Target (103)
Compound (178)
Article Title (87)
Article Author (222)
Assay (299)
udp-n-acetylmuramoyl-l-alanyl-d-glutamate--l-lysine ligase
udp-n-acetylmuramoyl-l-alanine:d-glutamate ligase
udp-n-acetylmuramoyl-l-alanyl-d-glutamate--2,6-diaminopimelate ligase
glutamate dehydrogenase
glutamate kainate
glutamate receptor
glutamate-ampa
glutamate-kainate
cystine/glutamate transporter
glutamate ampa 1
glutamate ampa 2
glutamate carboxypeptidase ii
glutamate decarboxylase 2
glutamate receptor 1
glutamate receptor 2
glutamate receptor 3
glutamate receptor 4
glutamate--cysteine ligase
glutamate--trna ligase
glutamate-kainate 5
glutamate-nmda-mk801
metabotropic glutamate 1
metabotropic glutamate 1a
metabotropic glutamate 4a
metabotropic glutamate 5
metabotropic glutamate 5a
metabotropic glutamate 8
metabotropic glutamate receptor
glutamate carboxypeptidase ii (gcpii)
glutamate metabotropic receptor 1
glutamate metabotropic receptor 5
glutamate receptor ionotropic ampa
glutamate receptor ionotropic kainate
glutamate receptor ionotropic, kainate
glutamate receptor, metabotropic 4
glutamate/aspartate transporter ii
metabotropic glutamate 3/1a
metabotropic glutamate receptor 1
metabotropic glutamate receptor 2
metabotropic glutamate receptor 3
metabotropic glutamate receptor 4
metabotropic glutamate receptor 5
metabotropic glutamate receptor 6
metabotropic glutamate receptor 7
metabotropic glutamate receptor 8
glutamate nmda receptor; grin1/grin2a
glutamate nmda receptor; grin1/grin2b
glutamate nmda receptor; grin1/grin2c
glutamate receptor ampa 1/2
glutamate receptor ampa 2/4
glutamate receptor ampa 3/4
glutamate receptor delta-2 subunit
glutamate receptor ionotropic kainate 2
glutamate receptor ionotropic, ampa 4
glutamate receptor ionotropic, kainate 1
glutamate receptor ionotropic, kainate 2
glutamate receptor ionotropic, kainate 3
glutamate receptor ionotropic, kainate 4
glutamate receptor ionotropic, kainate 5
glutamate receptor ionotropic, nmda 2a
glutamate receptor ionotropic, nmda 2b
glutamate receptor ionotropic, nmda 2c
glutamate receptor, metabotropic 2 precursor
glutamate--cysteine ligase catalytic subunit
ionotropic glutamate receptor nmda1/2b
metabotropic glutamate 1/5-d
metabotropic glutamate 5/1-f
metabotropic glutamate receptor 2/3
metabotropic glutamate receptor 4 (mglu4)
metabotropic glutamate receptor 4 [q124r]
metabotropic glutamate receptor 5 (mglu5a)
sodium-dependent glutamate/aspartate transporter
glutamate (nmda) receptor subunit zeta 1
glutamate [nmda] receptor associated protein 1
glutamate [nmda] receptor subunit epsilon 1
glutamate [nmda] receptor subunit epsilon 2
glutamate [nmda] receptor subunit epsilon 3
glutamate [nmda] receptor subunit epsilon 4
glutamate [nmda] receptor subunit epsilon-1
glutamate [nmda] receptor subunit epsilon-2
glutamate receptor ionotropic, nmda 1/2b
glutamate receptor ionotropic, nmda 1/2c
ionotropic glutamate receptor kainate 2/5
ionotropic glutamate receptor nmda 1/2c
ionotropic glutamate receptor nmda 1/2d
glutamate receptor ionotropic, nmda 1/2c/3b
udp-n-acetylmuramoylalanine--d-glutamate ligase (murgd)
5-hydroxytryptamine receptor 2a/metabotropic glutamate receptor 2
d(2) dopamine receptor/metabotropic glutamate receptor 5
glutamate receptor ionotropic, nmda 1 [f484a,t518l]/3a
glutamate receptor ionotropic, nmda 1 [f484a,t518l]/3b
isoform 1 of metabotropic glutamate receptor 5 (5a)
metabotropic glutamate receptor 1/2/3/4/5/6/7/8
guanine nucleotide-binding protein subunit alpha-15 [y147c]/metabotropic glutamate receptor 2
cathepsin l
cd40-l
ero1-l
l-aibat
l-ca
l-glutaminase
l-jak
procathepsin l
ribonuclease l
L-Glutamic acid (S)-Glu BDBM17657 (2S)-2-aminopentanedioic acid L-Glu Glutamate L-gluatmate L-Glutamate D-Glutamate L-[14C(U)]glutamate
2-aminopentanedioateglutamate glutamic acid dianion BDBM50013055 glutamate(2-) L-Glutamate
BDBM92992 L-glutamate gamma-methyl ester
BDBM82007 L-glutamate tetrazole L-2-L-2-amino-4-(5-tetrazolyl)butanoic acid
sodium dihydrogen phosphate NaH2PO4 monosodium phosphate CHEMBL1368 BDBM50155534 sodium phosphate, monobasic sodium dihydrogenphosphate sodium phosphate monobasic anhydrous phosphoric acid, monosodium salt
[Dibutylamino]-sulfonyl]-carbamicacid 2,6-di-isopropyl-phenylester,Monosodium salt BDBM50050242 CHEMBL21860
BDBM50050347 CHEMBL22422 Ethyl[[2,6-Bis(1-methylethyl)phenoxy]sulfonyl]carbamate,Monosodium salt
BDBM50050239 CHEMBL422930 Dodecyl[[[2,6-Bis(1-methylethyl)phenyl]amino]carbonyl]sulfamate,Monosodium salt
BDBM18119 Glutamate
CHEMBL21569 N-[2,6-Bis(1-methylethyl)phenyl]-N-[(dibutylamino)sulfonyl]urea,Monosodium salt BDBM50050251
BDBM85214 glutamate-AMPA
BDBM50050316 CHEMBL21350 2,6-Bis(1-methoxy)phenyl[[2,6-Bis(1-methylethyl)phenoxy]sulfonyl]carbamate,Monosodium salt
[4-Methoxy-2,6-Bis(methylisopropyl)]phenyl[[2,6-Bis(1-methylethyl)phenoxy]sulfonyl]carbamate,Monosodium salt BDBM50050207 CHEMBL280176
CHEMBL22669 [Methyl-(2-pyridin-2yl-ethyl)-amino]-sulfonyl]-carbamicacid 2,6-di-tert-butyl-4-methyl-phenylester,Monosodium salt BDBM50050310
BDBM50510130 FEMA NO. 2488 Fumaric Acid INS-297 NSC-2752 CHEBI:18012 E-297 INS NO.297 E297 Monosodium fumarate
N-[4-[[2-(2,4-Diamino-5-(2,3-dibromopropane)-5,6,7,8-tetrahydropyrido[3,2-d]pyrimidin-6-yl)methyl]amino]-3-bromobenzoyl]-L-glutamate CHEMBL477641 BDBM50266835
NaHCO3 sodium hydrogen carbonate bicarbonate of soda SODIUM BICARBONATE BDBM50155533 carbonic acid monosodium salt sodium hydrogencarbonate CHEMBL1353 sodium acid carbonate baking soda Natriumhydrogenkarbonat
somatostatin-28 L-Ser-L-Ala-L-Asn-L-Ser-L-Asn-L-Pro-L-Ala-L-Met-L-Ala-L-Pro-L-Arg-L-Glu-L-Arg-L-Lys-L-Ala-Gly-L-Cys(1)-L-Lys-L-Asn-L-Phe-L-Phe-L-Trp-L-Lys-L-Thr-L-Phe-L-Thr-L-Ser-L-Cys(1)-OH BDBM82460
BDBM85615 L-Phe-L-Val-L-Pro-L-Ile-L-Phe-L-Thr-L-Tyr-Gly-L-Glu-L-Leu-L-Gln-L-Arg-L-Leu-L-Gln-L-Glu-L-Lys-L-Glu-L-Arg-L-Asn-L-Lys-Gly-L-Gln-L-Hse-OH SK-896
BDBM86050 Ro 25-1553 Ac-L-His-L-Ser-L-Asp-L-Ala-L-Val-L-Phe-L-Thr-L-Glu-L-Asn-L-Tyr-L-Thr-L-Lys-L-Leu-L-Arg-L-Lys-L-Gln-L-Nle-L-Ala-L-Ala-L-Lys-L-Lys(1)-L-Tyr-L-Leu-L-Asn-L-Asp(1)-L-Leu-L-Lys-L-Lys-Gly-Gly-L-Thr-NH2
Cortistatin L-Asp-L-Arg-L-Met-L-Pro-L-Cys(1)-L-Arg-L-Asn-L-Phe-L-Phe-L-Trp-L-Lys-L-Thr-L-Phe-L-Ser-L-Ser-L-Cys(1)-L-Lys-OH BDBM85246 Cortistatin-17 CST17
CHEMBL509451 BDBM50263472 Bis(N-propylnoraporphin-11-O-yl) glutamate
BDBM86240 Alpha-Conotoxin MII Gly-L-Cys(1)-L-Cys(2)-L-Ser-L-Asn-L-Pro-L-Val-L-Cys(1)-L-His-L-Leu-L-Glu-L-His-L-Ser-L-Asn-L-Leu-L-Cys(2)-NH2
BDBM86145 RFRP-1 RFamide-related peptide 1 L-Met-L-Pro-L-His-L-Serr-L-Phe-L-Ala-L-Asn-L-Leu-L-Pro-L-Leu-L-Arg-L-Phe-NH2
ETPDCFWKYCV Human U-II L-Ala-Gly-L-Thr-L-Ala-L-Asp-L-Cys-L-Phe-L-Trp-L-Lys-L-Tyr-L-Cys-L-Val-OH Urotensin II BDBM86516
2-Deamino-L-Abu(1)-L-Lys-L-Asp(NH2)-L-Phe-L-Phe-L-Trp-L-Lys-L-Thr-L-Tyr-L-Thr-L-Ser-L-Abu(1)-OH CGP 23996 CGP-23996 BDBM82467
glutamic acid CHEMBL276389 Glutaminsaeure 2-aminopentanedioic acidglutamic acid Glutamate BDBM50002371
BDBM86143 RFRP-3 RFamide-related peptide 3 L-Val-L-Pro-L-Asn-L-Leu-L-Pro-L-Gln-L-Arg-L-Phe-NH2
Cyclo[L-Trp-D-Trp-L-Lys-L-Thr-L-Phe-(7-amino*heptanoyl-L-Phe-)] L-362855 L-362,855 BDBM82463
CH-275 CH275 BDBM85080 L-Cys(1)-L-Lys-L-Phe-L-Phe-D-Trp-4-[(Isopropylamino)methyl]-L-Phe-L-Thr-L-Phe-L-Thr-L-Ser-L-Cys(1)-OH
L-Cys(1)-L-Lys-L-Asn-4-Chloro-L-Phe-L-Phe-D-Trp-L-Lys-L-Thr-L-Phe-L-Thr-L-Ser-L-Cys(1)-OH BDBM82469 EC5-21 BIM 23003 BIM-23003
BDBM241961 L-isoserine-L-phenylalanine-L-valine (16b)
BDBM241962 L-isoserine-L-phenylglycine-L-valine (16c)
BDBM241963 L-isoserine-L-valine-L-phenylalanine (16d)
BDBM241964 L-isoserine-L-tyrosinase-L-valine (16e)
BDBM241965 L-isoserine-L-valine-L-valine (16f)
BDBM241966 L-isoserine-L-phenylglycine-L-phenylalanine (16g)
BDBM241967 L-isoserine-L-valine-L-leucyl (16h)
BDBM241969 L-isoserine-L-phenylglycine-L-leucyl (16k)
BDBM241970 L-isoserine-L-tyrosinase-L-leucyl (16l)
BDBM241971 L-isoserine-L-eucyl-L-tyrosinase (16m)
BDBM241972 L-isoserine-L-phenylalanine-L-phenylalanine (16n)
L-isoserine-L-leucyl-L-valine (16i) BDBM241968
haTRAP BDBM85087 L-Ala-4-Fluoro-L-Phe-L-Arg-3-cyclohexyl-L-Ala-N-amidino-L-Lys-L-Phe-NH2
BDBM50202358 CHEMBL387121 cyclo(-D-Tyr-L-Arg-L-Arg-L-Nal-L-Pro-)
BDBM50202361 CHEMBL387120 cyclo(-D-Tyr-L-Arg-L-Arg-L-Nal-L-Ala-)
CHEMBL218863 cyclo(-D-Tyr-L-Arg-L-Arg-L-Nal-L-Pic-) BDBM50202370
BDBM235705 L-Isoseryl-L-phenylalanyl-L-leucine hydrochloride (14b)
L-Isoseryl-L-leucyl-L-phenylalanine hydrochloride (14a) BDBM235704
BDBM82459 BIM 23058 BIM-23058 D-Phe-L-Phe-L-Tyr-D-Trp-L-Lys-L-Val-L-Phe-L-Thr-NH2
BDBM85519 L-797591 L-797,591
US9527857, L BDBM253920 US9464092, L
N-Methylcyclo[L-Ala-L-Tyr-D-Trp-L-Lys-L-Abu-L-Phe-] BIM-23027 BIM 23027 BDBM82455
D-Phe-L-Cys(1)-L-Tyr-D-Trp-L-Lys-L-Abu-L-Cys(1)-L-Thr-NH2 BIM-23023 BIM 23023 BDBM82465
6-Deoxy-L-galactose CHEMBL469449 L-fucose BDBM50242419 6-deoxy-L-galactopyranoseL-fucopyranose L-fucopyranose
CHEMBL408403 5-isoleucine-angiotensin II 5-L-isoleucineangiotensin II angiotensin II (human) US9624243, Angiotensin II L-alpha-aspartyl-L-arginyl-L-valyl-L-tyrosyl-L-isoleucyl-L-histidyl-L-prolyl-L-phenylalanine Ile(5)-angiotensin II N-(1-(N-(N-(N-(N-(N(2)-L-alpha-aspartyl-L-arginyl)-L-valyl)-L-tyrosyl)-L-isoleucyl)-L-histidyl)-L-prolyl)-L-phenylalanine isoleucine(5)-angiotensin II BDBM50236697 angiotensin II (mouse) Asp-Arg-Val-Tyr-Ile-His-Pro-Phe Angiotensin II human angiotensin II
Ac-L-Phe-L-Tyr BDBM36213
Ac-L-Tyr-L-Tyr BDBM36221
BDBM36217 Ac-L-Tyr-L-Phe
BDBM36241 Cbz-L-Phe-L-Pro
BDBM50176926 CHEMBL224628 L-norvalyl-L-prolinamide
BDBM50266654 CHEMBL476173 L-Tryptophan-L-glutamine
BDBM50266679 CHEMBL513911 L-Tryptophan-L-asparagine
CHEMBL224340 BDBM50176925 L-leucyl-L-prolinamide
CHEMBL224341 BDBM50176924 L-isoleucyl-L-prolinamide
CHEMBL375933 L-valyl-L-prolinamide BDBM50176929
CHEMBL388843 L-norleucyl-L-prolinamide BDBM50176919
CHEMBL477417 BDBM50266680 L-Tryptophan-L-arginine
Cbz-L-Ala-L-Phe BDBM36233
Cbz-L-Ala-L-Trp BDBM36237
Cbz-L-Ala-L-Tyr BDBM36235
Cbz-L-Phe-L-Val BDBM36239
Cbz-L-Pro-L-Phe BDBM36243
L-Tryptophan-L-leucine BDBM50266681 CHEMBL477627
L-phenylalanyl-L-prolinamide BDBM50176941 CHEMBL224610
US9539260, L US9763952, Example L BDBM204121
Z-L-Glu-L-Tyr BDBM36122
BDBM235700 L-Isoseryl-L-leucyl-L-phenylalanine methyl ester hydrochloride (13a)
BDBM235701 L-Isoseryl-L-phenylalanyl-L-leucine methyl ester hydrochloride (13b)
BDBM235702 L-Isoseryl-L-leucyl-L-phenylalanine benzyl ester hydrochloride (13c)
BDBM235703 L-Isoseryl-L-phenylalanyl-L-leucine benzyl ester hydrochloride (13d)
CHEMBL506616 c[L-Phe-D-pro-L-Phe-L-trp] BDBM50268462
BDBM50140035 CHEMBL408086 R-L-Y-E-L-L-H-G-A-G-N-H-A-A-G-I-L-T-L
L-365209 CHEMBL127686 (cyclo-[L-propyl-D-phenylalanyl-L-isoleucyl-D-dehydropiperazyl-L-dehydropiperazyl-D(N-methyl)phenylalanyl])(L-365,209) BDBM50001309
BDBM84617 L-Alaninamide,D-phenylalanyl-L-alanyl-L-tyrosyl-D-tryptophyl-L-lysyl-L-valyl-L-alanyl-3-(2-naphthalenyl)-(9CI) CAS_150155-59-2 BIM 23053
CHEMBL429376 BDBM50139964 S-C-R-L-Y-E-L-L-H-G-A-G-N-H-A-A-G-I-L-T S-C-R-L-Y-E-L-L-H-G-A-G-N-H-A-A-G-I-L-T-L
WO2022103411, Example S15 l-((S)-l-((2S,4R)-2-(((R)-3-([l,l'-biphenyl]-4-yl)-l-amino-l-oxopropan-2-yl)carbamoyl)-4-hydroxypyrrolidin-l-yl)-3,3-dimethyl-l-oxobutan-2-yl)-lH-l,2,3-triazole-4-carboxylic acid (Compound 15) BDBM552699
WO2022103411, Example S16 BDBM552700 l-((S)-l-((2S,4R)-2-(((R)-3-([l,l'-biphenyl]-4-yl)-l-amino-l-oxopropan-2-yl)carbamoyl)-4-hydroxypyrrolidin-l-yl)-3,3-dimethyl-l-oxobutan-2-yl)-lH-l,2,3-triazole-4-carboxamide (Compound 16)
G-L-Q-G-P-L-Q-R-L-L-Q-A-S-G-N-H-A-A-G-I-L-T-M CHEMBL409644 BDBM50139989 G-L-Q-G-R-L-P-R-L-L-Q-A-S-G-N-H-A-A-G-I-L-T-M
G-L-Q-G-R-L-Q-R-L-L-Q-A-S-G-N-A-A-A-G-I-L-T-M BDBM50292158 CHEMBL440806 G-L-Q-G-R-L-Q-R-L-L-Q-A-S-G-A-H-A-A-G-I-L-T-M
CHEMBL439167 L-L-H-G-A-G-N-H-A-A-G-I-L-T-L BDBM50139987
CHEMBL76232 D-Glu (2R)-2-aminopentanedioic acid D-[14C]Glu D-Glutamate BDBM26431
Ac-L-Phe-L-Trp-L-Phe-D-pro-NH2 BDBM50268589 CHEMBL499183
BDBM50202349 CHEMBL218771 cyclo(-D-Tyr-L-Arg-L-Ala-L-Nal-Gly-)
BDBM50202367 cyclo(-D-Tyr-L-Ala-L-Arg-L-Nal-Gly-) CHEMBL374108
BDBM50202368 CHEMBL375850 cyclo(-D-Tyr-L-Arg-L-Arg-L-MeNal-Gly-)
BDBM50202369 cyclo(-D-Tyr-L-Arg-L-Arg-L-Ala-Gly-) CHEMBL376513
BDBM50222726 CHEMBL393260 cyclo(-L-Am7(S2Py)-L-A1in-L-Ala-D-Pro-)
BDBM50268588 CHEMBL506595 Ac-D-pro-L-Phe-L-Trp-L-Phe-NH2
CHEMBL219075 cyclo(-D-Tyr-L-Arg-L-Arg-L-Ala-Sar-) BDBM50202373
CHEMBL219096 cyclo(-D-MeTyr-L-Arg-L-Arg-L-Nal-Gly-) BDBM50202366
CHEMBL219474 cyclo(-D-Tyr-L-Arg-L-Arg-L-Nal-Gly-) BDBM50202350
CHEMBL373420 BDBM50202341 cyclo(-D-Ala-L-Arg-L-Arg-L-Nal-Gly-)
CHEMBL393464 BDBM50222730 cyclo(-L-Am7(S2Py)-L-2MePhe-L-Ala-D-Pro-)
CHEMBL436536 BDBM50202351 cyclo(-D-Tyr-L-Arg-L-MeArg-L-Nal-Gly-)
CHEMBL502357 Ac-L-Trp-L-Phe-D-pro-L-Phe-NH2 BDBM50268590
US9790174, Example 85(l) US9481648, 85(l) US10435361, Example 85(l) BDBM256610
cyclo(-D-Tyr-L-MeArg-L-Arg-L-Nal-Gly-) CHEMBL374421 BDBM50202365
3-(2-Naphtyl)-D-Ala-L-Cys(1)-L-Tyr-D-Trp-L-Lys-L-Val-L-Cys(1)-L-Thr-NH2 BIM 23014 BDBM82470 BIM-23014 LANREOTIDE
BDBM84616 L-Alaninamide,4-chloro-D-phenylalanyl-L-alanyl-L-tyrosyl-D-tryptophyl-L-lysyl-L-valyl-L-alanyl-3-(2-naphthalenyl)-(9CI) BIM 23069 CAS_150155-67-2
BDBM84619 L-Threoninamide,3-(2-naphthalenyl)-D-alanyl-4-chloro-L-phenylalanyl-L-tyrosyl-D-tryptophyl-L-lysyl-L-threonyl-L-phenylalanyl-(9CI) BIM 23065 CAS_150155-63-8
CHEMBL427980 BDBM50140006 U-P-L-P-D-P-G-R-L-Y-E-L-L-H-G-A-G-N-H-A-A-G-I-L-T-L
WO2022103411, Example S17 BDBM552701 l-((S)-l-((2S,4R)-2-(((R)-3-([l,l'-biphenyl]-4-yl)-l-amino-l-oxopropan-2-yl)carbamoyl)-4-hydroxypyrrolidin-l-yl)-3,3-dimethyl-l-oxobutan-2-yl)-N-methyl-lH-l,2,3-triazole-4-carboxamide (Compound 17)
