Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Potency)
# tested GPCRs
(Potency)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
60096224 163324 0 None 43 2 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 320 4 5 5 -0.4 N[C@@]1(C(=O)O)C[C@H](NC(=O)c2ccccc2O)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
CHEMBL4068189 163324 0 None 43 2 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 320 4 5 5 -0.4 N[C@@]1(C(=O)O)C[C@H](NC(=O)c2ccccc2O)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
60096231 164434 15 None 48 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 334 5 4 5 -0.1 COc1cccc(C(=O)N[C@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)c1 10.1021/acs.jmedchem.7b01481
CHEMBL4081453 164434 15 None 48 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 334 5 4 5 -0.1 COc1cccc(C(=O)N[C@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)c1 10.1021/acs.jmedchem.7b01481
60096201 165347 0 None 5 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 320 4 5 5 -0.4 N[C@@]1(C(=O)O)C[C@H](NC(=O)c2cccc(O)c2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
CHEMBL4091735 165347 0 None 5 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 320 4 5 5 -0.4 N[C@@]1(C(=O)O)C[C@H](NC(=O)c2cccc(O)c2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
60096178 163660 0 None 10 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 338 4 4 4 0.6 N[C@@]1(C(=O)O)C[C@H](NC(=O)c2cccc(Cl)c2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
CHEMBL4071962 163660 0 None 10 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 338 4 4 4 0.6 N[C@@]1(C(=O)O)C[C@H](NC(=O)c2cccc(Cl)c2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
10353365 90022 1 None -13 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human mGluR3 assessed as effect on cAMP production in RGT cellsAgonist activity at human mGluR3 assessed as effect on cAMP production in RGT cells
ChEMBL 219 2 3 4 -1.8 N[C@@]1(C(=O)O)C[S+]([O-])[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm060917u
CHEMBL218710 90022 1 None -13 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human mGluR3 assessed as effect on cAMP production in RGT cellsAgonist activity at human mGluR3 assessed as effect on cAMP production in RGT cells
ChEMBL 219 2 3 4 -1.8 N[C@@]1(C(=O)O)C[S+]([O-])[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm060917u
10807972 42591 1 None -6 4 Rat 7.0 pEC50 = 7 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3Agonist potency against cloned Metabotropic glutamate receptor 3
ChEMBL 353 5 3 4 2.8 N[C@@](CC1c2ccccc2Oc2ccccc21)(C(=O)O)[C@H]1C[C@@H]1C(=O)O 10.1021/jm000346k
CHEMBL144151 42591 1 None -6 4 Rat 7.0 pEC50 = 7 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3Agonist potency against cloned Metabotropic glutamate receptor 3
ChEMBL 353 5 3 4 2.8 N[C@@](CC1c2ccccc2Oc2ccccc21)(C(=O)O)[C@H]1C[C@@H]1C(=O)O 10.1021/jm000346k
1310 9095 110 None -251 17 Human 6.0 pEC50 = 6 Functional
Agonist activity at wild type human recombinant mGlu3 receptor expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at wild type human recombinant mGlu3 receptor expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01124
1369 9095 110 None -251 17 Human 6.0 pEC50 = 6 Functional
Agonist activity at wild type human recombinant mGlu3 receptor expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at wild type human recombinant mGlu3 receptor expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01124
33032 9095 110 None -251 17 Human 6.0 pEC50 = 6 Functional
Agonist activity at wild type human recombinant mGlu3 receptor expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at wild type human recombinant mGlu3 receptor expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01124
44272391 9095 110 None -251 17 Human 6.0 pEC50 = 6 Functional
Agonist activity at wild type human recombinant mGlu3 receptor expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at wild type human recombinant mGlu3 receptor expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01124
88747398 9095 110 None -251 17 Human 6.0 pEC50 = 6 Functional
Agonist activity at wild type human recombinant mGlu3 receptor expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at wild type human recombinant mGlu3 receptor expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01124
CHEMBL575060 9095 110 None -251 17 Human 6.0 pEC50 = 6 Functional
Agonist activity at wild type human recombinant mGlu3 receptor expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at wild type human recombinant mGlu3 receptor expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01124
DB00142 9095 110 None -251 17 Human 6.0 pEC50 = 6 Functional
Agonist activity at wild type human recombinant mGlu3 receptor expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at wild type human recombinant mGlu3 receptor expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01124
71135411 130175 0 None -5 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assayAgonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 298 4 4 6 -0.3 Cc1nnc(S[C@@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)[nH]1 10.1021/acs.jmedchem.5b01124
CHEMBL3616848 130175 0 None -5 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assayAgonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 298 4 4 6 -0.3 Cc1nnc(S[C@@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)[nH]1 10.1021/acs.jmedchem.5b01124
49858118 7894 0 None -10 2 Human 5.0 pEC50 = 5.0 Functional
Positive allosteric modulator activity at human mGluR3 expressed in HEK cells in presence of glutamate EC10 concentration by Ca2+ functional assayPositive allosteric modulator activity at human mGluR3 expressed in HEK cells in presence of glutamate EC10 concentration by Ca2+ functional assay
ChEMBL 324 3 2 5 2.7 O/N=C\1/c2ccccc2OC2(C1C2)C(=O)Nc1ccc(cc1)OC 10.1021/jm101069m
6224 7894 0 None -10 2 Human 5.0 pEC50 = 5.0 Functional
Positive allosteric modulator activity at human mGluR3 expressed in HEK cells in presence of glutamate EC10 concentration by Ca2+ functional assayPositive allosteric modulator activity at human mGluR3 expressed in HEK cells in presence of glutamate EC10 concentration by Ca2+ functional assay
ChEMBL 324 3 2 5 2.7 O/N=C\1/c2ccccc2OC2(C1C2)C(=O)Nc1ccc(cc1)OC 10.1021/jm101069m
CHEMBL1630807 7894 0 None -10 2 Human 5.0 pEC50 = 5.0 Functional
Positive allosteric modulator activity at human mGluR3 expressed in HEK cells in presence of glutamate EC10 concentration by Ca2+ functional assayPositive allosteric modulator activity at human mGluR3 expressed in HEK cells in presence of glutamate EC10 concentration by Ca2+ functional assay
ChEMBL 324 3 2 5 2.7 O/N=C\1/c2ccccc2OC2(C1C2)C(=O)Nc1ccc(cc1)OC 10.1021/jm101069m
71135411 130175 0 None -5 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1.5 hrs by FLIPR assayAgonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1.5 hrs by FLIPR assay
ChEMBL 298 4 4 6 -0.3 Cc1nnc(S[C@@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)[nH]1 10.1021/acs.jmedchem.5b01124
CHEMBL3616848 130175 0 None -5 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1.5 hrs by FLIPR assayAgonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1.5 hrs by FLIPR assay
ChEMBL 298 4 4 6 -0.3 Cc1nnc(S[C@@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)[nH]1 10.1021/acs.jmedchem.5b01124
44361401 38115 0 None -1 5 Rat 8.0 pEC50 = 8.0 Functional
Metabotropic glutamate receptor 3 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 3 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 175 3 4 4 -1.9 N[C@H](C(=O)O)[C@H]1[C@@H](O)[C@@H]1C(=O)O 10.1021/jm030967o
CHEMBL140197 38115 0 None -1 5 Rat 8.0 pEC50 = 8.0 Functional
Metabotropic glutamate receptor 3 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 3 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 175 3 4 4 -1.9 N[C@H](C(=O)O)[C@H]1[C@@H](O)[C@@H]1C(=O)O 10.1021/jm030967o
60096231 164434 15 None 48 4 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing rat EAAT1/Galpha15 assessed as induction of increase in Ca2+ flux after 2.5 mins by Fluo-3 AM dye-based FLIPR assayAgonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing rat EAAT1/Galpha15 assessed as induction of increase in Ca2+ flux after 2.5 mins by Fluo-3 AM dye-based FLIPR assay
ChEMBL 334 5 4 5 -0.1 COc1cccc(C(=O)N[C@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)c1 10.1021/acs.jmedchem.7b01481
CHEMBL4081453 164434 15 None 48 4 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing rat EAAT1/Galpha15 assessed as induction of increase in Ca2+ flux after 2.5 mins by Fluo-3 AM dye-based FLIPR assayAgonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing rat EAAT1/Galpha15 assessed as induction of increase in Ca2+ flux after 2.5 mins by Fluo-3 AM dye-based FLIPR assay
ChEMBL 334 5 4 5 -0.1 COc1cccc(C(=O)N[C@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)c1 10.1021/acs.jmedchem.7b01481
71137011 130185 0 None -58 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assayAgonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 299 4 5 7 -1.0 Nc1nnc(S[C@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)[nH]1 10.1021/acs.jmedchem.5b01124
CHEMBL3616858 130185 0 None -58 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assayAgonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 299 4 5 7 -1.0 Nc1nnc(S[C@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)[nH]1 10.1021/acs.jmedchem.5b01124
53240406 130174 17 None -107 4 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant mGlu3 receptor D279E and Q306L mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant mGlu3 receptor D279E and Q306L mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 284 4 4 6 -0.6 N[C@@]1(C(=O)O)C[C@@H](Sc2nnc[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
CHEMBL3616847 130174 17 None -107 4 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant mGlu3 receptor D279E and Q306L mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant mGlu3 receptor D279E and Q306L mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 284 4 4 6 -0.6 N[C@@]1(C(=O)O)C[C@@H](Sc2nnc[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
53240406 130174 17 None -107 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assayAgonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 284 4 4 6 -0.6 N[C@@]1(C(=O)O)C[C@@H](Sc2nnc[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
CHEMBL3616847 130174 17 None -107 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assayAgonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 284 4 4 6 -0.6 N[C@@]1(C(=O)O)C[C@@H](Sc2nnc[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
49836087 7847 0 None -16 2 Human 4.9 pEC50 = 4.9 Functional
Positive allosteric modulator activity at human mGluR3 expressed in HEK cells in presence of glutamate EC10 concentration by Ca2+ functional assayPositive allosteric modulator activity at human mGluR3 expressed in HEK cells in presence of glutamate EC10 concentration by Ca2+ functional assay
ChEMBL 328 2 2 4 3.3 O/N=C\1/c2ccccc2OC2(C1C2)C(=O)Nc1ccc(cc1)Cl 10.1021/jm101069m
6222 7847 0 None -16 2 Human 4.9 pEC50 = 4.9 Functional
Positive allosteric modulator activity at human mGluR3 expressed in HEK cells in presence of glutamate EC10 concentration by Ca2+ functional assayPositive allosteric modulator activity at human mGluR3 expressed in HEK cells in presence of glutamate EC10 concentration by Ca2+ functional assay
ChEMBL 328 2 2 4 3.3 O/N=C\1/c2ccccc2OC2(C1C2)C(=O)Nc1ccc(cc1)Cl 10.1021/jm101069m
CHEMBL1630805 7847 0 None -16 2 Human 4.9 pEC50 = 4.9 Functional
Positive allosteric modulator activity at human mGluR3 expressed in HEK cells in presence of glutamate EC10 concentration by Ca2+ functional assayPositive allosteric modulator activity at human mGluR3 expressed in HEK cells in presence of glutamate EC10 concentration by Ca2+ functional assay
ChEMBL 328 2 2 4 3.3 O/N=C\1/c2ccccc2OC2(C1C2)C(=O)Nc1ccc(cc1)Cl 10.1021/jm101069m
1393 8321 64 None -4 6 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1.5 hrs by FLIPR assayAgonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1.5 hrs by FLIPR assay
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/acs.jmedchem.5b01124
1396 8321 64 None -4 6 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1.5 hrs by FLIPR assayAgonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1.5 hrs by FLIPR assay
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/acs.jmedchem.5b01124
213056 8321 64 None -4 6 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1.5 hrs by FLIPR assayAgonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1.5 hrs by FLIPR assay
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/acs.jmedchem.5b01124
CHEMBL8759 8321 64 None -4 6 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1.5 hrs by FLIPR assayAgonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1.5 hrs by FLIPR assay
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/acs.jmedchem.5b01124
1310 9095 110 None -251 17 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant mGlu3 receptor Q306L mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant mGlu3 receptor Q306L mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01124
1369 9095 110 None -251 17 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant mGlu3 receptor Q306L mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant mGlu3 receptor Q306L mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01124
33032 9095 110 None -251 17 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant mGlu3 receptor Q306L mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant mGlu3 receptor Q306L mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01124
44272391 9095 110 None -251 17 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant mGlu3 receptor Q306L mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant mGlu3 receptor Q306L mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01124
88747398 9095 110 None -251 17 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant mGlu3 receptor Q306L mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant mGlu3 receptor Q306L mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01124
CHEMBL575060 9095 110 None -251 17 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant mGlu3 receptor Q306L mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant mGlu3 receptor Q306L mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01124
DB00142 9095 110 None -251 17 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant mGlu3 receptor Q306L mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant mGlu3 receptor Q306L mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01124
67973913 143853 0 None -2 2 Human 6.8 pEC50 = 6.8 Functional
Antagonist activity at human mGlu3 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium mobilizationAntagonist activity at human mGlu3 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 333 4 0 4 3.4 Cc1ccc(N2CCn3nc(COc4ccccc4)cc3C2=O)cc1 10.1016/j.bmcl.2015.11.098
CHEMBL3747073 143853 0 None -2 2 Human 6.8 pEC50 = 6.8 Functional
Antagonist activity at human mGlu3 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium mobilizationAntagonist activity at human mGlu3 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 333 4 0 4 3.4 Cc1ccc(N2CCn3nc(COc4ccccc4)cc3C2=O)cc1 10.1016/j.bmcl.2015.11.098
1392 6861 48 None -5 4 Rat 5.8 pEC50 = 5.8 Functional
Effective concentration required for agonistic activity at Metabotropic glutamate receptor 3Effective concentration required for agonistic activity at Metabotropic glutamate receptor 3
ChEMBL 174 2 4 4 -1.8 OC(=O)[C@@H]1NC[C@@](C1)(N)C(=O)O 10.1016/s0960-894x(01)00329-8
5310984 6861 48 None -5 4 Rat 5.8 pEC50 = 5.8 Functional
Effective concentration required for agonistic activity at Metabotropic glutamate receptor 3Effective concentration required for agonistic activity at Metabotropic glutamate receptor 3
ChEMBL 174 2 4 4 -1.8 OC(=O)[C@@H]1NC[C@@](C1)(N)C(=O)O 10.1016/s0960-894x(01)00329-8
CHEMBL40086 6861 48 None -5 4 Rat 5.8 pEC50 = 5.8 Functional
Effective concentration required for agonistic activity at Metabotropic glutamate receptor 3Effective concentration required for agonistic activity at Metabotropic glutamate receptor 3
ChEMBL 174 2 4 4 -1.8 OC(=O)[C@@H]1NC[C@@](C1)(N)C(=O)O 10.1016/s0960-894x(01)00329-8
90643858 118643 0 None -25 2 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of rat mGluR3 receptor expressed in TREx293 cells by calcium mobilization assayPositive allosteric modulation of rat mGluR3 receptor expressed in TREx293 cells by calcium mobilization assay
ChEMBL 430 12 2 6 4.9 COc1cc(C(=O)O)ccc1OCCCCOc1ccc(C(=O)CC(C)C)c(O)c1C 10.1021/jm5000563
CHEMBL3287695 118643 0 None -25 2 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of rat mGluR3 receptor expressed in TREx293 cells by calcium mobilization assayPositive allosteric modulation of rat mGluR3 receptor expressed in TREx293 cells by calcium mobilization assay
ChEMBL 430 12 2 6 4.9 COc1cc(C(=O)O)ccc1OCCCCOc1ccc(C(=O)CC(C)C)c(O)c1C 10.1021/jm5000563
60096211 96834 0 None 1 4 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 242 3 4 4 -1.4 CC(=O)N[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/acs.jmedchem.7b01481
CHEMBL2381649 96834 0 None 1 4 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 242 3 4 4 -1.4 CC(=O)N[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/acs.jmedchem.7b01481
60096190 165292 0 None 9 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 322 4 4 4 0.1 N[C@@]1(C(=O)O)C[C@H](NC(=O)c2cccc(F)c2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
CHEMBL4091203 165292 0 None 9 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 322 4 4 4 0.1 N[C@@]1(C(=O)O)C[C@H](NC(=O)c2cccc(F)c2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
1395 9306 15 None -3 4 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at mGLUR3 expressed in CHO cellsAgonist activity at mGLUR3 expressed in CHO cells
ChEMBL 217 2 3 4 -1.2 O=C1C[C@@]([C@H]2[C@@H]1[C@]2(F)C(=O)O)(N)C(=O)O 10.1016/j.bmcl.2012.01.039
9837317 9306 15 None -3 4 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at mGLUR3 expressed in CHO cellsAgonist activity at mGLUR3 expressed in CHO cells
ChEMBL 217 2 3 4 -1.2 O=C1C[C@@]([C@H]2[C@@H]1[C@]2(F)C(=O)O)(N)C(=O)O 10.1016/j.bmcl.2012.01.039
CHEMBL121053 9306 15 None -3 4 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at mGLUR3 expressed in CHO cellsAgonist activity at mGLUR3 expressed in CHO cells
ChEMBL 217 2 3 4 -1.2 O=C1C[C@@]([C@H]2[C@@H]1[C@]2(F)C(=O)O)(N)C(=O)O 10.1016/j.bmcl.2012.01.039
1395 9306 15 None -3 4 Rat 8.7 pEC50 = 8.7 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3Agonist potency against cloned Metabotropic glutamate receptor 3
ChEMBL 217 2 3 4 -1.2 O=C1C[C@@]([C@H]2[C@@H]1[C@]2(F)C(=O)O)(N)C(=O)O 10.1021/jm000346k
9837317 9306 15 None -3 4 Rat 8.7 pEC50 = 8.7 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3Agonist potency against cloned Metabotropic glutamate receptor 3
ChEMBL 217 2 3 4 -1.2 O=C1C[C@@]([C@H]2[C@@H]1[C@]2(F)C(=O)O)(N)C(=O)O 10.1021/jm000346k
CHEMBL121053 9306 15 None -3 4 Rat 8.7 pEC50 = 8.7 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3Agonist potency against cloned Metabotropic glutamate receptor 3
ChEMBL 217 2 3 4 -1.2 O=C1C[C@@]([C@H]2[C@@H]1[C@]2(F)C(=O)O)(N)C(=O)O 10.1021/jm000346k
60096228 163566 0 None 2 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 320 4 5 5 -0.4 N[C@@]1(C(=O)O)C[C@H](NC(=O)c2ccc(O)cc2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
CHEMBL4070866 163566 0 None 2 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 320 4 5 5 -0.4 N[C@@]1(C(=O)O)C[C@H](NC(=O)c2ccc(O)cc2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
60096246 162726 0 None 6 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 334 5 4 5 -0.1 COc1ccc(C(=O)N[C@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)cc1 10.1021/acs.jmedchem.7b01481
CHEMBL4061162 162726 0 None 6 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 334 5 4 5 -0.1 COc1ccc(C(=O)N[C@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)cc1 10.1021/acs.jmedchem.7b01481
1377 8122 26 None -1 8 Rat 6.7 pEC50 = 6.7 Functional
Metabotropic glutamate receptor 3 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 3 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 203 4 4 4 -1.6 N[C@@H](C1[C@H]([C@@H]1C(=O)O)C(=O)O)C(=O)O 10.1021/jm030967o
5310979 8122 26 None -1 8 Rat 6.7 pEC50 = 6.7 Functional
Metabotropic glutamate receptor 3 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 3 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 203 4 4 4 -1.6 N[C@@H](C1[C@H]([C@@H]1C(=O)O)C(=O)O)C(=O)O 10.1021/jm030967o
CHEMBL284193 8122 26 None -1 8 Rat 6.7 pEC50 = 6.7 Functional
Metabotropic glutamate receptor 3 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 3 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 203 4 4 4 -1.6 N[C@@H](C1[C@H]([C@@H]1C(=O)O)C(=O)O)C(=O)O 10.1021/jm030967o
10353365 90022 1 None -13 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human mGluR3 assessed as effect on cAMP production in RGT cellsAgonist activity at human mGluR3 assessed as effect on cAMP production in RGT cells
ChEMBL 219 2 3 4 -1.8 N[C@@]1(C(=O)O)C[S+]([O-])[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm060917u
CHEMBL218710 90022 1 None -13 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human mGluR3 assessed as effect on cAMP production in RGT cellsAgonist activity at human mGluR3 assessed as effect on cAMP production in RGT cells
ChEMBL 219 2 3 4 -1.8 N[C@@]1(C(=O)O)C[S+]([O-])[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm060917u
53240406 130174 17 None -107 4 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant mGlu3 receptor D279E mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant mGlu3 receptor D279E mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 284 4 4 6 -0.6 N[C@@]1(C(=O)O)C[C@@H](Sc2nnc[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
CHEMBL3616847 130174 17 None -107 4 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant mGlu3 receptor D279E mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant mGlu3 receptor D279E mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 284 4 4 6 -0.6 N[C@@]1(C(=O)O)C[C@@H](Sc2nnc[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
71136653 130181 0 None -51 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assayAgonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 284 4 4 6 -0.6 N[C@@]1(C(=O)O)C[C@H](Sc2nnc[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
CHEMBL3616854 130181 0 None -51 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assayAgonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 284 4 4 6 -0.6 N[C@@]1(C(=O)O)C[C@H](Sc2nnc[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
71136640 130180 0 None -60 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assayAgonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 284 4 4 6 -0.6 N[C@@]1(C(=O)O)C[C@@H](Sc2c[nH]nn2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
CHEMBL3616853 130180 0 None -60 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assayAgonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 284 4 4 6 -0.6 N[C@@]1(C(=O)O)C[C@@H](Sc2c[nH]nn2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
1393 8321 64 None -4 6 Human 7.6 pEC50 = 7.6 Functional
Agonistic activity against Human Metabotropic glutamate receptor 3Agonistic activity against Human Metabotropic glutamate receptor 3
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm970719q
1396 8321 64 None -4 6 Human 7.6 pEC50 = 7.6 Functional
Agonistic activity against Human Metabotropic glutamate receptor 3Agonistic activity against Human Metabotropic glutamate receptor 3
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm970719q
213056 8321 64 None -4 6 Human 7.6 pEC50 = 7.6 Functional
Agonistic activity against Human Metabotropic glutamate receptor 3Agonistic activity against Human Metabotropic glutamate receptor 3
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm970719q
CHEMBL8759 8321 64 None -4 6 Human 7.6 pEC50 = 7.6 Functional
Agonistic activity against Human Metabotropic glutamate receptor 3Agonistic activity against Human Metabotropic glutamate receptor 3
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm970719q
11275666 96832 1 None -1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 200 2 4 4 -1.6 N[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/acs.jmedchem.7b01481
CHEMBL2381647 96832 1 None -1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 200 2 4 4 -1.6 N[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/acs.jmedchem.7b01481
1310 9095 110 None -251 17 Human 5.6 pEC50 = 5.6 Functional
Agonistic activity evaluated in CHO(Chinese hamster ovary) cells expressing chimeric mGluR3/1a receptorAgonistic activity evaluated in CHO(Chinese hamster ovary) cells expressing chimeric mGluR3/1a receptor
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/s0960-894x(99)00266-8
1369 9095 110 None -251 17 Human 5.6 pEC50 = 5.6 Functional
Agonistic activity evaluated in CHO(Chinese hamster ovary) cells expressing chimeric mGluR3/1a receptorAgonistic activity evaluated in CHO(Chinese hamster ovary) cells expressing chimeric mGluR3/1a receptor
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/s0960-894x(99)00266-8
33032 9095 110 None -251 17 Human 5.6 pEC50 = 5.6 Functional
Agonistic activity evaluated in CHO(Chinese hamster ovary) cells expressing chimeric mGluR3/1a receptorAgonistic activity evaluated in CHO(Chinese hamster ovary) cells expressing chimeric mGluR3/1a receptor
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/s0960-894x(99)00266-8
44272391 9095 110 None -251 17 Human 5.6 pEC50 = 5.6 Functional
Agonistic activity evaluated in CHO(Chinese hamster ovary) cells expressing chimeric mGluR3/1a receptorAgonistic activity evaluated in CHO(Chinese hamster ovary) cells expressing chimeric mGluR3/1a receptor
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/s0960-894x(99)00266-8
88747398 9095 110 None -251 17 Human 5.6 pEC50 = 5.6 Functional
Agonistic activity evaluated in CHO(Chinese hamster ovary) cells expressing chimeric mGluR3/1a receptorAgonistic activity evaluated in CHO(Chinese hamster ovary) cells expressing chimeric mGluR3/1a receptor
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/s0960-894x(99)00266-8
CHEMBL575060 9095 110 None -251 17 Human 5.6 pEC50 = 5.6 Functional
Agonistic activity evaluated in CHO(Chinese hamster ovary) cells expressing chimeric mGluR3/1a receptorAgonistic activity evaluated in CHO(Chinese hamster ovary) cells expressing chimeric mGluR3/1a receptor
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/s0960-894x(99)00266-8
DB00142 9095 110 None -251 17 Human 5.6 pEC50 = 5.6 Functional
Agonistic activity evaluated in CHO(Chinese hamster ovary) cells expressing chimeric mGluR3/1a receptorAgonistic activity evaluated in CHO(Chinese hamster ovary) cells expressing chimeric mGluR3/1a receptor
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/s0960-894x(99)00266-8
71131322 130184 0 None -43 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assayAgonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 334 5 4 6 0.3 N[C@@]1(C(=O)O)C[C@H](Sc2nnc(C(F)F)[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
CHEMBL3616857 130184 0 None -43 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assayAgonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 334 5 4 6 0.3 N[C@@]1(C(=O)O)C[C@H](Sc2nnc(C(F)F)[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
1393 8321 64 None -4 6 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/acs.jmedchem.7b01481
1396 8321 64 None -4 6 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/acs.jmedchem.7b01481
213056 8321 64 None -4 6 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/acs.jmedchem.7b01481
CHEMBL8759 8321 64 None -4 6 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/acs.jmedchem.7b01481
1393 8321 64 None -4 6 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assayAgonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/acs.jmedchem.5b01124
1396 8321 64 None -4 6 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assayAgonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/acs.jmedchem.5b01124
213056 8321 64 None -4 6 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assayAgonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/acs.jmedchem.5b01124
CHEMBL8759 8321 64 None -4 6 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assayAgonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/acs.jmedchem.5b01124
71136655 130179 0 None -12 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assayAgonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 326 5 4 6 0.5 CC(C)c1nnc(S[C@@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)[nH]1 10.1021/acs.jmedchem.5b01124
CHEMBL3616852 130179 0 None -12 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assayAgonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 326 5 4 6 0.5 CC(C)c1nnc(S[C@@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)[nH]1 10.1021/acs.jmedchem.5b01124
53240406 130174 17 None -107 4 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant mGlu3 receptor Q306L mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant mGlu3 receptor Q306L mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 284 4 4 6 -0.6 N[C@@]1(C(=O)O)C[C@@H](Sc2nnc[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
CHEMBL3616847 130174 17 None -107 4 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant mGlu3 receptor Q306L mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant mGlu3 receptor Q306L mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 284 4 4 6 -0.6 N[C@@]1(C(=O)O)C[C@@H](Sc2nnc[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
67973779 143882 0 None 1 2 Human 6.5 pEC50 = 6.5 Functional
Antagonist activity at human mGlu3 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium mobilizationAntagonist activity at human mGlu3 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 338 4 0 5 2.7 O=C1c2cc(COc3ccccn3)nn2CCN1c1ccc(F)cc1 10.1016/j.bmcl.2015.11.098
CHEMBL3747522 143882 0 None 1 2 Human 6.5 pEC50 = 6.5 Functional
Antagonist activity at human mGlu3 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium mobilizationAntagonist activity at human mGlu3 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 338 4 0 5 2.7 O=C1c2cc(COc3ccccn3)nn2CCN1c1ccc(F)cc1 10.1016/j.bmcl.2015.11.098
90098428 130183 0 None -60 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assayAgonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 352 4 4 6 0.4 N[C@@]1(C(=O)O)C[C@H](Sc2nnc(C(F)(F)F)[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
CHEMBL3616856 130183 0 None -60 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assayAgonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 352 4 4 6 0.4 N[C@@]1(C(=O)O)C[C@H](Sc2nnc(C(F)(F)F)[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
1392 6861 48 None -9 4 Human 5.5 pEC50 = 5.5 Functional
Agonistic activity evaluated in CHO(Chinese hamster ovary) cells expressing chimeric mGluR3/1a receptorAgonistic activity evaluated in CHO(Chinese hamster ovary) cells expressing chimeric mGluR3/1a receptor
ChEMBL 174 2 4 4 -1.8 OC(=O)[C@@H]1NC[C@@](C1)(N)C(=O)O 10.1016/s0960-894x(99)00266-8
5310984 6861 48 None -9 4 Human 5.5 pEC50 = 5.5 Functional
Agonistic activity evaluated in CHO(Chinese hamster ovary) cells expressing chimeric mGluR3/1a receptorAgonistic activity evaluated in CHO(Chinese hamster ovary) cells expressing chimeric mGluR3/1a receptor
ChEMBL 174 2 4 4 -1.8 OC(=O)[C@@H]1NC[C@@](C1)(N)C(=O)O 10.1016/s0960-894x(99)00266-8
CHEMBL40086 6861 48 None -9 4 Human 5.5 pEC50 = 5.5 Functional
Agonistic activity evaluated in CHO(Chinese hamster ovary) cells expressing chimeric mGluR3/1a receptorAgonistic activity evaluated in CHO(Chinese hamster ovary) cells expressing chimeric mGluR3/1a receptor
ChEMBL 174 2 4 4 -1.8 OC(=O)[C@@H]1NC[C@@](C1)(N)C(=O)O 10.1016/s0960-894x(99)00266-8
104766 6822 42 None -8 14 Human 4.5 pEC50 = 4.5 Functional
Agonistic activity evaluated in CHO(Chinese hamster ovary) cells expressing chimeric mGluR3/1a receptorAgonistic activity evaluated in CHO(Chinese hamster ovary) cells expressing chimeric mGluR3/1a receptor
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1016/s0960-894x(99)00266-8
1365 6822 42 None -8 14 Human 4.5 pEC50 = 4.5 Functional
Agonistic activity evaluated in CHO(Chinese hamster ovary) cells expressing chimeric mGluR3/1a receptorAgonistic activity evaluated in CHO(Chinese hamster ovary) cells expressing chimeric mGluR3/1a receptor
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1016/s0960-894x(99)00266-8
CHEMBL34453 6822 42 None -8 14 Human 4.5 pEC50 = 4.5 Functional
Agonistic activity evaluated in CHO(Chinese hamster ovary) cells expressing chimeric mGluR3/1a receptorAgonistic activity evaluated in CHO(Chinese hamster ovary) cells expressing chimeric mGluR3/1a receptor
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1016/s0960-894x(99)00266-8
44378268 126903 1 None - 1 Human 4.5 pEC50 = 4.5 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3Agonist potency against cloned Metabotropic glutamate receptor 3
ChEMBL 354 12 5 5 0.4 O=C(O)CC[C@H](CP(=O)(O)C[C@H](CCC(=O)O)C(=O)O)C(=O)O 10.1021/jm9905559
CHEMBL351166 126903 1 None - 1 Human 4.5 pEC50 = 4.5 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3Agonist potency against cloned Metabotropic glutamate receptor 3
ChEMBL 354 12 5 5 0.4 O=C(O)CC[C@H](CP(=O)(O)C[C@H](CCC(=O)O)C(=O)O)C(=O)O 10.1021/jm9905559
72714783 143859 0 None -21 2 Human 5.5 pEC50 = 5.5 Functional
Antagonist activity at human mGlu3 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium mobilizationAntagonist activity at human mGlu3 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 337 4 0 4 3.3 O=C1c2cc(OCc3ccccc3)nn2CCN1c1ccc(F)cc1 10.1016/j.bmcl.2015.11.098
CHEMBL3747116 143859 0 None -21 2 Human 5.5 pEC50 = 5.5 Functional
Antagonist activity at human mGlu3 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium mobilizationAntagonist activity at human mGlu3 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 337 4 0 4 3.3 O=C1c2cc(OCc3ccccc3)nn2CCN1c1ccc(F)cc1 10.1016/j.bmcl.2015.11.098
67974346 143759 0 None 3 2 Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at human mGlu3 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium mobilizationAntagonist activity at human mGlu3 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 355 4 0 4 3.4 O=C1c2cc(COc3ccc(F)cc3)nn2CCN1c1ccc(F)cc1 10.1016/j.bmcl.2015.11.098
CHEMBL3745812 143759 0 None 3 2 Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at human mGlu3 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium mobilizationAntagonist activity at human mGlu3 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 355 4 0 4 3.4 O=C1c2cc(COc3ccc(F)cc3)nn2CCN1c1ccc(F)cc1 10.1016/j.bmcl.2015.11.098
11344646 133554 1 None -2 3 Human 7.5 pEC50 = 7.5 Functional
Evaluation of the functional effect on cAMP responses in RGT cells expressing human mGlu3 receptorEvaluation of the functional effect on cAMP responses in RGT cells expressing human mGlu3 receptor
ChEMBL 199 2 3 3 -0.2 C[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/jm040222y
CHEMBL365368 133554 1 None -2 3 Human 7.5 pEC50 = 7.5 Functional
Evaluation of the functional effect on cAMP responses in RGT cells expressing human mGlu3 receptorEvaluation of the functional effect on cAMP responses in RGT cells expressing human mGlu3 receptor
ChEMBL 199 2 3 3 -0.2 C[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/jm040222y
60096194 163367 0 None 1 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 290 5 4 4 0.3 N[C@@]1(C(=O)O)C[C@H](NCc2ccccc2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
CHEMBL4068679 163367 0 None 1 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 290 5 4 4 0.3 N[C@@]1(C(=O)O)C[C@H](NCc2ccccc2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
44300820 20150 0 None 1 2 Rat 4.4 pEC50 = 4.4 Functional
Effective concentration required for agonistic activity at Metabotropic glutamate receptor 3Effective concentration required for agonistic activity at Metabotropic glutamate receptor 3
ChEMBL 265 4 3 5 -0.5 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2ccccn2)C1 10.1016/s0960-894x(01)00329-8
CHEMBL1192558 20150 0 None 1 2 Rat 4.4 pEC50 = 4.4 Functional
Effective concentration required for agonistic activity at Metabotropic glutamate receptor 3Effective concentration required for agonistic activity at Metabotropic glutamate receptor 3
ChEMBL 265 4 3 5 -0.5 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2ccccn2)C1 10.1016/s0960-894x(01)00329-8
CHEMBL543811 20150 0 None 1 2 Rat 4.4 pEC50 = 4.4 Functional
Effective concentration required for agonistic activity at Metabotropic glutamate receptor 3Effective concentration required for agonistic activity at Metabotropic glutamate receptor 3
ChEMBL 265 4 3 5 -0.5 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2ccccn2)C1 10.1016/s0960-894x(01)00329-8
1393 8321 64 None -4 6 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human mGluR3 assessed as effect on cAMP production in RGT cellsAgonist activity at human mGluR3 assessed as effect on cAMP production in RGT cells
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm060917u
1396 8321 64 None -4 6 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human mGluR3 assessed as effect on cAMP production in RGT cellsAgonist activity at human mGluR3 assessed as effect on cAMP production in RGT cells
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm060917u
213056 8321 64 None -4 6 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human mGluR3 assessed as effect on cAMP production in RGT cellsAgonist activity at human mGluR3 assessed as effect on cAMP production in RGT cells
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm060917u
CHEMBL8759 8321 64 None -4 6 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human mGluR3 assessed as effect on cAMP production in RGT cellsAgonist activity at human mGluR3 assessed as effect on cAMP production in RGT cells
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm060917u
1393 8321 64 None -5 6 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at mGLUR3 in rat cerebral cortex assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at mGLUR3 in rat cerebral cortex assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1016/j.bmcl.2012.01.039
1396 8321 64 None -5 6 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at mGLUR3 in rat cerebral cortex assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at mGLUR3 in rat cerebral cortex assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1016/j.bmcl.2012.01.039
213056 8321 64 None -5 6 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at mGLUR3 in rat cerebral cortex assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at mGLUR3 in rat cerebral cortex assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1016/j.bmcl.2012.01.039
CHEMBL8759 8321 64 None -5 6 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at mGLUR3 in rat cerebral cortex assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at mGLUR3 in rat cerebral cortex assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1016/j.bmcl.2012.01.039
1393 8321 64 None -4 6 Human 7.4 pEC50 = 7.4 Functional
Evaluation of the functional effect on cAMP responses in RGT cells expressing human mGlu3 receptorEvaluation of the functional effect on cAMP responses in RGT cells expressing human mGlu3 receptor
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm040222y
1396 8321 64 None -4 6 Human 7.4 pEC50 = 7.4 Functional
Evaluation of the functional effect on cAMP responses in RGT cells expressing human mGlu3 receptorEvaluation of the functional effect on cAMP responses in RGT cells expressing human mGlu3 receptor
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm040222y
213056 8321 64 None -4 6 Human 7.4 pEC50 = 7.4 Functional
Evaluation of the functional effect on cAMP responses in RGT cells expressing human mGlu3 receptorEvaluation of the functional effect on cAMP responses in RGT cells expressing human mGlu3 receptor
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm040222y
CHEMBL8759 8321 64 None -4 6 Human 7.4 pEC50 = 7.4 Functional
Evaluation of the functional effect on cAMP responses in RGT cells expressing human mGlu3 receptorEvaluation of the functional effect on cAMP responses in RGT cells expressing human mGlu3 receptor
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm040222y
1393 8321 64 None -4 6 Human 7.4 pEC50 = 7.4 Functional
Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human Metabotropic glutamate receptor 3Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human Metabotropic glutamate receptor 3
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm980616n
1396 8321 64 None -4 6 Human 7.4 pEC50 = 7.4 Functional
Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human Metabotropic glutamate receptor 3Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human Metabotropic glutamate receptor 3
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm980616n
213056 8321 64 None -4 6 Human 7.4 pEC50 = 7.4 Functional
Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human Metabotropic glutamate receptor 3Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human Metabotropic glutamate receptor 3
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm980616n
CHEMBL8759 8321 64 None -4 6 Human 7.4 pEC50 = 7.4 Functional
Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human Metabotropic glutamate receptor 3Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human Metabotropic glutamate receptor 3
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm980616n
10176324 121605 1 None -4 4 Rat 7.4 pEC50 = 7.4 Functional
Metabotropic glutamate receptor 3 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 3 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 173 3 3 3 -0.6 C[C@H]1[C@H](C(=O)O)[C@H]1[C@H](N)C(=O)O 10.1021/jm030967o
CHEMBL334160 121605 1 None -4 4 Rat 7.4 pEC50 = 7.4 Functional
Metabotropic glutamate receptor 3 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 3 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 173 3 3 3 -0.6 C[C@H]1[C@H](C(=O)O)[C@H]1[C@H](N)C(=O)O 10.1021/jm030967o
4408 31906 23 None - 1 Human 4.4 pEC50 = 4.4 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3Agonist potency against cloned Metabotropic glutamate receptor 3
ChEMBL 354 12 5 5 0.4 O=C(O)CCC(CP(=O)(O)CC(CCC(=O)O)C(=O)O)C(=O)O 10.1021/jm9905559
CHEMBL134749 31906 23 None - 1 Human 4.4 pEC50 = 4.4 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3Agonist potency against cloned Metabotropic glutamate receptor 3
ChEMBL 354 12 5 5 0.4 O=C(O)CCC(CP(=O)(O)CC(CCC(=O)O)C(=O)O)C(=O)O 10.1021/jm9905559
10197984 9199 44 None -1 5 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human mGLUR3 assessed as inhibition of forskolin-stimulated cAMP production by cell-based assayAgonist activity at human mGLUR3 assessed as inhibition of forskolin-stimulated cAMP production by cell-based assay
ChEMBL 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10.1016/j.bmcl.2012.01.039
1394 9199 44 None -1 5 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human mGLUR3 assessed as inhibition of forskolin-stimulated cAMP production by cell-based assayAgonist activity at human mGLUR3 assessed as inhibition of forskolin-stimulated cAMP production by cell-based assay
ChEMBL 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10.1016/j.bmcl.2012.01.039
CHEMBL275079 9199 44 None -1 5 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human mGLUR3 assessed as inhibition of forskolin-stimulated cAMP production by cell-based assayAgonist activity at human mGLUR3 assessed as inhibition of forskolin-stimulated cAMP production by cell-based assay
ChEMBL 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10.1016/j.bmcl.2012.01.039
10197984 9199 44 None -1 5 Human 8.3 pEC50 = 8.3 Functional
Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human Metabotropic glutamate receptor 3Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human Metabotropic glutamate receptor 3
ChEMBL 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10.1021/jm980616n
1394 9199 44 None -1 5 Human 8.3 pEC50 = 8.3 Functional
Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human Metabotropic glutamate receptor 3Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human Metabotropic glutamate receptor 3
ChEMBL 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10.1021/jm980616n
CHEMBL275079 9199 44 None -1 5 Human 8.3 pEC50 = 8.3 Functional
Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human Metabotropic glutamate receptor 3Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human Metabotropic glutamate receptor 3
ChEMBL 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10.1021/jm980616n
10197984 9199 44 None -1 5 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human mGluR3 assessed as effect on cAMP production in RGT cellsAgonist activity at human mGluR3 assessed as effect on cAMP production in RGT cells
ChEMBL 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10.1021/jm060917u
1394 9199 44 None -1 5 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human mGluR3 assessed as effect on cAMP production in RGT cellsAgonist activity at human mGluR3 assessed as effect on cAMP production in RGT cells
ChEMBL 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10.1021/jm060917u
CHEMBL275079 9199 44 None -1 5 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human mGluR3 assessed as effect on cAMP production in RGT cellsAgonist activity at human mGluR3 assessed as effect on cAMP production in RGT cells
ChEMBL 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10.1021/jm060917u
11220424 165740 0 None 3 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 304 4 4 4 -0.1 N[C@@]1(C(=O)O)C[C@H](NC(=O)c2ccccc2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
CHEMBL4095995 165740 0 None 3 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 304 4 4 4 -0.1 N[C@@]1(C(=O)O)C[C@H](NC(=O)c2ccccc2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
137659992 166015 0 None 8 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 338 4 4 4 0.6 N[C@@]1(C(=O)O)C[C@H](NC(=O)c2ccccc2Cl)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
CHEMBL4098939 166015 0 None 8 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 338 4 4 4 0.6 N[C@@]1(C(=O)O)C[C@H](NC(=O)c2ccccc2Cl)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
1310 9095 110 None -251 17 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant mGlu3 receptor D279E mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant mGlu3 receptor D279E mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01124
1369 9095 110 None -251 17 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant mGlu3 receptor D279E mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant mGlu3 receptor D279E mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01124
33032 9095 110 None -251 17 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant mGlu3 receptor D279E mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant mGlu3 receptor D279E mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01124
44272391 9095 110 None -251 17 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant mGlu3 receptor D279E mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant mGlu3 receptor D279E mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01124
88747398 9095 110 None -251 17 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant mGlu3 receptor D279E mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant mGlu3 receptor D279E mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01124
CHEMBL575060 9095 110 None -251 17 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant mGlu3 receptor D279E mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant mGlu3 receptor D279E mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01124
DB00142 9095 110 None -251 17 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant mGlu3 receptor D279E mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant mGlu3 receptor D279E mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01124
9815616 121578 6 None 1 4 Rat 7.3 pEC50 = 7.3 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3Agonist potency against cloned Metabotropic glutamate receptor 3
ChEMBL 203 2 3 3 -0.5 N[C@@]1(C(=O)O)[C@@H](F)C[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm000346k
CHEMBL334014 121578 6 None 1 4 Rat 7.3 pEC50 = 7.3 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3Agonist potency against cloned Metabotropic glutamate receptor 3
ChEMBL 203 2 3 3 -0.5 N[C@@]1(C(=O)O)[C@@H](F)C[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm000346k
4408 31906 23 None - 1 Human 4.4 pEC50 = 4.4 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3Agonist potency against cloned Metabotropic glutamate receptor 3
ChEMBL 354 12 5 5 0.4 O=C(O)CCC(CP(=O)(O)CC(CCC(=O)O)C(=O)O)C(=O)O 10.1021/jm9905559
CHEMBL134749 31906 23 None - 1 Human 4.4 pEC50 = 4.4 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3Agonist potency against cloned Metabotropic glutamate receptor 3
ChEMBL 354 12 5 5 0.4 O=C(O)CCC(CP(=O)(O)CC(CCC(=O)O)C(=O)O)C(=O)O 10.1021/jm9905559
9834591 144378 69 None -2 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human mGluR3 assessed as effect on cAMP production in RGT cellsAgonist activity at human mGluR3 assessed as effect on cAMP production in RGT cells
ChEMBL 235 2 3 5 -2.1 N[C@@]1(C(=O)O)CS(=O)(=O)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm060917u
CHEMBL375611 144378 69 None -2 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human mGluR3 assessed as effect on cAMP production in RGT cellsAgonist activity at human mGluR3 assessed as effect on cAMP production in RGT cells
ChEMBL 235 2 3 5 -2.1 N[C@@]1(C(=O)O)CS(=O)(=O)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm060917u
60096236 165201 0 None 3 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 322 4 4 4 0.1 N[C@@]1(C(=O)O)C[C@H](NC(=O)c2ccccc2F)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
CHEMBL4090293 165201 0 None 3 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 322 4 4 4 0.1 N[C@@]1(C(=O)O)C[C@H](NC(=O)c2ccccc2F)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
60096250 165700 0 None 1 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 338 4 4 4 0.6 N[C@@]1(C(=O)O)C[C@H](NC(=O)c2ccc(Cl)cc2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
CHEMBL4095567 165700 0 None 1 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 338 4 4 4 0.6 N[C@@]1(C(=O)O)C[C@H](NC(=O)c2ccc(Cl)cc2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
4408 31906 23 None - 1 Human 4.3 pEC50 = 4.3 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3Agonist potency against cloned Metabotropic glutamate receptor 3
ChEMBL 354 12 5 5 0.4 O=C(O)CCC(CP(=O)(O)CC(CCC(=O)O)C(=O)O)C(=O)O 10.1021/jm9905559
CHEMBL134749 31906 23 None - 1 Human 4.3 pEC50 = 4.3 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3Agonist potency against cloned Metabotropic glutamate receptor 3
ChEMBL 354 12 5 5 0.4 O=C(O)CCC(CP(=O)(O)CC(CCC(=O)O)C(=O)O)C(=O)O 10.1021/jm9905559
1310 9095 110 None -251 17 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human recombinant mGlu3 receptor D279E and Q306L mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant mGlu3 receptor D279E and Q306L mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01124
