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mGlu5 receptor

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Target not currently curated in GtoImmuPdb

Target id: 293

Nomenclature: mGlu5 receptor

Family: Metabotropic glutamate receptors

Gene and Protein Information Click here for help
class C G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 1212 11q14.2 GRM5 glutamate metabotropic receptor 5 59-60
Mouse 7 1203 7 D3 Grm5 glutamate receptor, metabotropic 5
Rat 7 1203 1q32 Grm5 glutamate metabotropic receptor 5 1,40
Previous and Unofficial Names Click here for help
mGluR5 | GPRC1E | glutamate receptor
Database Links Click here for help
Specialist databases
GPCRDB grm5_human (Hs), grm5_mouse (Mm), grm5_rat (Rn)
Other databases
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Structure of the human class C GPCR metabotropic glutamate receptor 5 transmembrane domain in complex with the negative allosteric modulator mavoglurant
PDB Id:  4OO9
Ligand:  mavoglurant
Resolution:  2.6Å
Species:  Human
References:  23
Natural/Endogenous Ligands Click here for help
L-glutamic acid
Comments: Other endogenous ligands include L-aspartic acid, L-serine-O-phosphate, NAAG and L-cysteine sulphinic acid

Download all structure-activity data for this target as a CSV file go icon to follow link

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
VU0424465 Small molecule or natural product Rn Agonist 6.8 pEC50 81
pEC50 6.8 (EC50 1.71x10-7 M) [81]
VU0092273 Small molecule or natural product Rn Agonist 5.9 pEC50 64
pEC50 5.9 (EC50 1.3x10-6 M) [64]
L-glutamic acid Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Hs Agonist 5.0 – 5.5 pEC50 71
pEC50 5.0 – 5.5 [71]
(S)-(+)-CBPG Small molecule or natural product Click here for species-specific activity table Rn Partial agonist 4.3 pEC50 55
pEC50 4.3 (EC50 4.7x10-5 M) [55]
quisqualate Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 7.5 pIC50 62
pIC50 7.5 [62]
L-glutamic acid Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Rn Full agonist 6.1 pIC50 62
pIC50 6.1 [62]
L-CCG-I Small molecule or natural product Click here for species-specific activity table Rn Full agonist 5.8 pIC50 62
pIC50 5.8 [62]
(1S,3R)-ACPD Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 5.7 pIC50 62
pIC50 5.7 [62]
ibotenic acid Small molecule or natural product Click here for species-specific activity table Rn Full agonist 5.7 pIC50 62
pIC50 5.7 [62]
3,5-DHPG Small molecule or natural product Click here for species-specific activity table Rn Partial agonist 5.4 pIC50 62
pIC50 5.4 [62]
(S)-3HPG Small molecule or natural product Click here for species-specific activity table Rn Partial agonist 5.0 pIC50 62
pIC50 5.0 [62]
CHPG Small molecule or natural product Hs Full agonist 3.4 pIC50 62
pIC50 3.4 [62]
View species-specific agonist tables
Agonist Comments
Indicated affinities were determined by displacement studies of [3H]quisqualate bound on HEK cell membranes expressing a recombinant rat mGlu5. This is the only study describing affinity values for these compounds. More information on agonist potencies determined from functional studies can be obtained from [83]. So far no differences have been reported for the agonist affinities between the rat and the human receptor.
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[11C]JNJ-16567083 Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Rn Antagonist 5.6 pKi 37
pKi 5.6 (Ki 2.366x10-6 M) [37]
methoxy-MPEP Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Antagonist 8.4 pIC50 29
pIC50 8.4 (IC50 3.6x10-9 M) [29]
Description: [3H]-M-MPEP displacement assay.
ACDPP Small molecule or natural product Hs Antagonist 6.9 pIC50 6
pIC50 6.9 [6]
(S)-4C3HPG Small molecule or natural product Click here for species-specific activity table Rn Antagonist 5.6 pIC50 62
pIC50 5.6 [62]
LY341495 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 5.1 pIC50 43
pIC50 5.1 [43]
DCG-IV Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 4.7 pIC50 62
pIC50 4.7 [62]
(S)-4CPG Small molecule or natural product Click here for species-specific activity table Rn Antagonist 4.6 pIC50 62
pIC50 4.6 [62]
(+)-MCPG Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 3.7 pIC50 62
pIC50 3.7 [62]
View species-specific antagonist tables
Antagonist Comments
Indicated affinities were determined by displacement studies of [3H]quisqualate bound on HEK cell membranes expressing a recombinant rat mGlu5 (except for LY341495 value determined from functional studies). This is the only study describing affinity values for these compounds.

