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
| |
| 127047647 | 139846 | None | 0 | Human | Functional | pEC50 | = | 10.2 | 10.2 | 22 | 2 | Positive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assay |
ChEMBL | 369 | 5 | 2 | 6 | 3.7 | CCc1cnc(Oc2ccc(NC(=O)c3ncccc3N)cc2Cl)nc1 | 10.1016/j.bmcl.2016.04.041 | ||
| CHEMBL3798517 | 139846 | None | 0 | Human | Functional | pEC50 | = | 10.2 | 10.2 | 22 | 2 | Positive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assay |
ChEMBL | 369 | 5 | 2 | 6 | 3.7 | CCc1cnc(Oc2ccc(NC(=O)c3ncccc3N)cc2Cl)nc1 | 10.1016/j.bmcl.2016.04.041 | ||
| 127046557 | 139814 | None | 3 | Human | Functional | pEC50 | = | 10.0 | 10.0 | 42 | 2 | Positive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assay |
ChEMBL | 392 | 3 | 2 | 5 | 3.4 | Nc1cccnc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1 | 10.1016/j.bmcl.2016.04.041 | ||
| CHEMBL3798234 | 139814 | None | 3 | Human | Functional | pEC50 | = | 10.0 | 10.0 | 42 | 2 | Positive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assay |
ChEMBL | 392 | 3 | 2 | 5 | 3.4 | Nc1cccnc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1 | 10.1016/j.bmcl.2016.04.041 | ||
| 127046775 | 139804 | None | 0 | Human | Functional | pEC50 | = | 9.6 | 9.6 | - | 1 | Positive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assay |
ChEMBL | 378 | 3 | 2 | 4 | 3.7 | Nc1cccnc1C(=O)Nc1ccc(N2Cc3ccccc3C2=O)c(Cl)c1 | 10.1016/j.bmcl.2016.04.041 | ||
| CHEMBL3798197 | 139804 | None | 0 | Human | Functional | pEC50 | = | 9.6 | 9.6 | - | 1 | Positive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assay |
ChEMBL | 378 | 3 | 2 | 4 | 3.7 | Nc1cccnc1C(=O)Nc1ccc(N2Cc3ccccc3C2=O)c(Cl)c1 | 10.1016/j.bmcl.2016.04.041 | ||
| 127048133 | 139689 | None | 0 | Human | Functional | pEC50 | = | 9.5 | 9.5 | - | 1 | Positive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assay |
ChEMBL | 408 | 4 | 2 | 5 | 3.7 | COc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3ncccc3N)cc1Cl)C2 | 10.1016/j.bmcl.2016.04.041 | ||
| CHEMBL3797445 | 139689 | None | 0 | Human | Functional | pEC50 | = | 9.5 | 9.5 | - | 1 | Positive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assay |
ChEMBL | 408 | 4 | 2 | 5 | 3.7 | COc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3ncccc3N)cc1Cl)C2 | 10.1016/j.bmcl.2016.04.041 | ||
| 127046558 | 139955 | None | 0 | Human | Functional | pEC50 | = | 9.2 | 9.2 | - | 1 | Positive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assay |
ChEMBL | 406 | 3 | 2 | 5 | 3.7 | Cc1cccc2c1C(=O)N(c1ccc(NC(=O)c3ncccc3N)cc1Cl)C2=O | 10.1016/j.bmcl.2016.04.041 | ||
| CHEMBL3799261 | 139955 | None | 0 | Human | Functional | pEC50 | = | 9.2 | 9.2 | - | 1 | Positive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assay |
ChEMBL | 406 | 3 | 2 | 5 | 3.7 | Cc1cccc2c1C(=O)N(c1ccc(NC(=O)c3ncccc3N)cc1Cl)C2=O | 10.1016/j.bmcl.2016.04.041 | ||
| 127047061 | 139762 | None | 0 | Human | Functional | pEC50 | = | 9.1 | 9.1 | - | 1 | Positive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assay |
ChEMBL | 420 | 5 | 2 | 4 | 4.2 | Nc1cccnc1C(=O)Nc1ccc(N2CC(Cc3ccccc3)CC2=O)c(Cl)c1 | 10.1016/j.bmcl.2016.04.041 | ||
| CHEMBL3797923 | 139762 | None | 0 | Human | Functional | pEC50 | = | 9.1 | 9.1 | - | 1 | Positive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assay |
ChEMBL | 420 | 5 | 2 | 4 | 4.2 | Nc1cccnc1C(=O)Nc1ccc(N2CC(Cc3ccccc3)CC2=O)c(Cl)c1 | 10.1016/j.bmcl.2016.04.041 | ||
| 127047065 | 139695 | None | 0 | Human | Functional | pEC50 | = | 9.0 | 9.0 | - | 1 | Positive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assay |
ChEMBL | 392 | 3 | 2 | 4 | 3.8 | Nc1cccnc1C(=O)Nc1ccc(N2CCc3ccccc3C2=O)c(Cl)c1 | 10.1016/j.bmcl.2016.04.041 | ||
| CHEMBL3797463 | 139695 | None | 0 | Human | Functional | pEC50 | = | 9.0 | 9.0 | - | 1 | Positive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assay |
ChEMBL | 392 | 3 | 2 | 4 | 3.8 | Nc1cccnc1C(=O)Nc1ccc(N2CCc3ccccc3C2=O)c(Cl)c1 | 10.1016/j.bmcl.2016.04.041 | ||
| 127046203 | 139677 | None | 0 | Human | Functional | pEC50 | = | 8.9 | 8.9 | - | 1 | Positive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assay |
ChEMBL | 379 | 3 | 2 | 5 | 3.1 | Nc1cccnc1C(=O)Nc1ccc(N2Cc3ncccc3C2=O)c(Cl)c1 | 10.1016/j.bmcl.2016.04.041 | ||
| CHEMBL3797390 | 139677 | None | 0 | Human | Functional | pEC50 | = | 8.9 | 8.9 | - | 1 | Positive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assay |
