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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

Contents:

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-q14.3 GRM5 glutamate metabotropic receptor 5 60-61
Mouse 7 1203 7 D3 Grm5 glutamate receptor, metabotropic 5
Rat 7 1203 1q32 Grm5 glutamate metabotropic receptor 5 1,41
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
Alphafold P41594 (Hs), Q3UVX5 (Mm), P31424 (Rn)
ChEMBL Target CHEMBL3227 (Hs), CHEMBL1641352 (Mm), CHEMBL2564 (Rn)
DrugBank Target P41594 (Hs)
Ensembl Gene ENSG00000168959 (Hs), ENSMUSG00000049583 (Mm), ENSRNOG00000016429 (Rn)
Entrez Gene 2915 (Hs), 108071 (Mm), 24418 (Rn)
Human Protein Atlas ENSG00000168959 (Hs)
KEGG Gene hsa:2915 (Hs), mmu:108071 (Mm), rno:24418 (Rn)
OMIM 604102 (Hs)
Pharos P41594 (Hs)
RefSeq Nucleotide NM_000842 (Hs), NM_001143831 (Hs), NM_001081414 (Mm), NM_017012 (Rn)
RefSeq Protein NP_000833 (Hs), NP_001137303 (Hs), NP_001074883 (Mm), NP_058708 (Rn)
UniProtKB P41594 (Hs), Q3UVX5 (Mm), P31424 (Rn)
Wikipedia GRM5 (Hs)
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 82
⤷ pEC50 6.8 (EC50 1.71x10-7 M) [82]
VU0092273 Small molecule or natural product Rn Agonist 5.9 pEC50 65
⤷ pEC50 5.9 (EC50 1.3x10-6 M) [65]
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 72
⤷ pEC50 5.0 – 5.5 [72]
(S)-(+)-CBPG Small molecule or natural product Click here for species-specific activity table Rn Partial agonist 4.3 pEC50 56
⤷ pEC50 4.3 (EC50 4.7x10-5 M) [56]
quisqualate Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 7.5 pIC50 63
⤷ pIC50 7.5 [63]
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 63
⤷ pIC50 6.1 [63]
L-CCG-I Small molecule or natural product Click here for species-specific activity table Rn Full agonist 5.8 pIC50 63
⤷ pIC50 5.8 [63]
(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 63
⤷ pIC50 5.7 [63]
ibotenic acid Small molecule or natural product Click here for species-specific activity table Rn Full agonist 5.7 pIC50 63
⤷ pIC50 5.7 [63]
3,5-DHPG Small molecule or natural product Click here for species-specific activity table Rn Partial agonist 5.4 pIC50 63
⤷ pIC50 5.4 [63]
(S)-3HPG Small molecule or natural product Click here for species-specific activity table Rn Partial agonist 5.0 pIC50 63
⤷ pIC50 5.0 [63]
CHPG Small molecule or natural product Hs Full agonist 3.4 pIC50 63
⤷ pIC50 3.4 [63]
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 [85]. 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 38
⤷ pKi 5.6 (Ki 2.366x10-6 M) [38]
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 63
⤷ pIC50 5.6 [63]
LY341495 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 5.1 pIC50 44
⤷ pIC50 5.1 [44]
DCG-IV Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 4.7 pIC50 63
⤷ pIC50 4.7 [63]
(S)-4CPG Small molecule or natural product Click here for species-specific activity table Rn Antagonist 4.6 pIC50 63
⤷ pIC50 4.6 [63]
(+)-MCPG Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 3.7 pIC50 63
⤷ pIC50 3.7 [63]
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 [85]. 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 [85]). (S)-4C3HPG has been reported to have slight partial agonist activity at this receptor [41].