1369 9095 110 None -251 17 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human recombinant mGlu3 receptor D279E and Q306L mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant mGlu3 receptor D279E and Q306L mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01124
33032 9095 110 None -251 17 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human recombinant mGlu3 receptor D279E and Q306L mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant mGlu3 receptor D279E and Q306L mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01124
44272391 9095 110 None -251 17 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human recombinant mGlu3 receptor D279E and Q306L mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant mGlu3 receptor D279E and Q306L mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01124
88747398 9095 110 None -251 17 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human recombinant mGlu3 receptor D279E and Q306L mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant mGlu3 receptor D279E and Q306L mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01124
CHEMBL575060 9095 110 None -251 17 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human recombinant mGlu3 receptor D279E and Q306L mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant mGlu3 receptor D279E and Q306L mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01124
DB00142 9095 110 None -251 17 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human recombinant mGlu3 receptor D279E and Q306L mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at human recombinant mGlu3 receptor D279E and Q306L mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01124
10330132 108159 1 None -10 2 Human 4.3 pEC50 = 4.3 Functional
Agonistic activity evaluated in CHO(Chinese hamster ovary) cells expressing chimeric mGluR3/1a receptorAgonistic activity evaluated in CHO(Chinese hamster ovary) cells expressing chimeric mGluR3/1a receptor
ChEMBL 189 2 4 5 -2.2 NN1C[C@@](N)(C(=O)O)C[C@@H]1C(=O)O 10.1016/s0960-894x(99)00266-8
CHEMBL297150 108159 1 None -10 2 Human 4.3 pEC50 = 4.3 Functional
Agonistic activity evaluated in CHO(Chinese hamster ovary) cells expressing chimeric mGluR3/1a receptorAgonistic activity evaluated in CHO(Chinese hamster ovary) cells expressing chimeric mGluR3/1a receptor
ChEMBL 189 2 4 5 -2.2 NN1C[C@@](N)(C(=O)O)C[C@@H]1C(=O)O 10.1016/s0960-894x(99)00266-8
127039660 143802 0 None -3 2 Human 6.3 pEC50 = 6.3 Functional
Antagonist activity at human mGlu3 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium mobilizationAntagonist activity at human mGlu3 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 351 4 0 4 3.7 O=C1c2cc(COc3ccccc3)nn2CCCN1c1ccc(F)cc1 10.1016/j.bmcl.2015.11.098
CHEMBL3746344 143802 0 None -3 2 Human 6.3 pEC50 = 6.3 Functional
Antagonist activity at human mGlu3 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium mobilizationAntagonist activity at human mGlu3 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 351 4 0 4 3.7 O=C1c2cc(COc3ccccc3)nn2CCCN1c1ccc(F)cc1 10.1016/j.bmcl.2015.11.098
53240406 130174 17 None -107 4 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at wild type human recombinant mGlu3 receptor expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at wild type human recombinant mGlu3 receptor expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 284 4 4 6 -0.6 N[C@@]1(C(=O)O)C[C@@H](Sc2nnc[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
CHEMBL3616847 130174 17 None -107 4 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at wild type human recombinant mGlu3 receptor expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assayAgonist activity at wild type human recombinant mGlu3 receptor expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assay
ChEMBL 284 4 4 6 -0.6 N[C@@]1(C(=O)O)C[C@@H](Sc2nnc[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
60096204 162903 0 None 2 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 322 4 4 4 0.1 N[C@@]1(C(=O)O)C[C@H](NC(=O)c2ccc(F)cc2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
CHEMBL4063336 162903 0 None 2 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 322 4 4 4 0.1 N[C@@]1(C(=O)O)C[C@H](NC(=O)c2ccc(F)cc2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
1368 9070 37 None -1 11 Rat 6.2 pEC50 = 6.2 Functional
Metabotropic glutamate receptor 3 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 3 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 10.1021/jm030967o
5310956 9070 37 None -1 11 Rat 6.2 pEC50 = 6.2 Functional
Metabotropic glutamate receptor 3 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 3 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 10.1021/jm030967o
CHEMBL280563 9070 37 None -1 11 Rat 6.2 pEC50 = 6.2 Functional
Metabotropic glutamate receptor 3 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 3 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 10.1021/jm030967o
1393 8321 64 None -5 6 Rat 7.2 pEC50 = 7.2 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3Agonist potency against cloned Metabotropic glutamate receptor 3
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm000346k
1396 8321 64 None -5 6 Rat 7.2 pEC50 = 7.2 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3Agonist potency against cloned Metabotropic glutamate receptor 3
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm000346k
213056 8321 64 None -5 6 Rat 7.2 pEC50 = 7.2 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3Agonist potency against cloned Metabotropic glutamate receptor 3
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm000346k
CHEMBL8759 8321 64 None -5 6 Rat 7.2 pEC50 = 7.2 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3Agonist potency against cloned Metabotropic glutamate receptor 3
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm000346k
155518933 177125 0 None 1 3 Human 6.2 pEC50 = 6.2 Functional
Allosteric agonist activity at human mGlu3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP production after 30 mins by cAMP reagent-based assayAllosteric agonist activity at human mGlu3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP production after 30 mins by cAMP reagent-based assay
ChEMBL 421 6 1 3 4.3 CNC(=O)N1CCCC(CN2CCC(OC(c3ccccc3)c3ccccc3)CC2)C1 10.1039/C8MD00524A
CHEMBL4447269 177125 0 None 1 3 Human 6.2 pEC50 = 6.2 Functional
Allosteric agonist activity at human mGlu3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP production after 30 mins by cAMP reagent-based assayAllosteric agonist activity at human mGlu3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP production after 30 mins by cAMP reagent-based assay
ChEMBL 421 6 1 3 4.3 CNC(=O)N1CCCC(CN2CCC(OC(c3ccccc3)c3ccccc3)CC2)C1 10.1039/C8MD00524A
67974411 143807 0 None -52 2 Human 5.2 pEC50 = 5.2 Functional
Antagonist activity at human mGlu3 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium mobilizationAntagonist activity at human mGlu3 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 338 4 0 5 2.7 O=C1c2cc(COc3ccccc3)nn2CCN1c1ccc(F)cn1 10.1016/j.bmcl.2015.11.098
CHEMBL3746457 143807 0 None -52 2 Human 5.2 pEC50 = 5.2 Functional
Antagonist activity at human mGlu3 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium mobilizationAntagonist activity at human mGlu3 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 338 4 0 5 2.7 O=C1c2cc(COc3ccccc3)nn2CCN1c1ccc(F)cn1 10.1016/j.bmcl.2015.11.098
10474978 20231 0 None -1 2 Rat 5.2 pEC50 = 5.2 Functional
Effective concentration required for agonistic activity at Metabotropic glutamate receptor 3Effective concentration required for agonistic activity at Metabotropic glutamate receptor 3
ChEMBL 309 5 3 6 0.0 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2ccccc2[N+](=O)[O-])C1 10.1016/s0960-894x(01)00329-8
CHEMBL1193146 20231 0 None -1 2 Rat 5.2 pEC50 = 5.2 Functional
Effective concentration required for agonistic activity at Metabotropic glutamate receptor 3Effective concentration required for agonistic activity at Metabotropic glutamate receptor 3
ChEMBL 309 5 3 6 0.0 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2ccccc2[N+](=O)[O-])C1 10.1016/s0960-894x(01)00329-8
CHEMBL544508 20231 0 None -1 2 Rat 5.2 pEC50 = 5.2 Functional
Effective concentration required for agonistic activity at Metabotropic glutamate receptor 3Effective concentration required for agonistic activity at Metabotropic glutamate receptor 3
ChEMBL 309 5 3 6 0.0 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2ccccc2[N+](=O)[O-])C1 10.1016/s0960-894x(01)00329-8
44361401 38115 0 None -1 5 Rat 8.2 pEC50 = 8.2 Functional
Metabotropic glutamate receptor 3 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 3 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 175 3 4 4 -1.9 N[C@H](C(=O)O)[C@H]1[C@@H](O)[C@@H]1C(=O)O 10.1021/jm030967o
CHEMBL140197 38115 0 None -1 5 Rat 8.2 pEC50 = 8.2 Functional
Metabotropic glutamate receptor 3 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 3 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 175 3 4 4 -1.9 N[C@H](C(=O)O)[C@H]1[C@@H](O)[C@@H]1C(=O)O 10.1021/jm030967o
60096183 166063 0 None 3 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 334 5 4 5 -0.1 COc1ccccc1C(=O)N[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/acs.jmedchem.7b01481
CHEMBL4099470 166063 0 None 3 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 334 5 4 5 -0.1 COc1ccccc1C(=O)N[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/acs.jmedchem.7b01481
10198133 213287 12 None -1 4 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human mGluR3 assessed as effect on cAMP production in RGT cellsAgonist activity at human mGluR3 assessed as effect on cAMP production in RGT cells
ChEMBL 203 2 3 4 -0.8 N[C@@]1(C(=O)O)CS[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm060917u
CHEMBL8839 213287 12 None -1 4 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human mGluR3 assessed as effect on cAMP production in RGT cellsAgonist activity at human mGluR3 assessed as effect on cAMP production in RGT cells
ChEMBL 203 2 3 4 -0.8 N[C@@]1(C(=O)O)CS[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm060917u
10198133 213287 12 None -1 4 Human 8.1 pEC50 = 8.1 Functional
Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human Metabotropic glutamate receptor 3Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human Metabotropic glutamate receptor 3
ChEMBL 203 2 3 4 -0.8 N[C@@]1(C(=O)O)CS[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm980616n
CHEMBL8839 213287 12 None -1 4 Human 8.1 pEC50 = 8.1 Functional
Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human Metabotropic glutamate receptor 3Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human Metabotropic glutamate receptor 3
ChEMBL 203 2 3 4 -0.8 N[C@@]1(C(=O)O)CS[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm980616n
71137012 130178 0 None -11 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assayAgonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 299 4 5 7 -1.0 Nc1nnc(S[C@@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)[nH]1 10.1021/acs.jmedchem.5b01124
CHEMBL3616851 130178 0 None -11 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assayAgonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 299 4 5 7 -1.0 Nc1nnc(S[C@@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)[nH]1 10.1021/acs.jmedchem.5b01124
67974644 143900 0 None -1 2 Human 7.1 pEC50 = 7.1 Functional
Antagonist activity at human mGlu3 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium mobilizationAntagonist activity at human mGlu3 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 337 4 0 4 3.3 O=C1c2cc(COc3ccccc3)nn2CCN1c1ccc(F)cc1 10.1016/j.bmcl.2015.11.098
CHEMBL3747735 143900 0 None -1 2 Human 7.1 pEC50 = 7.1 Functional
Antagonist activity at human mGlu3 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium mobilizationAntagonist activity at human mGlu3 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 337 4 0 4 3.3 O=C1c2cc(COc3ccccc3)nn2CCN1c1ccc(F)cc1 10.1016/j.bmcl.2015.11.098
9815616 121578 6 None -1 4 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human mGlu3 receptor expressed in CHO cell membranes by GTPgammaS binding assayAgonist activity at human mGlu3 receptor expressed in CHO cell membranes by GTPgammaS binding assay
ChEMBL 203 2 3 3 -0.5 N[C@@]1(C(=O)O)[C@@H](F)C[C@H]2[C@H](C(=O)O)[C@H]21 10.1016/j.ejmech.2020.112521
CHEMBL334014 121578 6 None -1 4 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human mGlu3 receptor expressed in CHO cell membranes by GTPgammaS binding assayAgonist activity at human mGlu3 receptor expressed in CHO cell membranes by GTPgammaS binding assay
ChEMBL 203 2 3 3 -0.5 N[C@@]1(C(=O)O)[C@@H](F)C[C@H]2[C@H](C(=O)O)[C@H]21 10.1016/j.ejmech.2020.112521
44300605 20127 0 None 3 3 Rat 5.1 pEC50 = 5.1 Functional
Effective concentration required for partial agonistic activity at Metabotropic glutamate receptor 3; Partial agonistEffective concentration required for partial agonistic activity at Metabotropic glutamate receptor 3; Partial agonist
ChEMBL 280 4 4 5 -0.2 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2ccc(O)cc2)C1 10.1016/s0960-894x(01)00329-8
CHEMBL1192345 20127 0 None 3 3 Rat 5.1 pEC50 = 5.1 Functional
Effective concentration required for partial agonistic activity at Metabotropic glutamate receptor 3; Partial agonistEffective concentration required for partial agonistic activity at Metabotropic glutamate receptor 3; Partial agonist
ChEMBL 280 4 4 5 -0.2 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2ccc(O)cc2)C1 10.1016/s0960-894x(01)00329-8
CHEMBL543568 20127 0 None 3 3 Rat 5.1 pEC50 = 5.1 Functional
Effective concentration required for partial agonistic activity at Metabotropic glutamate receptor 3; Partial agonistEffective concentration required for partial agonistic activity at Metabotropic glutamate receptor 3; Partial agonist
ChEMBL 280 4 4 5 -0.2 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2ccc(O)cc2)C1 10.1016/s0960-894x(01)00329-8
71137034 130177 0 None -7 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assayAgonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 334 5 4 6 0.3 N[C@@]1(C(=O)O)C[C@@H](Sc2nnc(C(F)F)[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
CHEMBL3616850 130177 0 None -7 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assayAgonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 334 5 4 6 0.3 N[C@@]1(C(=O)O)C[C@@H](Sc2nnc(C(F)F)[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
71136654 130186 0 None -3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assayAgonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 326 5 4 6 0.5 CC(C)c1nnc(S[C@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)[nH]1 10.1021/acs.jmedchem.5b01124
CHEMBL3616859 130186 0 None -3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assayAgonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 326 5 4 6 0.5 CC(C)c1nnc(S[C@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)[nH]1 10.1021/acs.jmedchem.5b01124
71137010 130176 0 None -5 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assayAgonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 352 4 4 6 0.4 N[C@@]1(C(=O)O)C[C@@H](Sc2nnc(C(F)(F)F)[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
CHEMBL3616849 130176 0 None -5 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assayAgonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 352 4 4 6 0.4 N[C@@]1(C(=O)O)C[C@@H](Sc2nnc(C(F)(F)F)[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
9815617 121277 7 None 1 2 Rat 7.1 pEC50 = 7.1 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3Agonist potency against cloned Metabotropic glutamate receptor 3
ChEMBL 203 2 3 3 -0.4 N[C@@]1(C(=O)O)CC[C@@H]2[C@H]1[C@@]2(F)C(=O)O 10.1021/jm000346k
CHEMBL333519 121277 7 None 1 2 Rat 7.1 pEC50 = 7.1 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3Agonist potency against cloned Metabotropic glutamate receptor 3
ChEMBL 203 2 3 3 -0.4 N[C@@]1(C(=O)O)CC[C@@H]2[C@H]1[C@@]2(F)C(=O)O 10.1021/jm000346k
71137010 130176 0 None -5 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1.5 hrs by FLIPR assayAgonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1.5 hrs by FLIPR assay
ChEMBL 352 4 4 6 0.4 N[C@@]1(C(=O)O)C[C@@H](Sc2nnc(C(F)(F)F)[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
CHEMBL3616849 130176 0 None -5 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1.5 hrs by FLIPR assayAgonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1.5 hrs by FLIPR assay
ChEMBL 352 4 4 6 0.4 N[C@@]1(C(=O)O)C[C@@H](Sc2nnc(C(F)(F)F)[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
117972250 149090 3 None -32 2 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGlu3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins in presence of orthosteric antagonist LY341495 by FLIPR assayPositive allosteric modulation of human mGlu3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins in presence of orthosteric antagonist LY341495 by FLIPR assay
ChEMBL 421 6 0 4 5.5 FC(F)(F)c1c(OC[C@H]2C[C@@H]2c2ccc(Cl)cc2)ccn2c(CC3CC3)nnc12 10.1016/j.bmc.2016.11.018
CHEMBL3885379 149090 3 None -32 2 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGlu3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins in presence of orthosteric antagonist LY341495 by FLIPR assayPositive allosteric modulation of human mGlu3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 30 mins in presence of orthosteric antagonist LY341495 by FLIPR assay
ChEMBL 421 6 0 4 5.5 FC(F)(F)c1c(OC[C@H]2C[C@@H]2c2ccc(Cl)cc2)ccn2c(CC3CC3)nnc12 10.1016/j.bmc.2016.11.018
49858117 7875 4 None -5 2 Human 5.1 pEC50 = 5.1 Functional
Positive allosteric modulator activity at human mGluR3 expressed in HEK cells in presence of glutamate EC10 concentration by Ca2+ functional assayPositive allosteric modulator activity at human mGluR3 expressed in HEK cells in presence of glutamate EC10 concentration by Ca2+ functional assay
ChEMBL 308 2 2 4 3.0 O/N=C\1/c2ccccc2OC2(C1C2)C(=O)Nc1ccc(cc1)C 10.1021/jm101069m
6223 7875 4 None -5 2 Human 5.1 pEC50 = 5.1 Functional
Positive allosteric modulator activity at human mGluR3 expressed in HEK cells in presence of glutamate EC10 concentration by Ca2+ functional assayPositive allosteric modulator activity at human mGluR3 expressed in HEK cells in presence of glutamate EC10 concentration by Ca2+ functional assay
ChEMBL 308 2 2 4 3.0 O/N=C\1/c2ccccc2OC2(C1C2)C(=O)Nc1ccc(cc1)C 10.1021/jm101069m
CHEMBL1630806 7875 4 None -5 2 Human 5.1 pEC50 = 5.1 Functional
Positive allosteric modulator activity at human mGluR3 expressed in HEK cells in presence of glutamate EC10 concentration by Ca2+ functional assayPositive allosteric modulator activity at human mGluR3 expressed in HEK cells in presence of glutamate EC10 concentration by Ca2+ functional assay
ChEMBL 308 2 2 4 3.0 O/N=C\1/c2ccccc2OC2(C1C2)C(=O)Nc1ccc(cc1)C 10.1021/jm101069m
71476419 130187 0 None -51 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assayAgonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 284 4 4 6 -0.6 N[C@@]1(C(=O)O)C[C@H](Sc2c[nH]nn2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
CHEMBL3616860 130187 0 None -51 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assayAgonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 284 4 4 6 -0.6 N[C@@]1(C(=O)O)C[C@H](Sc2c[nH]nn2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
71137008 130182 0 None -7 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assayAgonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 298 4 4 6 -0.3 Cc1nnc(S[C@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)[nH]1 10.1021/acs.jmedchem.5b01124
CHEMBL3616855 130182 0 None -7 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assayAgonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 298 4 4 6 -0.3 Cc1nnc(S[C@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)[nH]1 10.1021/acs.jmedchem.5b01124
9815616 121578 6 None 1 4 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat mGlu3 receptor expressed in CHO cell membranes by GTPgammaS binding assayAgonist activity at rat mGlu3 receptor expressed in CHO cell membranes by GTPgammaS binding assay
ChEMBL 203 2 3 3 -0.5 N[C@@]1(C(=O)O)[C@@H](F)C[C@H]2[C@H](C(=O)O)[C@H]21 10.1016/j.ejmech.2020.112521
CHEMBL334014 121578 6 None 1 4 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat mGlu3 receptor expressed in CHO cell membranes by GTPgammaS binding assayAgonist activity at rat mGlu3 receptor expressed in CHO cell membranes by GTPgammaS binding assay
ChEMBL 203 2 3 3 -0.5 N[C@@]1(C(=O)O)[C@@H](F)C[C@H]2[C@H](C(=O)O)[C@H]21 10.1016/j.ejmech.2020.112521
1378 9195 54 None 2 14 Human 8.0 pIC50 = 8 Functional
Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/jm970498o
1399 9195 54 None 2 14 Human 8.0 pIC50 = 8 Functional
Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/jm970498o
9819927 9195 54 None 2 14 Human 8.0 pIC50 = 8 Functional
Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/jm970498o
CHEMBL432038 9195 54 None 2 14 Human 8.0 pIC50 = 8 Functional
Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/jm970498o
44329032 119321 0 None 3 5 Rat 7.0 pIC50 = 7 Functional
Antagonistic activity against metabotropic glutamate receptor 3 (mGluR3) was evaluatedAntagonistic activity against metabotropic glutamate receptor 3 (mGluR3) was evaluated
ChEMBL 423 9 3 4 4.6 CCCCC[C@@H]1[C@H](C(=O)O)[C@H]1C(N)(CC1c2ccccc2Oc2ccccc21)C(=O)O 10.1016/s0960-894x(98)00510-1
CHEMBL329920 119321 0 None 3 5 Rat 7.0 pIC50 = 7 Functional
Antagonistic activity against metabotropic glutamate receptor 3 (mGluR3) was evaluatedAntagonistic activity against metabotropic glutamate receptor 3 (mGluR3) was evaluated
ChEMBL 423 9 3 4 4.6 CCCCC[C@@H]1[C@H](C(=O)O)[C@H]1C(N)(CC1c2ccccc2Oc2ccccc21)C(=O)O 10.1016/s0960-894x(98)00510-1
44328850 214830 0 None 1 4 Rat 6.0 pIC50 = 6 Functional
Antagonistic activity against metabotropic glutamate receptor 3 (mGluR3) was evaluatedAntagonistic activity against metabotropic glutamate receptor 3 (mGluR3) was evaluated
ChEMBL 367 5 3 4 3.1 C[C@@H]1[C@H](C(=O)O)[C@H]1C(N)(CC1c2ccccc2Oc2ccccc21)C(=O)O 10.1016/s0960-894x(98)00510-1
CHEMBL97574 214830 0 None 1 4 Rat 6.0 pIC50 = 6 Functional
Antagonistic activity against metabotropic glutamate receptor 3 (mGluR3) was evaluatedAntagonistic activity against metabotropic glutamate receptor 3 (mGluR3) was evaluated
ChEMBL 367 5 3 4 3.1 C[C@@H]1[C@H](C(=O)O)[C@H]1C(N)(CC1c2ccccc2Oc2ccccc21)C(=O)O 10.1016/s0960-894x(98)00510-1
122456191 169725 0 None -2 2 Rat 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assay
ChEMBL 344 6 0 5 3.0 O=c1nc(OCCOc2ccccc2)ccn1-c1ccc(F)c(F)c1 10.1021/acsmedchemlett.7b00249
CHEMBL4174544 169725 0 None -2 2 Rat 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assay
ChEMBL 344 6 0 5 3.0 O=c1nc(OCCOc2ccccc2)ccn1-c1ccc(F)c(F)c1 10.1021/acsmedchemlett.7b00249
122456191 169725 0 None -2 2 Rat 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assay
ChEMBL 344 6 0 5 3.0 O=c1nc(OCCOc2ccccc2)ccn1-c1ccc(F)c(F)c1 10.1021/acsmedchemlett.7b00249
CHEMBL4174544 169725 0 None -2 2 Rat 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assay
ChEMBL 344 6 0 5 3.0 O=c1nc(OCCOc2ccccc2)ccn1-c1ccc(F)c(F)c1 10.1021/acsmedchemlett.7b00249
60210837 97102 0 None - 1 Rat 5.0 pIC50 = 5.0 Functional
Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 minsNegative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 321 2 1 3 2.3 COc1ccc(C#Cc2ccc(C(=O)N3CC[C@@H](O)C3)cc2)cc1 10.1021/jm400439t
CHEMBL2385881 97102 0 None - 1 Rat 5.0 pIC50 = 5.0 Functional
Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 minsNegative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 321 2 1 3 2.3 COc1ccc(C#Cc2ccc(C(=O)N3CC[C@@H](O)C3)cc2)cc1 10.1021/jm400439t
122190324 130231 0 None 1 2 Rat 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 381 5 0 5 3.8 COc1ccc(OCc2cc3n(n2)[C@H](C)CN(c2ccc(F)cc2)C3=O)cc1 10.1021/acs.jmedchem.5b01005
CHEMBL3617508 130231 0 None 1 2 Rat 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 381 5 0 5 3.8 COc1ccc(OCc2cc3n(n2)[C@H](C)CN(c2ccc(F)cc2)C3=O)cc1 10.1021/acs.jmedchem.5b01005
122190324 130231 0 None 1 2 Rat 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 381 5 0 5 3.8 COc1ccc(OCc2cc3n(n2)[C@H](C)CN(c2ccc(F)cc2)C3=O)cc1 10.1021/acs.jmedchem.5b01005
CHEMBL3617508 130231 0 None 1 2 Rat 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 381 5 0 5 3.8 COc1ccc(OCc2cc3n(n2)[C@H](C)CN(c2ccc(F)cc2)C3=O)cc1 10.1021/acs.jmedchem.5b01005
11310142 9200 19 None -13 3 Human 6.0 pIC50 = 6.0 Functional
Evaluation of the functional effect on cAMP responses in RGT cells expressing human mGlu3 receptorEvaluation of the functional effect on cAMP responses in RGT cells expressing human mGlu3 receptor
ChEMBL 199 2 3 3 -0.2 C[C@@H]1C[C@@]([C@H]2[C@@H]1[C@@H]2C(=O)O)(N)C(=O)O 10.1021/jm040222y
11614 9200 19 None -13 3 Human 6.0 pIC50 = 6.0 Functional
Evaluation of the functional effect on cAMP responses in RGT cells expressing human mGlu3 receptorEvaluation of the functional effect on cAMP responses in RGT cells expressing human mGlu3 receptor
ChEMBL 199 2 3 3 -0.2 C[C@@H]1C[C@@]([C@H]2[C@@H]1[C@@H]2C(=O)O)(N)C(=O)O 10.1021/jm040222y
CHEMBL192051 9200 19 None -13 3 Human 6.0 pIC50 = 6.0 Functional
Evaluation of the functional effect on cAMP responses in RGT cells expressing human mGlu3 receptorEvaluation of the functional effect on cAMP responses in RGT cells expressing human mGlu3 receptor
ChEMBL 199 2 3 3 -0.2 C[C@@H]1C[C@@]([C@H]2[C@@H]1[C@@H]2C(=O)O)(N)C(=O)O 10.1021/jm040222y
10979251 96835 0 None -1 3 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as reversal of DCG-4-inhibited, forskolin-stimulated cAMP production after 1 hr by fluorescence assayAntagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as reversal of DCG-4-inhibited, forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 293 4 3 4 1.3 N[C@@]1(C(=O)O)C[C@@H](Sc2ccccc2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
CHEMBL2381650 96835 0 None -1 3 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as reversal of DCG-4-inhibited, forskolin-stimulated cAMP production after 1 hr by fluorescence assayAntagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as reversal of DCG-4-inhibited, forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 293 4 3 4 1.3 N[C@@]1(C(=O)O)C[C@@H](Sc2ccccc2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
134138062 154278 0 None 1 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assayAntagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 374 5 4 5 0.9 N[C@H]1[C@H]2[C@H](C(=O)O)[C@H]2[C@](N)(C(=O)O)[C@@H]1OCc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2016.10.067
CHEMBL3930511 154278 0 None 1 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assayAntagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 374 5 4 5 0.9 N[C@H]1[C@H]2[C@H](C(=O)O)[C@H]2[C@](N)(C(=O)O)[C@@H]1OCc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2016.10.067
122190330 130237 0 None 3 2 Rat 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 370 4 0 5 3.4 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ncccc3F)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617514 130237 0 None 3 2 Rat 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 370 4 0 5 3.4 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ncccc3F)nn21 10.1021/acs.jmedchem.5b01005
60204019 97104 0 None - 1 Rat 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 minsNegative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 349 2 1 3 3.1 COc1ccc(C#Cc2ccc(C(=O)N3CCCC(C)(O)C3)cc2)cc1 10.1021/jm400439t
CHEMBL2385883 97104 0 None - 1 Rat 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 minsNegative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 349 2 1 3 3.1 COc1ccc(C#Cc2ccc(C(=O)N3CCCC(C)(O)C3)cc2)cc1 10.1021/jm400439t
21309795 157602 0 None 3 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 327 4 3 3 1.8 N[C@@]1(C(=O)O)[C@H](Cc2ccc(F)c(Cl)c2)C[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.6b01119
CHEMBL3956934 157602 0 None 3 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 327 4 3 3 1.8 N[C@@]1(C(=O)O)[C@H](Cc2ccc(F)c(Cl)c2)C[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.6b01119
122190330 130237 0 None 3 2 Rat 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 370 4 0 5 3.4 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ncccc3F)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617514 130237 0 None 3 2 Rat 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 370 4 0 5 3.4 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ncccc3F)nn21 10.1021/acs.jmedchem.5b01005
60210864 97098 0 None - 1 Rat 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 minsNegative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 335 2 1 3 2.7 COc1ccc(C#Cc2ccc(C(=O)N3CCC[C@H](O)C3)cc2)cc1 10.1021/jm400439t
CHEMBL2385877 97098 0 None - 1 Rat 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 minsNegative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 335 2 1 3 2.7 COc1ccc(C#Cc2ccc(C(=O)N3CCC[C@H](O)C3)cc2)cc1 10.1021/jm400439t
122190328 130235 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 395 6 0 5 4.2 CCOc1ccc(OCc2cc3n(n2)[C@H](C)CN(c2ccc(F)cc2)C3=O)cc1 10.1021/acs.jmedchem.5b01005
CHEMBL3617512 130235 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 395 6 0 5 4.2 CCOc1ccc(OCc2cc3n(n2)[C@H](C)CN(c2ccc(F)cc2)C3=O)cc1 10.1021/acs.jmedchem.5b01005
122190328 130235 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 395 6 0 5 4.2 CCOc1ccc(OCc2cc3n(n2)[C@H](C)CN(c2ccc(F)cc2)C3=O)cc1 10.1021/acs.jmedchem.5b01005
CHEMBL3617512 130235 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 395 6 0 5 4.2 CCOc1ccc(OCc2cc3n(n2)[C@H](C)CN(c2ccc(F)cc2)C3=O)cc1 10.1021/acs.jmedchem.5b01005
122190321 130228 0 None -1 2 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 385 4 0 4 4.5 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ccc(Cl)cc3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617505 130228 0 None -1 2 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 385 4 0 4 4.5 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ccc(Cl)cc3)nn21 10.1021/acs.jmedchem.5b01005
122190321 130228 0 None -1 2 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 385 4 0 4 4.5 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ccc(Cl)cc3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617505 130228 0 None -1 2 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 385 4 0 4 4.5 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ccc(Cl)cc3)nn21 10.1021/acs.jmedchem.5b01005
90643961 118771 0 None 2 2 Rat 5.9 pIC50 = 5.9 Functional
Inhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentrationInhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentration
ChEMBL 382 3 0 6 3.9 COc1cccc(-c2cc3n(C)c(=O)c4ccc(-c5cccnc5)cc4n3n2)c1 10.1016/j.bmcl.2014.04.051
CHEMBL3288649 118771 0 None 2 2 Rat 5.9 pIC50 = 5.9 Functional
Inhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentrationInhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentration
ChEMBL 382 3 0 6 3.9 COc1cccc(-c2cc3n(C)c(=O)c4ccc(-c5cccnc5)cc4n3n2)c1 10.1016/j.bmcl.2014.04.051
122190318 130225 0 None -1 2 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 365 4 0 4 4.1 Cc1ccc(OCc2cc3n(n2)[C@H](C)CN(c2ccc(F)cc2)C3=O)cc1 10.1021/acs.jmedchem.5b01005
CHEMBL3617502 130225 0 None -1 2 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 365 4 0 4 4.1 Cc1ccc(OCc2cc3n(n2)[C@H](C)CN(c2ccc(F)cc2)C3=O)cc1 10.1021/acs.jmedchem.5b01005
69669820 190419 0 None 2 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 396 6 4 5 1.1 CC(=O)N[C@H]1[C@H]2[C@H](C(=O)O)[C@H]2[C@](N)(C(=O)O)[C@@H]1CSc1ccc(F)c(C)c1 10.1021/acs.jmedchem.6b01119
CHEMBL4746125 190419 0 None 2 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 396 6 4 5 1.1 CC(=O)N[C@H]1[C@H]2[C@H](C(=O)O)[C@H]2[C@](N)(C(=O)O)[C@@H]1CSc1ccc(F)c(C)c1 10.1021/acs.jmedchem.6b01119
CHEMBL4802570 190419 0 None 2 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 396 6 4 5 1.1 CC(=O)N[C@H]1[C@H]2[C@H](C(=O)O)[C@H]2[C@](N)(C(=O)O)[C@@H]1CSc1ccc(F)c(C)c1 10.1021/acs.jmedchem.6b01119
10710505 85513 0 None 1 2 Human 5.9 pIC50 = 5.9 Functional
Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3
ChEMBL 316 6 3 4 1.6 Cn1cc(CCC(N)(C(=O)O)[C@H]2C[C@@H]2C(=O)O)c2ccccc21 10.1021/jm970497w
CHEMBL2112580 85513 0 None 1 2 Human 5.9 pIC50 = 5.9 Functional
Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3
ChEMBL 316 6 3 4 1.6 Cn1cc(CCC(N)(C(=O)O)[C@H]2C[C@@H]2C(=O)O)c2ccccc21 10.1021/jm970497w
122190318 130225 0 None -1 2 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 365 4 0 4 4.1 Cc1ccc(OCc2cc3n(n2)[C@H](C)CN(c2ccc(F)cc2)C3=O)cc1 10.1021/acs.jmedchem.5b01005
CHEMBL3617502 130225 0 None -1 2 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 365 4 0 4 4.1 Cc1ccc(OCc2cc3n(n2)[C@H](C)CN(c2ccc(F)cc2)C3=O)cc1 10.1021/acs.jmedchem.5b01005
22448579 162557 0 None -4 2 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat mGluR3 expressed in CHO cells assessed as inhibition of glutamate-induced GIRK currentAntagonist activity at rat mGluR3 expressed in CHO cells assessed as inhibition of glutamate-induced GIRK current
ChEMBL 412 3 2 5 4.8 O=C1CC(c2cccc(-n3ccnc3)c2)=Nc2cc(O)c(-c3ccccc3F)cc2N1 10.1016/j.bmcl.2008.02.076
CHEMBL405895 162557 0 None -4 2 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat mGluR3 expressed in CHO cells assessed as inhibition of glutamate-induced GIRK currentAntagonist activity at rat mGluR3 expressed in CHO cells assessed as inhibition of glutamate-induced GIRK current
ChEMBL 412 3 2 5 4.8 O=C1CC(c2cccc(-n3ccnc3)c2)=Nc2cc(O)c(-c3ccccc3F)cc2N1 10.1016/j.bmcl.2008.02.076
44329031 115051 0 None 6 7 Rat 6.9 pIC50 = 6.9 Functional
Antagonistic activity against metabotropic glutamate receptor 3 (mGluR3) was evaluatedAntagonistic activity against metabotropic glutamate receptor 3 (mGluR3) was evaluated
ChEMBL 437 10 3 4 5.0 CCCCCC[C@@H]1[C@H](C(=O)O)[C@H]1C(N)(CC1c2ccccc2Oc2ccccc21)C(=O)O 10.1016/s0960-894x(98)00510-1
CHEMBL319732 115051 0 None 6 7 Rat 6.9 pIC50 = 6.9 Functional
Antagonistic activity against metabotropic glutamate receptor 3 (mGluR3) was evaluatedAntagonistic activity against metabotropic glutamate receptor 3 (mGluR3) was evaluated
ChEMBL 437 10 3 4 5.0 CCCCCC[C@@H]1[C@H](C(=O)O)[C@H]1C(N)(CC1c2ccccc2Oc2ccccc21)C(=O)O 10.1016/s0960-894x(98)00510-1
122190401 130288 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 388 4 0 5 3.5 C[C@@H]1CN(c2cc(F)ccc2F)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617624 130288 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 388 4 0 5 3.5 C[C@@H]1CN(c2cc(F)ccc2F)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
122190401 130288 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 388 4 0 5 3.5 C[C@@H]1CN(c2cc(F)ccc2F)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617624 130288 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 388 4 0 5 3.5 C[C@@H]1CN(c2cc(F)ccc2F)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
122190411 130298 0 None 2 2 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 402 4 0 5 4.4 C[C@@H]1CN(c2ccc(Cl)cc2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617634 130298 0 None 2 2 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 402 4 0 5 4.4 C[C@@H]1CN(c2ccc(Cl)cc2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
122456006 169073 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assay
ChEMBL 339 6 0 4 3.8 CC(COc1ccn(-c2ccc(F)cc2)c(=O)c1)Oc1ccccc1 10.1021/acsmedchemlett.7b00249
CHEMBL4164219 169073 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assay
ChEMBL 339 6 0 4 3.8 CC(COc1ccn(-c2ccc(F)cc2)c(=O)c1)Oc1ccccc1 10.1021/acsmedchemlett.7b00249
122190411 130298 0 None 2 2 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 402 4 0 5 4.4 C[C@@H]1CN(c2ccc(Cl)cc2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617634 130298 0 None 2 2 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 402 4 0 5 4.4 C[C@@H]1CN(c2ccc(Cl)cc2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
122456006 169073 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assay
ChEMBL 339 6 0 4 3.8 CC(COc1ccn(-c2ccc(F)cc2)c(=O)c1)Oc1ccccc1 10.1021/acsmedchemlett.7b00249
CHEMBL4164219 169073 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assay
ChEMBL 339 6 0 4 3.8 CC(COc1ccn(-c2ccc(F)cc2)c(=O)c1)Oc1ccccc1 10.1021/acsmedchemlett.7b00249
10456810 114656 0 None 7 5 Rat 6.9 pIC50 = 6.9 Functional
Antagonistic activity against metabotropic glutamate receptor 3 (mGluR3) was evaluatedAntagonistic activity against metabotropic glutamate receptor 3 (mGluR3) was evaluated
ChEMBL 457 8 3 4 4.7 NC(CC1c2ccccc2Oc2ccccc21)(C(=O)O)[C@H]1[C@H](CCc2ccccc2)[C@@H]1C(=O)O 10.1016/s0960-894x(98)00510-1
CHEMBL319279 114656 0 None 7 5 Rat 6.9 pIC50 = 6.9 Functional
Antagonistic activity against metabotropic glutamate receptor 3 (mGluR3) was evaluatedAntagonistic activity against metabotropic glutamate receptor 3 (mGluR3) was evaluated
ChEMBL 457 8 3 4 4.7 NC(CC1c2ccccc2Oc2ccccc21)(C(=O)O)[C@H]1[C@H](CCc2ccccc2)[C@@H]1C(=O)O 10.1016/s0960-894x(98)00510-1
90643970 118777 0 None -1 2 Rat 5.9 pIC50 = 5.9 Functional
Inhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentrationInhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentration
ChEMBL 464 3 1 6 3.8 Cn1c(=O)c2ccc(-c3cccc(S(N)(=O)=O)c3)cc2n2nc(-c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2014.04.051
CHEMBL3288664 118777 0 None -1 2 Rat 5.9 pIC50 = 5.9 Functional
Inhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentrationInhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentration
ChEMBL 464 3 1 6 3.8 Cn1c(=O)c2ccc(-c3cccc(S(N)(=O)=O)c3)cc2n2nc(-c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2014.04.051
134129940 149224 0 None 1 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assayAntagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 359 5 4 5 0.5 N[C@@]1(C(=O)O)[C@H](OCc2ccc(Cl)c(F)c2)[C@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1016/j.bmcl.2016.10.067
CHEMBL3890112 149224 0 None 1 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assayAntagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 359 5 4 5 0.5 N[C@@]1(C(=O)O)[C@H](OCc2ccc(Cl)c(F)c2)[C@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1016/j.bmcl.2016.10.067
122190323 130230 0 None 1 2 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 381 5 0 5 3.8 COc1cccc(OCc2cc3n(n2)[C@H](C)CN(c2ccc(F)cc2)C3=O)c1 10.1021/acs.jmedchem.5b01005
CHEMBL3617507 130230 0 None 1 2 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 381 5 0 5 3.8 COc1cccc(OCc2cc3n(n2)[C@H](C)CN(c2ccc(F)cc2)C3=O)c1 10.1021/acs.jmedchem.5b01005
122190323 130230 0 None 1 2 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 381 5 0 5 3.8 COc1cccc(OCc2cc3n(n2)[C@H](C)CN(c2ccc(F)cc2)C3=O)c1 10.1021/acs.jmedchem.5b01005
CHEMBL3617507 130230 0 None 1 2 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 381 5 0 5 3.8 COc1cccc(OCc2cc3n(n2)[C@H](C)CN(c2ccc(F)cc2)C3=O)c1 10.1021/acs.jmedchem.5b01005
53393854 90377 0 None 2 2 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 minsNegative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 335 2 1 3 2.7 COc1ccc(C#Cc2ccc(C(=O)N3CCCC(O)C3)cc2)cc1 10.1021/jm400439t
CHEMBL2204439 90377 0 None 2 2 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 minsNegative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 335 2 1 3 2.7 COc1ccc(C#Cc2ccc(C(=O)N3CCCC(O)C3)cc2)cc1 10.1021/jm400439t
1378 9195 54 None 2 14 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human mGLUR3 expressed in RGT cells assessed as inhibition of (1S,3R)-1-aminocyclopentane-1,3-dicarboxylic acid-induced inhibition of forskolin stimulated cyclic-AMPAntagonist activity at human mGLUR3 expressed in RGT cells assessed as inhibition of (1S,3R)-1-aminocyclopentane-1,3-dicarboxylic acid-induced inhibition of forskolin stimulated cyclic-AMP
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1016/j.bmcl.2012.01.039
1399 9195 54 None 2 14 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human mGLUR3 expressed in RGT cells assessed as inhibition of (1S,3R)-1-aminocyclopentane-1,3-dicarboxylic acid-induced inhibition of forskolin stimulated cyclic-AMPAntagonist activity at human mGLUR3 expressed in RGT cells assessed as inhibition of (1S,3R)-1-aminocyclopentane-1,3-dicarboxylic acid-induced inhibition of forskolin stimulated cyclic-AMP
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1016/j.bmcl.2012.01.039
9819927 9195 54 None 2 14 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human mGLUR3 expressed in RGT cells assessed as inhibition of (1S,3R)-1-aminocyclopentane-1,3-dicarboxylic acid-induced inhibition of forskolin stimulated cyclic-AMPAntagonist activity at human mGLUR3 expressed in RGT cells assessed as inhibition of (1S,3R)-1-aminocyclopentane-1,3-dicarboxylic acid-induced inhibition of forskolin stimulated cyclic-AMP
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1016/j.bmcl.2012.01.039
CHEMBL432038 9195 54 None 2 14 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human mGLUR3 expressed in RGT cells assessed as inhibition of (1S,3R)-1-aminocyclopentane-1,3-dicarboxylic acid-induced inhibition of forskolin stimulated cyclic-AMPAntagonist activity at human mGLUR3 expressed in RGT cells assessed as inhibition of (1S,3R)-1-aminocyclopentane-1,3-dicarboxylic acid-induced inhibition of forskolin stimulated cyclic-AMP
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1016/j.bmcl.2012.01.039
11281280 63182 0 None -1 3 Rat 7.9 pIC50 = 7.9 Functional
Antagonist activity at rat mGluR3 receptor expressed in CHO cells assessed as inhibition of GIRK currentAntagonist activity at rat mGluR3 receptor expressed in CHO cells assessed as inhibition of GIRK current
ChEMBL 409 2 1 3 5.8 Cc1cc(-c2cccc(C3=Nc4cc(C)c(C(F)(F)F)cc4NC(=O)C3)c2)ccn1 10.1016/j.bmcl.2010.09.125
CHEMBL1631859 63182 0 None -1 3 Rat 7.9 pIC50 = 7.9 Functional
Antagonist activity at rat mGluR3 receptor expressed in CHO cells assessed as inhibition of GIRK currentAntagonist activity at rat mGluR3 receptor expressed in CHO cells assessed as inhibition of GIRK current
ChEMBL 409 2 1 3 5.8 Cc1cc(-c2cccc(C3=Nc4cc(C)c(C(F)(F)F)cc4NC(=O)C3)c2)ccn1 10.1016/j.bmcl.2010.09.125
67705376 152117 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assayAntagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 416 6 4 5 1.1 CC(=O)N[C@H]1[C@H]2[C@H](C(=O)O)[C@H]2[C@](N)(C(=O)O)[C@@H]1OCc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2016.10.067
CHEMBL3913414 152117 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assayAntagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 416 6 4 5 1.1 CC(=O)N[C@H]1[C@H]2[C@H](C(=O)O)[C@H]2[C@](N)(C(=O)O)[C@@H]1OCc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2016.10.067
10515174 85506 0 None -1 2 Human 5.9 pIC50 = 5.9 Functional
Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3
ChEMBL 255 5 3 3 1.5 NC(CC1CCCCC1)(C(=O)O)[C@H]1C[C@@H]1C(=O)O 10.1021/jm970497w
CHEMBL2112574 85506 0 None -1 2 Human 5.9 pIC50 = 5.9 Functional
Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3
ChEMBL 255 5 3 3 1.5 NC(CC1CCCCC1)(C(=O)O)[C@H]1C[C@@H]1C(=O)O 10.1021/jm970497w
122190391 130278 0 None 7 2 Rat 6.9 pIC50 = 6.9 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 386 4 0 5 3.9 C[C@@H]1CN(c2ccccc2Cl)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617614 130278 0 None 7 2 Rat 6.9 pIC50 = 6.9 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 386 4 0 5 3.9 C[C@@H]1CN(c2ccccc2Cl)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
122190391 130278 0 None 7 2 Rat 6.9 pIC50 = 6.9 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 386 4 0 5 3.9 C[C@@H]1CN(c2ccccc2Cl)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617614 130278 0 None 7 2 Rat 6.9 pIC50 = 6.9 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 386 4 0 5 3.9 C[C@@H]1CN(c2ccccc2Cl)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
122190392 130279 0 None 12 2 Rat 6.8 pIC50 = 6.8 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 386 4 0 5 3.9 C[C@@H]1CN(c2cccc(Cl)c2)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617615 130279 0 None 12 2 Rat 6.8 pIC50 = 6.8 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 386 4 0 5 3.9 C[C@@H]1CN(c2cccc(Cl)c2)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
122190317 130224 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 365 4 0 4 4.1 Cc1cccc(OCc2cc3n(n2)[C@H](C)CN(c2ccc(F)cc2)C3=O)c1 10.1021/acs.jmedchem.5b01005
CHEMBL3617501 130224 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 365 4 0 4 4.1 Cc1cccc(OCc2cc3n(n2)[C@H](C)CN(c2ccc(F)cc2)C3=O)c1 10.1021/acs.jmedchem.5b01005
122190317 130224 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 365 4 0 4 4.1 Cc1cccc(OCc2cc3n(n2)[C@H](C)CN(c2ccc(F)cc2)C3=O)c1 10.1021/acs.jmedchem.5b01005
CHEMBL3617501 130224 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 365 4 0 4 4.1 Cc1cccc(OCc2cc3n(n2)[C@H](C)CN(c2ccc(F)cc2)C3=O)c1 10.1021/acs.jmedchem.5b01005
122455999 169745 0 None 5 2 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assay
ChEMBL 360 6 0 5 3.5 O=c1cc(OCCOc2cc(Cl)ccn2)ccn1-c1ccc(F)cc1 10.1021/acsmedchemlett.7b00249
CHEMBL4174878 169745 0 None 5 2 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assay
ChEMBL 360 6 0 5 3.5 O=c1cc(OCCOc2cc(Cl)ccn2)ccn1-c1ccc(F)cc1 10.1021/acsmedchemlett.7b00249
134154496 159289 0 None 1 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assayAntagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 341 5 4 5 0.3 N[C@@]1(C(=O)O)[C@H](OCc2ccc(Cl)cc2)[C@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1016/j.bmcl.2016.10.067
CHEMBL3971347 159289 0 None 1 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assayAntagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 341 5 4 5 0.3 N[C@@]1(C(=O)O)[C@H](OCc2ccc(Cl)cc2)[C@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1016/j.bmcl.2016.10.067
122190392 130279 0 None 12 2 Rat 6.8 pIC50 = 6.8 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 386 4 0 5 3.9 C[C@@H]1CN(c2cccc(Cl)c2)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617615 130279 0 None 12 2 Rat 6.8 pIC50 = 6.8 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 386 4 0 5 3.9 C[C@@H]1CN(c2cccc(Cl)c2)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
122455999 169745 0 None 5 2 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assay
ChEMBL 360 6 0 5 3.5 O=c1cc(OCCOc2cc(Cl)ccn2)ccn1-c1ccc(F)cc1 10.1021/acsmedchemlett.7b00249
CHEMBL4174878 169745 0 None 5 2 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assay
ChEMBL 360 6 0 5 3.5 O=c1cc(OCCOc2cc(Cl)ccn2)ccn1-c1ccc(F)cc1 10.1021/acsmedchemlett.7b00249
134132133 151567 0 None 1 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assayAntagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 375 5 4 5 1.0 N[C@@]1(C(=O)O)[C@H](OCc2ccc(Cl)c(Cl)c2)[C@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1016/j.bmcl.2016.10.067
CHEMBL3909237 151567 0 None 1 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assayAntagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 375 5 4 5 1.0 N[C@@]1(C(=O)O)[C@H](OCc2ccc(Cl)c(Cl)c2)[C@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1016/j.bmcl.2016.10.067
71137034 130177 0 None -7 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization after 1.5 hrs by FLIPR assayAntagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization after 1.5 hrs by FLIPR assay
ChEMBL 334 5 4 6 0.3 N[C@@]1(C(=O)O)C[C@@H](Sc2nnc(C(F)F)[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
CHEMBL3616850 130177 0 None -7 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization after 1.5 hrs by FLIPR assayAntagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization after 1.5 hrs by FLIPR assay
ChEMBL 334 5 4 6 0.3 N[C@@]1(C(=O)O)C[C@@H](Sc2nnc(C(F)F)[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
122190340 130247 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 382 5 0 6 3.2 COc1cccc(OCc2cc3n(n2)[C@H](C)CN(c2ccc(F)cc2)C3=O)n1 10.1021/acs.jmedchem.5b01005
CHEMBL3617524 130247 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 382 5 0 6 3.2 COc1cccc(OCc2cc3n(n2)[C@H](C)CN(c2ccc(F)cc2)C3=O)n1 10.1021/acs.jmedchem.5b01005
122190340 130247 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 382 5 0 6 3.2 COc1cccc(OCc2cc3n(n2)[C@H](C)CN(c2ccc(F)cc2)C3=O)n1 10.1021/acs.jmedchem.5b01005
CHEMBL3617524 130247 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 382 5 0 6 3.2 COc1cccc(OCc2cc3n(n2)[C@H](C)CN(c2ccc(F)cc2)C3=O)n1 10.1021/acs.jmedchem.5b01005
10807972 42591 1 None 3 4 Human 7.8 pIC50 = 7.8 Functional
Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3
ChEMBL 353 5 3 4 2.8 N[C@@](CC1c2ccccc2Oc2ccccc21)(C(=O)O)[C@H]1C[C@@H]1C(=O)O 10.1021/jm970497w
CHEMBL144151 42591 1 None 3 4 Human 7.8 pIC50 = 7.8 Functional
Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3
ChEMBL 353 5 3 4 2.8 N[C@@](CC1c2ccccc2Oc2ccccc21)(C(=O)O)[C@H]1C[C@@H]1C(=O)O 10.1021/jm970497w
1378 9195 54 None -2 14 Rat 7.8 pIC50 = 7.8 Functional
Antagonistic activity against metabotropic glutamate receptor 3 (mGluR3) was evaluatedAntagonistic activity against metabotropic glutamate receptor 3 (mGluR3) was evaluated
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1016/s0960-894x(98)00510-1
1399 9195 54 None -2 14 Rat 7.8 pIC50 = 7.8 Functional
Antagonistic activity against metabotropic glutamate receptor 3 (mGluR3) was evaluatedAntagonistic activity against metabotropic glutamate receptor 3 (mGluR3) was evaluated
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1016/s0960-894x(98)00510-1
9819927 9195 54 None -2 14 Rat 7.8 pIC50 = 7.8 Functional
Antagonistic activity against metabotropic glutamate receptor 3 (mGluR3) was evaluatedAntagonistic activity against metabotropic glutamate receptor 3 (mGluR3) was evaluated
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1016/s0960-894x(98)00510-1
CHEMBL432038 9195 54 None -2 14 Rat 7.8 pIC50 = 7.8 Functional
Antagonistic activity against metabotropic glutamate receptor 3 (mGluR3) was evaluatedAntagonistic activity against metabotropic glutamate receptor 3 (mGluR3) was evaluated
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1016/s0960-894x(98)00510-1
67637415 190466 0 None -2 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 438 7 4 7 1.9 Cc1cc(SC[C@@H]2[C@@H](Sc3nc[nH]n3)[C@H]3[C@H](C(=O)O)[C@H]3[C@]2(N)C(=O)O)ccc1F 10.1021/acs.jmedchem.6b01119
CHEMBL4759992 190466 0 None -2 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 438 7 4 7 1.9 Cc1cc(SC[C@@H]2[C@@H](Sc3nc[nH]n3)[C@H]3[C@H](C(=O)O)[C@H]3[C@]2(N)C(=O)O)ccc1F 10.1021/acs.jmedchem.6b01119
CHEMBL4803099 190466 0 None -2 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 438 7 4 7 1.9 Cc1cc(SC[C@@H]2[C@@H](Sc3nc[nH]n3)[C@H]3[C@H](C(=O)O)[C@H]3[C@]2(N)C(=O)O)ccc1F 10.1021/acs.jmedchem.6b01119
44348939 125272 0 None 2 2 Human 6.8 pIC50 = 6.8 Functional
Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3
ChEMBL 293 7 3 4 1.1 COc1cccc(CC[C@](N)(C(=O)O)C2C[C@@H]2C(=O)O)c1 10.1021/jm970498o
CHEMBL341457 125272 0 None 2 2 Human 6.8 pIC50 = 6.8 Functional
Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3
ChEMBL 293 7 3 4 1.1 COc1cccc(CC[C@](N)(C(=O)O)C2C[C@@H]2C(=O)O)c1 10.1021/jm970498o
44302608 107623 0 None 2 2 Human 4.8 pIC50 = 4.8 Functional
In vitro antagonist activity at recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.In vitro antagonist activity at recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.
ChEMBL 340 5 3 4 1.8 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2ccccc2-c2ccccc2)C1 10.1016/s0960-894x(98)00352-7
CHEMBL293434 107623 0 None 2 2 Human 4.8 pIC50 = 4.8 Functional
In vitro antagonist activity at recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.In vitro antagonist activity at recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.