BDBM50140022 CHEMBL411934 U-P-L-P-D-Ahx-L-L-H-G-A-G-N-H-A-A-G-I-L-T-L
CHEMBL406777 S-C-R-L-Y-E-L-L-H-G-A-G-N-H-A-A-G-I-L-T-L BDBM50139999
Cyclo[L-Pro-D-Phe-L-Ile-1,6-didehydro-D-Pyz-1,6-didehydro-L-Pyz-N-methyl-L-Phe-] J325.338D L-365,209 BDBM81895
BDBM50416760 2-butenedioic acid, (e)- E-297 INS NO.297 E297 Fumaricum acidum Fumarate Fumaric acid Allomaleic-acid FEMA NO. 2488 INS-297 NSC-2752 CHEBI:18012 Boletic-acid Monosodium fumarate
FUMARIC ACID BDBM50620915 2-butenedioic acid, (e)- E-297 INS NO.297 E297 Fumaricum acidum Fumarate Allomaleic-acid FEMA NO. 2488 INS-297 NSC-2752 CHEBI:18012 Boletic-acid Monosodium fumarate
BDBM36120 Z-L-Glu Cbz-L-Glu
BDBM50176928 L-valyl-L-proline hexylamide CHEMBL375490
BDBM50176933 CHEMBL390771 L-valyl-L-proline piperidinylamide
BDBM50245250 L-Leucyl-L-phenylalanine methylamide CHEMBL445994
BDBM50266632 CHEMBL476008 L-Tryptophan-L-aspartic acid
CHEMBL225596 BDBM50176912 L-valyl-L-proline cyclohexylmethylamide
CHEMBL376375 BDBM50176931 L-valyl-L-proline benzylamide
CHEMBL420996 BDBM50059646 L-Nitroarginine-methoxy-L-phenylalanine
US11267820, Compound l US10689395, Compound l BDBM448085
US9138393, L-Asparigine BDBM181137 US9144538, L-Asparigine
BDBM50139991 R-S-G-P-P-G-L-Q-G-R-L-Q-R-L-L-Q CHEMBL409188
N-[(2SR,3S)-3-Amino-5-carbamoyl-2-sulfanylpentanoyl]-L-phenylalanyl-L-glutamyl-L-threonyl-L-serine BDBM50073673
US20240415800, Compound 2-1 (L-DOPA) L-DOPA BDBM50130192 dihydroxyphenylalanine US11021454, Compound L-dopa L-3,4-dihydroxyphenylalanine BDBM60928
BDBM50140034 U-P-L-P-D-A-h-x-R-L-Y-E-L-L-H-G-A-G-N-H-A-A-G-I-L-T-L CHEMBL276022
BDBM552697 WO2022103411, Example S12 (2S,4R)-N-((R)-3-([l,l'-biphenyl]-4-yl)-l-amino-l-oxopropan-2-yl)-l-((R)-2-(4-(l-(acetamidomethyl)cyclopropyl)-lH-l,2,3-triazol-l-yl)-3,3-dimethylbutanoyl)-4-hydroxypyrrolidine-2-carboxamide ( Compound 12)
WO2022103411, Example S13 (2S,4R)-N-((R)-3-([l,l'-biphenyl]-4-yl)-l-amino-l-oxopropan-2-yl)-l-((S)-2-(4-(l-(acetamidomethyl)cyclopropyl)-lH-l,2,3-triazol-l-yl)-3,3-dimethylbutanoyl)-4-hydroxypyrrolidine-2-carboxamide ( Compound 13) BDBM552698
BDBM23737 MOCAc-Gly-Lys-Pro-Ile-Leu-Phe-Phe-Arg-Leu-Lys(Dnp)-D-Arg-NH2 (7- Methoxycoumarin- 4- yl)acetyl- Glycyl- L- Lysyl- L- Prolyl- L- Isoleucyl- L- Leucyl- L- Phenylalanyl- L- Phenylalanyl- L- Arginyl- L- Leucyl- Ne- (2,4- Dinitrophenyl)- L- Lysyl- D- Arginine Amide
CHEMBL415650 BDBM50140019 G-L-Q-G-R-L-A-R-L-L-Q-A-S-G-N--A-A-G-I-L-T-M
Ac-L-N-OMT-I-D-L-D-L-V-amide CHEMBL263010 BDBM50029332
Ac-L-N-pTyr-I-D-L-D-L-V-amide CHEMBL438997 BDBM50029333
BDBM50202359 cyclo(-D-Tyr-L-Arg-L-Arg-L-Nal-D-Ala-) CHEMBL375990
CHEMBL375168 cyclo(-D-Tyr-L-Arg-L-Arg-L-Nal-D-Pic-) BDBM50202372
CHEMBL375992 BDBM50202371 cyclo(-D-Tyr-D-Arg-L-Arg-L-Nal-L-Pro-)
cyclo(-D-Tyr-D-Arg-L-Arg-L-Nal-L-Ala-) BDBM50202360 CHEMBL376811
cyclo(-D-Tyr-D-Arg-L-Arg-L-Nal-L-Pic-) CHEMBL373637 BDBM50202353
cyclo(-D-Tyr-L-Arg-L-Arg-L-Nal-D-Pro-) CHEMBL387122 BDBM50202374
cyclo(-D-Tyr-L-Arg-L-Arg-L-Nal-beta-Ala-) CHEMBL375991 BDBM50202344
BDBM50139970 CHEMBL410918 R-S-G-P-P-G-L-Q-G-R-L-Q-R-L-L-Q-A-S-G-N-H-A-A-G-I-L-T-L
Cyclo[L-Pro-D-Trp-L-Ile-1,6-didehydro-D-Pyz-L-Pip-D-His-] J325.349J L-366,875 BDBM81894
BDBM552693 (2S,4R)-N-((R)-3-([l,l'-biphenyl]-4-yl)-l-amino-l-oxopropan-2-yl)-l-((2S)-2-(adamantan-l-yl)-2-(4-cyclopropyl-lH-l,2,3-triazol-l-yl)acetyl)-4-hydroxypyrrolidine-2-carboxamide (Compound 8) WO2022103411, Example S8
BDBM552718 WO2022103411, Example S34 l-((R)-l-((2S,4R)-2-(((R)-3-([l,l'-biphenyl]-4-yl)-l-amino-l-oxopropan-2-yl)carbamoyl)-4-hydroxypyrrolidin-l-yl)-3-methyl-l-oxobutan-2-yl)-5-methyl-lH-l,2,3-triazole-4-carboxylic acid (Compound 36) WO2022103411, Compound 36
WO2022103411, Example S35 BDBM552719 l-((S)-l-((2S,4R)-2-(((R)-3-([l,l'-biphenyl]-4-yl)-l-amino-l-oxopropan-2-yl)carbamoyl)-4-hydroxypyrrolidin-l-yl)-3-methyl-l-oxobutan-2-yl)-5-methyl-lH-l,2,3-triazole-4-carboxylic acid (Compound 37) WO2022103411, Compound 37
A-L-Q-G-R-L-Q-R-L-L-Q-A-S-G-N-H-A-A-G-I-L-T-M CHEMBL429374 BDBM50139997
BDBM50139966 G-L-Q-G-R-L-Q-R-L-L-Q-P-S-G-N-H-A-A-G-I-L-T-M CHEMBL204810
BDBM50139973 CHEMBL407866 G-L-Q-G-R-L-Q-P-L-L-Q-A-S-G-N-H-A-A-G-I-L-T-M
BDBM50139983 G-L-Q-G-A-L-Q-R-L-L-Q-A-S-G-N-H-A-A-G-I-L-T-M CHEMBL437920
BDBM50139992 CHEMBL411589 G-L-Q-A-R-L-Q-R-L-L-Q-A-S-G-N-H-A-A-G-I-L-T-M
BDBM50139994 G-L-Q-G-R-L-Q-R-L-L-Q-A-A-G-N-H-A-A-G-I-L-T-M CHEMBL428126
BDBM50140003 CHEMBL263625 G-L-Q-G-R-L-Q-R-L-L-Q-A-S-G-N-H-A-A-G-I-L-T-A
BDBM50140004 CHEMBL425940 P-L-Q-G-R-L-Q-R-L-L-Q-A-S-G-N-H-A-A-G-I-L-T-M
BDBM50140010 CHEMBL217721 G-L-Q-G-R-L-Q-R-L-L-Q-A-S-G-N-H-A-A-G-I-L-T-P
BDBM50140013 CHEMBL440613 G-L-Q-G-R-L-Q-R-L-L-Q-A-P-G-N-H-A-A-G-I-L-T-M
BDBM50140021 CHEMBL409745 G-L-Q-G-R-L-Q-R-L-L-Q-A-S-G-N-H-A-A-P-I-L-T-M
BDBM50140026 G-L-Q-G-R-L-Q-R-L-L-Q-A-S-G-N-H-A-A-A-I-L-T-M CHEMBL411097
BDBM50140030 CHEMBL412247 G-L-Q-G-R-L-Q-R--L-L-Q-A-S-G-N-H-A-A-G-I-L-A-M
BDBM50140031 G-L-Q-G-R-L-Q-R-L-L-Q-A-S-G-N-H-P-A-G-I-L-T-M CHEMBL268346
BDBM50140036 CHEMBL406591 G-L-Q-G-R-L-Q-R-L-L-Q-A-S-G-N-H-A-A-G-A-L-T-M
CHEMBL265993 G-L-Q-G-R-L-Q-R-L-L-Q-A-S-G-N-H-A-A-G-I-L-P-M BDBM50140009
CHEMBL269724 BDBM50139986 G-L-Q-G-R-L-Q-A-L-L-Q-A-S-G-N-H-A-A-G-I-L-T-M
CHEMBL408467 BDBM50292157 G-L-Q-G-R-L-Q-R-L-L-Q-A-S-A-N-H-A-A-G-I-L-T-M
CHEMBL409392 BDBM50139979 G-L-Q-G-R-L-Q-R-L-L-Q-A-S-G-N-H-A-P-G-I-L-T-M
CHEMBL437906 BDBM50139996 G-L-Q-G-R-L-Q-R-L-L-Q-A-S-G-N-H-A-A-G-P-L-T-M
CHEMBL438276 G-L-Q-G-R-L-Q-R-L-L-P-A-S-G-N-H-A-A-G-I-L-T-M BDBM50140028
CHEMBL439110 BDBM50139990 G-L-Q-G-R-L-Q-R-L-L-Q-A-S-G-N-P-A-A-G-I-L-T-M
CHEMBL441585 BDBM50140023 G-L-Q-P-R-L-Q-R-L-L-Q-A-S-G-N-H-A-A-G-I-L-T-M
G-L-P-G-R-L-Q-R-L-L-Q-A-S-G-N-H-A-A-G-I-L-T-M CHEMBL441924 BDBM50139969
G-L-Q-G-R-L-Q-R-L-L-A-A-S-G-N-H-A-A-G-I-L-T-M BDBM50140029 CHEMBL411048
G-L-Q-G-R-L-Q-R-L-L-Q-A-S-G-P-H-A-A-G-I-L-T-M BDBM50139960 CHEMBL428626
G-L-Q-G-R-L-Q-R-L-L-Q-A-S-P-N-H-A-A-G-I-L-T-M BDBM50139975 CHEMBL409323
T-C-S-C-R-L-Y-E-L-L-H-G-A-G-N-H-A-A-G-I-L-T-L BDBM50139974 CHEMBL268347
Shi, Q; Savage, JE; Hufeisen, SJ; Rauser, L; Grajkowska, E; Ernsberger, P; Wroblewski, JT; Nadeau, JH; Roth, BL L-homocysteine sulfinic acid and other acidic homocysteine derivatives are potent and selective metabotropic glutamate receptor agonists. J Pharmacol Exp Ther 305: 131 -42 (2003)
Selvam, C; Goudet, C; Oueslati, N; Pin, JP; Acher, FC L-(+)-2-Amino-4-thiophosphonobutyric acid (L-thioAP4), a new potent agonist of group III metabotropic glutamate receptors: increased distal acidity affords enhanced potency. J Med Chem 50: 4656 -64 (2007)
Huynh, TH; Erichsen, MN; Tora, AS; Goudet, C; Sagot, E; Assaf, Z; Thomsen, C; Brodbeck, R; Stensbøl, TB; Bjørn-Yoshimoto, WE; Nielsen, B; Pin, JP; Gefflaut, T; Bunch, L New 4-Functionalized Glutamate Analogues Are Selective Agonists at Metabotropic Glutamate Receptor Subtype 2 or Selective Agonists at Metabotropic Glutamate Receptor Group III. J Med Chem 59: 914 -24 (2016)
Rosowsky, A; Forsch, RA; Freisheim, JH; Moran, RG; Wick, M Methotrexate analogues. 19. Replacement of the glutamate side chain in classical antifolates by L-homocysteic acid and L-cysteic acid: effect on enzyme inhibition and antitumor activity. J Med Chem 27: 600 -4 (1984)
Tsukamoto, T; Majer, P; Vitharana, D; Ni, C; Hin, B; Lu, XC; Thomas, AG; Wozniak, KM; Calvin, DC; Wu, Y; Slusher, BS; Scarpetti, D; Bonneville, GW Enantiospecificity of glutamate carboxypeptidase II inhibition. J Med Chem 48: 2319 -24 (2005)
Glavas, S; Tanner, ME The inhibition of glutamate racemase by Bioorg Med Chem Lett 7: 2265 -2270 (1997)
Mavencamp, TL; Rhoderick, JF; Bridges, RJ; Esslinger, CS Synthesis and preliminary pharmacological evaluation of novel derivatives of L-beta-threo-benzylaspartate as inhibitors of the neuronal glutamate transporter EAAT3. Bioorg Med Chem 16: 7740 -8 (2008)
Conn, PJ; Pin, JP Pharmacology and functions of metabotropic glutamate receptors. Annu Rev Pharmacol Toxicol 37: 205 -37 (1997)
Gottschling, D; Ebel, H; Riether, D; Wellenzohn, B Pyrazolopyrimidines as metabotropic glutamate 5 receptor antagonists US Patent US9029360 (2015)
Nan, F; Bzdega, T; Pshenichkin, S; Wroblewski, JT; Wroblewska, B; Neale, JH; Kozikowski, AP Dual function glutamate-related ligands: discovery of a novel, potent inhibitor of glutamate carboxypeptidase II possessing mGluR3 agonist activity. J Med Chem 43: 772 -4 (2000)
Bräuner-Osborne, H; Egebjerg, J; Nielsen, EO; Madsen, U; Krogsgaard-Larsen, P Ligands for glutamate receptors: design and therapeutic prospects. J Med Chem 43: 2609 -45 (2000)
Knöpfel, T; Kuhn, R; Allgeier, H Metabotropic glutamate receptors: novel targets for drug development. J Med Chem 38: 1417 -26 (1995)
Conn, PJ; Lindsley, CW; Emmitte, KA; Engers, JL; Bollinger, KA; Breiner, MM Negative allosteric modulators of metabotropic glutamate receptor 3 US Patent US10399948 (2019)
Rosse, G Negative allosteric modulators of metabotropic glutamate receptor subtype. ACS Med Chem Lett 4: 500 -1 (2013)
Naples, MA; Hampson, DR Pharmacological profiles of the metabotropic glutamate receptor ligands. Neuropharmacology 40: 170 -7 (2001)
Choy, CJ; Fulton, MD; Davis, AL; Hopkins, M; Choi, JK; Anderson, MO; Berkman, CE Rationally designed sulfamides as glutamate carboxypeptidase II inhibitors. Chem Biol Drug Des 82: 612 -9 (2013)
Pietrancosta, N; Kessler, A; Favre-Besse, FC; Triballeau, N; Quentin, T; Giros, B; El Mestikawy, S; Acher, FC Rose Bengal analogs and vesicular glutamate transporters (VGLUTs). Bioorg Med Chem 18: 6922 -33 (2010)
Alaux, S; Kusk, M; Sagot, E; Bolte, J; Jensen, AA; Bräuner-Osborne, H; Gefflaut, T; Bunch, L Chemoenzymatic synthesis of a series of 4-substituted glutamate analogues and pharmacological characterization at human glutamate transporters subtypes 1-3. J Med Chem 48: 7980 -92 (2005)
Chou, LC; Chen, CT; Lee, JC; Way, TD; Huang, CH; Huang, SM; Teng, CM; Yamori, T; Wu, TS; Sun, CM; Chien, DS; Qian, K; Morris-Natschke, SL; Lee, KH; Huang, LJ; Kuo, SC Synthesis and preclinical evaluations of 2-(2-fluorophenyl)-6,7-methylenedioxyquinolin-4-one monosodium phosphate (CHM-1-P-Na) as a potent antitumor agent. J Med Chem 53: 1616 -26 (2010)
Kamenecka, TM; Bonnefous, C; Govek, S; Vernier, JM; Hutchinson, J; Chung, J; Reyes-Manalo, G; Anderson, JJ Dipyridyl amines: potent metabotropic glutamate subtype 5 receptor antagonists. Bioorg Med Chem Lett 15: 4350 -3 (2005)
Lundqvist, T; Fisher, SL; Kern, G; Folmer, RH; Xue, Y; Newton, DT; Keating, TA; Alm, RA; de Jonge, BL Exploitation of structural and regulatory diversity in glutamate racemases. Nature 447: 817 -822 (2007)
Nakamura, M; Kurihara, H; Suzuki, G; Mitsuya, M; Ohkubo, M; Ohta, H Isoxazolopyridone derivatives as allosteric metabotropic glutamate receptor 7 antagonists. Bioorg Med Chem Lett 20: 726 -9 (2010)
Schann, S; Mayer, S; Franchet, C; Frauli, M; Steinberg, E; Thomas, M; Baron, L; Neuville, P Chemical switch of a metabotropic glutamate receptor 2 silent allosteric modulator into dual metabotropic glutamate receptor 2/3 negative/positive allosteric modulators. J Med Chem 53: 8775 -9 (2010)
Kozikowski, AP; Araldi, GL; Flippen-Anderson, J; George, C; Pshenichkin, S; Surina, E; Wroblewski, J Synthesis and metabotropic glutamate receptor activity of a 2-aminobicyclo[3.2.0]heptane-2,5-dicarboxylic acid, a molecule possessing an extended glutamate conformation. Bioorg Med Chem Lett 8: 925 -30 (1999)
Bonnefous, C; Vernier, JM; Hutchinson, JH; Chung, J; Reyes-Manalo, G; Kamenecka, T Dipyridyl amides: potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists. Bioorg Med Chem Lett 15: 1197 -200 (2005)
Cosford, ND; Raveendra-Panickar, D; Sheffler, DJ Metabotropic glutamate receptor negative allosteric modulators (NAMS) and uses thereof US Patent US9969726 (2018)
Cosford, ND; Raveendra-Panickar, D; Sheffler, DJ; Hutchinson, JH; Gadient, RA Metabotropic glutamate receptor negative allosteric modulators (NAMs) and uses thereof US Patent US10597367 (2020)
Dhanya, RP; Sheffler, DJ; Cosford, ND; Dahl, R Metabotropic glutamate receptor positive allosteric modulators (PAMS) and uses thereof US Patent US10099993 (2018)
PubChem, PC Modulation of the Metabotropic Glutamate Receptor mGluR4: Rat PAM Potency PubChem Bioassay (2010)
PubChem, PC Modulation of the Metabotropic Glutamate Receptor mGluR4: Selectivity at mGluR1 PubChem Bioassay (2010)
PubChem, PC Modulation of the Metabotropic Glutamate Receptor mGluR4: Selectivity at mGluR2 PubChem Bioassay (2010)
PubChem, PC Modulation of the Metabotropic Glutamate Receptor mGluR4: Selectivity at mGluR3 PubChem Bioassay (2010)
PubChem, PC Modulation of the Metabotropic Glutamate Receptor mGluR4: Selectivity at mGluR4 PubChem Bioassay (2010)
PubChem, PC Modulation of the Metabotropic Glutamate Receptor mGluR4: Selectivity at mGluR5 PubChem Bioassay (2010)
PubChem, PC Modulation of the Metabotropic Glutamate Receptor mGluR4: Selectivity at mGluR6 PubChem Bioassay (2009)
PubChem, PC Modulation of the Metabotropic Glutamate Receptor mGluR4: Selectivity at mGluR7 PubChem Bioassay (2010)
PubChem, PC Modulation of the Metabotropic Glutamate Receptor mGluR4: Selectivity at mGluR8 PubChem Bioassay (2010)
Williams, K; Dattilo, M; Sabado, TN; Kashiwagi, K; Igarashi, K Pharmacology of delta2 glutamate receptors: effects of pentamidine and protons. J Pharmacol Exp Ther 305: 740 -8 (2003)
Vanejevs, M; Jatzke, C; Renner, S; Müller, S; Hechenberger, M; Bauer, T; Klochkova, A; Pyatkin, I; Kazyulkin, D; Aksenova, E; Shulepin, S; Timonina, O; Haasis, A; Gutcaits, A; Parsons, CG; Kauss, V; Weil, T Positive and negative modulation of group I metabotropic glutamate receptors. J Med Chem 51: 634 -47 (2008)
Synthesis and Structure-Activity Relationships for Glutamate Transporter Allosteric Modulators.
