Target Information
Target General Information | Top | |||||
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Target ID |
T99347
(Former ID: TTDC00100)
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Target Name |
Metabotropic glutamate receptor 5 (mGluR5)
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Synonyms |
MGLUR5; GPRC1E
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Gene Name |
GRM5
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Target Type |
Clinical trial target
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[1] | ||||
Disease | [+] 2 Target-related Diseases | + | ||||
1 | Fragile X chromosome [ICD-11: LD55] | |||||
2 | 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.
Click to Show/Hide
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BioChemical Class |
GPCR glutamate
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UniProt ID | ||||||
Sequence |
MVLLLILSVLLLKEDVRGSAQSSERRVVAHMPGDIIIGALFSVHHQPTVDKVHERKCGAV
REQYGIQRVEAMLHTLERINSDPTLLPNITLGCEIRDSCWHSAVALEQSIEFIRDSLISS EEEEGLVRCVDGSSSSFRSKKPIVGVIGPGSSSVAIQVQNLLQLFNIPQIAYSATSMDLS DKTLFKYFMRVVPSDAQQARAMVDIVKRYNWTYVSAVHTEGNYGESGMEAFKDMSAKEGI CIAHSYKIYSNAGEQSFDKLLKKLTSHLPKARVVACFCEGMTVRGLLMAMRRLGLAGEFL LLGSDGWADRYDVTDGYQREAVGGITIKLQSPDVKWFDDYYLKLRPETNHRNPWFQEFWQ HRFQCRLEGFPQENSKYNKTCNSSLTLKTHHVQDSKMGFVINAIYSMAYGLHNMQMSLCP GYAGLCDAMKPIDGRKLLESLMKTNFTGVSGDTILFDENGDSPGRYEIMNFKEMGKDYFD YINVGSWDNGELKMDDDEVWSKKSNIIRSVCSEPCEKGQIKVIRKGEVSCCWTCTPCKEN EYVFDEYTCKACQLGSWPTDDLTGCDLIPVQYLRWGDPEPIAAVVFACLGLLATLFVTVV FIIYRDTPVVKSSSRELCYIILAGICLGYLCTFCLIAKPKQIYCYLQRIGIGLSPAMSYS ALVTKTNRIARILAGSKKKICTKKPRFMSACAQLVIAFILICIQLGIIVALFIMEPPDIM HDYPSIREVYLICNTTNLGVVTPLGYNGLLILSCTFYAFKTRNVPANFNEAKYIAFTMYT TCIIWLAFVPIYFGSNYKIITMCFSVSLSATVALGCMFVPKVYIILAKPERNVRSAFTTS TVVRMHVGDGKSSSAASRSSSLVNLWKRRGSSGETLRYKDRRLAQHKSEIECFTPKGSMG NGGRATMSSSNGKSVTWAQNEKSSRGQHLWQRLSIHINKKENPNQTAVIKPFPKSTESRG LGAGAGAGGSAGGVGATGGAGCAGAGPGGPESPDAGPKALYDVAEAEEHFPAPARPRSPS PISTLSHRAGSASRTDDDVPSLHSEPVARSSSSQGSLMEQISSVVTRFTANISELNSMML STAAPSPGVGAPLCSSYLIPKEIQLPTTMTTFAEIQPLPAIEVTGGAQPAAGAQAAGDAA RESPAAGPEAAAAKPDLEELVALTPPSPFRDSVDSGSTTPNSPVSESALCIPSSPKYDTL IIRDYTQSSSSL Click to Show/Hide
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3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
HIT2.0 ID | T64P00 |
Drugs and Modes of Action | Top | |||||
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Clinical Trial Drug(s) | [+] 9 Clinical Trial Drugs | + | ||||
1 | ADX-48621 | Drug Info | Phase 2/3 | Parkinson disease | [2] | |
2 | AFQ056 | Drug Info | Phase 2/3 | Fragile X syndrome | [3], [4] | |
3 | ADX10059 | Drug Info | Phase 2 | Anxiety disorder | [5] | |
4 | RG-7090 | Drug Info | Phase 2 | Fragile X syndrome | [6] | |
5 | STX-107 | Drug Info | Phase 2 | Autism spectrum disorder | [7], [8] | |
6 | McN3377 | Drug Info | Phase 1/2 | Fragile X syndrome | [9], [10] | |
7 | MK-3328 | Drug Info | Phase 1 | Alzheimer disease | [11] | |
8 | RG7342 | Drug Info | Phase 1 | Schizophrenia | [12] | |
9 | [3H]fenobam | Drug Info | Phase 1 | Allodynia | [13] | |
Patented Agent(s) | [+] 5 Patented Agents | + | ||||
1 | Diazepinone derivative 1 | Drug Info | Patented | Reflux disease | [14] | |
2 | Diazepinone derivative 2 | Drug Info | Patented | Reflux disease | [14] | |
3 | Diazepinone derivative 3 | Drug Info | Patented | Reflux disease | [14] | |
4 | Diazepinone derivative 4 | Drug Info | Patented | Reflux disease | [14] | |
5 | Diazepinone derivative 5 | Drug Info | Patented | Reflux disease | [14] | |
Discontinued Drug(s) | [+] 4 Discontinued Drugs | + | ||||
1 | AZD2066 | Drug Info | Discontinued in Phase 2 | Chronic neuropathic pain | [15] | |
2 | AZD2516 | Drug Info | Discontinued in Phase 2 | Chronic neuropathic pain | [16] | |
3 | LY467711 | Drug Info | Terminated | Migraine | [17] | |
4 | LY525327 | Drug Info | Terminated | Migraine | [17] | |
Mode of Action | [+] 5 Modes of Action | + | ||||