ChEMBL | 379 | 3 | 2 | 5 | 3.1 | Nc1cccnc1C(=O)Nc1ccc(N2Cc3ncccc3C2=O)c(Cl)c1 | 10.1016/j.bmcl.2016.04.041 | ||
| 127046935 | 139828 | None | 0 | Human | Functional | pEC50 | = | 8.9 | 8.9 | - | 1 | Positive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assay |
ChEMBL | 398 | 3 | 2 | 4 | 4.3 | Nc1cccnc1C(=O)Nc1ccc(N2CC3(CCCCC3)CC2=O)c(Cl)c1 | 10.1016/j.bmcl.2016.04.041 | ||
| CHEMBL3798366 | 139828 | None | 0 | Human | Functional | pEC50 | = | 8.9 | 8.9 | - | 1 | Positive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assay |
ChEMBL | 398 | 3 | 2 | 4 | 4.3 | Nc1cccnc1C(=O)Nc1ccc(N2CC3(CCCCC3)CC2=O)c(Cl)c1 | 10.1016/j.bmcl.2016.04.041 | ||
| 127047648 | 139815 | None | 0 | Human | Functional | pEC50 | = | 8.9 | 8.9 | - | 1 | Positive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assay |
ChEMBL | 355 | 4 | 2 | 6 | 3.5 | Cc1ncc(Oc2ccc(NC(=O)c3ncccc3N)cc2Cl)cn1 | 10.1016/j.bmcl.2016.04.041 | ||
| CHEMBL3798239 | 139815 | None | 0 | Human | Functional | pEC50 | = | 8.9 | 8.9 | - | 1 | Positive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assay |
ChEMBL | 355 | 4 | 2 | 6 | 3.5 | Cc1ncc(Oc2ccc(NC(=O)c3ncccc3N)cc2Cl)cn1 | 10.1016/j.bmcl.2016.04.041 | ||
| 127047343 | 140034 | None | 0 | Human | Functional | pEC50 | = | 8.8 | 8.8 | - | 1 | Positive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assay |
ChEMBL | 386 | 5 | 2 | 4 | 4.0 | CC(C)CC1CC(=O)N(c2ccc(NC(=O)c3ncccc3N)cc2Cl)C1 | 10.1016/j.bmcl.2016.04.041 | ||
| CHEMBL3799708 | 140034 | None | 0 | Human | Functional | pEC50 | = | 8.8 | 8.8 | - | 1 | Positive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assay |
ChEMBL | 386 | 5 | 2 | 4 | 4.0 | CC(C)CC1CC(=O)N(c2ccc(NC(=O)c3ncccc3N)cc2Cl)C1 | 10.1016/j.bmcl.2016.04.041 | ||
| 127046934 | 139734 | None | 0 | Human | Functional | pEC50 | = | 8.7 | 8.7 | - | 1 | Positive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assay |
ChEMBL | 458 | 4 | 2 | 4 | 4.9 | Nc1cccnc1C(=O)Nc1ccc(N2CC(c3c(F)cccc3Cl)CC2=O)c(Cl)c1 | 10.1016/j.bmcl.2016.04.041 | ||
| CHEMBL3797777 | 139734 | None | 0 | Human | Functional | pEC50 | = | 8.7 | 8.7 | - | 1 | Positive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assay |
ChEMBL | 458 | 4 | 2 | 4 | 4.9 | Nc1cccnc1C(=O)Nc1ccc(N2CC(c3c(F)cccc3Cl)CC2=O)c(Cl)c1 | 10.1016/j.bmcl.2016.04.041 | ||
| 137647687 | 157848 | None | 0 | Human | Functional | pEC50 | = | 8 | 8.0 | - | 1 | Positive allosteric modulation of recombinant human mGlu4 receptor expressed in HEK293 cells co-expressing Gi/Gq assessed as increase in glutamate-induced calcium flux preincubated for 10 mins followed by glutamate addition measured for 3 mins by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of recombinant human mGlu4 receptor expressed in HEK293 cells co-expressing Gi/Gq assessed as increase in glutamate-induced calcium flux preincubated for 10 mins followed by glutamate addition measured for 3 mins by Fluo4-AM dye based fluorescence assay |
ChEMBL | 418 | 3 | 1 | 7 | 3.4 | CC(=O)N1CCC(Oc2ccc3oc(-c4cc5cccn5cn4)c/c(=N\O)c3c2)CC1 | 10.1021/acs.jmedchem.7b00991 | ||
| CHEMBL4082573 | 157848 | None | 0 | Human | Functional | pEC50 | = | 8 | 8.0 | - | 1 | Positive allosteric modulation of recombinant human mGlu4 receptor expressed in HEK293 cells co-expressing Gi/Gq assessed as increase in glutamate-induced calcium flux preincubated for 10 mins followed by glutamate addition measured for 3 mins by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of recombinant human mGlu4 receptor expressed in HEK293 cells co-expressing Gi/Gq assessed as increase in glutamate-induced calcium flux preincubated for 10 mins followed by glutamate addition measured for 3 mins by Fluo4-AM dye based fluorescence assay |
ChEMBL | 418 | 3 | 1 | 7 | 3.4 | CC(=O)N1CCC(Oc2ccc3oc(-c4cc5cccn5cn4)c/c(=N\O)c3c2)CC1 | 10.1021/acs.jmedchem.7b00991 | ||
| 1410 | 2274 | None | 38 | Human | Functional | pEC50 | = | 7 | 7.0 | -1 | 8 | Agonist activity at mGlu4 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu4 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method |
ChEMBL | 183 | 4 | 4 | 3 | -1.0 | OC(=O)[C@H](CCP(=O)(O)O)N | 10.1021/acs.jmedchem.7b01438 | ||
| 1412 | 2274 | None | 38 | Human | Functional | pEC50 | = | 7 | 7.0 | -1 | 8 | Agonist activity at mGlu4 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu4 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method |
