Ligand source activities (1 row/activity)





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127047647 146537 0 None 22 2 Human 10.2 pEC50 = 10.2 Functional
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 146537 0 None 22 2 Human 10.2 pEC50 = 10.2 Functional
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 146505 3 None 42 2 Human 10.0 pEC50 = 10.0 Functional
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 146505 3 None 42 2 Human 10.0 pEC50 = 10.0 Functional
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 146495 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
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 146495 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
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 146380 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
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 146380 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
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 146646 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
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 146646 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
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 146453 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
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 146453 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
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 146386 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
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 146386 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
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 146368 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
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 146368 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
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 146519 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
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 146519 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
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 146506 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
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 146506 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
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 146725 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
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 146725 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
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 146425 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
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 146425 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
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 164535 0 None - 1 Human 8.0 pEC50 = 8 Functional
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 164535 0 None - 1 Human 8.0 pEC50 = 8 Functional
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 9054 48 None -1 8 Human 7.0 pEC50 = 7 Functional
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 9054 48 None -1 8 Human 7.0 pEC50 = 7 Functional
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 9054 48 None -1 8 Human 7.0 pEC50 = 7 Functional
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 9054 48 None -1 8 Human 7.0 pEC50 = 7 Functional
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 9054 48 None -1 8 Human 7.0 pEC50 = 7 Functional
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 125898 0 None 2 3 Rat 7.0 pEC50 = 7 Functional
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 125898 0 None 2 3 Rat 7.0 pEC50 = 7 Functional
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 166631 0 None 46 4 Rat 7.0 pEC50 = 7 Functional
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 166631 0 None 46 4 Rat 7.0 pEC50 = 7 Functional
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 72326 0 None - 1 Human 7.0 pEC50 = 7 Functional
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 72326 0 None - 1 Human 7.0 pEC50 = 7 Functional
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 163733 0 None 1 3 Human 6.0 pEC50 = 6 Functional
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 163733 0 None 1 3 Human 6.0 pEC50 = 6 Functional
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 12354 0 None 4 4 Rat 6.0 pEC50 = 6 Functional
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 12354 0 None 4 4 Rat 6.0 pEC50 = 6 Functional
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 14990 0 None -1 5 Rat 6.0 pEC50 = 6 Functional
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 14990 0 None -1 5 Rat 6.0 pEC50 = 6 Functional
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 167690 0 None 12 2 Rat 6.0 pEC50 = 6 Functional
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 167690 0 None 12 2 Rat 6.0 pEC50 = 6 Functional
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 7762 46 None 1 2 Human 6.0 pEC50 = 6 Functional
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 7762 46 None 1 2 Human 6.0 pEC50 = 6 Functional
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 7762 46 None 1 2 Human 6.0 pEC50 = 6 Functional
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 7762 46 None 1 2 Human 6.0 pEC50 = 6 Functional
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 7762 46 None 1 2 Human 6.0 pEC50 = 6 Functional
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
CHEMBL1209431 7762 46 None 1 2 Human 6.0 pEC50 = 6 Functional
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
1314024 50406 12 None 1 2 Rat 6.0 pEC50 = 6 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 448 5 2 4 5.2 COc1cc(NC(=O)c2ccc(Br)o2)ccc1NC(=O)c1ccccc1Cl 10.1021/jm101271s
CHEMBL1509597 50406 12 None 1 2 Rat 6.0 pEC50 = 6 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 448 5 2 4 5.2 COc1cc(NC(=O)c2ccc(Br)o2)ccc1NC(=O)c1ccccc1Cl 10.1021/jm101271s
45484609 204033 0 None - 1 Human 5.0 pEC50 = 5 Functional
Allosteric modulator activity at human mGlu4 receptor expressed in CHO cells coexpressing Gqi5 assessed as effect on calcium fluxAllosteric modulator activity at human mGlu4 receptor expressed in CHO cells coexpressing Gqi5 assessed as effect on calcium flux
ChEMBL 328 3 2 2 3.5 CNC(=O)[C@@H]1CCCC[C@@H]1C(=O)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2009.07.072
CHEMBL568440 204033 0 None - 1 Human 5.0 pEC50 = 5 Functional
Allosteric modulator activity at human mGlu4 receptor expressed in CHO cells coexpressing Gqi5 assessed as effect on calcium fluxAllosteric modulator activity at human mGlu4 receptor expressed in CHO cells coexpressing Gqi5 assessed as effect on calcium flux
ChEMBL 328 3 2 2 3.5 CNC(=O)[C@@H]1CCCC[C@@H]1C(=O)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2009.07.072
45484637 205679 0 None - 1 Human 5.0 pEC50 = 5 Functional
Allosteric modulator activity at human mGlu4 receptor expressed in CHO cells coexpressing Gqi5 assessed as effect on calcium fluxAllosteric modulator activity at human mGlu4 receptor expressed in CHO cells coexpressing Gqi5 assessed as effect on calcium flux
ChEMBL 368 5 2 2 4.3 O=C(Nc1cc(Cl)cc(Cl)c1)[C@H]1CCCC[C@H]1C(=O)NCC1CC1 10.1016/j.bmcl.2009.07.072
CHEMBL584413 205679 0 None - 1 Human 5.0 pEC50 = 5 Functional
Allosteric modulator activity at human mGlu4 receptor expressed in CHO cells coexpressing Gqi5 assessed as effect on calcium fluxAllosteric modulator activity at human mGlu4 receptor expressed in CHO cells coexpressing Gqi5 assessed as effect on calcium flux
ChEMBL 368 5 2 2 4.3 O=C(Nc1cc(Cl)cc(Cl)c1)[C@H]1CCCC[C@H]1C(=O)NCC1CC1 10.1016/j.bmcl.2009.07.072
70683530 81019 0 None - 1 Human 5.0 pEC50 = 5 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 358 4 1 5 4.2 CCNC(=O)Oc1ccc2c(-c3cnn(-c4ccccc4)c3)ccnc2c1 10.1016/j.bmcl.2012.03.032
CHEMBL2023627 81019 0 None - 1 Human 5.0 pEC50 = 5 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 358 4 1 5 4.2 CCNC(=O)Oc1ccc2c(-c3cnn(-c4ccccc4)c3)ccnc2c1 10.1016/j.bmcl.2012.03.032
53373994 152090 0 None - 1 Human 5.0 pEC50 = 5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 217 2 2 5 2.2 c1cnc2c(Nc3nccs3)n[nH]c2c1 nan
CHEMBL3913233 152090 0 None - 1 Human 5.0 pEC50 = 5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 217 2 2 5 2.2 c1cnc2c(Nc3nccs3)n[nH]c2c1 nan
53374405 153901 1 None - 1 Human 7.0 pEC50 = 7 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 246 2 2 3 3.0 Fc1cc(F)cc(Nc2n[nH]c3cccnc23)c1 nan
CHEMBL3927518 153901 1 None - 1 Human 7.0 pEC50 = 7 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 246 2 2 3 3.0 Fc1cc(F)cc(Nc2n[nH]c3cccnc23)c1 nan
122196101 131014 0 None -20 2 Human 6.0 pEC50 = 6 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 394 3 1 4 4.6 Cc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(Cl)c2C1=O 10.1016/j.bmcl.2015.10.013
CHEMBL3634424 131014 0 None -20 2 Human 6.0 pEC50 = 6 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 394 3 1 4 4.6 Cc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(Cl)c2C1=O 10.1016/j.bmcl.2015.10.013
1092661 36328 12 None -1 2 Rat 6.0 pEC50 = 6 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 370 5 2 4 4.4 COc1cc(NC(=O)c2ccco2)ccc1NC(=O)c1ccccc1Cl 10.1021/jm101271s
CHEMBL1385271 36328 12 None -1 2 Rat 6.0 pEC50 = 6 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 370 5 2 4 4.4 COc1cc(NC(=O)c2ccco2)ccc1NC(=O)c1ccccc1Cl 10.1021/jm101271s
137645909 164799 0 None - 1 Human 6.0 pEC50 = 6 Functional
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 328 2 1 4 4.8 O/N=c1\cc(-c2cc3ccccc3cn2)oc2ccc(C3CC3)cc12 10.1021/acs.jmedchem.7b00991
CHEMBL4085608 164799 0 None - 1 Human 6.0 pEC50 = 6 Functional
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 328 2 1 4 4.8 O/N=c1\cc(-c2cc3ccccc3cn2)oc2ccc(C3CC3)cc12 10.1021/acs.jmedchem.7b00991
54670223 147284 0 None - 1 Human 6.0 pEC50 = 6 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 409 5 1 6 3.4 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccc(F)cc1F nan
CHEMBL3810046 147284 0 None - 1 Human 6.0 pEC50 = 6 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 409 5 1 6 3.4 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccc(F)cc1F nan
155564012 182182 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 295 3 2 5 3.9 CCc1nsc2cc(Nc3n[nH]c4ncccc34)ccc12 10.1021/acs.jmedchem.8b00994