Allosteric Modulators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
VU0409551 Small molecule or natural product Hs Positive 7.1 pKB 83
⤷ pKB 7.1 [83]
VU0360172 Small molecule or natural product Hs Positive 6.6 – 7.0 pKB 32,77
⤷ pKB 6.6 – 7.0 [32,77]
VU0483605 Small molecule or natural product Rn Positive 6.5 pKB 36
⤷ pKB 6.5 [36]
GS39783 Small molecule or natural product Ligand has a PDB structure Rn Neutral 6.3 pKB 36
⤷ pKB 6.3 [36]
PHCCC Small molecule or natural product Click here for species-specific activity table Rn Neutral 5.6 pKB 36
⤷ pKB 5.6 [36]
AZ12216052 Small molecule or natural product Rn Positive 5.4 pKB 36
⤷ pKB 5.4 [36]
NPS 2143 Small molecule or natural product Ligand has a PDB structure Rn Positive 5.1 pKB 36
⤷ pKB 5.1 [36]
CPCCOEt Small molecule or natural product Click here for species-specific activity table Rn Neutral 4.9 pKB 36
⤷ pKB 4.9 [36]
CGP7930 Small molecule or natural product Click here for species-specific activity table Rn Positive 4.8 pKB 36
⤷ pKB 4.8 [36]
[3H]CTEP Small molecule or natural product Ligand is labelled Ligand is radioactive Rn Negative 8.8 pKd 48
⤷ pKd 8.8 (Kd 1.5x10-9 M) [48]
[3H]CTEP Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Negative 8.8 pKd 48
⤷ pKd 8.8 (Kd 1.7x10-9 M) [48]
[3H]CTEP Small molecule or natural product Ligand is labelled Ligand is radioactive Mm Negative 8.7 pKd 48
⤷ pKd 8.7 (Kd 1.8x10-9 M) [48]
[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 75
⤷ pKd 7.5 [75]
[3H]fenobam Small molecule or natural product Ligand is labelled Ligand is radioactive Ligand has a PDB structure Rn Negative 7.3 pKd 75
⤷ pKd 7.3 [75]
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 101
⤷ pKi 8.5 [101]
AZD9272 Small molecule or natural product Hs Negative 8.4 pKi 76
⤷ pKi 8.4 (Ki 3.8x10-9 M) [76]
GRN-529 Small molecule or natural product Rn Negative 8.3 pKi 39
⤷ pKi 8.3 (Ki 5.4x10-9 M) [39]
CTEP Small molecule or natural product Mm Negative 8.0 pKi 48
⤷ pKi 8.0 (Ki 9.5x10-9 M) [48]
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 102
⤷ pKi 7.9 (Ki 1.2x10-8 M) [102]
compound 10 [PMID: 15482906] Small molecule or natural product Hs Negative 7.9 pKi 37
⤷ pKi 7.9 (Ki 1.2x10-8 M) [37]
CTEP Small molecule or natural product Rn Negative 7.9 pKi 48
⤷ pKi 7.9 (Ki 1.26x10-8 M) [48]
compound 8 [PMID: 15482908] Small molecule or natural product Rn Negative 7.8 pKi 91
⤷ pKi 7.8 (Ki 1.4x10-8 M) [91]
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 77
⤷ pKi 7.8 (Ki 1.6x10-8 M) [77]
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 40,48
⤷ pKi 7.7 – 7.8 (Ki 2x10-8 – 1.64x10-8 M) [40,48]
compound 10 [PMID: 15482908] Small molecule or natural product Rn Negative 7.7 pKi 91
⤷ pKi 7.7 (Ki 1.9x10-8 M) [91]
compound 23 [PMID: 17590335] Small molecule or natural product Rn Negative 7.7 pKi 58
⤷ pKi 7.7 (Ki 2.2x10-8 M) [58]
AZD6538 Small molecule or natural product Hs Negative 7.6 pKi 76
⤷ pKi 7.6 (Ki 2.8x10-8 M) [76]
compound 24d [PMID: 23357634] Small molecule or natural product Rn Negative 7.5 pKi 108
⤷ pKi 7.5 (Ki 3x10-8 M) [108]
basimglurant Small molecule or natural product Hs Negative 7.4 pKi 40
⤷ pKi 7.4 (Ki 3.6x10-8 M) [40]
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 92
⤷ pKi 7.4 (Ki 3.8x10-8 M) [92]
VU0366058 Small molecule or natural product Rn Negative 7.1 pKi 62
⤷ pKi 7.1 (Ki 8.4x10-8 M) [62]
compound 16a [PMID: 14697765] Small molecule or natural product Rn Negative 7.0 pKi 101
⤷ pKi 7.0 (Ki 9.1x10-8 M) [101]
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 101
⤷ pKi 6.8 (Ki 1.59x10-7 M) [101]
VU0360172 Small molecule or natural product Rn Positive 6.7 pKi 77
⤷ pKi 6.7 (Ki 1.95x10-7 M) [77]
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 78
⤷ pKi 6.5 (Ki 3x10-7 M) [78]
Br-5MPEPy Small molecule or natural product Rn Negative 6.5 pKi 78
⤷ pKi 6.5 (Ki 3x10-7 M) [78]
LSN2463359 Small molecule or natural product Ligand has a PDB structure 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 78
⤷ pKi 6.4 [78]
compound 18 [PMID: 21927650] Small molecule or natural product Rn Negative 6.3 pKi 49
⤷ pKi 6.3 (Ki 4.77x10-7 M) [49]
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 69
⤷ pKi 5.7 (Ki 2x10-6 M) [69]
