Ligand source activities (1 row/activity)
| Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
| 60096224 | 156636 | None | 0 | Human | Functional | pEC50 | = | 9.8 | 9.8 | 43 | 2 | 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 | 156636 | None | 0 | Human | Functional | pEC50 | = | 9.8 | 9.8 | 43 | 2 | 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 | 157747 | None | 19 | Human | Functional | pEC50 | = | 9.3 | 9.3 | 48 | 4 | 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 | 157747 | None | 19 | Human | Functional | pEC50 | = | 9.3 | 9.3 | 48 | 4 | 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 | 158660 | None | 0 | Human | Functional | pEC50 | = | 9.2 | 9.2 | 5 | 2 | 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 | 158660 | None | 0 | Human | Functional | pEC50 | = | 9.2 | 9.2 | 5 | 2 | 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 | 156973 | None | 0 | Human | Functional | pEC50 | = | 9.1 | 9.1 | 10 | 2 | 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 | 156973 | None | 0 | Human | Functional | pEC50 | = | 9.1 | 9.1 | 10 | 2 | 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 | 83279 | None | 1 | Human | Functional | pEC50 | = | 8.9 | 8.9 | -13 | 3 | 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 | 83279 | None | 1 | Human | Functional | pEC50 | = | 8.9 | 8.9 | -13 | 3 | 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 | 35826 | None | 1 | Rat | Functional | pEC50 | = | 7 | 7.0 | -6 | 4 | 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 | 35826 | None | 1 | Rat | Functional | pEC50 | = | 7 | 7.0 | -6 | 4 | 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 | 2315 | None | 61 | Human | Functional | pEC50 | = | 6 | 6.0 | -251 | 17 | 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 | 2315 | None | 61 | Human | Functional | pEC50 | = | 6 | 6.0 | -251 | 17 | 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 | 2315 | None | 61 | Human | Functional | pEC50 | = | 6 | 6.0 | -251 | 17 | 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 | 2315 | None | 61 | Human | Functional | pEC50 | = | 6 | 6.0 | -251 | 17 | 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 | 2315 | None | 61 | Human | Functional | pEC50 | = | 6 | 6.0 | -251 | 17 | 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 | 2315 | None | 61 | Human | Functional | pEC50 | = | 6 | 6.0 | -251 | 17 | 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 | 2315 | None | 61 | Human | Functional | pEC50 | = | 6 | 6.0 | -251 | 17 | 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 | 123464 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | -5 | 2 | 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 | 123464 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | -5 | 2 | 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 | 1110 | None | 0 | Human | Functional | pEC50 | = | 5.0 | 5.0 | -10 | 2 | 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 | 1110 | None | 0 | Human | Functional | pEC50 | = | 5.0 | 5.0 | -10 | 2 | 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 | 1110 | None | 0 | Human | Functional | pEC50 | = | 5.0 | 5.0 | -10 | 2 | 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 | 123464 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | -5 | 2 | 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 | 123464 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | -5 | 2 | 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 | 31349 | None | 0 | Rat | Functional | pEC50 | = | 8.0 | 8.0 | -1 | 5 | 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 | 31349 | None | 0 | Rat | Functional | pEC50 | = | 8.0 | 8.0 | -1 | 5 | 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 | 157747 | None | 19 | Human | Functional | pEC50 | = | 7.9 | 7.9 | 48 | 4 | 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 | 157747 | None | 19 | Human | Functional | pEC50 | = | 7.9 | 7.9 | 48 | 4 | 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 | 123474 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | -58 | 2 | 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 | 123474 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | -58 | 2 | 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 | 123463 | None | 21 | Human | Functional | pEC50 | = | 5.9 | 5.9 | -107 | 4 | 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 | 123463 | None | 21 | Human | Functional | pEC50 | = | 5.9 | 5.9 | -107 | 4 | 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 | 123463 | None | 21 | Human | Functional | pEC50 | = | 6.9 | 6.9 | -107 | 4 | 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 | 123463 | None | 21 | Human | Functional | pEC50 | = | 6.9 | 6.9 | -107 | 4 | 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 | 1061 | None | 0 | Human | Functional | pEC50 | = | 4.9 | 4.9 | -16 | 2 | 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 | 1061 | None | 0 | Human | Functional | pEC50 | = | 4.9 | 4.9 | -16 | 2 | 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 | 1061 | None | 0 | Human | Functional | pEC50 | = | 4.9 | 4.9 | -16 | 2 | 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 | 1539 | None | 42 | Human | Functional | pEC50 | = | 6.9 | 6.9 | -4 | 6 | 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 | 1539 | None | 42 | Human | Functional | pEC50 | = | 6.9 | 6.9 | -4 | 6 | 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 | 1539 | None | 42 | Human | Functional | pEC50 | = | 6.9 | 6.9 | -4 | 6 | 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 | 1539 | None | 42 | Human | Functional | pEC50 | = | 6.9 | 6.9 | -4 | 6 | 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 | 2315 | None | 61 | Human | Functional | pEC50 | = | 5.8 | 5.8 | -251 | 17 | 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 | 2315 | None | 61 | Human | Functional | pEC50 | = | 5.8 | 5.8 | -251 | 17 | 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 | 2315 | None | 61 | Human | Functional | pEC50 | = | 5.8 | 5.8 | -251 | 17 | 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 | 2315 | None | 61 | Human | Functional | pEC50 | = | 5.8 | 5.8 | -251 | 17 | 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 | 2315 | None | 61 | Human | Functional | pEC50 | = | 5.8 | 5.8 | -251 | 17 | 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 | 2315 | None | 61 | Human | Functional | pEC50 | = | 5.8 | 5.8 | -251 | 17 | 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 | 2315 | None | 61 | Human | Functional | pEC50 | = | 5.8 | 5.8 | -251 | 17 | 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 | ||
Showing 1 to 50 of 1,086 entries
| Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