CHEMBL4575642 182182 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 295 3 2 5 3.9 CCc1nsc2cc(Nc3n[nH]c4ncccc34)ccc12 10.1021/acs.jmedchem.8b00994
155564012 182182 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 295 3 2 5 3.9 CCc1nsc2cc(Nc3n[nH]c4ncccc34)ccc12 10.1021/acs.jmedchem.8b00994
CHEMBL4575642 182182 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 295 3 2 5 3.9 CCc1nsc2cc(Nc3n[nH]c4ncccc34)ccc12 10.1021/acs.jmedchem.8b00994
53373997 154550 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 279 2 2 4 3.4 Clc1cc(Nc2n[nH]c3cccnc23)cnc1Cl nan
CHEMBL3932566 154550 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 279 2 2 4 3.4 Clc1cc(Nc2n[nH]c3cccnc23)cnc1Cl nan
68374199 147311 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 377 5 1 5 3.1 O=C(Nc1ccn(S(=O)(=O)C(F)c2ccccc2F)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
CHEMBL3810364 147311 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 377 5 1 5 3.1 O=C(Nc1ccn(S(=O)(=O)C(F)c2ccccc2F)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
54670408 159195 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 441 5 1 6 4.1 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccccc1C(F)(F)F nan
CHEMBL3970594 159195 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 441 5 1 6 4.1 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccccc1C(F)(F)F nan
68374199 147311 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 377 5 1 5 3.1 O=C(Nc1ccn(S(=O)(=O)C(F)c2ccccc2F)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
CHEMBL3810364 147311 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 377 5 1 5 3.1 O=C(Nc1ccn(S(=O)(=O)C(F)c2ccccc2F)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
45111051 22660 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilization
ChEMBL 359 5 2 4 2.9 O=C(Nc1ccc(S(=O)(=O)NC2CCCCC2)cc1)c1ccccn1 10.1016/j.bmcl.2010.07.007
CHEMBL1223159 22660 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilization
ChEMBL 359 5 2 4 2.9 O=C(Nc1ccc(S(=O)(=O)NC2CCCCC2)cc1)c1ccccn1 10.1016/j.bmcl.2010.07.007
53375184 160034 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 258 3 2 4 2.8 COc1cc(Nc2n[nH]c3cccnc23)ccc1F nan
CHEMBL3977560 160034 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 258 3 2 4 2.8 COc1cc(Nc2n[nH]c3cccnc23)ccc1F nan
135125821 178886 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 358 3 1 6 2.1 Cc1nnc2ccc(C(=O)NC3CN(c4ccc(C#N)cn4)C3)cc2c1C 10.1016/j.bmcl.2019.126678
CHEMBL4472631 178886 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 358 3 1 6 2.1 Cc1nnc2ccc(C(=O)NC3CN(c4ccc(C#N)cn4)C3)cc2c1C 10.1016/j.bmcl.2019.126678
52913659 147194 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 341 4 1 5 2.7 Cc1cccc(S(=O)(=O)n2ccc(NC(=O)c3ccccn3)c2)c1 10.1016/j.bmcl.2016.05.029
CHEMBL3808963 147194 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 341 4 1 5 2.7 Cc1cccc(S(=O)(=O)n2ccc(NC(=O)c3ccccn3)c2)c1 10.1016/j.bmcl.2016.05.029
134191976 172375 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 375 5 2 8 3.5 Cc1cc(COc2nn(C)c3cc(Nc4n[nH]c5cccnc45)ccc23)on1 10.1016/j.bmcl.2018.06.034
CHEMBL4242783 172375 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 375 5 2 8 3.5 Cc1cc(COc2nn(C)c3cc(Nc4n[nH]c5cccnc45)ccc23)on1 10.1016/j.bmcl.2018.06.034
56649043 75561 0 None 1 2 Human 7.0 pEC50 = 7.0 Functional
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 421 3 1 7 2.3 O=C(Nc1ccc(N2S(=O)(=O)c3ccccc3S2(=O)=O)cc1)c1cscn1 10.1021/jm200956q
CHEMBL1921952 75561 0 None 1 2 Human 7.0 pEC50 = 7.0 Functional
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 421 3 1 7 2.3 O=C(Nc1ccc(N2S(=O)(=O)c3ccccc3S2(=O)=O)cc1)c1cscn1 10.1021/jm200956q
46869940 64669 4 None 1 2 Rat 7.0 pEC50 = 7.0 Functional
Positive allosteric modulator activity at rat mGlu4 receptor expressed in HEK293 cells assessed as effect on L-AP4-induced inositol phosphate accumulation incubated for 30 mins by florescence assayPositive allosteric modulator activity at rat mGlu4 receptor expressed in HEK293 cells assessed as effect on L-AP4-induced inositol phosphate accumulation incubated for 30 mins by florescence assay
ChEMBL 381 5 2 4 4.2 COc1cc(NC(=O)c2ccccn2)ccc1NC(=O)c1ccccc1Cl 10.1039/C4MD00208C
CHEMBL1672234 64669 4 None 1 2 Rat 7.0 pEC50 = 7.0 Functional
Positive allosteric modulator activity at rat mGlu4 receptor expressed in HEK293 cells assessed as effect on L-AP4-induced inositol phosphate accumulation incubated for 30 mins by florescence assayPositive allosteric modulator activity at rat mGlu4 receptor expressed in HEK293 cells assessed as effect on L-AP4-induced inositol phosphate accumulation incubated for 30 mins by florescence assay
ChEMBL 381 5 2 4 4.2 COc1cc(NC(=O)c2ccccn2)ccc1NC(=O)c1ccccc1Cl 10.1039/C4MD00208C
52913659 147194 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 341 4 1 5 2.7 Cc1cccc(S(=O)(=O)n2ccc(NC(=O)c3ccccn3)c2)c1 10.1016/j.bmcl.2016.05.029
CHEMBL3808963 147194 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 341 4 1 5 2.7 Cc1cccc(S(=O)(=O)n2ccc(NC(=O)c3ccccn3)c2)c1 10.1016/j.bmcl.2016.05.029
122419061 181852 0 None 1 2 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 339 3 2 7 3.7 CC(C)(C)Cc1nsc2cc(Nc3n[nH]c4nccnc34)cnc12 10.1021/acs.jmedchem.8b00994
CHEMBL4568302 181852 0 None 1 2 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 339 3 2 7 3.7 CC(C)(C)Cc1nsc2cc(Nc3n[nH]c4nccnc34)cnc12 10.1021/acs.jmedchem.8b00994
51003374 74583 0 None 1 2 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 357 4 2 4 4.3 O=C(Nc1ccc(NC(=O)c2cccs2)c(Cl)c1)c1ccccn1 10.1021/jm101271s
CHEMBL1909435 74583 0 None 1 2 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 357 4 2 4 4.3 O=C(Nc1ccc(NC(=O)c2cccs2)c(Cl)c1)c1ccccn1 10.1021/jm101271s
121485560 178351 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 325 3 3 6 3.5 CC(C)(O)c1nsc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
CHEMBL4464916 178351 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 325 3 3 6 3.5 CC(C)(O)c1nsc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
46836709 72316 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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 301 2 2 5 3.3 Fc1cccc(Nc2nc3c(s2)CCCc2n[nH]cc2-3)n1 10.1021/jm200290z
CHEMBL1830903 72316 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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 301 2 2 5 3.3 Fc1cccc(Nc2nc3c(s2)CCCc2n[nH]cc2-3)n1 10.1021/jm200290z
122419061 181852 0 None 1 2 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 339 3 2 7 3.7 CC(C)(C)Cc1nsc2cc(Nc3n[nH]c4nccnc34)cnc12 10.1021/acs.jmedchem.8b00994
CHEMBL4568302 181852 0 None 1 2 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 339 3 2 7 3.7 CC(C)(C)Cc1nsc2cc(Nc3n[nH]c4nccnc34)cnc12 10.1021/acs.jmedchem.8b00994
121485560 178351 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 325 3 3 6 3.5 CC(C)(O)c1nsc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
CHEMBL4464916 178351 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 325 3 3 6 3.5 CC(C)(O)c1nsc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
54670777 154115 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 435 6 1 6 3.9 O=C(Nc1nc(C2CC2)c(S(=O)(=O)Cc2ccc(F)cc2F)s1)c1ccccn1 nan
CHEMBL3929271 154115 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 435 6 1 6 3.9 O=C(Nc1nc(C2CC2)c(S(=O)(=O)Cc2ccc(F)cc2F)s1)c1ccccn1 nan
54670407 160852 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 415 6 1 6 4.2 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccc(C(C)C)cc1 nan
CHEMBL3984752 160852 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 415 6 1 6 4.2 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccc(C(C)C)cc1 nan
46869940 64669 4 None 1 2 Rat 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 381 5 2 4 4.2 COc1cc(NC(=O)c2ccccn2)ccc1NC(=O)c1ccccc1Cl 10.1021/jm101271s
CHEMBL1672234 64669 4 None 1 2 Rat 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 381 5 2 4 4.2 COc1cc(NC(=O)c2ccccn2)ccc1NC(=O)c1ccccc1Cl 10.1021/jm101271s
137648591 164509 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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 455 5 1 6 5.7 O/N=c1\cc(-c2cc3sccc3cn2)oc2ccc(CCCN3CCC(F)(F)CC3)cc12 10.1021/acs.jmedchem.7b00991
CHEMBL4082167 164509 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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 455 5 1 6 5.7 O/N=c1\cc(-c2cc3sccc3cn2)oc2ccc(CCCN3CCC(F)(F)CC3)cc12 10.1021/acs.jmedchem.7b00991
54670779 150605 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 463 5 1 6 4.1 O=C(Nc1nc(C(F)(F)F)c(S(=O)(=O)Cc2c(F)cccc2F)s1)c1ccccn1 nan
CHEMBL3901396 150605 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 463 5 1 6 4.1 O=C(Nc1nc(C(F)(F)F)c(S(=O)(=O)Cc2c(F)cccc2F)s1)c1ccccn1 nan
127025847 144504 0 None -1 2 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human mGlu4 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu4 receptor by cell based calcium mobilization
ChEMBL 398 3 1 5 3.3 Cn1ccnc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3758986 144504 0 None -1 2 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human mGlu4 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu4 receptor by cell based calcium mobilization
ChEMBL 398 3 1 5 3.3 Cn1ccnc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
54670684 158793 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 409 5 1 6 3.4 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1cc(F)ccc1F nan
CHEMBL3966945 158793 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 409 5 1 6 3.4 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1cc(F)ccc1F nan
10239 10815 29 None 1 5 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human mGlu4 expressed in CHO cells co-expressing Gqi5 (unknown origin) assessed as reduction in intracellular Ca2+ levels by Fluo-4-AM dye based fluorescence assayAgonist activity at human mGlu4 expressed in CHO cells co-expressing Gqi5 (unknown origin) assessed as reduction in intracellular Ca2+ levels by Fluo-4-AM dye based fluorescence assay
ChEMBL 359 4 1 4 4.8 Clc1ccc(nc1)Oc1ccc(cc1Cl)NC(=O)c1ccccn1 10.1039/C8MD00524A
73058507 10815 29 None 1 5 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human mGlu4 expressed in CHO cells co-expressing Gqi5 (unknown origin) assessed as reduction in intracellular Ca2+ levels by Fluo-4-AM dye based fluorescence assayAgonist activity at human mGlu4 expressed in CHO cells co-expressing Gqi5 (unknown origin) assessed as reduction in intracellular Ca2+ levels by Fluo-4-AM dye based fluorescence assay