Assaf, Z; Larsen, AP; Venskutonyte, R; Han, L; Abrahamsen, B; Nielsen, B; Gajhede, M; Kastrup, JS; Jensen, AA; Pickering, DS; Frydenvang, K; Gefflaut, T; Bunch, L Chemoenzymatic synthesis of new 2,4-syn-functionalized (S)-glutamate analogues and structure-activity relationship studies at ionotropic glutamate receptors and excitatory amino acid transporters. J Med Chem 56: 1614 -28 (2013)
Clark, BP; Baker, SR; Goldsworthy, J; Harris, JR; Kingston, AE (+)-2-Methyl-4-carboxyphenylglycine (LY367385) selectively antagonises metabotropic glutamate mGluR1 receptors Bioorg Med Chem Lett 7: 2777 -2780 (1997)
Volgraf, M; Gorostiza, P; Numano, R; Kramer, RH; Isacoff, EY; Trauner, D Allosteric control of an ionotropic glutamate receptor with an optical switch. Nat Chem Biol 2: 47 -52 (2006)
Lakkaraju, SK; Mbatia, H; Hanscom, M; Zhao, Z; Wu, J; Stoica, B; MacKerell, AD; Faden, AI; Xue, F Cyclopropyl-containing positive allosteric modulators of metabotropic glutamate receptor subtype 5. Bioorg Med Chem Lett 25: 2275 -9 (2015)
Kulkarni, SS; Nightingale, B; Dersch, CM; Rothman, RB; Newman, AH Design and synthesis of noncompetitive metabotropic glutamate receptor subtype 5 antagonists. Bioorg Med Chem Lett 16: 3371 -5 (2006)
PubChem, PC Modulation of the Metabotropic Glutamate Receptor mGluR4: Potency at human mGluR4 PubChem Bioassay (2010)
Bessis, AS; Bolte, J; Pin, JP; Acher, F New probes of the agonist binding site of metabotropic glutamate receptors. Bioorg Med Chem Lett 11: 1569 -72 (2001)
Barinka, C; Rovenská, M; Mlcochová, P; Hlouchová, K; Plechanovová, A; Majer, P; Tsukamoto, T; Slusher, BS; Konvalinka, J; Lubkowski, J Structural insight into the pharmacophore pocket of human glutamate carboxypeptidase II. J Med Chem 50: 3267 -73 (2007)
Shimamoto, K; Shigeri, Y; Yasuda-Kamatani, Y; Lebrun, B; Yumoto, N; Nakajima, T Syntheses of optically pure beta-hydroxyaspartate derivatives as glutamate transporter blockers. Bioorg Med Chem Lett 10: 2407 -10 (2001)
Hong, SP; Liu, KG; Ma, G; Sabio, M; Uberti, MA; Bacolod, MD; Peterson, J; Zou, ZZ; Robichaud, AJ; Doller, D Tricyclic thiazolopyrazole derivatives as metabotropic glutamate receptor 4 positive allosteric modulators. J Med Chem 54: 5070 -81 (2011)
Rosse, G Trisubstituted imidazoles as positive modulators of metabotropic glutamate receptor subtype 5. ACS Med Chem Lett 4: 819 -21 (2013)
Gasparini, F; Inderbitzin, W; Francotte, E; Lecis, G; Richert, P; Dragic, Z; Kuhn, R; Flor, PJ (+)-4-phosphonophenylglycine (PPG) a new group III selective metabotropic glutamate receptor agonist. Bioorg Med Chem Lett 10: 1241 -4 (2000)
Nataraja Sekhar, Y; Ravikumar, M; Ravi Shashi Nayana, M; Mallena, SC; Kishore Kumar, M 3D-QSAR studies of triazafluorenone inhibitors of metabotropic glutamate receptor subtype 1. Eur J Med Chem 43: 1025 -34 (2008)
Conn, PJ; Lindsley, CW; Emmitte, KA; Felts, AS; Bollinger, KA 4,5-substituted picolinamide and picolinonitrile metabotropic glutamate receptor 2 negative allosteric modulators US Patent US10538491 (2020)
Stanley, NJ; Hutchinson, MR; Kvist, T; Nielsen, B; Mathiesen, JM; Bräuner-Osborne, H; Avery, TD; Tiekink, ER; Pedersen, DS; Irvine, RJ; Abell, AD; Taylor, DK A new metabotropic glutamate receptor agonist with in vivo anti-allodynic activity. Bioorg Med Chem 18: 6089 -98 (2010)
Thomsen, C; Boel, E; Suzdak, PD Actions of phenylglycine analogs at subtypes of the metabotropic glutamate receptor family. Eur J Pharmacol 267: 77 -84 (1994)
Bertrand, HO; Bessis, AS; Pin, JP; Acher, FC Common and selective molecular determinants involved in metabotopic glutamate receptor agonist activity. J Med Chem 45: 3171 -83 (2002)
Kulkarni, SS; Newman, AH Discovery of heterobicyclic templates for novel metabotropic glutamate receptor subtype 5 antagonists. Bioorg Med Chem Lett 17: 2987 -91 (2007)
Plechanovová, A; Byun, Y; Alquicer, G; Skultétyová, L; Mloochová, P; Nemcová, A; Kim, HJ; Navrátil, M; Mease, R; Lubkowski, J; Pomper, M; Konvalinka, J; Rulíšek, L; Barinka, C Novel substrate-based inhibitors of human glutamate carboxypeptidase II with enhanced lipophilicity. J Med Chem 54: 7535 -46 (2011)
Parlow, JJ; Burney, MW; Case, BL; Girard, TJ; Hall, KA; Hiebsch, RR; Huff, RM; Lachance, RM; Mischke, DA; Rapp, SR; Woerndle, RS; Ennis, MD Piperazinyl-glutamate-pyrimidines as potent P2Y12 antagonists for inhibition of platelet aggregation. Bioorg Med Chem Lett 19: 6148 -56 (2009)
Geng, B; Basarab, G; Comita-Prevoir, J; Gowravaram, M; Hill, P; Kiely, A; Loch, J; MacPherson, L; Morningstar, M; Mullen, G; Osimboni, E; Satz, A; Eyermann, C; Lundqvist, T Potent and selective inhibitors of Helicobacter pylori glutamate racemase (MurI): pyridodiazepine amines. Bioorg Med Chem Lett 19: 930 -6 (2009)
Stoermer, D; Liu, Q; Hall, MR; Flanary, JM; Thomas, AG; Rojas, C; Slusher, BS; Tsukamoto, T Synthesis and biological evaluation of hydroxamate-Based inhibitors of glutamate carboxypeptidase II. Bioorg Med Chem Lett 13: 2097 -100 (2003)
Wright, RA; Arnold, MB; Wheeler, WJ; Ornstein, PL; Schoepp, DD [3H]LY341495 binding to group II metabotropic glutamate receptors in rat brain. J Pharmacol Exp Ther 298: 453 -60 (2001)
Ferraris, DV; Majer, P; Ni, C; Slusher, CE; Rais, R; Wu, Y; Wozniak, KM; Alt, J; Rojas, C; Slusher, BS; Tsukamoto, T d-Thiolactones as prodrugs of thiol-based glutamate carboxypeptidase II (GCPII) inhibitors. J Med Chem 57: 243 -7 (2014)
Sagot, E; Pickering, DS; Pu, X; Umberti, M; Stensbøl, TB; Nielsen, B; Chapelet, M; Bolte, J; Gefflaut, T; Bunch, L Chemo-enzymatic synthesis of a series of 2,4-syn-functionalized (S)-glutamate analogues: new insight into the structure-activity relation of ionotropic glutamate receptor subtypes 5, 6, and 7. J Med Chem 51: 4093 -103 (2008)
Malosh, C; Turlington, M; Bridges, TM; Rook, JM; Noetzel, MJ; Vinson, PN; Steckler, T; Lavreysen, H; Mackie, C; Bartolomé-Nebreda, JM; Conde-Ceide, S; Martínez-Viturro, CM; Piedrafita, M; Sánchez-Casado, MR; Macdonald, GJ; Daniels, JS; Jones, CK; Niswender, CM; Conn, PJ; Lindsley, CW; Stauffer, SR Acyl dihydropyrazolo[1,5-a]pyrimidinones as metabotropic glutamate receptor 5 positive allosteric modulators. Bioorg Med Chem Lett 25: 5115 -20 (2015)
Childress, ES; Wieting, JM; Felts, AS; Breiner, MM; Long, MF; Luscombe, VB; Rodriguez, AL; Cho, HP; Blobaum, AL; Niswender, CM; Emmitte, KA; Conn, PJ; Lindsley, CW Discovery of Novel Central Nervous System Penetrant Metabotropic Glutamate Receptor Subtype 2 (mGlu J Med Chem 62: 378 -384 (2019)
Varnes, JG; Marcus, AP; Mauger, RC; Throner, SR; Hoesch, V; King, MM; Wang, X; Sygowski, LA; Spear, N; Gadient, R; Brown, DG; Campbell, JB Discovery of novel positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5). Bioorg Med Chem Lett 21: 1402 -6 (2011)
Gates, C; Backos, DS; Reigan, P; Kang, HJ; Koerner, C; Mirzaei, J; Natale, NR Isoxazolo[3,4-d]pyridazinones positively modulate the metabotropic glutamate subtypes 2 and 4. Bioorg Med Chem 26: 4797 -4803 (2018)
Schkeryantz, JM; Kingston, AE; Johnson, MP Prospects for metabotropic glutamate 1 receptor antagonists in the treatment of neuropathic pain. J Med Chem 50: 2563 -8 (2007)
Gichinga, MG; Olson, JP; Butala, E; Navarro, HA; Gilmour, BP; Mascarella, SW; Carroll, FI Synthesis and Evaluation of Metabotropic Glutamate Receptor Subtype 5 Antagonists Based on Fenobam(). ACS Med Chem Lett 2: 882 -884 (2011)
Kozikowski, AP; Steensma, D; Varasi, M; Pshenichkin, S; Surina, E; Wroblewski, JT alpha-substituted quisqualic acid analogs: new metabotropic glutamate receptor group II selective antagonists. Bioorg Med Chem Lett 8: 447 -52 (1999)
Doornbos, MLJ; Wang, X; Vermond, SC; Peeters, L; Pérez-Benito, L; Trabanco, AA; Lavreysen, H; Cid, JM; Heitman, LH; Tresadern, G; IJzerman, AP Covalent Allosteric Probe for the Metabotropic Glutamate Receptor 2: Design, Synthesis, and Pharmacological Characterization. J Med Chem 62: 223 -233 (2019)
Chua, PC; Nagasawa, JY; Bleicher, LS; Munoz, B; Schweiger, EJ; Tehrani, L; Anderson, JJ; Cramer, M; Chung, J; Green, MD; King, CD; Reyes-Manalo, G; Cosford, ND Cyclohexenyl- and dehydropiperidinyl-alkynyl pyridines as potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists. Bioorg Med Chem Lett 15: 4589 -93 (2005)
Kulkarni, SS; Newman, AH Design and synthesis of novel heterobiaryl amides as metabotropic glutamate receptor subtype 5 antagonists. Bioorg Med Chem Lett 17: 2074 -9 (2007)
Tykvart, J; Schimer, J; Jancarík, A; Barinková, J; Navrátil, V; Starková, J; Šrámková, K; Konvalinka, J; Majer, P; Šácha, P Design of highly potent urea-based, exosite-binding inhibitors selective for glutamate carboxypeptidase II. J Med Chem 58: 4357 -63 (2015)
Kozikowski, AP; Nan, F; Conti, P; Zhang, J; Ramadan, E; Bzdega, T; Wroblewska, B; Neale, JH; Pshenichkin, S; Wroblewski, JT Design of remarkably simple, yet potent urea-based inhibitors of glutamate carboxypeptidase II (NAALADase). J Med Chem 44: 298 -301 (2001)
Geng, B; Breault, G; Comita-Prevoir, J; Petrichko, R; Eyermann, C; Lundqvist, T; Doig, P; Gorseth, E; Noonan, B Exploring 9-benzyl purines as inhibitors of glutamate racemase (MurI) in Gram-positive bacteria. Bioorg Med Chem Lett 18: 4368 -72 (2008)
Keck, TM; Zou, MF; Zhang, P; Rutledge, RP; Newman, AH Metabotropic glutamate receptor 5 negative allosteric modulators as novel tools for in vivo investigation. ACS Med Chem Lett 3: 544 -549 (2012)
Parlow, JJ; Burney, MW; Case, BL; Girard, TJ; Hall, KA; Harris, PK; Hiebsch, RR; Huff, RM; Lachance, RM; Mischke, DA; Rapp, SR; Woerndle, RS; Ennis, MD Piperazinyl glutamate pyridines as potent orally bioavailable P2Y12 antagonists for inhibition of platelet aggregation. J Med Chem 53: 2010 -37 (2010)
Parlow, JJ; Burney, MW; Case, BL; Girard, TJ; Hall, KA; Hiebsch, RR; Huff, RM; Lachance, RM; Mischke, DA; Rapp, SR; Woerndle, RS; Ennis, MD Piperazinyl-glutamate-pyridines as potent orally bioavailable P2Y12 antagonists for inhibition of platelet aggregation. Bioorg Med Chem Lett 19: 4657 -63 (2009)
Milbank, JB; Knauer, CS; Augelli-Szafran, CE; Sakkab-Tan, AT; Lin, KK; Yamagata, K; Hoffman, JK; Zhuang, N; Thomas, J; Galatsis, P; Wendt, JA; Mickelson, JW; Schwarz, RD; Kinsora, JJ; Lotarski, SM; Stakich, K; Gillespie, KK; Lam, WW; Mutlib, AE Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists. Bioorg Med Chem Lett 17: 4415 -8 (2007)
Poulsen, MH; Lucas, S; Bach, TB; Barslund, AF; Wenzler, C; Jensen, CB; Kristensen, AS; Strømgaard, K Structure-activity relationship studies of argiotoxins: selective and potent inhibitors of ionotropic glutamate receptors. J Med Chem 56: 1171 -81 (2013)
Conn, PJ; Lindsley, CW; Emmitte, KA; Engers, JL; Konkol, LC Substituted pyrazolo[1,5-a]pyrazines as negative allosteric modulators of metabotropic glutamate receptor 3 US Patent US9676782 (2017)
Flor, PJ; Gomeza, J; Tones, MA; Kuhn, R; Pin, JP; Knöpfel, T The C-terminal domain of the mGluR1 metabotropic glutamate receptor affects sensitivity to agonists. J Neurochem 67: 58 -63 (1996)
Grella, B; Adams, J; Berry, JF; Delahanty, G; Ferraris, DV; Majer, P; Ni, C; Shukla, K; Shuler, SA; Slusher, BS; Stathis, M; Tsukamoto, T The discovery and structure-activity relationships of indole-based inhibitors of glutamate carboxypeptidase II. Bioorg Med Chem Lett 20: 7222 -5 (2010)
Lolli, ML; Giordano, C; Pickering, DS; Rolando, B; Hansen, KB; Foti, A; Contreras-Sanz, A; Amir, A; Fruttero, R; Gasco, A; Nielsen, B; Johansen, TN 4-hydroxy-1,2,5-oxadiazol-3-yl moiety as bioisoster of the carboxy function. Synthesis, ionization constants, and molecular pharmacological characterization at ionotropic glutamate receptors of compounds related to glutamate and its homologues. J Med Chem 53: 4110 -8 (2010)
Terrett, JA; Chen, H; Constantineau-Forget, L; Larouche-Gauthier, R; Lépissier, L; Beaumier, F; Déry, M; Grand-Maître, C; Sturino, C; Volgraf, M; Villemure, E US Patent US10710994 (2020)
Ortega, R; Raviña, E; Masaguer, CF; Areias, F; Brea, J; Loza, MI; López, L; Selent, J; Pastor, M; Sanz, F Bioorg Med Chem Lett 19: 1773 -8 (2009)
Bengtsson, C; Blaho, S; Saitton, DB; Brickmann, K; Broddefalk, J; Davidsson, O; Drmota, T; Folmer, R; Hallberg, K; Hallén, S; Hovland, R; Isin, E; Johannesson, P; Kull, B; Larsson, LO; Löfgren, L; Nilsson, KE; Noeske, T; Oakes, N; Plowright, AT; Schnecke, V; Ståhlberg, P; Sörme, P; Wan, H; Wellner, E; Oster, L Bioorg Med Chem 19: 3039 -53 (2011)
Ringbom, T; Huss, U; Stenholm, A; Flock, S; Skattebøl, L; Perera, P; Bohlin, L J Nat Prod 64: 745 -9 (2001)
Nurminen, EM; Pihlavisto, M; Lázár, L; Pentikäinen, U; Fülöp, F; Pentikäinen, OT J Med Chem 54: 2143 -54 (2011)
Moltzen, EK; Pedersen, H; Bøgesø, KP; Meier, E; Frederiksen, K; Sánchez, C; Løve Lembøl, H J Med Chem 37: 4085 -99 (1995)
Zheng, M; Zheng, Y; Xue, Y; Liu, Y; An, L; Zhang, L; Ji, M; Xue, B; Wu, X; Gong, X; Gu, N; Zhan, X Chem Biol Drug Des 81: 399 -407 (2013)
Kaldor, SW; Kanouni, T; Arnold, L US Patent US11667634 (2023)
Axford, L; Boot, JR; Hotten, TM; Keenan, M; Martin, FM; Milutinovic, S; Moore, NA; O'Neill, MF; Pullar, IA; Tupper, DE; Van Belle, KR; Vivien, V Bioorg Med Chem Lett 13: 3277 -80 (2003)
Laqua, K; Klemm, M; Richard-Greenblatt, M; Richter, A; Liebe, L; Huang, T; Lin, S; Guardia, A; Pérez-Herran, E; Ballell, L; Av-Gay, Y; Imming, P Bioorg Med Chem 26: 3166 -3190 (2018)
Bao L
Wang, G; Dyatkina, N; Prhavc, M; Williams, C; Serebryany, V; Hu, Y; Huang, Y; Wan, J; Wu, X; Deval, J; Fung, A; Jin, Z; Tan, H; Shaw, K; Kang, H; Zhang, Q; Tam, Y; Stoycheva, A; Jekle, A; Smith, DB; Beigelman, L J Med Chem 62: 4555 -4570 (2019)
Chiellini, G; Nesi, G; Sestito, S; Chiarugi, S; Runfola, M; Espinoza, S; Sabatini, M; Bellusci, L; Laurino, A; Cichero, E; Gainetdinov, RR; Fossa, P; Raimondi, L; Zucchi, R; Rapposelli, S J Med Chem 59: 9825 -9836 (2016)