Modulator | [+] 65 Modulator drugs | + | ||||
1 | ADX-48621 | Drug Info | [18] | |||
2 | AFQ056 | Drug Info | [1] | |||
3 | ADX10059 | Drug Info | [19], [20] | |||
4 | McN3377 | Drug Info | [24] | |||
5 | MK-3328 | Drug Info | [25] | |||
6 | 6-aryl-imidazopyridine and 6-aryl-triazolopyridine carboxamide analog 1 | Drug Info | [14] | |||
7 | 6-aryl-imidazopyridine and 6-aryl-triazolopyridine carboxamide analog 2 | Drug Info | [14] | |||
8 | 6-aryl-imidazopyridine and 6-aryl-triazolopyridine carboxamide analog 3 | Drug Info | [14] | |||
9 | Bicarboxylic and tricarboxylic ethynyl derivative 1 | Drug Info | [14] | |||
10 | Bicarboxylic and tricarboxylic ethynyl derivative 2 | Drug Info | [14] | |||
11 | Bicarboxylic and tricarboxylic ethynyl derivative 3 | Drug Info | [14] | |||
12 | Bicyclic heteroaryl carboxamide analog 1 | Drug Info | [14] | |||
13 | Bicyclic heteroaryl carboxamide analog 2 | Drug Info | [14] | |||
14 | Bicyclic heteroaryl carboxamide analog 3 | Drug Info | [14] | |||
15 | Diazepinone derivative 1 | Drug Info | [14] | |||
16 | Diazepinone derivative 2 | Drug Info | [14] | |||
17 | Diazepinone derivative 3 | Drug Info | [14] | |||
18 | Diazepinone derivative 4 | Drug Info | [14] | |||
19 | Diazepinone derivative 5 | Drug Info | [14] | |||
20 | Ethynyl compound 1 | Drug Info | [14] | |||
21 | Ethynyl compound 2 | Drug Info | [14] | |||
22 | Ethynyl compound 3 | Drug Info | [14] | |||
23 | Ethynyl compound 4 | Drug Info | [14] | |||
24 | Ethynyl compound 5 | Drug Info | [14] | |||
25 | Ethynyl compound 6 | Drug Info | [14] | |||
26 | Ethynyl compound 7 | Drug Info | [14] | |||
27 | Heterocyclic derivative 1 | Drug Info | [14] | |||
28 | Heterocyclic derivative 2 | Drug Info | [14] | |||
29 | Heterocyclic derivative 3 | Drug Info | [14] | |||
30 | Imidazopyridine and triazolopyridine compound 1 | Drug Info | [14] | |||
31 | Imidazopyridine and triazolopyridine compound 2 | Drug Info | [14] | |||
32 | Imidazopyridine and triazolopyridine compound 3 | Drug Info | [14] | |||
33 | Imidazopyridine and triazolopyridine compound 4 | Drug Info | [14] | |||
34 | Imidazo[1,2-a]pyridine derivative 1 | Drug Info | [14] | |||
35 | N-alkylamide derivative 1 | Drug Info | [14] | |||
36 | N-alkylamide derivative 2 | Drug Info | [14] | |||
37 | PMID28067079-Compound-95 | Drug Info | [14] | |||
38 | PMID28067079-Compound-97 | Drug Info | [14] | |||
39 | PMID28067079-Compound-98 | Drug Info | [14] | |||
40 | Pyrazolopyrimidine derivative 1 | Drug Info | [14] | |||
41 | Pyrazolopyrimidine derivative 2 | Drug Info | [14] | |||
42 | Pyrazolopyrimidine derivative 3 | Drug Info | [14] | |||
43 | Pyrazolopyrimidine derivative 4 | Drug Info | [14] | |||
44 | Pyrazolopyrimidine derivative 5 | Drug Info | [14] | |||
45 | Pyrazolopyrimidine derivative 6 | Drug Info | [14] | |||
46 | Pyridine derivative 12 | Drug Info | [14] | |||
47 | Pyridine derivative 13 | Drug Info | [14] | |||
48 | Pyridine derivative 14 | Drug Info | [14] | |||
49 | Pyridine derivative 15 | Drug Info | [14] | |||
50 | Pyridine derivative 16 | Drug Info | [14] | |||
51 | Pyridine derivative 17 | Drug Info | [14] | |||
52 | Tetra-hydro-oxazolopyridine derivative 1 | Drug Info | [14] | |||
53 | Tetra-hydro-oxazolopyridine derivative 2 | Drug Info | [14] | |||
54 | Tetra-hydro-oxazolopyridine derivative 3 | Drug Info | [14] | |||
55 | Tetra-hydro-oxazolopyridine derivative 4 | Drug Info | [14] | |||
56 | Tetra-hydro-oxazolopyridine derivative 5 | Drug Info | [14] | |||
57 | Tetra-hydro-oxazolopyridine derivative 6 | Drug Info | [14] | |||
58 | Tetra-hydro-pyrazolopyrazine derivative 1 | Drug Info | [14] | |||
59 | Tetra-hydro-pyrazolopyrazine derivative 2 | Drug Info | [14] | |||
60 | Tetra-hydro-pyrazolopyrazine derivative 3 | Drug Info | [14] | |||
61 | Tetra-hydro-pyrazolopyrazine derivative 4 | Drug Info | [14] | |||
62 | Tetra-hydro-pyrazolopyrazine derivative 5 | Drug Info | [14] | |||