More information on agonist potencies determined from functional studies can be obtained from [83]. So far no differences have been reported for the antagonist affinities between the rat and the human receptor.

Surprisingly, although LY367385 and AIDA displace Quisqualate binding, no antagonistic activity of these compounds have been observed in functional studies (see [83]). (S)-4C3HPG has been reported to have slight partial agonist activity at this receptor [40].
Allosteric Modulators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
VU0483605 Small molecule or natural product Rn Positive 6.5 pKB 35
pKB 6.5 [35]
GS39783 Small molecule or natural product Ligand has a PDB structure Rn Neutral 6.3 pKB 35
pKB 6.3 [35]
PHCCC Small molecule or natural product Click here for species-specific activity table Rn Neutral 5.6 pKB 35
pKB 5.6 [35]
AZ12216052 Small molecule or natural product Rn Positive 5.4 pKB 35
pKB 5.4 [35]
NPS 2143 Small molecule or natural product Rn Positive 5.1 pKB 35
pKB 5.1 [35]
CPCCOEt Small molecule or natural product Click here for species-specific activity table Rn Neutral 4.9 pKB 35
pKB 4.9 [35]
CGP7930 Small molecule or natural product Click here for species-specific activity table Rn Positive 4.8 pKB 35
pKB 4.8 [35]
[3H]CTEP Small molecule or natural product Ligand is labelled Ligand is radioactive Rn Negative 8.8 pKd 47
pKd 8.8 (Kd 1.5x10-9 M) [47]
[3H]CTEP Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Negative 8.8 pKd 47
pKd 8.8 (Kd 1.7x10-9 M) [47]
[3H]CTEP Small molecule or natural product Ligand is labelled Ligand is radioactive Mm Negative 8.7 pKd 47
pKd 8.7 (Kd 1.8x10-9 M) [47]
[3H]methoxy-PEPy Small molecule or natural product Ligand is labelled Ligand is radioactive Rn Negative 8.5 pKd 20
pKd 8.5 (Kd 3.4x10-9 M) [20]
[3H]methoxymethyl-MTEP Small molecule or natural product Ligand is labelled Ligand is radioactive Rn Negative 7.7 pKd 20
pKd 7.7 (Kd 2x10-8 M) [20]
[3H]fenobam Small molecule or natural product Ligand is labelled Ligand is radioactive Ligand has a PDB structure Hs Negative 7.5 pKd 74
pKd 7.5 [74]
[3H]fenobam Small molecule or natural product Ligand is labelled Ligand is radioactive Ligand has a PDB structure Rn Negative 7.3 pKd 74
pKd 7.3 [74]
compound 20 [PMID: 16439120] Small molecule or natural product Rn Negative 9.0 pKi 13
pKi 9.0 (Ki 1x10-9 M) [13]
BOMA Small molecule or natural product Hs Negative 8.5 pKi 99
pKi 8.5 [99]
AZD9272 Small molecule or natural product Hs Negative 8.4 pKi 75
pKi 8.4 (Ki 3.8x10-9 M) [75]
GRN-529 Small molecule or natural product Rn Negative 8.3 pKi 38
pKi 8.3 (Ki 5.4x10-9 M) [38]
CTEP Small molecule or natural product Mm Negative 8.0 pKi 47
pKi 8.0 (Ki 9.5x10-9 M) [47]
compound 26 [PMID: 16439120] Small molecule or natural product Rn Negative 8.0 pKi 13
pKi 8.0 (Ki 1x10-8 M) [13]
compound 30 [PMID: 21757343] Small molecule or natural product Hs Negative 7.9 pKi 100
pKi 7.9 (Ki 1.2x10-8 M) [100]
compound 10 [PMID: 15482906] Small molecule or natural product Hs Negative 7.9 pKi 36
pKi 7.9 (Ki 1.2x10-8 M) [36]
CTEP Small molecule or natural product Rn Negative 7.9 pKi 47
