TTD_Target_ID Target_Name TTD_Drug_ID Drug_Name Drug_Highest_Status Drug_PubchemID Molecular_Formula Molecular_Weight Canonical_SMILES Activity Binder_Type T27137 Metabotropic glutamate receptor 1 D00ENY L-Glutamic Acid Approved 33032 C5H9NO4 147.13 C(CC(=O)O)[C@@H](C(=O)O)N EC50 = 156000 nM Poor binder T27137 Metabotropic glutamate receptor 1 D09YDQ STX-107 Phase 2 9794218 C11H8N2S 200.26 CC1=NC(=CS1)C#CC2=CN=CC=C2 IC50 ~ 100000 nM Poor binder T27137 Metabotropic glutamate receptor 1 D0U5CS LY354740 Discontinued in Phase 2 213056 C8H11NO4 185.18 C1C[C@]([C@H]2[C@@H]1[C@@H]2C(=O)O)(C(=O)O)N Ki ~ 100000 nM Poor binder T27137 Metabotropic glutamate receptor 1 B1KEW7 (1S,2S,3S)-2-[1-Amino-1-carboxy-2-(9H-xanthen-9-yl)-ethyl]-3-propyl-cyclopropanecarboxylic acid Investigative 44329024 C23H25NO5 395.4 CCC[C@@H]1[C@@H]([C@H]1C(CC2C3=CC=CC=C3OC4=CC=CC=C24)(C(=O)O)N)C(=O)O IC50 ~ 100000 nM Poor binder T27137 Metabotropic glutamate receptor 1 B1VT5M Iflwvshrwaivqf-sgihwfkdsa- Investigative 9991661 C12H13NO4 235.24 C1=CC=C(C=C1)[C@H]2[C@H]([C@@H]2C(=O)O)[C@H](C(=O)O)N Ki = 135000 nM Poor binder T27137 Metabotropic glutamate receptor 1 B1X7KZ (1S,2S,3S)-2-[1-Amino-1-carboxy-2-(9H-xanthen-9-yl)-ethyl]-3-hexyl-cyclopropanecarboxylic acid Investigative 44329031 C26H31NO5 437.5 CCCCCC[C@@H]1[C@@H]([C@H]1C(CC2C3=CC=CC=C3OC4=CC=CC=C24)(C(=O)O)N)C(=O)O IC50 = 54900 nM Poor binder T27137 Metabotropic glutamate receptor 1 B2C6GP 5-(4-Chlorophenyl)-1-(cyclohexylmethyl)-6-methyl-1H-pyrazolo[3,4-d]pyrimidin-4(5H)-one Investigative 44442427 C19H21ClN4O 356.8 CC1=NC2=C(C=NN2CC3CCCCC3)C(=O)N1C4=CC=C(C=C4)Cl IC50 ~ 100000 nM Poor binder T27137 Metabotropic glutamate receptor 1 B3BD1R 2-[(1S,2R,3R)-2-Carboxy-3-phenylcyclopropyl]-D-glycine Investigative 10513894 C12H13NO4 235.24 C1=CC=C(C=C1)[C@@H]2[C@@H]([C@@H]2C(=O)O)[C@H](C(=O)O)N IC50 = 140000 nM Poor binder T27137 Metabotropic glutamate receptor 1 B45BXQ (S)-2-Amino-4-(3,5-dioxo-[1,2,4]oxadiazolidin-2-yl)-butyric acid Investigative 11820180 C6H9N3O5 203.15 C(CN1C(=O)NC(=O)O1)[C@@H](C(=O)O)N Ki = 184000 nM Poor binder T27137 Metabotropic glutamate receptor 1 B4E2TO 4-(Amino-carboxy-methyl)-2-hydroxy-5-methyl-benzoic Acid Investigative 10036599 C10H11NO5 225.2 CC1=CC(=C(C=C1C(C(=O)O)N)O)C(=O)O IC50 = 73000 nM Poor binder T27137 Metabotropic glutamate receptor 1 B4JKT7 