ChEMBL 340 5 3 4 1.8 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2ccccc2-c2ccccc2)C1 10.1016/s0960-894x(98)00352-7
122190389 130276 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 370 4 0 5 3.4 C[C@@H]1CN(c2ccccc2F)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617612 130276 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 370 4 0 5 3.4 C[C@@H]1CN(c2ccccc2F)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
122190389 130276 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 370 4 0 5 3.4 C[C@@H]1CN(c2ccccc2F)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617612 130276 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 370 4 0 5 3.4 C[C@@H]1CN(c2ccccc2F)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
122190320 130227 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 385 4 0 4 4.5 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3cccc(Cl)c3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617504 130227 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 385 4 0 4 4.5 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3cccc(Cl)c3)nn21 10.1021/acs.jmedchem.5b01005
122190320 130227 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 385 4 0 4 4.5 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3cccc(Cl)c3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617504 130227 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 385 4 0 4 4.5 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3cccc(Cl)c3)nn21 10.1021/acs.jmedchem.5b01005
69669702 190454 0 None -3 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 354 5 4 5 0.9 Cc1cc(SC[C@@H]2[C@@H](N)[C@H]3[C@H](C(=O)O)[C@H]3[C@]2(N)C(=O)O)ccc1F 10.1021/acs.jmedchem.6b01119
CHEMBL4756556 190454 0 None -3 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 354 5 4 5 0.9 Cc1cc(SC[C@@H]2[C@@H](N)[C@H]3[C@H](C(=O)O)[C@H]3[C@]2(N)C(=O)O)ccc1F 10.1021/acs.jmedchem.6b01119
CHEMBL4802948 190454 0 None -3 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 354 5 4 5 0.9 Cc1cc(SC[C@@H]2[C@@H](N)[C@H]3[C@H](C(=O)O)[C@H]3[C@]2(N)C(=O)O)ccc1F 10.1021/acs.jmedchem.6b01119
90643956 118768 0 None 5 2 Rat 6.8 pIC50 = 6.8 Functional
Inhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentrationInhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentration
ChEMBL 352 2 0 5 3.9 Cn1c(=O)c2ccc(-c3cccnc3)cc2n2nc(-c3ccccc3)cc12 10.1016/j.bmcl.2014.04.051
CHEMBL3288639 118768 0 None 5 2 Rat 6.8 pIC50 = 6.8 Functional
Inhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentrationInhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentration
ChEMBL 352 2 0 5 3.9 Cn1c(=O)c2ccc(-c3cccnc3)cc2n2nc(-c3ccccc3)cc12 10.1016/j.bmcl.2014.04.051
122190334 130241 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 420 4 0 5 4.2 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3cc(C(F)(F)F)ccn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617518 130241 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 420 4 0 5 4.2 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3cc(C(F)(F)F)ccn3)nn21 10.1021/acs.jmedchem.5b01005
122190334 130241 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 420 4 0 5 4.2 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3cc(C(F)(F)F)ccn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617518 130241 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 420 4 0 5 4.2 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3cc(C(F)(F)F)ccn3)nn21 10.1021/acs.jmedchem.5b01005
60210864 97098 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 minsNegative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 335 2 1 3 2.7 COc1ccc(C#Cc2ccc(C(=O)N3CCC[C@H](O)C3)cc2)cc1 10.1021/jm400439t
CHEMBL2385877 97098 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 minsNegative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 335 2 1 3 2.7 COc1ccc(C#Cc2ccc(C(=O)N3CCC[C@H](O)C3)cc2)cc1 10.1021/jm400439t
22224852 102639 0 None 2 2 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity at rat mGluR3 expressed in CHO cells assessed as inhibition of glutamate-induced GIRK currentAntagonist activity at rat mGluR3 expressed in CHO cells assessed as inhibition of glutamate-induced GIRK current
ChEMBL 396 3 1 4 5.1 O=C1CC(c2cccc(-n3ccnc3)c2)=Nc2ccc(-c3ccc(F)cc3)cc2N1 10.1016/j.bmcl.2008.02.076
CHEMBL259054 102639 0 None 2 2 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity at rat mGluR3 expressed in CHO cells assessed as inhibition of glutamate-induced GIRK currentAntagonist activity at rat mGluR3 expressed in CHO cells assessed as inhibition of glutamate-induced GIRK current
ChEMBL 396 3 1 4 5.1 O=C1CC(c2cccc(-n3ccnc3)c2)=Nc2ccc(-c3ccc(F)cc3)cc2N1 10.1016/j.bmcl.2008.02.076
11211597 63082 0 None 1 3 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity at rat mGluR3 receptor expressed in CHO cells assessed as inhibition of GIRK currentAntagonist activity at rat mGluR3 receptor expressed in CHO cells assessed as inhibition of GIRK current
ChEMBL 395 2 1 3 5.5 Cc1cc(-c2cccc(C3=Nc4ccc(C(F)(F)F)cc4NC(=O)C3)c2)ccn1 10.1016/j.bmcl.2010.09.125
CHEMBL1629865 63082 0 None 1 3 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity at rat mGluR3 receptor expressed in CHO cells assessed as inhibition of GIRK currentAntagonist activity at rat mGluR3 receptor expressed in CHO cells assessed as inhibition of GIRK current
ChEMBL 395 2 1 3 5.5 Cc1cc(-c2cccc(C3=Nc4ccc(C(F)(F)F)cc4NC(=O)C3)c2)ccn1 10.1016/j.bmcl.2010.09.125
10688450 23376 0 None 1 2 Human 6.8 pIC50 = 6.8 Functional
Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3
ChEMBL 339 7 3 3 2.7 N[C@](CC(c1ccccc1)c1ccccc1)(C(=O)O)[C@H]1C[C@@H]1C(=O)O 10.1021/jm970498o
CHEMBL124078 23376 0 None 1 2 Human 6.8 pIC50 = 6.8 Functional
Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3
ChEMBL 339 7 3 3 2.7 N[C@](CC(c1ccccc1)c1ccccc1)(C(=O)O)[C@H]1C[C@@H]1C(=O)O 10.1021/jm970498o
134144441 157173 0 None 1 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assayAntagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 341 5 4 5 0.3 N[C@@]1(C(=O)O)[C@H](OCc2cccc(Cl)c2)[C@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1016/j.bmcl.2016.10.067
CHEMBL3953570 157173 0 None 1 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assayAntagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 341 5 4 5 0.3 N[C@@]1(C(=O)O)[C@H](OCc2cccc(Cl)c2)[C@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1016/j.bmcl.2016.10.067
44348993 121363 0 None -1 2 Human 6.8 pIC50 = 6.8 Functional
Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3
ChEMBL 297 6 3 3 1.8 N[C@@](CCc1cccc(Cl)c1)(C(=O)O)C1C[C@@H]1C(=O)O 10.1021/jm970498o
CHEMBL333771 121363 0 None -1 2 Human 6.8 pIC50 = 6.8 Functional
Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3
ChEMBL 297 6 3 3 1.8 N[C@@](CCc1cccc(Cl)c1)(C(=O)O)C1C[C@@H]1C(=O)O 10.1021/jm970498o
44348846 123790 0 None 1 2 Human 6.8 pIC50 = 6.8 Functional
Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3
ChEMBL 341 7 3 5 0.5 CS(=O)(=O)c1cccc(CC[C@](N)(C(=O)O)C2C[C@@H]2C(=O)O)c1 10.1021/jm970498o
CHEMBL2111822 123790 0 None 1 2 Human 6.8 pIC50 = 6.8 Functional
Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3
ChEMBL 341 7 3 5 0.5 CS(=O)(=O)c1cccc(CC[C@](N)(C(=O)O)C2C[C@@H]2C(=O)O)c1 10.1021/jm970498o
CHEMBL338911 123790 0 None 1 2 Human 6.8 pIC50 = 6.8 Functional
Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3
ChEMBL 341 7 3 5 0.5 CS(=O)(=O)c1cccc(CC[C@](N)(C(=O)O)C2C[C@@H]2C(=O)O)c1 10.1021/jm970498o
122456206 169005 0 None 1 2 Rat 6.8 pIC50 = 6.8 Functional
Negative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assay
ChEMBL 343 6 0 4 3.6 O=c1cc(OCCOc2ccccc2)ccn1-c1ccc(F)c(F)c1 10.1021/acsmedchemlett.7b00249
CHEMBL4163186 169005 0 None 1 2 Rat 6.8 pIC50 = 6.8 Functional
Negative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assay
ChEMBL 343 6 0 4 3.6 O=c1cc(OCCOc2ccccc2)ccn1-c1ccc(F)c(F)c1 10.1021/acsmedchemlett.7b00249
44345358 120127 0 None -1 2 Human 5.8 pIC50 = 5.8 Functional
Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3
ChEMBL 215 5 3 3 0.5 CC(C)C[C@](N)(C(=O)O)C1C[C@@H]1C(=O)O 10.1021/jm970497w
CHEMBL331753 120127 0 None -1 2 Human 5.8 pIC50 = 5.8 Functional
Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3
ChEMBL 215 5 3 3 0.5 CC(C)C[C@](N)(C(=O)O)C1C[C@@H]1C(=O)O 10.1021/jm970497w
122190402 130289 0 None 6 2 Rat 6.7 pIC50 = 6.7 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 388 4 0 5 3.5 C[C@@H]1CN(c2c(F)cccc2F)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617625 130289 0 None 6 2 Rat 6.7 pIC50 = 6.7 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 388 4 0 5 3.5 C[C@@H]1CN(c2c(F)cccc2F)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
122190402 130289 0 None 6 2 Rat 6.7 pIC50 = 6.7 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 388 4 0 5 3.5 C[C@@H]1CN(c2c(F)cccc2F)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617625 130289 0 None 6 2 Rat 6.7 pIC50 = 6.7 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 388 4 0 5 3.5 C[C@@H]1CN(c2c(F)cccc2F)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
122456206 169005 0 None 1 2 Rat 6.7 pIC50 = 6.7 Functional
Negative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assay
ChEMBL 343 6 0 4 3.6 O=c1cc(OCCOc2ccccc2)ccn1-c1ccc(F)c(F)c1 10.1021/acsmedchemlett.7b00249
CHEMBL4163186 169005 0 None 1 2 Rat 6.7 pIC50 = 6.7 Functional
Negative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assay
ChEMBL 343 6 0 4 3.6 O=c1cc(OCCOc2ccccc2)ccn1-c1ccc(F)c(F)c1 10.1021/acsmedchemlett.7b00249
122190400 130287 0 None 11 2 Rat 6.7 pIC50 = 6.7 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 388 4 0 5 3.5 C[C@@H]1CN(c2cccc(F)c2F)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617623 130287 0 None 11 2 Rat 6.7 pIC50 = 6.7 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 388 4 0 5 3.5 C[C@@H]1CN(c2cccc(F)c2F)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
134152341 160242 0 None 2 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assayAntagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 375 5 4 5 1.0 N[C@@]1(C(=O)O)[C@H](OCc2cc(Cl)ccc2Cl)[C@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1016/j.bmcl.2016.10.067
CHEMBL3979475 160242 0 None 2 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assayAntagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 375 5 4 5 1.0 N[C@@]1(C(=O)O)[C@H](OCc2cc(Cl)ccc2Cl)[C@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1016/j.bmcl.2016.10.067
122190325 130232 0 None - 1 Rat 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 419 4 0 4 4.8 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ccc(C(F)(F)F)cc3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617509 130232 0 None - 1 Rat 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 419 4 0 4 4.8 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ccc(C(F)(F)F)cc3)nn21 10.1021/acs.jmedchem.5b01005
122190400 130287 0 None 11 2 Rat 6.7 pIC50 = 6.7 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 388 4 0 5 3.5 C[C@@H]1CN(c2cccc(F)c2F)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617623 130287 0 None 11 2 Rat 6.7 pIC50 = 6.7 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 388 4 0 5 3.5 C[C@@H]1CN(c2cccc(F)c2F)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
122190325 130232 0 None - 1 Rat 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 419 4 0 4 4.8 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ccc(C(F)(F)F)cc3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617509 130232 0 None - 1 Rat 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 419 4 0 4 4.8 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ccc(C(F)(F)F)cc3)nn21 10.1021/acs.jmedchem.5b01005
122190390 130277 0 None 14 2 Rat 6.7 pIC50 = 6.7 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 370 4 0 5 3.4 C[C@@H]1CN(c2cccc(F)c2)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617613 130277 0 None 14 2 Rat 6.7 pIC50 = 6.7 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 370 4 0 5 3.4 C[C@@H]1CN(c2cccc(F)c2)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
122190390 130277 0 None 14 2 Rat 6.7 pIC50 = 6.7 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 370 4 0 5 3.4 C[C@@H]1CN(c2cccc(F)c2)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617613 130277 0 None 14 2 Rat 6.7 pIC50 = 6.7 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 370 4 0 5 3.4 C[C@@H]1CN(c2cccc(F)c2)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
122190393 130280 0 None 1 2 Rat 6.7 pIC50 = 6.7 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 386 4 0 5 3.9 C[C@@H]1CN(c2ccc(Cl)cc2)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617616 130280 0 None 1 2 Rat 6.7 pIC50 = 6.7 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 386 4 0 5 3.9 C[C@@H]1CN(c2ccc(Cl)cc2)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
44329024 215137 0 None 11 3 Rat 6.7 pIC50 = 6.7 Functional
Antagonistic activity against metabotropic glutamate receptor 3 (mGluR3) was evaluatedAntagonistic activity against metabotropic glutamate receptor 3 (mGluR3) was evaluated
ChEMBL 395 7 3 4 3.8 CCC[C@@H]1[C@H](C(=O)O)[C@H]1C(N)(CC1c2ccccc2Oc2ccccc21)C(=O)O 10.1016/s0960-894x(98)00510-1
CHEMBL99462 215137 0 None 11 3 Rat 6.7 pIC50 = 6.7 Functional
Antagonistic activity against metabotropic glutamate receptor 3 (mGluR3) was evaluatedAntagonistic activity against metabotropic glutamate receptor 3 (mGluR3) was evaluated
ChEMBL 395 7 3 4 3.8 CCC[C@@H]1[C@H](C(=O)O)[C@H]1C(N)(CC1c2ccccc2Oc2ccccc21)C(=O)O 10.1016/s0960-894x(98)00510-1
122190393 130280 0 None 1 2 Rat 6.7 pIC50 = 6.7 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 386 4 0 5 3.9 C[C@@H]1CN(c2ccc(Cl)cc2)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617616 130280 0 None 1 2 Rat 6.7 pIC50 = 6.7 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 386 4 0 5 3.9 C[C@@H]1CN(c2ccc(Cl)cc2)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
122190398 130285 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 382 5 0 6 3.2 COc1cccc(N2C[C@@H](C)n3nc(COc4ccc(F)cn4)cc3C2=O)c1 10.1021/acs.jmedchem.5b01005
CHEMBL3617621 130285 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 382 5 0 6 3.2 COc1cccc(N2C[C@@H](C)n3nc(COc4ccc(F)cn4)cc3C2=O)c1 10.1021/acs.jmedchem.5b01005
122190398 130285 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 382 5 0 6 3.2 COc1cccc(N2C[C@@H](C)n3nc(COc4ccc(F)cn4)cc3C2=O)c1 10.1021/acs.jmedchem.5b01005
CHEMBL3617621 130285 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 382 5 0 6 3.2 COc1cccc(N2C[C@@H](C)n3nc(COc4ccc(F)cn4)cc3C2=O)c1 10.1021/acs.jmedchem.5b01005
90643966 118775 0 None 1 2 Rat 5.7 pIC50 = 5.7 Functional
Inhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentrationInhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentration
ChEMBL 448 3 1 6 3.3 Cn1c(=O)c2ccc(-c3cccc(S(N)(=O)=O)c3)cc2n2nc(-c3ccc(F)cc3)cc12 10.1016/j.bmcl.2014.04.051
CHEMBL3288660 118775 0 None 1 2 Rat 5.7 pIC50 = 5.7 Functional
Inhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentrationInhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentration
ChEMBL 448 3 1 6 3.3 Cn1c(=O)c2ccc(-c3cccc(S(N)(=O)=O)c3)cc2n2nc(-c3ccc(F)cc3)cc12 10.1016/j.bmcl.2014.04.051
69669747 190432 11 None 2 4 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human recombinant mGlu3 stably expressed in golden hamster AV12 cell membrane co-expressing Galpha15 assessed as assessed as reduction in glutamate-induced calcium influx incubated for 90 to 120 min by Fluo-4-AM dye based FLIPR assayAntagonist activity at human recombinant mGlu3 stably expressed in golden hamster AV12 cell membrane co-expressing Galpha15 assessed as assessed as reduction in glutamate-induced calcium influx incubated for 90 to 120 min by Fluo-4-AM dye based FLIPR assay
ChEMBL 359 5 4 5 0.8 N[C@@]1(C(=O)O)[C@H](CSc2ccc(F)c(F)c2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
CHEMBL4751065 190432 11 None 2 4 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human recombinant mGlu3 stably expressed in golden hamster AV12 cell membrane co-expressing Galpha15 assessed as assessed as reduction in glutamate-induced calcium influx incubated for 90 to 120 min by Fluo-4-AM dye based FLIPR assayAntagonist activity at human recombinant mGlu3 stably expressed in golden hamster AV12 cell membrane co-expressing Galpha15 assessed as assessed as reduction in glutamate-induced calcium influx incubated for 90 to 120 min by Fluo-4-AM dye based FLIPR assay
ChEMBL 359 5 4 5 0.8 N[C@@]1(C(=O)O)[C@H](CSc2ccc(F)c(F)c2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
CHEMBL4802733 190432 11 None 2 4 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human recombinant mGlu3 stably expressed in golden hamster AV12 cell membrane co-expressing Galpha15 assessed as assessed as reduction in glutamate-induced calcium influx incubated for 90 to 120 min by Fluo-4-AM dye based FLIPR assayAntagonist activity at human recombinant mGlu3 stably expressed in golden hamster AV12 cell membrane co-expressing Galpha15 assessed as assessed as reduction in glutamate-induced calcium influx incubated for 90 to 120 min by Fluo-4-AM dye based FLIPR assay
ChEMBL 359 5 4 5 0.8 N[C@@]1(C(=O)O)[C@H](CSc2ccc(F)c(F)c2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
1378 9195 54 None 2 14 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human recombinant mGlu3 stably expressed in golden hamster AV12 cell membrane co-expressing Galpha15 assessed as assessed as reduction in glutamate-induced calcium influx incubated for 90 to 120 min by Fluo-4-AM dye based FLIPR assayAntagonist activity at human recombinant mGlu3 stably expressed in golden hamster AV12 cell membrane co-expressing Galpha15 assessed as assessed as reduction in glutamate-induced calcium influx incubated for 90 to 120 min by Fluo-4-AM dye based FLIPR assay
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/acs.jmedchem.6b01119
1399 9195 54 None 2 14 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human recombinant mGlu3 stably expressed in golden hamster AV12 cell membrane co-expressing Galpha15 assessed as assessed as reduction in glutamate-induced calcium influx incubated for 90 to 120 min by Fluo-4-AM dye based FLIPR assayAntagonist activity at human recombinant mGlu3 stably expressed in golden hamster AV12 cell membrane co-expressing Galpha15 assessed as assessed as reduction in glutamate-induced calcium influx incubated for 90 to 120 min by Fluo-4-AM dye based FLIPR assay
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/acs.jmedchem.6b01119
9819927 9195 54 None 2 14 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human recombinant mGlu3 stably expressed in golden hamster AV12 cell membrane co-expressing Galpha15 assessed as assessed as reduction in glutamate-induced calcium influx incubated for 90 to 120 min by Fluo-4-AM dye based FLIPR assayAntagonist activity at human recombinant mGlu3 stably expressed in golden hamster AV12 cell membrane co-expressing Galpha15 assessed as assessed as reduction in glutamate-induced calcium influx incubated for 90 to 120 min by Fluo-4-AM dye based FLIPR assay
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/acs.jmedchem.6b01119
CHEMBL432038 9195 54 None 2 14 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human recombinant mGlu3 stably expressed in golden hamster AV12 cell membrane co-expressing Galpha15 assessed as assessed as reduction in glutamate-induced calcium influx incubated for 90 to 120 min by Fluo-4-AM dye based FLIPR assayAntagonist activity at human recombinant mGlu3 stably expressed in golden hamster AV12 cell membrane co-expressing Galpha15 assessed as assessed as reduction in glutamate-induced calcium influx incubated for 90 to 120 min by Fluo-4-AM dye based FLIPR assay
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/acs.jmedchem.6b01119
67707808 155421 0 None -1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assayAntagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 432 6 4 6 1.3 COC(=O)N[C@H]1[C@H]2[C@H](C(=O)O)[C@H]2[C@](N)(C(=O)O)[C@@H]1OCc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2016.10.067
CHEMBL3939492 155421 0 None -1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assayAntagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 432 6 4 6 1.3 COC(=O)N[C@H]1[C@H]2[C@H](C(=O)O)[C@H]2[C@](N)(C(=O)O)[C@@H]1OCc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2016.10.067
44348859 23336 0 None 15 2 Human 6.7 pIC50 = 6.7 Functional
Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3
ChEMBL 278 6 4 4 0.7 Nc1cccc(CC[C@](N)(C(=O)O)C2C[C@@H]2C(=O)O)c1 10.1021/jm970498o
CHEMBL123842 23336 0 None 15 2 Human 6.7 pIC50 = 6.7 Functional
Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3
ChEMBL 278 6 4 4 0.7 Nc1cccc(CC[C@](N)(C(=O)O)C2C[C@@H]2C(=O)O)c1 10.1021/jm970498o
162658781 190470 0 None -1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 323 5 4 5 0.5 N[C@@]1(C(=O)O)[C@H](CSc2ccccc2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
CHEMBL4759209 190470 0 None -1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 323 5 4 5 0.5 N[C@@]1(C(=O)O)[C@H](CSc2ccccc2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
CHEMBL4803105 190470 0 None -1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 323 5 4 5 0.5 N[C@@]1(C(=O)O)[C@H](CSc2ccccc2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
122190408 130295 0 None 29 2 Rat 6.7 pIC50 = 6.7 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 386 4 0 5 3.9 C[C@@H]1CN(c2cccc(F)c2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617631 130295 0 None 29 2 Rat 6.7 pIC50 = 6.7 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 386 4 0 5 3.9 C[C@@H]1CN(c2cccc(F)c2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
137634033 163420 0 None 1 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human mGlu3 receptor expressed in HEK cells assessed as reversal of DCG-4 inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assayAntagonist activity at human mGlu3 receptor expressed in HEK cells assessed as reversal of DCG-4 inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 332 6 4 4 0.2 N[C@@]1(C(=O)O)C[C@H](NC(=O)CCc2ccccc2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
CHEMBL4069251 163420 0 None 1 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human mGlu3 receptor expressed in HEK cells assessed as reversal of DCG-4 inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assayAntagonist activity at human mGlu3 receptor expressed in HEK cells assessed as reversal of DCG-4 inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 332 6 4 4 0.2 N[C@@]1(C(=O)O)C[C@H](NC(=O)CCc2ccccc2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
122190408 130295 0 None 29 2 Rat 6.7 pIC50 = 6.7 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 386 4 0 5 3.9 C[C@@H]1CN(c2cccc(F)c2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617631 130295 0 None 29 2 Rat 6.7 pIC50 = 6.7 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 386 4 0 5 3.9 C[C@@H]1CN(c2cccc(F)c2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
122190333 130240 0 None - 1 Rat 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 366 4 0 5 3.5 Cc1ccnc(OCc2cc3n(n2)[C@H](C)CN(c2ccc(F)cc2)C3=O)c1 10.1021/acs.jmedchem.5b01005
CHEMBL3617517 130240 0 None - 1 Rat 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 366 4 0 5 3.5 Cc1ccnc(OCc2cc3n(n2)[C@H](C)CN(c2ccc(F)cc2)C3=O)c1 10.1021/acs.jmedchem.5b01005
122190333 130240 0 None - 1 Rat 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 366 4 0 5 3.5 Cc1ccnc(OCc2cc3n(n2)[C@H](C)CN(c2ccc(F)cc2)C3=O)c1 10.1021/acs.jmedchem.5b01005
CHEMBL3617517 130240 0 None - 1 Rat 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 366 4 0 5 3.5 Cc1ccnc(OCc2cc3n(n2)[C@H](C)CN(c2ccc(F)cc2)C3=O)c1 10.1021/acs.jmedchem.5b01005
44348706 123660 0 None -1 2 Human 6.7 pIC50 = 6.7 Functional
Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3
ChEMBL 281 6 3 3 1.3 N[C@@](CCc1ccc(F)cc1)(C(=O)O)C1C[C@@H]1C(=O)O 10.1021/jm970498o
CHEMBL338282 123660 0 None -1 2 Human 6.7 pIC50 = 6.7 Functional
Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3
ChEMBL 281 6 3 3 1.3 N[C@@](CCc1ccc(F)cc1)(C(=O)O)C1C[C@@H]1C(=O)O 10.1021/jm970498o
10091203 19723 0 None 1 3 Rat 4.7 pIC50 = 4.7 Functional
Inhibitory concentration required for antagonistic activity at Metabotropic glutamate receptor 3Inhibitory concentration required for antagonistic activity at Metabotropic glutamate receptor 3
ChEMBL 308 5 4 5 -0.2 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(C(C(=O)O)c2ccccc2)C1 10.1016/s0960-894x(01)00329-8
CHEMBL1189303 19723 0 None 1 3 Rat 4.7 pIC50 = 4.7 Functional
Inhibitory concentration required for antagonistic activity at Metabotropic glutamate receptor 3Inhibitory concentration required for antagonistic activity at Metabotropic glutamate receptor 3
ChEMBL 308 5 4 5 -0.2 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(C(C(=O)O)c2ccccc2)C1 10.1016/s0960-894x(01)00329-8
CHEMBL538489 19723 0 None 1 3 Rat 4.7 pIC50 = 4.7 Functional
Inhibitory concentration required for antagonistic activity at Metabotropic glutamate receptor 3Inhibitory concentration required for antagonistic activity at Metabotropic glutamate receptor 3
ChEMBL 308 5 4 5 -0.2 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(C(C(=O)O)c2ccccc2)C1 10.1016/s0960-894x(01)00329-8
122190395 130282 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 366 4 0 5 3.5 Cc1cccc(N2C[C@@H](C)n3nc(COc4ccc(F)cn4)cc3C2=O)c1 10.1021/acs.jmedchem.5b01005
CHEMBL3617618 130282 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 366 4 0 5 3.5 Cc1cccc(N2C[C@@H](C)n3nc(COc4ccc(F)cn4)cc3C2=O)c1 10.1021/acs.jmedchem.5b01005
122190395 130282 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 366 4 0 5 3.5 Cc1cccc(N2C[C@@H](C)n3nc(COc4ccc(F)cn4)cc3C2=O)c1 10.1021/acs.jmedchem.5b01005
CHEMBL3617618 130282 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 366 4 0 5 3.5 Cc1cccc(N2C[C@@H](C)n3nc(COc4ccc(F)cn4)cc3C2=O)c1 10.1021/acs.jmedchem.5b01005
162663798 190498 0 None -1 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 323 5 4 5 0.5 N[C@]1(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@@H]2[C@@H](O)[C@@H]1CSc1ccccc1 10.1021/acs.jmedchem.6b01119
CHEMBL4779554 190498 0 None -1 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 323 5 4 5 0.5 N[C@]1(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@@H]2[C@@H](O)[C@@H]1CSc1ccccc1 10.1021/acs.jmedchem.6b01119
CHEMBL4803378 190498 0 None -1 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 323 5 4 5 0.5 N[C@]1(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@@H]2[C@@H](O)[C@@H]1CSc1ccccc1 10.1021/acs.jmedchem.6b01119
122190407 130294 0 None 14 2 Rat 6.7 pIC50 = 6.7 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 386 4 0 5 3.9 C[C@@H]1CN(c2ccccc2F)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617630 130294 0 None 14 2 Rat 6.7 pIC50 = 6.7 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 386 4 0 5 3.9 C[C@@H]1CN(c2ccccc2F)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
122190423 130310 0 None 6 2 Rat 6.7 pIC50 = 6.7 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 404 4 0 5 4.0 C[C@@H]1CN(c2c(F)cccc2F)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617646 130310 0 None 6 2 Rat 6.7 pIC50 = 6.7 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 404 4 0 5 4.0 C[C@@H]1CN(c2c(F)cccc2F)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
122190423 130310 0 None 6 2 Rat 6.7 pIC50 = 6.7 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 404 4 0 5 4.0 C[C@@H]1CN(c2c(F)cccc2F)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617646 130310 0 None 6 2 Rat 6.7 pIC50 = 6.7 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 404 4 0 5 4.0 C[C@@H]1CN(c2c(F)cccc2F)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
122190407 130294 0 None 14 2 Rat 6.7 pIC50 = 6.7 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 386 4 0 5 3.9 C[C@@H]1CN(c2ccccc2F)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617630 130294 0 None 14 2 Rat 6.7 pIC50 = 6.7 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 386 4 0 5 3.9 C[C@@H]1CN(c2ccccc2F)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
67705089 159034 0 None -1 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assayAntagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 458 7 4 7 1.9 N[C@@]1(C(=O)O)[C@H](OCc2ccc(Cl)c(Cl)c2)[C@@H](Sc2nc[nH]n2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1016/j.bmcl.2016.10.067
CHEMBL3969063 159034 0 None -1 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assayAntagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 458 7 4 7 1.9 N[C@@]1(C(=O)O)[C@H](OCc2ccc(Cl)c(Cl)c2)[C@@H](Sc2nc[nH]n2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1016/j.bmcl.2016.10.067
10250423 19785 0 None 1 2 Rat 4.6 pIC50 = 4.6 Functional
Inhibitory concentration required for antagonistic activity at Metabotropic glutamate receptor 3Inhibitory concentration required for antagonistic activity at Metabotropic glutamate receptor 3
ChEMBL 364 4 3 4 1.5 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2ccccc2C#Cc2ccccc2)C1 10.1016/s0960-894x(01)00329-8
CHEMBL1189797 19785 0 None 1 2 Rat 4.6 pIC50 = 4.6 Functional
Inhibitory concentration required for antagonistic activity at Metabotropic glutamate receptor 3Inhibitory concentration required for antagonistic activity at Metabotropic glutamate receptor 3
ChEMBL 364 4 3 4 1.5 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2ccccc2C#Cc2ccccc2)C1 10.1016/s0960-894x(01)00329-8
CHEMBL539516 19785 0 None 1 2 Rat 4.6 pIC50 = 4.6 Functional
Inhibitory concentration required for antagonistic activity at Metabotropic glutamate receptor 3Inhibitory concentration required for antagonistic activity at Metabotropic glutamate receptor 3
ChEMBL 364 4 3 4 1.5 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2ccccc2C#Cc2ccccc2)C1 10.1016/s0960-894x(01)00329-8
122190339 130246 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 420 4 0 5 4.2 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3cccc(C(F)(F)F)n3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617523 130246 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 420 4 0 5 4.2 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3cccc(C(F)(F)F)n3)nn21 10.1021/acs.jmedchem.5b01005
71136654 130186 0 None -3 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization after 1.5 hrs by FLIPR assayAntagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization after 1.5 hrs by FLIPR assay
ChEMBL 326 5 4 6 0.5 CC(C)c1nnc(S[C@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)[nH]1 10.1021/acs.jmedchem.5b01124
CHEMBL3616859 130186 0 None -3 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization after 1.5 hrs by FLIPR assayAntagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization after 1.5 hrs by FLIPR assay
ChEMBL 326 5 4 6 0.5 CC(C)c1nnc(S[C@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)[nH]1 10.1021/acs.jmedchem.5b01124
122190339 130246 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 420 4 0 5 4.2 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3cccc(C(F)(F)F)n3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617523 130246 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 420 4 0 5 4.2 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3cccc(C(F)(F)F)n3)nn21 10.1021/acs.jmedchem.5b01005
122190338 130245 0 None -1 2 Rat 5.6 pIC50 = 5.6 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 366 4 0 5 3.5 Cc1cccc(OCc2cc3n(n2)[C@H](C)CN(c2ccc(F)cc2)C3=O)n1 10.1021/acs.jmedchem.5b01005
CHEMBL3617522 130245 0 None -1 2 Rat 5.6 pIC50 = 5.6 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 366 4 0 5 3.5 Cc1cccc(OCc2cc3n(n2)[C@H](C)CN(c2ccc(F)cc2)C3=O)n1 10.1021/acs.jmedchem.5b01005
71136640 130180 0 None -60 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as reversal of DCG-4-inhibited, forskolin-stimulated cAMP production after 1 hr by fluorescence assayAntagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as reversal of DCG-4-inhibited, forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 284 4 4 6 -0.6 N[C@@]1(C(=O)O)C[C@@H](Sc2c[nH]nn2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
CHEMBL3616853 130180 0 None -60 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as reversal of DCG-4-inhibited, forskolin-stimulated cAMP production after 1 hr by fluorescence assayAntagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as reversal of DCG-4-inhibited, forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 284 4 4 6 -0.6 N[C@@]1(C(=O)O)C[C@@H](Sc2c[nH]nn2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
134144056 157416 0 None 1 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assayAntagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 307 5 4 5 -0.3 N[C@@]1(C(=O)O)[C@H](OCc2ccccc2)[C@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1016/j.bmcl.2016.10.067
CHEMBL3955458 157416 0 None 1 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assayAntagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 307 5 4 5 -0.3 N[C@@]1(C(=O)O)[C@H](OCc2ccccc2)[C@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1016/j.bmcl.2016.10.067
122190338 130245 0 None -1 2 Rat 5.6 pIC50 = 5.6 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 366 4 0 5 3.5 Cc1cccc(OCc2cc3n(n2)[C@H](C)CN(c2ccc(F)cc2)C3=O)n1 10.1021/acs.jmedchem.5b01005
CHEMBL3617522 130245 0 None -1 2 Rat 5.6 pIC50 = 5.6 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 366 4 0 5 3.5 Cc1cccc(OCc2cc3n(n2)[C@H](C)CN(c2ccc(F)cc2)C3=O)n1 10.1021/acs.jmedchem.5b01005
1397 9307 15 None -1 8 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at mGLUR3 expressed in CHO cells assessed as inhibition of glutamate-induced inhibition of forskolin-stimulated cAMP productionAntagonist activity at mGLUR3 expressed in CHO cells assessed as inhibition of glutamate-induced inhibition of forskolin-stimulated cAMP production
ChEMBL 377 5 3 4 2.1 OC(=O)[C@]1(N)[C@H](OCc2ccc(c(c2)Cl)Cl)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O 10.1016/j.bmcl.2012.01.039
9886034 9307 15 None -1 8 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at mGLUR3 expressed in CHO cells assessed as inhibition of glutamate-induced inhibition of forskolin-stimulated cAMP productionAntagonist activity at mGLUR3 expressed in CHO cells assessed as inhibition of glutamate-induced inhibition of forskolin-stimulated cAMP production
ChEMBL 377 5 3 4 2.1 OC(=O)[C@]1(N)[C@H](OCc2ccc(c(c2)Cl)Cl)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O 10.1016/j.bmcl.2012.01.039
CHEMBL186453 9307 15 None -1 8 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at mGLUR3 expressed in CHO cells assessed as inhibition of glutamate-induced inhibition of forskolin-stimulated cAMP productionAntagonist activity at mGLUR3 expressed in CHO cells assessed as inhibition of glutamate-induced inhibition of forskolin-stimulated cAMP production
ChEMBL 377 5 3 4 2.1 OC(=O)[C@]1(N)[C@H](OCc2ccc(c(c2)Cl)Cl)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O 10.1016/j.bmcl.2012.01.039
162644419 190401 0 None -186 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 323 5 4 5 0.5 N[C@]1(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@@H]2[C@H](O)[C@@H]1CSc1ccccc1 10.1021/acs.jmedchem.6b01119
CHEMBL4778355 190401 0 None -186 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 323 5 4 5 0.5 N[C@]1(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@@H]2[C@H](O)[C@@H]1CSc1ccccc1 10.1021/acs.jmedchem.6b01119
CHEMBL4802356 190401 0 None -186 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 323 5 4 5 0.5 N[C@]1(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@@H]2[C@H](O)[C@@H]1CSc1ccccc1 10.1021/acs.jmedchem.6b01119
71131322 130184 0 None -43 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization after 1.5 hrs by FLIPR assayAntagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization after 1.5 hrs by FLIPR assay
ChEMBL 334 5 4 6 0.3 N[C@@]1(C(=O)O)C[C@H](Sc2nnc(C(F)F)[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
CHEMBL3616857 130184 0 None -43 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization after 1.5 hrs by FLIPR assayAntagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization after 1.5 hrs by FLIPR assay
ChEMBL 334 5 4 6 0.3 N[C@@]1(C(=O)O)C[C@H](Sc2nnc(C(F)F)[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
145949267 169596 6 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Negative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assay
ChEMBL 339 6 0 4 3.8 C[C@@H](COc1ccn(-c2ccc(F)cc2)c(=O)c1)Oc1ccccc1 10.1021/acsmedchemlett.7b00249
CHEMBL4172540 169596 6 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Negative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assay
ChEMBL 339 6 0 4 3.8 C[C@@H](COc1ccn(-c2ccc(F)cc2)c(=O)c1)Oc1ccccc1 10.1021/acsmedchemlett.7b00249
145949267 169596 6 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Negative allosteric modulation of rat mGlu3R expressed in HEK293 cells co-expressing Galpha15 assessed as decrease in glutamate-induced calcium mobilization preincubated for 2.5 mins followed by glutamate addition by S3 Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3R expressed in HEK293 cells co-expressing Galpha15 assessed as decrease in glutamate-induced calcium mobilization preincubated for 2.5 mins followed by glutamate addition by S3 Fluo-4-AM dye based fluorescence assay
ChEMBL 339 6 0 4 3.8 C[C@@H](COc1ccn(-c2ccc(F)cc2)c(=O)c1)Oc1ccccc1 10.1016/j.bmcl.2019.07.030
CHEMBL4172540 169596 6 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Negative allosteric modulation of rat mGlu3R expressed in HEK293 cells co-expressing Galpha15 assessed as decrease in glutamate-induced calcium mobilization preincubated for 2.5 mins followed by glutamate addition by S3 Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3R expressed in HEK293 cells co-expressing Galpha15 assessed as decrease in glutamate-induced calcium mobilization preincubated for 2.5 mins followed by glutamate addition by S3 Fluo-4-AM dye based fluorescence assay
ChEMBL 339 6 0 4 3.8 C[C@@H](COc1ccn(-c2ccc(F)cc2)c(=O)c1)Oc1ccccc1 10.1016/j.bmcl.2019.07.030
145949267 169596 6 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Negative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assay
ChEMBL 339 6 0 4 3.8 C[C@@H](COc1ccn(-c2ccc(F)cc2)c(=O)c1)Oc1ccccc1 10.1021/acsmedchemlett.7b00249
CHEMBL4172540 169596 6 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Negative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assay
ChEMBL 339 6 0 4 3.8 C[C@@H](COc1ccn(-c2ccc(F)cc2)c(=O)c1)Oc1ccccc1 10.1021/acsmedchemlett.7b00249
90643958 118769 0 None 6 2 Rat 6.6 pIC50 = 6.6 Functional
Inhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentrationInhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentration
ChEMBL 370 2 0 5 4.1 Cn1c(=O)c2ccc(-c3cccnc3)cc2n2nc(-c3cccc(F)c3)cc12 10.1016/j.bmcl.2014.04.051
CHEMBL3288644 118769 0 None 6 2 Rat 6.6 pIC50 = 6.6 Functional
Inhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentrationInhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentration
ChEMBL 370 2 0 5 4.1 Cn1c(=O)c2ccc(-c3cccnc3)cc2n2nc(-c3cccc(F)c3)cc12 10.1016/j.bmcl.2014.04.051
10607617 85511 0 None 2 2 Human 5.6 pIC50 = 5.6 Functional
Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3
ChEMBL 187 4 3 3 -0.1 CCC(N)(C(=O)O)[C@H]1C[C@@H]1C(=O)O 10.1021/jm970497w
CHEMBL2112579 85511 0 None 2 2 Human 5.6 pIC50 = 5.6 Functional
Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3
ChEMBL 187 4 3 3 -0.1 CCC(N)(C(=O)O)[C@H]1C[C@@H]1C(=O)O 10.1021/jm970497w
53240406 130174 17 None -107 4 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization after 1.5 hrs by FLIPR assayAntagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization after 1.5 hrs by FLIPR assay
ChEMBL 284 4 4 6 -0.6 N[C@@]1(C(=O)O)C[C@@H](Sc2nnc[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
CHEMBL3616847 130174 17 None -107 4 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization after 1.5 hrs by FLIPR assayAntagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization after 1.5 hrs by FLIPR assay
ChEMBL 284 4 4 6 -0.6 N[C@@]1(C(=O)O)C[C@@H](Sc2nnc[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
122190322 130229 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 381 5 0 5 3.8 COc1ccccc1OCc1cc2n(n1)[C@H](C)CN(c1ccc(F)cc1)C2=O 10.1021/acs.jmedchem.5b01005
CHEMBL3617506 130229 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 381 5 0 5 3.8 COc1ccccc1OCc1cc2n(n1)[C@H](C)CN(c1ccc(F)cc1)C2=O 10.1021/acs.jmedchem.5b01005
122190431 130318 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 387 4 0 6 3.3 C[C@@H]1CN(c2ccc(F)cn2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617654 130318 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 387 4 0 6 3.3 C[C@@H]1CN(c2ccc(F)cn2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
122190322 130229 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 381 5 0 5 3.8 COc1ccccc1OCc1cc2n(n1)[C@H](C)CN(c1ccc(F)cc1)C2=O 10.1021/acs.jmedchem.5b01005
CHEMBL3617506 130229 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 381 5 0 5 3.8 COc1ccccc1OCc1cc2n(n1)[C@H](C)CN(c1ccc(F)cc1)C2=O 10.1021/acs.jmedchem.5b01005
44348769 23553 0 None 3 2 Human 6.6 pIC50 = 6.6 Functional
Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3
ChEMBL 279 6 4 4 0.8 N[C@@](CCc1cccc(O)c1)(C(=O)O)C1C[C@@H]1C(=O)O 10.1021/jm970498o
CHEMBL124483 23553 0 None 3 2 Human 6.6 pIC50 = 6.6 Functional
Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3
ChEMBL 279 6 4 4 0.8 N[C@@](CCc1cccc(O)c1)(C(=O)O)C1C[C@@H]1C(=O)O 10.1021/jm970498o
122190431 130318 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 387 4 0 6 3.3 C[C@@H]1CN(c2ccc(F)cn2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617654 130318 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 387 4 0 6 3.3 C[C@@H]1CN(c2ccc(F)cn2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
118575176 130218 0 None -5 2 Rat 6.6 pIC50 = 6.6 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 351 4 0 4 3.8 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ccccc3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617495 130218 0 None -5 2 Rat 6.6 pIC50 = 6.6 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 351 4 0 4 3.8 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ccccc3)nn21 10.1021/acs.jmedchem.5b01005
122190396 130283 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 366 4 0 5 3.5 Cc1ccc(N2C[C@@H](C)n3nc(COc4ccc(F)cn4)cc3C2=O)cc1 10.1021/acs.jmedchem.5b01005
CHEMBL3617619 130283 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 366 4 0 5 3.5 Cc1ccc(N2C[C@@H](C)n3nc(COc4ccc(F)cn4)cc3C2=O)cc1 10.1021/acs.jmedchem.5b01005
118575176 130218 0 None -5 2 Rat 6.6 pIC50 = 6.6 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 351 4 0 4 3.8 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ccccc3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617495 130218 0 None -5 2 Rat 6.6 pIC50 = 6.6 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 351 4 0 4 3.8 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ccccc3)nn21 10.1021/acs.jmedchem.5b01005
122190396 130283 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 366 4 0 5 3.5 Cc1ccc(N2C[C@@H](C)n3nc(COc4ccc(F)cn4)cc3C2=O)cc1 10.1021/acs.jmedchem.5b01005
CHEMBL3617619 130283 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 366 4 0 5 3.5 Cc1ccc(N2C[C@@H](C)n3nc(COc4ccc(F)cn4)cc3C2=O)cc1 10.1021/acs.jmedchem.5b01005
140839138 169662 0 None 4 2 Rat 6.6 pIC50 = 6.6 Functional
Negative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assay
ChEMBL 350 6 0 5 3.3 N#Cc1cc(F)cc(-n2ccc(OCCOc3ccccc3)cc2=O)c1 10.1021/acsmedchemlett.7b00249
CHEMBL4173490 169662 0 None 4 2 Rat 6.6 pIC50 = 6.6 Functional
Negative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assay
ChEMBL 350 6 0 5 3.3 N#Cc1cc(F)cc(-n2ccc(OCCOc3ccccc3)cc2=O)c1 10.1021/acsmedchemlett.7b00249
67633340 190500 0 None -1 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 355 5 4 5 0.9 Cc1cc(SC[C@@H]2[C@@H](O)[C@@H]3[C@@H]([C@H]3C(=O)O)[C@]2(N)C(=O)O)ccc1F 10.1021/acs.jmedchem.6b01119
CHEMBL4780402 190500 0 None -1 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 355 5 4 5 0.9 Cc1cc(SC[C@@H]2[C@@H](O)[C@@H]3[C@@H]([C@H]3C(=O)O)[C@]2(N)C(=O)O)ccc1F 10.1021/acs.jmedchem.6b01119
CHEMBL4803381 190500 0 None -1 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 355 5 4 5 0.9 Cc1cc(SC[C@@H]2[C@@H](O)[C@@H]3[C@@H]([C@H]3C(=O)O)[C@]2(N)C(=O)O)ccc1F 10.1021/acs.jmedchem.6b01119
140839138 169662 0 None 4 2 Rat 6.6 pIC50 = 6.6 Functional
Negative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assay
ChEMBL 350 6 0 5 3.3 N#Cc1cc(F)cc(-n2ccc(OCCOc3ccccc3)cc2=O)c1 10.1021/acsmedchemlett.7b00249
CHEMBL4173490 169662 0 None 4 2 Rat 6.6 pIC50 = 6.6 Functional
Negative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assay
ChEMBL 350 6 0 5 3.3 N#Cc1cc(F)cc(-n2ccc(OCCOc3ccccc3)cc2=O)c1 10.1021/acsmedchemlett.7b00249
10473248 20958 0 None -4 3 Rat 4.6 pIC50 = 4.6 Functional
Inhibitory concentration required for antagonistic activity at Metabotropic glutamate receptor 3Inhibitory concentration required for antagonistic activity at Metabotropic glutamate receptor 3
ChEMBL 280 4 4 5 -0.2 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2ccccc2O)C1 10.1016/s0960-894x(01)00329-8
CHEMBL1198741 20958 0 None -4 3 Rat 4.6 pIC50 = 4.6 Functional
Inhibitory concentration required for antagonistic activity at Metabotropic glutamate receptor 3Inhibitory concentration required for antagonistic activity at Metabotropic glutamate receptor 3
ChEMBL 280 4 4 5 -0.2 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2ccccc2O)C1 10.1016/s0960-894x(01)00329-8
CHEMBL540015 20958 0 None -4 3 Rat 4.6 pIC50 = 4.6 Functional
Inhibitory concentration required for antagonistic activity at Metabotropic glutamate receptor 3Inhibitory concentration required for antagonistic activity at Metabotropic glutamate receptor 3
ChEMBL 280 4 4 5 -0.2 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2ccccc2O)C1 10.1016/s0960-894x(01)00329-8
162666357 190510 0 None -3 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 341 5 4 5 0.6 N[C@@]1(C(=O)O)[C@H](CSc2cccc(F)c2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
CHEMBL4784701 190510 0 None -3 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 341 5 4 5 0.6 N[C@@]1(C(=O)O)[C@H](CSc2cccc(F)c2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
CHEMBL4803523 190510 0 None -3 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 341 5 4 5 0.6 N[C@@]1(C(=O)O)[C@H](CSc2cccc(F)c2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
53240406 130174 17 None -107 4 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as reversal of DCG-4-inhibited, forskolin-stimulated cAMP production after 1 hr by fluorescence assayAntagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as reversal of DCG-4-inhibited, forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 284 4 4 6 -0.6 N[C@@]1(C(=O)O)C[C@@H](Sc2nnc[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
CHEMBL3616847 130174 17 None -107 4 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as reversal of DCG-4-inhibited, forskolin-stimulated cAMP production after 1 hr by fluorescence assayAntagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as reversal of DCG-4-inhibited, forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 284 4 4 6 -0.6 N[C@@]1(C(=O)O)C[C@@H](Sc2nnc[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
60210850 97105 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 minsNegative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 359 2 0 3 3.1 COc1ccc(C#Cc2ccc(C(=O)N3CC4CCC(=O)C4C3)cc2)cc1 10.1021/jm400439t
CHEMBL2385884 97105 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 minsNegative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 359 2 0 3 3.1 COc1ccc(C#Cc2ccc(C(=O)N3CC4CCC(=O)C4C3)cc2)cc1 10.1021/jm400439t
60210794 97101 0 None - 1 Rat 4.6 pIC50 = 4.6 Functional
Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 minsNegative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 321 2 1 3 2.3 COc1ccc(C#Cc2ccc(C(=O)N3CC[C@H](O)C3)cc2)cc1 10.1021/jm400439t
CHEMBL2385880 97101 0 None - 1 Rat 4.6 pIC50 = 4.6 Functional
Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 minsNegative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 321 2 1 3 2.3 COc1ccc(C#Cc2ccc(C(=O)N3CC[C@H](O)C3)cc2)cc1 10.1021/jm400439t
71476419 130187 0 None -51 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization after 1.5 hrs by FLIPR assayAntagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization after 1.5 hrs by FLIPR assay
ChEMBL 284 4 4 6 -0.6 N[C@@]1(C(=O)O)C[C@H](Sc2c[nH]nn2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
CHEMBL3616860 130187 0 None -51 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization after 1.5 hrs by FLIPR assayAntagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization after 1.5 hrs by FLIPR assay
ChEMBL 284 4 4 6 -0.6 N[C@@]1(C(=O)O)C[C@H](Sc2c[nH]nn2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
10783272 92897 0 None 15 2 Human 6.6 pIC50 = 6.6 Functional
Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3
ChEMBL 339 7 3 3 2.7 N[C@@](CC(c1ccccc1)c1ccccc1)(C(=O)O)[C@H]1C[C@@H]1C(=O)O 10.1021/jm970497w
CHEMBL2311086 92897 0 None 15 2 Human 6.6 pIC50 = 6.6 Functional
Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3
ChEMBL 339 7 3 3 2.7 N[C@@](CC(c1ccccc1)c1ccccc1)(C(=O)O)[C@H]1C[C@@H]1C(=O)O 10.1021/jm970497w
122190422 130309 0 None 9 2 Rat 6.6 pIC50 = 6.6 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 404 4 0 5 4.0 C[C@@H]1CN(c2ccc(F)cc2F)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617645 130309 0 None 9 2 Rat 6.6 pIC50 = 6.6 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 404 4 0 5 4.0 C[C@@H]1CN(c2ccc(F)cc2F)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
10732318 85518 0 None -6 2 Human 5.6 pIC50 = 5.6 Functional
Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3
ChEMBL 291 8 3 3 1.9 NC(CCCCc1ccccc1)(C(=O)O)[C@H]1C[C@@H]1C(=O)O 10.1021/jm970497w
CHEMBL2112585 85518 0 None -6 2 Human 5.6 pIC50 = 5.6 Functional
Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3
ChEMBL 291 8 3 3 1.9 NC(CCCCc1ccccc1)(C(=O)O)[C@H]1C[C@@H]1C(=O)O 10.1021/jm970497w
122190422 130309 0 None 9 2 Rat 6.6 pIC50 = 6.6 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 404 4 0 5 4.0 C[C@@H]1CN(c2ccc(F)cc2F)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617645 130309 0 None 9 2 Rat 6.6 pIC50 = 6.6 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 404 4 0 5 4.0 C[C@@H]1CN(c2ccc(F)cc2F)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
11269030 63078 0 None 1 3 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity at rat mGluR3 receptor expressed in CHO cells assessed as inhibition of GIRK currentAntagonist activity at rat mGluR3 receptor expressed in CHO cells assessed as inhibition of GIRK current
ChEMBL 381 2 1 3 5.2 O=C1CC(c2cccc(-c3ccncc3)c2)=Nc2ccc(C(F)(F)F)cc2N1 10.1016/j.bmcl.2010.09.125
CHEMBL1629861 63078 0 None 1 3 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity at rat mGluR3 receptor expressed in CHO cells assessed as inhibition of GIRK currentAntagonist activity at rat mGluR3 receptor expressed in CHO cells assessed as inhibition of GIRK current
ChEMBL 381 2 1 3 5.2 O=C1CC(c2cccc(-c3ccncc3)c2)=Nc2ccc(C(F)(F)F)cc2N1 10.1016/j.bmcl.2010.09.125
44328753 214533 0 None 16 6 Rat 7.5 pIC50 = 7.5 Functional
Antagonistic activity against metabotropic glutamate receptor 3 (mGluR3) was evaluatedAntagonistic activity against metabotropic glutamate receptor 3 (mGluR3) was evaluated
ChEMBL 409 8 3 4 4.2 CCCC[C@@H]1[C@H](C(=O)O)[C@H]1C(N)(CC1c2ccccc2Oc2ccccc21)C(=O)O 10.1016/s0960-894x(98)00510-1
CHEMBL95868 214533 0 None 16 6 Rat 7.5 pIC50 = 7.5 Functional
Antagonistic activity against metabotropic glutamate receptor 3 (mGluR3) was evaluatedAntagonistic activity against metabotropic glutamate receptor 3 (mGluR3) was evaluated
ChEMBL 409 8 3 4 4.2 CCCC[C@@H]1[C@H](C(=O)O)[C@H]1C(N)(CC1c2ccccc2Oc2ccccc21)C(=O)O 10.1016/s0960-894x(98)00510-1
86695984 156544 0 None -1 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assayAntagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 472 7 3 8 1.9 Cn1ncnc1S[C@@H]1[C@@H](OCc2ccc(Cl)c(Cl)c2)[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1016/j.bmcl.2016.10.067
CHEMBL3948272 156544 0 None -1 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assayAntagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 472 7 3 8 1.9 Cn1ncnc1S[C@@H]1[C@@H](OCc2ccc(Cl)c(Cl)c2)[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1016/j.bmcl.2016.10.067
122455994 169078 0 None 4 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assay
ChEMBL 326 6 0 5 2.8 O=c1nc(OCCOc2ccccc2)ccn1-c1ccc(F)cc1 10.1021/acsmedchemlett.7b00249
CHEMBL4164285 169078 0 None 4 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assay
ChEMBL 326 6 0 5 2.8 O=c1nc(OCCOc2ccccc2)ccn1-c1ccc(F)cc1 10.1021/acsmedchemlett.7b00249
90643964 118773 0 None 1 2 Rat 6.5 pIC50 = 6.5 Functional
Inhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentrationInhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentration
ChEMBL 386 2 0 5 4.6 Cn1c(=O)c2ccc(-c3cccnc3)cc2n2nc(-c3cccc(Cl)c3)cc12 10.1016/j.bmcl.2014.04.051
CHEMBL3288656 118773 0 None 1 2 Rat 6.5 pIC50 = 6.5 Functional
Inhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentrationInhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentration
ChEMBL 386 2 0 5 4.6 Cn1c(=O)c2ccc(-c3cccnc3)cc2n2nc(-c3cccc(Cl)c3)cc12 10.1016/j.bmcl.2014.04.051
122190432 130109 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 387 4 0 6 3.3 C[C@@H]1CN(c2cccc(F)n2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3616489 130109 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 387 4 0 6 3.3 C[C@@H]1CN(c2cccc(F)n2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
11310142 9200 19 None -13 3 Human 5.5 pIC50 = 5.5 Functional
Evaluation of the functional effect on cAMP responses in RGT cells expressing human mGlu3 receptorEvaluation of the functional effect on cAMP responses in RGT cells expressing human mGlu3 receptor
ChEMBL 199 2 3 3 -0.2 C[C@@H]1C[C@@]([C@H]2[C@@H]1[C@@H]2C(=O)O)(N)C(=O)O 10.1021/jm040222y
11614 9200 19 None -13 3 Human 5.5 pIC50 = 5.5 Functional
Evaluation of the functional effect on cAMP responses in RGT cells expressing human mGlu3 receptorEvaluation of the functional effect on cAMP responses in RGT cells expressing human mGlu3 receptor
ChEMBL 199 2 3 3 -0.2 C[C@@H]1C[C@@]([C@H]2[C@@H]1[C@@H]2C(=O)O)(N)C(=O)O 10.1021/jm040222y
CHEMBL192051 9200 19 None -13 3 Human 5.5 pIC50 = 5.5 Functional
Evaluation of the functional effect on cAMP responses in RGT cells expressing human mGlu3 receptorEvaluation of the functional effect on cAMP responses in RGT cells expressing human mGlu3 receptor
ChEMBL 199 2 3 3 -0.2 C[C@@H]1C[C@@]([C@H]2[C@@H]1[C@@H]2C(=O)O)(N)C(=O)O 10.1021/jm040222y
122190331 130238 0 None - 1 Rat 5.5 pIC50 = 5.5 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 420 4 0 5 4.2 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ncccc3C(F)(F)F)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617515 130238 0 None - 1 Rat 5.5 pIC50 = 5.5 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 420 4 0 5 4.2 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ncccc3C(F)(F)F)nn21 10.1021/acs.jmedchem.5b01005
122190432 130109 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 387 4 0 6 3.3 C[C@@H]1CN(c2cccc(F)n2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3616489 130109 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 387 4 0 6 3.3 C[C@@H]1CN(c2cccc(F)n2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
122455994 169078 0 None 4 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assay
ChEMBL 326 6 0 5 2.8 O=c1nc(OCCOc2ccccc2)ccn1-c1ccc(F)cc1 10.1021/acsmedchemlett.7b00249
CHEMBL4164285 169078 0 None 4 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assay
ChEMBL 326 6 0 5 2.8 O=c1nc(OCCOc2ccccc2)ccn1-c1ccc(F)cc1 10.1021/acsmedchemlett.7b00249
122190331 130238 0 None - 1 Rat 5.5 pIC50 = 5.5 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 420 4 0 5 4.2 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ncccc3C(F)(F)F)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617515 130238 0 None - 1 Rat 5.5 pIC50 = 5.5 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 420 4 0 5 4.2 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ncccc3C(F)(F)F)nn21 10.1021/acs.jmedchem.5b01005
11442010 63083 0 None 2 3 Rat 8.5 pIC50 = 8.5 Functional
Antagonist activity at rat mGluR3 receptor expressed in CHO cells assessed as inhibition of GIRK currentAntagonist activity at rat mGluR3 receptor expressed in CHO cells assessed as inhibition of GIRK current
ChEMBL 439 4 1 4 5.9 CCOc1cc2c(cc1C(F)(F)F)NC(=O)CC(c1cccc(-c3ccnc(C)c3)c1)=N2 10.1016/j.bmcl.2010.09.125
CHEMBL1629866 63083 0 None 2 3 Rat 8.5 pIC50 = 8.5 Functional
Antagonist activity at rat mGluR3 receptor expressed in CHO cells assessed as inhibition of GIRK currentAntagonist activity at rat mGluR3 receptor expressed in CHO cells assessed as inhibition of GIRK current
ChEMBL 439 4 1 4 5.9 CCOc1cc2c(cc1C(F)(F)F)NC(=O)CC(c1cccc(-c3ccnc(C)c3)c1)=N2 10.1016/j.bmcl.2010.09.125
11304010 63081 0 None -10 3 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity at rat mGluR3 receptor expressed in CHO cells assessed as inhibition of GIRK currentAntagonist activity at rat mGluR3 receptor expressed in CHO cells assessed as inhibition of GIRK current
ChEMBL 395 2 1 3 5.8 Cc1cc(-c2cccc(C3=Nc4cc(Cl)c(Cl)cc4NC(=O)C3)c2)ccn1 10.1016/j.bmcl.2010.09.125
CHEMBL1629864 63081 0 None -10 3 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity at rat mGluR3 receptor expressed in CHO cells assessed as inhibition of GIRK currentAntagonist activity at rat mGluR3 receptor expressed in CHO cells assessed as inhibition of GIRK current
ChEMBL 395 2 1 3 5.8 Cc1cc(-c2cccc(C3=Nc4cc(Cl)c(Cl)cc4NC(=O)C3)c2)ccn1 10.1016/j.bmcl.2010.09.125
6324634 154722 11 None -6 2 Human 4.5 pIC50 = 4.5 Functional
In vitro antagonist activity at recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.In vitro antagonist activity at recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.