63 | ADX-63365 | Drug Info | [25] | |||
64 | GRN-529 | Drug Info | [25] | |||
65 | LY-3390334 | Drug Info | [68] | |||
Antagonist | [+] 17 Antagonist drugs | + | ||||
1 | RG-7090 | Drug Info | [21] | |||
2 | STX-107 | Drug Info | [22], [23] | |||
3 | 2-(substituted ethynyl)quinoline derivative 1 | Drug Info | [14] | |||
4 | 2-(substituted ethynyl)quinoline derivative 2 | Drug Info | [14] | |||
5 | 2-(substituted ethynyl)quinoline derivative 3 | Drug Info | [14] | |||
6 | 2-(substituted ethynyl)quinoline derivative 4 | Drug Info | [14] | |||
7 | AZD2066 | Drug Info | [28] | |||
8 | AZD2516 | Drug Info | [28] | |||
9 | LY467711 | Drug Info | [24] | |||
10 | LY525327 | Drug Info | [24] | |||
11 | (+)-MCPG | Drug Info | [29] | |||
12 | (S)-4C3HPG | Drug Info | [29] | |||
13 | (S)-4CPG | Drug Info | [29] | |||
14 | ACDPP | Drug Info | [62] | |||
15 | CTEP | Drug Info | [25], [66] | |||
16 | GSK-2210875 | Drug Info | [25] | |||
17 | RTI-4229-982 | Drug Info | [25] | |||
Agonist | [+] 8 Agonist drugs | + | ||||
1 | RG7342 | Drug Info | [26] | |||
2 | (1S,3R)-ACPD | Drug Info | [29] | |||
3 | (S)-(+)-CBPG | Drug Info | [34] | |||
4 | (S)-3HPG | Drug Info | [29] | |||
5 | 3,5-DHPG | Drug Info | [29] | |||
6 | CHPG | Drug Info | [29] | |||
7 | ibotenate | Drug Info | [29] | |||
8 | L-CCG-I | Drug Info | [29] | |||
Modulator (allosteric modulator) | [+] 51 Modulator (allosteric modulator) drugs | + | ||||
1 | [3H]fenobam | Drug Info | [27] | |||
2 | 3,3'-difluorobenzaldazine | Drug Info | [49] | |||
3 | 5-MPEP | Drug Info | [59] | |||
4 | 5PAM523 | Drug Info | [60] | |||
5 | alloswitch-1 | Drug Info | [63] | |||
6 | BOMA | Drug Info | [57] | |||
7 | Br-5MPEPy | Drug Info | [59] | |||
8 | CPPHA | Drug Info | [64] | |||
9 | CPPZ | Drug Info | [65] | |||
10 | LSN2463359 | Drug Info | [67] | |||
11 | LSN2814617 | Drug Info | [67] | |||
12 | M-5MPEP | Drug Info | [59] | |||
13 | NCFP | Drug Info | [71] | |||
14 | PMID14697765C11a | Drug Info | [57] | |||
15 | PMID14697765C16a | Drug Info | [57] | |||
16 | PMID15482906C10 | Drug Info | [72] | |||
17 | PMID15482908C8 | Drug Info | [73] | |||
18 | PMID15686941C13 | Drug Info | [62] | |||
19 | PMID16439120C20 | Drug Info | [39] | |||
20 | PMID16439120C26 | Drug Info | [39] | |||
21 | PMID17189691C42 | Drug Info | [74] | |||
22 | PMID17723296C18 | Drug Info | [37] | |||
23 | PMID17936624C36 | Drug Info | [36] | |||
24 | PMID19931453C16m | Drug Info | [61] | |||
25 | PMID20598884C8 | Drug Info | [54] | |||
26 | PMID20809633C29b | Drug Info | [75] | |||
27 | PMID21295468C47 | Drug Info | [76] | |||
28 | PMID21757343C30 | Drug Info | [77] | |||
29 | PMID21927650C18 | Drug Info | [78] | |||
30 | PMID23357634C24d | Drug Info | [79] | |||
31 | PMID23374867C24 | Drug Info | [80] | |||
32 | PMID23434029C41 | Drug Info | [81] | |||
33 | PMID23434029C53 | Drug Info | [81] | |||
34 | PTeB | Drug Info | [50] | |||
35 | SP203 | Drug Info | [82] | |||
36 | VU-1545 | Drug Info | [56] | |||
37 | VU0092273 | Drug Info | [83] | |||
38 | VU0240382 | Drug Info | [83] | |||
39 | VU0285683 | Drug Info | [84] | |||
40 | VU0357121 | Drug Info | [85] | |||
41 | VU0360172 | Drug Info | [84] | |||
42 | VU0361747 | Drug Info | [83] | |||
43 | VU0364289 | Drug Info | [86] | |||
44 | VU0366058 | Drug Info | [87] | |||
45 | VU0404251 | Drug Info | [88] | |||
46 | VU0424465 | Drug Info | [89] | |||
47 | VU0463841 | Drug Info | [90] | |||
48 | [14C]MTEP | Drug Info | [91] | |||
49 | [3H]methoxy-PEPy | Drug Info | [92] | |||
50 | [3H]methoxymethyl-MTEP | Drug Info | [91], [92] | |||
51 | [3H]resolvin E1 | Drug Info | [30] | |||
Inhibitor | [+] 197 Inhibitor drugs | + | ||||
1 | (3-(2-methylquinolin-7-yl)phenyl)methanol | Drug Info | [30] | |||
2 | (3-Ethoxy-pyridin-2-yl)-pyridin-2-yl-amine | Drug Info | [31] | |||
3 | (E)-1-Adamantan-1-yl-3-quinolin-3-yl-propenone | Drug Info | [32] | |||
