Target Information

Target General Information

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Target ID

T99347 (Former ID: TTDC00100)

Target Name

Metabotropic glutamate receptor 5 (mGluR5)

Synonyms

MGLUR5; GPRC1E

Gene Name

GRM5

Target Type

Clinical trial target

[1]

Disease

[+] 2 Target-related Diseases

Fragile X chromosome [ICD-11: LD55]

Parkinsonism [ICD-11: 8A00]

Function

G-protein coupled receptor for glutamate. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors. Signaling activates a phosphatidylinositol-calcium second messenger system and generates a calcium-activated chloride current. Plays an important role in the regulation of synaptic plasticity and the modulation of the neural network activity.

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BioChemical Class

GPCR glutamate

UniProt ID

GRM5_HUMAN

Sequence

MVLLLILSVLLLKEDVRGSAQSSERRVVAHMPGDIIIGALFSVHHQPTVDKVHERKCGAV
REQYGIQRVEAMLHTLERINSDPTLLPNITLGCEIRDSCWHSAVALEQSIEFIRDSLISS
EEEEGLVRCVDGSSSSFRSKKPIVGVIGPGSSSVAIQVQNLLQLFNIPQIAYSATSMDLS
DKTLFKYFMRVVPSDAQQARAMVDIVKRYNWTYVSAVHTEGNYGESGMEAFKDMSAKEGI
CIAHSYKIYSNAGEQSFDKLLKKLTSHLPKARVVACFCEGMTVRGLLMAMRRLGLAGEFL
LLGSDGWADRYDVTDGYQREAVGGITIKLQSPDVKWFDDYYLKLRPETNHRNPWFQEFWQ
HRFQCRLEGFPQENSKYNKTCNSSLTLKTHHVQDSKMGFVINAIYSMAYGLHNMQMSLCP
GYAGLCDAMKPIDGRKLLESLMKTNFTGVSGDTILFDENGDSPGRYEIMNFKEMGKDYFD
YINVGSWDNGELKMDDDEVWSKKSNIIRSVCSEPCEKGQIKVIRKGEVSCCWTCTPCKEN
EYVFDEYTCKACQLGSWPTDDLTGCDLIPVQYLRWGDPEPIAAVVFACLGLLATLFVTVV
FIIYRDTPVVKSSSRELCYIILAGICLGYLCTFCLIAKPKQIYCYLQRIGIGLSPAMSYS
ALVTKTNRIARILAGSKKKICTKKPRFMSACAQLVIAFILICIQLGIIVALFIMEPPDIM
HDYPSIREVYLICNTTNLGVVTPLGYNGLLILSCTFYAFKTRNVPANFNEAKYIAFTMYT
TCIIWLAFVPIYFGSNYKIITMCFSVSLSATVALGCMFVPKVYIILAKPERNVRSAFTTS
TVVRMHVGDGKSSSAASRSSSLVNLWKRRGSSGETLRYKDRRLAQHKSEIECFTPKGSMG
NGGRATMSSSNGKSVTWAQNEKSSRGQHLWQRLSIHINKKENPNQTAVIKPFPKSTESRG
LGAGAGAGGSAGGVGATGGAGCAGAGPGGPESPDAGPKALYDVAEAEEHFPAPARPRSPS
PISTLSHRAGSASRTDDDVPSLHSEPVARSSSSQGSLMEQISSVVTRFTANISELNSMML
STAAPSPGVGAPLCSSYLIPKEIQLPTTMTTFAEIQPLPAIEVTGGAQPAAGAQAAGDAA
RESPAAGPEAAAAKPDLEELVALTPPSPFRDSVDSGSTTPNSPVSESALCIPSSPKYDTL
IIRDYTQSSSSL

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3D Structure

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AlphaFold

HIT2.0 ID

T64P00

Drugs and Modes of Action

Top

Clinical Trial Drug(s)

[+] 9 Clinical Trial Drugs

ADX-48621

Drug Info

Phase 2/3

Parkinson disease

[2]

AFQ056

Drug Info

Phase 2/3

Fragile X syndrome

[3], [4]

ADX10059

Drug Info

Phase 2

Anxiety disorder

[5]

RG-7090

Drug Info

Phase 2

Fragile X syndrome

[6]

STX-107

Drug Info

Phase 2

Autism spectrum disorder

[7], [8]

McN3377

Drug Info

Phase 1/2

Fragile X syndrome

[9], [10]

MK-3328

Drug Info

Phase 1

Alzheimer disease

[11]

RG7342

Drug Info

Phase 1

Schizophrenia

[12]

[3H]fenobam

Drug Info

Phase 1

Allodynia

[13]

Patented Agent(s)

[+] 5 Patented Agents

Diazepinone derivative 1

Drug Info

Patented

Reflux disease

[14]

Diazepinone derivative 2

Drug Info

Patented

Reflux disease

[14]

Diazepinone derivative 3

Drug Info

Patented

Reflux disease

[14]

Diazepinone derivative 4

Drug Info

Patented

Reflux disease

[14]

Diazepinone derivative 5

Drug Info

Patented

Reflux disease

[14]

Discontinued Drug(s)

[+] 4 Discontinued Drugs

AZD2066

Drug Info

Discontinued in Phase 2

Chronic neuropathic pain

[15]