Salimbeni, A; Paleari, F; Canevotti, R; Criscuoli, M; Criscuoli, M; Lippi, A; Angiolini, M; Belvisi, L; Scolastico, C; Colombo, L Bioorg Med Chem Lett 7: 2205 -2210 (1997)
Nasveschuk, CG; Gagnon, A; Garapaty-Rao, S; Balasubramanian, S; Campbell, R; Lee, C; Zhao, F; Bergeron, L; Cummings, R; Trojer, P; Audia, JE; Albrecht, BK; Harmange, JC ACS Med Chem Lett 5: 378 -83 (2014)
Manera, C; Betti, L; Cavallini, T; Giannaccini, G; Martinelli, A; Ortore, G; Saccomanni, G; Trincavelli, L; Tuccinardi, T; Ferrarini, PL Bioorg Med Chem Lett 15: 4604 -10 (2005)
Bialy, L; Lorenz, K; Wirth, K; Steinmeyer, K; Hessler, G; Pernerstorfer, J; Brendel, J US Patent US9598410 (2017)
Bilteanu L
Choi, WJ; Shi, ZD; Worthy, KM; Bindu, L; Karki, RG; Nicklaus, MC; Fisher, RJ; Burke, TR Bioorg Med Chem Lett 16: 5265 -9 (2006)
Wijtmans, M; Verzijl, D; Bergmans, S; Lai, M; Bosch, L; Smit, MJ; de Esch, IJ; Leurs, R Bioorg Med Chem 19: 3384 -93 (2011)
Sundén, H; Schäfer, A; Scheepstra, M; Leysen, S; Malo, M; Ma, JN; Burstein, ES; Ottmann, C; Brunsveld, L; Olsson, R J Med Chem 59: 1232 -8 (2016)
Assaf, Z; Larsen, AP; Venskutonyte, R; Han, L; Abrahamsen, B; Nielsen, B; Gajhede, M; Kastrup, JS; Jensen, AA; Pickering, DS; Frydenvang, K; Gefflaut, T; Bunch, L J Med Chem 56: 1614 -28 (2013)
LI, Y; CHEN, L; SHI, Z; HU, G; GENG, P; WANG, H; SHI, S; WANG, Y; TANG, P; YU, Y; ZHANG, C; YAN, P US Patent US20240368204 (2024)
Buzard, DJ; Lopez, L; Moody, J; Kawasaki, A; Schrader, TO; Kasem, M; Johnson, B; Zhu, X; Thoresen, L; Kim, SH; Gharbaoui, T; Sengupta, D; Calvano, L; Krishnan, A; Gao, Y; Semple, G; Edwards, J; Barden, J; Morgan, M; Usmani, K; Chen, C; Sadeque, A; Chen, W; Christopher, RJ; Thatte, J; Fu, L; Solomon, M; Whelan, K; Al-Shamma, H; Gatlin, J; Gaidarov, I; Anthony, T; Le, M; Unett, DJ; Stirn, S; Blackburn, A; Behan, DP; Jones, RM ACS Med Chem Lett 5: 1334 -9 (2014)
Musella, S; Carotenuto, L; Iraci, N; Baroli, G; Ciaglia, T; Nappi, P; Basilicata, MG; Salviati, E; Barrese, V; Vestuto, V; Pignataro, G; Pepe, G; Sommella, E; Di Sarno, V; Manfra, M; Campiglia, P; Gomez-Monterrey, I; Bertamino, A; Taglialatela, M; Ostacolo, C; Miceli, F J Med Chem 65: 11340 -11364 (2022)
Bao, J; Miao, S; Kayser, F; Kotliar, AJ; Baker, RK; Doss, GA; Felix, JP; Bugianesi, RM; Slaughter, RS; Kaczorowski, GJ; Garcia, ML; Ha, SN; Castonguay, L; Koo, GC; Shah, K; Springer, MS; Staruch, MJ; Parsons, WH; Rupprecht, KM Bioorg Med Chem Lett 15: 447 -51 (2004)
Merlino, F; Daniele, S; La Pietra, V; Di Maro, S; Di Leva, FS; Brancaccio, D; Tomassi, S; Giuntini, S; Cerofolini, L; Fragai, M; Luchinat, C; Reichart, F; Cavallini, C; Costa, B; Piccarducci, R; Taliani, S; Da Settimo, F; Martini, C; Kessler, H; Novellino, E; Marinelli, L J Med Chem 61: 4791 -4809 (2018)
Lanning, ME; Yu, W; Yap, JL; Chauhan, J; Chen, L; Whiting, E; Pidugu, LS; Atkinson, T; Bailey, H; Li, W; Roth, BM; Hynicka, L; Chesko, K; Toth, EA; Shapiro, P; MacKerell, AD; Wilder, PT; Fletcher, S Eur J Med Chem 113: 273 -92 (2016)
Verhoest, PR; Proulx-Lafrance, C; Corman, M; Chenard, L; Helal, CJ; Hou, X; Kleiman, R; Liu, S; Marr, E; Menniti, FS; Schmidt, CJ; Vanase-Frawley, M; Schmidt, AW; Williams, RD; Nelson, FR; Fonseca, KR; Liras, S J Med Chem 52: 7946 -9 (2009)
Chirieac L
Benz, J; Grether, U; Hornsperger, B; Kuhn, B; Richter, H; Kocer, B; O''Hara, F; Ritter, M; Tsuchiya, S; Collin, L; Johnson, SE; Bell, C US Patent US11390610 (2022)
Parmee, ER; He, J; Mastracchio, A; Edmondson, SD; Colwell, L; Eiermann, G; Feeney, WP; Habulihaz, B; He, H; Kilburn, R; Leiting, B; Lyons, K; Marsilio, F; Patel, RA; Petrov, A; Di Salvo, J; Wu, JK; Thornberry, NA; Weber, AE Bioorg Med Chem Lett 14: 43 -6 (2003)
Ford, DJ; Duggan, NM; Fry, SE; Ripoll-Rozada, J; Agten, SM; Liu, W; Corcilius, L; Hackeng, TM; van Oerle, R; Spronk, HMH; Ashhurst, AS; Mini Sasi, V; Kaczmarski, JA; Jackson, CJ; Pereira, PJB; Passioura, T; Suga, H; Payne, RJ J Med Chem 64: 7853 -7876 (2021)
Borsari, C; Jiménez-Antón, MD; Eick, J; Bifeld, E; Torrado, JJ; Olías-Molero, AI; Corral, MJ; Santarem, N; Baptista, C; Severi, L; Gul, S; Wolf, M; Kuzikov, M; Ellinger, B; Reinshagen, J; Witt, G; Linciano, P; Tait, A; Costantino, L; Luciani, R; Tejera Nevado, P; Zander-Dinse, D; Franco, CH; Ferrari, S; Moraes, CB; Cordeiro-da-Silva, A; Ponterini, G; Clos, J; Alunda, JM; Costi, MP Eur J Med Chem 183: (2019)
Rueeger, H; Rigollier, P; Yamaguchi, Y; Schmidlin, T; Schilling, W; Criscione, L; Whitebread, S; Chiesi, M; Walker, MW; Dhanoa, D; Islam, I; Zhang, J; Gluchowski, C Bioorg Med Chem Lett 10: 1175 -9 (2000)
Cutarella L
Meyers, MJ; Liu, J; Liu, Z; Ma, H; Dai, L; Adah, D; Zhao, S; Li, X; Liu, X; Lu, Y; Huang, Y; Tu, Z; Chen, X; Tortorella, MD ACS Med Chem Lett 10: 966 -971 (2019)
Vaz, RJ; Gao, Z; Pribish, J; Chen, X; Levell, J; Davis, L; Albert, E; Brollo, M; Ugolini, A; Cramer, DM; Cairns, J; Sides, K; Liu, F; Kwong, J; Kang, J; Rebello, S; Elliot, M; Lim, H; Chellaraj, V; Singleton, RW; Li, Y Bioorg Med Chem Lett 14: 6053 -6 (2004)
Deng, L; Diao, J; Chen, P; Pujari, V; Yao, Y; Cheng, G; Crick, DC; Prasad, BV; Song, Y J Med Chem 54: 4721 -34 (2011)
Leblond, B; Chauvignac, C; Taverne, T; Beausoleil, E; Casagrande, A; Desire, L; Pando, MP; Donello, JE; Yang, R US Patent US9670181 (2017)
Huang, A; Moretto, A; Janz, K; Lowe, M; Bedard, PW; Tam, S; Di, L; Clerin, V; Sushkova, N; Tchernychev, B; Tsao, DH; Keith, JC; Shaw, GD; Schaub, RG; Wang, Q; Kaila, N J Med Chem 53: 6003 -17 (2010)
Jiao, X; Zhang, Q; Zhang, Y; Shao, J; Ding, L; Tang, C; Feng, B Bioorg Med Chem Lett 67: (2022)
Wu, S; Fluxe, A; Sheffer, J; Janusz, JM; Blass, BE; White, R; Jackson, C; Hedges, R; Murawsky, M; Fang, B; Fadayel, GM; Hare, M; Djandjighian, L Bioorg Med Chem Lett 16: 6213 -8 (2006)
Doll, F; Dolci, L; Valette, H; Hinnen, F; Vaufrey, F; Guenther, I; Fuseau, C; Coulon, C; Bottlaender, M; Crouzel, C J Med Chem 42: 2251 -9 (1999)
Dong L
Arora, J; Bordeleau, M; Dube, L; Jarvie, K; Mazzocco, L; Peragine, J; Tehim, A; Egle, I Bioorg Med Chem Lett 15: 5253 -6 (2005)
Chaikuad, A; Diharce, J; Schröder, M; Foucourt, A; Leblond, B; Casagrande, AS; Désiré, L; Bonnet, P; Knapp, S; Besson, T J Med Chem 59: 10315 -10321 (2016)
Napolitano, C; Natoni, A; Santocanale, C; Evensen, L; Lorens, JB; Murphy, PV Bioorg Med Chem Lett 21: 1167 -70 (2011)
Dawson, MI; Xia, Z; Jiang, T; Ye, M; Fontana, JA; Farhana, L; Patel, B; Xue, LP; Bhuiyan, M; Pellicciari, R; Macchiarulo, A; Nuti, R; Zhang, XK; Han, YH; Tautz, L; Hobbs, PD; Jong, L; Waleh, N; Chao, WR; Feng, GS; Pang, Y; Su, Y J Med Chem 51: 5650 -62 (2008)
Heightman, TD; Berdini, V; Braithwaite, H; Buck, IM; Cassidy, M; Castro, J; Courtin, A; Day, JEH; East, C; Fazal, L; Graham, B; Griffiths-Jones, CM; Lyons, JF; Martins, V; Muench, S; Munck, JM; Norton, D; O'Reilly, M; Palmer, N; Pathuri, P; Reader, M; Rees, DC; Rich, SJ; Richardson, C; Saini, H; Thompson, NT; Wallis, NG; Walton, H; Wilsher, NE; Woolford, AJ; Cooke, M; Cousin, D; Onions, S; Shannon, J; Watts, J; Murray, CW J Med Chem 61: 4978 -4992 (2018)
Patel, PA; Kvaratskhelia, N; Mansour, Y; Antwi, J; Feng, L; Koneru, P; Kobe, MJ; Jena, N; Shi, G; Mohamed, MS; Li, C; Kessl, JJ; Fuchs, JR Bioorg Med Chem Lett 26: 4748 -4752 (2016)
Ledneczki, I; Horváth, A; Tapolcsányi, P; Éles, J; Molnár, KD; Vágó, I; Visegrády, A; Kiss, L; Szigetvári, Á; Kóti, J; Krámos, B; Mahó, S; Holm, P; Kolok, S; Fodor, L; Thán, M; Kostyalik, D; Balázs, O; Vastag, M; Greiner, I; Lévay, G; Lendvai, B; Némethy, Z Eur J Med Chem 222: (2021)
Cheung, AW; Danho, W; Swistok, J; Qi, L; Kurylko, G; Rowan, K; Yeon, M; Franco, L; Chu, XJ; Chen, L; Yagaloff, K Bioorg Med Chem Lett 13: 133 -7 (2002)
Braun, M; Ly, CQ; Castanedo, G; Gibbons, P; Lee, W; Rudolph, J; Blaquiere, NA; Schwarz, JB; Beveridge, R; Leclerc, J; Lemire, A; Fu, L US Patent US12071425 (2024)
Raghavan, S; Yang, Z; Mosley, RT; Schleif, WA; Gabryelski, L; Olsen, DB; Stahlhut, M; Kuo, LC; Emini, EA; Chapman, KT; Tata, JR Bioorg Med Chem Lett 12: 2855 -8 (2002)
Janusz, JM; Young, PA; Ridgeway, JM; Scherz, MW; Enzweiler, K; Wu, LI; Gan, L; Chen, J; Kellstein, DE; Green, SA; Tulich, JL; Rosario-Jansen, T; Magrisso, IJ; Wehmeyer, KR; Kuhlenbeck, DL; Eichhold, TH; Dobson, RL J Med Chem 41: 3515 -29 (1998)
Sun, X; Hong, Z; Liu, M; Guo, S; Yang, D; Wang, Y; Lan, T; Gao, L; Qi, H; Gong, P; Liu, Y Bioorg Med Chem 25: 2800 -2810 (2017)
Parr, BT; Pastor, R; Sellers, BD; Pei, Z; Jaipuri, FA; Castanedo, GM; Gazzard, L; Kumar, S; Li, X; Liu, W; Mendonca, R; Pavana, RK; Potturi, H; Shao, C; Velvadapu, V; Waldo, JP; Wu, G; Yuen, PW; Zhang, Z; Zhang, Y; Harris, SF; Oh, AJ; DiPasquale, A; Dement, K; La, H; Goon, L; Gustafson, A; VanderPorten, EC; Mautino, MR; Liu, Y ACS Med Chem Lett 11: 541 -549 (2020)
Hu, Y; Li, S; Liu, F; Geng, L; Shu, X; Zhang, J Bioorg Med Chem Lett 25: 4069 -73 (2015)
Perlikowska, R; Piekielna, J; Gentilucci, L; De Marco, R; Cerlesi, MC; Calo, G; Artali, R; Tömböly, C; Kluczyk, A; Janecka, A Eur J Med Chem 109: 276 -86 (2016)
McDermott, LA; Higgins, B; Simcox, M; Luk, KC; Nevins, T; Kolinsky, K; Smith, M; Yang, H; Li, JK; Chen, Y; Ke, J; Mallalieu, N; Egan, T; Kolis, S; Railkar, A; Gerber, L; Liu, JJ; Konzelmann, F; Zhang, Z; Flynn, T; Morales, O; Chen, Y Bioorg Med Chem Lett 16: 1950 -3 (2006)
Woodard, CL; Keenan, SM; Gerena, L; Welsh, WJ; Geyer, JA; Waters, NC Bioorg Med Chem Lett 17: 4961 -6 (2007)
Maccallini, C; Arias, F; Gallorini, M; Amoia, P; Ammazzalorso, A; De Filippis, B; Fantacuzzi, M; Giampietro, L; Cataldi, A; Camacho, ME; Amoroso, R ACS Med Chem Lett 11: 1470 -1475 (2020)
Grimster, NP; Gingipalli, L; Balazs, A; Barlaam, B; Boiko, S; Boyd, S; Dry, H; Goldberg, FW; Ikeda, T; Johnson, T; Kawatkar, S; Kemmitt, P; Lamont, S; Lorthioir, O; Mfuh, A; Patel, J; Pike, A; Read, J; Romero, R; Sarkar, U; Sha, L; Simpson, I; Song, K; Su, Q; Wang, H; Watson, D; Wu, A; Zehnder, TE; Zheng, X; Li, S; Dong, Z; Yang, D; Song, Y; Wang, P; Liu, X; Dowling, JE; Edmondson, SD Bioorg Med Chem Lett 91: (2023)
Ji, Q; Zhang, X; Du, Z; Gong, L; Wang, L; Gao, C; Du, M US Patent US11584726 (2023)
Ravez, S; Arsenlis, S; Barczyk, A; Dupont, A; Frédérick, R; Hesse, S; Kirsch, G; Depreux, P; Goossens, L Bioorg Med Chem 23: 7340 -7 (2015)
Goracci, L; Nurisso, A; Roussel, E; Pérès, B; Chaptal, V; Falson, P; Marminon, C; Jose, J; Le Borgne, M; Boumendjel, A Eur J Med Chem 248: (2023)
ZHANG, C; XIA, G; XIANG, Z; KE, Y; LOU, J; ZHAO, M; HAO, L US Patent US20240101552 (2024)
BROEKER, J; ABBOTT, J; CUI, J; FESIK, SW; GOLLNER, A; HERDEIS, L; HODGES, T; LITTLE, A; MANTOULIDIS, A; RAMHARTER, J; SARKAR, D; SOKOL, K; WATERSON, A; WUNBERG, T US Patent US20250019385 (2025)
Hu, C; Li, G; Mu, Y; Wu, W; Cao, B; Wang, Z; Yu, H; Guan, P; Han, L; Li, L; Huang, X J Med Chem 64: 6008 -6020 (2021)
He, L; Zhang, MY; Cox, M; Zhang, Q; Donnell, AF; Zhang, Y; Tarby, C; Gill, P; Subbaiah, MAM; Ramar, T; Reddy, M; Puttapaka, V; Li, YX; Sivaprakasam, P; Critton, D; Mulligan, D; Xie, C; Ramakrishnan, R; Nagar, J; Dudhgaonkar, S; Murtaza, A; Oderinde, MS; Schieven, GL; Mathur, A; Gavai, AV; Vite, G; Gangwar, S; Poudel, YB ACS Med Chem Lett 15: 189 -196 (2024)
Giraud, F; Bourhis, M; Ebrahimi, E; Herfindal, L; Choudhury, RR; Bjørnstad, R; Døskeland, SO; Anizon, F; Moreau, P Bioorg Med Chem 23: 7313 -23 (2015)
Pan, T; Xie, S; Zhou, Y; Hu, J; Luo, H; Li, X; Huang, L Bioorg Med Chem Lett 29: 2150 -2152 (2019)
Gardelli, C; Wada, H; Ray, A; Caffrey, M; Llinas, A; Shamovsky, I; Tholander, J; Larsson, J; Sivars, U; Hultin, L; Andersson, U; Sanganee, HJ; Stenvall, K; Leidvik, B; Gedda, K; Jinton, L; Rydén Landergren, M; Karabelas, K J Med Chem 61: 5974 -5987 (2018)
JIA, L; WANG, L; SHAO, Q; FENG, J; YANG, J; DU, Z US Patent US20240374581 (2024)
Jacobs, L; van der Westhuyzen, A; Pribut, N; Dentmon, ZW; Cui, D; D'Erasmo, MP; Bartsch, PW; Liu, K; Cox, RM; Greenlund, SF; Plemper, RK; Mitchell, D; Marlow, J; Andrews, MK; Krueger, RE; Sticher, ZM; Kolykhalov, AA; Natchus, MG; Zhou, B; Pelly, SC; Liotta, DC ACS Med Chem Lett 14: 1434 -1440 (2023)
Huynh, T; Chen, Z; Pang, S; Geng, J; Bandiera, T; Bindi, S; Vianello, P; Roletto, F; Thieffine, S; Galvani, A; Vaccaro, W; Poss, MA; Trainor, GL; Lorenzi, MV; Gottardis, M; Jayaraman, L; Purandare, AV Bioorg Med Chem Lett 19: 2924 -7 (2009)
Kliachyna, M; Santoni, G; Nussbaum, V; Renou, J; Sanson, B; Colletier, JP; Arboléas, M; Loiodice, M; Weik, M; Jean, L; Renard, PY; Nachon, F; Baati, R Eur J Med Chem 78: 455 -67 (2014)
Ni, S; Chen, X; Yu, Q; Xu, Y; Hu, Z; Zhang, J; Zhang, W; Li, B; Yang, X; Mao, F; Huang, J; Sun, Y; Li, J; Jia, L Eur J Med Chem 185: (2020)
A., AK; Irina, CM; M., HD; C., KJ; Jian, L; J., MP; L., RV; T., RM; A., SC; Zhe, W; Dong, X WIPO WO2022094012 (2022)
Xu, P; Xu, M; Jiang, L; Yang, Q; Luo, Z; Dauter, Z; Huang, M; Andreasen, PA J Med Chem 58: 8868 -76 (2015)
Li, M; Konteatis, Z; Nagaraja, N; Chen, Y; Zhou, S; Ma, G; Gross, S; Marjon, K; Hyer, ML; Mandley, E; Lein, M; Padyana, AK; Jin, L; Tong, S; Peters, R; Murtie, J; Travins, J; Medeiros, M; Liu, P; Frank, V; Judd, ET; Biller, SA; Marks, KM; Sui, Z; Reznik, SK J Med Chem 65: 4600 -4615 (2022)
Gardelli, C; Wada, H; Ray, A; Caffrey, M; Llinas, A; Shamovsky, I; Tholander, J; Larsson, J; Sivars, U; Hultin, L; Andersson, U; Sanganee, HJ; Stenvall, K; Leidvik, B; Gedda, K; Jinton, L; Rydén Landergren, M; Karabelas, K J Med Chem 61: 5974 -5987 (2018)
Flygare, J; Johansson, L; Lundbäck, T US Patent US11471446 (2022)
Kuo, GH; Deangelis, A; Emanuel, S; Wang, A; Zhang, Y; Connolly, PJ; Chen, X; Gruninger, RH; Rugg, C; Fuentes-Pesquera, A; Middleton, SA; Jolliffe, L; Murray, WV J Med Chem 48: 4535 -46 (2005)
Juknaite, L; Sugamata, Y; Tokiwa, K; Ishikawa, Y; Takamizawa, S; Eng, A; Sakai, R; Pickering, DS; Frydenvang, K; Swanson, GT; Kastrup, JS; Oikawa, M J Med Chem 56: 2283 -93 (2013)