ChEMBL 355 10 3 3 3.5 N[C@@H](C[C@H](CCCC(c1ccccc1)c1ccccc1)C(=O)O)C(=O)O 10.1016/s0960-894x(98)00352-7
CHEMBL39338 154722 11 None -6 2 Human 4.5 pIC50 = 4.5 Functional
In vitro antagonist activity at recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.In vitro antagonist activity at recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.
ChEMBL 355 10 3 3 3.5 N[C@@H](C[C@H](CCCC(c1ccccc1)c1ccccc1)C(=O)O)C(=O)O 10.1016/s0960-894x(98)00352-7
6324634 154722 11 None -6 2 Human 4.5 pIC50 = 4.5 Functional
Tested for agonist activity in non-neuronal cells (RGT) expressing human Metabotropic glutamate receptor 3 by measuring ACPD (3 uM) induced inhibition of forskolin (15 uM)-stimulated cAMP formationTested for agonist activity in non-neuronal cells (RGT) expressing human Metabotropic glutamate receptor 3 by measuring ACPD (3 uM) induced inhibition of forskolin (15 uM)-stimulated cAMP formation
ChEMBL 355 10 3 3 3.5 N[C@@H](C[C@H](CCCC(c1ccccc1)c1ccccc1)C(=O)O)C(=O)O 10.1016/s0960-894x(98)00091-2
CHEMBL39338 154722 11 None -6 2 Human 4.5 pIC50 = 4.5 Functional
Tested for agonist activity in non-neuronal cells (RGT) expressing human Metabotropic glutamate receptor 3 by measuring ACPD (3 uM) induced inhibition of forskolin (15 uM)-stimulated cAMP formationTested for agonist activity in non-neuronal cells (RGT) expressing human Metabotropic glutamate receptor 3 by measuring ACPD (3 uM) induced inhibition of forskolin (15 uM)-stimulated cAMP formation
ChEMBL 355 10 3 3 3.5 N[C@@H](C[C@H](CCCC(c1ccccc1)c1ccccc1)C(=O)O)C(=O)O 10.1016/s0960-894x(98)00091-2
60204018 97099 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 minsNegative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 335 2 1 3 2.7 COc1ccc(C#Cc2ccc(C(=O)N3CCC[C@@H](O)C3)cc2)cc1 10.1021/jm400439t
CHEMBL2385878 97099 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 minsNegative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 335 2 1 3 2.7 COc1ccc(C#Cc2ccc(C(=O)N3CCC[C@@H](O)C3)cc2)cc1 10.1021/jm400439t
CHEMBL2385888 97099 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 minsNegative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 335 2 1 3 2.7 COc1ccc(C#Cc2ccc(C(=O)N3CCC[C@@H](O)C3)cc2)cc1 10.1021/jm400439t
71136653 130181 0 None -51 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization after 1.5 hrs by FLIPR assayAntagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization after 1.5 hrs by FLIPR assay
ChEMBL 284 4 4 6 -0.6 N[C@@]1(C(=O)O)C[C@H](Sc2nnc[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
CHEMBL3616854 130181 0 None -51 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization after 1.5 hrs by FLIPR assayAntagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization after 1.5 hrs by FLIPR assay
ChEMBL 284 4 4 6 -0.6 N[C@@]1(C(=O)O)C[C@H](Sc2nnc[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
122190416 130303 0 None 16 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 398 5 0 6 3.7 COc1cccc(N2C[C@@H](C)n3nc(COc4ccc(Cl)cn4)cc3C2=O)c1 10.1021/acs.jmedchem.5b01005
CHEMBL3617639 130303 0 None 16 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 398 5 0 6 3.7 COc1cccc(N2C[C@@H](C)n3nc(COc4ccc(Cl)cn4)cc3C2=O)c1 10.1021/acs.jmedchem.5b01005
122190426 130313 0 None 3 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 411 4 0 6 3.7 C[C@@H]1CN(c2cc(F)cc(C#N)c2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617649 130313 0 None 3 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 411 4 0 6 3.7 C[C@@H]1CN(c2cc(F)cc(C#N)c2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
90643973 118779 0 None 1 2 Rat 5.5 pIC50 = 5.5 Functional
Inhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentrationInhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentration
ChEMBL 382 4 1 6 3.4 O=c1c2ccc(-c3cccnc3)cc2n2nc(-c3ccccc3)cc2n1CCO 10.1016/j.bmcl.2014.04.051
CHEMBL3288674 118779 0 None 1 2 Rat 5.5 pIC50 = 5.5 Functional
Inhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentrationInhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentration
ChEMBL 382 4 1 6 3.4 O=c1c2ccc(-c3cccnc3)cc2n2nc(-c3ccccc3)cc2n1CCO 10.1016/j.bmcl.2014.04.051
122190416 130303 0 None 16 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 398 5 0 6 3.7 COc1cccc(N2C[C@@H](C)n3nc(COc4ccc(Cl)cn4)cc3C2=O)c1 10.1021/acs.jmedchem.5b01005
CHEMBL3617639 130303 0 None 16 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 398 5 0 6 3.7 COc1cccc(N2C[C@@H](C)n3nc(COc4ccc(Cl)cn4)cc3C2=O)c1 10.1021/acs.jmedchem.5b01005
122190426 130313 0 None 3 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 411 4 0 6 3.7 C[C@@H]1CN(c2cc(F)cc(C#N)c2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617649 130313 0 None 3 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 411 4 0 6 3.7 C[C@@H]1CN(c2cc(F)cc(C#N)c2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
122190399 130286 0 None 4 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 382 5 0 6 3.2 COc1ccc(N2C[C@@H](C)n3nc(COc4ccc(F)cn4)cc3C2=O)cc1 10.1021/acs.jmedchem.5b01005
CHEMBL3617622 130286 0 None 4 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 382 5 0 6 3.2 COc1ccc(N2C[C@@H](C)n3nc(COc4ccc(F)cn4)cc3C2=O)cc1 10.1021/acs.jmedchem.5b01005
122190399 130286 0 None 4 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 382 5 0 6 3.2 COc1ccc(N2C[C@@H](C)n3nc(COc4ccc(F)cn4)cc3C2=O)cc1 10.1021/acs.jmedchem.5b01005
CHEMBL3617622 130286 0 None 4 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 382 5 0 6 3.2 COc1ccc(N2C[C@@H](C)n3nc(COc4ccc(F)cn4)cc3C2=O)cc1 10.1021/acs.jmedchem.5b01005
122190409 130296 0 None 16 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 402 4 0 5 4.4 C[C@@H]1CN(c2ccccc2Cl)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617632 130296 0 None 16 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 402 4 0 5 4.4 C[C@@H]1CN(c2ccccc2Cl)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
122190427 130314 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 369 4 0 6 3.1 C[C@@H]1CN(c2ccccn2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617650 130314 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 369 4 0 6 3.1 C[C@@H]1CN(c2ccccn2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
22224657 102947 0 None -2 2 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity at rat mGluR3 expressed in CHO cells assessed as inhibition of glutamate-induced GIRK currentAntagonist activity at rat mGluR3 expressed in CHO cells assessed as inhibition of glutamate-induced GIRK current
ChEMBL 396 3 1 4 5.1 O=C1CC(c2cccc(-n3ccnc3)c2)=Nc2ccc(-c3ccccc3F)cc2N1 10.1016/j.bmcl.2008.02.076
CHEMBL260636 102947 0 None -2 2 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity at rat mGluR3 expressed in CHO cells assessed as inhibition of glutamate-induced GIRK currentAntagonist activity at rat mGluR3 expressed in CHO cells assessed as inhibition of glutamate-induced GIRK current
ChEMBL 396 3 1 4 5.1 O=C1CC(c2cccc(-n3ccnc3)c2)=Nc2ccc(-c3ccccc3F)cc2N1 10.1016/j.bmcl.2008.02.076
9952648 103083 0 None -1 2 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity at rat mGluR3 receptor expressed in CHO cells assessed as inhibition of GIRK currentAntagonist activity at rat mGluR3 receptor expressed in CHO cells assessed as inhibition of GIRK current
ChEMBL 397 3 1 5 4.5 O=C1CC(c2cccc(-n3ccnn3)c2)=Nc2ccc(-c3ccccc3F)cc2N1 10.1016/j.bmcl.2010.09.125
CHEMBL261288 103083 0 None -1 2 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity at rat mGluR3 receptor expressed in CHO cells assessed as inhibition of GIRK currentAntagonist activity at rat mGluR3 receptor expressed in CHO cells assessed as inhibition of GIRK current
ChEMBL 397 3 1 5 4.5 O=C1CC(c2cccc(-n3ccnn3)c2)=Nc2ccc(-c3ccccc3F)cc2N1 10.1016/j.bmcl.2010.09.125
122190409 130296 0 None 16 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 402 4 0 5 4.4 C[C@@H]1CN(c2ccccc2Cl)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617632 130296 0 None 16 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 402 4 0 5 4.4 C[C@@H]1CN(c2ccccc2Cl)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
122190427 130314 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 369 4 0 6 3.1 C[C@@H]1CN(c2ccccn2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617650 130314 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 369 4 0 6 3.1 C[C@@H]1CN(c2ccccn2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
71681826 96836 0 None -1 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by HTRF assayAntagonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by HTRF assay
ChEMBL 293 4 3 4 1.3 N[C@@]1(C(=O)O)C[C@H](Sc2ccccc2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm4000165
CHEMBL2381651 96836 0 None -1 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by HTRF assayAntagonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by HTRF assay
ChEMBL 293 4 3 4 1.3 N[C@@]1(C(=O)O)C[C@H](Sc2ccccc2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm4000165
71681826 96836 0 None -1 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as reversal of DCG-4-inhibited, forskolin-stimulated cAMP production after 1 hr by fluorescence assayAntagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as reversal of DCG-4-inhibited, forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 293 4 3 4 1.3 N[C@@]1(C(=O)O)C[C@H](Sc2ccccc2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
CHEMBL2381651 96836 0 None -1 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as reversal of DCG-4-inhibited, forskolin-stimulated cAMP production after 1 hr by fluorescence assayAntagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as reversal of DCG-4-inhibited, forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 293 4 3 4 1.3 N[C@@]1(C(=O)O)C[C@H](Sc2ccccc2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
122190397 130284 0 None -1 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 382 5 0 6 3.2 COc1ccccc1N1C[C@@H](C)n2nc(COc3ccc(F)cn3)cc2C1=O 10.1021/acs.jmedchem.5b01005
CHEMBL3617620 130284 0 None -1 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 382 5 0 6 3.2 COc1ccccc1N1C[C@@H](C)n2nc(COc3ccc(F)cn3)cc2C1=O 10.1021/acs.jmedchem.5b01005
140839143 168984 0 None 18 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assay
ChEMBL 332 6 0 5 3.2 N#Cc1cccc(-n2ccc(OCCOc3ccccc3)cc2=O)c1 10.1021/acsmedchemlett.7b00249
CHEMBL4162785 168984 0 None 18 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assay
ChEMBL 332 6 0 5 3.2 N#Cc1cccc(-n2ccc(OCCOc3ccccc3)cc2=O)c1 10.1021/acsmedchemlett.7b00249
122190397 130284 0 None -1 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 382 5 0 6 3.2 COc1ccccc1N1C[C@@H](C)n2nc(COc3ccc(F)cn3)cc2C1=O 10.1021/acs.jmedchem.5b01005
CHEMBL3617620 130284 0 None -1 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 382 5 0 6 3.2 COc1ccccc1N1C[C@@H](C)n2nc(COc3ccc(F)cn3)cc2C1=O 10.1021/acs.jmedchem.5b01005
70051296 96833 0 None 1 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by HTRF assayAntagonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by HTRF assay
ChEMBL 242 3 4 4 -1.4 CC(=O)N[C@@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@@H]21 10.1021/jm4000165
CHEMBL2381648 96833 0 None 1 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by HTRF assayAntagonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by HTRF assay
ChEMBL 242 3 4 4 -1.4 CC(=O)N[C@@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@@H]21 10.1021/jm4000165
140839143 168984 0 None 18 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assay
ChEMBL 332 6 0 5 3.2 N#Cc1cccc(-n2ccc(OCCOc3ccccc3)cc2=O)c1 10.1021/acsmedchemlett.7b00249
CHEMBL4162785 168984 0 None 18 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assay
ChEMBL 332 6 0 5 3.2 N#Cc1cccc(-n2ccc(OCCOc3ccccc3)cc2=O)c1 10.1021/acsmedchemlett.7b00249
11310142 9200 19 None -13 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by HTRF assayAntagonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by HTRF assay
ChEMBL 199 2 3 3 -0.2 C[C@@H]1C[C@@]([C@H]2[C@@H]1[C@@H]2C(=O)O)(N)C(=O)O 10.1021/jm4000165
11614 9200 19 None -13 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by HTRF assayAntagonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by HTRF assay
ChEMBL 199 2 3 3 -0.2 C[C@@H]1C[C@@]([C@H]2[C@@H]1[C@@H]2C(=O)O)(N)C(=O)O 10.1021/jm4000165
CHEMBL192051 9200 19 None -13 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by HTRF assayAntagonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by HTRF assay
ChEMBL 199 2 3 3 -0.2 C[C@@H]1C[C@@]([C@H]2[C@@H]1[C@@H]2C(=O)O)(N)C(=O)O 10.1021/jm4000165
122190394 130281 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 366 4 0 5 3.5 Cc1ccccc1N1C[C@@H](C)n2nc(COc3ccc(F)cn3)cc2C1=O 10.1021/acs.jmedchem.5b01005
CHEMBL3617617 130281 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 366 4 0 5 3.5 Cc1ccccc1N1C[C@@H](C)n2nc(COc3ccc(F)cn3)cc2C1=O 10.1021/acs.jmedchem.5b01005
122190394 130281 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 366 4 0 5 3.5 Cc1ccccc1N1C[C@@H](C)n2nc(COc3ccc(F)cn3)cc2C1=O 10.1021/acs.jmedchem.5b01005
CHEMBL3617617 130281 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 366 4 0 5 3.5 Cc1ccccc1N1C[C@@H](C)n2nc(COc3ccc(F)cn3)cc2C1=O 10.1021/acs.jmedchem.5b01005
122190406 130293 0 None 28 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 371 4 0 6 2.8 C[C@@H]1CN(c2ccc(F)cn2)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617629 130293 0 None 28 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 371 4 0 6 2.8 C[C@@H]1CN(c2ccc(F)cn2)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
122456122 169525 0 None 4 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assay
ChEMBL 343 6 0 4 3.6 O=c1cc(OCCOc2cccc(F)c2)ccn1-c1ccc(F)cc1 10.1021/acsmedchemlett.7b00249
CHEMBL4171435 169525 0 None 4 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assay
ChEMBL 343 6 0 4 3.6 O=c1cc(OCCOc2cccc(F)c2)ccn1-c1ccc(F)cc1 10.1021/acsmedchemlett.7b00249
122190406 130293 0 None 28 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 371 4 0 6 2.8 C[C@@H]1CN(c2ccc(F)cn2)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617629 130293 0 None 28 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 371 4 0 6 2.8 C[C@@H]1CN(c2ccc(F)cn2)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
122456122 169525 0 None 4 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assay
ChEMBL 343 6 0 4 3.6 O=c1cc(OCCOc2cccc(F)c2)ccn1-c1ccc(F)cc1 10.1021/acsmedchemlett.7b00249
CHEMBL4171435 169525 0 None 4 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assay
ChEMBL 343 6 0 4 3.6 O=c1cc(OCCOc2cccc(F)c2)ccn1-c1ccc(F)cc1 10.1021/acsmedchemlett.7b00249
71137008 130182 0 None -7 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization after 1.5 hrs by FLIPR assayAntagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization after 1.5 hrs by FLIPR assay
ChEMBL 298 4 4 6 -0.3 Cc1nnc(S[C@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)[nH]1 10.1021/acs.jmedchem.5b01124
CHEMBL3616855 130182 0 None -7 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization after 1.5 hrs by FLIPR assayAntagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization after 1.5 hrs by FLIPR assay
ChEMBL 298 4 4 6 -0.3 Cc1nnc(S[C@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)[nH]1 10.1021/acs.jmedchem.5b01124
122190429 130316 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 387 4 0 6 3.3 C[C@@H]1CN(c2ncccc2F)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617652 130316 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 387 4 0 6 3.3 C[C@@H]1CN(c2ncccc2F)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
122190429 130316 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 387 4 0 6 3.3 C[C@@H]1CN(c2ncccc2F)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617652 130316 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 387 4 0 6 3.3 C[C@@H]1CN(c2ncccc2F)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
122190335 130242 0 None - 1 Rat 5.4 pIC50 = 5.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 382 5 0 6 3.2 COc1ccnc(OCc2cc3n(n2)[C@H](C)CN(c2ccc(F)cc2)C3=O)c1 10.1021/acs.jmedchem.5b01005
CHEMBL3617519 130242 0 None - 1 Rat 5.4 pIC50 = 5.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 382 5 0 6 3.2 COc1ccnc(OCc2cc3n(n2)[C@H](C)CN(c2ccc(F)cc2)C3=O)c1 10.1021/acs.jmedchem.5b01005
122190335 130242 0 None - 1 Rat 5.4 pIC50 = 5.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 382 5 0 6 3.2 COc1ccnc(OCc2cc3n(n2)[C@H](C)CN(c2ccc(F)cc2)C3=O)c1 10.1021/acs.jmedchem.5b01005
CHEMBL3617519 130242 0 None - 1 Rat 5.4 pIC50 = 5.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 382 5 0 6 3.2 COc1ccnc(OCc2cc3n(n2)[C@H](C)CN(c2ccc(F)cc2)C3=O)c1 10.1021/acs.jmedchem.5b01005
67705326 160027 0 None -2 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assayAntagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 457 7 4 6 2.5 N[C@@]1(C(=O)O)[C@H](OCc2ccc(Cl)c(Cl)c2)[C@@H](Sc2ncc[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1016/j.bmcl.2016.10.067
CHEMBL3977508 160027 0 None -2 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assayAntagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 457 7 4 6 2.5 N[C@@]1(C(=O)O)[C@H](OCc2ccc(Cl)c(Cl)c2)[C@@H](Sc2ncc[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1016/j.bmcl.2016.10.067
71137011 130185 0 None -58 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization after 1.5 hrs by FLIPR assayAntagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization after 1.5 hrs by FLIPR assay
ChEMBL 299 4 5 7 -1.0 Nc1nnc(S[C@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)[nH]1 10.1021/acs.jmedchem.5b01124
CHEMBL3616858 130185 0 None -58 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization after 1.5 hrs by FLIPR assayAntagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization after 1.5 hrs by FLIPR assay
ChEMBL 299 4 5 7 -1.0 Nc1nnc(S[C@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)[nH]1 10.1021/acs.jmedchem.5b01124
10237 10823 20 None 1 2 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 387 4 0 6 3.3 Clc1ccc(nc1)OCc1nn2c(c1)C(=O)N(C[C@H]2C)c1cccnc1F 10.1021/acs.jmedchem.5b01005
122190433 10823 20 None 1 2 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 387 4 0 6 3.3 Clc1ccc(nc1)OCc1nn2c(c1)C(=O)N(C[C@H]2C)c1cccnc1F 10.1021/acs.jmedchem.5b01005
CHEMBL3617655 10823 20 None 1 2 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 387 4 0 6 3.3 Clc1ccc(nc1)OCc1nn2c(c1)C(=O)N(C[C@H]2C)c1cccnc1F 10.1021/acs.jmedchem.5b01005
122190413 130300 0 None 9 2 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 382 4 0 5 4.0 Cc1cccc(N2C[C@@H](C)n3nc(COc4ccc(Cl)cn4)cc3C2=O)c1 10.1021/acs.jmedchem.5b01005
CHEMBL3617636 130300 0 None 9 2 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 382 4 0 5 4.0 Cc1cccc(N2C[C@@H](C)n3nc(COc4ccc(Cl)cn4)cc3C2=O)c1 10.1021/acs.jmedchem.5b01005
122456028 169506 0 None 5 2 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assay
ChEMBL 325 6 0 4 3.4 O=c1cc(OCCOc2ccccc2)ccn1-c1cccc(F)c1 10.1021/acsmedchemlett.7b00249
CHEMBL4171110 169506 0 None 5 2 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assay
ChEMBL 325 6 0 4 3.4 O=c1cc(OCCOc2ccccc2)ccn1-c1cccc(F)c1 10.1021/acsmedchemlett.7b00249
122456028 169506 0 None 5 2 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assay
ChEMBL 325 6 0 4 3.4 O=c1cc(OCCOc2ccccc2)ccn1-c1cccc(F)c1 10.1021/acsmedchemlett.7b00249
CHEMBL4171110 169506 0 None 5 2 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assay
ChEMBL 325 6 0 4 3.4 O=c1cc(OCCOc2ccccc2)ccn1-c1cccc(F)c1 10.1021/acsmedchemlett.7b00249
10237 10823 20 None 1 2 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 387 4 0 6 3.3 Clc1ccc(nc1)OCc1nn2c(c1)C(=O)N(C[C@H]2C)c1cccnc1F 10.1021/acs.jmedchem.5b01005
122190433 10823 20 None 1 2 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 387 4 0 6 3.3 Clc1ccc(nc1)OCc1nn2c(c1)C(=O)N(C[C@H]2C)c1cccnc1F 10.1021/acs.jmedchem.5b01005
CHEMBL3617655 10823 20 None 1 2 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 387 4 0 6 3.3 Clc1ccc(nc1)OCc1nn2c(c1)C(=O)N(C[C@H]2C)c1cccnc1F 10.1021/acs.jmedchem.5b01005
122190413 130300 0 None 9 2 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 382 4 0 5 4.0 Cc1cccc(N2C[C@@H](C)n3nc(COc4ccc(Cl)cn4)cc3C2=O)c1 10.1021/acs.jmedchem.5b01005
CHEMBL3617636 130300 0 None 9 2 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 382 4 0 5 4.0 Cc1cccc(N2C[C@@H](C)n3nc(COc4ccc(Cl)cn4)cc3C2=O)c1 10.1021/acs.jmedchem.5b01005
44329033 214759 0 None 9 5 Rat 7.4 pIC50 = 7.4 Functional
Antagonistic activity against metabotropic glutamate receptor 3 (mGluR3) was evaluatedAntagonistic activity against metabotropic glutamate receptor 3 (mGluR3) was evaluated
ChEMBL 409 7 3 4 4.1 CC(C)C[C@@H]1[C@H](C(=O)O)[C@H]1C(N)(CC1c2ccccc2Oc2ccccc21)C(=O)O 10.1016/s0960-894x(98)00510-1
CHEMBL97200 214759 0 None 9 5 Rat 7.4 pIC50 = 7.4 Functional
Antagonistic activity against metabotropic glutamate receptor 3 (mGluR3) was evaluatedAntagonistic activity against metabotropic glutamate receptor 3 (mGluR3) was evaluated
ChEMBL 409 7 3 4 4.1 CC(C)C[C@@H]1[C@H](C(=O)O)[C@H]1C(N)(CC1c2ccccc2Oc2ccccc21)C(=O)O 10.1016/s0960-894x(98)00510-1
44302686 207695 0 None 1 2 Human 4.4 pIC50 = 4.4 Functional
In vitro antagonist activity at recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.In vitro antagonist activity at recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.
ChEMBL 332 4 3 4 1.4 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2c(Cl)cccc2Cl)C1 10.1016/s0960-894x(98)00352-7
CHEMBL60164 207695 0 None 1 2 Human 4.4 pIC50 = 4.4 Functional
In vitro antagonist activity at recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.In vitro antagonist activity at recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.
ChEMBL 332 4 3 4 1.4 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2c(Cl)cccc2Cl)C1 10.1016/s0960-894x(98)00352-7
122190414 130301 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 382 4 0 5 4.0 Cc1ccc(N2C[C@@H](C)n3nc(COc4ccc(Cl)cn4)cc3C2=O)cc1 10.1021/acs.jmedchem.5b01005
CHEMBL3617637 130301 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 382 4 0 5 4.0 Cc1ccc(N2C[C@@H](C)n3nc(COc4ccc(Cl)cn4)cc3C2=O)cc1 10.1021/acs.jmedchem.5b01005
122190437 130322 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 387 4 0 6 3.3 C[C@@H]1CN(c2ccc(F)nc2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617659 130322 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 387 4 0 6 3.3 C[C@@H]1CN(c2ccc(F)nc2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
122190329 130236 0 None - 1 Rat 5.4 pIC50 = 5.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 435 5 0 5 4.7 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ccc(OC(F)(F)F)cc3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617513 130236 0 None - 1 Rat 5.4 pIC50 = 5.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 435 5 0 5 4.7 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ccc(OC(F)(F)F)cc3)nn21 10.1021/acs.jmedchem.5b01005
122190329 130236 0 None - 1 Rat 5.4 pIC50 = 5.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 435 5 0 5 4.7 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ccc(OC(F)(F)F)cc3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617513 130236 0 None - 1 Rat 5.4 pIC50 = 5.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 435 5 0 5 4.7 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ccc(OC(F)(F)F)cc3)nn21 10.1021/acs.jmedchem.5b01005
122190437 130322 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 387 4 0 6 3.3 C[C@@H]1CN(c2ccc(F)nc2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617659 130322 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 387 4 0 6 3.3 C[C@@H]1CN(c2ccc(F)nc2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
67637138 190397 0 None -2 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 341 5 4 5 0.6 N[C@@]1(C(=O)O)[C@H](CSc2ccc(F)cc2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
CHEMBL4776989 190397 0 None -2 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 341 5 4 5 0.6 N[C@@]1(C(=O)O)[C@H](CSc2ccc(F)cc2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
CHEMBL4802329 190397 0 None -2 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 341 5 4 5 0.6 N[C@@]1(C(=O)O)[C@H](CSc2ccc(F)cc2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
122190414 130301 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 382 4 0 5 4.0 Cc1ccc(N2C[C@@H](C)n3nc(COc4ccc(Cl)cn4)cc3C2=O)cc1 10.1021/acs.jmedchem.5b01005
CHEMBL3617637 130301 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 382 4 0 5 4.0 Cc1ccc(N2C[C@@H](C)n3nc(COc4ccc(Cl)cn4)cc3C2=O)cc1 10.1021/acs.jmedchem.5b01005
122190315 130222 0 None -1 2 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 387 4 0 4 4.1 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ccc(F)cc3F)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617499 130222 0 None -1 2 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 387 4 0 4 4.1 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ccc(F)cc3F)nn21 10.1021/acs.jmedchem.5b01005
122190424 130311 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 404 4 0 5 4.0 C[C@@H]1CN(c2cc(F)cc(F)c2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617647 130311 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 404 4 0 5 4.0 C[C@@H]1CN(c2cc(F)cc(F)c2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
122190315 130222 0 None -1 2 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 387 4 0 4 4.1 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ccc(F)cc3F)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617499 130222 0 None -1 2 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 387 4 0 4 4.1 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ccc(F)cc3F)nn21 10.1021/acs.jmedchem.5b01005
9952648 103083 0 None -1 2 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity at rat mGluR3 expressed in CHO cells assessed as inhibition of glutamate-induced GIRK currentAntagonist activity at rat mGluR3 expressed in CHO cells assessed as inhibition of glutamate-induced GIRK current
ChEMBL 397 3 1 5 4.5 O=C1CC(c2cccc(-n3ccnn3)c2)=Nc2ccc(-c3ccccc3F)cc2N1 10.1016/j.bmcl.2008.02.076
CHEMBL261288 103083 0 None -1 2 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity at rat mGluR3 expressed in CHO cells assessed as inhibition of glutamate-induced GIRK currentAntagonist activity at rat mGluR3 expressed in CHO cells assessed as inhibition of glutamate-induced GIRK current
ChEMBL 397 3 1 5 4.5 O=C1CC(c2cccc(-n3ccnn3)c2)=Nc2ccc(-c3ccccc3F)cc2N1 10.1016/j.bmcl.2008.02.076
44348911 23338 0 None -1 2 Human 6.4 pIC50 = 6.4 Functional
Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3
ChEMBL 331 6 3 3 2.1 N[C@@](CCc1cccc(C(F)(F)F)c1)(C(=O)O)C1C[C@@H]1C(=O)O 10.1021/jm970498o
CHEMBL123847 23338 0 None -1 2 Human 6.4 pIC50 = 6.4 Functional
Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3
ChEMBL 331 6 3 3 2.1 N[C@@](CCc1cccc(C(F)(F)F)c1)(C(=O)O)C1C[C@@H]1C(=O)O 10.1021/jm970498o
122190424 130311 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 404 4 0 5 4.0 C[C@@H]1CN(c2cc(F)cc(F)c2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617647 130311 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 404 4 0 5 4.0 C[C@@H]1CN(c2cc(F)cc(F)c2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
11503055 9179 3 None 31 2 Human 5.4 pIC50 = 5.4 Functional
Negative allosteric modulation of human mGlu3 receptor assessed as Ca2+ flux by FLIPR assayNegative allosteric modulation of human mGlu3 receptor assessed as Ca2+ flux by FLIPR assay
ChEMBL 400 4 1 4 3.9 Clc1ccc(c(c1)Cl)CN[C@H]1CCN(C1)c1ncc(cn1)Br 10.1021/jm400439t
9694 9179 3 None 31 2 Human 5.4 pIC50 = 5.4 Functional
Negative allosteric modulation of human mGlu3 receptor assessed as Ca2+ flux by FLIPR assayNegative allosteric modulation of human mGlu3 receptor assessed as Ca2+ flux by FLIPR assay
ChEMBL 400 4 1 4 3.9 Clc1ccc(c(c1)Cl)CN[C@H]1CCN(C1)c1ncc(cn1)Br 10.1021/jm400439t
CHEMBL2204436 9179 3 None 31 2 Human 5.4 pIC50 = 5.4 Functional
Negative allosteric modulation of human mGlu3 receptor assessed as Ca2+ flux by FLIPR assayNegative allosteric modulation of human mGlu3 receptor assessed as Ca2+ flux by FLIPR assay
ChEMBL 400 4 1 4 3.9 Clc1ccc(c(c1)Cl)CN[C@H]1CCN(C1)c1ncc(cn1)Br 10.1021/jm400439t
122190418 130305 0 None 11 2 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 393 4 0 6 3.6 C[C@@H]1CN(c2ccccc2C#N)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617641 130305 0 None 11 2 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 393 4 0 6 3.6 C[C@@H]1CN(c2ccccc2C#N)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
71136653 130181 0 None -51 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as reversal of DCG-4-inhibited, forskolin-stimulated cAMP production after 1 hr by fluorescence assayAntagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as reversal of DCG-4-inhibited, forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 284 4 4 6 -0.6 N[C@@]1(C(=O)O)C[C@H](Sc2nnc[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
CHEMBL3616854 130181 0 None -51 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as reversal of DCG-4-inhibited, forskolin-stimulated cAMP production after 1 hr by fluorescence assayAntagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as reversal of DCG-4-inhibited, forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 284 4 4 6 -0.6 N[C@@]1(C(=O)O)C[C@H](Sc2nnc[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
122190418 130305 0 None 11 2 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 393 4 0 6 3.6 C[C@@H]1CN(c2ccccc2C#N)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617641 130305 0 None 11 2 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 393 4 0 6 3.6 C[C@@H]1CN(c2ccccc2C#N)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
122190404 130291 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 353 4 0 6 2.6 C[C@@H]1CN(c2cccnc2)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617627 130291 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 353 4 0 6 2.6 C[C@@H]1CN(c2cccnc2)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
122190404 130291 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 353 4 0 6 2.6 C[C@@H]1CN(c2cccnc2)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617627 130291 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 353 4 0 6 2.6 C[C@@H]1CN(c2cccnc2)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
122190417 130304 0 None 10 2 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 398 5 0 6 3.7 COc1ccc(N2C[C@@H](C)n3nc(COc4ccc(Cl)cn4)cc3C2=O)cc1 10.1021/acs.jmedchem.5b01005
CHEMBL3617640 130304 0 None 10 2 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 398 5 0 6 3.7 COc1ccc(N2C[C@@H](C)n3nc(COc4ccc(Cl)cn4)cc3C2=O)cc1 10.1021/acs.jmedchem.5b01005
122190417 130304 0 None 10 2 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 398 5 0 6 3.7 COc1ccc(N2C[C@@H](C)n3nc(COc4ccc(Cl)cn4)cc3C2=O)cc1 10.1021/acs.jmedchem.5b01005
CHEMBL3617640 130304 0 None 10 2 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 398 5 0 6 3.7 COc1ccc(N2C[C@@H](C)n3nc(COc4ccc(Cl)cn4)cc3C2=O)cc1 10.1021/acs.jmedchem.5b01005
122456139 168861 0 None 17 2 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assay
ChEMBL 360 6 0 5 3.5 O=c1cc(OCCOc2ncccc2Cl)ccn1-c1ccc(F)cc1 10.1021/acsmedchemlett.7b00249
CHEMBL4160819 168861 0 None 17 2 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assay
ChEMBL 360 6 0 5 3.5 O=c1cc(OCCOc2ncccc2Cl)ccn1-c1ccc(F)cc1 10.1021/acsmedchemlett.7b00249
122456139 168861 0 None 17 2 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assay
ChEMBL 360 6 0 5 3.5 O=c1cc(OCCOc2ncccc2Cl)ccn1-c1ccc(F)cc1 10.1021/acsmedchemlett.7b00249
CHEMBL4160819 168861 0 None 17 2 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assay
ChEMBL 360 6 0 5 3.5 O=c1cc(OCCOc2ncccc2Cl)ccn1-c1ccc(F)cc1 10.1021/acsmedchemlett.7b00249
60204017 9351 30 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 minsNegative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 353 2 1 3 2.8 COc1ccc(cc1)C#Cc1ccc(c(c1)F)C(=O)N1CCC[C@H](C1)O 10.1021/jm400439t
8765 9351 30 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 minsNegative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 353 2 1 3 2.8 COc1ccc(cc1)C#Cc1ccc(c(c1)F)C(=O)N1CCC[C@H](C1)O 10.1021/jm400439t
CHEMBL2385886 9351 30 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 minsNegative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 353 2 1 3 2.8 COc1ccc(cc1)C#Cc1ccc(c(c1)F)C(=O)N1CCC[C@H](C1)O 10.1021/jm400439t
90643976 118782 0 None - 1 Rat 5.4 pIC50 = 5.4 Functional
Inhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentrationInhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentration
ChEMBL 402 2 0 5 5.1 Cn1c(=O)c2ccc(-c3ccc4ccncc4c3)cc2n2nc(-c3ccccc3)cc12 10.1016/j.bmcl.2014.04.051
CHEMBL3288680 118782 0 None - 1 Rat 5.4 pIC50 = 5.4 Functional
Inhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentrationInhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentration
ChEMBL 402 2 0 5 5.1 Cn1c(=O)c2ccc(-c3ccc4ccncc4c3)cc2n2nc(-c3ccccc3)cc12 10.1016/j.bmcl.2014.04.051
60204016 97107 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 minsNegative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 353 2 1 3 2.8 COc1ccc(C#Cc2ccc(C(=O)N3CCC[C@@H](O)C3)cc2F)cc1 10.1021/jm400439t
CHEMBL2385887 97107 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 minsNegative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 353 2 1 3 2.8 COc1ccc(C#Cc2ccc(C(=O)N3CCC[C@@H](O)C3)cc2F)cc1 10.1021/jm400439t
162652146 186992 0 None -1 2 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 289 5 4 5 -0.2 CC(C)SC[C@@H]1[C@@H](O)[C@@H]2[C@@H]([C@H]2C(=O)O)[C@]1(N)C(=O)O 10.1021/acs.jmedchem.6b01119
CHEMBL4749728 186992 0 None -1 2 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 289 5 4 5 -0.2 CC(C)SC[C@@H]1[C@@H](O)[C@@H]2[C@@H]([C@H]2C(=O)O)[C@]1(N)C(=O)O 10.1021/acs.jmedchem.6b01119
122190314 130221 0 None -5 2 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 369 4 0 4 4.0 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ccc(F)cc3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617498 130221 0 None -5 2 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 369 4 0 4 4.0 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ccc(F)cc3)nn21 10.1021/acs.jmedchem.5b01005
60204016 97107 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 minsNegative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 353 2 1 3 2.8 COc1ccc(C#Cc2ccc(C(=O)N3CCC[C@@H](O)C3)cc2F)cc1 10.1021/jm400439t
CHEMBL2385887 97107 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 minsNegative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 353 2 1 3 2.8 COc1ccc(C#Cc2ccc(C(=O)N3CCC[C@@H](O)C3)cc2F)cc1 10.1021/jm400439t
71137034 130177 0 None -7 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as reversal of DCG-4-inhibited, forskolin-stimulated cAMP production after 1 hr by fluorescence assayAntagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as reversal of DCG-4-inhibited, forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 334 5 4 6 0.3 N[C@@]1(C(=O)O)C[C@@H](Sc2nnc(C(F)F)[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
CHEMBL3616850 130177 0 None -7 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as reversal of DCG-4-inhibited, forskolin-stimulated cAMP production after 1 hr by fluorescence assayAntagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as reversal of DCG-4-inhibited, forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 334 5 4 6 0.3 N[C@@]1(C(=O)O)C[C@@H](Sc2nnc(C(F)F)[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
57338826 156406 0 None -1 5 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assayAntagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 375 5 4 5 1.0 N[C@@]1(C(=O)O)[C@H](OCc2ccc(Cl)c(Cl)c2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1016/j.bmcl.2016.10.067
CHEMBL3947221 156406 0 None -1 5 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assayAntagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 375 5 4 5 1.0 N[C@@]1(C(=O)O)[C@H](OCc2ccc(Cl)c(Cl)c2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1016/j.bmcl.2016.10.067
122190314 130221 0 None -5 2 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 369 4 0 4 4.0 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ccc(F)cc3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617498 130221 0 None -5 2 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 369 4 0 4 4.0 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ccc(F)cc3)nn21 10.1021/acs.jmedchem.5b01005
10852666 85516 0 None -1 2 Human 6.3 pIC50 = 6.3 Functional
Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3
ChEMBL 313 6 3 3 2.3 NC(CCc1cccc2ccccc12)(C(=O)O)[C@H]1C[C@@H]1C(=O)O 10.1021/jm970497w
CHEMBL2112583 85516 0 None -1 2 Human 6.3 pIC50 = 6.3 Functional
Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3
ChEMBL 313 6 3 3 2.3 NC(CCc1cccc2ccccc12)(C(=O)O)[C@H]1C[C@@H]1C(=O)O 10.1021/jm970497w
122190434 130319 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 387 4 0 6 3.3 C[C@@H]1CN(c2cnccc2F)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617656 130319 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 387 4 0 6 3.3 C[C@@H]1CN(c2cnccc2F)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
122190435 130320 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 387 4 0 6 3.3 C[C@@H]1CN(c2cncc(F)c2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617657 130320 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 387 4 0 6 3.3 C[C@@H]1CN(c2cncc(F)c2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
122190435 130320 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 387 4 0 6 3.3 C[C@@H]1CN(c2cncc(F)c2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617657 130320 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 387 4 0 6 3.3 C[C@@H]1CN(c2cncc(F)c2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
122190434 130319 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 387 4 0 6 3.3 C[C@@H]1CN(c2cnccc2F)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617656 130319 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 387 4 0 6 3.3 C[C@@H]1CN(c2cnccc2F)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
90643974 118780 0 None 3 2 Rat 6.3 pIC50 = 6.3 Functional
Inhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentrationInhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentration
ChEMBL 352 2 0 5 3.9 Cn1c(=O)c2ccc(-c3ccncc3)cc2n2nc(-c3ccccc3)cc12 10.1016/j.bmcl.2014.04.051
CHEMBL3288675 118780 0 None 3 2 Rat 6.3 pIC50 = 6.3 Functional
Inhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentrationInhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentration
ChEMBL 352 2 0 5 3.9 Cn1c(=O)c2ccc(-c3ccncc3)cc2n2nc(-c3ccccc3)cc12 10.1016/j.bmcl.2014.04.051
122190312 130219 0 None -2 2 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 369 4 0 4 4.0 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ccccc3F)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617496 130219 0 None -2 2 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 369 4 0 4 4.0 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ccccc3F)nn21 10.1021/acs.jmedchem.5b01005
122190425 130312 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 411 4 0 6 3.7 C[C@@H]1CN(c2cc(F)ccc2C#N)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617648 130312 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 411 4 0 6 3.7 C[C@@H]1CN(c2cc(F)ccc2C#N)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
71137010 130176 0 None -5 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as reversal of DCG-4-inhibited, forskolin-stimulated cAMP production after 1 hr by fluorescence assayAntagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as reversal of DCG-4-inhibited, forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 352 4 4 6 0.4 N[C@@]1(C(=O)O)C[C@@H](Sc2nnc(C(F)(F)F)[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
CHEMBL3616849 130176 0 None -5 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as reversal of DCG-4-inhibited, forskolin-stimulated cAMP production after 1 hr by fluorescence assayAntagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as reversal of DCG-4-inhibited, forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 352 4 4 6 0.4 N[C@@]1(C(=O)O)C[C@@H](Sc2nnc(C(F)(F)F)[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
122190425 130312 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 411 4 0 6 3.7 C[C@@H]1CN(c2cc(F)ccc2C#N)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617648 130312 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 411 4 0 6 3.7 C[C@@H]1CN(c2cc(F)ccc2C#N)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
90643963 118772 0 None 3 2 Rat 6.3 pIC50 = 6.3 Functional
Inhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentrationInhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentration
ChEMBL 366 2 0 5 4.2 Cc1cccc(-c2cc3n(C)c(=O)c4ccc(-c5cccnc5)cc4n3n2)c1 10.1016/j.bmcl.2014.04.051
CHEMBL3288653 118772 0 None 3 2 Rat 6.3 pIC50 = 6.3 Functional
Inhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentrationInhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentration
ChEMBL 366 2 0 5 4.2 Cc1cccc(-c2cc3n(C)c(=O)c4ccc(-c5cccnc5)cc4n3n2)c1 10.1016/j.bmcl.2014.04.051
122190312 130219 0 None -2 2 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 369 4 0 4 4.0 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ccccc3F)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617496 130219 0 None -2 2 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 369 4 0 4 4.0 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ccccc3F)nn21 10.1021/acs.jmedchem.5b01005
122190319 130226 0 None -1 2 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 385 4 0 4 4.5 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ccccc3Cl)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617503 130226 0 None -1 2 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 385 4 0 4 4.5 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ccccc3Cl)nn21 10.1021/acs.jmedchem.5b01005
122190319 130226 0 None -1 2 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 385 4 0 4 4.5 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ccccc3Cl)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617503 130226 0 None -1 2 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 385 4 0 4 4.5 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ccccc3Cl)nn21 10.1021/acs.jmedchem.5b01005
122190336 130243 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 370 4 0 5 3.4 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617520 130243 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 370 4 0 5 3.4 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
122190420 130307 0 None 6 2 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 393 4 0 6 3.6 C[C@@H]1CN(c2ccc(C#N)cc2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617643 130307 0 None 6 2 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 393 4 0 6 3.6 C[C@@H]1CN(c2ccc(C#N)cc2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
122190336 130243 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 370 4 0 5 3.4 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617520 130243 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 370 4 0 5 3.4 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
122190420 130307 0 None 6 2 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 393 4 0 6 3.6 C[C@@H]1CN(c2ccc(C#N)cc2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617643 130307 0 None 6 2 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 393 4 0 6 3.6 C[C@@H]1CN(c2ccc(C#N)cc2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
134137754 154726 0 None -1 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assayAntagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 400 6 3 5 2.3 [N-]=[N+]=N[C@H]1[C@H]2[C@H](C(=O)O)[C@H]2[C@](N)(C(=O)O)[C@@H]1OCc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2016.10.067
CHEMBL3933829 154726 0 None -1 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assayAntagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 400 6 3 5 2.3 [N-]=[N+]=N[C@H]1[C@H]2[C@H](C(=O)O)[C@H]2[C@](N)(C(=O)O)[C@@H]1OCc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2016.10.067
162665071 190507 0 None -1 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 323 5 4 5 0.5 N[C@@]1(C(=O)O)[C@H](CSc2ccccc2)[C@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
CHEMBL4781638 190507 0 None -1 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 323 5 4 5 0.5 N[C@@]1(C(=O)O)[C@H](CSc2ccccc2)[C@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
CHEMBL4803454 190507 0 None -1 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 323 5 4 5 0.5 N[C@@]1(C(=O)O)[C@H](CSc2ccccc2)[C@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
60210800 97097 0 None - 1 Rat 5.3 pIC50 = 5.3 Functional
Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 minsNegative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 349 3 0 3 3.3 COc1ccc(C#Cc2ccc(C(=O)N3CCCC(OC)C3)cc2)cc1 10.1021/jm400439t
CHEMBL2385876 97097 0 None - 1 Rat 5.3 pIC50 = 5.3 Functional
Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 minsNegative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 349 3 0 3 3.3 COc1ccc(C#Cc2ccc(C(=O)N3CCCC(OC)C3)cc2)cc1 10.1021/jm400439t
60210782 97106 0 None - 1 Rat 5.3 pIC50 = 5.3 Functional
Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 minsNegative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 361 2 1 3 2.9 COc1ccc(C#Cc2ccc(C(=O)N3CC4CCC(O)C4C3)cc2)cc1 10.1021/jm400439t
CHEMBL2385885 97106 0 None - 1 Rat 5.3 pIC50 = 5.3 Functional
Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 minsNegative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 361 2 1 3 2.9 COc1ccc(C#Cc2ccc(C(=O)N3CC4CCC(O)C4C3)cc2)cc1 10.1021/jm400439t
10826383 85517 0 None 1 2 Human 6.3 pIC50 = 6.3 Functional
Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3
ChEMBL 277 7 3 3 1.5 NC(CCCc1ccccc1)(C(=O)O)[C@H]1C[C@@H]1C(=O)O 10.1021/jm970497w
CHEMBL2112584 85517 0 None 1 2 Human 6.3 pIC50 = 6.3 Functional
Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3
ChEMBL 277 7 3 3 1.5 NC(CCCc1ccccc1)(C(=O)O)[C@H]1C[C@@H]1C(=O)O 10.1021/jm970497w
71136640 130180 0 None -60 2 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization after 1.5 hrs by FLIPR assayAntagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization after 1.5 hrs by FLIPR assay
ChEMBL 284 4 4 6 -0.6 N[C@@]1(C(=O)O)C[C@@H](Sc2c[nH]nn2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
CHEMBL3616853 130180 0 None -60 2 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization after 1.5 hrs by FLIPR assayAntagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization after 1.5 hrs by FLIPR assay
ChEMBL 284 4 4 6 -0.6 N[C@@]1(C(=O)O)C[C@@H](Sc2c[nH]nn2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
122190410 130297 0 None 5 2 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 402 4 0 5 4.4 C[C@@H]1CN(c2cccc(Cl)c2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617633 130297 0 None 5 2 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 402 4 0 5 4.4 C[C@@H]1CN(c2cccc(Cl)c2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
67633284 190426 0 None -5 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 391 5 4 5 1.8 N[C@@]1(C(=O)O)[C@H](CSc2ccc(Cl)c(Cl)c2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
CHEMBL4748699 190426 0 None -5 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 391 5 4 5 1.8 N[C@@]1(C(=O)O)[C@H](CSc2ccc(Cl)c(Cl)c2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
CHEMBL4802655 190426 0 None -5 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 391 5 4 5 1.8 N[C@@]1(C(=O)O)[C@H](CSc2ccc(Cl)c(Cl)c2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
122190410 130297 0 None 5 2 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 402 4 0 5 4.4 C[C@@H]1CN(c2cccc(Cl)c2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617633 130297 0 None 5 2 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 402 4 0 5 4.4 C[C@@H]1CN(c2cccc(Cl)c2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
10778385 85514 0 None 1 2 Human 6.2 pIC50 = 6.2 Functional
Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3
ChEMBL 269 6 3 4 1.2 NC(CCc1ccsc1)(C(=O)O)[C@H]1C[C@@H]1C(=O)O 10.1021/jm970497w
CHEMBL2112581 85514 0 None 1 2 Human 6.2 pIC50 = 6.2 Functional
Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3
ChEMBL 269 6 3 4 1.2 NC(CCc1ccsc1)(C(=O)O)[C@H]1C[C@@H]1C(=O)O 10.1021/jm970497w
122190412 130299 0 None 3 2 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 382 4 0 5 4.0 Cc1ccccc1N1C[C@@H](C)n2nc(COc3ccc(Cl)cn3)cc2C1=O 10.1021/acs.jmedchem.5b01005
CHEMBL3617635 130299 0 None 3 2 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 382 4 0 5 4.0 Cc1ccccc1N1C[C@@H](C)n2nc(COc3ccc(Cl)cn3)cc2C1=O 10.1021/acs.jmedchem.5b01005
122190412 130299 0 None 3 2 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 382 4 0 5 4.0 Cc1ccccc1N1C[C@@H](C)n2nc(COc3ccc(Cl)cn3)cc2C1=O 10.1021/acs.jmedchem.5b01005
CHEMBL3617635 130299 0 None 3 2 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 382 4 0 5 4.0 Cc1ccccc1N1C[C@@H](C)n2nc(COc3ccc(Cl)cn3)cc2C1=O 10.1021/acs.jmedchem.5b01005
60204017 9351 30 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 minsNegative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 353 2 1 3 2.8 COc1ccc(cc1)C#Cc1ccc(c(c1)F)C(=O)N1CCC[C@H](C1)O 10.1021/jm400439t
8765 9351 30 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 minsNegative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 353 2 1 3 2.8 COc1ccc(cc1)C#Cc1ccc(c(c1)F)C(=O)N1CCC[C@H](C1)O 10.1021/jm400439t
CHEMBL2385886 9351 30 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 minsNegative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 353 2 1 3 2.8 COc1ccc(cc1)C#Cc1ccc(c(c1)F)C(=O)N1CCC[C@H](C1)O 10.1021/jm400439t
11235624 63079 0 None 1 3 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity at rat mGluR3 receptor expressed in CHO cells assessed as inhibition of GIRK currentAntagonist activity at rat mGluR3 receptor expressed in CHO cells assessed as inhibition of GIRK current
ChEMBL 425 4 1 4 5.6 CCOc1cc2c(cc1C(F)(F)F)NC(=O)CC(c1cccc(-c3ccncc3)c1)=N2 10.1016/j.bmcl.2010.09.125
CHEMBL1629862 63079 0 None 1 3 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity at rat mGluR3 receptor expressed in CHO cells assessed as inhibition of GIRK currentAntagonist activity at rat mGluR3 receptor expressed in CHO cells assessed as inhibition of GIRK current
ChEMBL 425 4 1 4 5.6 CCOc1cc2c(cc1C(F)(F)F)NC(=O)CC(c1cccc(-c3ccncc3)c1)=N2 10.1016/j.bmcl.2010.09.125
69669747 190432 11 None 2 4 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 359 5 4 5 0.8 N[C@@]1(C(=O)O)[C@H](CSc2ccc(F)c(F)c2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
CHEMBL4751065 190432 11 None 2 4 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 359 5 4 5 0.8 N[C@@]1(C(=O)O)[C@H](CSc2ccc(F)c(F)c2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
CHEMBL4802733 190432 11 None 2 4 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 359 5 4 5 0.8 N[C@@]1(C(=O)O)[C@H](CSc2ccc(F)c(F)c2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
122190337 130244 0 None 4 2 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 386 4 0 5 3.9 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617521 130244 0 None 4 2 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 386 4 0 5 3.9 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
122190428 130315 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 369 4 0 6 3.1 C[C@@H]1CN(c2cccnc2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617651 130315 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 369 4 0 6 3.1 C[C@@H]1CN(c2cccnc2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
122190436 130321 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 394 4 0 7 3.0 C[C@@H]1CN(c2cncc(C#N)c2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617658 130321 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 394 4 0 7 3.0 C[C@@H]1CN(c2cncc(C#N)c2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
60204017 9351 30 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 minsNegative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 353 2 1 3 2.8 COc1ccc(cc1)C#Cc1ccc(c(c1)F)C(=O)N1CCC[C@H](C1)O 10.1021/jm400439t
8765 9351 30 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 minsNegative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 353 2 1 3 2.8 COc1ccc(cc1)C#Cc1ccc(c(c1)F)C(=O)N1CCC[C@H](C1)O 10.1021/jm400439t
CHEMBL2385886 9351 30 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 minsNegative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 353 2 1 3 2.8 COc1ccc(cc1)C#Cc1ccc(c(c1)F)C(=O)N1CCC[C@H](C1)O 10.1021/jm400439t
122190337 130244 0 None 4 2 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 386 4 0 5 3.9 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617521 130244 0 None 4 2 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 386 4 0 5 3.9 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
122190436 130321 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 394 4 0 7 3.0 C[C@@H]1CN(c2cncc(C#N)c2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617658 130321 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 394 4 0 7 3.0 C[C@@H]1CN(c2cncc(C#N)c2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
122190428 130315 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 369 4 0 6 3.1 C[C@@H]1CN(c2cccnc2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617651 130315 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 369 4 0 6 3.1 C[C@@H]1CN(c2cccnc2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
69669646 190458 0 None -2 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 351 5 4 5 1.1 Cc1ccc(SC[C@@H]2[C@@H](O)[C@@H]3[C@@H]([C@H]3C(=O)O)[C@]2(N)C(=O)O)cc1C 10.1021/acs.jmedchem.6b01119
CHEMBL4757159 190458 0 None -2 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 351 5 4 5 1.1 Cc1ccc(SC[C@@H]2[C@@H](O)[C@@H]3[C@@H]([C@H]3C(=O)O)[C@]2(N)C(=O)O)cc1C 10.1021/acs.jmedchem.6b01119
CHEMBL4802990 190458 0 None -2 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 351 5 4 5 1.1 Cc1ccc(SC[C@@H]2[C@@H](O)[C@@H]3[C@@H]([C@H]3C(=O)O)[C@]2(N)C(=O)O)cc1C 10.1021/acs.jmedchem.6b01119
10359073 161753 1 None 1 2 Human 5.2 pIC50 = 5.2 Functional
Tested for agonist activity in non-neuronal cells (RGT) expressing human Metabotropic glutamate receptor 3 by measuring ACPD (3 uM) induced inhibition of forskolin (15 uM)-stimulated cAMP formationTested for agonist activity in non-neuronal cells (RGT) expressing human Metabotropic glutamate receptor 3 by measuring ACPD (3 uM) induced inhibition of forskolin (15 uM)-stimulated cAMP formation
ChEMBL 327 8 3 3 2.7 N[C@@H](C[C@H](CC(c1ccccc1)c1ccccc1)C(=O)O)C(=O)O 10.1016/s0960-894x(98)00091-2
CHEMBL40123 161753 1 None 1 2 Human 5.2 pIC50 = 5.2 Functional
Tested for agonist activity in non-neuronal cells (RGT) expressing human Metabotropic glutamate receptor 3 by measuring ACPD (3 uM) induced inhibition of forskolin (15 uM)-stimulated cAMP formationTested for agonist activity in non-neuronal cells (RGT) expressing human Metabotropic glutamate receptor 3 by measuring ACPD (3 uM) induced inhibition of forskolin (15 uM)-stimulated cAMP formation
ChEMBL 327 8 3 3 2.7 N[C@@H](C[C@H](CC(c1ccccc1)c1ccccc1)C(=O)O)C(=O)O 10.1016/s0960-894x(98)00091-2
162658340 190465 0 None -1 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 405 6 4 5 1.9 N[C@@]1(C(=O)O)[C@H](CSCc2ccc(Cl)c(Cl)c2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
CHEMBL4760856 190465 0 None -1 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 405 6 4 5 1.9 N[C@@]1(C(=O)O)[C@H](CSCc2ccc(Cl)c(Cl)c2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
CHEMBL4803084 190465 0 None -1 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 405 6 4 5 1.9 N[C@@]1(C(=O)O)[C@H](CSCc2ccc(Cl)c(Cl)c2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
90098428 130183 0 None -60 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization after 1.5 hrs by FLIPR assayAntagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization after 1.5 hrs by FLIPR assay
ChEMBL 352 4 4 6 0.4 N[C@@]1(C(=O)O)C[C@H](Sc2nnc(C(F)(F)F)[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
CHEMBL3616856 130183 0 None -60 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization after 1.5 hrs by FLIPR assayAntagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization after 1.5 hrs by FLIPR assay
ChEMBL 352 4 4 6 0.4 N[C@@]1(C(=O)O)C[C@H](Sc2nnc(C(F)(F)F)[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
44302856 109508 0 None -1 2 Human 4.2 pIC50 = 4.2 Functional
In vitro antagonist activity at recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.In vitro antagonist activity at recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.