ChEMBL | 183 | 4 | 4 | 3 | -1.0 | OC(=O)[C@H](CCP(=O)(O)O)N | 10.1021/acs.jmedchem.7b01438 | ||
| 179394 | 2274 | None | 38 | Human | Functional | pEC50 | = | 7 | 7.0 | -1 | 8 | Agonist activity at mGlu4 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu4 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method |
ChEMBL | 183 | 4 | 4 | 3 | -1.0 | OC(=O)[C@H](CCP(=O)(O)O)N | 10.1021/acs.jmedchem.7b01438 | ||
| 57689795 | 2274 | None | 38 | Human | Functional | pEC50 | = | 7 | 7.0 | -1 | 8 | Agonist activity at mGlu4 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu4 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method |
ChEMBL | 183 | 4 | 4 | 3 | -1.0 | OC(=O)[C@H](CCP(=O)(O)O)N | 10.1021/acs.jmedchem.7b01438 | ||
| CHEMBL33567 | 2274 | None | 38 | Human | Functional | pEC50 | = | 7 | 7.0 | -1 | 8 | Agonist activity at mGlu4 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu4 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method |
ChEMBL | 183 | 4 | 4 | 3 | -1.0 | OC(=O)[C@H](CCP(=O)(O)O)N | 10.1021/acs.jmedchem.7b01438 | ||
| 57519364 | 119184 | None | 0 | Rat | Functional | pEC50 | = | 7 | 7.0 | 2 | 3 | Agonist activity at rat mGluR4 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR4 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay |
ChEMBL | 213 | 3 | 4 | 3 | -0.9 | NC1(C(=O)O)CC1(F)CP(=O)(O)O | 10.1016/j.bmcl.2015.04.043 | ||
| CHEMBL3427499 | 119184 | None | 0 | Rat | Functional | pEC50 | = | 7 | 7.0 | 2 | 3 | Agonist activity at rat mGluR4 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR4 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay |
ChEMBL | 213 | 3 | 4 | 3 | -0.9 | NC1(C(=O)O)CC1(F)CP(=O)(O)O | 10.1016/j.bmcl.2015.04.043 | ||
| 122197935 | 159946 | None | 0 | Rat | Functional | pEC50 | = | 7 | 7.0 | 46 | 4 | Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution. |
ChEMBL | 377 | 10 | 5 | 7 | 0.2 | COc1cc(C(O)P(=O)(O)CC[C@@H](N)C(=O)O)ccc1OCC(=O)O | nan | ||
| CHEMBL4106637 | 159946 | None | 0 | Rat | Functional | pEC50 | = | 7 | 7.0 | 46 | 4 | Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution. |
ChEMBL | 377 | 10 | 5 | 7 | 0.2 | COc1cc(C(O)P(=O)(O)CC[C@@H](N)C(=O)O)ccc1OCC(=O)O | nan | ||
| 53388362 | 65573 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization after 1 hr by FLIPR assay |
ChEMBL | 314 | 3 | 2 | 7 | 2.6 | COc1ccnc(Nc2nc3c(s2)CCCc2n[nH]cc2-3)n1 | 10.1021/jm200290z | ||
| CHEMBL1830915 | 65573 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization after 1 hr by FLIPR assay |
ChEMBL | 314 | 3 | 2 | 7 | 2.6 | COc1ccnc(Nc2nc3c(s2)CCCc2n[nH]cc2-3)n1 | 10.1021/jm200290z | ||
| 137640190 | 157046 | None | 0 | Human | Functional | pEC50 | = | 6 | 6.0 | 1 | 3 | Agonist activity at mGlu4 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu4 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay |
ChEMBL | 318 | 7 | 4 | 6 | 0.7 | N[C@@H](CCP(=O)(O)[C@H](O)c1cccc([N+](=O)[O-])c1)C(=O)O | 10.1021/acs.jmedchem.7b01438 | ||
| CHEMBL4072781 | 157046 | None | 0 | Human | Functional | pEC50 | = | 6 | 6.0 | 1 | 3 | Agonist activity at mGlu4 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu4 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay |
ChEMBL | 318 | 7 | 4 | 6 | 0.7 | N[C@@H](CCP(=O)(O)[C@H](O)c1cccc([N+](=O)[O-])c1)C(=O)O | 10.1021/acs.jmedchem.7b01438 | ||
| 46197780 | 5584 | None | 0 | Rat | Functional | pEC50 | = | 6 | 6.0 | 4 | 4 | Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate readerAgonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader |
ChEMBL | 273 | 7 | 4 | 4 | -0.2 | N[C@@H](CCP(=O)(O)CC(Cl)C(=O)O)C(=O)O | 10.1021/jm901523t | ||
| CHEMBL1076865 | 5584 | None | 0 | Rat | Functional | pEC50 | = | 6 | 6.0 | 4 | 4 | Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate readerAgonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader |
ChEMBL | 273 | 7 | 4 | 4 | -0.2 | N[C@@H](CCP(=O)(O)CC(Cl)C(=O)O)C(=O)O | 10.1021/jm901523t | ||
| 46197778 | 8220 | None | 0 | Rat | Functional | pEC50 | = | 6 | 6.0 | -1 | 5 | Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate readerAgonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader |
ChEMBL | 237 | 6 | 4 | 4 | -0.3 | N[C@@H](CCP(=O)(O)/C=C/C(=O)O)C(=O)O | 10.1021/jm901523t | ||