AZD2516

Drug Info

Discontinued in Phase 2

Chronic neuropathic pain

[16]

LY467711

Drug Info

Terminated

Migraine

[17]

LY525327

Drug Info

Terminated

Migraine

[17]

Mode of Action

[+] 5 Modes of Action

Modulator

[+] 65 Modulator drugs

ADX-48621

Drug Info

[18]

AFQ056

Drug Info

[1]

ADX10059

Drug Info

[19], [20]

McN3377

Drug Info

[24]

MK-3328

Drug Info

[25]

6-aryl-imidazopyridine and 6-aryl-triazolopyridine carboxamide analog 1

Drug Info

[14]

6-aryl-imidazopyridine and 6-aryl-triazolopyridine carboxamide analog 2

Drug Info

[14]

6-aryl-imidazopyridine and 6-aryl-triazolopyridine carboxamide analog 3

Drug Info

[14]

Bicarboxylic and tricarboxylic ethynyl derivative 1

Drug Info

[14]

Bicarboxylic and tricarboxylic ethynyl derivative 2

Drug Info

[14]

Bicarboxylic and tricarboxylic ethynyl derivative 3

Drug Info

[14]

Bicyclic heteroaryl carboxamide analog 1

Drug Info

[14]

Bicyclic heteroaryl carboxamide analog 2

Drug Info

[14]

Bicyclic heteroaryl carboxamide analog 3

Drug Info

[14]

Diazepinone derivative 1

Drug Info

[14]

Diazepinone derivative 2

Drug Info

[14]

Diazepinone derivative 3

Drug Info

[14]

Diazepinone derivative 4

Drug Info

[14]

Diazepinone derivative 5

Drug Info

[14]

Ethynyl compound 1

Drug Info

[14]

Ethynyl compound 2

Drug Info

[14]

Ethynyl compound 3

Drug Info

[14]

Ethynyl compound 4

Drug Info

[14]

Ethynyl compound 5

Drug Info

[14]

Ethynyl compound 6

Drug Info

[14]

Ethynyl compound 7

Drug Info

[14]

Heterocyclic derivative 1

Drug Info

[14]

Heterocyclic derivative 2

Drug Info

[14]

Heterocyclic derivative 3

Drug Info

[14]

Imidazopyridine and triazolopyridine compound 1

Drug Info

[14]

Imidazopyridine and triazolopyridine compound 2

Drug Info

[14]

Imidazopyridine and triazolopyridine compound 3

Drug Info

[14]

Imidazopyridine and triazolopyridine compound 4

Drug Info

[14]

Imidazo[1,2-a]pyridine derivative 1

Drug Info

[14]

N-alkylamide derivative 1

Drug Info

[14]

N-alkylamide derivative 2

Drug Info

[14]

PMID28067079-Compound-95

Drug Info

[14]

PMID28067079-Compound-97

Drug Info

[14]

PMID28067079-Compound-98

Drug Info

[14]

Pyrazolopyrimidine derivative 1

Drug Info

[14]

Pyrazolopyrimidine derivative 2

Drug Info

[14]

Pyrazolopyrimidine derivative 3

Drug Info

[14]

Pyrazolopyrimidine derivative 4

Drug Info

[14]

Pyrazolopyrimidine derivative 5

Drug Info

[14]

Pyrazolopyrimidine derivative 6

Drug Info

[14]

Pyridine derivative 12

Drug Info

[14]

Pyridine derivative 13

Drug Info

[14]

Pyridine derivative 14

Drug Info

[14]

Pyridine derivative 15

Drug Info

[14]

Pyridine derivative 16

Drug Info

[14]

Pyridine derivative 17

Drug Info

[14]

Tetra-hydro-oxazolopyridine derivative 1

Drug Info

[14]

Tetra-hydro-oxazolopyridine derivative 2

Drug Info

[14]

Tetra-hydro-oxazolopyridine derivative 3

Drug Info

[14]

Tetra-hydro-oxazolopyridine derivative 4

Drug Info

[14]

Tetra-hydro-oxazolopyridine derivative 5

Drug Info

[14]

Tetra-hydro-oxazolopyridine derivative 6

Drug Info

[14]

Tetra-hydro-pyrazolopyrazine derivative 1

Drug Info

[14]

Tetra-hydro-pyrazolopyrazine derivative 2

Drug Info

[14]

Tetra-hydro-pyrazolopyrazine derivative 3

Drug Info

[14]

Tetra-hydro-pyrazolopyrazine derivative 4

Drug Info

[14]

Tetra-hydro-pyrazolopyrazine derivative 5

Drug Info

[14]

ADX-63365

Drug Info

[25]

GRN-529

Drug Info

[25]

LY-3390334

Drug Info

[68]

Antagonist

[+] 17 Antagonist drugs

RG-7090

Drug Info

[21]

STX-107

Drug Info

[22], [23]

2-(substituted ethynyl)quinoline derivative 1

Drug Info

[14]

2-(substituted ethynyl)quinoline derivative 2

Drug Info

[14]

2-(substituted ethynyl)quinoline derivative 3

Drug Info

[14]

2-(substituted ethynyl)quinoline derivative 4

Drug Info

[14]

AZD2066

Drug Info

[28]

AZD2516

Drug Info

[28]

LY467711

Drug Info

[24]