ChEMBL 354 6 3 4 1.8 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(CC(c2ccccc2)c2ccccc2)C1 10.1016/s0960-894x(98)00352-7
CHEMBL304919 109508 0 None -1 2 Human 4.2 pIC50 = 4.2 Functional
In vitro antagonist activity at recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.In vitro antagonist activity at recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.
ChEMBL 354 6 3 4 1.8 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(CC(c2ccccc2)c2ccccc2)C1 10.1016/s0960-894x(98)00352-7
90643971 118778 0 None 1 2 Rat 6.2 pIC50 = 6.2 Functional
Inhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentrationInhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentration
ChEMBL 386 2 0 5 4.6 Cn1c(=O)c2ccc(-c3cccnc3)cc2n2nc(-c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2014.04.051
CHEMBL3288667 118778 0 None 1 2 Rat 6.2 pIC50 = 6.2 Functional
Inhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentrationInhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentration
ChEMBL 386 2 0 5 4.6 Cn1c(=O)c2ccc(-c3cccnc3)cc2n2nc(-c3ccc(Cl)cc3)cc12 10.1016/j.bmcl.2014.04.051
10587622 85515 0 None 1 2 Human 6.2 pIC50 = 6.2 Functional
Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3
ChEMBL 263 6 3 3 1.1 NC(CCc1ccccc1)(C(=O)O)[C@H]1C[C@@H]1C(=O)O 10.1021/jm970497w
CHEMBL2112582 85515 0 None 1 2 Human 6.2 pIC50 = 6.2 Functional
Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3
ChEMBL 263 6 3 3 1.1 NC(CCc1ccccc1)(C(=O)O)[C@H]1C[C@@H]1C(=O)O 10.1021/jm970497w
10587622 85515 0 None 1 2 Human 6.2 pIC50 = 6.2 Functional
Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3
ChEMBL 263 6 3 3 1.1 NC(CCc1ccccc1)(C(=O)O)[C@H]1C[C@@H]1C(=O)O 10.1021/jm970498o
CHEMBL2112582 85515 0 None 1 2 Human 6.2 pIC50 = 6.2 Functional
Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3
ChEMBL 263 6 3 3 1.1 NC(CCc1ccccc1)(C(=O)O)[C@H]1C[C@@H]1C(=O)O 10.1021/jm970498o
60204018 97099 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 minsNegative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 335 2 1 3 2.7 COc1ccc(C#Cc2ccc(C(=O)N3CCC[C@@H](O)C3)cc2)cc1 10.1021/jm400439t
CHEMBL2385878 97099 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 minsNegative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 335 2 1 3 2.7 COc1ccc(C#Cc2ccc(C(=O)N3CCC[C@@H](O)C3)cc2)cc1 10.1021/jm400439t
CHEMBL2385888 97099 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 minsNegative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 335 2 1 3 2.7 COc1ccc(C#Cc2ccc(C(=O)N3CCC[C@@H](O)C3)cc2)cc1 10.1021/jm400439t
56587994 10817 41 None -1 2 Human 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of mGlu3 assessed as inhibition of glutamate-induced calcium mobilization in presence of Galpha15 by cell based assayNegative allosteric modulation of mGlu3 assessed as inhibition of glutamate-induced calcium mobilization in presence of Galpha15 by cell based assay
ChEMBL 349 3 1 3 2.9 OC[C@@H]1CCCN(C1)C(=O)c1ccc(cc1)C#Cc1ccc(cc1)OC 10.1016/j.bmcl.2012.04.112
6225 10817 41 None -1 2 Human 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of mGlu3 assessed as inhibition of glutamate-induced calcium mobilization in presence of Galpha15 by cell based assayNegative allosteric modulation of mGlu3 assessed as inhibition of glutamate-induced calcium mobilization in presence of Galpha15 by cell based assay
ChEMBL 349 3 1 3 2.9 OC[C@@H]1CCCN(C1)C(=O)c1ccc(cc1)C#Cc1ccc(cc1)OC 10.1016/j.bmcl.2012.04.112
CHEMBL2204445 10817 41 None -1 2 Human 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of mGlu3 assessed as inhibition of glutamate-induced calcium mobilization in presence of Galpha15 by cell based assayNegative allosteric modulation of mGlu3 assessed as inhibition of glutamate-induced calcium mobilization in presence of Galpha15 by cell based assay
ChEMBL 349 3 1 3 2.9 OC[C@@H]1CCCN(C1)C(=O)c1ccc(cc1)C#Cc1ccc(cc1)OC 10.1016/j.bmcl.2012.04.112
60204018 97099 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 minsNegative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 335 2 1 3 2.7 COc1ccc(C#Cc2ccc(C(=O)N3CCC[C@@H](O)C3)cc2)cc1 10.1021/jm400439t
CHEMBL2385878 97099 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 minsNegative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 335 2 1 3 2.7 COc1ccc(C#Cc2ccc(C(=O)N3CCC[C@@H](O)C3)cc2)cc1 10.1021/jm400439t
CHEMBL2385888 97099 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 minsNegative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 335 2 1 3 2.7 COc1ccc(C#Cc2ccc(C(=O)N3CCC[C@@H](O)C3)cc2)cc1 10.1021/jm400439t
90643968 118776 0 None 6 2 Rat 7.2 pIC50 = 7.2 Functional
Inhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentrationInhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentration
ChEMBL 370 2 0 5 4.1 Cn1c(=O)c2ccc(-c3cccnc3)cc2n2nc(-c3ccc(F)cc3)cc12 10.1016/j.bmcl.2014.04.051
CHEMBL3288662 118776 0 None 6 2 Rat 7.2 pIC50 = 7.2 Functional
Inhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentrationInhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentration
ChEMBL 370 2 0 5 4.1 Cn1c(=O)c2ccc(-c3cccnc3)cc2n2nc(-c3ccc(F)cc3)cc12 10.1016/j.bmcl.2014.04.051
122190430 130317 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 394 4 0 7 3.0 C[C@@H]1CN(c2ncccc2C#N)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617653 130317 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 394 4 0 7 3.0 C[C@@H]1CN(c2ncccc2C#N)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
122190332 130239 0 None - 1 Rat 5.2 pIC50 = 5.2 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 382 5 0 6 3.2 COc1cccnc1OCc1cc2n(n1)[C@H](C)CN(c1ccc(F)cc1)C2=O 10.1021/acs.jmedchem.5b01005
CHEMBL3617516 130239 0 None - 1 Rat 5.2 pIC50 = 5.2 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 382 5 0 6 3.2 COc1cccnc1OCc1cc2n(n1)[C@H](C)CN(c1ccc(F)cc1)C2=O 10.1021/acs.jmedchem.5b01005
122190332 130239 0 None - 1 Rat 5.2 pIC50 = 5.2 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 382 5 0 6 3.2 COc1cccnc1OCc1cc2n(n1)[C@H](C)CN(c1ccc(F)cc1)C2=O 10.1021/acs.jmedchem.5b01005
CHEMBL3617516 130239 0 None - 1 Rat 5.2 pIC50 = 5.2 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 382 5 0 6 3.2 COc1cccnc1OCc1cc2n(n1)[C@H](C)CN(c1ccc(F)cc1)C2=O 10.1021/acs.jmedchem.5b01005
122190430 130317 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 394 4 0 7 3.0 C[C@@H]1CN(c2ncccc2C#N)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617653 130317 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 394 4 0 7 3.0 C[C@@H]1CN(c2ncccc2C#N)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
19702198 168101 16 None -1 2 Rat 4.2 pIC50 = 4.2 Functional
Inhibitory concentration required for antagonistic activity at Metabotropic glutamate receptor 3Inhibitory concentration required for antagonistic activity at Metabotropic glutamate receptor 3
ChEMBL 173 3 3 3 -0.5 CC(N)(C(=O)O)C1CC1C(=O)O 10.1016/s0960-894x(01)00329-8
CHEMBL412445 168101 16 None -1 2 Rat 4.2 pIC50 = 4.2 Functional
Inhibitory concentration required for antagonistic activity at Metabotropic glutamate receptor 3Inhibitory concentration required for antagonistic activity at Metabotropic glutamate receptor 3
ChEMBL 173 3 3 3 -0.5 CC(N)(C(=O)O)C1CC1C(=O)O 10.1016/s0960-894x(01)00329-8
122190415 130302 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 398 5 0 6 3.7 COc1ccccc1N1C[C@@H](C)n2nc(COc3ccc(Cl)cn3)cc2C1=O 10.1021/acs.jmedchem.5b01005
CHEMBL3617638 130302 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 398 5 0 6 3.7 COc1ccccc1N1C[C@@H](C)n2nc(COc3ccc(Cl)cn3)cc2C1=O 10.1021/acs.jmedchem.5b01005
122190415 130302 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 398 5 0 6 3.7 COc1ccccc1N1C[C@@H](C)n2nc(COc3ccc(Cl)cn3)cc2C1=O 10.1021/acs.jmedchem.5b01005
CHEMBL3617638 130302 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 398 5 0 6 3.7 COc1ccccc1N1C[C@@H](C)n2nc(COc3ccc(Cl)cn3)cc2C1=O 10.1021/acs.jmedchem.5b01005
90643959 118770 0 None 1 2 Rat 6.2 pIC50 = 6.2 Functional
Inhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentrationInhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentration
ChEMBL 460 4 1 7 3.2 COc1cccc(-c2cc3n(C)c(=O)c4ccc(-c5cccc(S(N)(=O)=O)c5)cc4n3n2)c1 10.1016/j.bmcl.2014.04.051
CHEMBL3288646 118770 0 None 1 2 Rat 6.2 pIC50 = 6.2 Functional
Inhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentrationInhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentration
ChEMBL 460 4 1 7 3.2 COc1cccc(-c2cc3n(C)c(=O)c4ccc(-c5cccc(S(N)(=O)=O)c5)cc4n3n2)c1 10.1016/j.bmcl.2014.04.051
1378 9195 54 None 2 14 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/acs.jmedchem.6b01119
1399 9195 54 None 2 14 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/acs.jmedchem.6b01119
9819927 9195 54 None 2 14 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/acs.jmedchem.6b01119
CHEMBL432038 9195 54 None 2 14 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/acs.jmedchem.6b01119
134155683 158140 0 None -1 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assayAntagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 377 5 3 4 2.0 N[C@@]1(C(=O)O)[C@H](OCc2ccc(Cl)c(Cl)c2)[C@@H](F)[C@H]2[C@H](C(=O)O)[C@H]21 10.1016/j.bmcl.2016.10.067
CHEMBL3961306 158140 0 None -1 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assayAntagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 377 5 3 4 2.0 N[C@@]1(C(=O)O)[C@H](OCc2ccc(Cl)c(Cl)c2)[C@@H](F)[C@H]2[C@H](C(=O)O)[C@H]21 10.1016/j.bmcl.2016.10.067
60204019 97104 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 minsNegative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 349 2 1 3 3.1 COc1ccc(C#Cc2ccc(C(=O)N3CCCC(C)(O)C3)cc2)cc1 10.1021/jm400439t
CHEMBL2385883 97104 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 minsNegative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 349 2 1 3 3.1 COc1ccc(C#Cc2ccc(C(=O)N3CCCC(C)(O)C3)cc2)cc1 10.1021/jm400439t
122190316 130223 0 None 2 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 365 4 0 4 4.1 Cc1ccccc1OCc1cc2n(n1)[C@H](C)CN(c1ccc(F)cc1)C2=O 10.1021/acs.jmedchem.5b01005
CHEMBL3617500 130223 0 None 2 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 365 4 0 4 4.1 Cc1ccccc1OCc1cc2n(n1)[C@H](C)CN(c1ccc(F)cc1)C2=O 10.1021/acs.jmedchem.5b01005
122190316 130223 0 None 2 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 365 4 0 4 4.1 Cc1ccccc1OCc1cc2n(n1)[C@H](C)CN(c1ccc(F)cc1)C2=O 10.1021/acs.jmedchem.5b01005
CHEMBL3617500 130223 0 None 2 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 365 4 0 4 4.1 Cc1ccccc1OCc1cc2n(n1)[C@H](C)CN(c1ccc(F)cc1)C2=O 10.1021/acs.jmedchem.5b01005
60210806 97100 0 None - 1 Rat 5.1 pIC50 = 5.1 Functional
Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 minsNegative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 309 4 2 3 2.2 COc1ccc(C#Cc2ccc(C(=O)NC(C)CO)cc2)cc1 10.1021/jm400439t
CHEMBL2385879 97100 0 None - 1 Rat 5.1 pIC50 = 5.1 Functional
Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 minsNegative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 309 4 2 3 2.2 COc1ccc(C#Cc2ccc(C(=O)NC(C)CO)cc2)cc1 10.1021/jm400439t
56587989 97103 0 None - 1 Rat 5.1 pIC50 = 5.1 Functional
Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 minsNegative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 335 3 1 3 2.5 COc1ccc(C#Cc2ccc(C(=O)N3CCC(CO)C3)cc2)cc1 10.1021/jm400439t
CHEMBL2385882 97103 0 None - 1 Rat 5.1 pIC50 = 5.1 Functional
Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 minsNegative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 335 3 1 3 2.5 COc1ccc(C#Cc2ccc(C(=O)N3CCC(CO)C3)cc2)cc1 10.1021/jm400439t
44329042 175862 0 None 33 5 Rat 7.1 pIC50 = 7.1 Functional
Antagonistic activity against metabotropic glutamate receptor 3 (mGluR3) was evaluatedAntagonistic activity against metabotropic glutamate receptor 3 (mGluR3) was evaluated
ChEMBL 381 6 3 4 3.5 CC[C@@H]1[C@H](C(=O)O)[C@H]1C(N)(CC1c2ccccc2Oc2ccccc21)C(=O)O 10.1016/s0960-894x(98)00510-1
CHEMBL439775 175862 0 None 33 5 Rat 7.1 pIC50 = 7.1 Functional
Antagonistic activity against metabotropic glutamate receptor 3 (mGluR3) was evaluatedAntagonistic activity against metabotropic glutamate receptor 3 (mGluR3) was evaluated
ChEMBL 381 6 3 4 3.5 CC[C@@H]1[C@H](C(=O)O)[C@H]1C(N)(CC1c2ccccc2Oc2ccccc21)C(=O)O 10.1016/s0960-894x(98)00510-1
21309795 157602 0 None 3 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assayAntagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 327 4 3 3 1.8 N[C@@]1(C(=O)O)[C@H](Cc2ccc(F)c(Cl)c2)C[C@H]2[C@H](C(=O)O)[C@H]21 10.1016/j.bmcl.2016.10.067
CHEMBL3956934 157602 0 None 3 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assayAntagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 327 4 3 3 1.8 N[C@@]1(C(=O)O)[C@H](Cc2ccc(F)c(Cl)c2)C[C@H]2[C@H](C(=O)O)[C@H]21 10.1016/j.bmcl.2016.10.067
10567792 85519 0 None -3 2 Human 6.1 pIC50 = 6.1 Functional
Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3
ChEMBL 321 6 3 3 2.5 NC(CCC12CC3CC(CC(C3)C1)C2)(C(=O)O)[C@H]1C[C@@H]1C(=O)O 10.1021/jm970497w
CHEMBL2112586 85519 0 None -3 2 Human 6.1 pIC50 = 6.1 Functional
Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3Ability to block 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in non-neuronal cell line expressing human Metabotropic glutamate receptor 3
ChEMBL 321 6 3 3 2.5 NC(CCC12CC3CC(CC(C3)C1)C2)(C(=O)O)[C@H]1C[C@@H]1C(=O)O 10.1021/jm970497w
53393854 90377 0 None 2 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 minsNegative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 335 2 1 3 2.7 COc1ccc(C#Cc2ccc(C(=O)N3CCCC(O)C3)cc2)cc1 10.1021/jm400439t
CHEMBL2204439 90377 0 None 2 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 minsNegative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 335 2 1 3 2.7 COc1ccc(C#Cc2ccc(C(=O)N3CCCC(O)C3)cc2)cc1 10.1021/jm400439t
10979251 96835 0 None -1 3 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization after 1.5 hrs by FLIPR assayAntagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization after 1.5 hrs by FLIPR assay
ChEMBL 293 4 3 4 1.3 N[C@@]1(C(=O)O)C[C@@H](Sc2ccccc2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
CHEMBL2381650 96835 0 None -1 3 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization after 1.5 hrs by FLIPR assayAntagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization after 1.5 hrs by FLIPR assay
ChEMBL 293 4 3 4 1.3 N[C@@]1(C(=O)O)C[C@@H](Sc2ccccc2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
86298614 118781 0 None 3 2 Rat 7.1 pIC50 = 7.1 Functional
Inhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentrationInhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentration
ChEMBL 353 2 0 6 3.3 Cn1c(=O)c2ccc(-c3cncnc3)cc2n2nc(-c3ccccc3)cc12 10.1016/j.bmcl.2014.04.051
CHEMBL3288676 118781 0 None 3 2 Rat 7.1 pIC50 = 7.1 Functional
Inhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentrationInhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentration
ChEMBL 353 2 0 6 3.3 Cn1c(=O)c2ccc(-c3cncnc3)cc2n2nc(-c3ccccc3)cc12 10.1016/j.bmcl.2014.04.051
44300389 20431 0 None 1 2 Rat 4.1 pIC50 = 4.1 Functional
Inhibitory concentration required for antagonistic activity at Metabotropic glutamate receptor 3Inhibitory concentration required for antagonistic activity at Metabotropic glutamate receptor 3
ChEMBL 342 4 3 4 0.9 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2ccccc2Br)C1 10.1016/s0960-894x(01)00329-8
CHEMBL1194613 20431 0 None 1 2 Rat 4.1 pIC50 = 4.1 Functional
Inhibitory concentration required for antagonistic activity at Metabotropic glutamate receptor 3Inhibitory concentration required for antagonistic activity at Metabotropic glutamate receptor 3
ChEMBL 342 4 3 4 0.9 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2ccccc2Br)C1 10.1016/s0960-894x(01)00329-8
CHEMBL552984 20431 0 None 1 2 Rat 4.1 pIC50 = 4.1 Functional
Inhibitory concentration required for antagonistic activity at Metabotropic glutamate receptor 3Inhibitory concentration required for antagonistic activity at Metabotropic glutamate receptor 3
ChEMBL 342 4 3 4 0.9 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2ccccc2Br)C1 10.1016/s0960-894x(01)00329-8
122190313 130220 0 None -10 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 369 4 0 4 4.0 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3cccc(F)c3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617497 130220 0 None -10 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 369 4 0 4 4.0 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3cccc(F)c3)nn21 10.1021/acs.jmedchem.5b01005
122190313 130220 0 None -10 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 369 4 0 4 4.0 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3cccc(F)c3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617497 130220 0 None -10 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 369 4 0 4 4.0 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3cccc(F)c3)nn21 10.1021/acs.jmedchem.5b01005
122190327 130234 0 None 2 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 376 4 0 5 3.7 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ccc(C#N)cc3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617511 130234 0 None 2 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 376 4 0 5 3.7 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ccc(C#N)cc3)nn21 10.1021/acs.jmedchem.5b01005
86298614 118781 0 None 3 2 Rat 7.1 pIC50 = 7.1 Functional
Inhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentrationInhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentration
ChEMBL 353 2 0 6 3.3 Cn1c(=O)c2ccc(-c3cncnc3)cc2n2nc(-c3ccccc3)cc12 10.1016/j.bmcl.2014.04.051
CHEMBL3288676 118781 0 None 3 2 Rat 7.1 pIC50 = 7.1 Functional
Inhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentrationInhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentration
ChEMBL 353 2 0 6 3.3 Cn1c(=O)c2ccc(-c3cncnc3)cc2n2nc(-c3ccccc3)cc12 10.1016/j.bmcl.2014.04.051
122190327 130234 0 None 2 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 376 4 0 5 3.7 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ccc(C#N)cc3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617511 130234 0 None 2 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 376 4 0 5 3.7 C[C@@H]1CN(c2ccc(F)cc2)C(=O)c2cc(COc3ccc(C#N)cc3)nn21 10.1021/acs.jmedchem.5b01005
10492773 23557 0 None 2 2 Human 7.1 pIC50 = 7.1 Functional
Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3
ChEMBL 277 6 3 3 1.4 Cc1cccc(CC[C@](N)(C(=O)O)[C@H]2C[C@@H]2C(=O)O)c1 10.1021/jm970498o
CHEMBL124501 23557 0 None 2 2 Human 7.1 pIC50 = 7.1 Functional
Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3
ChEMBL 277 6 3 3 1.4 Cc1cccc(CC[C@](N)(C(=O)O)[C@H]2C[C@@H]2C(=O)O)c1 10.1021/jm970498o
10828532 85540 0 None 22 2 Human 7.1 pIC50 = 7.1 Functional
Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3
ChEMBL 307 7 4 4 0.8 NC(CCc1cccc(C(=O)O)c1)(C(=O)O)[C@H]1C[C@@H]1C(=O)O 10.1021/jm970498o
CHEMBL2112634 85540 0 None 22 2 Human 7.1 pIC50 = 7.1 Functional
Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3
ChEMBL 307 7 4 4 0.8 NC(CCc1cccc(C(=O)O)c1)(C(=O)O)[C@H]1C[C@@H]1C(=O)O 10.1021/jm970498o
122190419 130306 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 393 4 0 6 3.6 C[C@@H]1CN(c2cccc(C#N)c2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617642 130306 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 393 4 0 6 3.6 C[C@@H]1CN(c2cccc(C#N)c2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
134139744 152737 0 None 1 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assayAntagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 375 5 4 5 1.0 N[C@@]1(C(=O)O)[C@H](OCc2cccc(Cl)c2Cl)[C@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1016/j.bmcl.2016.10.067
CHEMBL3918170 152737 0 None 1 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assayAntagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 375 5 4 5 1.0 N[C@@]1(C(=O)O)[C@H](OCc2cccc(Cl)c2Cl)[C@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1016/j.bmcl.2016.10.067
122190326 130233 0 None 3 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 379 5 0 4 4.4 CCc1ccc(OCc2cc3n(n2)[C@H](C)CN(c2ccc(F)cc2)C3=O)cc1 10.1021/acs.jmedchem.5b01005
CHEMBL3617510 130233 0 None 3 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 379 5 0 4 4.4 CCc1ccc(OCc2cc3n(n2)[C@H](C)CN(c2ccc(F)cc2)C3=O)cc1 10.1021/acs.jmedchem.5b01005
122190326 130233 0 None 3 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 379 5 0 4 4.4 CCc1ccc(OCc2cc3n(n2)[C@H](C)CN(c2ccc(F)cc2)C3=O)cc1 10.1021/acs.jmedchem.5b01005
CHEMBL3617510 130233 0 None 3 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 379 5 0 4 4.4 CCc1ccc(OCc2cc3n(n2)[C@H](C)CN(c2ccc(F)cc2)C3=O)cc1 10.1021/acs.jmedchem.5b01005
122190419 130306 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 393 4 0 6 3.6 C[C@@H]1CN(c2cccc(C#N)c2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617642 130306 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 393 4 0 6 3.6 C[C@@H]1CN(c2cccc(C#N)c2)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
134141510 153846 0 None 2 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assayAntagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 339 5 4 5 0.1 Cc1cc(CO[C@@H]2[C@H](O)[C@@H]3[C@@H]([C@H]3C(=O)O)[C@]2(N)C(=O)O)ccc1F 10.1016/j.bmcl.2016.10.067
CHEMBL3927108 153846 0 None 2 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assayAntagonist activity at recombinant human mGlu3 receptor expressed in hamster AV12 cells co-expressing human EAAT1 assessed as reduction of DCG-4-inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 339 5 4 5 0.1 Cc1cc(CO[C@@H]2[C@H](O)[C@@H]3[C@@H]([C@H]3C(=O)O)[C@]2(N)C(=O)O)ccc1F 10.1016/j.bmcl.2016.10.067
122190421 130308 0 None 7 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 404 4 0 5 4.0 C[C@@H]1CN(c2cccc(F)c2F)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617644 130308 0 None 7 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 404 4 0 5 4.0 C[C@@H]1CN(c2cccc(F)c2F)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
122190421 130308 0 None 7 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 404 4 0 5 4.0 C[C@@H]1CN(c2cccc(F)c2F)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617644 130308 0 None 7 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 404 4 0 5 4.0 C[C@@H]1CN(c2cccc(F)c2F)C(=O)c2cc(COc3ccc(Cl)cn3)nn21 10.1021/acs.jmedchem.5b01005
10358265 108903 0 None 2 2 Human 5.1 pIC50 = 5.1 Functional
In vitro antagonist activity at recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.In vitro antagonist activity at recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.
ChEMBL 314 4 3 4 1.3 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2cccc3ccccc23)C1 10.1016/s0960-894x(98)00352-7
CHEMBL302411 108903 0 None 2 2 Human 5.1 pIC50 = 5.1 Functional
In vitro antagonist activity at recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.In vitro antagonist activity at recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.
ChEMBL 314 4 3 4 1.3 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2cccc3ccccc23)C1 10.1016/s0960-894x(98)00352-7
71136655 130179 0 None -12 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as reversal of DCG-4-inhibited, forskolin-stimulated cAMP production after 1 hr by fluorescence assayAntagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as reversal of DCG-4-inhibited, forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 326 5 4 6 0.5 CC(C)c1nnc(S[C@@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)[nH]1 10.1021/acs.jmedchem.5b01124
CHEMBL3616852 130179 0 None -12 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as reversal of DCG-4-inhibited, forskolin-stimulated cAMP production after 1 hr by fluorescence assayAntagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as reversal of DCG-4-inhibited, forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 326 5 4 6 0.5 CC(C)c1nnc(S[C@@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)[nH]1 10.1021/acs.jmedchem.5b01124
122190405 130292 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 353 4 0 6 2.6 C[C@@H]1CN(c2ccncc2)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617628 130292 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 353 4 0 6 2.6 C[C@@H]1CN(c2ccncc2)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
90643954 118767 0 None 2 2 Rat 6.1 pIC50 = 6.1 Functional
Inhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentrationInhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentration
ChEMBL 430 3 1 6 3.2 Cn1c(=O)c2ccc(-c3cccc(S(N)(=O)=O)c3)cc2n2nc(-c3ccccc3)cc12 10.1016/j.bmcl.2014.04.051
CHEMBL3288636 118767 0 None 2 2 Rat 6.1 pIC50 = 6.1 Functional
Inhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentrationInhibition of rat mGlu3 receptor transfected in HEK293 cells coexpressing mouse Galpha15 assessed as decrease in glutamate-induced calcium signaling by fluorescence plate reader analysis in presence of glutamate at EC87 concentration
ChEMBL 430 3 1 6 3.2 Cn1c(=O)c2ccc(-c3cccc(S(N)(=O)=O)c3)cc2n2nc(-c3ccccc3)cc12 10.1016/j.bmcl.2014.04.051
122190405 130292 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 353 4 0 6 2.6 C[C@@H]1CN(c2ccncc2)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617628 130292 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 353 4 0 6 2.6 C[C@@H]1CN(c2ccncc2)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
10979251 96835 0 None -1 3 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by HTRF assayAntagonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by HTRF assay
ChEMBL 293 4 3 4 1.3 N[C@@]1(C(=O)O)C[C@@H](Sc2ccccc2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm4000165
CHEMBL2381650 96835 0 None -1 3 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by HTRF assayAntagonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by HTRF assay
ChEMBL 293 4 3 4 1.3 N[C@@]1(C(=O)O)C[C@@H](Sc2ccccc2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm4000165
122190403 130290 0 None 3 2 Rat 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 353 4 0 6 2.6 C[C@@H]1CN(c2ccccn2)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617626 130290 0 None 3 2 Rat 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 353 4 0 6 2.6 C[C@@H]1CN(c2ccccn2)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
122190403 130290 0 None 3 2 Rat 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 353 4 0 6 2.6 C[C@@H]1CN(c2ccccn2)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
CHEMBL3617626 130290 0 None 3 2 Rat 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor assessed as calcium mobilization by cell based fluorescence assay
ChEMBL 353 4 0 6 2.6 C[C@@H]1CN(c2ccccn2)C(=O)c2cc(COc3ccc(F)cn3)nn21 10.1021/acs.jmedchem.5b01005
122456062 169228 0 None -1 2 Rat 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assay
ChEMBL 325 6 0 4 3.4 O=c1cc(OCCOc2ccccc2)ccn1-c1ccc(F)cc1 10.1021/acsmedchemlett.7b00249
CHEMBL4166631 169228 0 None -1 2 Rat 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assay
ChEMBL 325 6 0 4 3.4 O=c1cc(OCCOc2ccccc2)ccn1-c1ccc(F)cc1 10.1021/acsmedchemlett.7b00249
10385210 19804 0 None -2 3 Rat 4.0 pIC50 = 4.0 Functional
Inhibitory concentration required for antagonistic activity at Metabotropic glutamate receptor 3Inhibitory concentration required for antagonistic activity at Metabotropic glutamate receptor 3
ChEMBL 309 5 3 6 0.0 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2cccc([N+](=O)[O-])c2)C1 10.1016/s0960-894x(01)00329-8
CHEMBL1189910 19804 0 None -2 3 Rat 4.0 pIC50 = 4.0 Functional
Inhibitory concentration required for antagonistic activity at Metabotropic glutamate receptor 3Inhibitory concentration required for antagonistic activity at Metabotropic glutamate receptor 3
ChEMBL 309 5 3 6 0.0 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2cccc([N+](=O)[O-])c2)C1 10.1016/s0960-894x(01)00329-8
CHEMBL539760 19804 0 None -2 3 Rat 4.0 pIC50 = 4.0 Functional
Inhibitory concentration required for antagonistic activity at Metabotropic glutamate receptor 3Inhibitory concentration required for antagonistic activity at Metabotropic glutamate receptor 3
ChEMBL 309 5 3 6 0.0 N[C@]1(C(=O)O)C[C@H](C(=O)O)N(Cc2cccc([N+](=O)[O-])c2)C1 10.1016/s0960-894x(01)00329-8
122456062 169228 0 None -1 2 Rat 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assay
ChEMBL 325 6 0 4 3.4 O=c1cc(OCCOc2ccccc2)ccn1-c1ccc(F)cc1 10.1021/acsmedchemlett.7b00249
CHEMBL4166631 169228 0 None -1 2 Rat 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu3 receptor expressed in TREX cells coexpressing Galpha15 assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured for 2.6 mins by Fluo-4 AM dye based fluorescence assay
ChEMBL 325 6 0 4 3.4 O=c1cc(OCCOc2ccccc2)ccn1-c1ccc(F)cc1 10.1021/acsmedchemlett.7b00249
71137012 130178 0 None -11 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization after 1.5 hrs by FLIPR assayAntagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization after 1.5 hrs by FLIPR assay
ChEMBL 299 4 5 7 -1.0 Nc1nnc(S[C@@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)[nH]1 10.1021/acs.jmedchem.5b01124
CHEMBL3616851 130178 0 None -11 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization after 1.5 hrs by FLIPR assayAntagonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of glutamate-stimulated Ca2+ mobilization after 1.5 hrs by FLIPR assay
ChEMBL 299 4 5 7 -1.0 Nc1nnc(S[C@@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)[nH]1 10.1021/acs.jmedchem.5b01124
162654849 190449 0 None 1 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 341 5 4 5 0.6 N[C@@]1(C(=O)O)[C@H](CSc2ccccc2F)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
CHEMBL4755204 190449 0 None 1 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 341 5 4 5 0.6 N[C@@]1(C(=O)O)[C@H](CSc2ccccc2F)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
CHEMBL4802906 190449 0 None 1 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assayAntagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
ChEMBL 341 5 4 5 0.6 N[C@@]1(C(=O)O)[C@H](CSc2ccccc2F)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
11298568 76150 1 None -5 2 Human 5.0 pIC50 = 5.0 Functional
Evaluation of the functional effect on cAMP responses in RGT cells expressing human mGlu3 receptorEvaluation of the functional effect on cAMP responses in RGT cells expressing human mGlu3 receptor
ChEMBL 199 2 3 3 -0.2 C[C@@H]1C[C@H]2[C@H](C(=O)O)[C@H]2[C@]1(N)C(=O)O 10.1021/jm040222y
CHEMBL192977 76150 1 None -5 2 Human 5.0 pIC50 = 5.0 Functional
Evaluation of the functional effect on cAMP responses in RGT cells expressing human mGlu3 receptorEvaluation of the functional effect on cAMP responses in RGT cells expressing human mGlu3 receptor
ChEMBL 199 2 3 3 -0.2 C[C@@H]1C[C@H]2[C@H](C(=O)O)[C@H]2[C@]1(N)C(=O)O 10.1021/jm040222y
137635882 162673 0 None -1 2 Human 5.0 pIC50 = 5 Functional
Antagonist activity at human mGlu3 receptor expressed in HEK cells assessed as reversal of DCG-4 inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assayAntagonist activity at human mGlu3 receptor expressed in HEK cells assessed as reversal of DCG-4 inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 310 4 4 4 0.2 N[C@@]1(C(=O)O)C[C@H](NC(=O)C2CCCCC2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
CHEMBL4060567 162673 0 None -1 2 Human 5.0 pIC50 = 5 Functional
Antagonist activity at human mGlu3 receptor expressed in HEK cells assessed as reversal of DCG-4 inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assayAntagonist activity at human mGlu3 receptor expressed in HEK cells assessed as reversal of DCG-4 inhibited forskolin-stimulated cAMP formation after 20 mins by HTRF assay
ChEMBL 310 4 4 4 0.2 N[C@@]1(C(=O)O)C[C@H](NC(=O)C2CCCCC2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
44322840 119348 0 None - 0 Human 7.0 pKi = 7 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL 201 2 4 4 -1.5 N[C@]1(C(=O)O)C2C(C[C@H]1O)[C@@H]2C(=O)O 10.1021/jm000007r
CHEMBL330097 119348 0 None - 0 Human 7.0 pKi = 7 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL 201 2 4 4 -1.5 N[C@]1(C(=O)O)C2C(C[C@H]1O)[C@@H]2C(=O)O 10.1021/jm000007r
1378 9195 54 None 2 14 Human 7.9 pKi = 7.9 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/jm000007r
1399 9195 54 None 2 14 Human 7.9 pKi = 7.9 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/jm000007r
9819927 9195 54 None 2 14 Human 7.9 pKi = 7.9 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/jm000007r
CHEMBL432038 9195 54 None 2 14 Human 7.9 pKi = 7.9 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/jm000007r
44322529 213645 1 None - 0 Human 6.7 pKi = 6.7 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL 367 6 3 4 3.1 N[C@H](C(=O)O)[C@@H]1[C@@H](C(=O)O)[C@@H]1CCC1c2ccccc2Oc2ccccc21 10.1021/jm000007r
CHEMBL90675 213645 1 None - 0 Human 6.7 pKi = 6.7 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL 367 6 3 4 3.1 N[C@H](C(=O)O)[C@@H]1[C@@H](C(=O)O)[C@@H]1CCC1c2ccccc2Oc2ccccc21 10.1021/jm000007r
44322921 213616 1 None - 0 Human 5.7 pKi = 5.7 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL 185 2 3 3 -0.5 N[C@@]1(C(=O)O)CC2CC1[C@H]2C(=O)O 10.1021/jm000007r
CHEMBL90501 213616 1 None - 0 Human 5.7 pKi = 5.7 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL 185 2 3 3 -0.5 N[C@@]1(C(=O)O)CC2CC1[C@H]2C(=O)O 10.1021/jm000007r
6324634 154722 11 None -6 2 Human 4.5 pKi = 4.5 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL 355 10 3 3 3.5 N[C@@H](C[C@H](CCCC(c1ccccc1)c1ccccc1)C(=O)O)C(=O)O 10.1021/jm000007r
CHEMBL39338 154722 11 None -6 2 Human 4.5 pKi = 4.5 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL 355 10 3 3 3.5 N[C@@H](C[C@H](CCCC(c1ccccc1)c1ccccc1)C(=O)O)C(=O)O 10.1021/jm000007r
1393 8321 64 None -4 6 Human 7.4 pKi = 7.4 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm000007r
1396 8321 64 None -4 6 Human 7.4 pKi = 7.4 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm000007r
213056 8321 64 None -4 6 Human 7.4 pKi = 7.4 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm000007r
CHEMBL8759 8321 64 None -4 6 Human 7.4 pKi = 7.4 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm000007r
10197984 9199 44 None -1 5 Human 8.3 pKi = 8.3 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10.1021/jm000007r
1394 9199 44 None -1 5 Human 8.3 pKi = 8.3 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10.1021/jm000007r
CHEMBL275079 9199 44 None -1 5 Human 8.3 pKi = 8.3 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10.1021/jm000007r
1370 10037 67 None - 6 Human 4.4 pKi = 4.4 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm000007r
1372 10037 67 None - 6 Human 4.4 pKi = 4.4 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm000007r
40539 10037 67 None - 6 Human 4.4 pKi = 4.4 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm000007r
6971145 10037 67 None - 6 Human 4.4 pKi = 4.4 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm000007r
CHEMBL279956 10037 67 None - 6 Human 4.4 pKi = 4.4 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm000007r
DB02999 10037 67 None - 6 Human 4.4 pKi = 4.4 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm000007r
1392 6861 48 None -9 4 Human 6.4 pKi = 6.4 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL 174 2 4 4 -1.8 OC(=O)[C@@H]1NC[C@@](C1)(N)C(=O)O 10.1021/jm000007r
5310984 6861 48 None -9 4 Human 6.4 pKi = 6.4 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL 174 2 4 4 -1.8 OC(=O)[C@@H]1NC[C@@](C1)(N)C(=O)O 10.1021/jm000007r
CHEMBL40086 6861 48 None -9 4 Human 6.4 pKi = 6.4 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL 174 2 4 4 -1.8 OC(=O)[C@@H]1NC[C@@](C1)(N)C(=O)O 10.1021/jm000007r
1368 9070 37 None - 11 Human 6.4 pKi = 6.4 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 10.1021/jm000007r
5310956 9070 37 None - 11 Human 6.4 pKi = 6.4 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 10.1021/jm000007r
CHEMBL280563 9070 37 None - 11 Human 6.4 pKi = 6.4 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 10.1021/jm000007r
10330132 108159 1 None -10 2 Human 4.3 pKi = 4.3 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL 189 2 4 5 -2.2 NN1C[C@@](N)(C(=O)O)C[C@@H]1C(=O)O 10.1021/jm000007r
CHEMBL297150 108159 1 None -10 2 Human 4.3 pKi = 4.3 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL 189 2 4 5 -2.2 NN1C[C@@](N)(C(=O)O)C[C@@H]1C(=O)O 10.1021/jm000007r
10359073 161753 1 None 1 2 Human 5.2 pKi = 5.2 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL 327 8 3 3 2.7 N[C@@H](C[C@H](CC(c1ccccc1)c1ccccc1)C(=O)O)C(=O)O 10.1021/jm000007r
CHEMBL40123 161753 1 None 1 2 Human 5.2 pKi = 5.2 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL 327 8 3 3 2.7 N[C@@H](C[C@H](CC(c1ccccc1)c1ccccc1)C(=O)O)C(=O)O 10.1021/jm000007r
10058694 213382 1 None - 0 Human 8.1 pKi = 8.1 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL 203 2 3 4 -0.8 N[C@@]1(C(=O)O)CSC2C1[C@H]2C(=O)O 10.1021/jm000007r
CHEMBL88999 213382 1 None - 0 Human 8.1 pKi = 8.1 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL 203 2 3 4 -0.8 N[C@@]1(C(=O)O)CSC2C1[C@H]2C(=O)O 10.1021/jm000007r
1310 9095 110 None -251 17 Human 5.1 pKi = 5.1 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm000007r
1369 9095 110 None -251 17 Human 5.1 pKi = 5.1 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm000007r
33032 9095 110 None -251 17 Human 5.1 pKi = 5.1 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm000007r
44272391 9095 110 None -251 17 Human 5.1 pKi = 5.1 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm000007r
88747398 9095 110 None -251 17 Human 5.1 pKi = 5.1 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm000007r
CHEMBL575060 9095 110 None -251 17 Human 5.1 pKi = 5.1 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm000007r
DB00142 9095 110 None -251 17 Human 5.1 pKi = 5.1 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm000007r
1310 9095 110 None -29 17 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
1369 9095 110 None -29 17 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
33032 9095 110 None -29 17 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
44272391 9095 110 None -29 17 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
88747398 9095 110 None -29 17 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
CHEMBL575060 9095 110 None -29 17 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
DB00142 9095 110 None -29 17 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
49836087 7847 0 None -16 2 Human 4.9 pEC50 = 4.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 328 2 2 4 3.3 O/N=C\1/c2ccccc2OC2(C1C2)C(=O)Nc1ccc(cc1)Cl 21105727
6222 7847 0 None -16 2 Human 4.9 pEC50 = 4.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 328 2 2 4 3.3 O/N=C\1/c2ccccc2OC2(C1C2)C(=O)Nc1ccc(cc1)Cl 21105727
CHEMBL1630805 7847 0 None -16 2 Human 4.9 pEC50 = 4.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 328 2 2 4 3.3 O/N=C\1/c2ccccc2OC2(C1C2)C(=O)Nc1ccc(cc1)Cl 21105727
49858118 7894 0 None -10 2 Human 5.0 pEC50 = 5.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 324 3 2 5 2.7 O/N=C\1/c2ccccc2OC2(C1C2)C(=O)Nc1ccc(cc1)OC 21105727
6224 7894 0 None -10 2 Human 5.0 pEC50 = 5.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 324 3 2 5 2.7 O/N=C\1/c2ccccc2OC2(C1C2)C(=O)Nc1ccc(cc1)OC 21105727
CHEMBL1630807 7894 0 None -10 2 Human 5.0 pEC50 = 5.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 324 3 2 5 2.7 O/N=C\1/c2ccccc2OC2(C1C2)C(=O)Nc1ccc(cc1)OC 21105727
49858117 7875 4 None -5 2 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 308 2 2 4 3.0 O/N=C\1/c2ccccc2OC2(C1C2)C(=O)Nc1ccc(cc1)C 21105727
6223 7875 4 None -5 2 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 308 2 2 4 3.0 O/N=C\1/c2ccccc2OC2(C1C2)C(=O)Nc1ccc(cc1)C 21105727
CHEMBL1630806 7875 4 None -5 2 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 308 2 2 4 3.0 O/N=C\1/c2ccccc2OC2(C1C2)C(=O)Nc1ccc(cc1)C 21105727
1310 9095 110 None -251 17 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
1369 9095 110 None -251 17 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
33032 9095 110 None -251 17 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
44272391 9095 110 None -251 17 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
88747398 9095 110 None -251 17 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
CHEMBL575060 9095 110 None -251 17 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
DB00142 9095 110 None -251 17 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
6219 9363 0 None -1 3 Rat 7.5 pEC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 401 1 1 3 4.0 N#Cc1cccc(c1)C1=Nc2ccc(cc2NC(=O)CC1)I 17416742
73755191 9363 0 None -1 3 Rat 7.5 pEC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 401 1 1 3 4.0 N#Cc1cccc(c1)C1=Nc2ccc(cc2NC(=O)CC1)I 17416742
11158623 10124 11 None -1 4 Rat 8.0 pIC50 < 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 423 2 1 3 6.2 O=C1CC(=Nc2c(N1)cc(c(c2)C)C(F)(F)F)c1cccc(c1)c1cc(C)nc(c1)C 20971004
6226 10124 11 None -1 4 Rat 8.0 pIC50 < 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 423 2 1 3 6.2 O=C1CC(=Nc2c(N1)cc(c(c2)C)C(F)(F)F)c1cccc(c1)c1cc(C)nc(c1)C 20971004
CHEMBL1629855 10124 11 None -1 4 Rat 8.0 pIC50 < 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 423 2 1 3 6.2 O=C1CC(=Nc2c(N1)cc(c(c2)C)C(F)(F)F)c1cccc(c1)c1cc(C)nc(c1)C 20971004
11503055 9179 3 None 31 2 Human 6.7 pIC50 = 6.7 Functional
Assessed in AV-12 cells expressing the human mGlu3, activated by glutamate as agonist.Assessed in AV-12 cells expressing the human mGlu3, activated by glutamate as agonist.