| CHEMBL1092243 | 8220 | None | 0 | Rat | Functional | pEC50 | = | 6 | 6.0 | -1 | 5 | Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate readerAgonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader |
ChEMBL | 237 | 6 | 4 | 4 | -0.3 | N[C@@H](CCP(=O)(O)/C=C/C(=O)O)C(=O)O | 10.1021/jm901523t | ||
| 122197960 | 161005 | None | 0 | Rat | Functional | pEC50 | = | 6 | 6.0 | 12 | 2 | Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution. |
ChEMBL | 331 | 9 | 4 | 5 | 0.7 | N[C@H](CCP(=O)(O)Cc1ccc(OCC(=O)O)cc1)C(=O)O | nan | ||
| CHEMBL4115286 | 161005 | None | 0 | Rat | Functional | pEC50 | = | 6 | 6.0 | 12 | 2 | Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution. |
ChEMBL | 331 | 9 | 4 | 5 | 0.7 | N[C@H](CCP(=O)(O)Cc1ccc(OCC(=O)O)cc1)C(=O)O | nan | ||
| 46911068 | 975 | None | 40 | Human | Functional | pEC50 | = | 6 | 6.0 | 1 | 2 | Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization after 1 hr by FLIPR assay |
ChEMBL | 197 | 2 | 1 | 3 | 2.2 | Nc1nccc(n1)/C=C/c1ccccc1 | 10.1021/jm200290z | ||
| 6235 | 975 | None | 40 | Human | Functional | pEC50 | = | 6 | 6.0 | 1 | 2 | Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization after 1 hr by FLIPR assay |
ChEMBL | 197 | 2 | 1 | 3 | 2.2 | Nc1nccc(n1)/C=C/c1ccccc1 | 10.1021/jm200290z | ||
| CHEMBL1209431 | 975 | None | 40 | Human | Functional | pEC50 | = | 6 | 6.0 | 1 | 2 | Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization after 1 hr by FLIPR assayPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization after 1 hr by FLIPR assay |
ChEMBL | 197 | 2 | 1 | 3 | 2.2 | Nc1nccc(n1)/C=C/c1ccccc1 | 10.1021/jm200290z | ||
| 46911068 | 975 | None | 40 | Human | Functional | pEC50 | = | 6 | 6.0 | 1 | 2 | Positive allosteric modulation of human mGluR4 expressed in CHO-K1 cells assessed as decrease in forskolin-induced intracellular cAMP accumulation after 1 hr by fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO-K1 cells assessed as decrease in forskolin-induced intracellular cAMP accumulation after 1 hr by fluorescence assay |
ChEMBL | 197 | 2 | 1 | 3 | 2.2 | Nc1nccc(n1)/C=C/c1ccccc1 | 10.1016/j.bmcl.2010.06.078 | ||
| 6235 | 975 | None | 40 | Human | Functional | pEC50 | = | 6 | 6.0 | 1 | 2 | Positive allosteric modulation of human mGluR4 expressed in CHO-K1 cells assessed as decrease in forskolin-induced intracellular cAMP accumulation after 1 hr by fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO-K1 cells assessed as decrease in forskolin-induced intracellular cAMP accumulation after 1 hr by fluorescence assay |
ChEMBL | 197 | 2 | 1 | 3 | 2.2 | Nc1nccc(n1)/C=C/c1ccccc1 | 10.1016/j.bmcl.2010.06.078 | ||
Showing 1 to 50 of 2,425 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
| |
| 44191180 | 198049 | None | 0 | Rat | Binding | pEC50 | = | 6 | 6.0 | - | 0 | Activity at rat mGluR4 receptor expressed in HEK293 cells assessed as effect on thallium fluxActivity at rat mGluR4 receptor expressed in HEK293 cells assessed as effect on thallium flux |
ChEMBL | 284 | 2 | 1 | 2 | 3.5 | O=C(Nc1ccc(F)c(C(F)(F)F)c1)c1ccccn1 | 10.1021/jm9005065 | ||
| CHEMBL555454 | 198049 | None | 0 | Rat | Binding | pEC50 | = | 6 | 6.0 | - | 0 | Activity at rat mGluR4 receptor expressed in HEK293 cells assessed as effect on thallium fluxActivity at rat mGluR4 receptor expressed in HEK293 cells assessed as effect on thallium flux |
ChEMBL | 284 | 2 | 1 | 2 | 3.5 | O=C(Nc1ccc(F)c(C(F)(F)F)c1)c1ccccn1 | 10.1021/jm9005065 | ||
| 1411 | 2361 | None | 44 | Human | Binding | pEC50 | = | 6 | 6.0 | - | 1 | Agonistic activity at Metabotropic glutamate receptor 4 expressed in mammalian cells by GTPgammaS binding assayAgonistic activity at Metabotropic glutamate receptor 4 expressed in mammalian cells by GTPgammaS binding assay |
ChEMBL | 185 | 4 | 4 | 4 | -1.5 | OC(=O)[C@H](COP(=O)(O)O)N | 10.1016/s0960-894x(00)00247-x | ||
| 4120 | 2361 | None | 44 | Human | Binding | pEC50 | = | 6 | 6.0 | - | 1 | Agonistic activity at Metabotropic glutamate receptor 4 expressed in mammalian cells by GTPgammaS binding assayAgonistic activity at Metabotropic glutamate receptor 4 expressed in mammalian cells by GTPgammaS binding assay |
ChEMBL | 185 | 4 | 4 | 4 | -1.5 | OC(=O)[C@H](COP(=O)(O)O)N | 10.1016/s0960-894x(00)00247-x | ||