ChEMBL 359 4 1 4 4.8 Clc1ccc(nc1)Oc1ccc(cc1Cl)NC(=O)c1ccccn1 10.1039/C8MD00524A
CHEMBL4162576 10815 29 None 1 5 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human mGlu4 expressed in CHO cells co-expressing Gqi5 (unknown origin) assessed as reduction in intracellular Ca2+ levels by Fluo-4-AM dye based fluorescence assayAgonist activity at human mGlu4 expressed in CHO cells co-expressing Gqi5 (unknown origin) assessed as reduction in intracellular Ca2+ levels by Fluo-4-AM dye based fluorescence assay
ChEMBL 359 4 1 4 4.8 Clc1ccc(nc1)Oc1ccc(cc1Cl)NC(=O)c1ccccn1 10.1039/C8MD00524A
10239 10815 29 None 1 5 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assay
ChEMBL 359 4 1 4 4.8 Clc1ccc(nc1)Oc1ccc(cc1Cl)NC(=O)c1ccccn1 10.1021/acsmedchemlett.7b00317
73058507 10815 29 None 1 5 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assay
ChEMBL 359 4 1 4 4.8 Clc1ccc(nc1)Oc1ccc(cc1Cl)NC(=O)c1ccccn1 10.1021/acsmedchemlett.7b00317
CHEMBL4162576 10815 29 None 1 5 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assay
ChEMBL 359 4 1 4 4.8 Clc1ccc(nc1)Oc1ccc(cc1Cl)NC(=O)c1ccccn1 10.1021/acsmedchemlett.7b00317
69938322 153269 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 338 4 2 6 3.9 Clc1cc(Nc2n[nH]c3cccnc23)ccc1Oc1cnccn1 nan
CHEMBL3922380 153269 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 338 4 2 6 3.9 Clc1cc(Nc2n[nH]c3cccnc23)ccc1Oc1cnccn1 nan
127026469 144479 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human mGlu4 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu4 receptor by cell based calcium mobilization
ChEMBL 398 3 1 5 3.3 Cn1ccnc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3758795 144479 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human mGlu4 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu4 receptor by cell based calcium mobilization
ChEMBL 398 3 1 5 3.3 Cn1ccnc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
6706 9146 8 None 1 8 Human 7.0 pEC50 = 7.0 Functional
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 347 9 5 6 0.2 OC(=O)COc1ccc(cc1)C(P(=O)(CC[C@@H](C(=O)O)N)O)O 10.1021/acs.jmedchem.7b01438
71041983 9146 8 None 1 8 Human 7.0 pEC50 = 7.0 Functional
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 347 9 5 6 0.2 OC(=O)COc1ccc(cc1)C(P(=O)(CC[C@@H](C(=O)O)N)O)O 10.1021/acs.jmedchem.7b01438
CHEMBL3114673 9146 8 None 1 8 Human 7.0 pEC50 = 7.0 Functional
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 347 9 5 6 0.2 OC(=O)COc1ccc(cc1)C(P(=O)(CC[C@@H](C(=O)O)N)O)O 10.1021/acs.jmedchem.7b01438
6706 9146 8 None -1 8 Rat 7.0 pEC50 = 7.0 Functional
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 347 9 5 6 0.2 OC(=O)COc1ccc(cc1)C(P(=O)(CC[C@@H](C(=O)O)N)O)O nan
71041983 9146 8 None -1 8 Rat 7.0 pEC50 = 7.0 Functional
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 347 9 5 6 0.2 OC(=O)COc1ccc(cc1)C(P(=O)(CC[C@@H](C(=O)O)N)O)O nan
CHEMBL3114673 9146 8 None -1 8 Rat 7.0 pEC50 = 7.0 Functional
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 347 9 5 6 0.2 OC(=O)COc1ccc(cc1)C(P(=O)(CC[C@@H](C(=O)O)N)O)O nan
51352627 165927 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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 277 1 1 5 3.0 O/N=c1\cc(-c2cc3cccn3cn2)oc2ccccc12 10.1021/acs.jmedchem.7b00991
CHEMBL4098106 165927 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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 277 1 1 5 3.0 O/N=c1\cc(-c2cc3cccn3cn2)oc2ccccc12 10.1021/acs.jmedchem.7b00991
6234 10810 68 None -3 2 Human 6.0 pEC50 = 6.0 Functional
Activity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilizationActivity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilization
ChEMBL 232 2 1 2 3.0 Clc1cccc(c1)NC(=O)c1ccccn1 10.1021/jm9005065
836002 10810 68 None -3 2 Human 6.0 pEC50 = 6.0 Functional
Activity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilizationActivity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilization
ChEMBL 232 2 1 2 3.0 Clc1cccc(c1)NC(=O)c1ccccn1 10.1021/jm9005065
CHEMBL556667 10810 68 None -3 2 Human 6.0 pEC50 = 6.0 Functional
Activity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilizationActivity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilization
ChEMBL 232 2 1 2 3.0 Clc1cccc(c1)NC(=O)c1ccccn1 10.1021/jm9005065
2442621 203090 16 None -1 2 Human 6.0 pEC50 = 6.0 Functional
Activity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilizationActivity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilization
ChEMBL 262 3 1 3 3.0 COc1ccc(NC(=O)c2ccccn2)cc1Cl 10.1021/jm9005065
CHEMBL562232 203090 16 None -1 2 Human 6.0 pEC50 = 6.0 Functional
Activity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilizationActivity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilization
ChEMBL 262 3 1 3 3.0 COc1ccc(NC(=O)c2ccccn2)cc1Cl 10.1021/jm9005065
6234 10810 68 None -3 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human mGlu4 receptor assessed as increase in calcium flux by Fluo-4 AM dye based analysisAgonist activity at human mGlu4 receptor assessed as increase in calcium flux by Fluo-4 AM dye based analysis
ChEMBL 232 2 1 2 3.0 Clc1cccc(c1)NC(=O)c1ccccn1 10.1016/j.ejmech.2022.114378
836002 10810 68 None -3 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human mGlu4 receptor assessed as increase in calcium flux by Fluo-4 AM dye based analysisAgonist activity at human mGlu4 receptor assessed as increase in calcium flux by Fluo-4 AM dye based analysis
ChEMBL 232 2 1 2 3.0 Clc1cccc(c1)NC(=O)c1ccccn1 10.1016/j.ejmech.2022.114378
CHEMBL556667 10810 68 None -3 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human mGlu4 receptor assessed as increase in calcium flux by Fluo-4 AM dye based analysisAgonist activity at human mGlu4 receptor assessed as increase in calcium flux by Fluo-4 AM dye based analysis
ChEMBL 232 2 1 2 3.0 Clc1cccc(c1)NC(=O)c1ccccn1 10.1016/j.ejmech.2022.114378
122197952 167351 0 None 13 3 Rat 6.0 pEC50 = 6.0 Functional
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 363 9 6 7 -0.1 N[C@H](CCP(=O)(O)C(O)c1ccc(OCC(=O)O)c(O)c1)C(=O)O nan
CHEMBL4112652 167351 0 None 13 3 Rat 6.0 pEC50 = 6.0 Functional
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 363 9 6 7 -0.1 N[C@H](CCP(=O)(O)C(O)c1ccc(OCC(=O)O)c(O)c1)C(=O)O nan
122197955 167373 0 None 10 3 Rat 6.0 pEC50 = 6.0 Functional
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 408 10 5 8 0.8 N[C@H](CCP(=O)(O)C(O)c1ccc(SCC(=O)O)c([N+](=O)[O-])c1)C(=O)O nan
CHEMBL4112800 167373 0 None 10 3 Rat 6.0 pEC50 = 6.0 Functional
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 408 10 5 8 0.8 N[C@H](CCP(=O)(O)C(O)c1ccc(SCC(=O)O)c([N+](=O)[O-])c1)C(=O)O nan
46836637 72317 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 317 2 2 5 3.8 Clc1cccc(Nc2nc3c(s2)CCCc2n[nH]cc2-3)n1 10.1021/jm200290z
CHEMBL1830904 72317 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 317 2 2 5 3.8 Clc1cccc(Nc2nc3c(s2)CCCc2n[nH]cc2-3)n1 10.1021/jm200290z
70693972 80922 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 289 2 0 3 4.2 Fc1ccccc1-n1cc(-c2ccnc3ccccc23)cn1 10.1016/j.bmcl.2012.03.032
CHEMBL2022869 80922 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 289 2 0 3 4.2 Fc1ccccc1-n1cc(-c2ccnc3ccccc23)cn1 10.1016/j.bmcl.2012.03.032
122196102 131015 0 None -22 2 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 378 3 1 4 4.1 Cc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(F)c2C1=O 10.1016/j.bmcl.2015.10.013
CHEMBL3634425 131015 0 None -22 2 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 378 3 1 4 4.1 Cc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(F)c2C1=O 10.1016/j.bmcl.2015.10.013
6234 10810 68 None -3 2 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 232 2 1 2 3.0 Clc1cccc(c1)NC(=O)c1ccccn1 10.1016/j.bmcl.2018.06.034
836002 10810 68 None -3 2 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 232 2 1 2 3.0 Clc1cccc(c1)NC(=O)c1ccccn1 10.1016/j.bmcl.2018.06.034
CHEMBL556667 10810 68 None -3 2 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 232 2 1 2 3.0 Clc1cccc(c1)NC(=O)c1ccccn1 10.1016/j.bmcl.2018.06.034
46853657 75562 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 433 3 1 6 2.4 O=C(Nc1ccc(N2S(=O)(=O)c3ccccc3S2(=O)=O)cc1F)c1ccccn1 10.1021/jm200956q
CHEMBL1921954 75562 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 433 3 1 6 2.4 O=C(Nc1ccc(N2S(=O)(=O)c3ccccc3S2(=O)=O)cc1F)c1ccccn1 10.1021/jm200956q
122193177 130710 6 None -34 3 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of human mGlu4 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay
ChEMBL 398 3 1 4 4.4 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
CHEMBL3628113 130710 6 None -34 3 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of human mGlu4 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay
ChEMBL 398 3 1 4 4.4 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
53375179 154288 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 274 3 2 4 3.4 COc1cc(Nc2n[nH]c3cccnc23)ccc1Cl nan
CHEMBL3930568 154288 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 274 3 2 4 3.4 COc1cc(Nc2n[nH]c3cccnc23)ccc1Cl nan
122196113 131025 0 None -32 2 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 381 3 1 5 3.7 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)nc1 10.1016/j.bmcl.2015.10.013
CHEMBL3634435 131025 0 None -32 2 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 381 3 1 5 3.7 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)nc1 10.1016/j.bmcl.2015.10.013
53374104 156793 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 337 4 2 5 4.5 Clc1cc(Nc2n[nH]c3cccnc23)ccc1Oc1ccccn1 nan
CHEMBL3950346 156793 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 337 4 2 5 4.5 Clc1cc(Nc2n[nH]c3cccnc23)ccc1Oc1ccccn1 nan
127025479 144508 0 None -51 2 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human mGlu4 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu4 receptor by cell based calcium mobilization
ChEMBL 411 3 1 5 4.5 Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3ncsc3C)cc1Cl)C2=O 10.1016/j.bmcl.2015.12.104
CHEMBL3759038 144508 0 None -51 2 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human mGlu4 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu4 receptor by cell based calcium mobilization