Guide to Pharmacology 400 4 1 4 3.9 Clc1ccc(c(c1)Cl)CN[C@H]1CCN(C1)c1ncc(cn1)Br 22607673
9694 9179 3 None 31 2 Human 6.7 pIC50 = 6.7 Functional
Assessed in AV-12 cells expressing the human mGlu3, activated by glutamate as agonist.Assessed in AV-12 cells expressing the human mGlu3, activated by glutamate as agonist.
Guide to Pharmacology 400 4 1 4 3.9 Clc1ccc(c(c1)Cl)CN[C@H]1CCN(C1)c1ncc(cn1)Br 22607673
CHEMBL2204436 9179 3 None 31 2 Human 6.7 pIC50 = 6.7 Functional
Assessed in AV-12 cells expressing the human mGlu3, activated by glutamate as agonist.Assessed in AV-12 cells expressing the human mGlu3, activated by glutamate as agonist.
Guide to Pharmacology 400 4 1 4 3.9 Clc1ccc(c(c1)Cl)CN[C@H]1CCN(C1)c1ncc(cn1)Br 22607673
56587994 10817 41 None 1 2 Rat 6.0 pIC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 349 3 1 3 2.9 OC[C@@H]1CCCN(C1)C(=O)c1ccc(cc1)C#Cc1ccc(cc1)OC 22607673
6225 10817 41 None 1 2 Rat 6.0 pIC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 349 3 1 3 2.9 OC[C@@H]1CCCN(C1)C(=O)c1ccc(cc1)C#Cc1ccc(cc1)OC 22607673
CHEMBL2204445 10817 41 None 1 2 Rat 6.0 pIC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 349 3 1 3 2.9 OC[C@@H]1CCCN(C1)C(=O)c1ccc(cc1)C#Cc1ccc(cc1)OC 22607673
60204017 9351 30 None - 1 Rat 6.2 pIC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 353 2 1 3 2.8 COc1ccc(cc1)C#Cc1ccc(c(c1)F)C(=O)N1CCC[C@H](C1)O 23718281
8765 9351 30 None - 1 Rat 6.2 pIC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 353 2 1 3 2.8 COc1ccc(cc1)C#Cc1ccc(c(c1)F)C(=O)N1CCC[C@H](C1)O 23718281
CHEMBL2385886 9351 30 None - 1 Rat 6.2 pIC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 353 2 1 3 2.8 COc1ccc(cc1)C#Cc1ccc(c(c1)F)C(=O)N1CCC[C@H](C1)O 23718281
10237 10823 20 None -1 2 Human 6.4 pIC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 387 4 0 6 3.3 Clc1ccc(nc1)OCc1nn2c(c1)C(=O)N(C[C@H]2C)c1cccnc1F 26335039
122190433 10823 20 None -1 2 Human 6.4 pIC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 387 4 0 6 3.3 Clc1ccc(nc1)OCc1nn2c(c1)C(=O)N(C[C@H]2C)c1cccnc1F 26335039
CHEMBL3617655 10823 20 None -1 2 Human 6.4 pIC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 387 4 0 6 3.3 Clc1ccc(nc1)OCc1nn2c(c1)C(=O)N(C[C@H]2C)c1cccnc1F 26335039
11158623 10124 11 None -50 4 Human 6.6 pIC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 423 2 1 3 6.2 O=C1CC(=Nc2c(N1)cc(c(c2)C)C(F)(F)F)c1cccc(c1)c1cc(C)nc(c1)C 22091727
6226 10124 11 None -50 4 Human 6.6 pIC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 423 2 1 3 6.2 O=C1CC(=Nc2c(N1)cc(c(c2)C)C(F)(F)F)c1cccc(c1)c1cc(C)nc(c1)C 22091727
CHEMBL1629855 10124 11 None -50 4 Human 6.6 pIC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 423 2 1 3 6.2 O=C1CC(=Nc2c(N1)cc(c(c2)C)C(F)(F)F)c1cccc(c1)c1cc(C)nc(c1)C 22091727
6220 9364 0 None -1 3 Rat 7.7 pIC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 405 2 1 3 5.4 O=C1CCC(=Nc2c(N1)ccc(c2)Br)c1cccc(c1)c1ccncc1 17416742
73755192 9364 0 None -1 3 Rat 7.7 pIC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 405 2 1 3 5.4 O=C1CCC(=Nc2c(N1)ccc(c2)Br)c1cccc(c1)c1ccncc1 17416742
6221 9365 0 None -1 3 Rat 7.7 pIC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 354 1 1 4 3.6 N#Cc1nccc(c1)C1=Nc2ccc(cc2NC(=O)CC1)Br 17416742
73755193 9365 0 None -1 3 Rat 7.7 pIC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 354 1 1 4 3.6 N#Cc1nccc(c1)C1=Nc2ccc(cc2NC(=O)CC1)Br 17416742




Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Affinity)
# tested GPCRs
(Affinity)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
9794208 96825 4 None - 0 Human 10.0 pEC50 = 10.0 Binding
Agonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assay
ChEMBL 199 2 3 4 -1.3 N[C@@]1(C(=O)O)CC(=O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/jm4000165
CHEMBL2381640 96825 4 None - 0 Human 10.0 pEC50 = 10.0 Binding
Agonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assay
ChEMBL 199 2 3 4 -1.3 N[C@@]1(C(=O)O)CC(=O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/jm4000165
139119037 96837 2 None - 0 Human 9.6 pEC50 = 9.6 Binding
Agonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assay
ChEMBL 203 2 3 3 -0.5 N[C@@]1(C(=O)O)C[C@@H](F)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm4000165
15479143 96837 2 None - 0 Human 9.6 pEC50 = 9.6 Binding
Agonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assay
ChEMBL 203 2 3 3 -0.5 N[C@@]1(C(=O)O)C[C@@H](F)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm4000165
CHEMBL2381652 96837 2 None - 0 Human 9.6 pEC50 = 9.6 Binding
Agonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assay
ChEMBL 203 2 3 3 -0.5 N[C@@]1(C(=O)O)C[C@@H](F)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm4000165
6603885 108978 23 None - 0 Rat 5.0 pEC50 = 5 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR3 in ratConcentration for half maximal activation of metabotropic glutamate mGluR3 in rat
ChEMBL 158 2 3 5 -0.5 N[C@H](C(=O)O)c1cc(O)no1 10.1021/jm00009a001
6971208 108978 23 None - 0 Rat 5.0 pEC50 = 5 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR3 in ratConcentration for half maximal activation of metabotropic glutamate mGluR3 in rat
ChEMBL 158 2 3 5 -0.5 N[C@H](C(=O)O)c1cc(O)no1 10.1021/jm00009a001
CHEMBL30285 108978 23 None - 0 Rat 5.0 pEC50 = 5 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR3 in ratConcentration for half maximal activation of metabotropic glutamate mGluR3 in rat
ChEMBL 158 2 3 5 -0.5 N[C@H](C(=O)O)c1cc(O)no1 10.1021/jm00009a001
90643879 118650 0 None - 0 Rat 6.0 pEC50 = 6.0 Binding
Positive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assayPositive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assay
ChEMBL 456 12 2 6 5.4 COc1ccc(C(=O)O)cc1OCCCCOc1ccc(C(=O)CC2CCCC2)c(O)c1C 10.1021/jm5000563
CHEMBL3287702 118650 0 None - 0 Rat 6.0 pEC50 = 6.0 Binding
Positive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assayPositive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assay
ChEMBL 456 12 2 6 5.4 COc1ccc(C(=O)O)cc1OCCCCOc1ccc(C(=O)CC2CCCC2)c(O)c1C 10.1021/jm5000563
164609979 191354 0 None - 0 Rat 6.0 pEC50 = 6.0 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 444 10 2 6 5.1 COc1ccc(C(=O)O)cc1OC[C@@H](C)COc1ccc(C(=O)CC(C)(C)C)c(O)c1C 10.1016/j.bmcl.2021.128342
CHEMBL4848547 191354 0 None - 0 Rat 6.0 pEC50 = 6.0 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 444 10 2 6 5.1 COc1ccc(C(=O)O)cc1OC[C@@H](C)COc1ccc(C(=O)CC(C)(C)C)c(O)c1C 10.1016/j.bmcl.2021.128342
164619502 192979 0 None - 0 Rat 6.0 pEC50 = 6.0 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 432 9 2 5 5.3 Cc1c(OC[C@@H](C)COc2ccc(C(=O)O)c(F)c2)ccc(C(=O)CC(C)(C)C)c1O 10.1016/j.bmcl.2021.128342
CHEMBL4872955 192979 0 None - 0 Rat 6.0 pEC50 = 6.0 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 432 9 2 5 5.3 Cc1c(OC[C@@H](C)COc2ccc(C(=O)O)c(F)c2)ccc(C(=O)CC(C)(C)C)c1O 10.1016/j.bmcl.2021.128342
164621278 192311 0 None - 0 Rat 6.0 pEC50 = 6.0 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 418 8 2 5 5.0 Cc1c(OC[C@H](C)Oc2ccc(F)c(C(=O)O)c2)ccc(C(=O)CC(C)(C)C)c1O 10.1016/j.bmcl.2021.128342
CHEMBL4862801 192311 0 None - 0 Rat 6.0 pEC50 = 6.0 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 418 8 2 5 5.0 Cc1c(OC[C@H](C)Oc2ccc(F)c(C(=O)O)c2)ccc(C(=O)CC(C)(C)C)c1O 10.1016/j.bmcl.2021.128342
164620998 192652 0 None - 0 Rat 6.0 pEC50 = 6.0 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 432 10 2 5 5.4 Cc1c(OCCCCOc2ccc(C(=O)O)c(F)c2)ccc(C(=O)CC(C)(C)C)c1O 10.1016/j.bmcl.2021.128342
CHEMBL4868114 192652 0 None - 0 Rat 6.0 pEC50 = 6.0 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 432 10 2 5 5.4 Cc1c(OCCCCOc2ccc(C(=O)O)c(F)c2)ccc(C(=O)CC(C)(C)C)c1O 10.1016/j.bmcl.2021.128342
164619969 192308 0 None - 0 Rat 6.0 pEC50 = 6.0 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 418 8 2 5 5.0 Cc1c(O[C@@H](C)COc2ccc(F)c(C(=O)O)c2)ccc(C(=O)CC(C)(C)C)c1O 10.1016/j.bmcl.2021.128342
CHEMBL4862778 192308 0 None - 0 Rat 6.0 pEC50 = 6.0 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 418 8 2 5 5.0 Cc1c(O[C@@H](C)COc2ccc(F)c(C(=O)O)c2)ccc(C(=O)CC(C)(C)C)c1O 10.1016/j.bmcl.2021.128342
90643874 118645 0 None - 0 Rat 5.9 pEC50 = 5.9 Binding
Positive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assayPositive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assay
ChEMBL 434 11 2 5 5.5 Cc1c(OCCCCOc2ccc(C(=O)O)cc2Cl)ccc(C(=O)CC(C)C)c1O 10.1021/jm5000563
CHEMBL3287697 118645 0 None - 0 Rat 5.9 pEC50 = 5.9 Binding
Positive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assayPositive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assay
ChEMBL 434 11 2 5 5.5 Cc1c(OCCCCOc2ccc(C(=O)O)cc2Cl)ccc(C(=O)CC(C)C)c1O 10.1021/jm5000563
164610619 191533 0 None - 0 Rat 5.9 pEC50 = 5.9 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 432 9 2 5 5.3 Cc1c(OC[C@@H](C)COc2ccc(F)c(C(=O)O)c2)ccc(C(=O)CC(C)(C)C)c1O 10.1016/j.bmcl.2021.128342
CHEMBL4850952 191533 0 None - 0 Rat 5.9 pEC50 = 5.9 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 432 9 2 5 5.3 Cc1c(OC[C@@H](C)COc2ccc(F)c(C(=O)O)c2)ccc(C(=O)CC(C)(C)C)c1O 10.1016/j.bmcl.2021.128342
71681823 96829 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assay
ChEMBL 226 3 3 4 -0.2 [N-]=[N+]=N[C@@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@@H]21 10.1021/jm4000165
CHEMBL2381644 96829 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assay
ChEMBL 226 3 3 4 -0.2 [N-]=[N+]=N[C@@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@@H]21 10.1021/jm4000165
164627219 193160 0 None - 0 Rat 5.9 pEC50 = 5.9 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 418 8 2 5 5.0 Cc1c(OC[C@@H](C)Oc2ccc(F)c(C(=O)O)c2)ccc(C(=O)CC(C)(C)C)c1O 10.1016/j.bmcl.2021.128342
CHEMBL4875653 193160 0 None - 0 Rat 5.9 pEC50 = 5.9 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 418 8 2 5 5.0 Cc1c(OC[C@@H](C)Oc2ccc(F)c(C(=O)O)c2)ccc(C(=O)CC(C)(C)C)c1O 10.1016/j.bmcl.2021.128342
164614107 191909 0 None - 0 Rat 5.9 pEC50 = 5.9 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 432 10 2 5 5.4 Cc1c(OCCCCOc2ccc(C(=O)O)cc2F)ccc(C(=O)CC(C)(C)C)c1O 10.1016/j.bmcl.2021.128342
CHEMBL4856556 191909 0 None - 0 Rat 5.9 pEC50 = 5.9 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 432 10 2 5 5.4 Cc1c(OCCCCOc2ccc(C(=O)O)cc2F)ccc(C(=O)CC(C)(C)C)c1O 10.1016/j.bmcl.2021.128342
164609025 191220 0 None - 0 Rat 6.9 pEC50 = 6.9 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 448 10 2 5 5.9 Cc1c(OCCCCOc2ccc(Cl)c(C(=O)O)c2)ccc(C(=O)CC(C)(C)C)c1O 10.1016/j.bmcl.2021.128342
CHEMBL4846460 191220 0 None - 0 Rat 6.9 pEC50 = 6.9 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 448 10 2 5 5.9 Cc1c(OCCCCOc2ccc(Cl)c(C(=O)O)c2)ccc(C(=O)CC(C)(C)C)c1O 10.1016/j.bmcl.2021.128342
164611059 191358 0 None - 0 Rat 5.9 pEC50 = 5.9 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 432 9 2 5 5.3 Cc1c(OC[C@@H](C)COc2ccc(C(=O)O)cc2F)ccc(C(=O)CC(C)(C)C)c1O 10.1016/j.bmcl.2021.128342
CHEMBL4848600 191358 0 None - 0 Rat 5.9 pEC50 = 5.9 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 432 9 2 5 5.3 Cc1c(OC[C@@H](C)COc2ccc(C(=O)O)cc2F)ccc(C(=O)CC(C)(C)C)c1O 10.1016/j.bmcl.2021.128342
164611874 191893 0 None - 0 Rat 5.9 pEC50 = 5.9 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 428 9 2 5 5.4 Cc1cc(OC[C@H](C)COc2ccc(C(=O)CC(C)(C)C)c(O)c2C)ccc1C(=O)O 10.1016/j.bmcl.2021.128342
CHEMBL4856242 191893 0 None - 0 Rat 5.9 pEC50 = 5.9 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 428 9 2 5 5.4 Cc1cc(OC[C@H](C)COc2ccc(C(=O)CC(C)(C)C)c(O)c2C)ccc1C(=O)O 10.1016/j.bmcl.2021.128342
70052526 96827 2 None - 1 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assay
ChEMBL 201 2 4 4 -1.5 N[C@@]1(C(=O)O)C[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/jm4000165
CHEMBL2381642 96827 2 None - 1 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assay
ChEMBL 201 2 4 4 -1.5 N[C@@]1(C(=O)O)C[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/jm4000165
90643871 118641 0 None - 0 Rat 5.9 pEC50 = 5.9 Binding
Positive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assayPositive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assay
ChEMBL 418 11 2 5 5.0 Cc1c(OCCCCOc2ccc(C(=O)O)cc2F)ccc(C(=O)CC(C)C)c1O 10.1021/jm5000563
CHEMBL3287693 118641 0 None - 0 Rat 5.9 pEC50 = 5.9 Binding
Positive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assayPositive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assay
ChEMBL 418 11 2 5 5.0 Cc1c(OCCCCOc2ccc(C(=O)O)cc2F)ccc(C(=O)CC(C)C)c1O 10.1021/jm5000563
90643860 118626 0 None - 0 Rat 5.8 pEC50 = 5.8 Binding
Positive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assayPositive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assay
ChEMBL 400 11 2 5 4.9 Cc1c(OCCCCOc2cccc(C(=O)O)c2)ccc(C(=O)CC(C)C)c1O 10.1021/jm5000563
CHEMBL3287675 118626 0 None - 0 Rat 5.8 pEC50 = 5.8 Binding
Positive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assayPositive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assay
ChEMBL 400 11 2 5 4.9 Cc1c(OCCCCOc2cccc(C(=O)O)c2)ccc(C(=O)CC(C)C)c1O 10.1021/jm5000563
164611067 191395 0 None - 0 Rat 5.8 pEC50 = 5.8 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 444 10 2 6 5.1 COc1cc(OC[C@H](C)COc2ccc(C(=O)CC(C)(C)C)c(O)c2C)ccc1C(=O)O 10.1016/j.bmcl.2021.128342
CHEMBL4849142 191395 0 None - 0 Rat 5.8 pEC50 = 5.8 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 444 10 2 6 5.1 COc1cc(OC[C@H](C)COc2ccc(C(=O)CC(C)(C)C)c(O)c2C)ccc1C(=O)O 10.1016/j.bmcl.2021.128342
70051926 96826 2 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assay
ChEMBL 197 2 3 3 -0.3 C=C1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/jm4000165
CHEMBL2381641 96826 2 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assay
ChEMBL 197 2 3 3 -0.3 C=C1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/jm4000165
90643887 118671 0 None - 0 Rat 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assayPositive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assay
ChEMBL 444 11 2 6 5.3 COc1ccc(C(=O)O)cc1OCCCCOc1ccc(C(=O)CC(C)(C)C)c(O)c1C 10.1021/jm5000563
CHEMBL3287723 118671 0 None - 0 Rat 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assayPositive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assay
ChEMBL 444 11 2 6 5.3 COc1ccc(C(=O)O)cc1OCCCCOc1ccc(C(=O)CC(C)(C)C)c(O)c1C 10.1021/jm5000563
164615875 192223 0 None - 0 Rat 5.8 pEC50 = 5.8 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 428 9 2 5 5.4 Cc1cc(C(=O)O)ccc1OC[C@H](C)COc1ccc(C(=O)CC(C)(C)C)c(O)c1C 10.1016/j.bmcl.2021.128342
CHEMBL4861618 192223 0 None - 0 Rat 5.8 pEC50 = 5.8 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 428 9 2 5 5.4 Cc1cc(C(=O)O)ccc1OC[C@H](C)COc1ccc(C(=O)CC(C)(C)C)c(O)c1C 10.1016/j.bmcl.2021.128342
164623088 192264 0 None - 0 Rat 5.8 pEC50 = 5.8 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 448 9 2 5 5.8 Cc1c(OC[C@@H](C)COc2ccc(C(=O)O)cc2Cl)ccc(C(=O)CC(C)(C)C)c1O 10.1016/j.bmcl.2021.128342
CHEMBL4862244 192264 0 None - 0 Rat 5.8 pEC50 = 5.8 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 448 9 2 5 5.8 Cc1c(OC[C@@H](C)COc2ccc(C(=O)O)cc2Cl)ccc(C(=O)CC(C)(C)C)c1O 10.1016/j.bmcl.2021.128342
11344646 133554 1 None 1 2 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assay
ChEMBL 199 2 3 3 -0.2 C[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/jm4000165
CHEMBL365368 133554 1 None 1 2 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assay
ChEMBL 199 2 3 3 -0.2 C[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/jm4000165
164610947 192030 0 None - 0 Rat 6.8 pEC50 = 6.8 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 415 10 2 6 4.7 Cc1c(OCCCCOc2cncc(C(=O)O)c2)ccc(C(=O)CC(C)(C)C)c1O 10.1016/j.bmcl.2021.128342
CHEMBL4858387 192030 0 None - 0 Rat 6.8 pEC50 = 6.8 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 415 10 2 6 4.7 Cc1c(OCCCCOc2cncc(C(=O)O)c2)ccc(C(=O)CC(C)(C)C)c1O 10.1016/j.bmcl.2021.128342
90643883 118666 0 None - 0 Rat 5.7 pEC50 = 5.7 Binding
Positive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assayPositive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assay
ChEMBL 416 12 2 6 4.6 CCCC(=O)c1ccc(OCCCCOc2c(OC)cccc2C(=O)O)c(C)c1O 10.1021/jm5000563
CHEMBL3287718 118666 0 None - 0 Rat 5.7 pEC50 = 5.7 Binding
Positive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assayPositive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assay
ChEMBL 416 12 2 6 4.6 CCCC(=O)c1ccc(OCCCCOc2c(OC)cccc2C(=O)O)c(C)c1O 10.1021/jm5000563
164609925 192046 0 None - 0 Rat 5.7 pEC50 = 5.7 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 430 9 2 6 4.9 COc1ccc(C(=O)O)cc1O[C@H](C)COc1ccc(C(=O)CC(C)(C)C)c(O)c1C 10.1016/j.bmcl.2021.128342
CHEMBL4858717 192046 0 None - 0 Rat 5.7 pEC50 = 5.7 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 430 9 2 6 4.9 COc1ccc(C(=O)O)cc1O[C@H](C)COc1ccc(C(=O)CC(C)(C)C)c(O)c1C 10.1016/j.bmcl.2021.128342
90643869 118639 0 None - 0 Rat 5.7 pEC50 = 5.7 Binding
Positive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assayPositive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assay
ChEMBL 414 11 2 5 5.2 Cc1cc(C(=O)O)ccc1OCCCCOc1ccc(C(=O)CC(C)C)c(O)c1C 10.1021/jm5000563
CHEMBL3287691 118639 0 None - 0 Rat 5.7 pEC50 = 5.7 Binding
Positive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assayPositive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assay
ChEMBL 414 11 2 5 5.2 Cc1cc(C(=O)O)ccc1OCCCCOc1ccc(C(=O)CC(C)C)c(O)c1C 10.1021/jm5000563
90643873 118644 0 None - 0 Rat 5.7 pEC50 = 5.7 Binding
Positive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assayPositive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assay
ChEMBL 456 13 2 6 5.4 Cc1c(OCCCCOCOc2ccc(C(=O)O)cc2)ccc(C(=O)CC2CCCC2)c1O 10.1021/jm5000563
CHEMBL3287696 118644 0 None - 0 Rat 5.7 pEC50 = 5.7 Binding
Positive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assayPositive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assay
ChEMBL 456 13 2 6 5.4 Cc1c(OCCCCOCOc2ccc(C(=O)O)cc2)ccc(C(=O)CC2CCCC2)c1O 10.1021/jm5000563
60096211 96834 0 None 5 2 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assay
ChEMBL 242 3 4 4 -1.4 CC(=O)N[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/jm4000165
CHEMBL2381649 96834 0 None 5 2 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assay
ChEMBL 242 3 4 4 -1.4 CC(=O)N[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/jm4000165
90643863 118633 0 None - 0 Rat 5.7 pEC50 = 5.7 Binding
Positive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assayPositive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assay
ChEMBL 434 11 2 5 5.5 Cc1c(OCCCCOc2ccc(C(=O)O)c(Cl)c2)ccc(C(=O)CC(C)C)c1O 10.1021/jm5000563
CHEMBL3287683 118633 0 None - 0 Rat 5.7 pEC50 = 5.7 Binding
Positive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assayPositive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assay
ChEMBL 434 11 2 5 5.5 Cc1c(OCCCCOc2ccc(C(=O)O)c(Cl)c2)ccc(C(=O)CC(C)C)c1O 10.1021/jm5000563
164624284 192808 0 None - 0 Rat 5.7 pEC50 = 5.7 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 448 9 2 5 5.8 Cc1c(OC[C@@H](C)COc2ccc(Cl)c(C(=O)O)c2)ccc(C(=O)CC(C)(C)C)c1O 10.1016/j.bmcl.2021.128342
CHEMBL4870631 192808 0 None - 0 Rat 5.7 pEC50 = 5.7 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 448 9 2 5 5.8 Cc1c(OC[C@@H](C)COc2ccc(Cl)c(C(=O)O)c2)ccc(C(=O)CC(C)(C)C)c1O 10.1016/j.bmcl.2021.128342
164613604 191963 0 None - 0 Rat 5.7 pEC50 = 5.7 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 430 9 2 6 4.9 COc1ccc(C(=O)O)cc1O[C@@H](C)COc1ccc(C(=O)CC(C)(C)C)c(O)c1C 10.1016/j.bmcl.2021.128342
CHEMBL4857426 191963 0 None - 0 Rat 5.7 pEC50 = 5.7 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 430 9 2 6 4.9 COc1ccc(C(=O)O)cc1O[C@@H](C)COc1ccc(C(=O)CC(C)(C)C)c(O)c1C 10.1016/j.bmcl.2021.128342
90643864 118634 0 None - 0 Rat 5.7 pEC50 = 5.7 Binding
Positive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assayPositive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assay
ChEMBL 460 11 2 5 6.1 Cc1c(OCCCCOc2ccc(C(=O)O)c(Cl)c2)ccc(C(=O)CC2CCCC2)c1O 10.1021/jm5000563
CHEMBL3287684 118634 0 None - 0 Rat 5.7 pEC50 = 5.7 Binding
Positive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assayPositive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assay
ChEMBL 460 11 2 5 6.1 Cc1c(OCCCCOc2ccc(C(=O)O)c(Cl)c2)ccc(C(=O)CC2CCCC2)c1O 10.1021/jm5000563
71681825 96830 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assay
ChEMBL 226 3 3 4 -0.2 [N-]=[N+]=N[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/jm4000165
CHEMBL2381645 96830 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assay
ChEMBL 226 3 3 4 -0.2 [N-]=[N+]=N[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/jm4000165
11275666 96832 1 None 15 2 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assay
ChEMBL 200 2 4 4 -1.6 N[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/jm4000165
CHEMBL2381647 96832 1 None 15 2 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assay
ChEMBL 200 2 4 4 -1.6 N[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/jm4000165
164612248 191669 0 None - 0 Rat 5.6 pEC50 = 5.6 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 418 8 2 5 5.0 Cc1c(O[C@H](C)COc2ccc(F)c(C(=O)O)c2)ccc(C(=O)CC(C)(C)C)c1O 10.1016/j.bmcl.2021.128342
CHEMBL4852903 191669 0 None - 0 Rat 5.6 pEC50 = 5.6 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 418 8 2 5 5.0 Cc1c(O[C@H](C)COc2ccc(F)c(C(=O)O)c2)ccc(C(=O)CC(C)(C)C)c1O 10.1016/j.bmcl.2021.128342
90643866 118636 0 None - 0 Rat 5.6 pEC50 = 5.6 Binding
Positive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assayPositive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assay
ChEMBL 444 11 2 5 5.5 Cc1c(OCCCCOc2ccc(F)c(C(=O)O)c2)ccc(C(=O)CC2CCCC2)c1O 10.1021/jm5000563
CHEMBL3287688 118636 0 None - 0 Rat 5.6 pEC50 = 5.6 Binding
Positive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assayPositive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assay
ChEMBL 444 11 2 5 5.5 Cc1c(OCCCCOc2ccc(F)c(C(=O)O)c2)ccc(C(=O)CC2CCCC2)c1O 10.1021/jm5000563
90643889 118674 0 None - 0 Rat 6.6 pEC50 = 6.6 Binding
Positive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assayPositive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assay
ChEMBL 432 10 2 5 5.4 Cc1c(OCCCCOc2ccc(F)c(C(=O)O)c2)ccc(C(=O)CC(C)(C)C)c1O 10.1021/jm5000563
CHEMBL3287726 118674 0 None - 0 Rat 6.6 pEC50 = 6.6 Binding
Positive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assayPositive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assay
ChEMBL 432 10 2 5 5.4 Cc1c(OCCCCOc2ccc(F)c(C(=O)O)c2)ccc(C(=O)CC(C)(C)C)c1O 10.1021/jm5000563
1393 8321 64 None -1 6 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assay
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm4000165
1396 8321 64 None -1 6 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assay
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm4000165
213056 8321 64 None -1 6 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assay
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm4000165
CHEMBL8759 8321 64 None -1 6 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assay
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm4000165
56929215 118624 0 None - 0 Rat 5.6 pEC50 = 5.6 Binding
Positive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assayPositive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assay
ChEMBL 400 11 2 5 4.9 Cc1c(OCCCCOc2ccc(C(=O)O)cc2)ccc(C(=O)CC(C)C)c1O 10.1021/jm5000563
CHEMBL3287671 118624 0 None - 0 Rat 5.6 pEC50 = 5.6 Binding
Positive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assayPositive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assay
ChEMBL 400 11 2 5 4.9 Cc1c(OCCCCOc2ccc(C(=O)O)cc2)ccc(C(=O)CC(C)C)c1O 10.1021/jm5000563
1377 8122 26 None -2 6 Rat 6.5 pEC50 = 6.5 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR3 in ratConcentration for half maximal activation of metabotropic glutamate mGluR3 in rat
ChEMBL 203 4 4 4 -1.6 N[C@@H](C1[C@H]([C@@H]1C(=O)O)C(=O)O)C(=O)O 10.1021/jm00009a001
5310979 8122 26 None -2 6 Rat 6.5 pEC50 = 6.5 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR3 in ratConcentration for half maximal activation of metabotropic glutamate mGluR3 in rat
ChEMBL 203 4 4 4 -1.6 N[C@@H](C1[C@H]([C@@H]1C(=O)O)C(=O)O)C(=O)O 10.1021/jm00009a001
CHEMBL284193 8122 26 None -2 6 Rat 6.5 pEC50 = 6.5 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR3 in ratConcentration for half maximal activation of metabotropic glutamate mGluR3 in rat
ChEMBL 203 4 4 4 -1.6 N[C@@H](C1[C@H]([C@@H]1C(=O)O)C(=O)O)C(=O)O 10.1021/jm00009a001
86765132 118673 0 None - 0 Rat 6.5 pEC50 = 6.5 Binding
Positive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assayPositive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assay
ChEMBL 428 10 2 5 5.6 Cc1c(OCCCCOc2ccc(C(=O)CC(C)(C)C)c(O)c2C)cccc1C(=O)O 10.1021/jm5000563
CHEMBL3287725 118673 0 None - 0 Rat 6.5 pEC50 = 6.5 Binding
Positive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assayPositive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assay
ChEMBL 428 10 2 5 5.6 Cc1c(OCCCCOc2ccc(C(=O)CC(C)(C)C)c(O)c2C)cccc1C(=O)O 10.1021/jm5000563
1310 9095 110 None -1 18 Rat 5.5 pEC50 = 5.5 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR3 in ratConcentration for half maximal activation of metabotropic glutamate mGluR3 in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
1369 9095 110 None -1 18 Rat 5.5 pEC50 = 5.5 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR3 in ratConcentration for half maximal activation of metabotropic glutamate mGluR3 in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
33032 9095 110 None -1 18 Rat 5.5 pEC50 = 5.5 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR3 in ratConcentration for half maximal activation of metabotropic glutamate mGluR3 in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
44272391 9095 110 None -1 18 Rat 5.5 pEC50 = 5.5 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR3 in ratConcentration for half maximal activation of metabotropic glutamate mGluR3 in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
88747398 9095 110 None -1 18 Rat 5.5 pEC50 = 5.5 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR3 in ratConcentration for half maximal activation of metabotropic glutamate mGluR3 in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
CHEMBL575060 9095 110 None -1 18 Rat 5.5 pEC50 = 5.5 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR3 in ratConcentration for half maximal activation of metabotropic glutamate mGluR3 in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
DB00142 9095 110 None -1 18 Rat 5.5 pEC50 = 5.5 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR3 in ratConcentration for half maximal activation of metabotropic glutamate mGluR3 in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
6604704 108177 35 None - 0 Human 4.5 pEC50 = 4.5 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 3 (mGluR3)Compound was tested for the inhibition of Metabotropic glutamate receptor 3 (mGluR3)
ChEMBL 173 2 3 3 -0.3 N[C@@]1(C(=O)O)CC[C@H](C(=O)O)C1 10.1021/jm970719q
CHEMBL29726 108177 35 None - 0 Human 4.5 pEC50 = 4.5 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 3 (mGluR3)Compound was tested for the inhibition of Metabotropic glutamate receptor 3 (mGluR3)
ChEMBL 173 2 3 3 -0.3 N[C@@]1(C(=O)O)CC[C@H](C(=O)O)C1 10.1021/jm970719q
164627946 193163 0 None - 0 Rat 6.5 pEC50 = 6.5 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 428 10 2 5 5.6 Cc1ccc(OCCCCOc2ccc(C(=O)CC(C)(C)C)c(O)c2C)cc1C(=O)O 10.1016/j.bmcl.2021.128342
CHEMBL4875695 193163 0 None - 0 Rat 6.5 pEC50 = 6.5 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 428 10 2 5 5.6 Cc1ccc(OCCCCOc2ccc(C(=O)CC(C)(C)C)c(O)c2C)cc1C(=O)O 10.1016/j.bmcl.2021.128342
90643888 118672 0 None - 0 Rat 6.5 pEC50 = 6.5 Binding
Positive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assayPositive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assay
ChEMBL 444 11 2 6 5.3 COc1cc(C(=O)O)ccc1OCCCCOc1ccc(C(=O)CC(C)(C)C)c(O)c1C 10.1021/jm5000563
CHEMBL3287724 118672 0 None - 0 Rat 6.5 pEC50 = 6.5 Binding
Positive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assayPositive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assay
ChEMBL 444 11 2 6 5.3 COc1cc(C(=O)O)ccc1OCCCCOc1ccc(C(=O)CC(C)(C)C)c(O)c1C 10.1021/jm5000563
1310 9095 110 None -1 18 Rat 5.5 pEC50 = 5.5 Binding
Agonist activity at rat mGlu3 receptor by FRET based mGlu sensor assayAgonist activity at rat mGlu3 receptor by FRET based mGlu sensor assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
1369 9095 110 None -1 18 Rat 5.5 pEC50 = 5.5 Binding
Agonist activity at rat mGlu3 receptor by FRET based mGlu sensor assayAgonist activity at rat mGlu3 receptor by FRET based mGlu sensor assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
33032 9095 110 None -1 18 Rat 5.5 pEC50 = 5.5 Binding
Agonist activity at rat mGlu3 receptor by FRET based mGlu sensor assayAgonist activity at rat mGlu3 receptor by FRET based mGlu sensor assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
44272391 9095 110 None -1 18 Rat 5.5 pEC50 = 5.5 Binding
Agonist activity at rat mGlu3 receptor by FRET based mGlu sensor assayAgonist activity at rat mGlu3 receptor by FRET based mGlu sensor assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
88747398 9095 110 None -1 18 Rat 5.5 pEC50 = 5.5 Binding
Agonist activity at rat mGlu3 receptor by FRET based mGlu sensor assayAgonist activity at rat mGlu3 receptor by FRET based mGlu sensor assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
CHEMBL575060 9095 110 None -1 18 Rat 5.5 pEC50 = 5.5 Binding
Agonist activity at rat mGlu3 receptor by FRET based mGlu sensor assayAgonist activity at rat mGlu3 receptor by FRET based mGlu sensor assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
DB00142 9095 110 None -1 18 Rat 5.5 pEC50 = 5.5 Binding
Agonist activity at rat mGlu3 receptor by FRET based mGlu sensor assayAgonist activity at rat mGlu3 receptor by FRET based mGlu sensor assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
90643861 118627 0 None - 0 Rat 5.5 pEC50 = 5.5 Binding
Positive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assayPositive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assay
ChEMBL 426 11 2 5 5.4 Cc1c(OCCCCOc2cccc(C(=O)O)c2)ccc(C(=O)CC2CCCC2)c1O 10.1021/jm5000563
CHEMBL3287676 118627 0 None - 0 Rat 5.5 pEC50 = 5.5 Binding
Positive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assayPositive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assay
ChEMBL 426 11 2 5 5.4 Cc1c(OCCCCOc2cccc(C(=O)O)c2)ccc(C(=O)CC2CCCC2)c1O 10.1021/jm5000563
164623240 192499 0 None - 0 Rat 5.4 pEC50 = 5.4 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 430 9 2 6 4.9 COc1ccc(C(=O)O)cc1OC[C@H](C)Oc1ccc(C(=O)CC(C)(C)C)c(O)c1C 10.1016/j.bmcl.2021.128342
CHEMBL4865723 192499 0 None - 0 Rat 5.4 pEC50 = 5.4 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 430 9 2 6 4.9 COc1ccc(C(=O)O)cc1OC[C@H](C)Oc1ccc(C(=O)CC(C)(C)C)c(O)c1C 10.1016/j.bmcl.2021.128342
164616933 191844 0 None - 0 Rat 6.4 pEC50 = 6.4 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 444 10 2 6 5.1 COc1ccc(C(=O)O)cc1OC[C@H](C)COc1ccc(C(=O)CC(C)(C)C)c(O)c1C 10.1016/j.bmcl.2021.128342
CHEMBL4855540 191844 0 None - 0 Rat 6.4 pEC50 = 6.4 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 444 10 2 6 5.1 COc1ccc(C(=O)O)cc1OC[C@H](C)COc1ccc(C(=O)CC(C)(C)C)c(O)c1C 10.1016/j.bmcl.2021.128342
90643876 118647 0 None - 0 Rat 5.4 pEC50 = 5.4 Binding
Positive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assayPositive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assay
ChEMBL 414 11 2 5 5.2 Cc1cc(OCCCCOc2ccc(C(=O)CC(C)C)c(O)c2C)ccc1C(=O)O 10.1021/jm5000563
CHEMBL3287699 118647 0 None - 0 Rat 5.4 pEC50 = 5.4 Binding
Positive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assayPositive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assay
ChEMBL 414 11 2 5 5.2 Cc1cc(OCCCCOc2ccc(C(=O)CC(C)C)c(O)c2C)ccc1C(=O)O 10.1021/jm5000563
164624303 192836 0 None - 0 Rat 5.4 pEC50 = 5.4 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 432 9 2 5 5.3 Cc1c(OC[C@@H](C)COc2cc(C(=O)O)ccc2F)ccc(C(=O)CC(C)(C)C)c1O 10.1016/j.bmcl.2021.128342
CHEMBL4871013 192836 0 None - 0 Rat 5.4 pEC50 = 5.4 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 432 9 2 5 5.3 Cc1c(OC[C@@H](C)COc2cc(C(=O)O)ccc2F)ccc(C(=O)CC(C)(C)C)c1O 10.1016/j.bmcl.2021.128342
1370 10037 67 None - 8 Rat 4.4 pEC50 = 4.4 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR3 in ratConcentration for half maximal activation of metabotropic glutamate mGluR3 in rat
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm00009a001
1372 10037 67 None - 8 Rat 4.4 pEC50 = 4.4 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR3 in ratConcentration for half maximal activation of metabotropic glutamate mGluR3 in rat
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm00009a001
40539 10037 67 None - 8 Rat 4.4 pEC50 = 4.4 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR3 in ratConcentration for half maximal activation of metabotropic glutamate mGluR3 in rat
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm00009a001
6971145 10037 67 None - 8 Rat 4.4 pEC50 = 4.4 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR3 in ratConcentration for half maximal activation of metabotropic glutamate mGluR3 in rat
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm00009a001
CHEMBL279956 10037 67 None - 8 Rat 4.4 pEC50 = 4.4 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR3 in ratConcentration for half maximal activation of metabotropic glutamate mGluR3 in rat
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm00009a001
DB02999 10037 67 None - 8 Rat 4.4 pEC50 = 4.4 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR3 in ratConcentration for half maximal activation of metabotropic glutamate mGluR3 in rat
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm00009a001
90643886 118669 0 None - 0 Rat 6.4 pEC50 = 6.4 Binding
Positive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assayPositive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assay
ChEMBL 404 11 2 5 4.8 CCCC(=O)c1ccc(OCCCCOc2ccc(F)c(C(=O)O)c2)c(C)c1O 10.1021/jm5000563
CHEMBL3287721 118669 0 None - 0 Rat 6.4 pEC50 = 6.4 Binding
Positive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assayPositive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assay
ChEMBL 404 11 2 5 4.8 CCCC(=O)c1ccc(OCCCCOc2ccc(F)c(C(=O)O)c2)c(C)c1O 10.1021/jm5000563
164616255 191727 0 None - 0 Rat 6.3 pEC50 = 6.3 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 445 10 2 5 5.1 CNC(=O)c1cc(OCCCCOc2ccc(C(=O)CC(C)(C)C)c(O)c2C)ccc1F 10.1016/j.bmcl.2021.128342
CHEMBL4853748 191727 0 None - 0 Rat 6.3 pEC50 = 6.3 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 445 10 2 5 5.1 CNC(=O)c1cc(OCCCCOc2ccc(C(=O)CC(C)(C)C)c(O)c2C)ccc1F 10.1016/j.bmcl.2021.128342
164608826 191246 0 None - 0 Rat 6.3 pEC50 = 6.3 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 444 11 2 6 5.3 COc1ccc(OCCCCOc2ccc(C(=O)CC(C)(C)C)c(O)c2C)cc1C(=O)O 10.1016/j.bmcl.2021.128342
CHEMBL4846872 191246 0 None - 0 Rat 6.3 pEC50 = 6.3 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 444 11 2 6 5.3 COc1ccc(OCCCCOc2ccc(C(=O)CC(C)(C)C)c(O)c2C)cc1C(=O)O 10.1016/j.bmcl.2021.128342
90643884 118667 0 None - 0 Rat 6.3 pEC50 = 6.3 Binding
Positive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assayPositive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assay
ChEMBL 416 12 2 6 4.6 CCCC(=O)c1ccc(OCCCCOc2cc(C(=O)O)ccc2OC)c(C)c1O 10.1021/jm5000563
CHEMBL3287719 118667 0 None - 0 Rat 6.3 pEC50 = 6.3 Binding
Positive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assayPositive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assay
ChEMBL 416 12 2 6 4.6 CCCC(=O)c1ccc(OCCCCOc2cc(C(=O)O)ccc2OC)c(C)c1O 10.1021/jm5000563
164611777 191704 0 None - 0 Rat 6.3 pEC50 = 6.3 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 444 10 2 6 5.1 COc1cc(C(=O)O)ccc1OC[C@H](C)COc1ccc(C(=O)CC(C)(C)C)c(O)c1C 10.1016/j.bmcl.2021.128342
CHEMBL4853369 191704 0 None - 0 Rat 6.3 pEC50 = 6.3 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 444 10 2 6 5.1 COc1cc(C(=O)O)ccc1OC[C@H](C)COc1ccc(C(=O)CC(C)(C)C)c(O)c1C 10.1016/j.bmcl.2021.128342
71681824 96831 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assay
ChEMBL 200 2 4 4 -1.6 N[C@@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@@H]21 10.1021/jm4000165
CHEMBL2381646 96831 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assay
ChEMBL 200 2 4 4 -1.6 N[C@@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@@H]21 10.1021/jm4000165
1310 9095 110 None -1 18 Rat 7.2 pEC50 = 7.2 Binding
Agonist activity at rat mGlu3 receptor expressed in HEK293 cells by [35S]GTP-gamma binding assayAgonist activity at rat mGlu3 receptor expressed in HEK293 cells by [35S]GTP-gamma binding assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
1369 9095 110 None -1 18 Rat 7.2 pEC50 = 7.2 Binding
Agonist activity at rat mGlu3 receptor expressed in HEK293 cells by [35S]GTP-gamma binding assayAgonist activity at rat mGlu3 receptor expressed in HEK293 cells by [35S]GTP-gamma binding assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
33032 9095 110 None -1 18 Rat 7.2 pEC50 = 7.2 Binding
Agonist activity at rat mGlu3 receptor expressed in HEK293 cells by [35S]GTP-gamma binding assayAgonist activity at rat mGlu3 receptor expressed in HEK293 cells by [35S]GTP-gamma binding assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
44272391 9095 110 None -1 18 Rat 7.2 pEC50 = 7.2 Binding
Agonist activity at rat mGlu3 receptor expressed in HEK293 cells by [35S]GTP-gamma binding assayAgonist activity at rat mGlu3 receptor expressed in HEK293 cells by [35S]GTP-gamma binding assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
88747398 9095 110 None -1 18 Rat 7.2 pEC50 = 7.2 Binding
Agonist activity at rat mGlu3 receptor expressed in HEK293 cells by [35S]GTP-gamma binding assayAgonist activity at rat mGlu3 receptor expressed in HEK293 cells by [35S]GTP-gamma binding assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
CHEMBL575060 9095 110 None -1 18 Rat 7.2 pEC50 = 7.2 Binding
Agonist activity at rat mGlu3 receptor expressed in HEK293 cells by [35S]GTP-gamma binding assayAgonist activity at rat mGlu3 receptor expressed in HEK293 cells by [35S]GTP-gamma binding assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
DB00142 9095 110 None -1 18 Rat 7.2 pEC50 = 7.2 Binding
Agonist activity at rat mGlu3 receptor expressed in HEK293 cells by [35S]GTP-gamma binding assayAgonist activity at rat mGlu3 receptor expressed in HEK293 cells by [35S]GTP-gamma binding assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
90643881 118662 0 None - 0 Rat 6.2 pEC50 = 6.2 Binding
Positive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assayPositive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assay
ChEMBL 416 11 2 6 4.5 COc1ccc(C(=O)O)cc1OCCCCOc1ccc(C(=O)C(C)C)c(O)c1C 10.1021/jm5000563
CHEMBL3287714 118662 0 None - 0 Rat 6.2 pEC50 = 6.2 Binding
Positive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assayPositive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assay
ChEMBL 416 11 2 6 4.5 COc1ccc(C(=O)O)cc1OCCCCOc1ccc(C(=O)C(C)C)c(O)c1C 10.1021/jm5000563
11084869 96828 2 None - 1 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assay
ChEMBL 201 2 4 4 -1.5 N[C@@]1(C(=O)O)C[C@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/jm4000165
CHEMBL2381643 96828 2 None - 1 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assayAgonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assay
ChEMBL 201 2 4 4 -1.5 N[C@@]1(C(=O)O)C[C@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/jm4000165
1310 9095 110 None 1 18 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human mGluR3 receptor expressed in HEK cellsAgonist activity at human mGluR3 receptor expressed in HEK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1039/C1MD00186H
1369 9095 110 None 1 18 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human mGluR3 receptor expressed in HEK cellsAgonist activity at human mGluR3 receptor expressed in HEK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1039/C1MD00186H
33032 9095 110 None 1 18 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human mGluR3 receptor expressed in HEK cellsAgonist activity at human mGluR3 receptor expressed in HEK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1039/C1MD00186H
44272391 9095 110 None 1 18 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human mGluR3 receptor expressed in HEK cellsAgonist activity at human mGluR3 receptor expressed in HEK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1039/C1MD00186H
88747398 9095 110 None 1 18 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human mGluR3 receptor expressed in HEK cellsAgonist activity at human mGluR3 receptor expressed in HEK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1039/C1MD00186H
CHEMBL575060 9095 110 None 1 18 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human mGluR3 receptor expressed in HEK cellsAgonist activity at human mGluR3 receptor expressed in HEK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1039/C1MD00186H
DB00142 9095 110 None 1 18 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human mGluR3 receptor expressed in HEK cellsAgonist activity at human mGluR3 receptor expressed in HEK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1039/C1MD00186H
1310 9095 110 None -1 18 Rat 7.2 pEC50 = 7.2 Binding
Agonist activity at rat mGlu3 receptor expressed in HEK293 cells by [35S]GTP-gamma binding assayAgonist activity at rat mGlu3 receptor expressed in HEK293 cells by [35S]GTP-gamma binding assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
1369 9095 110 None -1 18 Rat 7.2 pEC50 = 7.2 Binding
Agonist activity at rat mGlu3 receptor expressed in HEK293 cells by [35S]GTP-gamma binding assayAgonist activity at rat mGlu3 receptor expressed in HEK293 cells by [35S]GTP-gamma binding assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
33032 9095 110 None -1 18 Rat 7.2 pEC50 = 7.2 Binding
Agonist activity at rat mGlu3 receptor expressed in HEK293 cells by [35S]GTP-gamma binding assayAgonist activity at rat mGlu3 receptor expressed in HEK293 cells by [35S]GTP-gamma binding assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
44272391 9095 110 None -1 18 Rat 7.2 pEC50 = 7.2 Binding
Agonist activity at rat mGlu3 receptor expressed in HEK293 cells by [35S]GTP-gamma binding assayAgonist activity at rat mGlu3 receptor expressed in HEK293 cells by [35S]GTP-gamma binding assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
88747398 9095 110 None -1 18 Rat 7.2 pEC50 = 7.2 Binding
Agonist activity at rat mGlu3 receptor expressed in HEK293 cells by [35S]GTP-gamma binding assayAgonist activity at rat mGlu3 receptor expressed in HEK293 cells by [35S]GTP-gamma binding assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
CHEMBL575060 9095 110 None -1 18 Rat 7.2 pEC50 = 7.2 Binding
Agonist activity at rat mGlu3 receptor expressed in HEK293 cells by [35S]GTP-gamma binding assayAgonist activity at rat mGlu3 receptor expressed in HEK293 cells by [35S]GTP-gamma binding assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
DB00142 9095 110 None -1 18 Rat 7.2 pEC50 = 7.2 Binding
Agonist activity at rat mGlu3 receptor expressed in HEK293 cells by [35S]GTP-gamma binding assayAgonist activity at rat mGlu3 receptor expressed in HEK293 cells by [35S]GTP-gamma binding assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
90643858 118643 0 None - 0 Rat 6.2 pEC50 = 6.2 Binding
Positive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assayPositive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assay
ChEMBL 430 12 2 6 4.9 COc1cc(C(=O)O)ccc1OCCCCOc1ccc(C(=O)CC(C)C)c(O)c1C 10.1021/jm5000563
CHEMBL3287695 118643 0 None - 0 Rat 6.2 pEC50 = 6.2 Binding
Positive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assayPositive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assay
ChEMBL 430 12 2 6 4.9 COc1cc(C(=O)O)ccc1OCCCCOc1ccc(C(=O)CC(C)C)c(O)c1C 10.1021/jm5000563
90643880 118657 0 None - 0 Rat 5.2 pEC50 = 5.2 Binding
Positive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assayPositive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assay
ChEMBL 402 11 2 6 4.2 CCC(=O)c1ccc(OCCCCOc2cc(C(=O)O)ccc2OC)c(C)c1O 10.1021/jm5000563
CHEMBL3287709 118657 0 None - 0 Rat 5.2 pEC50 = 5.2 Binding
Positive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assayPositive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assay
ChEMBL 402 11 2 6 4.2 CCC(=O)c1ccc(OCCCCOc2cc(C(=O)O)ccc2OC)c(C)c1O 10.1021/jm5000563
164624801 192990 0 None - 0 Rat 6.2 pEC50 = 6.2 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 432 9 2 5 5.3 Cc1c(OC[C@H](C)COc2ccc(F)c(C(=O)O)c2)ccc(C(=O)CC(C)(C)C)c1O 10.1016/j.bmcl.2021.128342
CHEMBL4873125 192990 0 None - 0 Rat 6.2 pEC50 = 6.2 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 432 9 2 5 5.3 Cc1c(OC[C@H](C)COc2ccc(F)c(C(=O)O)c2)ccc(C(=O)CC(C)(C)C)c1O 10.1016/j.bmcl.2021.128342
164617451 191731 0 None - 0 Rat 6.2 pEC50 = 6.2 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 444 11 2 6 5.3 COc1cc(OCCCCOc2ccc(C(=O)CC(C)(C)C)c(O)c2C)cc(C(=O)O)c1 10.1016/j.bmcl.2021.128342
CHEMBL4853794 191731 0 None - 0 Rat 6.2 pEC50 = 6.2 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 444 11 2 6 5.3 COc1cc(OCCCCOc2ccc(C(=O)CC(C)(C)C)c(O)c2C)cc(C(=O)O)c1 10.1016/j.bmcl.2021.128342
90643878 118649 0 None - 0 Rat 6.1 pEC50 = 6.1 Binding
Positive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assayPositive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assay
ChEMBL 430 12 2 6 4.9 COc1ccc(C(=O)O)cc1OCCCCOc1ccc(C(=O)CC(C)C)c(O)c1C 10.1021/jm5000563
CHEMBL3287701 118649 0 None - 0 Rat 6.1 pEC50 = 6.1 Binding
Positive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assayPositive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assay
ChEMBL 430 12 2 6 4.9 COc1ccc(C(=O)O)cc1OCCCCOc1ccc(C(=O)CC(C)C)c(O)c1C 10.1021/jm5000563
164621310 192344 0 None - 0 Rat 7.1 pEC50 = 7.1 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 429 10 2 6 5.0 Cc1ncc(OCCCCOc2ccc(C(=O)CC(C)(C)C)c(O)c2C)cc1C(=O)O 10.1016/j.bmcl.2021.128342
CHEMBL4863303 192344 0 None - 0 Rat 7.1 pEC50 = 7.1 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 429 10 2 6 5.0 Cc1ncc(OCCCCOc2ccc(C(=O)CC(C)(C)C)c(O)c2C)cc1C(=O)O 10.1016/j.bmcl.2021.128342
1377 8122 26 None -2 6 Rat 7.1 pEC50 = 7.1 Binding
Agonist activity at rat mGlu3 receptor by FRET based mGlu sensor assayAgonist activity at rat mGlu3 receptor by FRET based mGlu sensor assay