6-Methyl-1-phenyl-5-(4-(trifluoromethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4(5H)-one Investigative 44442420 C19H13F3N4O2 386.3 CC1=NC2=C(C=NN2C3=CC=CC=C3)C(=O)N1C4=CC=C(C=C4)OC(F)(F)F IC50 ~ 100000 nM Poor binder T27137 Metabotropic glutamate receptor 1 B4SK1A (2S)-2-(3''-Carboxymethylbicyclo[1.1.1]pentyl)glycine Investigative 44569859 C10H15NO4 213.23 C1C2(CC1(C2)CC(=O)O)C[C@@H](C(=O)O)N Ki = 59000 nM Poor binder T27137 Metabotropic glutamate receptor 1 B54BWE (2R,4R)-4-Amino-1-naphthalen-2-ylmethyl-pyrrolidine-2,4-dicarboxylic acid Investigative 44302609 C17H18N2O4 314.34 C1[C@@H](N(C[C@]1(C(=O)O)N)CC2=CC3=CC=CC=C3C=C2)C(=O)O IC50 = 133000 nM Poor binder T27137 Metabotropic glutamate receptor 1 B56RAI 2-(2,6-Dichloro-phenyl)-7-ethyl-5-(2-methoxy-phenyl)-5H-thiazolo[3,2-a]pyrimidine-6-carboxylic acid dimethylaminomethyl ester Investigative 44322537 C25H25Cl2N3O3S 518.5 CCC1=C(C(N2C=C(SC2=N1)C3=C(C=CC=C3Cl)Cl)C4=CC=CC=C4OC)C(=O)OCN(C)C Ki ~ 100000 nM Poor binder T27137 Metabotropic glutamate receptor 1 B6BH5N 4-Amino-2-thia-bicyclo[3.1.0]hexane-4,6-dicarboxylic acid Investigative 10198133 C7H9NO4S 203.22 C1[C@]([C@@H]2[C@H]([C@@H]2S1)C(=O)O)(C(=O)O)N EC50 ~ 100000 nM Poor binder T27137 Metabotropic glutamate receptor 1 B6YQR3 N,N-Diethyl-1-methyl-6-(pyridin-2-ylmethoxy)pyrazolo[3,4-b]pyrazine-3-carboxamide Investigative 76332628 C17H20N6O2 340.4 CCN(CC)C(=O)C1=NN(C2=NC(=CN=C12)OCC3=CC=CC=N3)C IC50 ~ 50000 nM Poor binder T27137 Metabotropic glutamate receptor 1 B76ASZ [1-Methyl-6-(pyridin-2-ylmethoxy)pyrazolo[3,4-b]pyridin-3-yl]-morpholin-4-ylmethanone Investigative 76332629 C18H19N5O3 353.4 CN1C2=C(C=CC(=N2)OCC3=CC=CC=N3)C(=N1)C(=O)N4CCOCC4 IC50 ~ 50000 nM Poor binder T27137 Metabotropic glutamate receptor 1 B7GQ1B 4-(6-Methyl-4-oxo-1-phenyl-1H-pyrazolo[3,4-d]pyrimidin-5(4H)-yl)benzenesulfonamide Investigative 44442421 C18H15N5O3S 381.4 CC1=NC2=C(C=NN2C3=CC=CC=C3)C(=O)N1C4=CC=C(C=C4)S(=O)(=O)N IC50 ~ 100000 nM Poor binder T27137 Metabotropic glutamate receptor 1 B7VM5K trans-ACPD Investigative 73537 C7H11NO4 173.17 C1C[C@@](C[C@H]1C(=O)O)(C(=O)O)N EC50 = 127000 nM Poor binder T27137 Metabotropic glutamate receptor 1 B89BZX (1S,2S,3R)-2-[(S)-Amino(carboxy)methyl]-3-cyclopropylcyclopropane-1-carboxylic acid Investigative 46927956 C9H13NO4 199.2 C1CC1[C@@H]2[C@@H]([C@H]2C(=O)O)[C@@H](C(=O)O)N EC50 ~ 100000 