J., CJ; Schulz, BW; C., BB; Thomas, C; Timothy, C; Michel, G; Jan, GP; Sabina, HR; Julie, L; Thomas, MM; Prasuna, P; K., RY; Jagadeeswar, RT; Claudio, S; Lino, V; Jinglan, Z WIPO WO2022109573 (2022)
Vogensen, SB; Jørgensen, L; Madsen, KK; Jurik, A; Borkar, N; Rosatelli, E; Nielsen, B; Ecker, GF; Schousboe, A; Clausen, RP Bioorg Med Chem 23: 2480 -8 (2015)
Thurmond, RL; Beavers, MP; Cai, H; Meduna, SP; Gustin, DJ; Sun, S; Almond, HJ; Karlsson, L; Edwards, JP J Med Chem 47: 4799 -801 (2004)
Marhefka, CA; Moore, BM; Bishop, TC; Kirkovsky, L; Mukherjee, A; Dalton, JT; Miller, DD J Med Chem 44: 1729 -40 (2001)
Bach, P; Knerr, L; Fjellström, O; Hansson, K; Mattsson, C; Gustafsson, D Bioorg Med Chem Lett 24: 821 -7 (2014)
Kong L
Rejman, D; Rabatinová, A; Pombinho, AR; Kovačková, S; Pohl, R; Zborníková, E; Kolář, M; Bogdanová, K; Nyč, O; Sanderová, H; Látal, T; Bartůněk, P; Krásný, L J Med Chem 54: 7884 -98 (2011)
A., AK; Irina, CM; M., HD; C., KJ; Jian, L; J., MP; L., RV; T., RM; A., SC; Zhe, W; Dong, X WIPO WO2022094012 (2022)
Desjardins, M; Desgagnes, J; Lacoste, L; Yang, F; Morin, M; Lapointe, J; Chenevert, R Bioorg Med Chem Lett 7: 2363 -2366 (1997)
Lad L
Jiang, X; Zhou, L; Wei, D; Meng, H; Liu, Y; Lai, L Bioorg Med Chem Lett 18: 6549 -52 (2008)
Green, N; Hu, Y; Janz, K; Li, HQ; Kaila, N; Guler, S; Thomason, J; Joseph-McCarthy, D; Tam, SY; Hotchandani, R; Wu, J; Huang, A; Wang, Q; Leung, L; Pelker, J; Marusic, S; Hsu, S; Telliez, JB; Hall, JP; Cuozzo, JW; Lin, LL J Med Chem 50: 4728 -45 (2007)
Li, L; Chenna, BC; Yang, KS; Cole, TR; Goodall, ZT; Giardini, M; Moghadamchargari, Z; Hernandez, EA; Gomez, J; Calvet, CM; Bernatchez, JA; Mellott, DM; Zhu, J; Rademacher, A; Thomas, D; Blankenship, LR; Drelich, A; Laganowsky, A; Tseng, CK; Liu, WR; Wand, AJ; Cruz-Reyes, J; Siqueira-Neto, JL; Meek, TD J Med Chem 64: 11267 -11287 (2021)
Shin, Y; Noel, R; Banerjee, S; Kojetin, D; Song, X; He, Y; Lin, L; Cameron, MD; Burris, TP; Kamenecka, TM Bioorg Med Chem Lett 22: 4413 -7 (2012)
Littman, L; Tokar, C; Venkatraman, S; Roon, RJ; Koerner, JF; Robinson, MB; Johnson, RL J Med Chem 42: 1639 -47 (1999)
Fang, A; Luo, H; Liu, L; Fan, H; Zhou, Y; Yao, Y; Zhang, Y Bioorg Med Chem Lett 27: 5450 -5453 (2017)
Roaten, JB; Kazanietz, MG; Sweatman, TW; Lothstein, L; Israel, M; Parrill, AL J Med Chem 44: 1028 -34 (2001)
Sun, Y; Lu, L; Yao, W; He, C; Zhang, F US Patent US10040790 (2018)
Berardi, F; Giudice, G; Perrone, R; Tortorella, V; Govoni, S; Lucchi, L J Med Chem 39: 4255 -60 (1996)
Luo L
Fang, Y; Chen, Y; Feng, G; Ma, L Bioorg Med Chem 19: 1167 -71 (2011)
Brand, S; Ko, EJ; Viayna, E; Thompson, S; Spinks, D; Thomas, M; Sandberg, L; Francisco, AF; Jayawardhana, S; Smith, VC; Jansen, C; De Rycker, M; Thomas, J; MacLean, L; Osuna-Cabello, M; Riley, J; Scullion, P; Stojanovski, L; Simeons, FRC; Epemolu, O; Shishikura, Y; Crouch, SD; Bakshi, TS; Nixon, CJ; Reid, IH; Hill, AP; Underwood, TZ; Hindley, SJ; Robinson, SA; Kelly, JM; Fiandor, JM; Wyatt, PG; Marco, M; Miles, TJ; Read, KD; Gilbert, IH J Med Chem 60: 7284 -7299 (2017)
Manzoni, L; Gornati, D; Manzotti, M; Cairati, S; Bossi, A; Arosio, D; Lecis, D; Seneci, P Bioorg Med Chem Lett 26: 4613 -4619 (2016)
La Pietra, V; La Regina, G; Coluccia, A; Famiglini, V; Pelliccia, S; Plotkin, B; Eldar-Finkelman, H; Brancale, A; Ballatore, C; Crowe, A; Brunden, KR; Marinelli, L; Novellino, E; Silvestri, R J Med Chem 56: 10066 -78 (2013)
O'Neill, DJ; Adedoyin, A; Bray, JA; Deecher, DC; Fensome, A; Goldberg, JA; Harrison, J; Leventhal, L; Mann, C; Mark, L; Nogle, L; Sullivan, NR; Spangler, TB; Terefenko, EA; Trybulski, EJ; Uveges, AJ; Vu, A; Whiteside, GT; Zhang, P J Med Chem 54: 6824 -31 (2011)
Arora, J; Bordeleau, M; Dube, L; Jarvie, K; Mazzocco, L; Peragine, J; Tehim, A; Egle, I Bioorg Med Chem Lett 15: 5253 -6 (2005)
Ananthan, S; Saini, SK; Zhou, G; Hobrath, JV; Padmalayam, I; Zhai, L; Bostwick, JR; Antonio, T; Reith, ME; McDowell, S; Cho, E; McAleer, L; Taylor, M; Luedtke, RR J Med Chem 57: 7042 -60 (2014)
Shahbazi Nia, S; Hossain, MA; Ji, G; Jonnalagadda, SK; Obeng, S; Rahman, MA; Sifat, AE; Nozohouri, S; Blackwell, C; Patel, D; Thompson, J; Runyon, S; Hiranita, T; McCurdy, CR; McMahon, L; Abbruscato, TJ; Trippier, PC; Neugebauer, V; German, NA Eur J Med Chem 254: (2023)
Bongartz, JA; Meerpoel, L; Boeckx, GM; Van Lommen, GR; Buyck, CF; Obrecht, D; Ermert, P; Luther, A US Patent US9688696 (2017)
Wei, Q; Mei, L; Yang, Y; Ma, H; Chen, H; Zhang, H; Zhou, J Bioorg Med Chem 26: 3866 -3874 (2018)
Shen, J; Yu, K; Meng, T; Ma, L; Zask, A; Meng, L; Wang, X; Chen, Y US Patent US9796732 (2017)
Cappelli, A; Manini, M; Valenti, S; Castriconi, F; Giuliani, G; Anzini, M; Brogi, S; Butini, S; Gemma, S; Campiani, G; Giorgi, G; Mennuni, L; Lanza, M; Giordani, A; Caselli, G; Letari, O; Makovec, F Eur J Med Chem 63: 85 -94 (2013)
Ward, JS; Merritt, L; Calligaro, DO; Bymaster, FP; Shannon, HE; Mitch, CH; Whitesitt, C; Brunsting, D; Sheardown, MJ; Olesen, PH; Swedberg, MD; Jeppesen, L; Sauerberg, P J Med Chem 41: 379 -92 (1998)
Wang, Y; Liu, JJ; Dransfield, PJ; Zhu, L; Wang, Z; Du, X; Jiao, X; Su, Y; Li, AR; Brown, SP; Kasparian, A; Vimolratana, M; Yu, M; Pattaropong, V; Houze, JB; Swaminath, G; Tran, T; Nguyen, K; Guo, Q; Zhang, J; Zhuang, R; Li, F; Miao, L; Bartberger, MD; Correll, TL; Chow, D; Wong, S; Luo, J; Lin, DC; Medina, JC ACS Med Chem Lett 4: 551 -5 (2013)
Tang, J; Liu, F; Nagy, E; Miller, L; Kirby, KA; Wilson, DJ; Wu, B; Sarafianos, SG; Parniak, MA; Wang, Z J Med Chem 59: 2648 -59 (2016)
Dolušic, E; Larrieu, P; Blanc, S; Sapunaric, F; Norberg, B; Moineaux, L; Colette, D; Stroobant, V; Pilotte, L; Colau, D; Ferain, T; Fraser, G; Galleni, M; Galeni, M; Frère, JM; Masereel, B; Van den Eynde, B; Wouters, J; Frédérick, R Bioorg Med Chem 19: 1550 -61 (2011)
Caligiuri, M; Molz, L; Liu, Q; Kaplan, F; Xu, JP; Majeti, JZ; Ramos-Kelsey, R; Murthi, K; Lievens, S; Tavernier, J; Kley, N Chem Biol 13: 711 -22 (2006)
Ranise, A; Spallarossa, A; Cesarini, S; Bondavalli, F; Schenone, S; Bruno, O; Menozzi, G; Fossa, P; Mosti, L; La Colla, M; Sanna, G; Murreddu, M; Collu, G; Busonera, B; Marongiu, ME; Pani, A; La Colla, P; Loddo, R J Med Chem 48: 3858 -73 (2005)
Zechner, M; Castro Jaramillo, CA; Zubler, NS; Taddio, MF; Mu, L; Altmann, KH; Krämer, SD J Med Chem 66: 6782 -6797 (2023)
Nepovimova, E; Korabecny, J; Dolezal, R; Babkova, K; Ondrejicek, A; Jun, D; Sepsova, V; Horova, A; Hrabinova, M; Soukup, O; Bukum, N; Jost, P; Muckova, L; Kassa, J; Malinak, D; Andrs, M; Kuca, K J Med Chem 58: 8985 -9003 (2015)
Blake, JF; Burkard, M; Chan, J; Chen, H; Chou, KJ; Diaz, D; Dudley, DA; Gaudino, JJ; Gould, SE; Grina, J; Hunsaker, T; Liu, L; Martinson, M; Moreno, D; Mueller, L; Orr, C; Pacheco, P; Qin, A; Rasor, K; Ren, L; Robarge, K; Shahidi-Latham, S; Stults, J; Sullivan, F; Wang, W; Yin, J; Zhou, A; Belvin, M; Merchant, M; Moffat, J; Schwarz, JB J Med Chem 59: 5650 -60 (2016)
Andersen, CB; Wan, Y; Chang, JW; Riggs, B; Lee, C; Liu, Y; Sessa, F; Villa, F; Kwiatkowski, N; Suzuki, M; Nallan, L; Heald, R; Musacchio, A; Gray, NS ACS Chem Biol 3: 180 -92 (2008)
Banerjee, A; Narayana, L; Raje, FA; Pisal, DV; Kadam, PA; Gullapalli, S; Kumar, H; More, SV; Bajpai, M; Sangana, RR; Jadhav, S; Gudi, GS; Khairatkar-Joshi, N; Merugu, RR; Voleti, SR; Gharat, LA Bioorg Med Chem Lett 23: 6747 -54 (2013)
Chrovian, CC; Soyode-Johnson, A; Stenne, B; Pippel, DJ; Schoellerman, J; Lord, B; Needham, AS; Xia, C; Coe, KJ; Sepassi, K; Schoetens, F; Scott, B; Nguyen, L; Jiang, X; Koudriakova, T; Balana, B; Letavic, MA J Med Chem 63: 9181 -9196 (2020)
Nordvall, G; Sundquist, S; Glas, G; Gogoll, A; Nilvebrant, L; Hacksell, U J Med Chem 35: 1541 -50 (1992)
O'Neill, DJ; Adedoyin, A; Bray, JA; Deecher, DC; Fensome, A; Goldberg, JA; Harrison, J; Leventhal, L; Mann, C; Mark, L; Nogle, L; Sullivan, NR; Spangler, TB; Terefenko, EA; Trybulski, EJ; Uveges, AJ; Vu, A; Whiteside, GT; Zhang, P J Med Chem 54: 6824 -31 (2011)
Oste L
Liao, M; Zhang, J; Wang, G; Wang, L; Liu, J; Ouyang, L; Liu, B J Med Chem 64: 2382 -2418 (2021)
Zhang, Z; Li, J; Chen, H; Huang, J; Song, X; Tu, ZC; Zhang, Z; Peng, L; Zhou, Y; Ding, K J Med Chem 65: 3249 -3265 (2022)
Rathje, OH; Perryman, L; Payne, RJ; Hamprecht, DW J Med Chem 66: 11216 -11236 (2023)
Sweis, RF; Hunt, JA; Sinclair, PJ; Chen, Y; Eveland, SS; Guo, Q; Hyland, SA; Milot, DP; Cumiskey, AM; Latham, M; Rosa, R; Peterson, L; Sparrow, CP; Anderson, MS Bioorg Med Chem Lett 21: 2597 -600 (2011)
Caroff, E; Meyer, EA; Äänismaa, P; Froidevaux, S; Keller, M; Piali, L J Med Chem 65: 11533 -11549 (2022)
Dolušic, E; Larrieu, P; Blanc, S; Sapunaric, F; Norberg, B; Moineaux, L; Colette, D; Stroobant, V; Pilotte, L; Colau, D; Ferain, T; Fraser, G; Galleni, M; Galeni, M; Frère, JM; Masereel, B; Van den Eynde, B; Wouters, J; Frédérick, R Bioorg Med Chem 19: 1550 -61 (2011)
Pisani, L; Catto, M; Nicolotti, O; Grossi, G; Di Braccio, M; Soto-Otero, R; Mendez-Alvarez, E; Stefanachi, A; Gadaleta, D; Carotti, A Eur J Med Chem 70: 723 -39 (2013)
Travelli, C; Aprile, S; Mattoteia, D; Colombo, G; Clemente, N; Scanziani, E; Terrazzino, S; Alisi, MA; Polenzani, L; Grosa, G; Genazzani, AA; Tron, GC; Galli, U Eur J Med Chem 181: (2019)
Di Maro, S; Di Leva, FS; Trotta, AM; Brancaccio, D; Portella, L; Aurilio, M; Tomassi, S; Messere, A; Sementa, D; Lastoria, S; Carotenuto, A; Novellino, E; Scala, S; Marinelli, L J Med Chem 60: 9641 -9652 (2017)
Monn, JA; Prieto, L; Taboada, L; Hao, J; Reinhard, MR; Henry, SS; Beadle, CD; Walton, L; Man, T; Rudyk, H; Clark, B; Tupper, D; Baker, SR; Lamas, C; Montero, C; Marcos, A; Blanco, J; Bures, M; Clawson, DK; Atwell, S; Lu, F; Wang, J; Russell, M; Heinz, BA; Wang, X; Carter, JH; Getman, BG; Catlow, JT; Swanson, S; Johnson, BG; Shaw, DB; McKinzie, DL J Med Chem 58: 7526 -48 (2015)
Lebon, F; Pégurier, C; Ledecq, M; Mathieu, B; Bosman, N; Frycia, A; Lengelé, S; Dhurke, K; Kanduluru, AK; Meunier, S; Wagner, A; Wolff, C; Provins, L Bioorg Med Chem Lett 22: 3978 -82 (2012)
Oliveira, JP; Freitas, RF; Melo, LS; Barros, TG; Santos, JA; Juliano, MA; Pinheiro, S; Blaber, M; Juliano, L; Muri, EM; Puzer, L ACS Med Chem Lett 5: 128 -32 (2014)
Cheung, AW; Danho, W; Swistok, J; Qi, L; Kurylko, G; Rowan, K; Yeon, M; Franco, L; Chu, XJ; Chen, L; Yagaloff, K Bioorg Med Chem Lett 13: 133 -7 (2002)
Wang, Y; Qin, L; Chen, W; Chen, Q; Sun, J; Wang, G Eur J Med Chem 226: (2021)
Castelhano, AL; Dong, H; Fyfe, MC; Gardner, LS; Kamikozawa, Y; Kurabayashi, S; Nawano, M; Ohashi, R; Procter, MJ; Qiu, L; Rasamison, CM; Schofield, KL; Shah, VK; Ueta, K; Williams, GM; Witter, D; Yasuda, K Bioorg Med Chem Lett 15: 1501 -4 (2005)
Asghar, A; Yousuf, M; Mubeen, H; Nazir, R; Haruna, K; Onawole, AT; Rasheed, L Bioorg Med Chem 27: 2397 -2404 (2019)
Schroeder, B; Demirel, P; Fischer, C; Masri, E; Kallis, S; Redl, L; Rudolf, T; Bergemann, S; Arkona, C; Nitsche, C; Bartenschlager, R; Rademann, J ACS Med Chem Lett 12: 1955 -1961 (2021)
Blake, JF; Burkard, M; Chan, J; Chen, H; Chou, KJ; Diaz, D; Dudley, DA; Gaudino, JJ; Gould, SE; Grina, J; Hunsaker, T; Liu, L; Martinson, M; Moreno, D; Mueller, L; Orr, C; Pacheco, P; Qin, A; Rasor, K; Ren, L; Robarge, K; Shahidi-Latham, S; Stults, J; Sullivan, F; Wang, W; Yin, J; Zhou, A; Belvin, M; Merchant, M; Moffat, J; Schwarz, JB J Med Chem 59: 5650 -60 (2016)
Tanini, D; Ricci, L; Capperucci, A; Di Cesare Mannelli, L; Ghelardini, C; Peat, TS; Carta, F; Angeli, A; Supuran, CT Eur J Med Chem 181: (2019)
Roberts L
Rusconi L
Sorrenti, V; Pittalà, V; Romeo, G; Amata, E; Dichiara, M; Marrazzo, A; Turnaturi, R; Prezzavento, O; Barbagallo, I; Vanella, L; Rescifina, A; Floresta, G; Tibullo, D; Di Raimondo, F; Intagliata, S; Salerno, L Eur J Med Chem 158: 937 -950 (2018)
Sutherlin, DP; Baker, S; Bisconte, A; Blaney, PM; Brown, A; Chan, BK; Chantry, D; Castanedo, G; DePledge, P; Goldsmith, P; Goldstein, DM; Hancox, T; Kaur, J; Knowles, D; Kondru, R; Lesnick, J; Lucas, MC; Lewis, C; Murray, J; Nadin, AJ; Nonomiya, J; Pang, J; Pegg, N; Price, S; Reif, K; Safina, BS; Salphati, L; Staben, S; Seward, EM; Shuttleworth, S; Sohal, S; Sweeney, ZK; Ultsch, M; Waszkowycz, B; Wei, B Bioorg Med Chem Lett 22: 4296 -302 (2012)
Ahmed, S; James, K; Owen, CP; Patel, CK; Sampson, L Bioorg Med Chem Lett 12: 1279 -82 (2002)
Santana, L; González-Díaz, H; Quezada, E; Uriarte, E; Yáñez, M; Viña, D; Orallo, F J Med Chem 51: 6740 -51 (2008)
Wood, L; Whittaker, M; Timmis, DJ; Thompson, TM; Saroglou, L; Miller, A; Davidson, AH; Christodoulou, MS; Cackett, KS; Bowles, SA; Bebbington, DS Bioorg Med Chem Lett 3: 1499 -1504 (1993)
Di Capua, A; Sticozzi, C; Brogi, S; Brindisi, M; Cappelli, A; Sautebin, L; Rossi, A; Pace, S; Ghelardini, C; Di Cesare Mannelli, L; Valacchi, G; Giorgi, G; Giordani, A; Poce, G; Biava, M; Anzini, M Eur J Med Chem 109: 99 -106 (2016)
Wasilewicz, A; Kirchweger, B; Bojkova, D; Abi Saad, MJ; Langeder, J; Bütikofer, M; Adelsberger, S; Grienke, U; Cinatl, J; Petermann, O; Scapozza, L; Orts, J; Kirchmair, J; Rabenau, HF; Rollinger, JM J Nat Prod 86: 264 -275 (2023)
Bouaboula, M; Brollo, M; Certal, V; El-Ahmad, Y; Filoche-Romme, B; Halley, F; McCort, G; Schio, L; Tabart, M; Terrier, C; Thompson, F US Patent US9714221 (2017)
Schwink, L; Stengelin, S; Gossel, M; Wirth, K US Patent US8552199 (2013)
Liu, J; Li, AR; Wang, Y; Johnson, MG; Su, Y; Shen, W; Wang, X; Lively, S; Brown, M; Lai, S; Gonzalez Lopez De Turiso, F; Xu, Q; Van Lengerich, B; Schmitt, M; Fu, Z; Sun, Y; Lawlis, S; Seitz, L; Danao, J; Wait, J; Ye, Q; Tang, HL; Grillo, M; Collins, TL; Sullivan, TJ; Medina, JC ACS Med Chem Lett 2: 326 -330 (2011)
Yu, G; Mason, HJ; Wu, X; Wang, J; Chong, S; Dorough, G; Henwood, A; Pongrac, R; Seliger, L; He, B; Normandin, D; Adam, L; Krupinski, J; Macor, JE J Med Chem 44: 1025 -7 (2001)
