPR18, GPR55 and GPR119 |
N-oleoylethanolamide
N-palmitoylethanolamine SEA |
GPR119 |
GPR119 |
Gpr119 |
Gpr119 |
Proposed ligand, two publications |
| G protein-coupled estrogen receptor | ||||||
| Family name | Ligand | Official IUPHAR receptor name | Human gene symbol | Rat gene symbol | Mouse gene symbol | Comment |
| G protein-coupled estrogen receptor |
17β-estradiol
|
GPER |
GPER1 |
Gper1 |
Gper1 |
Southern et al. (2013) were unable to detect 17β-estradiol-GPER engagement using the PathHunter™ β-Arrestin recruitment assay [...]. |
| Histamine receptors | ||||||
| Family name | Ligand | Official IUPHAR receptor name | Human gene symbol | Rat gene symbol | Mouse gene symbol | Comment |
| Histamine receptors |
histamine
|
H1 receptor |
HRH1 |
Hrh1 |
Hrh1 |
|
| Histamine receptors |
histamine
|
H2 receptor |
HRH2 |
Hrh2 |
Hrh2 |
|
| Histamine receptors |
histamine
|
H3 receptor |
HRH3 |
Hrh3 |
Hrh3 |
|
| Histamine receptors |
CCL16
{Sp: Human}
histamine |
H4 receptor |
HRH4 |
Hrh4 |
Hrh4 |
|
| Hydroxycarboxylic acid receptors | ||||||
| Family name | Ligand | Official IUPHAR receptor name | Human gene symbol | Rat gene symbol | Mouse gene symbol | Comment |
| Hydroxycarboxylic acid receptors |
L-lactic acid
|
HCA1 receptor |
HCAR1 |
Hcar1 |
Hcar1 |
Proposed ligand, two publications |
| Hydroxycarboxylic acid receptors |
butyric acid
β-D-hydroxybutyric acid |
HCA2 receptor |
HCAR2 |
Hcar2 |
Hcar2 |
|
| Hydroxycarboxylic acid receptors |
3-hydroxyoctanoic acid
|
HCA3 receptor |
HCAR3 |
|||
| Kisspeptin receptor | ||||||
| Family name | Ligand | Official IUPHAR receptor name | Human gene symbol | Rat gene symbol | Mouse gene symbol | Comment |
| Kisspeptin receptor |
kisspeptin-10
{Sp: Human}
kisspeptin-13 {Sp: Human} kisspeptin-14 {Sp: Human} kisspeptin-54 {Sp: Human} kisspeptin-52 {Sp: Mouse} kisspeptin-10 {Sp: Mouse, Rat} kisspeptin-52 {Sp: Rat} |
kisspeptin receptor |
KISS1R |
Kiss1r |
||