ChEMBL 411 3 1 5 4.5 Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3ncsc3C)cc1Cl)C2=O 10.1016/j.bmcl.2015.12.104
51003236 64672 0 None 1 2 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 386 5 2 3 5.1 COc1cc(NC(=O)C2CCCCC2)ccc1NC(=O)c1ccccc1Cl 10.1021/jm101271s
CHEMBL1672237 64672 0 None 1 2 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 386 5 2 3 5.1 COc1cc(NC(=O)C2CCCCC2)ccc1NC(=O)c1ccccc1Cl 10.1021/jm101271s
51003233 64670 0 None 1 2 Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 382 5 2 5 3.6 COc1cc(NC(=O)c2cnccn2)ccc1NC(=O)c1ccccc1Cl 10.1021/jm101271s
CHEMBL1672235 64670 0 None 1 2 Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 382 5 2 5 3.6 COc1cc(NC(=O)c2cnccn2)ccc1NC(=O)c1ccccc1Cl 10.1021/jm101271s
122193177 130710 6 None -34 3 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of human mGlu4 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay
ChEMBL 398 3 1 4 4.4 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
CHEMBL3628113 130710 6 None -34 3 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of human mGlu4 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay
ChEMBL 398 3 1 4 4.4 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
162661457 188213 0 None -1 3 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 396 3 1 4 4.2 Cc1cc(N2C(=O)c3cccc(F)c3C2=O)c(F)cc1NC(=O)c1occc1C 10.1016/j.bmcl.2020.127724
CHEMBL4764083 188213 0 None -1 3 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 396 3 1 4 4.2 Cc1cc(N2C(=O)c3cccc(F)c3C2=O)c(F)cc1NC(=O)c1occc1C 10.1016/j.bmcl.2020.127724
53374214 157464 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 278 2 2 3 4.0 Clc1ccc(Nc2n[nH]c3cccnc23)cc1Cl nan
CHEMBL3955855 157464 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 278 2 2 3 4.0 Clc1ccc(Nc2n[nH]c3cccnc23)cc1Cl nan
51003374 74583 0 None -1 2 Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 357 4 2 4 4.3 O=C(Nc1ccc(NC(=O)c2cccs2)c(Cl)c1)c1ccccn1 10.1021/jm101271s
CHEMBL1909435 74583 0 None -1 2 Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 357 4 2 4 4.3 O=C(Nc1ccc(NC(=O)c2cccs2)c(Cl)c1)c1ccccn1 10.1021/jm101271s
57519364 125898 0 None 2 3 Rat 4.9 pEC50 = 4.9 Functional
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 125898 0 None 2 3 Rat 4.9 pEC50 = 4.9 Functional
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
51003325 64680 0 None 1 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 403 4 2 3 5.0 O=C(Nc1ccc(NC(=O)c2ccc(F)cc2Cl)c(Cl)c1)c1ccccn1 10.1021/jm101271s
CHEMBL1672245 64680 0 None 1 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 403 4 2 3 5.0 O=C(Nc1ccc(NC(=O)c2ccc(F)cc2Cl)c(Cl)c1)c1ccccn1 10.1021/jm101271s
122193175 130708 0 None -34 2 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of human mGlu4 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay
ChEMBL 414 3 1 4 4.9 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
CHEMBL3628111 130708 0 None -34 2 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of human mGlu4 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay
ChEMBL 414 3 1 4 4.9 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
46197776 15128 0 None 1 3 Rat 4.9 pEC50 = 4.9 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 253 8 4 4 -0.1 N[C@@H](CCP(=O)(O)CCCC(=O)O)C(=O)O 10.1021/jm901523t
CHEMBL1093009 15128 0 None 1 3 Rat 4.9 pEC50 = 4.9 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 253 8 4 4 -0.1 N[C@@H](CCP(=O)(O)CCCC(=O)O)C(=O)O 10.1021/jm901523t
122193175 130708 0 None -34 2 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of human mGlu4 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay
ChEMBL 414 3 1 4 4.9 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
CHEMBL3628111 130708 0 None -34 2 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of human mGlu4 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay
ChEMBL 414 3 1 4 4.9 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
53374110 159856 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 306 3 2 5 2.2 CS(=O)(=O)c1ccc(Nc2n[nH]c3cccnc23)cc1F nan
CHEMBL3976079 159856 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 306 3 2 5 2.2 CS(=O)(=O)c1ccc(Nc2n[nH]c3cccnc23)cc1F nan
135126573 176411 0 None 1 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 401 3 1 5 3.6 Cc1nnc2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cc2c1C 10.1016/j.bmcl.2019.126678
CHEMBL4437035 176411 0 None 1 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 401 3 1 5 3.6 Cc1nnc2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cc2c1C 10.1016/j.bmcl.2019.126678
134198083 172282 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 397 4 3 6 3.1 Cn1nc(C(=O)NC2CC(F)(F)C2)c2ccc(Nc3n[nH]c4cccnc34)cc21 10.1016/j.bmcl.2018.06.034
CHEMBL4240579 172282 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 397 4 3 6 3.1 Cn1nc(C(=O)NC2CC(F)(F)C2)c2ccc(Nc3n[nH]c4cccnc34)cc21 10.1016/j.bmcl.2018.06.034
53373665 154737 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 338 4 2 6 3.9 Clc1cc(Nc2n[nH]c3cccnc23)ccc1Oc1ncccn1 nan
CHEMBL3933898 154737 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 338 4 2 6 3.9 Clc1cc(Nc2n[nH]c3cccnc23)ccc1Oc1ncccn1 nan
67377858 157975 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 262 2 2 3 3.5 Fc1ccc(Cl)cc1Nc1n[nH]c2cccnc12 nan
CHEMBL3959843 157975 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 262 2 2 3 3.5 Fc1ccc(Cl)cc1Nc1n[nH]c2cccnc12 nan
136503369 164128 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 318 2 1 5 3.9 COc1ccc2/c(=N/O)cc(-c3cc4ccccc4cn3)oc2c1 10.1021/acs.jmedchem.7b00991
CHEMBL4077754 164128 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 318 2 1 5 3.9 COc1ccc2/c(=N/O)cc(-c3cc4ccccc4cn3)oc2c1 10.1021/acs.jmedchem.7b00991
58058380 164552 0 None 2 2 Human 4.9 pEC50 = 4.9 Functional
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 363 8 5 8 0.3 COc1cc(C(N)P(=O)(O)CC[C@H](N)C(=O)O)cc([N+](=O)[O-])c1O 10.1021/acs.jmedchem.7b01438
CHEMBL4082769 164552 0 None 2 2 Human 4.9 pEC50 = 4.9 Functional
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 363 8 5 8 0.3 COc1cc(C(N)P(=O)(O)CC[C@H](N)C(=O)O)cc([N+](=O)[O-])c1O 10.1021/acs.jmedchem.7b01438
134190218 178419 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 321 5 2 5 4.7 CCCC(C)c1noc2cc(Nc3n[nH]c4ncccc34)ccc12 10.1021/acs.jmedchem.8b00994
CHEMBL4465813 178419 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 321 5 2 5 4.7 CCCC(C)c1noc2cc(Nc3n[nH]c4ncccc34)ccc12 10.1021/acs.jmedchem.8b00994
54670595 160797 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 441 5 1 6 4.4 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1c(Cl)cccc1Cl nan
CHEMBL3984173 160797 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 441 5 1 6 4.4 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1c(Cl)cccc1Cl nan
134190218 178419 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 321 5 2 5 4.7 CCCC(C)c1noc2cc(Nc3n[nH]c4ncccc34)ccc12 10.1021/acs.jmedchem.8b00994
CHEMBL4465813 178419 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 321 5 2 5 4.7 CCCC(C)c1noc2cc(Nc3n[nH]c4ncccc34)ccc12 10.1021/acs.jmedchem.8b00994
52935190 154058 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 398 4 1 6 2.7 O=C(Nc1cnn(S(=O)(=O)c2cc(F)c(F)cc2Cl)c1)c1ccccn1 nan
CHEMBL3928811 154058 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 398 4 1 6 2.7 O=C(Nc1cnn(S(=O)(=O)c2cc(F)c(F)cc2Cl)c1)c1ccccn1 nan
1092658 34936 11 None -1 2 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 386 5 2 4 4.9 COc1cc(NC(=O)c2cccs2)ccc1NC(=O)c1ccccc1Cl 10.1021/jm101271s
CHEMBL1373422 34936 11 None -1 2 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 386 5 2 4 4.9 COc1cc(NC(=O)c2cccs2)ccc1NC(=O)c1ccccc1Cl 10.1021/jm101271s
49862695 21905 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
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 198 2 1 4 1.6 Nc1nccc(/C=C/c2ccccn2)n1 10.1016/j.bmcl.2010.06.078
CHEMBL1209743 21905 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
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 198 2 1 4 1.6 Nc1nccc(/C=C/c2ccccn2)n1 10.1016/j.bmcl.2010.06.078
60096231 164434 15 None -5011 4 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at recombinant human mGlu4 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 mGlu4 receptor expressed in hamster AV12 cells co-expressing rat EAAT1/Galpha15 assessed as induction of increase in Ca2+ flux after 2.5 mins by Fluo-3 AM dye-based FLIPR assay
ChEMBL 334 5 4 5 -0.1 COc1cccc(C(=O)N[C@H]2C[C@@](N)(C(=O)O)[C@@H]3[C@@H](C(=O)O)[C@H]23)c1 10.1021/acs.jmedchem.7b01481
CHEMBL4081453 164434 15 None -5011 4 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at recombinant human mGlu4 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 mGlu4 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
122196107 131020 0 None -25 2 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 376 4 1 5 3.7 COc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2ccccc2C1=O 10.1016/j.bmcl.2015.10.013
CHEMBL3634430 131020 0 None -25 2 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 376 4 1 5 3.7 COc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2ccccc2C1=O 10.1016/j.bmcl.2015.10.013
69938798 160544 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 268 2 2 4 3.6 Fc1ccc(Nc2n[nH]c3scnc23)cc1Cl nan
CHEMBL3982008 160544 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 268 2 2 4 3.6 Fc1ccc(Nc2n[nH]c3scnc23)cc1Cl nan
145983574 172505 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 332 2 2 5 3.6 Cn1nc(C(F)(F)F)c2ccc(Nc3n[nH]c4cccnc34)cc21 10.1016/j.bmcl.2018.06.034
CHEMBL4246041 172505 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 332 2 2 5 3.6 Cn1nc(C(F)(F)F)c2ccc(Nc3n[nH]c4cccnc34)cc21 10.1016/j.bmcl.2018.06.034
69938823 156776 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 276 2 1 4 3.5 Cn1nc2cccnc2c1Nc1ccc(F)c(Cl)c1 nan
CHEMBL3950175 156776 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 276 2 1 4 3.5 Cn1nc2cccnc2c1Nc1ccc(F)c(Cl)c1 nan
57519364 125898 0 None 2 3 Rat 6.9 pEC50 = 6.9 Functional
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 125898 0 None 2 3 Rat 6.9 pEC50 = 6.9 Functional
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
70683532 81025 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 249 2 0 3 3.6 Cc1nccc(-c2cnn(-c3ccccc3)c2)c1C 10.1016/j.bmcl.2012.03.032