Borsari, C; Jiménez-Antón, MD; Eick, J; Bifeld, E; Torrado, JJ; Olías-Molero, AI; Corral, MJ; Santarem, N; Baptista, C; Severi, L; Gul, S; Wolf, M; Kuzikov, M; Ellinger, B; Reinshagen, J; Witt, G; Linciano, P; Tait, A; Costantino, L; Luciani, R; Tejera Nevado, P; Zander-Dinse, D; Franco, CH; Ferrari, S; Moraes, CB; Cordeiro-da-Silva, A; Ponterini, G; Clos, J; Alunda, JM; Costi, MP Eur J Med Chem 183: (2019)
Leroux, F; Bosc, D; Beghyn, T; Hermant, P; Warenghem, S; Landry, V; Pottiez, V; Guillaume, V; Charton, J; Herledan, A; Urata, S; Liang, W; Sheng, L; Tang, WJ; Deprez, B; Deprez-Poulain, R Eur J Med Chem 179: 557 -566 (2019)
Qiu, Z; Lin, X; Zhou, M; Liu, Y; Zhu, W; Chen, W; Zhang, W; Guo, L; Liu, H; Wu, G; Huang, M; Jiang, M; Xu, Z; Zhou, Z; Qin, N; Ren, S; Qiu, H; Zhong, S; Zhang, Y; Zhang, Y; Wu, X; Shi, L; Shen, F; Mao, Y; Zhou, X; Yang, W; Wu, JZ; Yang, G; Mayweg, AV; Shen, HC; Tang, G J Med Chem 59: 7651 -66 (2016)
Skora, L; Jahnke, W ACS Med Chem Lett 8: 632 -635 (2017)
Focken, T; Burford, K; Grimwood, ME; Zenova, A; Andrez, JC; Gong, W; Wilson, M; Taron, M; Decker, S; Lofstrand, V; Chowdhury, S; Shuart, N; Lin, S; Goodchild, SJ; Young, C; Soriano, M; Tari, PK; Waldbrook, M; Nelkenbrecher, K; Kwan, R; Lindgren, A; de Boer, G; Lee, S; Sojo, L; DeVita, RJ; Cohen, CJ; Wesolowski, SS; Johnson, JP; Dehnhardt, CM; Empfield, JR J Med Chem 62: 9618 -9641 (2019)
Squarcialupi, L; Colotta, V; Catarzi, D; Varano, F; Filacchioni, G; Varani, K; Corciulo, C; Vincenzi, F; Borea, PA; Ghelardini, C; Di Cesare Mannelli, L; Ciancetta, A; Moro, S J Med Chem 56: 2256 -69 (2013)
Stanca L
Diaz, P; Michel, S; Stella, L; Charpentier, B Bioorg Med Chem Lett 7: 2289 -2294 (1997)
Brand, S; Ko, EJ; Viayna, E; Thompson, S; Spinks, D; Thomas, M; Sandberg, L; Francisco, AF; Jayawardhana, S; Smith, VC; Jansen, C; De Rycker, M; Thomas, J; MacLean, L; Osuna-Cabello, M; Riley, J; Scullion, P; Stojanovski, L; Simeons, FRC; Epemolu, O; Shishikura, Y; Crouch, SD; Bakshi, TS; Nixon, CJ; Reid, IH; Hill, AP; Underwood, TZ; Hindley, SJ; Robinson, SA; Kelly, JM; Fiandor, JM; Wyatt, PG; Marco, M; Miles, TJ; Read, KD; Gilbert, IH J Med Chem 60: 7284 -7299 (2017)
Chien, HC; Colas, C; Finke, K; Springer, S; Stoner, L; Zur, AA; Venteicher, B; Campbell, J; Hall, C; Flint, A; Augustyn, E; Hernandez, C; Heeren, N; Hansen, L; Anthony, A; Bauer, J; Fotiadis, D; Schlessinger, A; Giacomini, KM; Thomas, AA J Med Chem 61: 7358 -7373 (2018)
Salah, M; Tahoun, M; Rudzitis-Auth, J; Stotz, L; van Koppen, CJ; Laschke, MW; Abdelsamie, AS; Frotscher, M J Med Chem 66: 8975 -8992 (2023)
Sun, L; Ying, W; Chae, J; Kowalczyk-Przewloka, T; Zhang, S; Chimmanamada, DU; Foley, KP; Du, Z; Li, H; James, D; Ng, HP; Demko, Z; Zhou, D; Qin, S US Patent US9206162 (2015)
Syrjänen, L; Kuuslahti, M; Tolvanen, M; Vullo, D; Parkkila, S; Supuran, CT Bioorg Med Chem 23: 2303 -9 (2015)
Monn, JA; Prieto, L; Taboada, L; Hao, J; Reinhard, MR; Henry, SS; Beadle, CD; Walton, L; Man, T; Rudyk, H; Clark, B; Tupper, D; Baker, SR; Lamas, C; Montero, C; Marcos, A; Blanco, J; Bures, M; Clawson, DK; Atwell, S; Lu, F; Wang, J; Russell, M; Heinz, BA; Wang, X; Carter, JH; Getman, BG; Catlow, JT; Swanson, S; Johnson, BG; Shaw, DB; McKinzie, DL J Med Chem 58: 7526 -48 (2015)
Goehring, RR; Tafesse, L; Youngman, MA US Patent US8987287 (2015)
Zhou, X; Gou, K; Xu, J; Jian, L; Luo, Y; Li, C; Guan, X; Qiu, J; Zou, J; Zhang, Y; Zhong, X; Zeng, T; Zhou, Y; Xiao, Y; Yang, X; Chen, W; Gao, P; Liu, C; Zhou, Y; Tao, L; Liu, X; Cen, X; Chen, Q; Sun, Q; Luo, Y; Zhao, Y J Med Chem 66: 14755 -14786 (2023)
Wu, S; Vossius, S; Rahmouni, S; Miletic, AV; Vang, T; Vazquez-Rodriguez, J; Cerignoli, F; Arimura, Y; Williams, S; Hayes, T; Moutschen, M; Vasile, S; Pellecchia, M; Mustelin, T; Tautz, L J Med Chem 52: 6716 -23 (2009)
Smith, ND; Poon, SF; Huang, D; Green, M; King, C; Tehrani, L; Roppe, JR; Chung, J; Chapman, DP; Cramer, M; Cosford, ND Bioorg Med Chem Lett 14: 5481 -4 (2004)
Camodeca, C; Nuti, E; Tepshi, L; Boero, S; Tuccinardi, T; Stura, EA; Poggi, A; Zocchi, MR; Rossello, A Eur J Med Chem 111: 193 -201 (2016)
Williamson, DS; Smith, GP; Mikkelsen, GK; Jensen, T; Acheson-Dossang, P; Badolo, L; Bedford, ST; Chell, V; Chen, IJ; Dokurno, P; Hentzer, M; Newland, S; Ray, SC; Shaw, T; Surgenor, AE; Terry, L; Wang, Y; Christensen, KV J Med Chem 64: 10312 -10332 (2021)
Toll L
Harper, S; Avolio, S; Pacini, B; Di Filippo, M; Altamura, S; Tomei, L; Paonessa, G; Di Marco, S; Carfi, A; Giuliano, C; Padron, J; Bonelli, F; Migliaccio, G; De Francesco, R; Laufer, R; Rowley, M; Narjes, F J Med Chem 48: 4547 -57 (2005)
Zhang, A; Ding, J; Xie, H; Song, Z; Xue, Y; Tong, L; Geng, M US Patent US10829491 (2020)
Manera, C; Betti, L; Cavallini, T; Giannaccini, G; Martinelli, A; Ortore, G; Saccomanni, G; Trincavelli, L; Tuccinardi, T; Ferrarini, PL Bioorg Med Chem Lett 15: 4604 -10 (2005)
Walpole, C; Ko, SY; Brown, M; Beattie, D; Campbell, E; Dickenson, F; Ewan, S; Hughes, GA; Lemaire, M; Lerpiniere, J; Patel, S; Urban, L J Med Chem 41: 3159 -73 (1998)
Sorrenti, V; Pittalà, V; Romeo, G; Amata, E; Dichiara, M; Marrazzo, A; Turnaturi, R; Prezzavento, O; Barbagallo, I; Vanella, L; Rescifina, A; Floresta, G; Tibullo, D; Di Raimondo, F; Intagliata, S; Salerno, L Eur J Med Chem 158: 937 -950 (2018)
Zhang, Z; Chu, XJ; Liu, JJ; Ding, Q; Zhang, J; Bartkovitz, D; Jiang, N; Karnachi, P; So, SS; Tovar, C; Filipovic, ZM; Higgins, B; Glenn, K; Packman, K; Vassilev, L; Graves, B ACS Med Chem Lett 5: 124 -7 (2014)
Sheth, PR; Shipps, GW; Seghezzi, W; Smith, CK; Chuang, CC; Sanden, D; Basso, AD; Vilenchik, L; Gray, K; Annis, DA; Nickbarg, E; Ma, Y; Lahue, B; Herbst, R; Le, HV Biochemistry 49: 8350 -8 (2010)
Zampieri, D; Laurini, E; Vio, L; Fermeglia, M; Pricl, S; Wünsch, B; Schepmann, D; Mamolo, MG Eur J Med Chem 90: 797 -808 (2015)
Redwan, IN; Dyrager, C; Solano, C; Fernández de Trocóniz, G; Voisin, L; Bliman, D; Meloche, S; Grøtli, M Eur J Med Chem 85: 127 -38 (2014)
Sahlberg, C; Noréen, R; Engelhardt, P; Högberg, M; Kangasmetsä, J; Vrang, L; Zhang, H Bioorg Med Chem Lett 8: 1511 -6 (1999)
MAO, Q; WANG, W; TAN, Y; LIANG, B; WANG, L; WU, C; ZHANG, Y; CHEN, S US Patent US20240368178 (2024)
Monn, JA; Prieto, L; Taboada, L; Hao, J; Reinhard, MR; Henry, SS; Beadle, CD; Walton, L; Man, T; Rudyk, H; Clark, B; Tupper, D; Baker, SR; Lamas, C; Montero, C; Marcos, A; Blanco, J; Bures, M; Clawson, DK; Atwell, S; Lu, F; Wang, J; Russell, M; Heinz, BA; Wang, X; Carter, JH; Getman, BG; Catlow, JT; Swanson, S; Johnson, BG; Shaw, DB; McKinzie, DL J Med Chem 58: 7526 -48 (2015)
McDermott, LA; Iyer, P; Vernetti, L; Rimer, S; Sun, J; Boby, M; Yang, T; Fioravanti, M; O'Neill, J; Wang, L; Drakes, D; Katt, W; Huang, Q; Cerione, R Bioorg Med Chem 24: 1819 -39 (2016)
Zheng, M; Li, C; Zhou, M; Jia, R; Cai, G; She, F; Wei, L; Wang, S; Yu, J; Wang, D; Calcul, L; Sun, X; Luo, X; Cheng, F; Li, Q; Wang, Y; Cai, J J Med Chem 64: 11219 -11228 (2021)
Hebach, C; Kallen, J; Nozulak, J; Tintelnot-Blomley, M; Widler, L US Patent US9670193 (2017)
Hemmerling, M; Edman, K; Lepistö, M; Eriksson, A; Ivanova, S; Dahmén, J; Rehwinkel, H; Berger, M; Hendrickx, R; Dearman, M; Jensen, TJ; Wissler, L; Hansson, T Bioorg Med Chem Lett 26: 5741 -5748 (2016)
Wood, L; Whittaker, M; Timmis, DJ; Thompson, TM; Saroglou, L; Miller, A; Davidson, AH; Christodoulou, MS; Cackett, KS; Bowles, SA; Bebbington, DS Bioorg Med Chem Lett 3: 1499 -1504 (1993)
Lu, L; Wu, L; Qian, D; Yao, W US Patent US11667635 (2023)
Louvel, J; Guo, D; Agliardi, M; Mocking, TA; Kars, R; Pham, TP; Xia, L; de Vries, H; Brussee, J; Heitman, LH; Ijzerman, AP J Med Chem 57: 3213 -22 (2014)
Xianfeng, L; Hongying, Y; Bo, Z; Xiufang, Z WIPO WO2022112139 (2022)
Bennett, F; Jiang, J; Pasternak, A; Dong, S; Gu, X; Scott, JD; Tang, H; Zhao, Z; Huang, Y; Hunter, D; Yang, D; Young, K; Xiao, L; Zhang, Z; Fu, J; Bai, Y; Zheng, Z; Zhang, X US Patent US10227331 (2019)
Deng, X; Deng, X; Ning, W; Xin, L; Li, Q; Hu, Z; Xie, B; Liang, K; Min, C; Dong, C; Huang, J; Zhou, HB J Med Chem 66: 11094 -11117 (2023)
Jerome, KD; Hepperle, ME; Walker, JK; Xing, L; Devraj, RV; Benson, AG; Baldus, JE; Selness, SR Bioorg Med Chem Lett 20: 3146 -9 (2010)
Desai, MC; Hui, HC; Liu, H; Sun, J; Xu, L US Patent US8987313 (2015)
Lu, B; Cao, H; Cao, J; Huang, S; Hu, Q; Liu, D; Shen, R; Shen, X; Tao, W; Wan, H; Wang, D; Yan, Y; Yang, L; Zhang, J; Zhang, L; Zhang, L; Zhang, M Bioorg Med Chem Lett 26: 819 -23 (2016)
Mosberg, HI; Yeomans, L; Harland, AA; Bender, AM; Sobczyk-Kojiro, K; Anand, JP; Clark, MJ; Jutkiewicz, EM; Traynor, JR J Med Chem 56: 2139 -49 (2013)
Liu, J; He, S; Jian, T; Dobbelaar, PH; Sebhat, IK; Lin, LS; Goodman, A; Guo, C; Guzzo, PR; Hadden, M; Henderson, AJ; Pattamana, K; Ruenz, M; Sargent, BJ; Swenson, B; Yet, L; Tamvakopoulos, C; Peng, Q; Pan, J; Kan, Y; Palyha, O; Kelly, TM; Guan, XM; Howard, AD; Marsh, DJ; Metzger, JM; Reitman, ML; Wyvratt, MJ; Nargund, RP Bioorg Med Chem Lett 20: 2074 -7 (2010)
Hoyt, SB; Petrilli, W; London, C; Liang, GB; Tata, J; Hu, Q; Yin, L; van Koppen, CJ; Hartmann, RW; Struthers, M; Wisniewski, T; Ren, N; Bopp, C; Sok, A; Cai, TQ; Stribling, S; Pai, LY; Ma, X; Metzger, J; Verras, A; McMasters, D; Chen, Q; Tung, E; Tang, W; Salituro, G; Buist, N; Clemas, J; Zhou, G; Gibson, J; Maxwell, CA; Lassman, M; McLaughlin, T; Castro-Perez, J; Szeto, D; Forrest, G; Hajdu, R; Rosenbach, M; Xiong, Y ACS Med Chem Lett 6: 861 -5 (2015)
Choi, K; Siegel, M; Piper, JL; Yuan, L; Cho, E; Strnad, P; Omary, B; Rich, KM; Khosla, C Chem Biol 12: 469 -75 (2005)
REINER, JJ; PANTSAR, T; FLÖTGEN, D; LAUFER, S; ZENDER, L; HENNING, M US Patent US20240101538 (2024)
Adams, JA; Bechle, BM; Dutra, JK; Garnsey, MR; Hou, X; Lee, J; Nason, II, DM; O''Neil, SV; Rankic, DA; Wang, Y; Wright, AS; Zhang, L; Zhang, L; Edmonds, DJ US Patent US20240150334 (2024)
Beveridge, RE; Wallweber, HA; Ashkenazi, A; Beresini, M; Clark, KR; Gibbons, P; Ghiro, E; Kaufman, S; Larivée, A; Leblanc, M; Leclerc, JP; Lemire, A; Ly, C; Rudolph, J; Schwarz, JB; Srivastava, S; Wang, W; Zhao, L; Braun, MG ACS Med Chem Lett 11: 2389 -2396 (2020)
Shen, L; Zhang, Y; Wang, A; Sieber-McMaster, E; Chen, X; Pelton, P; Xu, JZ; Yang, M; Zhu, P; Zhou, L; Reuman, M; Hu, Z; Russell, R; Gibbs, AC; Ross, H; Demarest, K; Murray, WV; Kuo, GH Bioorg Med Chem 16: 3321 -41 (2008)
Zhu, L; Hu, Y; Wu, W; Dai, L; Duan, X; Yang, Y; Sun, Y; Han, Y; Peng, Y; Kong, F; Luo, H; Yang, L; Xu, H; Guo, M; Zhong, Z; Wang, S US Patent US10829492 (2020)
Zigmond, E; Ben Ya'acov, A; Lee, H; Lichtenstein, Y; Shalev, Z; Smith, Y; Zolotarov, L; Ziv, E; Kalman, R; Le, HV; Lu, H; Silverman, RB; Ilan, Y ACS Med Chem Lett 6: 840 -4 (2015)
Lücking, U; Böhnke, N; Scholz, A; Lienau, P; Siemeister, G; Bömer, U; Kosemund, D; Bohlmann, R; Zorn, L US Patent US9670161 (2017)
ChEMBL_71703 (CHEMBL680917) Inhibition of N-acetyl-L-aspartyl-[3H]L-glutamate binding to glutamate carboxypeptidase II (GCP II)
ChEBML_70193 Compound was evaluated for its ability to inhibit Glutamate carboxypeptidase-II using N-acetyl-L-aspartyl-[3H]L-glutamate as substrate
ChEMBL_71705 (CHEMBL680919) In vitro inhibitory activity against glutamate carboxypeptidase II (GCP II) using N-acetyl-L-aspartyl-[3H]L-glutamate as a substrate
ChEMBL_1291203 (CHEMBL3116809) Inhibition of human recombinant GCP2 using N-acetyl-L-aspartyl[3H]-L-glutamate as substrate
ChEMBL_1924289 (CHEMBL4427245) Negative allosteric modulation of human recombinant mGluR5 expressed in HEK293 cells assessed as L-glutamate-induced intracellular calcium mobilization incubated for 20 mins before L-glutamate addition
ChEMBL_558148 (CHEMBL959077) Inhibition of Enterococcus faecalis murI assessed as effect on conversion of D-glutamate to L-glutamate at pH 8.0 by HPLC
ChEMBL_851405 (CHEMBL2156338) Inhibition of human recombinant GCP2 using N-acetyl-L-aspartyl-[3H]-L-glutamate as substrate by microplate assay
ChEMBL_1627458 (CHEMBL3869979) Positive allosteric modulation activity at human mGluR5A expressed in HEK293(ZF) cells co-expressing rat glutamate-aspartate transporter assessed as increase in L-glutamate-induced Ca2+ flux preincubated for 60 mins followed by L-glutamate addition measured for 100 sec by calcium-4 dye based FLIPR assay
ChEMBL_212282 (CHEMBL819149) In vitro inhibitory activity against Staphylococcus aureus UDP-N-acetylmuramoyl-L-alanyl-D-glutamate synthetase
ChEMBL_451962 (CHEMBL901120) Blockade of L-glutamate/glycine-activated rat NR1/NR2A NMDA receptor expressed in Xenopus oocytes
ChEMBL_1453676 (CHEMBL3363782) Inhibition of human recombinant N-terminal Avi-tagged glutamate carboxypeptidase 2 extracellular domain (44 to 750 amino acids) using pteroyl-di-L-glutamate substrate by HPLC method
ChEMBL_1831187 (CHEMBL4331195) Inhibition of xCT-mediated cystein/glutamate transporter (unknown origin) assessed as reduction in L-[14C]cyctein uptake
ChEMBL_1801543 (CHEMBL4273835) Inhibition of recombinant rat Gi coupled mGlu2 receptor expressed in CHO cells assessed as suppression of L-glutamate-induced decrease in cAMP level pretreated for 1 hr followed by L-glutamate/forskolin addition and measured after 30 mins by FRET assay
ChEMBL_430991 (CHEMBL916419) Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL_430992 (CHEMBL916420) Antagonist activity at human mGluR5 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL_432827 (CHEMBL914095) Activity at human recombinant mGluR5 expressed in L(tk-) cells assessed as inhibition of glutamate-induced calcium release
ChEBML_71704 Inhibition of Glutamate carboxypeptidase II
ChEBML_89232 Binding affinity against Ionotropic glutamate receptor using ACPD sensitive [3H]- glutamate displacement from rat forebrain preparations
ChEBML_219021 Compound was tested in vitro for binding affinity against mGluR4a metabotropic glutamate receptor, using [3H]L-AP4 as the radioligand.