ChEMBL 203 4 4 4 -1.6 N[C@@H](C1[C@H]([C@@H]1C(=O)O)C(=O)O)C(=O)O 10.1021/acs.jmedchem.5b01333
5310979 8122 26 None -2 6 Rat 7.1 pEC50 = 7.1 Binding
Agonist activity at rat mGlu3 receptor by FRET based mGlu sensor assayAgonist activity at rat mGlu3 receptor by FRET based mGlu sensor assay
ChEMBL 203 4 4 4 -1.6 N[C@@H](C1[C@H]([C@@H]1C(=O)O)C(=O)O)C(=O)O 10.1021/acs.jmedchem.5b01333
CHEMBL284193 8122 26 None -2 6 Rat 7.1 pEC50 = 7.1 Binding
Agonist activity at rat mGlu3 receptor by FRET based mGlu sensor assayAgonist activity at rat mGlu3 receptor by FRET based mGlu sensor assay
ChEMBL 203 4 4 4 -1.6 N[C@@H](C1[C@H]([C@@H]1C(=O)O)C(=O)O)C(=O)O 10.1021/acs.jmedchem.5b01333
104766 6822 42 None -10 11 Rat 5.1 pEC50 = 5.1 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR3 in ratConcentration for half maximal activation of metabotropic glutamate mGluR3 in rat
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1021/jm00009a001
1365 6822 42 None -10 11 Rat 5.1 pEC50 = 5.1 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR3 in ratConcentration for half maximal activation of metabotropic glutamate mGluR3 in rat
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1021/jm00009a001
CHEMBL34453 6822 42 None -10 11 Rat 5.1 pEC50 = 5.1 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR3 in ratConcentration for half maximal activation of metabotropic glutamate mGluR3 in rat
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1021/jm00009a001
164616491 192170 0 None - 0 Rat 6.1 pEC50 = 6.1 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 430 9 2 6 4.9 COc1ccc(C(=O)O)cc1OC[C@@H](C)Oc1ccc(C(=O)CC(C)(C)C)c(O)c1C 10.1016/j.bmcl.2021.128342
CHEMBL4860693 192170 0 None - 0 Rat 6.1 pEC50 = 6.1 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 430 9 2 6 4.9 COc1ccc(C(=O)O)cc1OC[C@@H](C)Oc1ccc(C(=O)CC(C)(C)C)c(O)c1C 10.1016/j.bmcl.2021.128342
164620553 192548 0 None - 0 Rat 6.1 pEC50 = 6.1 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 448 9 2 5 5.8 Cc1c(OC[C@@H](C)COc2ccc(C(=O)O)c(Cl)c2)ccc(C(=O)CC(C)(C)C)c1O 10.1016/j.bmcl.2021.128342
CHEMBL4866466 192548 0 None - 0 Rat 6.1 pEC50 = 6.1 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 448 9 2 5 5.8 Cc1c(OC[C@@H](C)COc2ccc(C(=O)O)c(Cl)c2)ccc(C(=O)CC(C)(C)C)c1O 10.1016/j.bmcl.2021.128342
164625596 192521 0 None - 0 Rat 6.1 pEC50 = 6.1 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 428 10 2 5 5.6 Cc1ccc(C(=O)O)cc1OCCCCOc1ccc(C(=O)CC(C)(C)C)c(O)c1C 10.1016/j.bmcl.2021.128342
CHEMBL4866163 192521 0 None - 0 Rat 6.1 pEC50 = 6.1 Binding
Positive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assayPositive allosteric modulator activity at rat mGlu3 receptor transfected in GIRK channel overexpressing cells assessed as potentiation of glutamate-induced response by thallium mobilization assay
ChEMBL 428 10 2 5 5.6 Cc1ccc(C(=O)O)cc1OCCCCOc1ccc(C(=O)CC(C)(C)C)c(O)c1C 10.1016/j.bmcl.2021.128342
139054390 211702 106 None - 5 Rat 5.1 pEC50 = 5.1 Binding
Effect on Metabotropic glutamate receptor 3Effect on Metabotropic glutamate receptor 3
ChEMBL 147 4 3 3 -0.7 N[C@H](CCC(=O)O)C(=O)O 10.1021/jm9703597
23327 211702 106 None - 5 Rat 5.1 pEC50 = 5.1 Binding
Effect on Metabotropic glutamate receptor 3Effect on Metabotropic glutamate receptor 3
ChEMBL 147 4 3 3 -0.7 N[C@H](CCC(=O)O)C(=O)O 10.1021/jm9703597
CHEMBL76232 211702 106 None - 5 Rat 5.1 pEC50 = 5.1 Binding
Effect on Metabotropic glutamate receptor 3Effect on Metabotropic glutamate receptor 3
ChEMBL 147 4 3 3 -0.7 N[C@H](CCC(=O)O)C(=O)O 10.1021/jm9703597
90643865 118635 0 None - 0 Rat 6.0 pEC50 = 6.0 Binding
Positive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assayPositive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assay
ChEMBL 418 11 2 5 5.0 Cc1c(OCCCCOc2ccc(F)c(C(=O)O)c2)ccc(C(=O)CC(C)C)c1O 10.1021/jm5000563
CHEMBL3287687 118635 0 None - 0 Rat 6.0 pEC50 = 6.0 Binding
Positive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assayPositive allosteric modulation of rat mGluR3 receptor expressed in HEK293 cells assessed as potentiation of glutamate-induced thallium flux incubated for 2.5 mins prior to glutamate addition measured after 2.5 mins by GIRK assay
ChEMBL 418 11 2 5 5.0 Cc1c(OCCCCOc2ccc(F)c(C(=O)O)c2)ccc(C(=O)CC(C)C)c1O 10.1021/jm5000563
70052526 96827 2 None - 1 Human 8.0 pIC50 = 8.0 Binding
Agonist activity at mGlu3 (unknown origin)Agonist activity at mGlu3 (unknown origin)
ChEMBL 201 2 4 4 -1.5 N[C@@]1(C(=O)O)C[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
CHEMBL2381642 96827 2 None - 1 Human 8.0 pIC50 = 8.0 Binding
Agonist activity at mGlu3 (unknown origin)Agonist activity at mGlu3 (unknown origin)
ChEMBL 201 2 4 4 -1.5 N[C@@]1(C(=O)O)C[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
145949267 169596 6 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Negative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium flux preincubated for 5 mins followed by glutamate addition and measured after 2 mins by BTC-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium flux preincubated for 5 mins followed by glutamate addition and measured after 2 mins by BTC-AM-dye based fluorescence assay
ChEMBL 339 6 0 4 3.8 C[C@@H](COc1ccn(-c2ccc(F)cc2)c(=O)c1)Oc1ccccc1 10.1016/j.bmcl.2019.07.030
CHEMBL4172540 169596 6 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Negative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium flux preincubated for 5 mins followed by glutamate addition and measured after 2 mins by BTC-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium flux preincubated for 5 mins followed by glutamate addition and measured after 2 mins by BTC-AM-dye based fluorescence assay
ChEMBL 339 6 0 4 3.8 C[C@@H](COc1ccn(-c2ccc(F)cc2)c(=O)c1)Oc1ccccc1 10.1016/j.bmcl.2019.07.030
10089411 14299 0 None - 1 Rat 5.9 pIC50 = 5.9 Binding
Compound was evaluated for the inhibition of binding of [3H]glutamate against rat recombinant Metabotropic glutamate receptor 3 expressed in HEK293 cellsCompound was evaluated for the inhibition of binding of [3H]glutamate against rat recombinant Metabotropic glutamate receptor 3 expressed in HEK293 cells
ChEMBL 353 5 3 4 2.7 NC(C(=O)O)[C@@H]1[C@@H](C(=O)O)[C@@H]1CC1c2ccccc2Oc2ccccc21 10.1016/s0960-894x(01)00656-4
CHEMBL108735 14299 0 None - 1 Rat 5.9 pIC50 = 5.9 Binding
Compound was evaluated for the inhibition of binding of [3H]glutamate against rat recombinant Metabotropic glutamate receptor 3 expressed in HEK293 cellsCompound was evaluated for the inhibition of binding of [3H]glutamate against rat recombinant Metabotropic glutamate receptor 3 expressed in HEK293 cells
ChEMBL 353 5 3 4 2.7 NC(C(=O)O)[C@@H]1[C@@H](C(=O)O)[C@@H]1CC1c2ccccc2Oc2ccccc21 10.1016/s0960-894x(01)00656-4
155533264 178603 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Negative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium fluxNegative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium flux
ChEMBL 335 6 0 4 4.0 Cc1cccc(-n2ccc(OC[C@H](C)Oc3ccccc3)cc2=O)c1 10.1016/j.bmcl.2019.07.030
CHEMBL4468538 178603 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Negative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium fluxNegative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium flux
ChEMBL 335 6 0 4 4.0 Cc1cccc(-n2ccc(OC[C@H](C)Oc3ccccc3)cc2=O)c1 10.1016/j.bmcl.2019.07.030
155556417 181278 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Negative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium fluxNegative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium flux
ChEMBL 349 7 0 4 4.2 Cc1cccc(-n2ccc(OC[C@H](C)COc3ccccc3)cc2=O)c1 10.1016/j.bmcl.2019.07.030
CHEMBL4554871 181278 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Negative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium fluxNegative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium flux
ChEMBL 349 7 0 4 4.2 Cc1cccc(-n2ccc(OC[C@H](C)COc3ccccc3)cc2=O)c1 10.1016/j.bmcl.2019.07.030
1378 9195 54 None -5 10 Rat 7.9 pIC50 = 7.9 Binding
Concentration required to inhibit metabotropic glutamate receptor 3 activity of rat expressed in CHO cellsConcentration required to inhibit metabotropic glutamate receptor 3 activity of rat expressed in CHO cells
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/jm0400294
1399 9195 54 None -5 10 Rat 7.9 pIC50 = 7.9 Binding
Concentration required to inhibit metabotropic glutamate receptor 3 activity of rat expressed in CHO cellsConcentration required to inhibit metabotropic glutamate receptor 3 activity of rat expressed in CHO cells
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/jm0400294
9819927 9195 54 None -5 10 Rat 7.9 pIC50 = 7.9 Binding
Concentration required to inhibit metabotropic glutamate receptor 3 activity of rat expressed in CHO cellsConcentration required to inhibit metabotropic glutamate receptor 3 activity of rat expressed in CHO cells
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/jm0400294
CHEMBL432038 9195 54 None -5 10 Rat 7.9 pIC50 = 7.9 Binding
Concentration required to inhibit metabotropic glutamate receptor 3 activity of rat expressed in CHO cellsConcentration required to inhibit metabotropic glutamate receptor 3 activity of rat expressed in CHO cells
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/jm0400294
155542406 179905 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Negative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium fluxNegative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium flux
ChEMBL 369 7 0 4 4.6 C[C@H](COc1ccccc1)COc1ccn(-c2cccc(Cl)c2)c(=O)c1 10.1016/j.bmcl.2019.07.030
CHEMBL4520808 179905 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Negative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium fluxNegative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium flux
ChEMBL 369 7 0 4 4.6 C[C@H](COc1ccccc1)COc1ccn(-c2cccc(Cl)c2)c(=O)c1 10.1016/j.bmcl.2019.07.030
56587994 10817 41 None - 0 Human 5.8 pIC50 = 5.8 Binding
Negative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assayNegative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assay
ChEMBL 349 3 1 3 2.9 OC[C@@H]1CCCN(C1)C(=O)c1ccc(cc1)C#Cc1ccc(cc1)OC 10.1016/j.bmcl.2012.04.112
6225 10817 41 None - 0 Human 5.8 pIC50 = 5.8 Binding
Negative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assayNegative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assay
ChEMBL 349 3 1 3 2.9 OC[C@@H]1CCCN(C1)C(=O)c1ccc(cc1)C#Cc1ccc(cc1)OC 10.1016/j.bmcl.2012.04.112
CHEMBL2204445 10817 41 None - 0 Human 5.8 pIC50 = 5.8 Binding
Negative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assayNegative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assay
ChEMBL 349 3 1 3 2.9 OC[C@@H]1CCCN(C1)C(=O)c1ccc(cc1)C#Cc1ccc(cc1)OC 10.1016/j.bmcl.2012.04.112
56587994 10817 41 None - 0 Human 5.8 pIC50 = 5.8 Binding
Negative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assayNegative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assay
ChEMBL 349 3 1 3 2.9 OC[C@@H]1CCCN(C1)C(=O)c1ccc(cc1)C#Cc1ccc(cc1)OC 10.1016/j.bmcl.2012.04.112
6225 10817 41 None - 0 Human 5.8 pIC50 = 5.8 Binding
Negative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assayNegative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assay
ChEMBL 349 3 1 3 2.9 OC[C@@H]1CCCN(C1)C(=O)c1ccc(cc1)C#Cc1ccc(cc1)OC 10.1016/j.bmcl.2012.04.112
CHEMBL2204445 10817 41 None - 0 Human 5.8 pIC50 = 5.8 Binding
Negative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assayNegative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assay
ChEMBL 349 3 1 3 2.9 OC[C@@H]1CCCN(C1)C(=O)c1ccc(cc1)C#Cc1ccc(cc1)OC 10.1016/j.bmcl.2012.04.112
155563014 182068 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Negative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium fluxNegative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium flux
ChEMBL 335 6 0 4 4.0 Cc1cccc(-n2ccc(O[C@H](C)COc3ccccc3)cc2=O)c1 10.1016/j.bmcl.2019.07.030
CHEMBL4572957 182068 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Negative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium fluxNegative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium flux
ChEMBL 335 6 0 4 4.0 Cc1cccc(-n2ccc(O[C@H](C)COc3ccccc3)cc2=O)c1 10.1016/j.bmcl.2019.07.030
1378 9195 54 None -5 10 Rat 7.8 pIC50 = 7.8 Binding
Compound was evaluated for the inhibition of binding of [3H]glutamate against rat recombinant mGluR3 receptors expressed in HEK293 cellsCompound was evaluated for the inhibition of binding of [3H]glutamate against rat recombinant mGluR3 receptors expressed in HEK293 cells
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1016/s0960-894x(01)00656-4
1399 9195 54 None -5 10 Rat 7.8 pIC50 = 7.8 Binding
Compound was evaluated for the inhibition of binding of [3H]glutamate against rat recombinant mGluR3 receptors expressed in HEK293 cellsCompound was evaluated for the inhibition of binding of [3H]glutamate against rat recombinant mGluR3 receptors expressed in HEK293 cells
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1016/s0960-894x(01)00656-4
9819927 9195 54 None -5 10 Rat 7.8 pIC50 = 7.8 Binding
Compound was evaluated for the inhibition of binding of [3H]glutamate against rat recombinant mGluR3 receptors expressed in HEK293 cellsCompound was evaluated for the inhibition of binding of [3H]glutamate against rat recombinant mGluR3 receptors expressed in HEK293 cells
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1016/s0960-894x(01)00656-4
CHEMBL432038 9195 54 None -5 10 Rat 7.8 pIC50 = 7.8 Binding
Compound was evaluated for the inhibition of binding of [3H]glutamate against rat recombinant mGluR3 receptors expressed in HEK293 cellsCompound was evaluated for the inhibition of binding of [3H]glutamate against rat recombinant mGluR3 receptors expressed in HEK293 cells
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1016/s0960-894x(01)00656-4
11503055 9179 3 None - 0 Human 6.7 pIC50 = 6.7 Binding
Negative allosteric modulation of human mGlu3 expressed in AV-12 cells in presence of glutamate EC90 concentration by FLIPR assayNegative allosteric modulation of human mGlu3 expressed in AV-12 cells in presence of glutamate EC90 concentration by FLIPR assay
ChEMBL 400 4 1 4 3.9 Clc1ccc(c(c1)Cl)CN[C@H]1CCN(C1)c1ncc(cn1)Br 10.1016/j.bmcl.2012.04.112
9694 9179 3 None - 0 Human 6.7 pIC50 = 6.7 Binding
Negative allosteric modulation of human mGlu3 expressed in AV-12 cells in presence of glutamate EC90 concentration by FLIPR assayNegative allosteric modulation of human mGlu3 expressed in AV-12 cells in presence of glutamate EC90 concentration by FLIPR assay
ChEMBL 400 4 1 4 3.9 Clc1ccc(c(c1)Cl)CN[C@H]1CCN(C1)c1ncc(cn1)Br 10.1016/j.bmcl.2012.04.112
CHEMBL2204436 9179 3 None - 0 Human 6.7 pIC50 = 6.7 Binding
Negative allosteric modulation of human mGlu3 expressed in AV-12 cells in presence of glutamate EC90 concentration by FLIPR assayNegative allosteric modulation of human mGlu3 expressed in AV-12 cells in presence of glutamate EC90 concentration by FLIPR assay
ChEMBL 400 4 1 4 3.9 Clc1ccc(c(c1)Cl)CN[C@H]1CCN(C1)c1ncc(cn1)Br 10.1016/j.bmcl.2012.04.112
53393868 90379 7 None - 0 Human 5.7 pIC50 = 5.7 Binding
Negative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assayNegative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assay
ChEMBL 349 3 1 3 2.9 COc1ccc(C#Cc2ccc(C(=O)N3CCCC(CO)C3)cc2)cc1 10.1016/j.bmcl.2012.04.112
CHEMBL2204442 90379 7 None - 0 Human 5.7 pIC50 = 5.7 Binding
Negative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assayNegative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assay
ChEMBL 349 3 1 3 2.9 COc1ccc(C#Cc2ccc(C(=O)N3CCCC(CO)C3)cc2)cc1 10.1016/j.bmcl.2012.04.112
53393868 90379 7 None - 0 Human 5.7 pIC50 = 5.7 Binding
Negative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assayNegative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assay
ChEMBL 349 3 1 3 2.9 COc1ccc(C#Cc2ccc(C(=O)N3CCCC(CO)C3)cc2)cc1 10.1016/j.bmcl.2012.04.112
CHEMBL2204442 90379 7 None - 0 Human 5.7 pIC50 = 5.7 Binding
Negative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assayNegative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assay
ChEMBL 349 3 1 3 2.9 COc1ccc(C#Cc2ccc(C(=O)N3CCCC(CO)C3)cc2)cc1 10.1016/j.bmcl.2012.04.112
1397 9307 15 None -2 5 Rat 7.6 pIC50 = 7.6 Binding
Concentration required to inhibit metabotropic glutamate receptor 3 activity of rat expressed in CHO cellsConcentration required to inhibit metabotropic glutamate receptor 3 activity of rat expressed in CHO cells
ChEMBL 377 5 3 4 2.1 OC(=O)[C@]1(N)[C@H](OCc2ccc(c(c2)Cl)Cl)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O 10.1021/jm0400294
9886034 9307 15 None -2 5 Rat 7.6 pIC50 = 7.6 Binding
Concentration required to inhibit metabotropic glutamate receptor 3 activity of rat expressed in CHO cellsConcentration required to inhibit metabotropic glutamate receptor 3 activity of rat expressed in CHO cells
ChEMBL 377 5 3 4 2.1 OC(=O)[C@]1(N)[C@H](OCc2ccc(c(c2)Cl)Cl)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O 10.1021/jm0400294
CHEMBL186453 9307 15 None -2 5 Rat 7.6 pIC50 = 7.6 Binding
Concentration required to inhibit metabotropic glutamate receptor 3 activity of rat expressed in CHO cellsConcentration required to inhibit metabotropic glutamate receptor 3 activity of rat expressed in CHO cells
ChEMBL 377 5 3 4 2.1 OC(=O)[C@]1(N)[C@H](OCc2ccc(c(c2)Cl)Cl)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O 10.1021/jm0400294
53393854 90377 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Negative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assayNegative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assay
ChEMBL 335 2 1 3 2.7 COc1ccc(C#Cc2ccc(C(=O)N3CCCC(O)C3)cc2)cc1 10.1016/j.bmcl.2012.04.112
CHEMBL2204439 90377 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Negative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assayNegative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assay
ChEMBL 335 2 1 3 2.7 COc1ccc(C#Cc2ccc(C(=O)N3CCCC(O)C3)cc2)cc1 10.1016/j.bmcl.2012.04.112
53393854 90377 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Negative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assayNegative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assay
ChEMBL 335 2 1 3 2.7 COc1ccc(C#Cc2ccc(C(=O)N3CCCC(O)C3)cc2)cc1 10.1016/j.bmcl.2012.04.112
CHEMBL2204439 90377 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Negative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assayNegative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assay
ChEMBL 335 2 1 3 2.7 COc1ccc(C#Cc2ccc(C(=O)N3CCCC(O)C3)cc2)cc1 10.1016/j.bmcl.2012.04.112
1393 8321 64 None -1 6 Human 7.6 pIC50 = 7.6 Binding
Agonist activity at mGlu3 (unknown origin)Agonist activity at mGlu3 (unknown origin)
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/acs.jmedchem.6b01119
1396 8321 64 None -1 6 Human 7.6 pIC50 = 7.6 Binding
Agonist activity at mGlu3 (unknown origin)Agonist activity at mGlu3 (unknown origin)
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/acs.jmedchem.6b01119
213056 8321 64 None -1 6 Human 7.6 pIC50 = 7.6 Binding
Agonist activity at mGlu3 (unknown origin)Agonist activity at mGlu3 (unknown origin)
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/acs.jmedchem.6b01119
CHEMBL8759 8321 64 None -1 6 Human 7.6 pIC50 = 7.6 Binding
Agonist activity at mGlu3 (unknown origin)Agonist activity at mGlu3 (unknown origin)
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/acs.jmedchem.6b01119
11158623 10124 11 None - 2 Human 6.6 pIC50 = 6.6 Binding
Negative allosteric modulation of mGlu3 by cell-based assayNegative allosteric modulation of mGlu3 by cell-based assay
ChEMBL 423 2 1 3 6.2 O=C1CC(=Nc2c(N1)cc(c(c2)C)C(F)(F)F)c1cccc(c1)c1cc(C)nc(c1)C 10.1016/j.bmcl.2012.04.112
6226 10124 11 None - 2 Human 6.6 pIC50 = 6.6 Binding
Negative allosteric modulation of mGlu3 by cell-based assayNegative allosteric modulation of mGlu3 by cell-based assay
ChEMBL 423 2 1 3 6.2 O=C1CC(=Nc2c(N1)cc(c(c2)C)C(F)(F)F)c1cccc(c1)c1cc(C)nc(c1)C 10.1016/j.bmcl.2012.04.112
CHEMBL1629855 10124 11 None - 2 Human 6.6 pIC50 = 6.6 Binding
Negative allosteric modulation of mGlu3 by cell-based assayNegative allosteric modulation of mGlu3 by cell-based assay
ChEMBL 423 2 1 3 6.2 O=C1CC(=Nc2c(N1)cc(c(c2)C)C(F)(F)F)c1cccc(c1)c1cc(C)nc(c1)C 10.1016/j.bmcl.2012.04.112
11158623 10124 11 None - 2 Human 6.6 pIC50 = 6.6 Binding
Negative allosteric modulation of mGlu3 receptor (unknown origin)Negative allosteric modulation of mGlu3 receptor (unknown origin)
ChEMBL 423 2 1 3 6.2 O=C1CC(=Nc2c(N1)cc(c(c2)C)C(F)(F)F)c1cccc(c1)c1cc(C)nc(c1)C 10.1021/jm400439t
6226 10124 11 None - 2 Human 6.6 pIC50 = 6.6 Binding
Negative allosteric modulation of mGlu3 receptor (unknown origin)Negative allosteric modulation of mGlu3 receptor (unknown origin)
ChEMBL 423 2 1 3 6.2 O=C1CC(=Nc2c(N1)cc(c(c2)C)C(F)(F)F)c1cccc(c1)c1cc(C)nc(c1)C 10.1021/jm400439t
CHEMBL1629855 10124 11 None - 2 Human 6.6 pIC50 = 6.6 Binding
Negative allosteric modulation of mGlu3 receptor (unknown origin)Negative allosteric modulation of mGlu3 receptor (unknown origin)
ChEMBL 423 2 1 3 6.2 O=C1CC(=Nc2c(N1)cc(c(c2)C)C(F)(F)F)c1cccc(c1)c1cc(C)nc(c1)C 10.1021/jm400439t
155544343 180158 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Negative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium fluxNegative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium flux
ChEMBL 355 6 0 4 4.3 C[C@H](COc1ccccc1)Oc1ccn(-c2ccc(Cl)cc2)c(=O)c1 10.1016/j.bmcl.2019.07.030
CHEMBL4527797 180158 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Negative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium fluxNegative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium flux
ChEMBL 355 6 0 4 4.3 C[C@H](COc1ccccc1)Oc1ccn(-c2ccc(Cl)cc2)c(=O)c1 10.1016/j.bmcl.2019.07.030
68290289 124432 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Negative allosteric modulation at mGluR3 (unknown origin)Negative allosteric modulation at mGluR3 (unknown origin)
ChEMBL 337 4 0 4 3.6 O=C1N(c2ccc(F)cc2)CCc2nc(COc3ccccc3)cn21 10.1016/j.bmcl.2015.01.038
CHEMBL3401195 124432 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Negative allosteric modulation at mGluR3 (unknown origin)Negative allosteric modulation at mGluR3 (unknown origin)
ChEMBL 337 4 0 4 3.6 O=C1N(c2ccc(F)cc2)CCc2nc(COc3ccccc3)cn21 10.1016/j.bmcl.2015.01.038
155538767 180040 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Negative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium fluxNegative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium flux
ChEMBL 339 6 0 4 3.8 C[C@H](COc1ccccc1)Oc1ccn(-c2ccc(F)cc2)c(=O)c1 10.1016/j.bmcl.2019.07.030
CHEMBL4524912 180040 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Negative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium fluxNegative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium flux
ChEMBL 339 6 0 4 3.8 C[C@H](COc1ccccc1)Oc1ccn(-c2ccc(F)cc2)c(=O)c1 10.1016/j.bmcl.2019.07.030
155541818 179847 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Negative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium fluxNegative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium flux
ChEMBL 349 7 0 4 4.2 Cc1cccc(-n2ccc(OC[C@@H](C)COc3ccccc3)cc2=O)c1 10.1016/j.bmcl.2019.07.030
CHEMBL4519557 179847 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Negative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium fluxNegative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium flux
ChEMBL 349 7 0 4 4.2 Cc1cccc(-n2ccc(OC[C@@H](C)COc3ccccc3)cc2=O)c1 10.1016/j.bmcl.2019.07.030
155518189 177047 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Negative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium fluxNegative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium flux
ChEMBL 353 7 0 4 4.1 CC(COc1ccccc1)COc1ccn(-c2ccc(F)cc2)c(=O)c1 10.1016/j.bmcl.2019.07.030
CHEMBL4446121 177047 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Negative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium fluxNegative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium flux
ChEMBL 353 7 0 4 4.1 CC(COc1ccccc1)COc1ccn(-c2ccc(F)cc2)c(=O)c1 10.1016/j.bmcl.2019.07.030
155567480 182679 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Negative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium fluxNegative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium flux
ChEMBL 349 7 0 4 4.2 Cc1cccc(-n2ccc(OCC(C)COc3ccccc3)cc2=O)c1 10.1016/j.bmcl.2019.07.030
CHEMBL4586828 182679 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Negative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium fluxNegative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium flux
ChEMBL 349 7 0 4 4.2 Cc1cccc(-n2ccc(OCC(C)COc3ccccc3)cc2=O)c1 10.1016/j.bmcl.2019.07.030
56587985 90380 2 None - 0 Human 5.5 pIC50 = 5.5 Binding
Negative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assayNegative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assay
ChEMBL 349 3 1 3 2.9 COc1ccc(C#Cc2ccc(C(=O)N3CCC[C@H](CO)C3)cc2)cc1 10.1016/j.bmcl.2012.04.112
CHEMBL2204446 90380 2 None - 0 Human 5.5 pIC50 = 5.5 Binding
Negative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assayNegative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assay
ChEMBL 349 3 1 3 2.9 COc1ccc(C#Cc2ccc(C(=O)N3CCC[C@H](CO)C3)cc2)cc1 10.1016/j.bmcl.2012.04.112
53338952 90375 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Negative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assayNegative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assay
ChEMBL 335 2 1 3 2.7 COc1ccc(C#Cc2ccc(C(=O)N3CCC(O)CC3)cc2)cc1 10.1016/j.bmcl.2012.04.112
CHEMBL2204437 90375 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Negative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assayNegative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assay
ChEMBL 335 2 1 3 2.7 COc1ccc(C#Cc2ccc(C(=O)N3CCC(O)CC3)cc2)cc1 10.1016/j.bmcl.2012.04.112
53338952 90375 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Negative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assayNegative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assay
ChEMBL 335 2 1 3 2.7 COc1ccc(C#Cc2ccc(C(=O)N3CCC(O)CC3)cc2)cc1 10.1016/j.bmcl.2012.04.112
CHEMBL2204437 90375 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Negative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assayNegative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assay
ChEMBL 335 2 1 3 2.7 COc1ccc(C#Cc2ccc(C(=O)N3CCC(O)CC3)cc2)cc1 10.1016/j.bmcl.2012.04.112
155512594 176441 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Negative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium fluxNegative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium flux
ChEMBL 347 4 0 4 3.9 Cc1cccc(-n2ccc(OCC3CCc4ccccc4O3)cc2=O)c1 10.1016/j.bmcl.2019.07.030
CHEMBL4437442 176441 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Negative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium fluxNegative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium flux
ChEMBL 347 4 0 4 3.9 Cc1cccc(-n2ccc(OCC3CCc4ccccc4O3)cc2=O)c1 10.1016/j.bmcl.2019.07.030
11503055 9179 3 None - 0 Human 5.4 pIC50 = 5.4 Binding
Negative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assayNegative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assay
ChEMBL 400 4 1 4 3.9 Clc1ccc(c(c1)Cl)CN[C@H]1CCN(C1)c1ncc(cn1)Br 10.1016/j.bmcl.2012.04.112
9694 9179 3 None - 0 Human 5.4 pIC50 = 5.4 Binding
Negative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assayNegative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assay
ChEMBL 400 4 1 4 3.9 Clc1ccc(c(c1)Cl)CN[C@H]1CCN(C1)c1ncc(cn1)Br 10.1016/j.bmcl.2012.04.112
CHEMBL2204436 9179 3 None - 0 Human 5.4 pIC50 = 5.4 Binding
Negative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assayNegative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assay
ChEMBL 400 4 1 4 3.9 Clc1ccc(c(c1)Cl)CN[C@H]1CCN(C1)c1ncc(cn1)Br 10.1016/j.bmcl.2012.04.112
56587992 90376 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Negative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assayNegative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assay
ChEMBL 349 2 1 3 3.1 COc1ccc(C#Cc2ccc(C(=O)N3CCC(C)(O)CC3)cc2)cc1 10.1016/j.bmcl.2012.04.112
CHEMBL2204438 90376 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Negative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assayNegative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assay
ChEMBL 349 2 1 3 3.1 COc1ccc(C#Cc2ccc(C(=O)N3CCC(C)(O)CC3)cc2)cc1 10.1016/j.bmcl.2012.04.112
56587992 90376 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Negative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assayNegative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assay
ChEMBL 349 2 1 3 3.1 COc1ccc(C#Cc2ccc(C(=O)N3CCC(C)(O)CC3)cc2)cc1 10.1016/j.bmcl.2012.04.112
CHEMBL2204438 90376 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Negative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assayNegative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assay
ChEMBL 349 2 1 3 3.1 COc1ccc(C#Cc2ccc(C(=O)N3CCC(C)(O)CC3)cc2)cc1 10.1016/j.bmcl.2012.04.112
155522365 177440 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Negative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium fluxNegative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium flux
ChEMBL 355 6 0 4 4.3 C[C@H](COc1ccccc1)Oc1ccn(-c2cccc(Cl)c2)c(=O)c1 10.1016/j.bmcl.2019.07.030
CHEMBL4451520 177440 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Negative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium fluxNegative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium flux
ChEMBL 355 6 0 4 4.3 C[C@H](COc1ccccc1)Oc1ccn(-c2cccc(Cl)c2)c(=O)c1 10.1016/j.bmcl.2019.07.030
56587985 90380 2 None - 0 Human 5.3 pIC50 = 5.3 Binding
Negative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assayNegative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assay
ChEMBL 349 3 1 3 2.9 COc1ccc(C#Cc2ccc(C(=O)N3CCC[C@H](CO)C3)cc2)cc1 10.1016/j.bmcl.2012.04.112
CHEMBL2204446 90380 2 None - 0 Human 5.3 pIC50 = 5.3 Binding
Negative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assayNegative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assay
ChEMBL 349 3 1 3 2.9 COc1ccc(C#Cc2ccc(C(=O)N3CCC[C@H](CO)C3)cc2)cc1 10.1016/j.bmcl.2012.04.112
56587978 90378 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Negative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assayNegative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assay
ChEMBL 363 3 1 3 3.0 COc1ccc(C#Cc2ccc(C(=O)N3CCC[C@H](C(=O)O)C3)cc2)cc1 10.1016/j.bmcl.2012.04.112
CHEMBL2204440 90378 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Negative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assayNegative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assay
ChEMBL 363 3 1 3 3.0 COc1ccc(C#Cc2ccc(C(=O)N3CCC[C@H](C(=O)O)C3)cc2)cc1 10.1016/j.bmcl.2012.04.112
56587978 90378 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Negative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assayNegative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assay
ChEMBL 363 3 1 3 3.0 COc1ccc(C#Cc2ccc(C(=O)N3CCC[C@H](C(=O)O)C3)cc2)cc1 10.1016/j.bmcl.2012.04.112
CHEMBL2204440 90378 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Negative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assayNegative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assay
ChEMBL 363 3 1 3 3.0 COc1ccc(C#Cc2ccc(C(=O)N3CCC[C@H](C(=O)O)C3)cc2)cc1 10.1016/j.bmcl.2012.04.112
11084869 96828 2 None - 1 Human 8.2 pIC50 = 8.2 Binding
Agonist activity at mGlu3 (unknown origin)Agonist activity at mGlu3 (unknown origin)
ChEMBL 201 2 4 4 -1.5 N[C@@]1(C(=O)O)C[C@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
CHEMBL2381643 96828 2 None - 1 Human 8.2 pIC50 = 8.2 Binding
Agonist activity at mGlu3 (unknown origin)Agonist activity at mGlu3 (unknown origin)
ChEMBL 201 2 4 4 -1.5 N[C@@]1(C(=O)O)C[C@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
68290572 124415 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Negative allosteric modulation at mGluR3 (unknown origin)Negative allosteric modulation at mGluR3 (unknown origin)
ChEMBL 335 4 0 5 3.2 O=c1n(-c2ccc(F)cc2)ccc2nc(COc3ccccc3)cn12 10.1016/j.bmcl.2015.01.038
CHEMBL3401177 124415 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Negative allosteric modulation at mGluR3 (unknown origin)Negative allosteric modulation at mGluR3 (unknown origin)
ChEMBL 335 4 0 5 3.2 O=c1n(-c2ccc(F)cc2)ccc2nc(COc3ccccc3)cn12 10.1016/j.bmcl.2015.01.038
9885546 117315 0 None - 1 Rat 7.1 pIC50 = 7.1 Binding
Compound was evaluated for the inhibition of binding of [3H]glutamate against rat recombinant Metabotropic glutamate receptor 3 expressed in HEK293 cellsCompound was evaluated for the inhibition of binding of [3H]glutamate against rat recombinant Metabotropic glutamate receptor 3 expressed in HEK293 cells
ChEMBL 367 6 3 4 3.1 NC(C(=O)O)[C@@H]1[C@@H](C(=O)O)[C@@H]1CCC1c2ccccc2Oc2ccccc21 10.1016/s0960-894x(01)00656-4
CHEMBL325140 117315 0 None - 1 Rat 7.1 pIC50 = 7.1 Binding
Compound was evaluated for the inhibition of binding of [3H]glutamate against rat recombinant Metabotropic glutamate receptor 3 expressed in HEK293 cellsCompound was evaluated for the inhibition of binding of [3H]glutamate against rat recombinant Metabotropic glutamate receptor 3 expressed in HEK293 cells
ChEMBL 367 6 3 4 3.1 NC(C(=O)O)[C@@H]1[C@@H](C(=O)O)[C@@H]1CCC1c2ccccc2Oc2ccccc21 10.1016/s0960-894x(01)00656-4
155517751 177017 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Negative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium fluxNegative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium flux
ChEMBL 351 4 0 4 3.7 O=c1cc(OCC2CCc3ccccc3O2)ccn1-c1ccc(F)cc1 10.1016/j.bmcl.2019.07.030
CHEMBL4445711 177017 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Negative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium fluxNegative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium flux
ChEMBL 351 4 0 4 3.7 O=c1cc(OCC2CCc3ccccc3O2)ccn1-c1ccc(F)cc1 10.1016/j.bmcl.2019.07.030
155536972 179015 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Negative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium fluxNegative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium flux
ChEMBL 369 7 0 4 4.6 C[C@H](COc1ccccc1)COc1ccn(-c2ccc(Cl)cc2)c(=O)c1 10.1016/j.bmcl.2019.07.030
CHEMBL4474204 179015 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Negative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium fluxNegative allosteric modulation of rat mGlu3R expressed in HEK cells harboring GIRK assessed as reduction in glutamate-induced thallium flux
ChEMBL 369 7 0 4 4.6 C[C@H](COc1ccccc1)COc1ccn(-c2ccc(Cl)cc2)c(=O)c1 10.1016/j.bmcl.2019.07.030
10353365 90022 1 None 5 2 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]LY341495 from human recombinant mGluR3 in RGT cellsDisplacement of [3H]LY341495 from human recombinant mGluR3 in RGT cells
ChEMBL 219 2 3 4 -1.8 N[C@@]1(C(=O)O)C[S+]([O-])[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm060917u
CHEMBL218710 90022 1 None 5 2 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]LY341495 from human recombinant mGluR3 in RGT cellsDisplacement of [3H]LY341495 from human recombinant mGluR3 in RGT cells
ChEMBL 219 2 3 4 -1.8 N[C@@]1(C(=O)O)C[S+]([O-])[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm060917u
60096178 163660 0 None 181 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation countingDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation counting
ChEMBL 338 4 4 4 0.6 N[C@@]1(C(=O)O)C[C@H](NC(=O)c2cccc(Cl)c2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
CHEMBL4071962 163660 0 None 181 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation countingDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation counting
ChEMBL 338 4 4 4 0.6 N[C@@]1(C(=O)O)C[C@H](NC(=O)c2cccc(Cl)c2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
60096231 164434 15 None 446 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation countingDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation counting
ChEMBL 334 5 4 5 -0.1 COc1cccc(C(=O)N[C@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)c1 10.1021/acs.jmedchem.7b01481
CHEMBL4081453 164434 15 None 446 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation countingDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation counting
ChEMBL 334 5 4 5 -0.1 COc1cccc(C(=O)N[C@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)c1 10.1021/acs.jmedchem.7b01481
1378 9195 54 None 1 10 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/acs.jmedchem.6b01119
1399 9195 54 None 1 10 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/acs.jmedchem.6b01119
9819927 9195 54 None 1 10 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/acs.jmedchem.6b01119
CHEMBL432038 9195 54 None 1 10 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/acs.jmedchem.6b01119
60096224 163324 0 None 32 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation countingDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation counting
ChEMBL 320 4 5 5 -0.4 N[C@@]1(C(=O)O)C[C@H](NC(=O)c2ccccc2O)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
CHEMBL4068189 163324 0 None 32 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation countingDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation counting
ChEMBL 320 4 5 5 -0.4 N[C@@]1(C(=O)O)C[C@H](NC(=O)c2ccccc2O)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
10197984 9199 44 None -2 5 Human 6.0 pKi = 6.0 Binding
Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.
ChEMBL 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10.1021/jm980616n
1394 9199 44 None -2 5 Human 6.0 pKi = 6.0 Binding
Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.
ChEMBL 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10.1021/jm980616n
CHEMBL275079 9199 44 None -2 5 Human 6.0 pKi = 6.0 Binding
Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.
ChEMBL 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10.1021/jm980616n
1393 8321 64 None -1 6 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation countingDisplacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation counting
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/acs.jmedchem.5b01124
1396 8321 64 None -1 6 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation countingDisplacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation counting
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/acs.jmedchem.5b01124
213056 8321 64 None -1 6 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation countingDisplacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation counting
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/acs.jmedchem.5b01124
CHEMBL8759 8321 64 None -1 6 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation countingDisplacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation counting
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/acs.jmedchem.5b01124
1393 8321 64 None -1 6 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation countingDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation counting
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/acs.jmedchem.7b01481
1396 8321 64 None -1 6 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation countingDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation counting
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/acs.jmedchem.7b01481
213056 8321 64 None -1 6 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation countingDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation counting
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/acs.jmedchem.7b01481
CHEMBL8759 8321 64 None -1 6 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation countingDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation counting
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/acs.jmedchem.7b01481
60096194 163367 0 None 10 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation countingDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation counting
ChEMBL 290 5 4 4 0.3 N[C@@]1(C(=O)O)C[C@H](NCc2ccccc2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
CHEMBL4068679 163367 0 None 10 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation countingDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation counting
ChEMBL 290 5 4 4 0.3 N[C@@]1(C(=O)O)C[C@H](NCc2ccccc2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
1393 8321 64 None -1 6 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]LY-341,495 binding to recombinant human mGlu3 receptorsInhibition of [3H]LY-341,495 binding to recombinant human mGlu3 receptors
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm050235r
1396 8321 64 None -1 6 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]LY-341,495 binding to recombinant human mGlu3 receptorsInhibition of [3H]LY-341,495 binding to recombinant human mGlu3 receptors
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm050235r
213056 8321 64 None -1 6 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]LY-341,495 binding to recombinant human mGlu3 receptorsInhibition of [3H]LY-341,495 binding to recombinant human mGlu3 receptors
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm050235r
CHEMBL8759 8321 64 None -1 6 Human 6.9 pKi = 6.9 Binding
Inhibition of [3H]LY-341,495 binding to recombinant human mGlu3 receptorsInhibition of [3H]LY-341,495 binding to recombinant human mGlu3 receptors
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm050235r
71136653 130181 0 None -2 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation countingDisplacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation counting
ChEMBL 284 4 4 6 -0.6 N[C@@]1(C(=O)O)C[C@H](Sc2nnc[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
CHEMBL3616854 130181 0 None -2 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation countingDisplacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation counting
ChEMBL 284 4 4 6 -0.6 N[C@@]1(C(=O)O)C[C@H](Sc2nnc[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
10979251 96835 0 None 3 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation countingDisplacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation counting
ChEMBL 293 4 3 4 1.3 N[C@@]1(C(=O)O)C[C@@H](Sc2ccccc2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
CHEMBL2381650 96835 0 None 3 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation countingDisplacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation counting
ChEMBL 293 4 3 4 1.3 N[C@@]1(C(=O)O)C[C@@H](Sc2ccccc2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
10197984 9199 44 None -2 5 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.
ChEMBL 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10.1021/jm980616n
1394 9199 44 None -2 5 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.
ChEMBL 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10.1021/jm980616n
CHEMBL275079 9199 44 None -2 5 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.
ChEMBL 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10.1021/jm980616n
11298568 76150 1 None 6 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-341495 binding to membranes expressing recombinant human Metabotropic glutamate receptor 3Displacement of [3H]-341495 binding to membranes expressing recombinant human Metabotropic glutamate receptor 3
ChEMBL 199 2 3 3 -0.2 C[C@@H]1C[C@H]2[C@H](C(=O)O)[C@H]2[C@]1(N)C(=O)O 10.1021/jm040222y
CHEMBL192977 76150 1 None 6 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-341495 binding to membranes expressing recombinant human Metabotropic glutamate receptor 3Displacement of [3H]-341495 binding to membranes expressing recombinant human Metabotropic glutamate receptor 3
ChEMBL 199 2 3 3 -0.2 C[C@@H]1C[C@H]2[C@H](C(=O)O)[C@H]2[C@]1(N)C(=O)O 10.1021/jm040222y
11347391 73626 0 None -2 2 Rat 7.8 pKi = 7.8 Binding
Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008
ChEMBL 309 5 3 4 0.8 N[C@@]1(C(=O)O)[C@H](OCc2ccccc2)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O 10.1021/jm0400294
CHEMBL186214 73626 0 None -2 2 Rat 7.8 pKi = 7.8 Binding
Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008
ChEMBL 309 5 3 4 0.8 N[C@@]1(C(=O)O)[C@H](OCc2ccccc2)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O 10.1021/jm0400294
53240406 130174 17 None -1 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation countingDisplacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation counting
ChEMBL 284 4 4 6 -0.6 N[C@@]1(C(=O)O)C[C@@H](Sc2nnc[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
CHEMBL3616847 130174 17 None -1 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation countingDisplacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation counting
ChEMBL 284 4 4 6 -0.6 N[C@@]1(C(=O)O)C[C@@H](Sc2nnc[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
71136655 130179 0 None 1 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation countingDisplacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation counting
ChEMBL 326 5 4 6 0.5 CC(C)c1nnc(S[C@@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)[nH]1 10.1021/acs.jmedchem.5b01124
CHEMBL3616852 130179 0 None 1 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation countingDisplacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation counting
ChEMBL 326 5 4 6 0.5 CC(C)c1nnc(S[C@@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)[nH]1 10.1021/acs.jmedchem.5b01124
162658340 190465 0 None 1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 405 6 4 5 1.9 N[C@@]1(C(=O)O)[C@H](CSCc2ccc(Cl)c(Cl)c2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
CHEMBL4760856 190465 0 None 1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 405 6 4 5 1.9 N[C@@]1(C(=O)O)[C@H](CSCc2ccc(Cl)c(Cl)c2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
CHEMBL4803084 190465 0 None 1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 405 6 4 5 1.9 N[C@@]1(C(=O)O)[C@H](CSCc2ccc(Cl)c(Cl)c2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
10198133 213287 12 None 6 2 Human 6.8 pKi = 6.8 Binding
Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.
ChEMBL 203 2 3 4 -0.8 N[C@@]1(C(=O)O)CS[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm980616n
CHEMBL8839 213287 12 None 6 2 Human 6.8 pKi = 6.8 Binding
Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.