pKi 7.9 (Ki 1.26x10-8 M) [47]
compound 8 [PMID: 15482908] Small molecule or natural product Rn Negative 7.8 pKi 89
pKi 7.8 (Ki 1.4x10-8 M) [89]
MTEP Small molecule or natural product Hs Negative 7.8 pKi 10
pKi 7.8 (Ki 1.6x10-8 M) [10]
VU0285683 Small molecule or natural product Rn Negative 7.8 pKi 76
pKi 7.8 (Ki 1.6x10-8 M) [76]
compound 29b [PMID: 20809633] Small molecule or natural product Rn Negative 7.8 pKi 12
pKi 7.8 (Ki 1.7x10-8 M) [12]
CTEP Small molecule or natural product Hs Negative 7.7 – 7.8 pKi 39,47
pKi 7.7 – 7.8 (Ki 2x10-8 – 1.64x10-8 M) [39,47]
compound 10 [PMID: 15482908] Small molecule or natural product Rn Negative 7.7 pKi 89
pKi 7.7 (Ki 1.9x10-8 M) [89]
compound 23 [PMID: 17590335] Small molecule or natural product Rn Negative 7.7 pKi 57
pKi 7.7 (Ki 2.2x10-8 M) [57]
AZD6538 Small molecule or natural product Hs Negative 7.6 pKi 75
pKi 7.6 (Ki 2.8x10-8 M) [75]
compound 24d [PMID: 23357634] Small molecule or natural product Rn Negative 7.5 pKi 106
pKi 7.5 (Ki 3x10-8 M) [106]
basimglurant Small molecule or natural product Hs Negative 7.4 pKi 39
pKi 7.4 (Ki 3.6x10-8 M) [39]
Description: Reduction of antagonist MPEP binding to mGlu5 receptors in vitro
compound 16m [PMID: 19931453] Small molecule or natural product Hs Negative 7.4 pKi 90
pKi 7.4 (Ki 3.8x10-8 M) [90]
VU0366058 Small molecule or natural product Rn Negative 7.1 pKi 61
pKi 7.1 (Ki 8.4x10-8 M) [61]
compound 16a [PMID: 14697765] Small molecule or natural product Rn Negative 7.0 pKi 99
pKi 7.0 (Ki 9.1x10-8 M) [99]
compound 42 [PMID: 17189691] Small molecule or natural product Rn Negative 7.0 pKi 14
pKi 7.0 (Ki 9.5x10-8 M) [14]
compound 8 [PMID: 20598884] Small molecule or natural product Rn Negative 7.0 pKi 25
pKi 7.0 (Ki 1.02x10-7 M) [25]
VU-1545 Small molecule or natural product Rn Positive 6.8 pKi 22
pKi 6.8 (Ki 1.56x10-7 M) [22]
compound 11a [PMID: 14697765] Small molecule or natural product Rn Negative 6.8 pKi 99
pKi 6.8 (Ki 1.59x10-7 M) [99]
VU0360172 Small molecule or natural product Rn Positive 6.7 pKi 76
pKi 6.7 (Ki 1.95x10-7 M) [76]
compound 27 [PMID: 20598884] Small molecule or natural product Rn Negative 6.7 pKi 25
pKi 6.7 (Ki 2.06x10-7 M) [25]
VU-29 Small molecule or natural product Rn Positive 6.6 pKi 16
pKi 6.6 (Ki 2.44x10-7 M) [16]
M-5MPEP Small molecule or natural product Rn Negative 6.5 pKi 77
pKi 6.5 (Ki 3x10-7 M) [77]
Br-5MPEPy Small molecule or natural product Rn Negative 6.5 pKi 77
pKi 6.5 (Ki 3x10-7 M) [77]
LSN2463359 Small molecule or natural product Rn Positive 6.4 pKi 31
pKi 6.4 (Ki 3.77x10-7 M) [31]
5-MPEP Small molecule or natural product Rn Neutral 6.4 pKi 77
pKi 6.4 [77]
compound 18 [PMID: 21927650] Small molecule or natural product Rn Negative 6.3 pKi 48
pKi 6.3 (Ki 4.77x10-7 M) [48]
LSN2814617 Small molecule or natural product Rn Positive 5.9 pKi 31
pKi 5.9 (Ki 1.34x10-6 M) [31]
5PAM523 Small molecule or natural product Rn Positive 5.7 pKi 68
pKi 5.7 (Ki 2x10-6 M) [68]
CPPZ Small molecule or natural product Rn Positive 5.5 pKi 91
pKi 5.5 (Ki 3.1x10-6 M) [91]
ADX-47273 Small molecule or natural product Rn Positive 5.4 pKi 31
pKi 5.4 (Ki 3.65x10-6 M) [31]