nM Poor binder T27137 Metabotropic glutamate receptor 1 B8B3PA 5-(4-Chlorophenyl)-6-methyl-1-(pyridin-2-yl)-1H-pyrazolo[3,4-d]pyrimidin-4(5H)-one Investigative 44442433 C17H12ClN5O 337.8 CC1=NC2=C(C=NN2C3=CC=CC=N3)C(=O)N1C4=CC=C(C=C4)Cl IC50 ~ 100000 nM Poor binder T27137 Metabotropic glutamate receptor 1 B8K6VC (S)-4-(Amino(carboxy)methyl)cubane-1-carboxylic acid Investigative 10198359 C11H11NO4 221.21 C12C3C4C1(C5C2C3(C45)C(=O)O)[C@@H](C(=O)O)N IC50 = 76000 nM Poor binder T27137 Metabotropic glutamate receptor 1 BD93ST 2-[(1R,2R,3S)-2-Carboxy-3-phenylcyclopropyl]-L-glycine Investigative 10489913 C12H13NO4 235.24 C1=CC=C(C=C1)[C@H]2[C@H]([C@@H]2C(=O)O)[C@@H](C(=O)O)N Ki = 60000 nM Poor binder T27137 Metabotropic glutamate receptor 1 BDX52N (1S,2S,3S)-2-[1-Amino-1-carboxy-2-(9H-xanthen-9-yl)-ethyl]-3-butyl-cyclopropanecarboxylic acid Investigative 44328753 C24H27NO5 409.5 CCCC[C@@H]1[C@@H]([C@H]1C(CC2C3=CC=CC=C3OC4=CC=CC=C24)(C(=O)O)N)C(=O)O IC50 = 57000 nM Poor binder T27137 Metabotropic glutamate receptor 1 BGI1S7 alpha-Methyl-4-carboxyphenylglycine Investigative 1222 C10H11NO4 209.2 CC(C1=CC=C(C=C1)C(=O)O)(C(=O)O)N Ki = 50000 nM Poor binder T27137 Metabotropic glutamate receptor 1 BH3E4M (S)-4-((1-Carboxyethyl)amino)benzoic acid Investigative 22884216 C10H11NO4 209.2 C[C@@H](C(=O)O)NC1=CC=C(C=C1)C(=O)O IC50 = 57000 nM Poor binder T27137 Metabotropic glutamate receptor 1 BIGT98 (1R,2S,4R,5R)-2-Amino-bicyclo[2.1.1]hexane-2,5-dicarboxylic acid Investigative 10775369 C8H11NO4 185.18 C1[C@@H]2C[C@]([C@H]1[C@@H]2C(=O)O)(C(=O)O)N EC50 = 121000 nM Poor binder T27137 Metabotropic glutamate receptor 1 BJ59AS Cyclopropaneacetic acid, alpha-amino-2-sulfo-, (alphaS,1S,2R)- Investigative 17758554 C5H9NO5S 195.2 C1[C@H]([C@@H]1S(=O)(=O)O)[C@@H](C(=O)O)N Ki = 77000 nM Poor binder T27137 Metabotropic glutamate receptor 1 BJ9L3T (1S,2S,3S)-2-[1-Amino-1-carboxy-2-(9H-xanthen-9-yl)-ethyl]-3-ethyl-cyclopropanecarboxylic acid Investigative 44329042 C22H23NO5 381.4 CC[C@@H]1[C@@H]([C@H]1C(CC2C3=CC=CC=C3OC4=CC=CC=C24)(C(=O)O)N)C(=O)O IC50 ~ 100000 nM Poor binder T27137 Metabotropic glutamate receptor 1 BJSK27 1-Methyl-N-[(3-methyl-1,2-oxazol-5-yl)methyl]-6-(pyridin-2-ylmethoxy)pyrazolo[3,4-b]pyridine-3-carboxamide Investigative 76318078 C19H18N6O3 378.4 CC1=NOC(=C1)CNC(=O)C2=NN(C3=C2C=CC(=N3)OCC4=CC=CC=N4)C IC50 ~ 50000 nM Poor