| 9794208 | 90084 | None | 2 | Human | Binding | pEC50 | = | 10.0 | 10.0 | - | 0 | 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 | 90084 | None | 2 | Human | Binding | pEC50 | = | 10.0 | 10.0 | - | 0 | 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 | 90096 | None | 0 | Human | Binding | pEC50 | = | 9.6 | 9.6 | - | 0 | 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 | 90096 | None | 0 | Human | Binding | pEC50 | = | 9.6 | 9.6 | - | 0 | 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 | 90096 | None | 0 | Human | Binding | pEC50 | = | 9.6 | 9.6 | - | 0 | 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 | 102256 | None | 18 | Rat | Binding | pEC50 | = | 5 | 5.0 | - | 0 | 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 | 102256 | None | 18 | Rat | Binding | pEC50 | = | 5 | 5.0 | - | 0 | 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 | 102256 | None | 18 | Rat | Binding | pEC50 | = | 5 | 5.0 | - | 0 | 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 | 111936 | None | 0 | Rat | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | 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 | 111936 | None | 0 | Rat | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | 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 | 184681 | None | 0 | Rat | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | 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 | 184681 | None | 0 | Rat | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | 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 | 186306 | None | 0 | Rat | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | 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 | 186306 | None | 0 | Rat | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | 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 | 185638 | None | 0 | Rat | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | 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 | 185638 | None | 0 | Rat | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | 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 | 185979 | None | 0 | Rat | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | 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 | 185979 | None | 0 | Rat | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | 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 | 185635 | None | 0 | Rat | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | 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 | 185635 | None | 0 | Rat | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | 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 | 111931 | None | 0 | Rat | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | 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 | 111931 | None | 0 | Rat | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | 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 | 184860 | None | 0 | Rat | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | 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 | 184860 | None | 0 | Rat | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | 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 | 90088 | None | 0 | Human | Binding | pEC50 | = | 7.9 | 7.9 | - | 0 | 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 | 90088 | None | 0 | Human | Binding | pEC50 | = | 7.9 | 7.9 | - | 0 | 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 | 186487 | None | 0 | Rat | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | 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 | 186487 | None | 0 | Rat | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | 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 | 185236 | None | 0 | Rat | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | 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 | 185236 | None | 0 | Rat | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | 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 | 184547 | None | 0 | Rat | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | 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 | 184547 | None | 0 | Rat | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | 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 | 184685 | None | 0 | Rat | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | 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 | 184685 | None | 0 | Rat | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | 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 | 185220 | None | 0 | Rat | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | 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 | 185220 | None | 0 | Rat | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | 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 | 90086 | None | 1 | Human | Binding | pEC50 | = | 7.9 | 7.9 | - | 1 | 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 | 90086 | None | 1 | Human | Binding | pEC50 | = | 7.9 | 7.9 | - | 1 | 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 | 111927 | None | 0 | Rat | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | 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 | 111927 | None | 0 | Rat | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | 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 | 111912 | None | 0 | Rat | Binding | pEC50 | = | 5.8 | 5.8 | - | 0 | 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 | 111912 | None | 0 | Rat | Binding | pEC50 | = | 5.8 | 5.8 | - | 0 | 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 | 184722 | None | 0 | Rat | Binding | pEC50 | = | 5.8 | 5.8 | - | 0 | 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 | 184722 | None | 0 | Rat | Binding | pEC50 | = | 5.8 | 5.8 | - | 0 | 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 | 90085 | None | 1 | Human | Binding | pEC50 | = | 7.8 | 7.8 | - | 0 | 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 | 90085 | None | 1 | Human | Binding | pEC50 | = | 7.8 | 7.8 | - | 0 | 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 | 111957 | None | 0 | Rat | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | 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 | 111957 | None | 0 | Rat | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | 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 | 185550 | None | 0 | Rat | Binding | pEC50 | = | 5.8 | 5.8 | - | 0 | 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 | 185550 | None | 0 | Rat | Binding | pEC50 | = | 5.8 | 5.8 | - | 0 | 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 | ||
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