ChEMBL_2371116 Inhibition of human EAAT2 transfected in MDCK cells assessed as reduction in L-[3H]glutamate uptake measured upto 30 mins
ChEMBL_72848 (CHEMBL680873) Potentiation of responses mediated by 100 uM L-glutamate in transfected HEK293 cells expressing human homomeric iGluR4 flip receptors.
ChEMBL_2281818 Inhibition of Helicobacter pylori Glutamate racemase
ChEMBL_71700 (CHEMBL680914) Binding affinity against Glutamate Racemase
ChEMBL_89232 (CHEMBL699724) Binding affinity against Ionotropic glutamate receptor using ACPD sensitive [3H]- glutamate displacement from rat forebrain preparations
ChEBML_1580973 Inhibition of human BCATm (28 to 392 residues) using L-Leucine and alpha-ketogluterate as substrate assessed as L-glutamate production after 10 mins by Amplex red dye based L-GOx and HRP enzyme coupled assay
ChEMBL_2262434 (CHEMBL5217445) Inhibition of human GGT1 expressed in Pichia pastoris assessed as inhibition of GSH hydrolysis measured by L-glutamate release assay
ChEMBL_480059 (CHEMBL933581) Inhibition of NR1/NR2B receptor expressed in xenopus oocytes assessed as effect on L-glutamate and glycine-induced current response
ChEMBL_480061 (CHEMBL933583) Activity at NR1/NR2A receptor expressed in xenopus oocytes assessed as effect on L-glutamate and glycine-induced current response
ChEMBL_480063 (CHEMBL933585) Inhibition of NR1/NR2A receptor expressed in xenopus oocytes assessed as effect on L-glutamate and glycine-induced current response
ChEMBL_1580973 (CHEMBL3812805) Inhibition of human BCATm (28 to 392 residues) using L-Leucine and alpha-ketogluterate as substrate assessed as L-glutamate production after 10 mins by Amplex red dye based L-GOx and HRP enzyme coupled assay
ChEMBL_106031 (CHEMBL718203) Ability to displace [3H]LY-341,495 at glutamate-site on Metabotropic glutamate receptor 2; No significant displacement
ChEMBL_312889 (CHEMBL826437) Antagonistic activity against Metabotropic glutamate receptor 5 in [Ca2+] flux assay using glutamate (10 uM) as agonist
ChEMBL_312890 (CHEMBL826438) Antagonistic activity against Metabotropic glutamate receptor 5 in [Ca2+] flux assay using glutamate (10 uM) as agonist
ChEMBL_1972756 (CHEMBL4605574) Inhibition of NLRP3 inflammasome activation in LPS-primed human THP1 cells assessed as reduction in TNF alpha level preincubated for 1 hr followed by addition of monosodium urate crystals further incubated for 16 hrs and measured post monosodium urate crystals addition 1 hr by ELISA method
ChEMBL_1578233 (CHEMBL3807497) Positive allosteric modulation of human mGlu5A receptor expressed in HEK293 cells coexpressing rat glutamate-aspartate transporter assessed as potentiation of L-glutamate-induced Ca2+ signal incubated for 60 mins by calcium 4 dye based FLIPR assay
ChEMBL_440414 (CHEMBL890728) Agonist activity at rat recombinant NMDA NR1 receptor expressed in xenopus laevis oocyte assessed as inhibition of L-glutamate-stimulated current
ChEMBL_607278 (CHEMBL1072820) Competitive inhibition of [3H]L-glutamate uptake at amino acid transport system xc- in human SNB19 cells by liquid scintillation counting
ChEMBL_607279 (CHEMBL1072821) Inhibition of amino acid transport system xc- in human SNB19 cells assessed as [3H]L-glutamate uptake by liquid scintillation counting
ChEMBL_698079 (CHEMBL1645999) Antagonist activity at rat mGluR5 expressed in HEK293 cells assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR assay
ChEMBL_927332 (CHEMBL3069533) Non-competitive inhibition of Zea mays cv. Jeff( maize) leaf glutamine synthetase using L-glutamate as substrate Lineweaver-Burk plot analysis
ChEMBL_943155 (CHEMBL2345731) Antagonist activity at human mGluR5 expressed in HEK293 cells assessed as inhibition of L-glutamate-induced calcium mobilization by FDSS6000 assay
ChEMBL_973445 (CHEMBL2410484) Negative allosteric modulation of human mGluR1 expressed in CHO cells assessed as inhibition of L-glutamate-induced intracellular cAMP accumulation treated 5 mins before L-quisqualate addition by FLIPR assay
ChEBML_105897 Effective concentration against metabotropic glutamate receptor 2
ChEBML_106692 Effective concentration against Metabotropic glutamate receptor 4
ChEMBL_104283 (CHEMBL711718) Effect on Metabotropic glutamate receptor 5
ChEMBL_104459 (CHEMBL712802) Effect on Metabotropic glutamate receptor 6
ChEMBL_104482 (CHEMBL712463) Effect on Metabotropic glutamate receptor 7
ChEMBL_105564 (CHEMBL711160) Binding affinity towards Glutamate (rPCP) receptor
ChEMBL_105720 (CHEMBL719087) Effect on Metabotropic glutamate receptor 1
ChEMBL_106196 (CHEMBL884501) Effect on Metabotropic glutamate receptor 2
ChEMBL_106390 (CHEMBL717245) Effect on Metabotropic glutamate receptor 3
ChEMBL_106691 (CHEMBL714672) Effect on Metabotropic glutamate receptor 4
ChEMBL_475324 (CHEMBL924551) Inhibition of Helicobacter pylori glutamate racemase
ChEMBL_902833 (CHEMBL3062127) Inhibition of Streptococcus pneumoniae glutamate racemase
ChEBML_218860 Compound was tested in vitro for binding affinity against mGluR1a metabotropic glutamate receptor, using [3H]glutamate as the radioligand.
ChEMBL_2465808 Positive allosteric modulation of EAAT2 in Sprague-Dawley rat microglial cells assessed as increase in glutamate uptake preincubated for 10 mins followed by 3-H-L-glutamate addition and measured after 10 mins by microplate scintillation counter analysis
ChEMBL_2465823 Negative allosteric modulation of EAAT2 in Sprague-Dawley rat microglial cells assessed as decrease in glutamate uptake preincubated for 10 mins followed by 3-H-L-glutamate addition and measured after 10 mins by microplate scintillation counter analysis
ChEMBL_1569844 (CHEMBL3788049) Negative allosteric modulation activity at recombinant human mGluR1a expressed in CHO cells assessed as inhibition of L-glutamate-induced intracellular Ca2+ mobilization
ChEMBL_1569845 (CHEMBL3788050) Negative allosteric modulation activity at recombinant human mGluR5a expressed in CHO cells assessed as inhibition of L-glutamate-induced intracellular Ca2+ mobilization
ChEMBL_460668 (CHEMBL927734) Antagonist activity at human mGluR5 expressed in CHO cells assessed as L-glutamate induced potentiation of intracellular calcium level by FLIPR assay
ChEMBL_571445 (CHEMBL1032756) Agonist activity at human mGluR5 transiently transfected in BHK cells assessed as potentiation of L-glutamate-induced calcium flux by FLIPR assay
ChEMBL_598101 (CHEMBL1038283) Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL_598102 (CHEMBL1038284) Antagonist activity at human mGluR5 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL_598186 (CHEMBL1045180) Antagonist activity at human mGluR2 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL_598187 (CHEMBL1045181) Antagonist activity at human mGluR8 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL_598188 (CHEMBL1045182) Antagonist activity at rat mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL_748641 (CHEMBL1780494) Negative allosteric modulation of human mGluR5 expressed in HEK293 cells assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR assay
ChEMBL_748643 (CHEMBL1780496) Positive allosteric modulation of human mGluR5 expressed in HEK293 cells assessed as increase of L-glutamate-induced calcium mobilization by FLIPR assay
ChEMBL_851506 (CHEMBL2156622) Antagonist activity at human mGluR5a expressed in mouse L(tk-) cells assessed as inhibition of glutamate-induced Ca2+ influx by FLIPR assay
ChEMBL_105563 (CHEMBL711159) Compound was tested for its ability to displace metabotropic glutamate binding to rat brain membranes using [3H]glutamate radioligand.
ChEMBL_2262830 (CHEMBL5217841) Inhibition of NLRP3 inflammasome activation in LPS-stimulated human whole blood assessed as reduction in ILbeta secretion in presence of monosodium urate
ChEMBL_105884 (CHEMBL717934) Binding affinity towards metabotropic glutamate receptor mGluR1
ChEMBL_105898 (CHEMBL717759) Effective concentration against Metabotropic glutamate receptor 2
ChEMBL_106056 (CHEMBL718222) Binding affinity at Metabotropic glutamate receptor 2
ChEMBL_106687 (CHEMBL714668) Binding affinity at Metabotropic glutamate receptor 4
ChEMBL_106692 (CHEMBL714821) Effective concentration against Metabotropic glutamate receptor 4
ChEMBL_106711 (CHEMBL715717) Binding affinity towards metabotropic glutamate receptor mGluR4a
ChEMBL_304142 (CHEMBL840258) Binding affinity against metabotropic glutamate receptor 2
ChEMBL_304180 (CHEMBL829176) Effective concentration against Metabotropic glutamate receptor 4
ChEMBL_305883 (CHEMBL874546) Inhibitory concentration against human metabotropic glutamate receptor
ChEMBL_605563 (CHEMBL1067317) Inhibition of human cloned glutamate carboxypeptidase 2
ChEMBL_71706 (CHEMBL680920) Inhibitory concentration required against Glutamate carboxypeptidase II
ChEMBL_71836 (CHEMBL683667) Inhibition constant against mammalian glutamate dehydrogenase (GDH)
ChEMBL_842443 (CHEMBL2092116) Inhibition of Helicobacter pylori J99 glutamate racemase
ChEMBL_2371103 Inhibition of human EAAT3 transfected in African green monkey COS-1 cells assessed as inhibition of [3H]L-glutamate uptake by measuring inhibition constant
ChEMBL_2371107 Inhibition of human EAAT2 transfected in African green monkey COS-1 cells assessed as inhibition of [3H]L-glutamate uptake by measuring inhibition constant
ChEMBL_2371108 Inhibition of human EAAT1 transfected in African green monkey COS-1 cells assessed as inhibition of [3H]L-glutamate uptake by measuring inhibition constant
ChEMBL_2465784 Negative allosteric modulation of EAAT1 (unknown origin) transfected in African green monkey COS-7 cells assessed as increase in glutamate uptake preincubated for 10 mins followed by 3-H-L-glutamate addition and measured after 10 mins by scintillation counter analysis
ChEMBL_2465785 Positive allosteric modulation of EAAT3 (unknown origin) transfected in African green monkey COS-7 cells assessed as increase in glutamate uptake preincubated for 10 mins followed by 3-H-L-glutamate addition and measured after 10 mins by scintillation counter analysis
ChEMBL_2465786 Positive allosteric modulation of EAAT1 (unknown origin) transfected in African green monkey COS-7 cells assessed as increase in glutamate uptake preincubated for 10 mins followed by 3-H-L-glutamate addition and measured after 10 mins by scintillation counter analysis
ChEMBL_2465787 Positive allosteric modulation of EAAT2 (unknown origin) transfected in African green monkey COS-7 cells assessed as increase in glutamate uptake preincubated for 10 mins followed by 3-H-L-glutamate addition and measured after 10 mins by scintillation counter analysis
ChEMBL_2465788 Negative allosteric modulation of EAAT2 (unknown origin) transfected in African green monkey COS-7 cells assessed as decrease in glutamate uptake preincubated for 10 mins followed by 3-H-L-glutamate addition and measured after 10 mins by scintillation counter analysis
ChEMBL_2465789 Negative allosteric modulation of EAAT3 (unknown origin) transfected in African green monkey COS-7 cells assessed as increase in glutamate uptake preincubated for 10 mins followed by 3-H-L-glutamate addition and measured after 10 mins by scintillation counter analysis
ChEMBL_686639 (CHEMBL1292492) Antagonist activity at human recombinant NR1-1a/NR2B receptor expressed in mouse L(tk-) cells assessed as inhibition of (S)-glutamate/glycine-stimulated excitotoxicity treated 30 mins before (S)-glutamate/glycine challenge measured after 4 hrs by LDH release assay
ChEBML_105879 Effect of compound on Metabotropic glutamate receptor 1 expressed in HEK 293 cells was determined by measuring IP production relative to glutamate
ChEMBL_140617 (CHEMBL752265) Inhibition of N-methyl-D-aspartate glutamate receptor-evoked increase of intracellular Ca+ in cells expressing NMDA glutamate receptor 1/2B
ChEMBL_1837822 (CHEMBL4337955) Inhibition of human GLS1 assessed as reduction in glutamate production in presence of NADPH-dependent glutamate dehydrogenase by coupled biochemical assay
ChEMBL_1497035 (CHEMBL3579845) Inhibition of antiTEV-tagged GCP2 extracellular portion (aa 44-750) (unknown origin) using folyl-di-L-glutamate as substrate by HPLC-based enzymatic assay
ChEMBL_480064 (CHEMBL929340) Inhibition of N-terminal domain truncated NR1/NR2B receptor expressed in xenopus oocytes assessed as effect on L-glutamate and glycine-induced current response
ChEBML_104290 Antagonistic activity against Metabotropic glutamate receptor 5 was determined
ChEBML_104467 Antagonistic activity against Metabotropic glutamate receptor 6 was determined
ChEBML_105728 Antagonistic activity against Metabotropic glutamate receptor 1 was determined
ChEMBL_104277 (CHEMBL711712) Agonist potency against cloned metabotropic glutamate receptor 5
ChEMBL_105893 (CHEMBL717754) Agonistic activity against Human Metabotropic glutamate receptor 2
ChEMBL_106040 (CHEMBL717363) Inhibitory activity against human Metabotropic glutamate receptor 2
ChEMBL_106052 (CHEMBL718218) Antagonist potency against cloned Metabotropic glutamate receptor 2
ChEMBL_106055 (CHEMBL718221) Potency against cloned Metabotropic glutamate receptor 2 agonist
ChEMBL_106370 (CHEMBL718736) Agonistic activity against Human Metabotropic glutamate receptor 3
ChEMBL_106387 (CHEMBL717242) Agonist potency against cloned Metabotropic glutamate receptor 3
ChEMBL_106539 (CHEMBL714800) Agonist potency against cloned Metabotropic glutamate receptor 3
ChEMBL_305830 (CHEMBL829572) Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL_305855 (CHEMBL832715) Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL_71834 (CHEMBL683665) Apparent inhibition constant against mammalian glutamate dehydrogenase (GDH)
ChEMBL_803066 (CHEMBL1954372) Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL_803067 (CHEMBL1954373) Antagonist activity at human metabotropic glutamate receptor 5
ChEMBL_803068 (CHEMBL1954374) Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL_105879 (CHEMBL717930) Effect of compound on Metabotropic glutamate receptor 1 expressed in HEK 293 cells was determined by measuring IP production relative to glutamate
ChEMBL_106397 (CHEMBL717252) Compound was evaluated for the inhibition of binding of [3H]glutamate against rat recombinant Metabotropic glutamate receptor 3 expressed in HEK293 cells
ChEMBL_1579150 (CHEMBL3811870) Inhibition of GLS1 in human PC3 cells assessed as cellular glutamate depletion levels after 6 hrs by Glutamate Oxidase/ AmplexRed coupled assay
ChEMBL_546002 (CHEMBL1027706) Positive allosteric modulator activity at rat mGlu5 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced response relative to glutamate
ChEMBL_1516909 (CHEMBL3618962) Inhibition of human cloned BCATm expressed in Escherichia coli BL21 DE3 assessed as L-glutamate production from alpha-ketoglutarate after 10 mins by fluorescent assay
ChEMBL_1526364 (CHEMBL3637425) Antagonist activity at rat mGluR5 expressed in CHO cells assessed as inhibition of L-glutamate-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL_1623092 (CHEMBL3865444) Positive allosteric modulation of mGlu5 receptor (unknown origin) assessed as increase in L-glutamate-induced calcium release after 60 mins by cell based FLIPR assay
ChEMBL_1934148 (CHEMBL4479800) Negative allosteric modulation of human mGluR5A transfected in HEK293 cells assessed as inhibition of L-glutamate-induced calcium release after 10 mins by FLIPR assay
ChEMBL_969986 (CHEMBL2405252) Negative allosteric modulation of human mGlu5 receptor expressed in HEK293 cells assessed as inhibition of L-glutamate-induced activity after 1 hr by FLIPR assay
ChEMBL_969988 (CHEMBL2405254) Positive allosteric modulation of human mGlu5 receptor expressed in HEK293 cells assessed as potentiation of L-glutamate-induced activity after 1 hr by FLIPR assay
ChEMBL_104274 (CHEMBL711709) Tested in vitro against human recombinant Metabotropic glutamate receptor 5 stably expressed in LtK cells by [Ca2+] flux assay using glutamate as antagonist
ChEMBL_106032 (CHEMBL718204) Antagonistic activity against stimulation of GTP (gamma) 35 S binding by glutamate in membranes from CHO cells expressing human Metabotropic glutamate receptor 2
ChEMBL_106053 (CHEMBL718219) Antagonistic activity against stimulation of GTP (gamma) 35 S binding by glutamate in membranes from CHO cells expressing human Metabotropic glutamate receptor 2
ChEMBL_1704159 (CHEMBL4055392) Antagonist activity at open state of GluA1 (unknown origin) assessed as reduction in glutamate-induced current response in presence of 2 mM glutamate
ChEMBL_1704160 (CHEMBL4055393) Antagonist activity at closed state of GluA3 (unknown origin) assessed as reduction in glutamate-induced current response in presence of 100 uM glutamate
ChEMBL_1704161 (CHEMBL4055394) Antagonist activity at open state of GluA3 (unknown origin) assessed as reduction in glutamate-induced current response in presence of 3 mM glutamate
ChEMBL_1704162 (CHEMBL4055395) Antagonist activity at closed state of GluA4 (unknown origin) assessed as reduction in glutamate-induced current response in presence of 100 uM glutamate
ChEMBL_1704163 (CHEMBL4055396) Antagonist activity at open state of GluA4 (unknown origin) assessed as reduction in glutamate-induced current response in presence of 3 mM glutamate
ChEMBL_303758 (CHEMBL829801) Inhibitory constant against (S)-glutamate and glycine evoked currents mediated by N-methyl-D-aspartate glutamate receptor NR1a/NR2A expressed in Xenopus oocytes
ChEMBL_303759 (CHEMBL828982) Inhibitory constant against (S)-glutamate and glycine evoked currents mediated by N-methyl-D-aspartate glutamate receptor NR1a/NR2B expressed in Xenopus oocytes
ChEMBL_303760 (CHEMBL828983) Inhibitory constant against (S)-glutamate and glycine evoked currents mediated by N-methyl-D-aspartate glutamate receptor NR1a/NR2C expressed in Xenopus oocytes
ChEMBL_794160 (CHEMBL1931945) Inhibition of glutamate carboxypeptidase 2 in human LNCAP cells assessed as glutamate formation using NAAG as substrate after 60 mins by fluorometric analysis
ChEMBL_140848 (CHEMBL752332) In vitro ability to displace [3H]L-689,560 binding to glycine site on the N-methyl-D-aspartate (NMDA) glutamate receptor 1 from rat cortical membranes
ChEMBL_1934139 (CHEMBL4479791) Positive allosteric modulation of human mGluR5A transfected in HEK293 cells assessed as potentiation of L-glutamate-induced calcium release incubated for 10 mins by FLIPR assay
ChEMBL_598189 (CHEMBL1045183) Antagonist activity at human mGluR1 receptor quisqualic acid binding site expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL_772170 (CHEMBL1838227) Inhibition of xc-cystine-glutamate antiporter-mediated cystine uptake in human U87 cells using L-[14C]cystine as substrate after 15 mins by liquid scintillation counting
ChEBML_104293 Tested for the agonistic activity against Metabotropic glutamate receptor 5
ChEBML_104466 Tested for the agonistic activity against Metabotropic glutamate receptor 6
ChEBML_104628 Antagonistic activity against metabotropic glutamate receptor 1 (mGluR1) was evaluated
ChEBML_104631 Antagonistic activity against metabotropic glutamate receptor 3 (mGluR3) was evaluated
ChEBML_104633 Antagonistic activity against metabotropic glutamate receptor 4 (mGluR4) was evaluated
ChEBML_104635 Antagonistic activity against metabotropic glutamate receptor 5 (mGluR5) was evaluated
ChEBML_104636 Antagonistic activity against metabotropic glutamate receptor 7 (mGluR7) was evaluated
ChEBML_104637 Antagonistic activity against metabotropic glutamate receptor 8 (mGluR8) was evaluated
ChEBML_105723 Tested for the agonistic activity against Metabotropic glutamate receptor 1
ChEBML_71835 In vitro inhibitory activity against bovine liver glutamate dehydrogenase (GDH)
ChEBML_71837 Inhibition of bovine glutamate dehydrogenase (GDH) enzyme by competitive inhibition
ChEBML_71843 Inhibition towards glutamate racemase was determined and expressed as KI
ChEMBL_105708 (CHEMBL719076) Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL_106050 (CHEMBL718216) Agonist potency against cloned Metabotropic glutamate receptor 2 agonist
ChEMBL_106051 (CHEMBL718217) Agonist potency against cloned Metabotropic glutamate receptor 2 partial
ChEMBL_106054 (CHEMBL718220) Partial agonist potency against cloned Metabotropic glutamate receptor 2
ChEMBL_106207 (CHEMBL872681) Antagonistic activity against Metabotropic glutamate receptor 2 was determined
ChEMBL_106227 (CHEMBL715054) Binding affinity towards metabotropic glutamate receptor 2 was determined
ChEMBL_106365 (CHEMBL714443) Binding affinity towards metabotropic glutamate receptor 2 was determined
ChEMBL_106371 (CHEMBL718737) Effective concentration against human cloned Metabotropic glutamate receptor 3
ChEMBL_106538 (CHEMBL714799) Binding affinity towards Metabotropic glutamate receptor 3 was determined
ChEMBL_106541 (CHEMBL714802) Binding affinity towards metabotropic glutamate receptor 3 was determined
ChEMBL_304169 (CHEMBL830007) Effective concentration against metabotropic glutamate receptor 5 of rat
ChEMBL_304192 (CHEMBL829187) Effective concentration against D309A mutant Metabotropic glutamate receptor 4
ChEMBL_90128 (CHEMBL700581) Potency on Ionotropic glutamate receptor AMPA in hippocampal neurons
ChEBML_104491 Tested for agonist activity in non-neuronal cells (RGT) expressing human Metabotropic glutamate receptor 8 by measuring L-AP4 (0.3 uM of forskolin) (15 uM)-stimulated cAMP formation
ChEMBL_104275 (CHEMBL711710) Tested in vitro binding affinity for displacement of [3H]M-MPEP from membrane of L(-tk) cells expressing the Metabotropic glutamate receptor 5, activity expressed as IC50
ChEMBL_1474583 (CHEMBL3423872) Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay
ChEMBL_1474584 (CHEMBL3423873) Antagonist activity at human mGluR5 expressed in human embryonic kidney cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay
ChEMBL_1538273 (CHEMBL3737385) Positive allosteric modification of human recombinant mGlu5 receptor expressed in U2OS cells assessed as potentiation of glutamate-induced Ca2+ flux in presence of EC20 glutamate
ChEMBL_1704158 (CHEMBL4055391) Antagonist activity at closed state of GluA1 (unknown origin) assessed as reduction in glutamate-induced current response in presence of 40 to 50 uM glutamate
ChEMBL_2018950 (CHEMBL4672528) Inhibition of human kidney glutaminase assessed as reduction in glutamate production in presence of NADPH-dependent glutamate dehydrogenase preincubated 60 mins by coupled biochemical assay
ChEMBL_501594 (CHEMBL987723) Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEBML_104460 Effective concentration required for agonistic activity at Metabotropic glutamate receptor 6
ChEBML_106391 Effective concentration required for agonistic activity at Metabotropic glutamate receptor 3
ChEMBL_104293 (CHEMBL709909) Tested for the agonistic activity against Metabotropic glutamate receptor 5
ChEMBL_104311 (CHEMBL718130) Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
ChEMBL_104479 (CHEMBL712461) Agonist potency against cloned Metabotropic glutamate receptor 7 (mGluR-7).