binder T27137 Metabotropic glutamate receptor 1 BK6I9B 2-[(3-Methylphenyl)amino]-7,8-dihydroquinazolin-5(6H)-one Investigative 17228330 C15H15N3O 253.3 CC1=CC(=CC=C1)NC2=NC=C3C(=N2)CCCC3=O IC50 ~ 100000 nM Poor binder T27137 Metabotropic glutamate receptor 1 BKY9E8 4-Carboxyphenylglycine Investigative 5115 C9H9NO4 195.17 C1=CC(=CC=C1C(C(=O)O)N)C(=O)O IC50 = 65000 nM Poor binder T27137 Metabotropic glutamate receptor 1 BL2OD9 6-Methyl-1,5-di(pyrazin-2-yl)-1H-pyrazolo[3,4-d]pyrimidin-4(5H)-one Investigative 44442436 C14H10N8O 306.28 CC1=NC2=C(C=NN2C3=NC=CN=C3)C(=O)N1C4=NC=CN=C4 IC50 ~ 100000 nM Poor binder T27137 Metabotropic glutamate receptor 1 BPG7E9 (1S,2S,3S)-2-[1-Amino-1-carboxy-2-(9H-xanthen-9-yl)-ethyl]-3-phenethyl-cyclopropanecarboxylic acid Investigative 10456810 C28H27NO5 457.5 C1=CC=C(C=C1)CC[C@@H]2[C@@H]([C@H]2C(CC3C4=CC=CC=C4OC5=CC=CC=C35)(C(=O)O)N)C(=O)O IC50 ~ 100000 nM Poor binder T27137 Metabotropic glutamate receptor 1 BQK1P0 (1S,2S,3S)-2-[1-Amino-1-carboxy-2-(9H-xanthen-9-yl)-ethyl]-3-methyl-cyclopropanecarboxylic acid Investigative 44328850 C21H21NO5 367.4 C[C@@H]1[C@@H]([C@H]1C(CC2C3=CC=CC=C3OC4=CC=CC=C24)(C(=O)O)N)C(=O)O IC50 ~ 100000 nM Poor binder T27137 Metabotropic glutamate receptor 1 BQV60X N-Ethyl-1-methyl-6-[(6-methylpyridin-2-yl)methoxy]pyrazolo[3,4-b]pyridine-3-carboxamide Investigative 76321785 C17H19N5O2 325.4 CCNC(=O)C1=NN(C2=C1C=CC(=N2)OCC3=CC=CC(=N3)C)C IC50 ~ 50000 nM Poor binder T27137 Metabotropic glutamate receptor 1 BRSO72 (S)-2-Amino-3-(4-butyl-3-hydroxy-isoxazol-5-yl)-propionic acid Investigative 10263168 C10H16N2O4 228.24 CCCCC1=C(ONC1=O)C[C@@H](C(=O)O)N Ki = 110000 nM Poor binder T27137 Metabotropic glutamate receptor 1 BS4J2I N-(4-Fluorophenyl)-4,5,6,7-tetrahydro-1,3-benzothiazol-2-amine Investigative 685051 C13H13FN2S 248.32 C1CCC2=C(C1)N=C(S2)NC3=CC=C(C=C3)F IC50 = 64000 nM Poor binder T27137 Metabotropic glutamate receptor 1 BSX63D (1S,2S,3S)-2-[1-Amino-1-carboxy-2-(9H-xanthen-9-yl)-ethyl]-3-isobutyl-cyclopropanecarboxylic acid Investigative 44329033 C24H27NO5 409.5 CC(C)C[C@@H]1[C@@H]([C@H]1C(CC2C3=CC=CC=C3OC4=CC=CC=C24)(C(=O)O)N)C(=O)O IC50 ~ 100000 nM Poor binder T27137 Metabotropic glutamate receptor 1 BV5UC8 (1S,2S,3R)-2-[(S)-Amino(carboxy)methyl]-3-cyclohexylcyclopropane-1-carboxylic acid Investigative 52944782 C12H19NO4 241.28 