| 57689797 | 2361 | None | 44 | Human | Binding | pEC50 | = | 6 | 6.0 | - | 1 | Agonistic activity at Metabotropic glutamate receptor 4 expressed in mammalian cells by GTPgammaS binding assayAgonistic activity at Metabotropic glutamate receptor 4 expressed in mammalian cells by GTPgammaS binding assay |
ChEMBL | 185 | 4 | 4 | 4 | -1.5 | OC(=O)[C@H](COP(=O)(O)O)N | 10.1016/s0960-894x(00)00247-x | ||
| 68841 | 2361 | None | 44 | Human | Binding | pEC50 | = | 6 | 6.0 | - | 1 | Agonistic activity at Metabotropic glutamate receptor 4 expressed in mammalian cells by GTPgammaS binding assayAgonistic activity at Metabotropic glutamate receptor 4 expressed in mammalian cells by GTPgammaS binding assay |
ChEMBL | 185 | 4 | 4 | 4 | -1.5 | OC(=O)[C@H](COP(=O)(O)O)N | 10.1016/s0960-894x(00)00247-x | ||
| CHEMBL284377 | 2361 | None | 44 | Human | Binding | pEC50 | = | 6 | 6.0 | - | 1 | Agonistic activity at Metabotropic glutamate receptor 4 expressed in mammalian cells by GTPgammaS binding assayAgonistic activity at Metabotropic glutamate receptor 4 expressed in mammalian cells by GTPgammaS binding assay |
ChEMBL | 185 | 4 | 4 | 4 | -1.5 | OC(=O)[C@H](COP(=O)(O)O)N | 10.1016/s0960-894x(00)00247-x | ||
| DB04522 | 2361 | None | 44 | Human | Binding | pEC50 | = | 6 | 6.0 | - | 1 | Agonistic activity at Metabotropic glutamate receptor 4 expressed in mammalian cells by GTPgammaS binding assayAgonistic activity at Metabotropic glutamate receptor 4 expressed in mammalian cells by GTPgammaS binding assay |
ChEMBL | 185 | 4 | 4 | 4 | -1.5 | OC(=O)[C@H](COP(=O)(O)O)N | 10.1016/s0960-894x(00)00247-x | ||
| 46911068 | 975 | None | 40 | Rat | Binding | pEC50 | = | 6 | 6.0 | - | 0 | Positive allosteric modulation of rat mGluR4 expressed in CHO-K1 cellsPositive allosteric modulation of rat mGluR4 expressed in CHO-K1 cells |
ChEMBL | 197 | 2 | 1 | 3 | 2.2 | Nc1nccc(n1)/C=C/c1ccccc1 | 10.1016/j.bmcl.2010.06.078 | ||
| 6235 | 975 | None | 40 | Rat | Binding | pEC50 | = | 6 | 6.0 | - | 0 | Positive allosteric modulation of rat mGluR4 expressed in CHO-K1 cellsPositive allosteric modulation of rat mGluR4 expressed in CHO-K1 cells |
ChEMBL | 197 | 2 | 1 | 3 | 2.2 | Nc1nccc(n1)/C=C/c1ccccc1 | 10.1016/j.bmcl.2010.06.078 | ||
| CHEMBL1209431 | 975 | None | 40 | Rat | Binding | pEC50 | = | 6 | 6.0 | - | 0 | Positive allosteric modulation of rat mGluR4 expressed in CHO-K1 cellsPositive allosteric modulation of rat mGluR4 expressed in CHO-K1 cells |
ChEMBL | 197 | 2 | 1 | 3 | 2.2 | Nc1nccc(n1)/C=C/c1ccccc1 | 10.1016/j.bmcl.2010.06.078 | ||
| 45110506 | 116209 | None | 0 | Human | Binding | pEC50 | = | 7 | 7.0 | - | 0 | Displacement of [3H]-N-(4-{[(2- Chlorophenyl)amino]sulfonyl} phenyl )pyridine-2-carboxamide from human mGlu4 receptor after 30 mins by scintillation counting analysisDisplacement of [3H]-N-(4-{[(2- Chlorophenyl)amino]sulfonyl} phenyl )pyridine-2-carboxamide from human mGlu4 receptor after 30 mins by scintillation counting analysis |
ChEMBL | 435 | 3 | 1 | 4 | 4.2 | Cc1cccc2c1C(=O)N(c1ccc(NC(=O)c3ccccn3)cc1Br)C2=O | 10.1021/jm501245b | ||
| CHEMBL3357578 | 116209 | None | 0 | Human | Binding | pEC50 | = | 7 | 7.0 | - | 0 | Displacement of [3H]-N-(4-{[(2- Chlorophenyl)amino]sulfonyl} phenyl )pyridine-2-carboxamide from human mGlu4 receptor after 30 mins by scintillation counting analysisDisplacement of [3H]-N-(4-{[(2- Chlorophenyl)amino]sulfonyl} phenyl )pyridine-2-carboxamide from human mGlu4 receptor after 30 mins by scintillation counting analysis |
ChEMBL | 435 | 3 | 1 | 4 | 4.2 | Cc1cccc2c1C(=O)N(c1ccc(NC(=O)c3ccccn3)cc1Br)C2=O | 10.1021/jm501245b | ||
| 56649043 | 68808 | None | 0 | Rat | Binding | pEC50 | = | 7.0 | 7.0 | - | 0 | Positive allosteric modulator activity at rat mGlu4 receptor by thallium flux assayPositive allosteric modulator activity at rat mGlu4 receptor by thallium flux assay |
ChEMBL | 421 | 3 | 1 | 7 | 2.3 | O=C(Nc1ccc(N2S(=O)(=O)c3ccccc3S2(=O)=O)cc1)c1cscn1 | 10.1021/jm200956q | ||
| CHEMBL1921952 | 68808 | None | 0 | Rat | Binding | pEC50 | = | 7.0 | 7.0 | - | 0 | Positive allosteric modulator activity at rat mGlu4 receptor by thallium flux assayPositive allosteric modulator activity at rat mGlu4 receptor by thallium flux assay |
ChEMBL | 421 | 3 | 1 | 7 | 2.3 | O=C(Nc1ccc(N2S(=O)(=O)c3ccccc3S2(=O)=O)cc1)c1cscn1 | 10.1021/jm200956q | ||
| 10239 | 4043 | None | 32 | Human | Binding | pEC50 | = | 7.0 | 7.0 | - | 0 | Positive allosteric modulation of mGluR4 (unknown origin)Positive allosteric modulation of mGluR4 (unknown origin) |