4 | (E)-3-[2-(2-methyl-4-thiazolyl)vinyl]pyridine | Drug Info | [33] | |||
5 | 1-(3-(2-methylquinolin-7-yl)phenyl)ethanone | Drug Info | [30] | |||
6 | 2-(2-Methyl-thiazol-4-ylethynyl)-pyridine | Drug Info | [35] | |||
7 | 2-(2-methylquinolin-7-yl)benzonitrile | Drug Info | [30] | |||
8 | 2-(3,4-dimethylphenyl)-1,8-naphthyridine | Drug Info | [36] | |||
9 | 2-(3,5-dichlorophenyl)pyrido[2,3-d]pyrimidine | Drug Info | [37] | |||
10 | 2-(3,5-difluorophenyl)-7-methyl-1,8-naphthyridine | Drug Info | [36] | |||
11 | 2-(3,5-dimethoxyphenyl)-1,8-naphthyridine | Drug Info | [36] | |||
12 | 2-(3-(2-methylquinolin-7-yl)phenyl)acetonitrile | Drug Info | [30] | |||
13 | 2-(3-(3-methoxyphenoxy)prop-1-ynyl)pyridine | Drug Info | [38] | |||
14 | 2-(3-(benzyloxy)phenyl)isoindoline-1,3-dione | Drug Info | [39] | |||
15 | 2-(3-bromophenyl)-7-methyl-1,8-naphthyridine | Drug Info | [36] | |||
16 | 2-(3-bromophenyl)-7-methylpyrido[2,3-d]pyrimidine | Drug Info | [37] | |||
17 | 2-(3-bromophenyl)pyrido[2,3-d]pyrimidine | Drug Info | [37] | |||
18 | 2-(3-chlorobenzyloxy)-6-chloroisonicotinonitrile | Drug Info | [39] | |||
19 | 2-(3-chlorophenyl)-7-methyl-1,8-naphthyridine | Drug Info | [36] | |||
20 | 2-(4-(3-chlorophenyl)but-1-ynyl)-6-methylpyridine | Drug Info | [40] | |||
21 | 2-(m-tolylethynyl)pyrimidine | Drug Info | [41] | |||
22 | 2-(phenylethynyl)pyrimidine | Drug Info | [41] | |||
23 | 2-(pyridin-2-yl)-4-(m-tolylthio)pyrimidine | Drug Info | [42] | |||
24 | 2-Benzoxy-5-(2-methylquinolin-7-yl)benzonitrile | Drug Info | [23] | |||
25 | 2-benzyloxy-7,8-dihydro-6H-quinolin-5-one | Drug Info | [43] | |||
26 | 2-bromo-4-(3-fluorophenylethynyl)thiazole | Drug Info | [33] | |||
27 | 2-Chloro-5-(2-methylquinolin-7-yl)nicotinonitrile | Drug Info | [23] | |||
28 | 2-chloro-N-(3-(3-chlorobenzamido)phenyl)benzamide | Drug Info | [44] | |||
29 | 2-Cyclohex-1-enylethynyl-pyridine | Drug Info | [45] | |||
30 | 2-Cyclohexylethynyl-pyridine | Drug Info | [45] | |||
31 | 2-Cyclopent-1-enylethynyl-pyridine | Drug Info | [45] | |||
32 | 2-ethoxy-5-(m-tolylethynyl)pyrimidine | Drug Info | [41] | |||
33 | 2-ethynyl-4-(3-fluorophenylethynyl)thiazole | Drug Info | [33] | |||
34 | 2-m-tolyl-1,8-naphthyridine | Drug Info | [36] | |||
35 | 2-methyl-4-(2-thienylethynyl)thiazole | Drug Info | [33] | |||
36 | 2-methyl-4-(3-thienylethynyl)thiazole | Drug Info | [33] | |||
37 | 2-methyl-4-(m-tolylethynyl)thiazole | Drug Info | [33] | |||
38 | 2-Methyl-4-o-tolylethynyl-thiazole | Drug Info | [35] | |||
39 | 2-Methyl-4-p-tolylethynyl-thiazole | Drug Info | [35] | |||
40 | 2-Methyl-4-phenylethynyl-thiazole | Drug Info | [35] | |||
41 | 2-methyl-6-(3-(p-tolyloxy)prop-1-ynyl)pyridine | Drug Info | [38] | |||
42 | 2-methyl-6-(3-(phenylthio)prop-1-ynyl)pyridine | Drug Info | [40] | |||
43 | 2-methyl-6-(4-phenylbut-1-ynyl)pyridine | Drug Info | [40] | |||
44 | 2-methyl-6-(4-phenylpent-1-ynyl)pyridine | Drug Info | [40] | |||
45 | 2-methyl-6-(5-phenylpent-1-ynyl)pyridine | Drug Info | [40] | |||
46 | 2-methyl-6-(phenylethynyl)pyridine | Drug Info | [46], [47] | |||
47 | 2-methyl-7-(pyridin-3-yl)quinoline | Drug Info | [30] | |||
48 | 2-methyl-7-m-tolyl-1,6-naphthyridine | Drug Info | [36] | |||
49 | 2-methyl-7-m-tolyl-1,8-naphthyridine | Drug Info | [36] | |||
50 | 2-methyl-7-m-tolylquinoline | Drug Info | [30] | |||
51 | 2-methyl-7-phenyl-1,8-naphthyridine | Drug Info | [36] | |||
52 | 2-methyl-7-phenylquinoline | Drug Info | [30] | |||
53 | 2-phenyl-1,8-naphthyridine | Drug Info | [36] | |||
54 | 2-Phenyl-5-(2-methylthiazol-4ylethynyl)pyridine | Drug Info | [48] | |||
55 | 2-phenylethynyl-5,6,7,8-tetrahydro-quinolin-5-ol | Drug Info | [43] | |||
56 | 2-phenylethynyl-5,6,7,8-tetrahydro-quinoline | Drug Info | [43] | |||
57 | 2-phenylethynyl-7,8-dihydro-6H-quinolin-5-one | Drug Info | [43] | |||
58 | 2-[(2-methyl-4-thiazolyl)ethynyl]pyrazine | Drug Info | [33] | |||