CHEMBL2023633 81025 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 249 2 0 3 3.6 Cc1nccc(-c2cnn(-c3ccccc3)c2)c1C 10.1016/j.bmcl.2012.03.032
162674608 190160 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 334 6 3 6 3.3 COCCNc1nccc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1016/j.bmcl.2018.10.050
CHEMBL4797966 190160 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 334 6 3 6 3.3 COCCNc1nccc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1016/j.bmcl.2018.10.050
134192044 172479 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 318 4 2 5 3.9 CCn1nc(C2CC2)c2ccc(Nc3n[nH]c4cccnc34)cc21 10.1016/j.bmcl.2018.06.034
CHEMBL4241223 172479 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 318 4 2 5 3.9 CCn1nc(C2CC2)c2ccc(Nc3n[nH]c4cccnc34)cc21 10.1016/j.bmcl.2018.06.034
CHEMBL4245437 172479 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 318 4 2 5 3.9 CCn1nc(C2CC2)c2ccc(Nc3n[nH]c4cccnc34)cc21 10.1016/j.bmcl.2018.06.034
46884751 15012 0 None 4 2 Rat 4.9 pEC50 = 4.9 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 253 7 4 4 -0.2 CC(CP(=O)(O)CC[C@H](N)C(=O)O)C(=O)O 10.1021/jm901523t
CHEMBL1092311 15012 0 None 4 2 Rat 4.9 pEC50 = 4.9 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 253 7 4 4 -0.2 CC(CP(=O)(O)CC[C@H](N)C(=O)O)C(=O)O 10.1021/jm901523t
135126302 176917 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 351 3 1 5 2.4 Cc1nnc2ccc(C(=O)NC3CN(c4ncccc4F)C3)cc2c1C 10.1016/j.bmcl.2019.126678
CHEMBL4444129 176917 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 351 3 1 5 2.4 Cc1nnc2ccc(C(=O)NC3CN(c4ncccc4F)C3)cc2c1C 10.1016/j.bmcl.2019.126678
52913660 147148 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 341 4 1 5 2.7 Cc1ccc(S(=O)(=O)n2ccc(NC(=O)c3ccccn3)c2)cc1 10.1016/j.bmcl.2016.05.029
CHEMBL3808424 147148 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 341 4 1 5 2.7 Cc1ccc(S(=O)(=O)n2ccc(NC(=O)c3ccccn3)c2)cc1 10.1016/j.bmcl.2016.05.029
49865350 22692 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilization
ChEMBL 405 5 2 4 3.9 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2Cl)cc1)c1cccc(F)n1 10.1016/j.bmcl.2010.07.007
CHEMBL1223241 22692 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilization
ChEMBL 405 5 2 4 3.9 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2Cl)cc1)c1cccc(F)n1 10.1016/j.bmcl.2010.07.007
134190225 182480 0 None 1 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 283 2 2 5 3.3 Cc1noc2c(F)cc(Nc3n[nH]c4ncccc34)cc12 10.1021/acs.jmedchem.8b00994
CHEMBL4582128 182480 0 None 1 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 283 2 2 5 3.3 Cc1noc2c(F)cc(Nc3n[nH]c4ncccc34)cc12 10.1021/acs.jmedchem.8b00994
122197962 167202 0 None 13 2 Rat 5.9 pEC50 = 5.9 Functional
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 415 10 4 6 1.6 N[C@H](CCP(=O)(O)Cc1ccc(OCC(=O)O)c(OC(F)(F)F)c1)C(=O)O nan
CHEMBL4111386 167202 0 None 13 2 Rat 5.9 pEC50 = 5.9 Functional
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 415 10 4 6 1.6 N[C@H](CCP(=O)(O)Cc1ccc(OCC(=O)O)c(OC(F)(F)F)c1)C(=O)O nan
122197945 167008 0 None 2 3 Rat 4.9 pEC50 = 4.9 Functional
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 333 9 5 6 0.1 N[C@H](CCP(=O)(O)C(O)c1ccc(OCCO)cc1)C(=O)O nan
CHEMBL4109799 167008 0 None 2 3 Rat 4.9 pEC50 = 4.9 Functional
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 333 9 5 6 0.1 N[C@H](CCP(=O)(O)C(O)c1ccc(OCCO)cc1)C(=O)O nan
52913660 147148 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 341 4 1 5 2.7 Cc1ccc(S(=O)(=O)n2ccc(NC(=O)c3ccccn3)c2)cc1 10.1016/j.bmcl.2016.05.029
CHEMBL3808424 147148 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 341 4 1 5 2.7 Cc1ccc(S(=O)(=O)n2ccc(NC(=O)c3ccccn3)c2)cc1 10.1016/j.bmcl.2016.05.029
134190225 182480 0 None 1 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 283 2 2 5 3.3 Cc1noc2c(F)cc(Nc3n[nH]c4ncccc34)cc12 10.1021/acs.jmedchem.8b00994
CHEMBL4582128 182480 0 None 1 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 283 2 2 5 3.3 Cc1noc2c(F)cc(Nc3n[nH]c4ncccc34)cc12 10.1021/acs.jmedchem.8b00994
52913766 147181 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 361 4 1 5 3.0 O=C(Nc1ccn(S(=O)(=O)c2ccc(Cl)cc2)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
CHEMBL3808806 147181 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 361 4 1 5 3.0 O=C(Nc1ccn(S(=O)(=O)c2ccc(Cl)cc2)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
52913766 147181 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 361 4 1 5 3.0 O=C(Nc1ccn(S(=O)(=O)c2ccc(Cl)cc2)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
CHEMBL3808806 147181 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 361 4 1 5 3.0 O=C(Nc1ccn(S(=O)(=O)c2ccc(Cl)cc2)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
51347211 161113 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 360 4 1 6 2.2 Cc1cc(S(=O)(=O)n2cc(NC(=O)c3ccccn3)cn2)ccc1F nan
CHEMBL3986803 161113 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 360 4 1 6 2.2 Cc1cc(S(=O)(=O)n2cc(NC(=O)c3ccccn3)cn2)ccc1F nan
127047649 146867 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 393 3 2 5 3.5 O=C(Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1)c1ncccc1O 10.1016/j.bmcl.2016.04.041
CHEMBL3800579 146867 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 393 3 2 5 3.5 O=C(Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1)c1ncccc1O 10.1016/j.bmcl.2016.04.041
1310 9095 110 None -426 17 Rat 4.9 pEC50 = 4.9 Functional
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 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2015.04.043
1369 9095 110 None -426 17 Rat 4.9 pEC50 = 4.9 Functional
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 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2015.04.043
33032 9095 110 None -426 17 Rat 4.9 pEC50 = 4.9 Functional
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 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2015.04.043
44272391 9095 110 None -426 17 Rat 4.9 pEC50 = 4.9 Functional
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 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2015.04.043
88747398 9095 110 None -426 17 Rat 4.9 pEC50 = 4.9 Functional
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 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2015.04.043
CHEMBL575060 9095 110 None -426 17 Rat 4.9 pEC50 = 4.9 Functional
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 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2015.04.043
DB00142 9095 110 None -426 17 Rat 4.9 pEC50 = 4.9 Functional
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 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2015.04.043
127046203 146368 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 146368 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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
135125589 177217 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 367 3 1 5 2.9 Cc1nnc2ccc(C(=O)NC3CN(c4ccc(Cl)cn4)C3)cc2c1C 10.1016/j.bmcl.2019.126678
CHEMBL4448578 177217 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 367 3 1 5 2.9 Cc1nnc2ccc(C(=O)NC3CN(c4ccc(Cl)cn4)C3)cc2c1C 10.1016/j.bmcl.2019.126678
136503371 162577 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 289 1 1 5 3.3 O/N=c1\cc(-c2cc3cnccc3cn2)oc2ccccc12 10.1021/acs.jmedchem.7b00991
CHEMBL4059644 162577 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 289 1 1 5 3.3 O/N=c1\cc(-c2cc3cnccc3cn2)oc2ccccc12 10.1021/acs.jmedchem.7b00991
52935414 157649 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 380 4 1 6 2.6 O=C(Nc1cnn(S(=O)(=O)c2ccc(Cl)cc2F)c1)c1ccccn1 nan
CHEMBL3957303 157649 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 380 4 1 6 2.6 O=C(Nc1cnn(S(=O)(=O)c2ccc(Cl)cc2F)c1)c1ccccn1 nan
162648102 186683 0 None -1 5 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 378 3 1 4 4.1 Cc1cc(NC(=O)c2occc2C)c(F)cc1N1C(=O)c2ccccc2C1=O 10.1016/j.bmcl.2020.127724
CHEMBL4745982 186683 0 None -1 5 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 378 3 1 4 4.1 Cc1cc(NC(=O)c2occc2C)c(F)cc1N1C(=O)c2ccccc2C1=O 10.1016/j.bmcl.2020.127724
134190210 181174 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 321 5 2 5 4.7 CCC(CC)c1noc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
CHEMBL4552309 181174 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 321 5 2 5 4.7 CCC(CC)c1noc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
53373993 155200 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 281 2 3 3 3.2 Cc1ccc(NC(=O)Nc2n[nH]c3cccnc23)cc1C nan
CHEMBL3937739 155200 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 281 2 3 3 3.2 Cc1ccc(NC(=O)Nc2n[nH]c3cccnc23)cc1C nan
134189992 180657 0 None -2 2 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 321 3 2 5 4.4 CC(C)(C)Cc1noc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
CHEMBL4539629 180657 0 None -2 2 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 321 3 2 5 4.4 CC(C)(C)Cc1noc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
127046935 146519 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 146519 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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
134190210 181174 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 321 5 2 5 4.7 CCC(CC)c1noc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
CHEMBL4552309 181174 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 321 5 2 5 4.7 CCC(CC)c1noc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
134191958 172734 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 318 3 2 5 3.6 Cn1nc(C2(C)CC2)c2ccc(Nc3n[nH]c4ncccc34)cc21 10.1016/j.bmcl.2018.06.034
CHEMBL4251433 172734 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 318 3 2 5 3.6 Cn1nc(C2(C)CC2)c2ccc(Nc3n[nH]c4ncccc34)cc21 10.1016/j.bmcl.2018.06.034
134191550 187175 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 359 3 2 6 3.0 CN1CCN(c2nccc3cc(Nc4n[nH]c5cccnc45)ccc23)CC1 10.1016/j.bmcl.2018.10.050
CHEMBL4751941 187175 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 359 3 2 6 3.0 CN1CCN(c2nccc3cc(Nc4n[nH]c5cccnc45)ccc23)CC1 10.1016/j.bmcl.2018.10.050
54670776 154577 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 451 6 1 6 4.4 O=C(Nc1nc(C2CC2)c(S(=O)(=O)Cc2ccc(Cl)cc2F)s1)c1ccccn1 nan
CHEMBL3932737 154577 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 451 6 1 6 4.4 O=C(Nc1nc(C2CC2)c(S(=O)(=O)Cc2ccc(Cl)cc2F)s1)c1ccccn1 nan