ChEMBL | 359 | 4 | 1 | 4 | 4.8 | Clc1ccc(nc1)Oc1ccc(cc1Cl)NC(=O)c1ccccn1 | 10.1016/j.bmcl.2022.129106 | ||
| 73058507 | 4043 | None | 32 | Human | Binding | pEC50 | = | 7.0 | 7.0 | - | 0 | Positive allosteric modulation of mGluR4 (unknown origin)Positive allosteric modulation of mGluR4 (unknown origin) |
ChEMBL | 359 | 4 | 1 | 4 | 4.8 | Clc1ccc(nc1)Oc1ccc(cc1Cl)NC(=O)c1ccccn1 | 10.1016/j.bmcl.2022.129106 | ||
| CHEMBL4162576 | 4043 | None | 32 | Human | Binding | pEC50 | = | 7.0 | 7.0 | - | 0 | Positive allosteric modulation of mGluR4 (unknown origin)Positive allosteric modulation of mGluR4 (unknown origin) |
ChEMBL | 359 | 4 | 1 | 4 | 4.8 | Clc1ccc(nc1)Oc1ccc(cc1Cl)NC(=O)c1ccccn1 | 10.1016/j.bmcl.2022.129106 | ||
| 162662802 | 182162 | None | 0 | Rat | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | Positive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells co- expressing GIRK channel by thallium mobilization assayPositive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells co- expressing GIRK channel by thallium mobilization assay |
ChEMBL | 298 | 2 | 2 | 3 | 2.2 | Cc1cc(Cl)cc(NC(=O)[C@@H]2CSCCC(=O)N2)c1 | 10.1016/j.bmcl.2021.127838 | ||
| CHEMBL4781269 | 182162 | None | 0 | Rat | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | Positive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells co- expressing GIRK channel by thallium mobilization assayPositive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells co- expressing GIRK channel by thallium mobilization assay |
ChEMBL | 298 | 2 | 2 | 3 | 2.2 | Cc1cc(Cl)cc(NC(=O)[C@@H]2CSCCC(=O)N2)c1 | 10.1016/j.bmcl.2021.127838 | ||
| 3956 | 4035 | None | 58 | Rat | Binding | pEC50 | = | 7.0 | 7.0 | - | 0 | Activity at rat mGluR4 receptor expressed in HEK293 cells assessed as effect on thallium fluxActivity at rat mGluR4 receptor expressed in HEK293 cells assessed as effect on thallium flux |
ChEMBL | 262 | 3 | 1 | 3 | 3.0 | COc1cc(ccc1Cl)NC(=O)c1ccccn1 | 10.1021/jm9005065 | ||
| 44191096 | 4035 | None | 58 | Rat | Binding | pEC50 | = | 7.0 | 7.0 | - | 0 | Activity at rat mGluR4 receptor expressed in HEK293 cells assessed as effect on thallium fluxActivity at rat mGluR4 receptor expressed in HEK293 cells assessed as effect on thallium flux |
ChEMBL | 262 | 3 | 1 | 3 | 3.0 | COc1cc(ccc1Cl)NC(=O)c1ccccn1 | 10.1021/jm9005065 | ||
| CHEMBL562551 | 4035 | None | 58 | Rat | Binding | pEC50 | = | 7.0 | 7.0 | - | 0 | Activity at rat mGluR4 receptor expressed in HEK293 cells assessed as effect on thallium fluxActivity at rat mGluR4 receptor expressed in HEK293 cells assessed as effect on thallium flux |
ChEMBL | 262 | 3 | 1 | 3 | 3.0 | COc1cc(ccc1Cl)NC(=O)c1ccccn1 | 10.1021/jm9005065 | ||
| 729510 | 24959 | None | 16 | Rat | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | Positive allosteric modulation of rat mGlu4 receptor expressed in human HEK293 cells co-expressing GIRK potassium channels assessed as potentiation of carbachol-induced thallium flux measured between 10 to 20 secsPositive allosteric modulation of rat mGlu4 receptor expressed in human HEK293 cells co-expressing GIRK potassium channels assessed as potentiation of carbachol-induced thallium flux measured between 10 to 20 secs |
ChEMBL | 322 | 4 | 2 | 4 | 3.1 | O=C(COc1ccccc1Br)c1ccc(O)cc1O | 10.1016/j.bmcl.2011.09.131 | ||
| CHEMBL1346011 | 24959 | None | 16 | Rat | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | Positive allosteric modulation of rat mGlu4 receptor expressed in human HEK293 cells co-expressing GIRK potassium channels assessed as potentiation of carbachol-induced thallium flux measured between 10 to 20 secsPositive allosteric modulation of rat mGlu4 receptor expressed in human HEK293 cells co-expressing GIRK potassium channels assessed as potentiation of carbachol-induced thallium flux measured between 10 to 20 secs |
ChEMBL | 322 | 4 | 2 | 4 | 3.1 | O=C(COc1ccccc1Br)c1ccc(O)cc1O | 10.1016/j.bmcl.2011.09.131 | ||
| 162662065 | 181514 | None | 0 | Rat | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | Positive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells co- expressing GIRK channel by thallium mobilization assayPositive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells co- expressing GIRK channel by thallium mobilization assay |