ChEMBL_104492 (CHEMBL712473) Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).
ChEMBL_104629 (CHEMBL715576) Antagonistic activity against metabotropic glutamate receptor 2 (mGluR2) was evaluated
ChEMBL_106049 (CHEMBL718215) Agonist potency against cloned Metabotropic glutamate receptor 2 (mGluR-2).
ChEMBL_106202 (CHEMBL713192) Tested for the agonistic activity against Metabotropic glutamate receptor 2
ChEMBL_106213 (CHEMBL713201) Tested for the agonistic activity against Metabotropic glutamate receptor 2
ChEMBL_106383 (CHEMBL717238) Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL_106386 (CHEMBL717241) Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL_225980 (CHEMBL854763) Ability to inhibit the GTP/glutamate-induced polymerization of tubulin
ChEMBL_303286 (CHEMBL828279) Inhibition of [3H]-KA binding to iontropic glutamate receptor 5
ChEMBL_303287 (CHEMBL828280) Inhibition of [3H]KA binding to iontropic glutamate receptor 6
ChEMBL_306372 (CHEMBL828343) Inhibitory concentration against human metabotropic glutamate receptor 1 transmembrane domain
ChEMBL_71843 (CHEMBL681701) Inhibition towards glutamate racemase was determined and expressed as KI
ChEMBL_1368981 Positive allosteric modulator activity at rat mGlu1 receptor expressed in HEK293 cells assessed as glutamate-induced calcium mobilization treated 140s prior to glutamate challenge by fluorescence assay
ChEMBL_523080 (CHEMBL1004110) Antagonist activity at rat mGluR5 expressed in HEK293A cells assessed as glutamate-induced calcium flux preincubated for 140 sec before glutamate challenge by calcium fluorescence assay
ChEMBL_911964 (CHEMBL3058795) Inhibition of Setaria cervi glutamate cysteine ligase using glutamate as substrate incubated for 10 min prior to substrate addition measured for 5 min by spectrophotometric analysis
ChEMBL_1552623 (CHEMBL3762562) Antagonist activity against recombinant rat GluA2(Q)i expressed in xenopus oocytes assessed as inhibition of L-glutamate-induced intracellular calcium levels by two electrode voltage clamp method
ChEMBL_2235657 (CHEMBL5149429) Positive allosteric modulation of mGlu2 receptor (unknown origin) expressed in human Flp-In-T-REx-293 cells in presence of L-glutamate by luciferase based GloSensor cAMP Assay
ChEMBL_2283603 Positive allosteric modulator activity at GluN2A NMDA receptor (unknown origin) expressed in CHO cells co-expressing GluN1a in the presence of L-glutamate and glycine by Ca2+ influx assay
ChEMBL_2283608 Positive allosteric modulator activity at GluN2B NMDA receptor (unknown origin) expressed in CHO cells co-expressing GluN1a in the presence of L-glutamate and glycine by Ca2+ influx assay
ChEMBL_2283610 Positive allosteric modulator activity at GluN2C NMDA receptor (unknown origin) expressed in CHO cells co-expressing GluN1a in the presence of L-glutamate and glycine by Ca2+ influx assay
ChEMBL_2283612 Positive allosteric modulator activity at GluN2D NMDA receptor (unknown origin) expressed in CHO cells co-expressing GluN1a in the presence of L-glutamate and glycine by Ca2+ influx assay
ChEMBL_858345 (CHEMBL2168560) Negative allosteric modulation of human recombinant mGluR5 expressed in HEK293 cells expressing GLAST assessed as inhibition of glutamate-stimulated IP accumulation incubated for 10 mins prior to glutamate challenge measured 30 mins post glutamate challenge by scintillation counter in presence of [3H]myo-inositol
ChEBML_106557 Tested for agonist activity in non-neuronal cells (RGT) expressing human Metabotropic glutamate receptor 4 by measuring L-AP4 (3 uM) induced inhibition of forskolin (15 uM)-stimulated cAMP formation
ChEMBL_2116197 (CHEMBL4825138) Inhibition of human GluN1-1a/NR2A receptor expressed in transgenic mouse fibroblast cells assessed as inhibition of L-glutamate-induced excitotoxicity by measuring LDH activity by cell based assay
ChEMBL_2116199 (CHEMBL4825140) Inhibition of human GluN1-1a/NR2B receptor expressed in transgenic mouse fibroblast cells assessed as inhibition of L-glutamate-induced excitotoxicity by measuring LDH activity by cell based assay
ChEBML_141033 Inhibitory activity against N-methyl-D-aspartate glutamate receptor 2A in rat
ChEBML_141161 Inhibitory activity against N-methyl-D-aspartate glutamate receptor 2B in rat
ChEBML_72010 Compound was evaluated for the binding affinity against glutamate vesicular transport (GVT)
ChEMBL_104281 (CHEMBL711716) Concentration for half maximal activation of metabotropic glutamate mGluR5a in rat
ChEMBL_104282 (CHEMBL711717) Concentration for half maximal activation of metabotropic glutamate mGluR5b in rat
ChEMBL_104301 (CHEMBL709916) Compound was tested for the inhibition of Metabotropic glutamate receptor 5
ChEMBL_104306 (CHEMBL880764) Compound was tested for the inhibition of Metabotropic glutamate receptor 5
ChEMBL_104458 (CHEMBL712801) Concentration for half maximal activation of metabotropic glutamate mGluR6 in rat
ChEMBL_104471 (CHEMBL712388) Compound was tested for the inhibition of Metabotropic glutamate receptor 6
ChEMBL_104473 (CHEMBL712390) Compound was tested for the inhibition of Metabotropic glutamate receptor 6
ChEMBL_104478 (CHEMBL712460) Concentration for half maximal activation of metabotropic glutamate mGluR7 in human
ChEMBL_104481 (CHEMBL879748) Concentration for half maximal activation of metabotropic glutamate mGluR7 in rat
ChEMBL_104621 (CHEMBL715569) Concentration for half maximal activation of metabotropic glutamate mGluR8 in mouse
ChEMBL_105571 (CHEMBL709768) Concentration for half maximal activation of metabotropic glutamate mGluR1b in human
ChEMBL_105576 (CHEMBL709773) Concentration for half maximal activation of metabotropic glutamate mGluR1b in human
ChEMBL_105717 (CHEMBL719084) Concentration for half maximal activation of metabotropic glutamate mGluR1a in rat
ChEMBL_105718 (CHEMBL719085) Concentration for half maximal activation of metabotropic glutamate mGluR1b in rat
ChEMBL_105719 (CHEMBL719086) Concentration for half maximal activation of metabotropic glutamate mGluR1c in rat
ChEMBL_105866 (CHEMBL717334) Compound was tested for the inhibition of Metabotropic glutamate receptor 1
ChEMBL_105876 (CHEMBL717927) Compound was tested for the inhibition of Metabotropic glutamate receptor 1
ChEMBL_105881 (CHEMBL717932) Tested for in vitro antagonistic activity against Metabotropic glutamate receptor 1
ChEMBL_105883 (CHEMBL877741) Antagonist activity of compound at Metabotropic glutamate receptor 1 was determined
ChEMBL_105896 (CHEMBL717757) Concentration for half maximal activation of metabotropic glutamate mGluR2 in human
ChEMBL_106064 (CHEMBL718229) Concentration for half maximal activation of metabotropic glutamate mGluR2 in rat
ChEMBL_106197 (CHEMBL714614) Effective concentration required for agonistic activity at Metabotropic glutamate receptor 2
ChEMBL_106209 (CHEMBL713198) Inhibitory concentration required for antagonistic activity at Metabotropic glutamate receptor 2
ChEMBL_106389 (CHEMBL717244) Concentration for half maximal activation of metabotropic glutamate mGluR3 in rat
ChEMBL_106391 (CHEMBL717246) Effective concentration required for agonistic activity at Metabotropic glutamate receptor 3
ChEMBL_106552 (CHEMBL884506) Concentration for half maximal activation of metabotropic glutamate mGluR4a in human
ChEMBL_106560 (CHEMBL716502) Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)
ChEMBL_106690 (CHEMBL714671) Concentration for half maximal activation of metabotropic glutamate mGluR4a in rat
ChEMBL_106701 (CHEMBL714003) Compound was tested for the inhibition of Metabotropic glutamate receptor 4
ChEMBL_106709 (CHEMBL714010) Compound was tested for the inhibition of Metabotropic glutamate receptor 4
ChEMBL_106717 (CHEMBL715723) Concentration for half maximal activation of metabotropic glutamate mGluR5a in human
ChEMBL_140703 (CHEMBL751722) Compound with the N-methyl-D-aspartate glutamate receptor blocking activity
ChEMBL_141020 (CHEMBL747509) Antagonistic activity against N-methyl-D-aspartate glutamate receptor 1/2A.
ChEMBL_141026 (CHEMBL748097) Antagonistic activity against N-methyl-D-aspartate glutamate receptor 1/2B.
ChEMBL_141029 (CHEMBL749383) Antagonistic activity against N-methyl-D-aspartate glutamate receptor 1/2C.
ChEMBL_176822 (CHEMBL780515) Inhibitory effect against veratridine-induced glutamate release from rat brain slices
ChEMBL_213567 (CHEMBL816124) Compound was evaluated for the inhibition of Vesicular glutamate transporter (VGLUT)
ChEMBL_303149 (CHEMBL829123) Binding affinity for kainate Glutamate receptor GluR5 expressed in Sf9 cells
ChEMBL_303150 (CHEMBL829124) Binding affinity for kainate Glutamate receptor GluR6 expressed in Sf9 cells
ChEMBL_303327 (CHEMBL840052) Inhibition of [3H]AMPA binding to human Ionotropic glutamate receptor 2
ChEMBL_312509 (CHEMBL833257) Inhibitory concentration towards human glutamate receptor 5 in calcium flux assay
ChEMBL_335664 (CHEMBL860564) Inhibition of glutamate-induced calcium influx in human mGluR5d by FLIPR
ChEMBL_348518 (CHEMBL865700) Inhibition of glutamate-induced calcium influx in human mGluR5d by FLIPR
ChEMBL_445397 (CHEMBL895688) Agonist activity at GluR4 expressed in Xenopus oocyte cells S-Glutamate
ChEMBL_88653 (CHEMBL702868) Potency on Ionotropic glutamate receptor kainate in dorsal root ganglion cells
ChEMBL_90132 (CHEMBL700585) Ability to inhibit [3H]AMPA binding to Ionotropic glutamate receptor AMPA
ChEMBL_90287 (CHEMBL697506) Binding affinity towards Ionotropic glutamate receptor AMPA 2 from rat brain
ChEMBL_90295 (CHEMBL698775) Binding affinity towards Ionotropic glutamate receptor AMPA 3 from rat brain
ChEMBL_90456 (CHEMBL699991) Inhibition of [3H]kainate binding at ionotropic glutamate receptor kainate 2
ChEMBL_141027 (CHEMBL748098) Antagonistic activity for suppression of membrane current response elicited by fixed concentration of glycine and glutamate in Xenopus oocyte expressing N-methyl-D-aspartate glutamate receptor 1/2B
ChEMBL_629920 (CHEMBL1108384) Antagonist activity at rat mGluR5 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium flux preincubated for 140 secs before glutamate challenge by calcium fluorescence assay
ChEMBL_1810577 (CHEMBL4310037) Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL_1996229 (CHEMBL4630124) Positive allosteric modulation of recombinant rat GluN1a/GluN2C receptor expressed in Xenopus laevis oocytes assessed as increase in glycine/L-glutamate-induced channel current by two-electrode voltage clamp method
ChEMBL_1996230 (CHEMBL4630125) Positive allosteric modulation of recombinant rat GluN1a/GluN2D receptor expressed in Xenopus laevis oocytes assessed as increase in glycine/L-glutamate-induced channel current by two-electrode voltage clamp method
ChEMBL_927333 (CHEMBL3069534) Inhibition of Zea mays cv. Jeff (maize) leaf glutamine synthetase using L-glutamate as substrate assessed as inorganic phosphate production after 20 min by malachite green assay relative to control
Induced Intracellular Calcium Assay Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR), and CHO cells stably expressing human mGluR1. L-glutamate induced robust calcium responses via human mGluR1 in a concentration-dependent manner and in the low micromolar range.
ChEBML_1695892 Negative allosteric modulation of human recombinant mGluR5 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium mobilization preincubated for 2 mins followed glutamate addition measured by fluorescence assay
ChEMBL_1368986 Positive allosteric modulator activity at rat mGlu8 receptor expressed in HEK293 cells assessed as glutamate-induced GIRK channel-mediated thallium flux treated 140s prior to glutamate challenge by fluorescence analysis
ChEMBL_744536 (CHEMBL1772557) Partial antagonist activity at mGluR5 receptor expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium flux preincubated for 140 secs before glutamate challenge by calcium fluorescence assay
ChEMBL_911963 (CHEMBL3058794) Inhibition of Rattus norvegicus Wistar (rat) rat glutamate cysteine ligase using glutamate as substrate incubated for 10 min prior to substrate addition measured for 5 min by spectrophotometric analysis
ChEBML_55079 Inhibitory activity against dihydrofolate reductase in Lactobacillus casei was determined (glutamate residue 2)
ChEBML_71990 Compound was tested for agonistic activity at Glutamate receptor 5 using HEK293 cells
ChEBML_71992 Compound was tested for agonistic activity at Glutamate receptor 6 using HEK293 cells
ChEMBL_105882 (CHEMBL717933) Antagonist activity of compound at Metabotropic glutamate receptor 1 alpha was determined
ChEMBL_106223 (CHEMBL713618) Compound was tested for the inhibition of metabotropic glutamate receptor 2 (mGluR2).
ChEMBL_106230 (CHEMBL878220) Compound was tested for the inhibition of metabotropic glutamate receptor 2 (mGluR2).
ChEMBL_106537 (CHEMBL714798) Compound was tested for the inhibition of Metabotropic glutamate receptor 3 (mGluR3)
ChEMBL_141033 (CHEMBL749387) Inhibitory activity against N-methyl-D-aspartate glutamate receptor 2A in rat
ChEMBL_141288 (CHEMBL747355) Inhibition of the response to glutamate/glycine in NR1a/NR2B expressing cells
ChEMBL_213568 (CHEMBL816125) Estimated inhibitory conc. against Vesicular glutamate transporter (VGLUT), using Cheng-Prushoff equation
ChEMBL_213569 (CHEMBL874091) Inhibitory conc. against Vesicular glutamate transporter (VGLUT), derived from Lineweaver-Burke analysis
ChEMBL_2206399 (CHEMBL5119107) Activation of human EAAT2 transfected in COS7 cells assessed as glutamate uptake
ChEMBL_2206405 (CHEMBL5119113) Activation of human EAAT2 transfected in Glial cells assessed as glutamate uptake
ChEMBL_2217850 (CHEMBL5130982) Activation of human EAAT2 expressed in COS cells assessed as glutamate uptake
ChEMBL_302234 (CHEMBL828854) Dissociation constant of radiolabeled compound against recombinant human Metabotropic glutamate receptor 8
ChEMBL_303109 (CHEMBL829619) Binding affinity for ionotropic Glutamate receptor AMPA 1 expressed in Sf9 cells
ChEMBL_303110 (CHEMBL829620) Binding affinity for ionotropic Glutamate receptor AMPA 2 expressed in Sf9 cells
ChEMBL_303111 (CHEMBL876377) Binding affinity for ionotropic Glutamate receptor AMPA 3 expressed in Sf9 cells
ChEMBL_303112 (CHEMBL829621) Binding affinity for ionotropic Glutamate receptor AMPA 4 expressed in Sf9 cells
ChEMBL_341810 (CHEMBL865012) Inhibition of glutamate-induced calcium influx in HEK293 cells expressing human GLUK6
ChEMBL_341812 (CHEMBL865014) Inhibition of glutamate-induced calcium influx in HEK293 cells expressing human GLUA1
ChEMBL_341813 (CHEMBL865015) Inhibition of glutamate-induced calcium influx in HEK293 cells expressing human GLUA2
ChEMBL_341814 (CHEMBL865016) Inhibition of glutamate-induced calcium influx in HEK293 cells expressing human GLUA3
ChEMBL_341815 (CHEMBL865017) Inhibition of glutamate-induced calcium influx in HEK293 cells expressing human GLUA4
ChEMBL_90133 (CHEMBL701233) Ability to inhibit [3H]CGS-19,755 binding to Ionotropic glutamate receptor AMPA
ChEMBL_90597 (CHEMBL701553) Ability to bind to Ionotropic glutamate receptor ionotropic kainate 3 was evaluated
ChEMBL_90601 (CHEMBL701557) Ability to bind to Ionotropic glutamate receptor kainate (kainate 2) was evaluated.
ChEMBL_1831188 (CHEMBL4331196) Inhibition of cystine/glutamate antiporter system xc- in human HT1080 cells assessed as reduction in L-[3,3'-14C]-cystine uptake in presence of Na+ free uptake buffer by scintillation counting assay
ChEMBL_1831189 (CHEMBL4331197) Inhibition of cystine/glutamate antiporter system xc- in human Calu1 cells assessed as reduction in L-[3,3'-14C]-cystine uptake in presence of Na+ free uptake buffer by scintillation counting assay
ChEMBL_744538 (CHEMBL1772559) Positive allosteric modulator activity at mGluR5 receptor expressed in HEK293A cells assessed as effect on glutamate-induced calcium flux preincubated for 140 secs before glutamate challenge by calcium fluorescence assay
ChEMBL_744540 (CHEMBL1772561) Negative allosteric modulator activity at mGluR5 receptor expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium flux preincubated for 140 secs before glutamate challenge by calcium fluorescence assay