59 | 3-(1,5-naphthyridin-3-yl)benzonitrile | Drug Info | [36] | |||
60 | 3-(1,8-naphthyridin-2-yl)benzonitrile | Drug Info | [36] | |||
61 | 3-(1-Pyridin-2-yl-1H-pyrazol-3-yl)-benzonitrile | Drug Info | [50] | |||
62 | 3-(1-Pyridin-2-yl-1H-pyrazol-4-yl)-benzonitrile | Drug Info | [50] | |||
63 | 3-(1-Pyridin-2-yl-1H-pyrrol-3-yl)-benzonitrile | Drug Info | [50] | |||
64 | 3-(2-methylbenzo[d]thiazol-5-yl)benzonitrile | Drug Info | [51] | |||
65 | 3-(2-methylquinolin-7-yl)benzonitrile | Drug Info | [30] | |||
66 | 3-(2-methylquinolin-7-yl)phenol | Drug Info | [30] | |||
67 | 3-(2-Pyridin-2-yl-2H-tetrazol-5-yl)-benzonitrile | Drug Info | [50] | |||
68 | 3-(3,4-dimethylphenyl)-1,5-naphthyridine | Drug Info | [36] | |||
69 | 3-(3-(3-chlorobenzyloxy)-5-methylphenyl)pyridine | Drug Info | [39] | |||
70 | 3-(3-bromophenylethynyl)-5-methyl[1,2,4]triazine | Drug Info | [52] | |||
71 | 3-(3-methylphenylethynyl)-5-methyl[1,2,4]triazine | Drug Info | [52] | |||
72 | 3-(3-Pyridin-2-yl-pyrazol-1-yl)-benzonitrile | Drug Info | [50] | |||
73 | 3-(3-Pyridin-2-yl-pyrrol-1-yl)-benzonitrile | Drug Info | [50] | |||
74 | 3-(4-Pyridin-2-yl-imidazol-1-yl)-benzonitrile | Drug Info | [50] | |||
75 | 3-(4-Pyridin-2-yl-pyrazol-1-yl)-benzonitrile | Drug Info | [50] | |||
76 | 3-(5-Pyridin-2-yl-tetrazol-2-yl)-benzonitrile | Drug Info | [50] | |||
77 | 3-(6-fluoroquinazolin-4-ylamino)benzonitrile | Drug Info | [47] | |||
78 | 3-(7-methyl-1,8-naphthyridin-2-yl)benzonitrile | Drug Info | [36] | |||
79 | 3-biphenyl-4-ylethynyl-5-methyl-[1,2,4]triazine | Drug Info | [52] | |||
80 | 3-bromo-5-(2-methylquinolin-7-yl)benzonitrile | Drug Info | [30] | |||
81 | 3-bromo-5-[(2-methyl-4-thiazolyl)ethynyl]pyridine | Drug Info | [33] | |||
82 | 3-bromo-N-(6-methylpyridin-2-yl)benzamide | Drug Info | [53] | |||
83 | 3-chloro-5-(2-methylquinolin-7-yl)benzonitrile | Drug Info | [30] | |||
84 | 3-chloro-N-(3-isobutyramidophenyl)benzamide | Drug Info | [44] | |||
85 | 3-chloro-N-(4-methylthiazol-2-yl)benzamide | Drug Info | [53] | |||
86 | 3-chloro-N-(6-chloropyridin-2-yl)benzamide | Drug Info | [53] | |||
87 | 3-chloro-N-(6-methylpyridin-2-yl)benzamide | Drug Info | [48] | |||
88 | 3-cyano-5-fluoro-N-(3-fluorophenyl)benzamide | Drug Info | [54] | |||
89 | 3-cyano-5-fluoro-N-(pyridin-2-yl)benzamide | Drug Info | [54] | |||
90 | 3-cyano-5-fluoro-N-m-tolylbenzamide | Drug Info | [54] | |||
91 | 3-cyano-5-fluoro-N-phenylbenzamide | Drug Info | [54] | |||
92 | 3-cyano-N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamide | Drug Info | [55], [56] | |||
93 | 3-cyano-N-(1,4-diphenyl-1H-pyrazol-5-yl)benzamide | Drug Info | [56] | |||
94 | 3-cyano-N-(3-cyanophenyl)-5-fluorobenzamide | Drug Info | [54] | |||
95 | 3-cyano-N-(3-ethylphenyl)-5-fluorobenzamide | Drug Info | [54] | |||
96 | 3-cyano-N-(3-ethynylphenyl)-5-fluorobenzamide | Drug Info | [54] | |||
97 | 3-cyano-N-(6-ethylpyridin-2-yl)-5-fluorobenzamide | Drug Info | [54] | |||
98 | 3-cyano-N-(6-methylpyridin-2-yl)benzamide | Drug Info | [48] | |||
99 | 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 |
Target Poor or Non Binders | Top | |||||
---|---|---|---|---|---|---|
Target Poor or Non Binders |
Target Profiles in Patients | Top | |||||
---|---|---|---|---|---|---|
Target Expression Profile (TEP) |
Target Affiliated Biological Pathways | Top | |||||
---|---|---|---|---|---|---|
KEGG Pathway | [+] 7 KEGG Pathways | + | ||||
1 | Calcium signaling pathway | |||||
2 | Neuroactive ligand-receptor interaction | |||||
3 | Gap junction | |||||
4 | Long-term potentiation | |||||
5 | Retrograde endocannabinoid signaling | |||||
6 | Glutamatergic synapse | |||||
7 | Huntington's disease | |||||
Panther Pathway | [+] 4 Panther Pathways | + | ||||
1 | Heterotrimeric G-protein signaling pathway-Gq alpha and Go alpha mediated pathway | |||||
2 | Metabotropic glutamate receptor group III pathway | |||||
3 | Metabotropic glutamate receptor group I pathway | |||||