ChEMBL | 454 | 2 | 2 | 3 | 2.6 | O=C1CCSC[C@@H](C(=O)Nc2cc(Br)cc(I)c2)N1 | 10.1016/j.bmcl.2021.127838 | ||
| CHEMBL4763684 | 181514 | None | 0 | Rat | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | Positive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells co- expressing GIRK channel by thallium mobilization assayPositive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells co- expressing GIRK channel by thallium mobilization assay |
ChEMBL | 454 | 2 | 2 | 3 | 2.6 | O=C1CCSC[C@@H](C(=O)Nc2cc(Br)cc(I)c2)N1 | 10.1016/j.bmcl.2021.127838 | ||
| 6234 | 4038 | None | 47 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | Positive allosteric modulator activity at human mGlu4 receptorPositive allosteric modulator activity at human mGlu4 receptor |
ChEMBL | 232 | 2 | 1 | 2 | 3.0 | Clc1cccc(c1)NC(=O)c1ccccn1 | 10.1016/j.bmcl.2015.07.031 | ||
| 836002 | 4038 | None | 47 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | Positive allosteric modulator activity at human mGlu4 receptorPositive allosteric modulator activity at human mGlu4 receptor |
ChEMBL | 232 | 2 | 1 | 2 | 3.0 | Clc1cccc(c1)NC(=O)c1ccccn1 | 10.1016/j.bmcl.2015.07.031 | ||
| CHEMBL556667 | 4038 | None | 47 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | Positive allosteric modulator activity at human mGlu4 receptorPositive allosteric modulator activity at human mGlu4 receptor |
ChEMBL | 232 | 2 | 1 | 2 | 3.0 | Clc1cccc(c1)NC(=O)c1ccccn1 | 10.1016/j.bmcl.2015.07.031 | ||
| 1410 | 2274 | None | 38 | Rat | Binding | pEC50 | = | 5.9 | 5.9 | -2 | 6 | Concentration for half maximal activation of metabotropic glutamate mGluR4a in ratConcentration for half maximal activation of metabotropic glutamate mGluR4a in rat |
ChEMBL | 183 | 4 | 4 | 3 | -1.0 | OC(=O)[C@H](CCP(=O)(O)O)N | 10.1021/jm00009a001 | ||
| 1412 | 2274 | None | 38 | Rat | Binding | pEC50 | = | 5.9 | 5.9 | -2 | 6 | Concentration for half maximal activation of metabotropic glutamate mGluR4a in ratConcentration for half maximal activation of metabotropic glutamate mGluR4a in rat |
ChEMBL | 183 | 4 | 4 | 3 | -1.0 | OC(=O)[C@H](CCP(=O)(O)O)N | 10.1021/jm00009a001 | ||
| 179394 | 2274 | None | 38 | Rat | Binding | pEC50 | = | 5.9 | 5.9 | -2 | 6 | Concentration for half maximal activation of metabotropic glutamate mGluR4a in ratConcentration for half maximal activation of metabotropic glutamate mGluR4a in rat |
ChEMBL | 183 | 4 | 4 | 3 | -1.0 | OC(=O)[C@H](CCP(=O)(O)O)N | 10.1021/jm00009a001 | ||
| 57689795 | 2274 | None | 38 | Rat | Binding | pEC50 | = | 5.9 | 5.9 | -2 | 6 | Concentration for half maximal activation of metabotropic glutamate mGluR4a in ratConcentration for half maximal activation of metabotropic glutamate mGluR4a in rat |
ChEMBL | 183 | 4 | 4 | 3 | -1.0 | OC(=O)[C@H](CCP(=O)(O)O)N | 10.1021/jm00009a001 | ||
| CHEMBL33567 | 2274 | None | 38 | Rat | Binding | pEC50 | = | 5.9 | 5.9 | -2 | 6 | Concentration for half maximal activation of metabotropic glutamate mGluR4a in ratConcentration for half maximal activation of metabotropic glutamate mGluR4a in rat |
ChEMBL | 183 | 4 | 4 | 3 | -1.0 | OC(=O)[C@H](CCP(=O)(O)O)N | 10.1021/jm00009a001 | ||
| 1310 | 2315 | None | 61 | Rat | Binding | pEC50 | = | 4.9 | 4.9 | -26 | 18 | Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 4Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 4 |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | OC(=O)CC[C@@H](C(=O)O)N | 10.1021/jm020122x | ||
| 1369 | 2315 | None | 61 | Rat | Binding | pEC50 | = | 4.9 | 4.9 | -26 | 18 | Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 4Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 4 |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | OC(=O)CC[C@@H](C(=O)O)N | 10.1021/jm020122x | ||
| 33032 | 2315 | None | 61 | Rat | Binding | pEC50 | = | 4.9 | 4.9 | -26 | 18 | Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 4Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 4 |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | OC(=O)CC[C@@H](C(=O)O)N | 10.1021/jm020122x | ||
| 44272391 | 2315 | None | 61 | Rat | Binding | pEC50 | = | 4.9 | 4.9 | -26 | 18 | Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 4Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 4 |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | OC(=O)CC[C@@H](C(=O)O)N | 10.1021/jm020122x | ||