CPPZ Small molecule or natural product Rn Positive 5.5 pKi 93
⤷ pKi 5.5 (Ki 3.1x10-6 M) [93]
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 Ligand has a PDB structure Rn Positive 4.3 pKi 36
⤷ pKi 4.3 [36]
VU0424465 Small molecule or natural product Rn Positive 8.8 pEC50 82
⤷ pEC50 8.8 (EC50 1.5x10-9 M) [82]
VU0404251 Small molecule or natural product Rn Positive 8.1 pEC50 55
⤷ pEC50 8.1 (EC50 7.2x10-9 M) [55]
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 45,50
⤷ pEC50 7.6 – 8.0 [45,50]
VU0360172 Small molecule or natural product Rn Positive 7.8 pEC50 77
⤷ pEC50 7.8 (EC50 1.6x10-8 M) [77]
CDPPB Small molecule or natural product Rn Positive 7.7 pEC50 50
⤷ pEC50 7.7 [50]
LSN2463359 Small molecule or natural product Ligand has a PDB structure Rn Positive 7.6 pEC50 31
⤷ pEC50 7.6 (EC50 2.4x10-8 M) [31]
LSN2463359 Small molecule or natural product Ligand has a PDB structure 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 33
⤷ pEC50 7.5 (EC50 3.3x10-8 M) [33]
VU0092273 Small molecule or natural product Rn Positive 7.5 pEC50 65
⤷ pEC50 7.5 (EC50 3.5x10-8 M) [65]
VU0240382 Small molecule or natural product Rn Positive 7.4 pEC50 65
⤷ pEC50 7.4 (EC50 3.9x10-8 M) [65]
compound 47 [PMID: 21295468] Small molecule or natural product Hs Positive 7.3 pEC50 98
⤷ pEC50 7.3 (EC50 5.01x10-8 M) [98]
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 55
⤷ pEC50 7.2 (EC50 7x10-8 M) [55]
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 65
⤷ pEC50 6.9 (EC50 1.26x10-7 M) [65]
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 69
⤷ pEC50 6.7 (EC50 2.01x10-7 M) [69]
5PAM523 Small molecule or natural product Rn Positive 6.5 pEC50 69
⤷ pEC50 6.5 (EC50 3.11x10-7 M) [69]
NCFP Small molecule or natural product Rn Positive 6.0 – 6.7 pEC50 64
⤷ pEC50 6.7 (EC50 2.14x10-7 M) EC50 with high mGlu5 expression [64]
pEC50 6.4 (EC50 3.7x10-7 M) EC50 with low mGlu5 expression [64]
pEC50 6.0 (EC50 9.69x10-7 M) EC50 from assay using rat astrocytes [64]
CPPZ Small molecule or natural product Hs Positive 6.3 pEC50 93
⤷ pEC50 6.3 (EC50 5x10-7 M) [93]
VU0364289 Small molecule or natural product Rn Positive 5.8 pEC50 109
⤷ pEC50 5.8 (EC50 1.6x10-6 M) [109]
SP203 Small molecule or natural product Rn Negative 10.4 pIC50 89
⤷ pIC50 10.4 (IC50 3.6x10-11 M) [89]
compound 18 [PMID: 17723296] Small molecule or natural product Rn Negative 9.1 pIC50 103
⤷ pIC50 9.1 (IC50 7.2x10-10 M) [103]
compound 23 [PMID: 17590335] Small molecule or natural product Rn Negative 9.1 pIC50 58
⤷ pIC50 9.1 (IC50 8x10-10 M) [58]
MTEB Small molecule or natural product Hs Negative 8.7 pIC50 101
⤷ pIC50 8.7 [101]
GRN-529 Small molecule or natural product Hs Negative 8.6 pIC50 39
⤷ pIC50 8.6 (IC50 2.6x10-9 M) [39]
compound 8 [PMID: 15482908] Small molecule or natural product Hs Negative 8.4 pIC50 91
⤷ pIC50 8.4 (IC50 3.9x10-9 M) [91]
[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 29,66
⤷ pIC50 8.4 [29]
pIC50 8.3 [66]
compound 10 [PMID: 15482906] Small molecule or natural product Hs Negative 8.2 pIC50 37
⤷ pIC50 8.2 (IC50 6.7x10-9 M) [37]
AZD9272 Small molecule or natural product Hs Negative 8.1 pIC50 76
⤷ pIC50 8.1 (IC50 7.6x10-9 M) [76]
alloswitch-1 Small molecule or natural product Primary target of this compound Ligand has a PDB structure Rn Negative 8.1 pIC50 74
⤷ pIC50 8.1 (IC50 8.6x10-9 M) [74]
Description: Inhibition of agonist-induced IP accumulation.
CTEP Small molecule or natural product Hs Negative 7.9 – 8.2 pIC50 48
⤷ pIC50 7.9 – 8.2 (IC50 1.14x10-8 – 6.4x10-9 M) [48]
compound 30 [PMID: 21757343] Small molecule or natural product Rn Negative 7.9 pIC50 102
⤷ pIC50 7.9 (IC50 1.2x10-8 M) [102]
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 76
⤷ pIC50 7.9 (IC50 1.34x10-8 M) [76]
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 102
⤷ pIC50 7.8 (IC50 1.7x10-8 M) [102]
compound 24 [PMID: 23374867] Small molecule or natural product Hs Negative 7.7 pIC50 34
⤷ pIC50 7.7 (IC50 1.9x10-8 M) [34]
[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 101
⤷ pIC50 7.7 (IC50 2.2x10-8 M) [101]
compound 24d [PMID: 23357634] Small molecule or natural product Hs Negative 7.6 pIC50 108
⤷ pIC50 7.6 (IC50 2.3x10-8 M) [108]