LY525327

Drug Info

[24]

(+)-MCPG

Drug Info

[29]

(S)-4C3HPG

Drug Info

[29]

(S)-4CPG

Drug Info

[29]

ACDPP

Drug Info

[62]

CTEP

Drug Info

[25], [66]

GSK-2210875

Drug Info

[25]

RTI-4229-982

Drug Info

[25]

Agonist

[+] 8 Agonist drugs

RG7342

Drug Info

[26]

(1S,3R)-ACPD

Drug Info

[29]

(S)-(+)-CBPG

Drug Info

[34]

(S)-3HPG

Drug Info

[29]

3,5-DHPG

Drug Info

[29]

CHPG

Drug Info

[29]

ibotenate

Drug Info

[29]

L-CCG-I

Drug Info

[29]

Modulator (allosteric modulator)

[+] 51 Modulator (allosteric modulator) drugs

[3H]fenobam

Drug Info

[27]

3,3'-difluorobenzaldazine

Drug Info

[49]

5-MPEP

Drug Info

[59]

5PAM523

Drug Info

[60]

alloswitch-1

Drug Info

[63]

BOMA

Drug Info

[57]

Br-5MPEPy

Drug Info

[59]

CPPHA

Drug Info

[64]

CPPZ

Drug Info

[65]

LSN2463359

Drug Info

[67]

LSN2814617

Drug Info

[67]

M-5MPEP

Drug Info

[59]

NCFP

Drug Info

[71]

PMID14697765C11a

Drug Info

[57]

PMID14697765C16a

Drug Info

[57]

PMID15482906C10

Drug Info

[72]

PMID15482908C8

Drug Info

[73]

PMID15686941C13

Drug Info

[62]

PMID16439120C20

Drug Info

[39]

PMID16439120C26

Drug Info

[39]

PMID17189691C42

Drug Info

[74]

PMID17723296C18

Drug Info

[37]

PMID17936624C36

Drug Info

[36]

PMID19931453C16m

Drug Info

[61]

PMID20598884C8

Drug Info

[54]

PMID20809633C29b

Drug Info

[75]

PMID21295468C47

Drug Info

[76]

PMID21757343C30

Drug Info

[77]

PMID21927650C18

Drug Info

[78]

PMID23357634C24d

Drug Info

[79]

PMID23374867C24

Drug Info

[80]

PMID23434029C41

Drug Info

[81]

PMID23434029C53

Drug Info

[81]

PTeB

Drug Info

[50]

SP203

Drug Info

[82]

VU-1545

Drug Info

[56]

VU0092273

Drug Info

[83]

VU0240382

Drug Info

[83]

VU0285683

Drug Info

[84]

VU0357121

Drug Info

[85]

VU0360172

Drug Info

[84]

VU0361747

Drug Info

[83]

VU0364289

Drug Info

[86]

VU0366058

Drug Info

[87]

VU0404251

Drug Info

[88]

VU0424465

Drug Info

[89]

VU0463841

Drug Info

[90]

[14C]MTEP

Drug Info

[91]

[3H]methoxy-PEPy

Drug Info

[92]

[3H]methoxymethyl-MTEP

Drug Info

[91], [92]

[3H]resolvin E1

Drug Info

[30]

Inhibitor

[+] 197 Inhibitor drugs

(3-(2-methylquinolin-7-yl)phenyl)methanol

Drug Info

[30]

(3-Ethoxy-pyridin-2-yl)-pyridin-2-yl-amine

Drug Info

[31]

(E)-1-Adamantan-1-yl-3-quinolin-3-yl-propenone

Drug Info

[32]

(E)-3-[2-(2-methyl-4-thiazolyl)vinyl]pyridine

Drug Info

[33]

1-(3-(2-methylquinolin-7-yl)phenyl)ethanone

Drug Info

[30]

2-(2-Methyl-thiazol-4-ylethynyl)-pyridine

Drug Info

[35]

2-(2-methylquinolin-7-yl)benzonitrile

Drug Info

[30]

2-(3,4-dimethylphenyl)-1,8-naphthyridine

Drug Info

[36]

2-(3,5-dichlorophenyl)pyrido[2,3-d]pyrimidine

Drug Info

[37]

2-(3,5-difluorophenyl)-7-methyl-1,8-naphthyridine

Drug Info

[36]

2-(3,5-dimethoxyphenyl)-1,8-naphthyridine

Drug Info

[36]

2-(3-(2-methylquinolin-7-yl)phenyl)acetonitrile

Drug Info

[30]

2-(3-(3-methoxyphenoxy)prop-1-ynyl)pyridine

Drug Info

[38]

2-(3-(benzyloxy)phenyl)isoindoline-1,3-dione

Drug Info

[39]

2-(3-bromophenyl)-7-methyl-1,8-naphthyridine

Drug Info

[36]

2-(3-bromophenyl)-7-methylpyrido[2,3-d]pyrimidine

Drug Info

[37]

2-(3-bromophenyl)pyrido[2,3-d]pyrimidine

Drug Info

[37]

2-(3-chlorobenzyloxy)-6-chloroisonicotinonitrile

Drug Info

[39]

2-(3-chlorophenyl)-7-methyl-1,8-naphthyridine

Drug Info

[36]