ChEMBL 203 2 3 4 -0.8 N[C@@]1(C(=O)O)CS[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm980616n
60096211 96834 0 None 5 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation countingDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation counting
ChEMBL 242 3 4 4 -1.4 CC(=O)N[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/acs.jmedchem.7b01481
CHEMBL2381649 96834 0 None 5 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation countingDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation counting
ChEMBL 242 3 4 4 -1.4 CC(=O)N[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/acs.jmedchem.7b01481
162658781 190470 0 None 1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 323 5 4 5 0.5 N[C@@]1(C(=O)O)[C@H](CSc2ccccc2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
CHEMBL4759209 190470 0 None 1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 323 5 4 5 0.5 N[C@@]1(C(=O)O)[C@H](CSc2ccccc2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
CHEMBL4803105 190470 0 None 1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 323 5 4 5 0.5 N[C@@]1(C(=O)O)[C@H](CSc2ccccc2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
60096190 165292 0 None 102 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation countingDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation counting
ChEMBL 322 4 4 4 0.1 N[C@@]1(C(=O)O)C[C@H](NC(=O)c2cccc(F)c2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
CHEMBL4091203 165292 0 None 102 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation countingDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation counting
ChEMBL 322 4 4 4 0.1 N[C@@]1(C(=O)O)C[C@H](NC(=O)c2cccc(F)c2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
60096201 165347 0 None 13 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation countingDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation counting
ChEMBL 320 4 5 5 -0.4 N[C@@]1(C(=O)O)C[C@H](NC(=O)c2cccc(O)c2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
CHEMBL4091735 165347 0 None 13 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation countingDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation counting
ChEMBL 320 4 5 5 -0.4 N[C@@]1(C(=O)O)C[C@H](NC(=O)c2cccc(O)c2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
60096250 165700 0 None 60 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation countingDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation counting
ChEMBL 338 4 4 4 0.6 N[C@@]1(C(=O)O)C[C@H](NC(=O)c2ccc(Cl)cc2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
CHEMBL4095567 165700 0 None 60 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation countingDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation counting
ChEMBL 338 4 4 4 0.6 N[C@@]1(C(=O)O)C[C@H](NC(=O)c2ccc(Cl)cc2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
69669747 190432 11 None 2 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 359 5 4 5 0.8 N[C@@]1(C(=O)O)[C@H](CSc2ccc(F)c(F)c2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
CHEMBL4751065 190432 11 None 2 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 359 5 4 5 0.8 N[C@@]1(C(=O)O)[C@H](CSc2ccc(F)c(F)c2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
CHEMBL4802733 190432 11 None 2 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 359 5 4 5 0.8 N[C@@]1(C(=O)O)[C@H](CSc2ccc(F)c(F)c2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
67705089 159034 0 None 2 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-LY459477 from human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing human EAAT1 after 90 mins by liquid scintillation counting methodDisplacement of [3H]-LY459477 from human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing human EAAT1 after 90 mins by liquid scintillation counting method
ChEMBL 458 7 4 7 1.9 N[C@@]1(C(=O)O)[C@H](OCc2ccc(Cl)c(Cl)c2)[C@@H](Sc2nc[nH]n2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1016/j.bmcl.2016.10.067
CHEMBL3969063 159034 0 None 2 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-LY459477 from human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing human EAAT1 after 90 mins by liquid scintillation counting methodDisplacement of [3H]-LY459477 from human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing human EAAT1 after 90 mins by liquid scintillation counting method
ChEMBL 458 7 4 7 1.9 N[C@@]1(C(=O)O)[C@H](OCc2ccc(Cl)c(Cl)c2)[C@@H](Sc2nc[nH]n2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1016/j.bmcl.2016.10.067
60096183 166063 0 None 6 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation countingDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation counting
ChEMBL 334 5 4 5 -0.1 COc1ccccc1C(=O)N[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/acs.jmedchem.7b01481
CHEMBL4099470 166063 0 None 6 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation countingDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation counting
ChEMBL 334 5 4 5 -0.1 COc1ccccc1C(=O)N[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/acs.jmedchem.7b01481
162663798 190498 0 None 1 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 323 5 4 5 0.5 N[C@]1(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@@H]2[C@@H](O)[C@@H]1CSc1ccccc1 10.1021/acs.jmedchem.6b01119
CHEMBL4779554 190498 0 None 1 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 323 5 4 5 0.5 N[C@]1(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@@H]2[C@@H](O)[C@@H]1CSc1ccccc1 10.1021/acs.jmedchem.6b01119
CHEMBL4803378 190498 0 None 1 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 323 5 4 5 0.5 N[C@]1(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@@H]2[C@@H](O)[C@@H]1CSc1ccccc1 10.1021/acs.jmedchem.6b01119
162666357 190510 0 None 1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 341 5 4 5 0.6 N[C@@]1(C(=O)O)[C@H](CSc2cccc(F)c2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
CHEMBL4784701 190510 0 None 1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 341 5 4 5 0.6 N[C@@]1(C(=O)O)[C@H](CSc2cccc(F)c2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
CHEMBL4803523 190510 0 None 1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 341 5 4 5 0.6 N[C@@]1(C(=O)O)[C@H](CSc2cccc(F)c2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
162644419 190401 0 None 1 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 323 5 4 5 0.5 N[C@]1(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@@H]2[C@H](O)[C@@H]1CSc1ccccc1 10.1021/acs.jmedchem.6b01119
CHEMBL4778355 190401 0 None 1 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 323 5 4 5 0.5 N[C@]1(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@@H]2[C@H](O)[C@@H]1CSc1ccccc1 10.1021/acs.jmedchem.6b01119
CHEMBL4802356 190401 0 None 1 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 323 5 4 5 0.5 N[C@]1(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@@H]2[C@H](O)[C@@H]1CSc1ccccc1 10.1021/acs.jmedchem.6b01119
71136640 130180 0 None -1 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation countingDisplacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation counting
ChEMBL 284 4 4 6 -0.6 N[C@@]1(C(=O)O)C[C@@H](Sc2c[nH]nn2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
CHEMBL3616853 130180 0 None -1 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation countingDisplacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation counting
ChEMBL 284 4 4 6 -0.6 N[C@@]1(C(=O)O)C[C@@H](Sc2c[nH]nn2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
69669646 190458 0 None -1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 351 5 4 5 1.1 Cc1ccc(SC[C@@H]2[C@@H](O)[C@@H]3[C@@H]([C@H]3C(=O)O)[C@]2(N)C(=O)O)cc1C 10.1021/acs.jmedchem.6b01119
CHEMBL4757159 190458 0 None -1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 351 5 4 5 1.1 Cc1ccc(SC[C@@H]2[C@@H](O)[C@@H]3[C@@H]([C@H]3C(=O)O)[C@]2(N)C(=O)O)cc1C 10.1021/acs.jmedchem.6b01119
CHEMBL4802990 190458 0 None -1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 351 5 4 5 1.1 Cc1ccc(SC[C@@H]2[C@@H](O)[C@@H]3[C@@H]([C@H]3C(=O)O)[C@]2(N)C(=O)O)cc1C 10.1021/acs.jmedchem.6b01119
162665071 190507 0 None 1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 323 5 4 5 0.5 N[C@@]1(C(=O)O)[C@H](CSc2ccccc2)[C@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
CHEMBL4781638 190507 0 None 1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 323 5 4 5 0.5 N[C@@]1(C(=O)O)[C@H](CSc2ccccc2)[C@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
CHEMBL4803454 190507 0 None 1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 323 5 4 5 0.5 N[C@@]1(C(=O)O)[C@H](CSc2ccccc2)[C@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
137659992 166015 0 None 14 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation countingDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation counting
ChEMBL 338 4 4 4 0.6 N[C@@]1(C(=O)O)C[C@H](NC(=O)c2ccccc2Cl)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
CHEMBL4098939 166015 0 None 14 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation countingDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation counting
ChEMBL 338 4 4 4 0.6 N[C@@]1(C(=O)O)C[C@H](NC(=O)c2ccccc2Cl)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
71681826 96836 0 None 4 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation countingDisplacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation counting
ChEMBL 293 4 3 4 1.3 N[C@@]1(C(=O)O)C[C@H](Sc2ccccc2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
CHEMBL2381651 96836 0 None 4 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation countingDisplacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation counting
ChEMBL 293 4 3 4 1.3 N[C@@]1(C(=O)O)C[C@H](Sc2ccccc2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
137634033 163420 0 None 2 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation countingDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation counting
ChEMBL 332 6 4 4 0.2 N[C@@]1(C(=O)O)C[C@H](NC(=O)CCc2ccccc2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
CHEMBL4069251 163420 0 None 2 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation countingDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation counting
ChEMBL 332 6 4 4 0.2 N[C@@]1(C(=O)O)C[C@H](NC(=O)CCc2ccccc2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
11275666 96832 1 None 15 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation countingDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation counting
ChEMBL 200 2 4 4 -1.6 N[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/acs.jmedchem.7b01481
CHEMBL2381647 96832 1 None 15 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation countingDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation counting
ChEMBL 200 2 4 4 -1.6 N[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/acs.jmedchem.7b01481
11382367 73711 0 None -1 2 Rat 8.5 pKi = 8.5 Binding
Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008
ChEMBL 345 5 3 4 1.1 N[C@@]1(C(=O)O)[C@H](OCc2ccc(F)c(F)c2)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O 10.1021/jm0400294
CHEMBL186630 73711 0 None -1 2 Rat 8.5 pKi = 8.5 Binding
Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008
ChEMBL 345 5 3 4 1.1 N[C@@]1(C(=O)O)[C@H](OCc2ccc(F)c(F)c2)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O 10.1021/jm0400294
44361401 38115 0 None 7 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards metabotropic glutamate receptor 3 was determinedBinding affinity towards metabotropic glutamate receptor 3 was determined
ChEMBL 175 3 4 4 -1.9 N[C@H](C(=O)O)[C@H]1[C@@H](O)[C@@H]1C(=O)O 10.1021/jm030967o
CHEMBL140197 38115 0 None 7 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards metabotropic glutamate receptor 3 was determinedBinding affinity towards metabotropic glutamate receptor 3 was determined
ChEMBL 175 3 4 4 -1.9 N[C@H](C(=O)O)[C@H]1[C@@H](O)[C@@H]1C(=O)O 10.1021/jm030967o
1378 9195 54 None -5 10 Rat 8.5 pKi = 8.5 Binding
Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/jm0400294
1399 9195 54 None -5 10 Rat 8.5 pKi = 8.5 Binding
Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/jm0400294
9819927 9195 54 None -5 10 Rat 8.5 pKi = 8.5 Binding
Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/jm0400294
CHEMBL432038 9195 54 None -5 10 Rat 8.5 pKi = 8.5 Binding
Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/jm0400294
1395 9306 15 None -2 2 Rat 8.4 pKi = 8.4 Binding
Tested for binding affinity against Metabotropic glutamate receptor 3 in CHO cells using [3H]-7 as radioligandTested for binding affinity against Metabotropic glutamate receptor 3 in CHO cells using [3H]-7 as radioligand
ChEMBL 217 2 3 4 -1.2 O=C1C[C@@]([C@H]2[C@@H]1[C@]2(F)C(=O)O)(N)C(=O)O 10.1021/jm000346k
9837317 9306 15 None -2 2 Rat 8.4 pKi = 8.4 Binding
Tested for binding affinity against Metabotropic glutamate receptor 3 in CHO cells using [3H]-7 as radioligandTested for binding affinity against Metabotropic glutamate receptor 3 in CHO cells using [3H]-7 as radioligand
ChEMBL 217 2 3 4 -1.2 O=C1C[C@@]([C@H]2[C@@H]1[C@]2(F)C(=O)O)(N)C(=O)O 10.1021/jm000346k
CHEMBL121053 9306 15 None -2 2 Rat 8.4 pKi = 8.4 Binding
Tested for binding affinity against Metabotropic glutamate receptor 3 in CHO cells using [3H]-7 as radioligandTested for binding affinity against Metabotropic glutamate receptor 3 in CHO cells using [3H]-7 as radioligand
ChEMBL 217 2 3 4 -1.2 O=C1C[C@@]([C@H]2[C@@H]1[C@]2(F)C(=O)O)(N)C(=O)O 10.1021/jm000346k
11257636 175151 0 None -1 2 Rat 8.4 pKi = 8.4 Binding
Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008
ChEMBL 385 6 3 4 2.4 N[C@@]1(C(=O)O)[C@H](OC(c2ccccc2)c2ccccc2)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O 10.1021/jm0400294
CHEMBL434536 175151 0 None -1 2 Rat 8.4 pKi = 8.4 Binding
Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008
ChEMBL 385 6 3 4 2.4 N[C@@]1(C(=O)O)[C@H](OC(c2ccccc2)c2ccccc2)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O 10.1021/jm0400294
11310142 9200 19 None -1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-341495 binding to membranes expressing recombinant human Metabotropic glutamate receptor 3Displacement of [3H]-341495 binding to membranes expressing recombinant human Metabotropic glutamate receptor 3
ChEMBL 199 2 3 3 -0.2 C[C@@H]1C[C@@]([C@H]2[C@@H]1[C@@H]2C(=O)O)(N)C(=O)O 10.1021/jm040222y
11614 9200 19 None -1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-341495 binding to membranes expressing recombinant human Metabotropic glutamate receptor 3Displacement of [3H]-341495 binding to membranes expressing recombinant human Metabotropic glutamate receptor 3
ChEMBL 199 2 3 3 -0.2 C[C@@H]1C[C@@]([C@H]2[C@@H]1[C@@H]2C(=O)O)(N)C(=O)O 10.1021/jm040222y
CHEMBL192051 9200 19 None -1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-341495 binding to membranes expressing recombinant human Metabotropic glutamate receptor 3Displacement of [3H]-341495 binding to membranes expressing recombinant human Metabotropic glutamate receptor 3
ChEMBL 199 2 3 3 -0.2 C[C@@H]1C[C@@]([C@H]2[C@@H]1[C@@H]2C(=O)O)(N)C(=O)O 10.1021/jm040222y
69669702 190454 0 None -1 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 354 5 4 5 0.9 Cc1cc(SC[C@@H]2[C@@H](N)[C@H]3[C@H](C(=O)O)[C@H]3[C@]2(N)C(=O)O)ccc1F 10.1021/acs.jmedchem.6b01119
CHEMBL4756556 190454 0 None -1 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 354 5 4 5 0.9 Cc1cc(SC[C@@H]2[C@@H](N)[C@H]3[C@H](C(=O)O)[C@H]3[C@]2(N)C(=O)O)ccc1F 10.1021/acs.jmedchem.6b01119
CHEMBL4802948 190454 0 None -1 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 354 5 4 5 0.9 Cc1cc(SC[C@@H]2[C@@H](N)[C@H]3[C@H](C(=O)O)[C@H]3[C@]2(N)C(=O)O)ccc1F 10.1021/acs.jmedchem.6b01119
162654849 190449 0 None 1 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 341 5 4 5 0.6 N[C@@]1(C(=O)O)[C@H](CSc2ccccc2F)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
CHEMBL4755204 190449 0 None 1 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 341 5 4 5 0.6 N[C@@]1(C(=O)O)[C@H](CSc2ccccc2F)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
CHEMBL4802906 190449 0 None 1 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 341 5 4 5 0.6 N[C@@]1(C(=O)O)[C@H](CSc2ccccc2F)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
10807972 42591 1 None -1 2 Rat 8.4 pKi = 8.4 Binding
Tested for binding affinity against Metabotropic glutamate receptor 3 in CHO cells using [3H]-7 as radioligandTested for binding affinity against Metabotropic glutamate receptor 3 in CHO cells using [3H]-7 as radioligand
ChEMBL 353 5 3 4 2.8 N[C@@](CC1c2ccccc2Oc2ccccc21)(C(=O)O)[C@H]1C[C@@H]1C(=O)O 10.1021/jm000346k
CHEMBL144151 42591 1 None -1 2 Rat 8.4 pKi = 8.4 Binding
Tested for binding affinity against Metabotropic glutamate receptor 3 in CHO cells using [3H]-7 as radioligandTested for binding affinity against Metabotropic glutamate receptor 3 in CHO cells using [3H]-7 as radioligand
ChEMBL 353 5 3 4 2.8 N[C@@](CC1c2ccccc2Oc2ccccc21)(C(=O)O)[C@H]1C[C@@H]1C(=O)O 10.1021/jm000346k
60096204 162903 0 None 75 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation countingDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation counting
ChEMBL 322 4 4 4 0.1 N[C@@]1(C(=O)O)C[C@H](NC(=O)c2ccc(F)cc2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
CHEMBL4063336 162903 0 None 75 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation countingDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation counting
ChEMBL 322 4 4 4 0.1 N[C@@]1(C(=O)O)C[C@H](NC(=O)c2ccc(F)cc2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
1397 9307 15 None -2 5 Rat 8.4 pKi = 8.4 Binding
Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008
ChEMBL 377 5 3 4 2.1 OC(=O)[C@]1(N)[C@H](OCc2ccc(c(c2)Cl)Cl)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O 10.1021/jm0400294
9886034 9307 15 None -2 5 Rat 8.4 pKi = 8.4 Binding
Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008
ChEMBL 377 5 3 4 2.1 OC(=O)[C@]1(N)[C@H](OCc2ccc(c(c2)Cl)Cl)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O 10.1021/jm0400294
CHEMBL186453 9307 15 None -2 5 Rat 8.4 pKi = 8.4 Binding
Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008
ChEMBL 377 5 3 4 2.1 OC(=O)[C@]1(N)[C@H](OCc2ccc(c(c2)Cl)Cl)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O 10.1021/jm0400294
1397 9307 15 None -2 5 Human 8.4 pKi = 8.4 Binding
Binding affinity to mGLUR3Binding affinity to mGLUR3
ChEMBL 377 5 3 4 2.1 OC(=O)[C@]1(N)[C@H](OCc2ccc(c(c2)Cl)Cl)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O 10.1016/j.bmcl.2012.01.039
9886034 9307 15 None -2 5 Human 8.4 pKi = 8.4 Binding
Binding affinity to mGLUR3Binding affinity to mGLUR3
ChEMBL 377 5 3 4 2.1 OC(=O)[C@]1(N)[C@H](OCc2ccc(c(c2)Cl)Cl)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O 10.1016/j.bmcl.2012.01.039
CHEMBL186453 9307 15 None -2 5 Human 8.4 pKi = 8.4 Binding
Binding affinity to mGLUR3Binding affinity to mGLUR3
ChEMBL 377 5 3 4 2.1 OC(=O)[C@]1(N)[C@H](OCc2ccc(c(c2)Cl)Cl)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O 10.1016/j.bmcl.2012.01.039
67637415 190466 0 None 1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 438 7 4 7 1.9 Cc1cc(SC[C@@H]2[C@@H](Sc3nc[nH]n3)[C@H]3[C@H](C(=O)O)[C@H]3[C@]2(N)C(=O)O)ccc1F 10.1021/acs.jmedchem.6b01119
CHEMBL4759992 190466 0 None 1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 438 7 4 7 1.9 Cc1cc(SC[C@@H]2[C@@H](Sc3nc[nH]n3)[C@H]3[C@H](C(=O)O)[C@H]3[C@]2(N)C(=O)O)ccc1F 10.1021/acs.jmedchem.6b01119
CHEMBL4803099 190466 0 None 1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 438 7 4 7 1.9 Cc1cc(SC[C@@H]2[C@@H](Sc3nc[nH]n3)[C@H]3[C@H](C(=O)O)[C@H]3[C@]2(N)C(=O)O)ccc1F 10.1021/acs.jmedchem.6b01119
60096246 162726 0 None 40 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation countingDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation counting
ChEMBL 334 5 4 5 -0.1 COc1ccc(C(=O)N[C@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)cc1 10.1021/acs.jmedchem.7b01481
CHEMBL4061162 162726 0 None 40 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation countingDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation counting
ChEMBL 334 5 4 5 -0.1 COc1ccc(C(=O)N[C@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)cc1 10.1021/acs.jmedchem.7b01481
10198133 213287 12 None 6 2 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.
ChEMBL 203 2 3 4 -0.8 N[C@@]1(C(=O)O)CS[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm980616n
CHEMBL8839 213287 12 None 6 2 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.
ChEMBL 203 2 3 4 -0.8 N[C@@]1(C(=O)O)CS[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm980616n
10198133 213287 12 None 6 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LY341495 from human recombinant mGluR3 in RGT cellsDisplacement of [3H]LY341495 from human recombinant mGluR3 in RGT cells
ChEMBL 203 2 3 4 -0.8 N[C@@]1(C(=O)O)CS[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm060917u
CHEMBL8839 213287 12 None 6 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LY341495 from human recombinant mGluR3 in RGT cellsDisplacement of [3H]LY341495 from human recombinant mGluR3 in RGT cells
ChEMBL 203 2 3 4 -0.8 N[C@@]1(C(=O)O)CS[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm060917u
11279365 74334 0 None -1 2 Rat 8.3 pKi = 8.3 Binding
Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008
ChEMBL 343 5 3 4 1.5 N[C@@]1(C(=O)O)[C@H](OCc2ccc(Cl)cc2)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O 10.1021/jm0400294
CHEMBL189814 74334 0 None -1 2 Rat 8.3 pKi = 8.3 Binding
Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008
ChEMBL 343 5 3 4 1.5 N[C@@]1(C(=O)O)[C@H](OCc2ccc(Cl)cc2)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O 10.1021/jm0400294
9815617 121277 7 None -1 2 Rat 7.4 pKi = 7.4 Binding
Tested for binding affinity against Metabotropic glutamate receptor 3 in CHO cells using [3H]-7 as radioligandTested for binding affinity against Metabotropic glutamate receptor 3 in CHO cells using [3H]-7 as radioligand
ChEMBL 203 2 3 3 -0.4 N[C@@]1(C(=O)O)CC[C@@H]2[C@H]1[C@@]2(F)C(=O)O 10.1021/jm000346k
CHEMBL333519 121277 7 None -1 2 Rat 7.4 pKi = 7.4 Binding
Tested for binding affinity against Metabotropic glutamate receptor 3 in CHO cells using [3H]-7 as radioligandTested for binding affinity against Metabotropic glutamate receptor 3 in CHO cells using [3H]-7 as radioligand
ChEMBL 203 2 3 3 -0.4 N[C@@]1(C(=O)O)CC[C@@H]2[C@H]1[C@@]2(F)C(=O)O 10.1021/jm000346k
137656301 165461 0 None 1 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation countingDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation counting
ChEMBL 324 5 4 4 0.6 N[C@@]1(C(=O)O)C[C@H](NC(=O)CC2CCCCC2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
CHEMBL4093017 165461 0 None 1 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation countingDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation counting
ChEMBL 324 5 4 4 0.6 N[C@@]1(C(=O)O)C[C@H](NC(=O)CC2CCCCC2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
90098428 130183 0 None -5 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation countingDisplacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation counting
ChEMBL 352 4 4 6 0.4 N[C@@]1(C(=O)O)C[C@H](Sc2nnc(C(F)(F)F)[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
CHEMBL3616856 130183 0 None -5 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation countingDisplacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation counting
ChEMBL 352 4 4 6 0.4 N[C@@]1(C(=O)O)C[C@H](Sc2nnc(C(F)(F)F)[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
10353365 90022 1 None 5 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LY341495 from human recombinant mGluR3 in RGT cellsDisplacement of [3H]LY341495 from human recombinant mGluR3 in RGT cells
ChEMBL 219 2 3 4 -1.8 N[C@@]1(C(=O)O)C[S+]([O-])[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm060917u
CHEMBL218710 90022 1 None 5 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LY341495 from human recombinant mGluR3 in RGT cellsDisplacement of [3H]LY341495 from human recombinant mGluR3 in RGT cells
ChEMBL 219 2 3 4 -1.8 N[C@@]1(C(=O)O)C[S+]([O-])[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm060917u
11405687 73231 0 None -2 2 Rat 8.3 pKi = 8.3 Binding
Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008
ChEMBL 359 5 3 4 2.0 N[C@@]1(C(=O)O)[C@H](OCc2ccc3ccccc3c2)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O 10.1021/jm0400294
CHEMBL185210 73231 0 None -2 2 Rat 8.3 pKi = 8.3 Binding
Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008
ChEMBL 359 5 3 4 2.0 N[C@@]1(C(=O)O)[C@H](OCc2ccc3ccccc3c2)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O 10.1021/jm0400294
60096236 165201 0 None 38 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation countingDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation counting
ChEMBL 322 4 4 4 0.1 N[C@@]1(C(=O)O)C[C@H](NC(=O)c2ccccc2F)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
CHEMBL4090293 165201 0 None 38 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation countingDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation counting
ChEMBL 322 4 4 4 0.1 N[C@@]1(C(=O)O)C[C@H](NC(=O)c2ccccc2F)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
10197984 9199 44 None -2 5 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.
ChEMBL 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10.1021/jm980616n
1394 9199 44 None -2 5 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.
ChEMBL 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10.1021/jm980616n
CHEMBL275079 9199 44 None -2 5 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.
ChEMBL 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10.1021/jm980616n
10197984 9199 44 None -2 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LY341495 from human recombinant mGluR3 in RGT cellsDisplacement of [3H]LY341495 from human recombinant mGluR3 in RGT cells
ChEMBL 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10.1021/jm060917u
1394 9199 44 None -2 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LY341495 from human recombinant mGluR3 in RGT cellsDisplacement of [3H]LY341495 from human recombinant mGluR3 in RGT cells
ChEMBL 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10.1021/jm060917u
CHEMBL275079 9199 44 None -2 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LY341495 from human recombinant mGluR3 in RGT cellsDisplacement of [3H]LY341495 from human recombinant mGluR3 in RGT cells
ChEMBL 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10.1021/jm060917u
67633340 190500 0 None 1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 355 5 4 5 0.9 Cc1cc(SC[C@@H]2[C@@H](O)[C@@H]3[C@@H]([C@H]3C(=O)O)[C@]2(N)C(=O)O)ccc1F 10.1021/acs.jmedchem.6b01119
CHEMBL4780402 190500 0 None 1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 355 5 4 5 0.9 Cc1cc(SC[C@@H]2[C@@H](O)[C@@H]3[C@@H]([C@H]3C(=O)O)[C@]2(N)C(=O)O)ccc1F 10.1021/acs.jmedchem.6b01119
CHEMBL4803381 190500 0 None 1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 355 5 4 5 0.9 Cc1cc(SC[C@@H]2[C@@H](O)[C@@H]3[C@@H]([C@H]3C(=O)O)[C@]2(N)C(=O)O)ccc1F 10.1021/acs.jmedchem.6b01119
11344646 133554 1 None 1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-341495 binding to membranes expressing recombinant human Metabotropic glutamate receptor 3Displacement of [3H]-341495 binding to membranes expressing recombinant human Metabotropic glutamate receptor 3
ChEMBL 199 2 3 3 -0.2 C[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/jm040222y
CHEMBL365368 133554 1 None 1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-341495 binding to membranes expressing recombinant human Metabotropic glutamate receptor 3Displacement of [3H]-341495 binding to membranes expressing recombinant human Metabotropic glutamate receptor 3
ChEMBL 199 2 3 3 -0.2 C[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/jm040222y
1393 8321 64 None -2 6 Rat 7.3 pKi = 7.3 Binding
Tested for binding affinity against Metabotropic glutamate receptor 3 in CHO cells using [3H]-7 as radioligandTested for binding affinity against Metabotropic glutamate receptor 3 in CHO cells using [3H]-7 as radioligand
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm000346k
1396 8321 64 None -2 6 Rat 7.3 pKi = 7.3 Binding
Tested for binding affinity against Metabotropic glutamate receptor 3 in CHO cells using [3H]-7 as radioligandTested for binding affinity against Metabotropic glutamate receptor 3 in CHO cells using [3H]-7 as radioligand
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm000346k
213056 8321 64 None -2 6 Rat 7.3 pKi = 7.3 Binding
Tested for binding affinity against Metabotropic glutamate receptor 3 in CHO cells using [3H]-7 as radioligandTested for binding affinity against Metabotropic glutamate receptor 3 in CHO cells using [3H]-7 as radioligand
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm000346k
CHEMBL8759 8321 64 None -2 6 Rat 7.3 pKi = 7.3 Binding
Tested for binding affinity against Metabotropic glutamate receptor 3 in CHO cells using [3H]-7 as radioligandTested for binding affinity against Metabotropic glutamate receptor 3 in CHO cells using [3H]-7 as radioligand
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm000346k
71137010 130176 0 None 1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation countingDisplacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation counting
ChEMBL 352 4 4 6 0.4 N[C@@]1(C(=O)O)C[C@@H](Sc2nnc(C(F)(F)F)[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
CHEMBL3616849 130176 0 None 1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation countingDisplacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation counting
ChEMBL 352 4 4 6 0.4 N[C@@]1(C(=O)O)C[C@@H](Sc2nnc(C(F)(F)F)[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
71131322 130184 0 None -4 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation countingDisplacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation counting
ChEMBL 334 5 4 6 0.3 N[C@@]1(C(=O)O)C[C@H](Sc2nnc(C(F)F)[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
CHEMBL3616857 130184 0 None -4 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation countingDisplacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation counting
ChEMBL 334 5 4 6 0.3 N[C@@]1(C(=O)O)C[C@H](Sc2nnc(C(F)F)[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
1310 9095 110 None 1 18 Human 7.2 pKi = 7.2 Binding
Binding affinity to human mGluR3 receptor expressed in HEK cellsBinding affinity to human mGluR3 receptor expressed in HEK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1039/C1MD00186H
1369 9095 110 None 1 18 Human 7.2 pKi = 7.2 Binding
Binding affinity to human mGluR3 receptor expressed in HEK cellsBinding affinity to human mGluR3 receptor expressed in HEK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1039/C1MD00186H
33032 9095 110 None 1 18 Human 7.2 pKi = 7.2 Binding
Binding affinity to human mGluR3 receptor expressed in HEK cellsBinding affinity to human mGluR3 receptor expressed in HEK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1039/C1MD00186H
44272391 9095 110 None 1 18 Human 7.2 pKi = 7.2 Binding
Binding affinity to human mGluR3 receptor expressed in HEK cellsBinding affinity to human mGluR3 receptor expressed in HEK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1039/C1MD00186H
88747398 9095 110 None 1 18 Human 7.2 pKi = 7.2 Binding
Binding affinity to human mGluR3 receptor expressed in HEK cellsBinding affinity to human mGluR3 receptor expressed in HEK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1039/C1MD00186H
CHEMBL575060 9095 110 None 1 18 Human 7.2 pKi = 7.2 Binding
Binding affinity to human mGluR3 receptor expressed in HEK cellsBinding affinity to human mGluR3 receptor expressed in HEK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1039/C1MD00186H
DB00142 9095 110 None 1 18 Human 7.2 pKi = 7.2 Binding
Binding affinity to human mGluR3 receptor expressed in HEK cellsBinding affinity to human mGluR3 receptor expressed in HEK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1039/C1MD00186H
11310142 9200 19 None -1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-341495 binding to membranes expressing recombinant human Metabotropic glutamate receptor 3Displacement of [3H]-341495 binding to membranes expressing recombinant human Metabotropic glutamate receptor 3
ChEMBL 199 2 3 3 -0.2 C[C@@H]1C[C@@]([C@H]2[C@@H]1[C@@H]2C(=O)O)(N)C(=O)O 10.1021/jm040222y
11614 9200 19 None -1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-341495 binding to membranes expressing recombinant human Metabotropic glutamate receptor 3Displacement of [3H]-341495 binding to membranes expressing recombinant human Metabotropic glutamate receptor 3
ChEMBL 199 2 3 3 -0.2 C[C@@H]1C[C@@]([C@H]2[C@@H]1[C@@H]2C(=O)O)(N)C(=O)O 10.1021/jm040222y
CHEMBL192051 9200 19 None -1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-341495 binding to membranes expressing recombinant human Metabotropic glutamate receptor 3Displacement of [3H]-341495 binding to membranes expressing recombinant human Metabotropic glutamate receptor 3
ChEMBL 199 2 3 3 -0.2 C[C@@H]1C[C@@]([C@H]2[C@@H]1[C@@H]2C(=O)O)(N)C(=O)O 10.1021/jm040222y
71137012 130178 0 None 1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation countingDisplacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation counting
ChEMBL 299 4 5 7 -1.0 Nc1nnc(S[C@@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)[nH]1 10.1021/acs.jmedchem.5b01124
CHEMBL3616851 130178 0 None 1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation countingDisplacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation counting
ChEMBL 299 4 5 7 -1.0 Nc1nnc(S[C@@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)[nH]1 10.1021/acs.jmedchem.5b01124
11220424 165740 0 None 43 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation countingDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation counting
ChEMBL 304 4 4 4 -0.1 N[C@@]1(C(=O)O)C[C@H](NC(=O)c2ccccc2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
CHEMBL4095995 165740 0 None 43 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation countingDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation counting
ChEMBL 304 4 4 4 -0.1 N[C@@]1(C(=O)O)C[C@H](NC(=O)c2ccccc2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
67637138 190397 0 None 1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 341 5 4 5 0.6 N[C@@]1(C(=O)O)[C@H](CSc2ccc(F)cc2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
CHEMBL4776989 190397 0 None 1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 341 5 4 5 0.6 N[C@@]1(C(=O)O)[C@H](CSc2ccc(F)cc2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
CHEMBL4802329 190397 0 None 1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 341 5 4 5 0.6 N[C@@]1(C(=O)O)[C@H](CSc2ccc(F)cc2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
162652146 186992 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 289 5 4 5 -0.2 CC(C)SC[C@@H]1[C@@H](O)[C@@H]2[C@@H]([C@H]2C(=O)O)[C@]1(N)C(=O)O 10.1021/acs.jmedchem.6b01119
CHEMBL4749728 186992 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 289 5 4 5 -0.2 CC(C)SC[C@@H]1[C@@H](O)[C@@H]2[C@@H]([C@H]2C(=O)O)[C@]1(N)C(=O)O 10.1021/acs.jmedchem.6b01119
71135411 130175 0 None 1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation countingDisplacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation counting
ChEMBL 298 4 4 6 -0.3 Cc1nnc(S[C@@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)[nH]1 10.1021/acs.jmedchem.5b01124
CHEMBL3616848 130175 0 None 1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation countingDisplacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation counting
ChEMBL 298 4 4 6 -0.3 Cc1nnc(S[C@@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)[nH]1 10.1021/acs.jmedchem.5b01124
71137034 130177 0 None 1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation countingDisplacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation counting
ChEMBL 334 5 4 6 0.3 N[C@@]1(C(=O)O)C[C@@H](Sc2nnc(C(F)F)[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
CHEMBL3616850 130177 0 None 1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation countingDisplacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation counting
ChEMBL 334 5 4 6 0.3 N[C@@]1(C(=O)O)C[C@@H](Sc2nnc(C(F)F)[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
71476419 130187 0 None 1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation countingDisplacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation counting
ChEMBL 284 4 4 6 -0.6 N[C@@]1(C(=O)O)C[C@H](Sc2c[nH]nn2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
CHEMBL3616860 130187 0 None 1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation countingDisplacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation counting
ChEMBL 284 4 4 6 -0.6 N[C@@]1(C(=O)O)C[C@H](Sc2c[nH]nn2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
9815616 121578 6 None -1 2 Rat 7.2 pKi = 7.2 Binding
Tested for binding affinity against Metabotropic glutamate receptor 3 in CHO cells using [3H]-7 as radioligandTested for binding affinity against Metabotropic glutamate receptor 3 in CHO cells using [3H]-7 as radioligand
ChEMBL 203 2 3 3 -0.5 N[C@@]1(C(=O)O)[C@@H](F)C[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm000346k
CHEMBL334014 121578 6 None -1 2 Rat 7.2 pKi = 7.2 Binding
Tested for binding affinity against Metabotropic glutamate receptor 3 in CHO cells using [3H]-7 as radioligandTested for binding affinity against Metabotropic glutamate receptor 3 in CHO cells using [3H]-7 as radioligand
ChEMBL 203 2 3 3 -0.5 N[C@@]1(C(=O)O)[C@@H](F)C[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm000346k
10130658 73527 0 None -2 2 Rat 7.2 pKi = 7.2 Binding
Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008
ChEMBL 219 2 4 4 -1.4 N[C@@]1(C(=O)O)[C@H](O)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O 10.1021/jm0400294
CHEMBL185822 73527 0 None -2 2 Rat 7.2 pKi = 7.2 Binding
Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008
ChEMBL 219 2 4 4 -1.4 N[C@@]1(C(=O)O)[C@H](O)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O 10.1021/jm0400294
71137011 130185 0 None -2 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation countingDisplacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation counting
ChEMBL 299 4 5 7 -1.0 Nc1nnc(S[C@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)[nH]1 10.1021/acs.jmedchem.5b01124
CHEMBL3616858 130185 0 None -2 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation countingDisplacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation counting
ChEMBL 299 4 5 7 -1.0 Nc1nnc(S[C@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)[nH]1 10.1021/acs.jmedchem.5b01124
69669820 190419 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 396 6 4 5 1.1 CC(=O)N[C@H]1[C@H]2[C@H](C(=O)O)[C@H]2[C@](N)(C(=O)O)[C@@H]1CSc1ccc(F)c(C)c1 10.1021/acs.jmedchem.6b01119
CHEMBL4746125 190419 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 396 6 4 5 1.1 CC(=O)N[C@H]1[C@H]2[C@H](C(=O)O)[C@H]2[C@](N)(C(=O)O)[C@@H]1CSc1ccc(F)c(C)c1 10.1021/acs.jmedchem.6b01119
CHEMBL4802570 190419 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 396 6 4 5 1.1 CC(=O)N[C@H]1[C@H]2[C@H](C(=O)O)[C@H]2[C@](N)(C(=O)O)[C@@H]1CSc1ccc(F)c(C)c1 10.1021/acs.jmedchem.6b01119
137635882 162673 0 None 1 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation countingDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation counting
ChEMBL 310 4 4 4 0.2 N[C@@]1(C(=O)O)C[C@H](NC(=O)C2CCCCC2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
CHEMBL4060567 162673 0 None 1 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation countingDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation counting
ChEMBL 310 4 4 4 0.2 N[C@@]1(C(=O)O)C[C@H](NC(=O)C2CCCCC2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
71137008 130182 0 None 2 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation countingDisplacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation counting
ChEMBL 298 4 4 6 -0.3 Cc1nnc(S[C@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)[nH]1 10.1021/acs.jmedchem.5b01124
CHEMBL3616855 130182 0 None 2 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation countingDisplacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation counting
ChEMBL 298 4 4 6 -0.3 Cc1nnc(S[C@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)[nH]1 10.1021/acs.jmedchem.5b01124
71136654 130186 0 None 4 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation countingDisplacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation counting
ChEMBL 326 5 4 6 0.5 CC(C)c1nnc(S[C@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)[nH]1 10.1021/acs.jmedchem.5b01124
CHEMBL3616859 130186 0 None 4 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation countingDisplacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation counting
ChEMBL 326 5 4 6 0.5 CC(C)c1nnc(S[C@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)[nH]1 10.1021/acs.jmedchem.5b01124
10192719 72888 0 None -2 2 Rat 7.1 pKi = 7.1 Binding
Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008
ChEMBL 233 3 3 4 -0.8 CO[C@@H]1C[C@@H]2[C@H]([C@]1(N)C(=O)O)[C@@]2(F)C(=O)O 10.1021/jm0400294
CHEMBL183956 72888 0 None -2 2 Rat 7.1 pKi = 7.1 Binding
Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008
ChEMBL 233 3 3 4 -0.8 CO[C@@H]1C[C@@H]2[C@H]([C@]1(N)C(=O)O)[C@@]2(F)C(=O)O 10.1021/jm0400294
60096228 163566 0 None 5 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation countingDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation counting
ChEMBL 320 4 5 5 -0.4 N[C@@]1(C(=O)O)C[C@H](NC(=O)c2ccc(O)cc2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
CHEMBL4070866 163566 0 None 5 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation countingDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation counting
ChEMBL 320 4 5 5 -0.4 N[C@@]1(C(=O)O)C[C@H](NC(=O)c2ccc(O)cc2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.7b01481
10198133 213287 12 None 6 2 Human 8.0 pKi = 8.0 Binding
Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.
ChEMBL 203 2 3 4 -0.8 N[C@@]1(C(=O)O)CS[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm980616n
CHEMBL8839 213287 12 None 6 2 Human 8.0 pKi = 8.0 Binding
Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.
ChEMBL 203 2 3 4 -0.8 N[C@@]1(C(=O)O)CS[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm980616n
67633284 190426 0 None -1 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 391 5 4 5 1.8 N[C@@]1(C(=O)O)[C@H](CSc2ccc(Cl)c(Cl)c2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
CHEMBL4748699 190426 0 None -1 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 391 5 4 5 1.8 N[C@@]1(C(=O)O)[C@H](CSc2ccc(Cl)c(Cl)c2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
CHEMBL4802655 190426 0 None -1 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation methodDisplacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
ChEMBL 391 5 4 5 1.8 N[C@@]1(C(=O)O)[C@H](CSc2ccc(Cl)c(Cl)c2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
9834591 144378 69 None 1 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LY341495 from human recombinant mGluR3 in RGT cellsDisplacement of [3H]LY341495 from human recombinant mGluR3 in RGT cells
ChEMBL 235 2 3 5 -2.1 N[C@@]1(C(=O)O)CS(=O)(=O)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm060917u
CHEMBL375611 144378 69 None 1 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LY341495 from human recombinant mGluR3 in RGT cellsDisplacement of [3H]LY341495 from human recombinant mGluR3 in RGT cells
ChEMBL 235 2 3 5 -2.1 N[C@@]1(C(=O)O)CS(=O)(=O)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm060917u
1393 8321 64 None -1 6 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-341495 binding to membranes expressing recombinant human Metabotropic glutamate receptor 3Displacement of [3H]-341495 binding to membranes expressing recombinant human Metabotropic glutamate receptor 3
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm040222y
1396 8321 64 None -1 6 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-341495 binding to membranes expressing recombinant human Metabotropic glutamate receptor 3Displacement of [3H]-341495 binding to membranes expressing recombinant human Metabotropic glutamate receptor 3
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm040222y
213056 8321 64 None -1 6 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-341495 binding to membranes expressing recombinant human Metabotropic glutamate receptor 3Displacement of [3H]-341495 binding to membranes expressing recombinant human Metabotropic glutamate receptor 3
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm040222y
CHEMBL8759 8321 64 None -1 6 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-341495 binding to membranes expressing recombinant human Metabotropic glutamate receptor 3Displacement of [3H]-341495 binding to membranes expressing recombinant human Metabotropic glutamate receptor 3
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm040222y
1393 8321 64 None -1 6 Human 7.0 pKi = 7.0 Binding
Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm980616n
1396 8321 64 None -1 6 Human 7.0 pKi = 7.0 Binding
Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm980616n
213056 8321 64 None -1 6 Human 7.0 pKi = 7.0 Binding
Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm980616n
CHEMBL8759 8321 64 None -1 6 Human 7.0 pKi = 7.0 Binding
Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm980616n
1393 8321 64 None -1 6 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LY341495 from human recombinant mGluR3 in RGT cellsDisplacement of [3H]LY341495 from human recombinant mGluR3 in RGT cells
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm060917u
1396 8321 64 None -1 6 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LY341495 from human recombinant mGluR3 in RGT cellsDisplacement of [3H]LY341495 from human recombinant mGluR3 in RGT cells
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm060917u
213056 8321 64 None -1 6 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LY341495 from human recombinant mGluR3 in RGT cellsDisplacement of [3H]LY341495 from human recombinant mGluR3 in RGT cells
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm060917u
CHEMBL8759 8321 64 None -1 6 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LY341495 from human recombinant mGluR3 in RGT cellsDisplacement of [3H]LY341495 from human recombinant mGluR3 in RGT cells
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm060917u
1378 9195 54 None -5 10 Rat 7.3 pKd None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10884552
1399 9195 54 None -5 10 Rat 7.3 pKd None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10884552
9819927 9195 54 None -5 10 Rat 7.3 pKd None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10884552
CHEMBL432038 9195 54 None -5 10 Rat 7.3 pKd None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10884552
1378 9195 54 None 1 10 Human 9.1 pKd None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10530814
1399 9195 54 None 1 10 Human 9.1 pKd None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10530814
9819927 9195 54 None 1 10 Human 9.1 pKd None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10530814
CHEMBL432038 9195 54 None 1 10 Human 9.1 pKd None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10530814
12310764 8751 64 Functional -14 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 158 2 3 4 -0.9 OC(=O)C(c1o[nH]c(=O)c1)N None
1233 8751 64 Functional -14 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 158 2 3 4 -0.9 OC(=O)C(c1o[nH]c(=O)c1)N None
1371 8751 64 Functional -14 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 158 2 3 4 -0.9 OC(=O)C(c1o[nH]c(=O)c1)N None
CHEMBL284895 8751 64 Functional -14 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 158 2 3 4 -0.9 OC(=O)C(c1o[nH]c(=O)c1)N None
1370 10037 67 Functional -1202 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N None
1372 10037 67 Functional -1202 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N None
40539 10037 67 Functional -1202 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N None
6971145 10037 67 Functional -1202 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N None
CHEMBL279956 10037 67 Functional -1202 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N None
DB02999 10037 67 Functional -1202 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N None
139054390 211702 106 Functional -1 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 N[C@H](CCC(=O)O)C(=O)O None
23327 211702 106 Functional -1 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 N[C@H](CCC(=O)O)C(=O)O None
CHEMBL76232 211702 106 Functional -1 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 N[C@H](CCC(=O)O)C(=O)O None
114827 223111 0 3H-LY341495 -4 3 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 185 2 3 3 -0.5 C1CC(C2C1C2C(=O)O)(C(=O)O)N None
None 223113 0 Functional -3 3 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 203 4 4 4 -1.6 C1(C(C1C(=O)O)C(=O)O)C(C(=O)O)N None
210320 224512 0 None - 1 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 304 9 5 5 -1.6 CC(=O)N[C@@H](CC(=O)N[C@@H](CCC(O)=O)C(O)=O)C(O)=O None
1310 9095 110 Functional 1 18 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
1369 9095 110 Functional 1 18 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
33032 9095 110 Functional 1 18 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
44272391 9095 110 Functional 1 18 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
88747398 9095 110 Functional 1 18 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
CHEMBL575060 9095 110 Functional 1 18 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
DB00142 9095 110 Functional 1 18 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
1310 9095 110 None 1 18 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
1369 9095 110 None 1 18 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
33032 9095 110 None 1 18 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
44272391 9095 110 None 1 18 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
88747398 9095 110 None 1 18 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
CHEMBL575060 9095 110 None 1 18 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
DB00142 9095 110 None 1 18 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
None 222951 0 Functional -1 7 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 173 2 3 3 -0.3 C1CC(CC1C(=O)O)(C(=O)O)N None
1405 9486 0 None - 1 Human 4.7 pKi = 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 304 9 5 5 -1.6 OC(=O)CC[C@@H](C(=O)O)NC(=O)[C@@H](NC(=O)C)CC(=O)O 10884552
188803 9486 0 None - 1 Human 4.7 pKi = 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 304 9 5 5 -1.6 OC(=O)CC[C@@H](C(=O)O)NC(=O)[C@@H](NC(=O)C)CC(=O)O 10884552
CHEMBL1329032 9486 0 None - 1 Human 4.7 pKi = 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 304 9 5 5 -1.6 OC(=O)CC[C@@H](C(=O)O)NC(=O)[C@@H](NC(=O)C)CC(=O)O 10884552
11310142 9200 19 None -1 2 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 199 2 3 3 -0.2 C[C@@H]1C[C@@]([C@H]2[C@@H]1[C@@H]2C(=O)O)(N)C(=O)O 26341392
11614 9200 19 None -1 2 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 199 2 3 3 -0.2 C[C@@H]1C[C@@]([C@H]2[C@@H]1[C@@H]2C(=O)O)(N)C(=O)O 26341392
CHEMBL192051 9200 19 None -1 2 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 199 2 3 3 -0.2 C[C@@H]1C[C@@]([C@H]2[C@@H]1[C@@H]2C(=O)O)(N)C(=O)O 26341392
1373 9253 51 None -6 5 Human 3.8 pKi None 3.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 209 3 3 3 0.6 OC(=O)c1ccc(cc1)[C@@](C(=O)O)(N)C 10530814
139055582 9253 51 None -6 5 Human 3.8 pKi None 3.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 209 3 3 3 0.6 OC(=O)c1ccc(cc1)[C@@](C(=O)O)(N)C 10530814
446355 9253 51 None -6 5 Human 3.8 pKi None 3.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 209 3 3 3 0.6 OC(=O)c1ccc(cc1)[C@@](C(=O)O)(N)C 10530814
CHEMBL257626 9253 51 None -6 5 Human 3.8 pKi None 3.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 209 3 3 3 0.6 OC(=O)c1ccc(cc1)[C@@](C(=O)O)(N)C 10530814
DB04256 9253 51 None -6 5 Human 3.8 pKi None 3.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 209 3 3 3 0.6 OC(=O)c1ccc(cc1)[C@@](C(=O)O)(N)C 10530814
104766 6822 42 None -12 11 Human 4.7 pKi None 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10530814
1365 6822 42 None -12 11 Human 4.7 pKi None 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10530814
CHEMBL34453 6822 42 None -12 11 Human 4.7 pKi None 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10530814
104766 6822 42 None -10 11 Rat 4.8 pKi None 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10884552
1365 6822 42 None -10 11 Rat 4.8 pKi None 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10884552
CHEMBL34453 6822 42 None -10 11 Rat 4.8 pKi None 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10884552
10197984 9199 44 None -2 5 Human 4.8 pKi None 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10090786
1394 9199 44 None -2 5 Human 4.8 pKi None 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10090786
CHEMBL275079 9199 44 None -2 5 Human 4.8 pKi None 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10090786
1392 6861 48 None 1 2 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 174 2 4 4 -1.8 OC(=O)[C@@H]1NC[C@@](C1)(N)C(=O)O 10530814
5310984 6861 48 None 1 2 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 174 2 4 4 -1.8 OC(=O)[C@@H]1NC[C@@](C1)(N)C(=O)O 10530814
CHEMBL40086 6861 48 None 1 2 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 174 2 4 4 -1.8 OC(=O)[C@@H]1NC[C@@](C1)(N)C(=O)O 10530814
1400 8320 0 None 7 2 Rat 5.4 pKi None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 175 5 3 3 0.0 CC[C@@](C(=O)O)(CCC(=O)O)N 10884552
5311079 8320 0 None 7 2 Rat 5.4 pKi None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 175 5 3 3 0.0 CC[C@@](C(=O)O)(CCC(=O)O)N 10884552
CHEMBL1450466 8320 0 None 7 2 Rat 5.4 pKi None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 175 5 3 3 0.0 CC[C@@](C(=O)O)(CCC(=O)O)N 10884552
1310 9095 110 None -1 18 Rat 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10884552
1369 9095 110 None -1 18 Rat 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10884552
33032 9095 110 None -1 18 Rat 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10884552
44272391 9095 110 None -1 18 Rat 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10884552
88747398 9095 110 None -1 18 Rat 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10884552
CHEMBL575060 9095 110 None -1 18 Rat 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10884552
DB00142 9095 110 None -1 18 Rat 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10884552
1368 9070 37 None -2 11 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 10884552
5310956 9070 37 None -2 11 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 10884552
CHEMBL280563 9070 37 None -2 11 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 10884552
1377 8122 26 None -2 6 Rat 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 4 4 4 -1.6 N[C@@H](C1[C@H]([C@@H]1C(=O)O)C(=O)O)C(=O)O 10884552
5310979 8122 26 None -2 6 Rat 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 4 4 4 -1.6 N[C@@H](C1[C@H]([C@@H]1C(=O)O)C(=O)O)C(=O)O 10884552
CHEMBL284193 8122 26 None -2 6 Rat 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 4 4 4 -1.6 N[C@@H](C1[C@H]([C@@H]1C(=O)O)C(=O)O)C(=O)O 10884552
1377 8122 26 None 1 6 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 4 4 4 -1.6 N[C@@H](C1[C@H]([C@@H]1C(=O)O)C(=O)O)C(=O)O 10530814
5310979 8122 26 None 1 6 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 4 4 4 -1.6 N[C@@H](C1[C@H]([C@@H]1C(=O)O)C(=O)O)C(=O)O 10530814
CHEMBL284193 8122 26 None 1 6 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 4 4 4 -1.6 N[C@@H](C1[C@H]([C@@H]1C(=O)O)C(=O)O)C(=O)O 10530814
1393 8321 64 None -2 6 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10884552
1396 8321 64 None -2 6 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10884552
213056 8321 64 None -2 6 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10884552
CHEMBL8759 8321 64 None -2 6 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10884552
1368 9070 37 None -1 11 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 10530814
5310956 9070 37 None -1 11 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 10530814
CHEMBL280563 9070 37 None -1 11 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 10530814
1310 9095 110 None 1 18 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10530814
1369 9095 110 None 1 18 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10530814
33032 9095 110 None 1 18 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10530814
44272391 9095 110 None 1 18 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10530814
88747398 9095 110 None 1 18 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10530814
CHEMBL575060 9095 110 None 1 18 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10530814
DB00142 9095 110 None 1 18 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10530814
1378 9195 54 None -5 10 Rat 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10884552
1399 9195 54 None -5 10 Rat 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10884552
9819927 9195 54 None -5 10 Rat 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10884552
CHEMBL432038 9195 54 None -5 10 Rat 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10884552
1397 9307 15 None -2 5 Rat 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 377 5 3 4 2.1 OC(=O)[C@]1(N)[C@H](OCc2ccc(c(c2)Cl)Cl)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O 14975669
1397 9307 15 None -2 5 Rat 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 377 5 3 4 2.1 OC(=O)[C@]1(N)[C@H](OCc2ccc(c(c2)Cl)Cl)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O 15317467
9886034 9307 15 None -2 5 Rat 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 377 5 3 4 2.1 OC(=O)[C@]1(N)[C@H](OCc2ccc(c(c2)Cl)Cl)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O 14975669
9886034 9307 15 None -2 5 Rat 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 377 5 3 4 2.1 OC(=O)[C@]1(N)[C@H](OCc2ccc(c(c2)Cl)Cl)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O 15317467
CHEMBL186453 9307 15 None -2 5 Rat 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 377 5 3 4 2.1 OC(=O)[C@]1(N)[C@H](OCc2ccc(c(c2)Cl)Cl)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O 14975669
CHEMBL186453 9307 15 None -2 5 Rat 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 377 5 3 4 2.1 OC(=O)[C@]1(N)[C@H](OCc2ccc(c(c2)Cl)Cl)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O 15317467
1393 8321 64 None -1 6 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10530814
1396 8321 64 None -1 6 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10530814
213056 8321 64 None -1 6 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10530814
CHEMBL8759 8321 64 None -1 6 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10530814
1378 9195 54 None 1 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10530814
1399 9195 54 None 1 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10530814
9819927 9195 54 None 1 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10530814
CHEMBL432038 9195 54 None 1 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10530814