4 | Endogenous cannabinoid signaling | |||||
Reactome | [+] 2 Reactome Pathways | + | ||||
1 | G alpha (q) signalling events | |||||
2 | Class C/3 (Metabotropic glutamate/pheromone receptors) | |||||
WikiPathways | [+] 5 WikiPathways | + | ||||
1 | Hypothetical Network for Drug Addiction | |||||
2 | GPCRs, Class C Metabotropic glutamate, pheromone | |||||
3 | Gastrin-CREB signalling pathway via PKC and MAPK | |||||
4 | GPCR ligand binding | |||||
5 | GPCR downstream signaling |
Target-Related Models and Studies | Top | |||||
---|---|---|---|---|---|---|
Target Validation |
References | Top | |||||
---|---|---|---|---|---|---|
REF 1 | Metabolism and disposition of the metabotropic glutamate receptor 5 antagonist (mGluR5) mavoglurant (AFQ056) in healthy subjects. Drug Metab Dispos. 2013 Sep;41(9):1626-41. | |||||
REF 2 | ClinicalTrials.gov (NCT04857359) Dipraglurant (ADX48621) for the Treatment of Patients With Parkinson's Disease Receiving Levodopa-based Therapy. U.S. National Institutes of Health. | |||||
REF 3 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7586). | |||||
REF 4 | ClinicalTrials.gov (NCT01433354) Long-term, Safety and Tolerability Study of AFQ056 in Adolescent Patients With Fragile X Syndrome (Open-label). U.S. National Institutes of Health. | |||||
REF 5 | ClinicalTrials.gov (NCT00820105) ADX10059 Migraine Prevention Study. U.S. National Institutes of Health. | |||||
REF 6 | ClinicalTrials.gov (NCT01750957) A Study of RO4917523 in Pediatric Patients With Fragile X Syndrome. U.S. National Institutes of Health. | |||||
REF 7 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 3336). | |||||
REF 8 | ClinicalTrials.gov (NCT01325740) A Study to Assess the Tolerability of a Single Dose of STX107 in Adults With Fragile X Syndrome. U.S. National Institutes of Health. | |||||
REF 9 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1434). | |||||
REF 10 | ClinicalTrials.gov (NCT00637221) Open Label Study Investigating Safety and Efficacy of NPL2009 50 mg - 150 mg on Prepulse Inhibition Tests and Continuous Performance Tasks, Adults With Fragile X Syndrome. U.S. National Institutes of Health. | |||||
REF 11 | ClinicalTrials.gov (NCT00954538) Safety, Radiation Dosimetry, Biokinetics, and Effectiveness of [18F]MK3328 (MK-3328-001). U.S. National Institutes of Health. | |||||
REF 12 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800040973) | |||||
REF 13 | ClinicalTrials.gov (NCT01981395) Fenobam on Heat/Capsaicin Induced Hyperalgesia in Healthy Volunteers. U.S. National Institutes of Health. | |||||
REF 14 | mGlu5 negative allosteric modulators: a patent review (2013 - 2016).Expert Opin Ther Pat. 2017 Jun;27(6):691-706. | |||||
REF 15 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027605) | |||||
REF 16 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029648) | |||||
REF 17 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015556) | |||||
REF 18 | Pipeline of Addex Pharma. Addex Pharma. 2009. | |||||
REF 19 | A proof-of-concept study evaluating the effect of ADX10059, a metabotropic glutamate receptor-5 negative allosteric modulator, on acid exposure and... Gut. 2009 Sep;58(9):1192-9. | |||||
REF 20 | Novel treatments of GERD: focus on the lower esophageal sphincter. Eur Rev Med Pharmacol Sci. 2008 Aug;12 Suppl 1:103-10. | |||||
REF 21 | The challenges of clinical trials in fragile X syndrome. Psychopharmacology (Berl) 2014; 231(6): 1237-1250. | |||||
REF 22 | Social Communication is an Emerging Target for Pharmacotherapy in Autism Spectrum Disorder - A Review of the Literature on Potential Agents. J Can Acad Child Adolesc Psychiatry. 2014 February; 23(1):20-30. | |||||
REF 23 | Structure-activity relationships in a novel series of 7-substituted-aryl quinolines and 5-substituted-aryl benzothiazoles at the metabotropic gluta... Bioorg Med Chem. 2010 May 1;18(9):3026-35. | |||||