2-(4-(3-chlorophenyl)but-1-ynyl)-6-methylpyridine

Drug Info

[40]

2-(m-tolylethynyl)pyrimidine

Drug Info

[41]

2-(phenylethynyl)pyrimidine

Drug Info

[41]

2-(pyridin-2-yl)-4-(m-tolylthio)pyrimidine

Drug Info

[42]

2-Benzoxy-5-(2-methylquinolin-7-yl)benzonitrile

Drug Info

[23]

2-benzyloxy-7,8-dihydro-6H-quinolin-5-one

Drug Info

[43]

2-bromo-4-(3-fluorophenylethynyl)thiazole

Drug Info

[33]

2-Chloro-5-(2-methylquinolin-7-yl)nicotinonitrile

Drug Info

[23]

2-chloro-N-(3-(3-chlorobenzamido)phenyl)benzamide

Drug Info

[44]

2-Cyclohex-1-enylethynyl-pyridine

Drug Info

[45]

2-Cyclohexylethynyl-pyridine

Drug Info

[45]

2-Cyclopent-1-enylethynyl-pyridine

Drug Info

[45]

2-ethoxy-5-(m-tolylethynyl)pyrimidine

Drug Info

[41]

2-ethynyl-4-(3-fluorophenylethynyl)thiazole

Drug Info

[33]

2-m-tolyl-1,8-naphthyridine

Drug Info

[36]

2-methyl-4-(2-thienylethynyl)thiazole

Drug Info

[33]

2-methyl-4-(3-thienylethynyl)thiazole

Drug Info

[33]

2-methyl-4-(m-tolylethynyl)thiazole

Drug Info

[33]

2-Methyl-4-o-tolylethynyl-thiazole

Drug Info

[35]

2-Methyl-4-p-tolylethynyl-thiazole

Drug Info

[35]

2-Methyl-4-phenylethynyl-thiazole

Drug Info

[35]

2-methyl-6-(3-(p-tolyloxy)prop-1-ynyl)pyridine

Drug Info

[38]

2-methyl-6-(3-(phenylthio)prop-1-ynyl)pyridine

Drug Info

[40]

2-methyl-6-(4-phenylbut-1-ynyl)pyridine

Drug Info

[40]

2-methyl-6-(4-phenylpent-1-ynyl)pyridine

Drug Info

[40]

2-methyl-6-(5-phenylpent-1-ynyl)pyridine

Drug Info

[40]

2-methyl-6-(phenylethynyl)pyridine

Drug Info

[46], [47]

2-methyl-7-(pyridin-3-yl)quinoline

Drug Info

[30]

2-methyl-7-m-tolyl-1,6-naphthyridine

Drug Info

[36]

2-methyl-7-m-tolyl-1,8-naphthyridine

Drug Info

[36]

2-methyl-7-m-tolylquinoline

Drug Info

[30]

2-methyl-7-phenyl-1,8-naphthyridine

Drug Info

[36]

2-methyl-7-phenylquinoline

Drug Info

[30]

2-phenyl-1,8-naphthyridine

Drug Info

[36]

2-Phenyl-5-(2-methylthiazol-4ylethynyl)pyridine

Drug Info

[48]

2-phenylethynyl-5,6,7,8-tetrahydro-quinolin-5-ol

Drug Info

[43]

2-phenylethynyl-5,6,7,8-tetrahydro-quinoline

Drug Info

[43]

2-phenylethynyl-7,8-dihydro-6H-quinolin-5-one

Drug Info

[43]

2-[(2-methyl-4-thiazolyl)ethynyl]pyrazine

Drug Info

[33]

3-(1,5-naphthyridin-3-yl)benzonitrile

Drug Info

[36]

3-(1,8-naphthyridin-2-yl)benzonitrile

Drug Info

[36]

3-(1-Pyridin-2-yl-1H-pyrazol-3-yl)-benzonitrile

Drug Info

[50]

3-(1-Pyridin-2-yl-1H-pyrazol-4-yl)-benzonitrile

Drug Info

[50]

3-(1-Pyridin-2-yl-1H-pyrrol-3-yl)-benzonitrile

Drug Info

[50]

3-(2-methylbenzo[d]thiazol-5-yl)benzonitrile

Drug Info

[51]

3-(2-methylquinolin-7-yl)benzonitrile

Drug Info

[30]

3-(2-methylquinolin-7-yl)phenol

Drug Info

[30]

3-(2-Pyridin-2-yl-2H-tetrazol-5-yl)-benzonitrile

Drug Info

[50]

3-(3,4-dimethylphenyl)-1,5-naphthyridine

Drug Info

[36]

3-(3-(3-chlorobenzyloxy)-5-methylphenyl)pyridine

Drug Info

[39]

3-(3-bromophenylethynyl)-5-methyl[1,2,4]triazine

Drug Info

[52]

3-(3-methylphenylethynyl)-5-methyl[1,2,4]triazine

Drug Info

[52]

3-(3-Pyridin-2-yl-pyrazol-1-yl)-benzonitrile

Drug Info

[50]

3-(3-Pyridin-2-yl-pyrrol-1-yl)-benzonitrile

Drug Info

[50]

3-(4-Pyridin-2-yl-imidazol-1-yl)-benzonitrile

Drug Info

[50]

3-(4-Pyridin-2-yl-pyrazol-1-yl)-benzonitrile

Drug Info

[50]