| 88747398 | 2315 | None | 61 | Rat | Binding | pEC50 | = | 4.9 | 4.9 | -26 | 18 | Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 4Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 4 |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | OC(=O)CC[C@@H](C(=O)O)N | 10.1021/jm020122x | ||
| CHEMBL575060 | 2315 | None | 61 | Rat | Binding | pEC50 | = | 4.9 | 4.9 | -26 | 18 | Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 4Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 4 |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | OC(=O)CC[C@@H](C(=O)O)N | 10.1021/jm020122x | ||
| DB00142 | 2315 | None | 61 | Rat | Binding | pEC50 | = | 4.9 | 4.9 | -26 | 18 | Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 4Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 4 |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | OC(=O)CC[C@@H](C(=O)O)N | 10.1021/jm020122x | ||
| 139054390 | 207381 | None | 56 | Rat | Binding | pEC50 | = | 4.9 | 4.9 | - | 5 | Effect on Metabotropic glutamate receptor 4Effect on Metabotropic glutamate receptor 4 |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | N[C@H](CCC(=O)O)C(=O)O | 10.1021/jm9703597 | ||
| 23327 | 207381 | None | 56 | Rat | Binding | pEC50 | = | 4.9 | 4.9 | - | 5 | Effect on Metabotropic glutamate receptor 4Effect on Metabotropic glutamate receptor 4 |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | N[C@H](CCC(=O)O)C(=O)O | 10.1021/jm9703597 | ||
| CHEMBL76232 | 207381 | None | 56 | Rat | Binding | pEC50 | = | 4.9 | 4.9 | - | 5 | Effect on Metabotropic glutamate receptor 4Effect on Metabotropic glutamate receptor 4 |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | N[C@H](CCC(=O)O)C(=O)O | 10.1021/jm9703597 | ||
| 134190222 | 172593 | None | 0 | Rat | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | Positive allosteric modulation of rat mGlu4 receptor expressed in HEK cells co-expressing GIRK1/2 assessed as increase in glutamate-induced thallium flux preincubated for 140 secs followed by glutamate addition and measured after 2.5 mins by FluoZin-2-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu4 receptor expressed in HEK cells co-expressing GIRK1/2 assessed as increase in glutamate-induced thallium flux preincubated for 140 secs followed by glutamate addition and measured after 2.5 mins by FluoZin-2-AM dye based fluorescence assay |
ChEMBL | 283 | 2 | 2 | 5 | 3.3 | Cc1noc2ccc(Nc3n[nH]c4cc(F)cnc34)cc12 | 10.1021/acs.jmedchem.8b00994 | ||
| CHEMBL4483053 | 172593 | None | 0 | Rat | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | Positive allosteric modulation of rat mGlu4 receptor expressed in HEK cells co-expressing GIRK1/2 assessed as increase in glutamate-induced thallium flux preincubated for 140 secs followed by glutamate addition and measured after 2.5 mins by FluoZin-2-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu4 receptor expressed in HEK cells co-expressing GIRK1/2 assessed as increase in glutamate-induced thallium flux preincubated for 140 secs followed by glutamate addition and measured after 2.5 mins by FluoZin-2-AM dye based fluorescence assay |
ChEMBL | 283 | 2 | 2 | 5 | 3.3 | Cc1noc2ccc(Nc3n[nH]c4cc(F)cnc34)cc12 | 10.1021/acs.jmedchem.8b00994 | ||
| 127046557 | 139814 | None | 3 | Rat | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | Positive allosteric modulator activity at rat mGlu4 receptorPositive allosteric modulator activity at rat mGlu4 receptor |
ChEMBL | 392 | 3 | 2 | 5 | 3.4 | Nc1cccnc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1 | 10.1016/j.bmcl.2016.04.041 | ||
| CHEMBL3798234 | 139814 | None | 3 | Rat | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | Positive allosteric modulator activity at rat mGlu4 receptorPositive allosteric modulator activity at rat mGlu4 receptor |
ChEMBL | 392 | 3 | 2 | 5 | 3.4 | Nc1cccnc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1 | 10.1016/j.bmcl.2016.04.041 | ||
| 1411 | 2361 | None | 44 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 1 | Concentration for half maximal activation of metabotropic glutamate mGluR4a in humanConcentration for half maximal activation of metabotropic glutamate mGluR4a in human |
ChEMBL | 185 | 4 | 4 | 4 | -1.5 | OC(=O)[C@H](COP(=O)(O)O)N | 10.1021/jm00009a001 | ||
Showing 1 to 50 of 682 entries