25138329 72296 5 None - 1 Human 7.9 pEC50 = 7.9 Functional
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 257 3 2 5 3.0 Cc1sc(Nc2ccccn2)nc1-c1cn[nH]c1 10.1021/jm200290z
CHEMBL1830694 72296 5 None - 1 Human 7.9 pEC50 = 7.9 Functional
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 257 3 2 5 3.0 Cc1sc(Nc2ccccn2)nc1-c1cn[nH]c1 10.1021/jm200290z
1410 9054 48 None -1 8 Human 6.9 pEC50 = 6.9 Functional
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 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.7b01438
1412 9054 48 None -1 8 Human 6.9 pEC50 = 6.9 Functional
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 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.7b01438
179394 9054 48 None -1 8 Human 6.9 pEC50 = 6.9 Functional
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 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.7b01438
57689795 9054 48 None -1 8 Human 6.9 pEC50 = 6.9 Functional
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 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.7b01438
CHEMBL33567 9054 48 None -1 8 Human 6.9 pEC50 = 6.9 Functional
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 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.7b01438
127030387 145884 0 None 3 3 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 217 5 4 4 -1.0 N[C@@H](C[C@]1(C(=O)O)C[C@H]1C(=O)O)C(=O)O 10.1021/acs.jmedchem.5b01333
CHEMBL3786667 145884 0 None 3 3 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 217 5 4 4 -1.0 N[C@@H](C[C@]1(C(=O)O)C[C@H]1C(=O)O)C(=O)O 10.1021/acs.jmedchem.5b01333
1410 9054 48 None -1 8 Rat 6.9 pEC50 = 6.9 Functional
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 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm901523t
1412 9054 48 None -1 8 Rat 6.9 pEC50 = 6.9 Functional
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 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm901523t
179394 9054 48 None -1 8 Rat 6.9 pEC50 = 6.9 Functional
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 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm901523t
57689795 9054 48 None -1 8 Rat 6.9 pEC50 = 6.9 Functional
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 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm901523t
CHEMBL33567 9054 48 None -1 8 Rat 6.9 pEC50 = 6.9 Functional
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 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm901523t
1410 9054 48 None -1 8 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells coexpressing Gq/Gi and EAAC1 assessed as intracellular calcium production measured every 1.5 secs for 60 secs by Fluo-4-AM based fluorometryAgonist activity at rat mGlu4 receptor expressed in HEK293 cells coexpressing Gq/Gi and EAAC1 assessed as intracellular calcium production measured every 1.5 secs for 60 secs by Fluo-4-AM based fluorometry
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmc.2012.06.006
1412 9054 48 None -1 8 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells coexpressing Gq/Gi and EAAC1 assessed as intracellular calcium production measured every 1.5 secs for 60 secs by Fluo-4-AM based fluorometryAgonist activity at rat mGlu4 receptor expressed in HEK293 cells coexpressing Gq/Gi and EAAC1 assessed as intracellular calcium production measured every 1.5 secs for 60 secs by Fluo-4-AM based fluorometry
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmc.2012.06.006
179394 9054 48 None -1 8 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells coexpressing Gq/Gi and EAAC1 assessed as intracellular calcium production measured every 1.5 secs for 60 secs by Fluo-4-AM based fluorometryAgonist activity at rat mGlu4 receptor expressed in HEK293 cells coexpressing Gq/Gi and EAAC1 assessed as intracellular calcium production measured every 1.5 secs for 60 secs by Fluo-4-AM based fluorometry
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmc.2012.06.006
57689795 9054 48 None -1 8 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells coexpressing Gq/Gi and EAAC1 assessed as intracellular calcium production measured every 1.5 secs for 60 secs by Fluo-4-AM based fluorometryAgonist activity at rat mGlu4 receptor expressed in HEK293 cells coexpressing Gq/Gi and EAAC1 assessed as intracellular calcium production measured every 1.5 secs for 60 secs by Fluo-4-AM based fluorometry
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmc.2012.06.006
CHEMBL33567 9054 48 None -1 8 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells coexpressing Gq/Gi and EAAC1 assessed as intracellular calcium production measured every 1.5 secs for 60 secs by Fluo-4-AM based fluorometryAgonist activity at rat mGlu4 receptor expressed in HEK293 cells coexpressing Gq/Gi and EAAC1 assessed as intracellular calcium production measured every 1.5 secs for 60 secs by Fluo-4-AM based fluorometry
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmc.2012.06.006
1443 8100 36 None 2 5 Rat 6.9 pEC50 = 6.9 Functional
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 183 4 4 3 -1.0 OC(=O)[C@@H](CCP(=O)(O)O)N nan
1550579 8100 36 None 2 5 Rat 6.9 pEC50 = 6.9 Functional
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 183 4 4 3 -1.0 OC(=O)[C@@H](CCP(=O)(O)O)N nan
CHEMBL1319383 8100 36 None 2 5 Rat 6.9 pEC50 = 6.9 Functional
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 183 4 4 3 -1.0 OC(=O)[C@@H](CCP(=O)(O)O)N nan
122197939 167473 0 None 89 3 Rat 6.9 pEC50 = 6.9 Functional
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 411 10 5 7 0.9 COc1cc(C(O)P(=O)(O)CC[C@@H](N)C(=O)O)cc(Cl)c1OCC(=O)O nan
CHEMBL4113547 167473 0 None 89 3 Rat 6.9 pEC50 = 6.9 Functional
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 411 10 5 7 0.9 COc1cc(C(O)P(=O)(O)CC[C@@H](N)C(=O)O)cc(Cl)c1OCC(=O)O nan
136503386 165846 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 294 1 1 5 4.0 O/N=c1\cc(-c2cc3ccsc3cn2)oc2ccccc12 10.1021/acs.jmedchem.7b00991
CHEMBL4097178 165846 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 294 1 1 5 4.0 O/N=c1\cc(-c2cc3ccsc3cn2)oc2ccccc12 10.1021/acs.jmedchem.7b00991
53387726 72303 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 284 2 2 6 2.6 c1cc(Nc2nc3c(s2)CCCc2n[nH]cc2-3)ncn1 10.1021/jm200290z
CHEMBL1830709 72303 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 284 2 2 6 2.6 c1cc(Nc2nc3c(s2)CCCc2n[nH]cc2-3)ncn1 10.1021/jm200290z
53387886 72311 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 288 2 2 4 3.8 c1[nH]nc2c1-c1nc(NC3CCCCC3)sc1CCC2 10.1021/jm200290z
CHEMBL1830897 72311 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 288 2 2 4 3.8 c1[nH]nc2c1-c1nc(NC3CCCCC3)sc1CCC2 10.1021/jm200290z
134189992 180657 0 None -2 2 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 321 3 2 5 4.4 CC(C)(C)Cc1noc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
CHEMBL4539629 180657 0 None -2 2 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 321 3 2 5 4.4 CC(C)(C)Cc1noc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
49862528 21859 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 275 2 1 3 3.0 Nc1ncc(Br)c(/C=C/c2ccccc2)n1 10.1016/j.bmcl.2010.06.078
CHEMBL1209521 21859 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 275 2 1 3 3.0 Nc1ncc(Br)c(/C=C/c2ccccc2)n1 10.1016/j.bmcl.2010.06.078
56649126 75566 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 397 3 1 5 2.7 O=C(Nc1ccc(N2C(=O)[C@@H]3[C@@H]4CC[C@@H](O4)[C@@H]3C2=O)c(Cl)c1)c1ccccn1 10.1021/jm200956q
CHEMBL1921960 75566 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 397 3 1 5 2.7 O=C(Nc1ccc(N2C(=O)[C@@H]3[C@@H]4CC[C@@H](O4)[C@@H]3C2=O)c(Cl)c1)c1ccccn1 10.1021/jm200956q
122197947 167166 0 None 5 2 Rat 4.9 pEC50 = 4.9 Functional
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 347 9 5 6 0.2 N[C@H](CCP(=O)(O)C(O)c1cccc(OCC(=O)O)c1)C(=O)O nan
CHEMBL4111192 167166 0 None 5 2 Rat 4.9 pEC50 = 4.9 Functional
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 347 9 5 6 0.2 N[C@H](CCP(=O)(O)C(O)c1cccc(OCC(=O)O)c1)C(=O)O nan
49865401 22723 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilization
ChEMBL 413 7 2 6 3.2 COc1ccccc1NS(=O)(=O)c1ccc(NC(=O)c2ccccn2)cc1OC 10.1016/j.bmcl.2010.07.007
CHEMBL1223316 22723 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilization
ChEMBL 413 7 2 6 3.2 COc1ccccc1NS(=O)(=O)c1ccc(NC(=O)c2ccccn2)cc1OC 10.1016/j.bmcl.2010.07.007
134191660 189242 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 409 3 2 6 4.7 Cn1nc(C(F)(F)F)cc1-c1nccc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1016/j.bmcl.2018.10.050
CHEMBL4786373 189242 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 409 3 2 6 4.7 Cn1nc(C(F)(F)F)cc1-c1nccc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1016/j.bmcl.2018.10.050
135125800 178009 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 367 3 1 5 2.9 Cc1nnc2ccc(C(=O)NC3CN(c4cccc(Cl)n4)C3)cc2c1C 10.1016/j.bmcl.2019.126678
CHEMBL4459708 178009 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 367 3 1 5 2.9 Cc1nnc2ccc(C(=O)NC3CN(c4cccc(Cl)n4)C3)cc2c1C 10.1016/j.bmcl.2019.126678
51003234 64671 0 None -1 2 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 382 5 2 5 3.6 COc1cc(NC(=O)c2ccncn2)ccc1NC(=O)c1ccccc1Cl 10.1021/jm101271s
CHEMBL1672236 64671 0 None -1 2 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 382 5 2 5 3.6 COc1cc(NC(=O)c2ccncn2)ccc1NC(=O)c1ccccc1Cl 10.1021/jm101271s
54670124 153633 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 391 5 1 6 3.2 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccccc1F nan
CHEMBL3925193 153633 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 391 5 1 6 3.2 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccccc1F nan
53322767 64684 0 None 1 2 Rat 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 371 4 1 5 4.0 COc1ccccc1C(=O)n1ccc2cc(NC(=O)c3ccccn3)ccc21 10.1021/jm101271s
CHEMBL1672257 64684 0 None 1 2 Rat 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 371 4 1 5 4.0 COc1ccccc1C(=O)n1ccc2cc(NC(=O)c3ccccn3)ccc21 10.1021/jm101271s
134189964 182638 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 279 3 2 5 3.4 CCc1noc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
CHEMBL4585748 182638 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 279 3 2 5 3.4 CCc1noc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