3-(5-Pyridin-2-yl-tetrazol-2-yl)-benzonitrile

Drug Info

[50]

3-(6-fluoroquinazolin-4-ylamino)benzonitrile

Drug Info

[47]

3-(7-methyl-1,8-naphthyridin-2-yl)benzonitrile

Drug Info

[36]

3-biphenyl-4-ylethynyl-5-methyl-[1,2,4]triazine

Drug Info

[52]

3-bromo-5-(2-methylquinolin-7-yl)benzonitrile

Drug Info

[30]

3-bromo-5-[(2-methyl-4-thiazolyl)ethynyl]pyridine

Drug Info

[33]

3-bromo-N-(6-methylpyridin-2-yl)benzamide

Drug Info

[53]

3-chloro-5-(2-methylquinolin-7-yl)benzonitrile

Drug Info

[30]

3-chloro-N-(3-isobutyramidophenyl)benzamide

Drug Info

[44]

3-chloro-N-(4-methylthiazol-2-yl)benzamide

Drug Info

[53]

3-chloro-N-(6-chloropyridin-2-yl)benzamide

Drug Info

[53]

3-chloro-N-(6-methylpyridin-2-yl)benzamide

Drug Info

[48]

3-cyano-5-fluoro-N-(3-fluorophenyl)benzamide

Drug Info

[54]

3-cyano-5-fluoro-N-(pyridin-2-yl)benzamide

Drug Info

[54]

3-cyano-5-fluoro-N-m-tolylbenzamide

Drug Info

[54]

3-cyano-5-fluoro-N-phenylbenzamide

Drug Info

[54]

3-cyano-N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide

Drug Info

[55], [56]

3-cyano-N-(1,4-diphenyl-1H-pyrazol-5-yl)benzamide

Drug Info

[56]

3-cyano-N-(3-cyanophenyl)-5-fluorobenzamide

Drug Info

[54]

3-cyano-N-(3-ethylphenyl)-5-fluorobenzamide

Drug Info

[54]

3-cyano-N-(3-ethynylphenyl)-5-fluorobenzamide

Drug Info

[54]

3-cyano-N-(6-ethylpyridin-2-yl)-5-fluorobenzamide

Drug Info

[54]

3-cyano-N-(6-methylpyridin-2-yl)benzamide

Drug Info

[48]

3-ethoxy-5-(2-methylquinolin-7-yl)benzonitrile

Drug Info

[30]

100

3-fluoro-5-(1,6-naphthyridin-7-yl)benzonitrile

Drug Info

[36]

101

3-fluoro-5-(2-methylquinolin-7-yl)benzonitrile

Drug Info

[30]

102

3-hydroxy-5-(2-methylquinolin-7-yl)benzonitrile

Drug Info

[30]

103

3-iodo-N-(6-methylpyridin-2-yl)benzamide

Drug Info

[53]

104

3-isobutoxy-5-(2-methylquinolin-7-yl)benzonitrile

Drug Info

[30]

105

3-m-tolyl-1,5-naphthyridine

Drug Info

[36]

106

3-methoxy-5-(1,5-naphthyridin-3-yl)benzonitrile

Drug Info

[36]

107

3-methoxy-5-(1,6-naphthyridin-7-yl)benzonitrile

Drug Info

[36]

108

3-methoxy-5-(2-methylquinolin-7-yl)benzonitrile

Drug Info

[30]

109

3-methoxy-N-(4-methylthiazol-2-yl)benzamide

Drug Info

[53]

110

3-methoxy-N-(6-methylpyridin-2-yl)benzamide

Drug Info

[53]

111

3-methyl-5-(2-methylquinolin-7-yl)benzonitrile

Drug Info

[30]

112

3-methyl-N-(6-methylpyridin-2-yl)benzamide

Drug Info

[53]

113

3-nitro-N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide

Drug Info

[56]

114

3-Phenyl-1-(2-methylthiazol-4-ylethynyl)benzene

Drug Info

[48]

115

3-[(2,5-dimethyl-4-thiazolyl)ethynyl]pyridine

Drug Info

[33]

116

3-[(2-methyl-4-thiazolyl)ethynyl]-5-vinylpyridine

Drug Info

[33]

117

3-[(2-methyl-4-thiazolyl)ethynyl]benzamide

Drug Info

[33]

118

3-[(2-methyl-4-thiazolyl)ethynyl]benzonitrile

Drug Info

[33], [57]

119

3-[(2-methyl-4-thiazolyl)ethynyl]phenol

Drug Info

[33]

120

3-[(5-ethyl-2-methyl-4-thiazolyl)ethynyl]pyridine

Drug Info

[33]

121

3-[(6-Methylpyridin-2-yl)ethynyl]benzonitrile

Drug Info

[48]

122

4-(2-(3-fluorophenyl)ethynyl)-2-methylthiazole

Drug Info

[33]

123

4-(2-(4-fluorophenyl)ethynyl)-2-methylthiazole

Drug Info

[33]

124

4-(2-fluorophenylethynyl)-2-methylthiazole

Drug Info

[33]

125

4-(2-methoxyphenylethynyl)-2-methylthiazole

Drug Info

[33]

126

4-(2-Methyl-thiazol-4-ylethynyl)-pyridine

Drug Info

[35]