cinacalcet Small molecule or natural product Approved drug Rn Positive 4.3 pKi 35
pKi 4.3 [35]
VU0424465 Small molecule or natural product Rn Positive 8.8 pEC50 81
pEC50 8.8 (EC50 1.5x10-9 M) [81]
VU0404251 Small molecule or natural product Rn Positive 8.1 pEC50 54
pEC50 8.1 (EC50 7.2x10-9 M) [54]
VU-29 Small molecule or natural product Rn Positive 8.1 pEC50 16
pEC50 8.1 (EC50 9x10-9 M) [16]
VU-1545 Small molecule or natural product Hs Positive 8.0 pEC50 22
pEC50 8.0 (EC50 9.6x10-9 M) [22]
VU0463841 Small molecule or natural product Rn Negative 7.9 pEC50 2
pEC50 7.9 (EC50 1.3x10-8 M) [2]
compound 41 [PMID: 23434029] Small molecule or natural product Hs Negative 7.9 pEC50 15
pEC50 7.9 (EC50 1.3x10-8 M) [15]
CDPPB Small molecule or natural product Hs Positive 7.6 – 8.0 pEC50 44,49
pEC50 7.6 – 8.0 [44,49]
VU0360172 Small molecule or natural product Rn Positive 7.8 pEC50 76
pEC50 7.8 (EC50 1.6x10-8 M) [76]
CDPPB Small molecule or natural product Rn Positive 7.7 pEC50 49
pEC50 7.7 [49]
LSN2463359 Small molecule or natural product Rn Positive 7.6 pEC50 31
pEC50 7.6 (EC50 2.4x10-8 M) [31]
LSN2463359 Small molecule or natural product Hs Positive 7.5 pEC50 31
pEC50 7.5 (EC50 3.3x10-8 M) [31]
VU0357121 Small molecule or natural product Rn Positive 7.5 pEC50 32
pEC50 7.5 (EC50 3.3x10-8 M) [32]
VU0092273 Small molecule or natural product Rn Positive 7.5 pEC50 64
pEC50 7.5 (EC50 3.5x10-8 M) [64]
VU0240382 Small molecule or natural product Rn Positive 7.4 pEC50 64
pEC50 7.4 (EC50 3.9x10-8 M) [64]
compound 47 [PMID: 21295468] Small molecule or natural product Hs Positive 7.3 pEC50 96
pEC50 7.3 (EC50 5.01x10-8 M) [96]
LSN2814617 Small molecule or natural product Hs Positive 7.3 pEC50 31
pEC50 7.3 (EC50 5.2x10-8 M) [31]
ADX-47273 Small molecule or natural product Rn Positive 7.3 pEC50 31
pEC50 7.3 (EC50 5.5x10-8 M) [31]
VU0404251 Small molecule or natural product Hs Positive 7.2 pEC50 54
pEC50 7.2 (EC50 7x10-8 M) [54]
LSN2814617 Small molecule or natural product Rn Positive 7.0 pEC50 31
pEC50 7.0 (EC50 9.3x10-8 M) [31]
VU0361747 Small molecule or natural product Rn Positive 6.9 pEC50 64
pEC50 6.9 (EC50 1.26x10-7 M) [64]
ADX-47273 Small molecule or natural product Hs Positive 6.8 pEC50 31
pEC50 6.8 (EC50 1.57x10-7 M) [31]
5PAM523 Small molecule or natural product Hs Positive 6.7 pEC50 68
pEC50 6.7 (EC50 2.01x10-7 M) [68]
5PAM523 Small molecule or natural product Rn Positive 6.5 pEC50 68
pEC50 6.5 (EC50 3.11x10-7 M) [68]
NCFP Small molecule or natural product Rn Positive 6.0 – 6.7 pEC50 63
pEC50 6.7 (EC50 2.14x10-7 M) EC50 with high mGlu5 expression [63]
pEC50 6.4 (EC50 3.7x10-7 M) EC50 with low mGlu5 expression [63]
pEC50 6.0 (EC50 9.69x10-7 M) EC50 from assay using rat astrocytes [63]
CPPZ Small molecule or natural product Hs Positive 6.3 pEC50 91
pEC50 6.3 (EC50 5x10-7 M) [91]
VU0364289 Small molecule or natural product Rn Positive 5.8 pEC50 107
pEC50 5.8 (EC50 1.6x10-6 M) [107]
SP203 Small molecule or natural product Rn Negative 10.4 pIC50 87
pIC50 10.4 (IC50 3.6x10-11 M) [87]
compound 18 [PMID: 17723296] Small molecule or natural product Rn Negative 9.1 pIC50 101
pIC50 9.1 (IC50 7.2x10-10 M) [101]