127047648 146506 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 146506 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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
134189964 182638 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 279 3 2 5 3.4 CCc1noc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
CHEMBL4585748 182638 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 279 3 2 5 3.4 CCc1noc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
46853681 75478 0 None 1 2 Human 6.9 pEC50 = 6.9 Functional
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 415 3 1 6 2.2 O=C(Nc1ccc(N2S(=O)(=O)c3ccccc3S2(=O)=O)cc1)c1ccccn1 10.1021/jm200956q
CHEMBL1921855 75478 0 None 1 2 Human 6.9 pEC50 = 6.9 Functional
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 415 3 1 6 2.2 O=C(Nc1ccc(N2S(=O)(=O)c3ccccc3S2(=O)=O)cc1)c1ccccn1 10.1021/jm200956q
134191553 186440 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 366 5 3 5 4.9 c1ccc(CNc2nccc3cc(Nc4n[nH]c5cccnc45)ccc23)cc1 10.1016/j.bmcl.2018.10.050
CHEMBL4743261 186440 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 366 5 3 5 4.9 c1ccc(CNc2nccc3cc(Nc4n[nH]c5cccnc45)ccc23)cc1 10.1016/j.bmcl.2018.10.050
52934973 155880 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 360 4 1 6 2.2 Cc1ccc(S(=O)(=O)n2cc(NC(=O)c3ccccn3)cn2)cc1F nan
CHEMBL3943144 155880 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 360 4 1 6 2.2 Cc1ccc(S(=O)(=O)n2cc(NC(=O)c3ccccn3)cn2)cc1F nan
134190176 177475 0 None -2 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 266 2 2 6 2.5 Cc1noc2ccc(Nc3n[nH]c4nccnc34)cc12 10.1021/acs.jmedchem.8b00994
CHEMBL4451827 177475 0 None -2 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 266 2 2 6 2.5 Cc1noc2ccc(Nc3n[nH]c4nccnc34)cc12 10.1021/acs.jmedchem.8b00994
52935410 156165 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 380 4 1 6 2.6 O=C(Nc1cnn(S(=O)(=O)c2ccc(F)c(Cl)c2)c1)c1ccccn1 nan
CHEMBL3945496 156165 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 380 4 1 6 2.6 O=C(Nc1cnn(S(=O)(=O)c2ccc(F)c(Cl)c2)c1)c1ccccn1 nan
135125807 181561 0 None 2 2 Rat 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 392 3 1 6 2.8 Cc1nnc2ccc(C(=O)NC3CN(c4ncc(C#N)cc4Cl)C3)cc2c1C 10.1016/j.bmcl.2019.126678
CHEMBL4561636 181561 0 None 2 2 Rat 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 392 3 1 6 2.8 Cc1nnc2ccc(C(=O)NC3CN(c4ncc(C#N)cc4Cl)C3)cc2c1C 10.1016/j.bmcl.2019.126678
53375079 151339 24 None - 1 Human 6.9 pEC50 = 6.9 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 244 2 2 3 3.4 Clc1cccc(Nc2n[nH]c3cccnc23)c1 nan
CHEMBL3907429 151339 24 None - 1 Human 6.9 pEC50 = 6.9 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 244 2 2 3 3.4 Clc1cccc(Nc2n[nH]c3cccnc23)c1 nan
134190176 177475 0 None -2 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 266 2 2 6 2.5 Cc1noc2ccc(Nc3n[nH]c4nccnc34)cc12 10.1021/acs.jmedchem.8b00994
CHEMBL4451827 177475 0 None -2 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 266 2 2 6 2.5 Cc1noc2ccc(Nc3n[nH]c4nccnc34)cc12 10.1021/acs.jmedchem.8b00994
135126567 178837 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 407 4 1 5 3.8 Cc1nnc2ccc(C(=O)NC3CN(c4ncc(C5CC5)cc4Cl)C3)cc2c1C 10.1016/j.bmcl.2019.126678
CHEMBL4471979 178837 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 407 4 1 5 3.8 Cc1nnc2ccc(C(=O)NC3CN(c4ncc(C5CC5)cc4Cl)C3)cc2c1C 10.1016/j.bmcl.2019.126678
54670499 147185 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 423 6 1 6 3.6 CCc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1c(F)cccc1F nan
CHEMBL3808861 147185 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 423 6 1 6 3.6 CCc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1c(F)cccc1F nan
137641505 164835 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 318 2 1 5 3.9 COc1ccc2oc(-c3cc4ccccc4cn3)c/c(=N\O)c2c1 10.1021/acs.jmedchem.7b00991
CHEMBL4085967 164835 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 318 2 1 5 3.9 COc1ccc2oc(-c3cc4ccccc4cn3)c/c(=N\O)c2c1 10.1021/acs.jmedchem.7b00991
88889458 154781 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 407 5 1 6 3.7 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1cccc(Cl)c1 nan
CHEMBL3934325 154781 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 407 5 1 6 3.7 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1cccc(Cl)c1 nan
46836565 72314 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 297 2 2 5 3.5 Cc1cccc(Nc2nc3c(s2)CCCc2n[nH]cc2-3)n1 10.1021/jm200290z
CHEMBL1830900 72314 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 297 2 2 5 3.5 Cc1cccc(Nc2nc3c(s2)CCCc2n[nH]cc2-3)n1 10.1021/jm200290z
4644726 201807 10 None - 1 Human 5.9 pEC50 = 5.9 Functional
Activity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilizationActivity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilization
ChEMBL 266 2 1 2 3.6 O=C(Nc1ccc(Cl)c(Cl)c1)c1ccccn1 10.1021/jm9005065
CHEMBL549330 201807 10 None - 1 Human 5.9 pEC50 = 5.9 Functional
Activity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilizationActivity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilization
ChEMBL 266 2 1 2 3.6 O=C(Nc1ccc(Cl)c(Cl)c1)c1ccccn1 10.1021/jm9005065
87618914 165963 0 None 4 2 Human 5.9 pEC50 = 5.9 Functional
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 363 8 4 8 0.6 N[C@@H](CCP(=O)(O)C(O)c1cc([N+](=O)[O-])cc([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4098424 165963 0 None 4 2 Human 5.9 pEC50 = 5.9 Functional
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 363 8 4 8 0.6 N[C@@H](CCP(=O)(O)C(O)c1cc([N+](=O)[O-])cc([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
729510 31723 22 None -1 2 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as potentiation of EC20 glutamate-induced calcium mobilization after 2.5 minsPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as potentiation of EC20 glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 322 4 2 4 3.1 O=C(COc1ccccc1Br)c1ccc(O)cc1O 10.1016/j.bmcl.2011.09.131
CHEMBL1346011 31723 22 None -1 2 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as potentiation of EC20 glutamate-induced calcium mobilization after 2.5 minsPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as potentiation of EC20 glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 322 4 2 4 3.1 O=C(COc1ccccc1Br)c1ccc(O)cc1O 10.1016/j.bmcl.2011.09.131
46869950 66420 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 357 3 1 4 3.3 CC1(C)CC(=O)N(c2ccc(NC(=O)c3ccccn3)cc2Cl)C1=O 10.1021/jm200956q
CHEMBL1721009 66420 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 357 3 1 4 3.3 CC1(C)CC(=O)N(c2ccc(NC(=O)c3ccccn3)cc2Cl)C1=O 10.1021/jm200956q
54670497 149534 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 439 6 1 6 4.1 CCc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1c(F)cccc1Cl nan
CHEMBL3892535 149534 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 439 6 1 6 4.1 CCc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1c(F)cccc1Cl nan
127026067 144626 0 None -6 2 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human mGlu4 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu4 receptor by cell based calcium mobilization
ChEMBL 411 3 1 5 4.5 Cc1cccc2c1C(=O)N(c1ccc(NC(=O)c3ncsc3C)cc1Cl)C2=O 10.1016/j.bmcl.2015.12.104
CHEMBL3760018 144626 0 None -6 2 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human mGlu4 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu4 receptor by cell based calcium mobilization
ChEMBL 411 3 1 5 4.5 Cc1cccc2c1C(=O)N(c1ccc(NC(=O)c3ncsc3C)cc1Cl)C2=O 10.1016/j.bmcl.2015.12.104
53322767 64684 0 None -1 2 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 371 4 1 5 4.0 COc1ccccc1C(=O)n1ccc2cc(NC(=O)c3ccccn3)ccc21 10.1021/jm101271s
CHEMBL1672257 64684 0 None -1 2 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 371 4 1 5 4.0 COc1ccccc1C(=O)n1ccc2cc(NC(=O)c3ccccn3)ccc21 10.1021/jm101271s
53324349 64683 0 None 1 2 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 393 3 1 4 4.8 O=C(Nc1ccc2c(ccn2C(=O)c2ccc(F)cc2Cl)c1)c1ccccn1 10.1021/jm101271s
CHEMBL1672256 64683 0 None 1 2 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 393 3 1 4 4.8 O=C(Nc1ccc2c(ccn2C(=O)c2ccc(F)cc2Cl)c1)c1ccccn1 10.1021/jm101271s
53374212 159485 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 228 2 2 3 2.8 Fc1ccc(Nc2n[nH]c3cccnc23)cc1 nan
CHEMBL3972978 159485 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 228 2 2 3 2.8 Fc1ccc(Nc2n[nH]c3cccnc23)cc1 nan
137653133 165686 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
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 263 2 1 3 3.9 O/N=c1\cc(/C=C/c2ccccc2)oc2ccccc12 10.1021/acs.jmedchem.7b00991
CHEMBL4095448 165686 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
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 263 2 1 3 3.9 O/N=c1\cc(/C=C/c2ccccc2)oc2ccccc12 10.1021/acs.jmedchem.7b00991
145982965 172160 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 265 2 2 6 2.0 Cn1nnc2ccc(Nc3n[nH]c4cccnc34)cc21 10.1016/j.bmcl.2018.06.034
CHEMBL4237744 172160 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 265 2 2 6 2.0 Cn1nnc2ccc(Nc3n[nH]c4cccnc34)cc21 10.1016/j.bmcl.2018.06.034
52934736 147154 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 356 4 1 6 2.4 Cc1ccc(S(=O)(=O)n2cc(NC(=O)c3ccccn3)cn2)cc1C nan
CHEMBL3808486 147154 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 356 4 1 6 2.4 Cc1ccc(S(=O)(=O)n2cc(NC(=O)c3ccccn3)cn2)cc1C nan
1314024 50406 12 None -1 2 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 448 5 2 4 5.2 COc1cc(NC(=O)c2ccc(Br)o2)ccc1NC(=O)c1ccccc1Cl 10.1021/jm101271s
CHEMBL1509597 50406 12 None -1 2 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 448 5 2 4 5.2 COc1cc(NC(=O)c2ccc(Br)o2)ccc1NC(=O)c1ccccc1Cl 10.1021/jm101271s
53375177 159842 1 None - 1 Human 5.8 pEC50 = 5.8 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 210 2 2 3 2.7 c1ccc(Nc2n[nH]c3cccnc23)cc1 nan
CHEMBL3975979 159842 1 None - 1 Human 5.8 pEC50 = 5.8 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 210 2 2 3 2.7 c1ccc(Nc2n[nH]c3cccnc23)cc1 nan
53375176 149821 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 278 2 2 3 3.7 FC(F)(F)c1cccc(Nc2n[nH]c3cccnc23)c1 nan
CHEMBL3894951 149821 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 278 2 2 3 3.7 FC(F)(F)c1cccc(Nc2n[nH]c3cccnc23)c1 nan
53374400 155180 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 264 2 2 3 3.1 Fc1cc(Nc2n[nH]c3cccnc23)cc(F)c1F nan