127

4-(3,5-difluorophenylethynyl)-2-methylthiazole

Drug Info

[33]

128

4-(3-bromophenoxy)-6-chloroquinazoline

Drug Info

[47]

129

4-(3-bromophenylthio)-2-(pyridin-2-yl)pyrimidine

Drug Info

[42]

130

4-(3-chlorophenylethynyl)-2-methylthiazole

Drug Info

[33]

131

4-(3-chlorophenylthio)-2-(pyridin-2-yl)pyrimidine

Drug Info

[42]

132

4-(3-fluorophenylethynyl)-2-thiazolylamine

Drug Info

[33]

133

4-(3-methoxyphenylethynyl)-2-methylthiazole

Drug Info

[33]

134

4-(3-pyridylethynyl)-2-thiazolylamine

Drug Info

[33]

135

4-(4-chlorophenylthio)-2-(pyridin-2-yl)pyrimidine

Drug Info

[42]

136

4-Biphenyl-2-ylethynyl-2-methyl-thiazole

Drug Info

[35]

137

4-Biphenyl-4-ylethynyl-2-methyl-thiazole

Drug Info

[35]

138

4-cyano-N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide

Drug Info

[56]

139

5-((6-Methylpyridin-2-yl)ethynyl)nicotinonitrile

Drug Info

[23]

140

5-(2-(2,5-dimethylphenyl)ethynyl)pyrimidine

Drug Info

[58]

141

5-(2-(3,5-difluorophenyl)ethynyl)pyrimidine

Drug Info

[58]

142

5-(2-(3-chlorophenyl)ethynyl)pyrimidine

Drug Info

[58]

143

5-(2-(4-fluoro-3-methylphenyl)ethynyl)pyrimidine

Drug Info

[58]

144

5-(2-m-tolylethynyl)pyrimidine

Drug Info

[58]

145

5-(2-Methylquinolin-7-yl)-2-phenylbenzonitrile

Drug Info

[23]

146

5-(2-Methylquinolin-7-yl)-2-phenylnicotinonitrile

Drug Info

[23]

147

5-(2-methylquinolin-7-yl)isophthalonitrile

Drug Info

[30]

148

5-(2-methylquinolin-7-yl)nicotinonitrile

Drug Info

[30]

149

5-(3-chlorophenylethynyl)-5-methyl[1,2,4]triazine

Drug Info

[52]

150

5-(phenylethynyl)pyrimidine

Drug Info

[58]

151

5-Biphenyl-4-ylethynyl-pyrimidine

Drug Info

[58]

152

5-Chloro-2-(2-methylquinolin-7-yl)benzonitrile

Drug Info

[23]

153

5-methyl-3-phenylethynyl[1,2,4]triazine

Drug Info

[52]

154

5-[(2-methyl-4-thiazolyl)ethynyl]pyrimidine

Drug Info

[33]

155

6-(4-chlorophenylamino)-N,N-diethylnicotinamide

Drug Info

[61]

156

6-bromo-N-(3-bromophenyl)quinazolin-4-amine

Drug Info

[47]

157

6-bromo-N-(3-chlorophenyl)quinazolin-4-amine

Drug Info

[47]

158

6-bromo-N-(3-fluorophenyl)quinazolin-4-amine

Drug Info

[47]

159

6-bromo-N-m-tolylquinazolin-4-amine

Drug Info

[47]

160

6-chloro-N-(3-chlorophenyl)quinazolin-4-amine

Drug Info

[47]

161

6-fluoro-N-m-tolylquinazolin-4-amine

Drug Info

[47]

162

6-phenylethynyl-nicotinic acid methyl ester

Drug Info

[43]

163

7-(2-methoxyphenyl)-2-methylquinoline

Drug Info

[30]

164

7-(3,5-dimethoxyphenyl)-1,6-naphthyridine

Drug Info

[36]

165

7-(3-(methoxymethyl)phenyl)-2-methylquinoline

Drug Info

[30]

166

7-(3-chlorophenyl)-2-methylquinoline

Drug Info

[30]

167

7-(3-fluoro-5-methylphenyl)-1,6-naphthyridine

Drug Info

[36]

168

7-(3-fluorophenyl)-2-methylquinoline

Drug Info

[30]

169

7-(3-methoxyphenyl)-2-methyl-1,6-naphthyridine

Drug Info

[36]

170

7-(3-methoxyphenyl)-2-methylquinoline

Drug Info

[30]

171

7-(4,6-dimethoxypyrimidin-2-yl)-2-methylquinoline

Drug Info

[51]

172

7-(4,6-dimethylpyrimidin-2-yl)-2-methylquinoline

Drug Info

[51]

173

7-(4-methoxyphenyl)-2-methylquinoline

Drug Info

[30]

174

7-(4-methoxypyrimidin-2-yl)-2-methylquinoline

Drug Info

[51]

175

7-bromo-N-(3-bromophenyl)isoquinolin-1-amine

Drug Info

[47]

176

7-m-tolyl-1,6-naphthyridine

Drug Info

[36]

177

7-methyl-2-m-tolylpyrido[2,3-d]pyrimidine

Drug Info

[37]

178

7-methyl-2-phenylpyrido[2,3-d]pyrimidine

Drug Info

[37]