REF 24 | Glutamate- and GABA-based CNS therapeutics. Curr Opin Pharmacol. 2006 Feb;6(1):7-17. | |||||
REF 25 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 293). | |||||
REF 26 | Clinical pipeline report, company report or official report of Roche. | |||||
REF 27 | Fenobam: a clinically validated nonbenzodiazepine anxiolytic is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agon... J Pharmacol Exp Ther. 2005 Nov;315(2):711-21. | |||||
REF 28 | Clinical pipeline report, company report or official report of AstraZeneca (2009). | |||||
REF 29 | Characterization of [(3)H]Quisqualate binding to recombinant rat metabotropic glutamate 1a and 5a receptors and to rat and human brain sections. J Neurochem. 2000 Dec;75(6):2590-601. | |||||
REF 30 | Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists. Bioorg Med Chem Lett. 2007 Aug 15;17(16):4415-8. | |||||
REF 31 | Dipyridyl amines: potent metabotropic glutamate subtype 5 receptor antagonists. Bioorg Med Chem Lett. 2005 Oct 1;15(19):4350-3. | |||||
REF 32 | Synergism of virtual screening and medicinal chemistry: identification and optimization of allosteric antagonists of metabotropic glutamate recepto... Bioorg Med Chem. 2009 Aug 1;17(15):5708-15. | |||||
REF 33 | Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic g... J Med Chem. 2006 Feb 9;49(3):1080-100. | |||||
REF 34 | 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. | |||||
REF 35 | 5-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-2,3'-bipyridine: a highly potent, orally active metabotropic glutamate subtype 5 (mGlu5) receptor antagonist... Bioorg Med Chem Lett. 2004 Aug 2;14(15):3993-6. | |||||
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. | |||||
REF 39 | 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. | |||||
REF 53 | 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. | |||||
REF 55 | 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. | |||||
REF 56 | 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. | |||||
REF 57 | Discovery of novel modulators of metabotropic glutamate receptor subtype-5. Bioorg Med Chem. 2004 Jan 2;12(1):17-21. | |||||
REF 58 | Synthesis and SAR of a mGluR5 allosteric partial antagonist lead: unexpected modulation of pharmacology with slight structural modifications to a 5... Bioorg Med Chem Lett. 2008 Jul 15;18(14):4098-101. | |||||
REF 59 | 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. | |||||
REF 60 | Mechanism based neurotoxicity of mGlu5 positive allosteric modulators--development challenges for a promising novel antipsychotic target. Neuropharmacology. 2014 Jul;82:161-73. | |||||
REF 61 | 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 | An allosteric modulator to control endogenous G protein-coupled receptors with light. Nat Chem Biol. 2014 Oct;10(10):813-5. | |||||
REF 64 | 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. | |||||
REF 65 | Preclinical profile of a novel metabotropic glutamate receptor 5 positive allosteric modulator. Eur J Pharmacol. 2011 Jun 1;659(2-3):146-54. | |||||
REF 66 | CTEP: a novel, potent, long-acting, and orally bioavailable metabotropic glutamate receptor 5 inhibitor. J Pharmacol Exp Ther. 2011 Nov;339(2):474-86. | |||||
REF 67 | In vitro characterisation of the novel positive allosteric modulators of the mGlu receptor, LSN2463359 and LSN2814617, and their effects on sleep architecture and operant responding in the rat. Neuropharmacology. 2013 Jan;64:224-39. | |||||
REF 68 | Inhibition of group I metabotropic glutamate receptor responses in vivo in rats by a new generation of carboxyphenylglycine-like amino acid antagon... Neurosci Lett. 2002 Sep 20;330(2):127-30. | |||||
REF 69 | Design and synthesis of novel heterobiaryl amides as metabotropic glutamate receptor subtype 5 antagonists. Bioorg Med Chem Lett. 2007 Apr 1;17(7):2074-9. | |||||