compound 23 [PMID: 17590335] Small molecule or natural product Rn Negative 9.1 pIC50 57
pIC50 9.1 (IC50 8x10-10 M) [57]
MTEB Small molecule or natural product Hs Negative 8.7 pIC50 99
pIC50 8.7 [99]
GRN-529 Small molecule or natural product Hs Negative 8.6 pIC50 38
pIC50 8.6 (IC50 2.6x10-9 M) [38]
compound 8 [PMID: 15482908] Small molecule or natural product Hs Negative 8.4 pIC50 89
pIC50 8.4 (IC50 3.9x10-9 M) [89]
[3H]M-MPEP Small molecule or natural product Ligand is labelled Ligand is radioactive Ligand has a PDB structure Hs Negative 8.3 – 8.4 pIC50 29,65
pIC50 8.4 [29]
pIC50 8.3 [65]
compound 10 [PMID: 15482906] Small molecule or natural product Hs Negative 8.2 pIC50 36
pIC50 8.2 (IC50 6.7x10-9 M) [36]
AZD9272 Small molecule or natural product Hs Negative 8.1 pIC50 75
pIC50 8.1 (IC50 7.6x10-9 M) [75]
alloswitch-1 Small molecule or natural product Primary target of this compound Rn Negative 8.1 pIC50 73
pIC50 8.1 (IC50 8.6x10-9 M) [73]
Description: Inhibition of agonist-induced IP accumulation.
CTEP Small molecule or natural product Hs Negative 7.9 – 8.2 pIC50 47
pIC50 7.9 – 8.2 (IC50 1.14x10-8 – 6.4x10-9 M) [47]
compound 30 [PMID: 21757343] Small molecule or natural product Rn Negative 7.9 pIC50 100
pIC50 7.9 (IC50 1.2x10-8 M) [100]
VU0463841 Small molecule or natural product Rn Negative 7.9 pIC50 2
pIC50 7.9 (IC50 1.3x10-8 M) [2]
AZD6538 Small molecule or natural product Hs Negative 7.9 pIC50 75
pIC50 7.9 (IC50 1.34x10-8 M) [75]
compound 29b [PMID: 20809633] Small molecule or natural product Hs Negative 7.8 pIC50 12
pIC50 7.8 (IC50 1.6x10-8 M) [12]
compound 30 [PMID: 21757343] Small molecule or natural product Hs Negative 7.8 pIC50 100
pIC50 7.8 (IC50 1.7x10-8 M) [100]
compound 24 [PMID: 23374867] Small molecule or natural product Hs Negative 7.7 pIC50 33
pIC50 7.7 (IC50 1.9x10-8 M) [33]
[14C]MTEP Small molecule or natural product Ligand is labelled Ligand is radioactive Rn Negative 7.7 pIC50 3
pIC50 7.7 [3]
dipraglurant Small molecule or natural product Hs Negative 7.7 pIC50 15
pIC50 7.7 (IC50 2x10-8 M) [15]
compound 16a [PMID: 14697765] Small molecule or natural product Hs Negative 7.7 pIC50 99
pIC50 7.7 (IC50 2.2x10-8 M) [99]
compound 24d [PMID: 23357634] Small molecule or natural product Hs Negative 7.6 pIC50 106
pIC50 7.6 (IC50 2.3x10-8 M) [106]
VU0285683 Small molecule or natural product Rn Negative 7.6 pIC50 76
pIC50 7.6 (IC50 2.44x10-8 M) [76]
MPEP Small molecule or natural product Click here for species-specific activity table Hs Negative 7.4 – 7.7 pIC50 29-30
pIC50 7.4 – 7.7 [29-30]
compound 13 [PMID: 15686941] Small molecule or natural product Hs Negative 7.6 pIC50 6
pIC50 7.6 (IC50 2.8x10-8 M) [6]
methoxymethyl-MTEP Small molecule or natural product Rn Negative 7.5 pIC50 3
pIC50 7.5 (IC50 3x10-8 M) [3]
compound 16m [PMID: 19931453] Small molecule or natural product Hs Negative 7.5 pIC50 90
pIC50 7.5 (IC50 3.2x10-8 M) [90]
compound 11a [PMID: 14697765] Small molecule or natural product Hs Negative 7.4 pIC50 99
pIC50 7.4 (IC50 4.1x10-8 M) [99]
GSK2210875 Small molecule or natural product Hs Negative 7.4 pIC50 70
pIC50 7.4 (IC50 4x10-8 M) [70]