179

N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide

Drug Info

[56]

180

N-(1,4-diphenyl-1H-pyrazol-5-yl)benzamide

Drug Info

[56]

181

N-(2-phenylimidazo[1,2-a]pyridin-3-yl)benzamide

Drug Info

[56]

182

N-(3-(3-cyanobenzamido)phenyl)-2-methoxybenzamide

Drug Info

[44]

183

N-(3-acetamidophenyl)-3-chlorobenzamide

Drug Info

[44]

184

N-(3-bromophenyl)-6-chloroquinazolin-4-amine

Drug Info

[47]

185

N-(3-bromophenyl)-6-fluoroquinazolin-4-amine

Drug Info

[47]

186

N-(3-chlorophenyl)-3-cyano-5-fluorobenzamide

Drug Info

[54]

187

N-(3-chlorophenyl)-6-fluoroquinazolin-4-amine

Drug Info

[47]

188

N-(3-chlorophenyl)-6-methoxyquinazolin-4-amine

Drug Info

[47]

189

N-(3-chlorophenyl)-6-nitroquinazolin-4-amine

Drug Info

[47]

190

N-(6-methylpyridin-2-yl)-5-phenylpicolinamide

Drug Info

[69]

191

N-(6-methylpyridin-2-yl)-6-phenylnicotinamide

Drug Info

[48]

192

N-(6-methylpyridin-2-yl)biphenyl-3-carboxamide

Drug Info

[48]

193

N-cyclopentyl-6-(2-phenylethynyl)nicotinamide

Drug Info

[70]

194

N-[4-(3-pyridylethynyl)-2-thiazolyl]acetamide

Drug Info

[33]

195

SIB-1757

Drug Info

[53]

196

SIB-1893

Drug Info

[53]

197

[3H]quisqualate

Drug Info

[93]

Chemical Structure based Activity Landscape of Target

Top

Drug Property Profile of Target

Top

(1) Molecular Weight (mw) based Drug Clustering

(2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering

(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering

(4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering

(5) Rotatable Bond Count (rotbonds) based Drug Clustering

(6) Topological Polar Surface Area (polararea) based Drug Clustering

"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five

Co-Targets

Top

Co-Targets

Co-Targets Info

Target Poor or Non Binders

Top

Target Poor or Non Binders

Target Poor or Non Binders Info

Target Profiles in Patients

Top

Target Expression
Profile (TEP)

Target Expression Profile Info

Target Affiliated Biological Pathways

Top

KEGG Pathway

[+] 7 KEGG Pathways

Calcium signaling pathway

Neuroactive ligand-receptor interaction

Gap junction

Long-term potentiation

Retrograde endocannabinoid signaling

Glutamatergic synapse

Huntington's disease

Panther Pathway

[+] 4 Panther Pathways

Heterotrimeric G-protein signaling pathway-Gq alpha and Go alpha mediated pathway

Metabotropic glutamate receptor group III pathway

Metabotropic glutamate receptor group I pathway

Endogenous cannabinoid signaling

Reactome

[+] 2 Reactome Pathways

G alpha (q) signalling events

Class C/3 (Metabotropic glutamate/pheromone receptors)

WikiPathways

[+] 5 WikiPathways

Hypothetical Network for Drug Addiction

GPCRs, Class C Metabotropic glutamate, pheromone

Gastrin-CREB signalling pathway via PKC and MAPK

GPCR ligand binding

GPCR downstream signaling

Target-Related Models and Studies

Top

Target Validation

Target Validation Info

References

Top

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REF 2

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REF 3

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Biochemical and electrophysiological studies on (S)-(+)-2-(3'-carboxybicyclo(1.1.1)pentyl)-glycine (CBPG), a novel mGlu5 receptor agonist endowed with mGlu1 receptor antagonist activity. Neuropharmacology. 1999 Jul;38(7):917-26.

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REF 36

Synthesis and SAR comparison of regioisomeric aryl naphthyridines as potent mGlu5 receptor antagonists. Bioorg Med Chem Lett. 2007 Dec 1;17(23):6525-8.

REF 37

Synthesis and SAR of 2-aryl pyrido[2,3-d]pyrimidines as potent mGlu5 receptor antagonists. Bioorg Med Chem Lett. 2007 Oct 1;17(19):5396-9.

REF 38

A new series of pyridinyl-alkynes as antagonists of the metabotropic glutamate receptor 5 (mGluR5). Bioorg Med Chem Lett. 2006 Sep 15;16(18):4792-5.

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Arylmethoxypyridines as novel, potent and orally active mGlu5 receptor antagonists. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1892-7.

REF 40

Structure-activity relationships for the linker in a series of pyridinyl-alkynes that are antagonists of the metabotropic glutamate receptor 5 (mGl... Bioorg Med Chem Lett. 2006 Sep 15;16(18):4788-91.

REF 41

Discovery of molecular switches that modulate modes of metabotropic glutamate receptor subtype 5 (mGlu5) pharmacology in vitro and in vivo within a... J Med Chem. 2009 Jul 23;52(14):4103-6.

REF 42

Structure-activity relationship of thiopyrimidines as mGluR5 antagonists. Bioorg Med Chem Lett. 2006 May 1;16(9):2467-9.

REF 43

Positive and negative modulation of group I metabotropic glutamate receptors. J Med Chem. 2008 Feb 14;51(3):634-47.