REF 70 | Discovery of a potent and brain penetrant mGluR5 positive allosteric modulator. Bioorg Med Chem Lett. 2009 Jun 15;19(12):3275-8. | |||||
REF 71 | A novel metabotropic glutamate receptor 5 positive allosteric modulator acts at a unique site and confers stimulus bias to mGlu5 signaling. Mol Pharmacol. 2013 Apr;83(4):835-47. | |||||
REF 72 | 2-(2-[3-(pyridin-3-yloxy)phenyl]-2H-tetrazol-5-yl) pyridine: a highly potent, orally active, metabotropic glutamate subtype 5 (mGlu5) receptor antagonist. Bioorg Med Chem Lett. 2004 Nov 15;14(22):5473-6. | |||||
REF 73 | 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. | |||||
REF 74 | Rational design, synthesis, and structure-activity relationship of benzoxazolones: new potent mglu5 receptor antagonists based on the fenobam struc... Bioorg Med Chem Lett. 2007 Mar 1;17(5):1302-6. | |||||
REF 75 | Design, synthesis, and structure-activity relationships of novel bicyclic azole-amines as negative allosteric modulators of metabotropic glutamate receptor 5. J Med Chem. 2010 Oct 14;53(19):7107-18. | |||||
REF 76 | Discovery of novel positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5). Bioorg Med Chem Lett. 2011 Mar 1;21(5):1402-6. | |||||
REF 77 | 6-Aryl-3-pyrrolidinylpyridines as mGlu5 receptor negative allosteric modulators. Bioorg Med Chem Lett. 2011 Aug 15;21(16):4891-9. | |||||
REF 78 | (3-Cyano-5-fluorophenyl)biaryl negative allosteric modulators of mGlu(5): Discovery of a new tool compound with activity in the OSS mouse model of addiction. ACS Chem Neurosci. 2011 Aug 17;2(8):471-482. | |||||
REF 79 | 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 | Synthesis and simple 18F-labeling of 3-fluoro-5-(2-(2-(fluoromethyl)thiazol-4-yl)ethynyl)benzonitrile as a high affinity radioligand for imaging mo... J Med Chem. 2007 Jul 12;50(14):3256-66. | |||||
REF 83 | Functional impact of allosteric agonist activity of selective positive allosteric modulators of metabotropic glutamate receptor subtype 5 in regulating central nervous system function. Mol Pharmacol.2012 Feb;81(2):120-33. | |||||
REF 84 | Discovery of novel allosteric modulators of metabotropic glutamate receptor subtype 5 reveals chemical and functional diversity and in vivo activity in rat behavioral models of anxiolytic and antipsychotic activity. Mol Pharmacol. 2010 Dec;78(6):1105-23. | |||||
REF 85 | Discovery of a Novel Chemical Class of mGlu(5) Allosteric Ligands with Distinct Modes of Pharmacology. ACS Chem Neurosci. 2010 Oct 20;1(10):702-716. | |||||
REF 86 | Discovery of N-Aryl Piperazines as Selective mGlu(5) Potentiators with Efficacy in a Rodent Model Predictive of Anti-Psychotic Activity. ACS Med Chem Lett. 2010 Nov 11;1(8):433-438. | |||||
REF 87 | Discovery of 2-(2-benzoxazoyl amino)-4-aryl-5-cyanopyrimidine as negative allosteric modulators (NAMs) of metabotropic glutamate receptor (mGlu : from an artificial neural network virtual screen to an in vivo tool compound. ChemMedChem. 2012 Mar 5;7(3):406-14. | |||||
REF 88 | Optimization of an ether series of mGlu5 positive allosteric modulators: molecular determinants of MPEP-site interaction crossover. Bioorg Med Chem Lett. 2012 Oct 15;22(20):6481-5. | |||||
REF 89 | Unique signaling profiles of positive allosteric modulators of metabotropic glutamate receptor subtype 5 determine differences in in vivo activity. Biol Psychiatry. 2013 Mar 15;73(6):501-9. | |||||
REF 90 | Substituted 1-Phenyl-3-(pyridin-2-yl)urea negative allosteric modulators of mGlu5: discovery of a new tool compound VU0463841 with activity in rat models of cocaine addiction. ACS Chem Neurosci. 2013Aug 21;4(8):1217-28. | |||||
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. | |||||
REF 93 | Excitatory amino acid receptor ligands: resolution, absolute stereochemistry, and enantiopharmacology of 2-amino-3-(4-butyl-3-hydroxyisoxazol-5-yl)... J Med Chem. 1998 Mar 12;41(6):930-9. |
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