C1CCC(CC1)[C@@H]2[C@@H]([C@H]2C(=O)O)[C@@H](C(=O)O)N EC50 ~ 100000 nM Poor binder T27137 Metabotropic glutamate receptor 1 BWD4G0 5-(3-Chlorophenyl)-6-methyl-1-phenyl-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one Investigative 697713 C18H13ClN4O 336.8 CC1=NC2=C(C=NN2C3=CC=CC=C3)C(=O)N1C4=CC(=CC=C4)Cl IC50 ~ 100000 nM Poor binder T27137 Metabotropic glutamate receptor 1 BX3R5D (RS)-4-Carboxy-3-hydroxyphenylglycine Investigative 1297 C9H9NO5 211.17 C1=CC(=C(C=C1C(C(=O)O)N)O)C(=O)O IC50 = 200000 nM Poor binder T27137 Metabotropic glutamate receptor 1 BXO13N 9-Dimethylamino-3-(4-cyclohexylphenyl)-3H-5-thia-1,3,6-triazafluoren-4-one Investigative 11682866 C23H24N4OS 404.5 CN(C)C1=C2C3=C(C(=O)N(C=N3)C4=CC=C(C=C4)C5CCCCC5)SC2=NC=C1 IC50 ~ 100000 nM Poor binder T27137 Metabotropic glutamate receptor 1 BY1UF5 2-Amino-3-hydroxy-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid(HYDIA) Investigative 44322840 C8H11NO5 201.18 C1[C@H]([C@](C2C1[C@@H]2C(=O)O)(C(=O)O)N)O Ki ~ 100000 nM Poor binder T27137 Metabotropic glutamate receptor 1 BZ10NG 2-(Amino-carboxy-methyl)-3-methyl-cyclopropanecarboxylic acid Investigative 10176324 C7H11NO4 173.17 C[C@@H]1[C@@H]([C@H]1C(=O)O)[C@@H](C(=O)O)N EC50 ~ 100000 nM Poor binder T27137 Metabotropic glutamate receptor 1 BZPS47 L-Homocysteic acid Investigative 177491 C4H9NO5S 183.19 C(CS(=O)(=O)O)[C@@H](C(=O)O)N Ki = 87000 nM Poor binder T27137 Metabotropic glutamate receptor 1 D05TFE SIB-1757 Investigative 5218788 C12H11N3O 213.23 . Ki ~ 100000 nM Poor binder T27137 Metabotropic glutamate receptor 1 D06PAK LY-389795 Investigative 10058694 C7H9NO4S 203.22 C1[C@](C2[C@H](C2S1)C(=O)O)(C(=O)O)N Ki ~ 100000 nM Poor binder T27137 Metabotropic glutamate receptor 1 D07GRG LY-379268 Investigative 10197984 C7H9NO5 187.15 C1[C@]([C@@H]2[C@H]([C@@H]2O1)C(=O)O)(C(=O)O)N Ki ~ 100000 nM Poor binder T27137 Metabotropic glutamate receptor 1 D09UBS Ro64-5229 Investigative 10428048 C17H19Cl2N3O 352.3 C1CCCC(CC1)O/C(=C\\N2C=NC=N2)/C3=C(C=CC=C3Cl)Cl Ki ~ 100000 nM Poor binder T27137 Metabotropic glutamate receptor 1 D0EK6P (2R,4R)-4-aminopyrrolidine-2,4-dicarboxylate Investigative 5310984 C6H10N2O4 174.15 C1[C@@H](NC[C@]1(C(=O)O)N)C(=O)O Ki ~ 100000 nM Poor binder T27137 Metabotropic glutamate receptor 1 D0Q6VH SIB-1893 Investigative 5311432 C14H13N 195.26 CC1=NC(=CC=C1)/C=C/C2=CC=CC=C2 Ki ~ 100000 nM Poor binder