REF 44

Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS. Bioorg Med Chem Lett. 2009 Dec 1;19(23):6502-6.

REF 45

Cyclohexenyl- and dehydropiperidinyl-alkynyl pyridines as potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists. Bioorg Med Chem Lett. 2005 Oct 15;15(20):4589-93.

REF 46

2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a potent, selective and systemically active mGlu5 receptor antagonist. Neuropharmacology. 1999 Oct;38(10):1493-503.

REF 47

Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5. Bioorg Med Chem Lett. 2009 Dec 1;19(23):6623-6.

REF 48

Structure-activity relationships comparing N-(6-methylpyridin-yl)-substituted aryl amides to 2-methyl-6-(substituted-arylethynyl)pyridines or 2-met... J Med Chem. 2009 Jun 11;52(11):3563-75.

REF 49

A family of highly selective allosteric modulators of the metabotropic glutamate receptor subtype 5. Mol Pharmacol. 2003 Sep;64(3):731-40.

REF 50

Discovery of novel heteroarylazoles that are metabotropic glutamate subtype 5 receptor antagonists with anxiolytic activity. J Med Chem. 2004 Sep 9;47(19):4645-8. Letter

REF 51

Discovery of heterobicyclic templates for novel metabotropic glutamate receptor subtype 5 antagonists. Bioorg Med Chem Lett. 2007 Jun 1;17(11):2987-91.

REF 52

Synthesis and pharmacological evaluation of phenylethynyl[1,2,4]methyltriazines as analogues of 3-methyl-6-(phenylethynyl)pyridine. J Med Chem. 2007 Jul 12;50(14):3388-91.

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Design and synthesis of noncompetitive metabotropic glutamate receptor subtype 5 antagonists. Bioorg Med Chem Lett. 2006 Jul 1;16(13):3371-5.

REF 54

3-Cyano-5-fluoro-N-arylbenzamides as negative allosteric modulators of mGlu(5): Identification of easily prepared tool compounds with CNS exposure ... Bioorg Med Chem Lett. 2010 Aug 1;20(15):4390-4.

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Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H- pyrazol-5-yl)benzamides that potentiate receptor function in vivo. JMed Chem. 2004 Nov 18;47(24):5825-8.

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Substituent effects of N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides on positive allosteric modulation of the metabotropic glutamate-5 receptor in rat... J Med Chem. 2006 Jun 1;49(11):3332-44.

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A close structural analog of 2-methyl-6-(phenylethynyl)-pyridine acts as a neutral allosteric site ligand on metabotropic glutamate receptor subtyp... Mol Pharmacol. 2005 Dec;68(6):1793-802.

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Mechanism based neurotoxicity of mGlu5 positive allosteric modulators--development challenges for a promising novel antipsychotic target. Neuropharmacology. 2014 Jul;82:161-73.

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Piperidyl amides as novel, potent and orally active mGlu5 receptor antagonists with anxiolytic-like activity. Bioorg Med Chem Lett. 2010 Jan 1;20(1):184-8.

REF 62

Dipyridyl amides: potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists. Bioorg Med Chem Lett. 2005 Feb 15;15(4):1197-200.

REF 63

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A novel selective allosteric modulator potentiates the activity of native metabotropic glutamate receptor subtype 5 in rat forebrain. J Pharmacol Exp Ther. 2004 May;309(2):568-77.

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CTEP: a novel, potent, long-acting, and orally bioavailable metabotropic glutamate receptor 5 inhibitor. J Pharmacol Exp Ther. 2011 Nov;339(2):474-86.

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Discovery of highly potent, selective, orally bioavailable, metabotropic glutamate subtype 5 (mGlu5) receptor antagonists devoid of cytochrome P450 1A2 inhibitory activity. Bioorg Med Chem Lett. 2004Nov 15;14(22):5481-4.

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Discovery and structure-activity relationship of 1,3-cyclohexyl amide derivatives as novel mGluR5 negative allosteric modulators. Bioorg Med Chem Lett. 2013 Mar 1;23(5):1398-406.

REF 80

Discovery of (1R,2R)-N-(4-(6-isopropylpyridin-2-yl)-3-(2-methyl-2H-indazol-5-yl)isothiazol-5-yl)-2-methylcyclopropanecarboxamide, a potent and orally efficacious mGlu5 receptor negative allosteric modulator. Bioorg Med Chem Lett. 2013 Mar 1;23(5):1249-52.

REF 81

Discovery of biological evaluation of pyrazole/imidazole amides as mGlu5 receptor negative allosteric modulators. Bioorg Med Chem Lett. 2013 Apr 1;23(7):2134-9.

REF 82

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REF 84

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REF 85

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REF 86

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REF 87

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REF 90

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REF 91

[3H]Methoxymethyl-3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine binding to metabotropic glutamate receptor subtype 5 in rodent brain: in vitro and in vivo characterization. J Pharmacol Exp Ther. 2002 Dec;303(3):1044-51.

REF 92

[3H]-methoxymethyl-MTEP and [3H]-methoxy-PEPy: potent and selective radioligands for the metabotropic glutamate subtype 5 (mGlu5) receptor. Bioorg Med Chem Lett. 2003 Feb 10;13(3):351-4.

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