CHEMBL3937590 155180 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 264 2 2 3 3.1 Fc1cc(Nc2n[nH]c3cccnc23)cc(F)c1F nan
135126260 178597 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 399 5 1 6 2.9 Cc1nnc2ccc(C(=O)NC3CN(c4ccc(OC(F)F)nc4)C3)cc2c1C 10.1016/j.bmcl.2019.126678
CHEMBL4468494 178597 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 399 5 1 6 2.9 Cc1nnc2ccc(C(=O)NC3CN(c4ccc(OC(F)F)nc4)C3)cc2c1C 10.1016/j.bmcl.2019.126678
52934736 147154 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 356 4 1 6 2.4 Cc1ccc(S(=O)(=O)n2cc(NC(=O)c3ccccn3)cn2)cc1C 10.1016/j.bmcl.2016.05.029
CHEMBL3808486 147154 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 356 4 1 6 2.4 Cc1ccc(S(=O)(=O)n2cc(NC(=O)c3ccccn3)cn2)cc1C 10.1016/j.bmcl.2016.05.029
52934736 147154 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 356 4 1 6 2.4 Cc1ccc(S(=O)(=O)n2cc(NC(=O)c3ccccn3)cn2)cc1C 10.1016/j.bmcl.2016.05.029
CHEMBL3808486 147154 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 356 4 1 6 2.4 Cc1ccc(S(=O)(=O)n2cc(NC(=O)c3ccccn3)cn2)cc1C 10.1016/j.bmcl.2016.05.029
53373763 157833 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 245 2 2 4 2.8 Clc1cc(Nc2n[nH]c3cccnc23)ccn1 nan
CHEMBL3958765 157833 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 245 2 2 4 2.8 Clc1cc(Nc2n[nH]c3cccnc23)ccn1 nan
16061421 163300 0 None 1 3 Human 6.8 pEC50 = 6.8 Functional
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 308 7 4 7 0.3 N[C@@H](CCP(=O)(O)C(O)c1ccc([N+](=O)[O-])o1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4067923 163300 0 None 1 3 Human 6.8 pEC50 = 6.8 Functional
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 308 7 4 7 0.3 N[C@@H](CCP(=O)(O)C(O)c1ccc([N+](=O)[O-])o1)C(=O)O 10.1021/acs.jmedchem.7b01438
122197940 166786 0 None 43 3 Rat 6.8 pEC50 = 6.8 Functional
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 503 10 5 7 0.8 COc1cc(C(O)P(=O)(O)CC[C@@H](N)C(=O)O)cc(I)c1OCC(=O)O nan
CHEMBL4107881 166786 0 None 43 3 Rat 6.8 pEC50 = 6.8 Functional
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 503 10 5 7 0.8 COc1cc(C(O)P(=O)(O)CC[C@@H](N)C(=O)O)cc(I)c1OCC(=O)O nan
54670499 147185 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 423 6 1 6 3.6 CCc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1c(F)cccc1F 10.1016/j.bmcl.2016.05.029
CHEMBL3808861 147185 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 423 6 1 6 3.6 CCc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1c(F)cccc1F 10.1016/j.bmcl.2016.05.029
137658747 165932 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 440 5 1 7 4.1 O/N=c1\cc(-c2cc3cccn3cn2)oc2ccc(OCCN3CCC(F)(F)CC3)cc12 10.1021/acs.jmedchem.7b00991
CHEMBL4098128 165932 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 440 5 1 7 4.1 O/N=c1\cc(-c2cc3cccn3cn2)oc2ccc(OCCN3CCC(F)(F)CC3)cc12 10.1021/acs.jmedchem.7b00991
44191180 202372 0 None -1 2 Human 5.8 pEC50 = 5.8 Functional
Activity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilizationActivity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilization
ChEMBL 284 2 1 2 3.5 O=C(Nc1ccc(F)c(C(F)(F)F)c1)c1ccccn1 10.1021/jm9005065
CHEMBL555454 202372 0 None -1 2 Human 5.8 pEC50 = 5.8 Functional
Activity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilizationActivity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilization
ChEMBL 284 2 1 2 3.5 O=C(Nc1ccc(F)c(C(F)(F)F)c1)c1ccccn1 10.1021/jm9005065
57765529 162616 0 None 3 2 Human 5.8 pEC50 = 5.8 Functional
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 363 8 4 8 0.6 N[C@@H](CCP(=O)(O)C(O)c1ccc([N+](=O)[O-])cc1[N+](=O)[O-])C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4060017 162616 0 None 3 2 Human 5.8 pEC50 = 5.8 Functional
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 363 8 4 8 0.6 N[C@@H](CCP(=O)(O)C(O)c1ccc([N+](=O)[O-])cc1[N+](=O)[O-])C(=O)O 10.1021/acs.jmedchem.7b01438
46918015 162647 0 None 3 4 Human 5.8 pEC50 = 5.8 Functional
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 334 7 5 7 0.4 N[C@@H](CCP(=O)(O)C(O)c1ccc(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4060360 162647 0 None 3 4 Human 5.8 pEC50 = 5.8 Functional
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 334 7 5 7 0.4 N[C@@H](CCP(=O)(O)C(O)c1ccc(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
24780091 163848 0 None 2 2 Human 4.8 pEC50 = 4.8 Functional
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 341 6 4 4 1.8 N[C@@H](CCP(=O)(O)C(O)c1ccc(C(F)(F)F)cc1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4074114 163848 0 None 2 2 Human 4.8 pEC50 = 4.8 Functional
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 341 6 4 4 1.8 N[C@@H](CCP(=O)(O)C(O)c1ccc(C(F)(F)F)cc1)C(=O)O 10.1021/acs.jmedchem.7b01438
137661492 166272 0 None 1 2 Human 4.8 pEC50 = 4.8 Functional
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 295 6 5 7 -0.2 Nc1ncc(C(O)P(=O)(O)CC[C@H](N)C(=O)O)s1 10.1021/acs.jmedchem.7b01438
CHEMBL4101796 166272 0 None 1 2 Human 4.8 pEC50 = 4.8 Functional
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 295 6 5 7 -0.2 Nc1ncc(C(O)P(=O)(O)CC[C@H](N)C(=O)O)s1 10.1021/acs.jmedchem.7b01438
1310 9095 110 None -1513 17 Human 4.8 pEC50 = 4.8 Functional
Agonistic activity at mGlu4a receptor expressed in CHO cellsAgonistic activity at mGlu4a receptor expressed in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm9602569
1369 9095 110 None -1513 17 Human 4.8 pEC50 = 4.8 Functional
Agonistic activity at mGlu4a receptor expressed in CHO cellsAgonistic activity at mGlu4a receptor expressed in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm9602569
33032 9095 110 None -1513 17 Human 4.8 pEC50 = 4.8 Functional
Agonistic activity at mGlu4a receptor expressed in CHO cellsAgonistic activity at mGlu4a receptor expressed in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm9602569
44272391 9095 110 None -1513 17 Human 4.8 pEC50 = 4.8 Functional
Agonistic activity at mGlu4a receptor expressed in CHO cellsAgonistic activity at mGlu4a receptor expressed in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm9602569
88747398 9095 110 None -1513 17 Human 4.8 pEC50 = 4.8 Functional
Agonistic activity at mGlu4a receptor expressed in CHO cellsAgonistic activity at mGlu4a receptor expressed in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm9602569
CHEMBL575060 9095 110 None -1513 17 Human 4.8 pEC50 = 4.8 Functional
Agonistic activity at mGlu4a receptor expressed in CHO cellsAgonistic activity at mGlu4a receptor expressed in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm9602569
DB00142 9095 110 None -1513 17 Human 4.8 pEC50 = 4.8 Functional
Agonistic activity at mGlu4a receptor expressed in CHO cellsAgonistic activity at mGlu4a receptor expressed in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm9602569
52935622 150388 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 376 4 1 6 2.7 Cc1cc(S(=O)(=O)n2cc(NC(=O)c3ccccn3)cn2)ccc1Cl nan
CHEMBL3899605 150388 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 376 4 1 6 2.7 Cc1cc(S(=O)(=O)n2cc(NC(=O)c3ccccn3)cn2)ccc1Cl nan
121231187 157022 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 355 4 2 5 4.7 Fc1cc(Nc2n[nH]c3cccnc23)ccc1Oc1ccc(Cl)cn1 nan
CHEMBL3952349 157022 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 355 4 2 5 4.7 Fc1cc(Nc2n[nH]c3cccnc23)ccc1Oc1ccc(Cl)cn1 nan
54670499 147185 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 423 6 1 6 3.6 CCc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1c(F)cccc1F 10.1016/j.bmcl.2016.05.029
CHEMBL3808861 147185 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 423 6 1 6 3.6 CCc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1c(F)cccc1F 10.1016/j.bmcl.2016.05.029
54670688 152822 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 391 5 1 6 3.2 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccc(F)cc1 nan
CHEMBL3918824 152822 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 391 5 1 6 3.2 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccc(F)cc1 nan
51003236 64672 0 None -1 2 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 386 5 2 3 5.1 COc1cc(NC(=O)C2CCCCC2)ccc1NC(=O)c1ccccc1Cl 10.1021/jm101271s
CHEMBL1672237 64672 0 None -1 2 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 386 5 2 3 5.1 COc1cc(NC(=O)C2CCCCC2)ccc1NC(=O)c1ccccc1Cl 10.1021/jm101271s
121231188 152076 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 370 4 2 4 5.8 Clc1ccc(Oc2ccc(Nc3n[nH]c4cccnc34)cc2Cl)cc1 nan
CHEMBL3913098 152076 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 370 4 2 4 5.8 Clc1ccc(Oc2ccc(Nc3n[nH]c4cccnc34)cc2Cl)cc1 nan
53373769 152146 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 314 3 2 5 3.4 Clc1cc(Nc2n[nH]c3cccnc23)cnc1N1CCCC1 nan
CHEMBL3913712 152146 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 314 3 2 5 3.4 Clc1cc(Nc2n[nH]c3cccnc23)cnc1N1CCCC1 nan
53373766 159793 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 263 2 2 4 2.9 Fc1ccc(Nc2n[nH]c3nccnc23)cc1Cl nan
CHEMBL3975540 159793 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 263 2 2 4 2.9 Fc1ccc(Nc2n[nH]c3nccnc23)cc1Cl nan
134190222 179269 0 None -12 2 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 283 2 2 5 3.3 Cc1noc2ccc(Nc3n[nH]c4cc(F)cnc34)cc12 10.1021/acs.jmedchem.8b00994
CHEMBL4483053 179269 0 None -12 2 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 283 2 2 5 3.3 Cc1noc2ccc(Nc3n[nH]c4cc(F)cnc34)cc12 10.1021/acs.jmedchem.8b00994
127028298 144582 0 None -6 2 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human mGlu4 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu4 receptor by cell based calcium mobilization
ChEMBL 414 3 1 5 3.8 Cn1ccnc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3759647 144582 0 None -6 2 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human mGlu4 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu4 receptor by cell based calcium mobilization
ChEMBL 414 3 1 5 3.8 Cn1ccnc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
46869951 66073 0 None 2 2 Human 6.8 pEC50 = 6.8 Functional
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 397 3 1 4 4.2 O=C(Nc1ccc(N2C(=O)CC3(CCCCC3)C2=O)c(Cl)c1)c1ccccn1 10.1021/jm200956q
CHEMBL1705230 66073 0 None 2 2 Human 6.8 pEC50 = 6.8 Functional
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 397 3 1 4 4.2 O=C(Nc1ccc(N2C(=O)CC3(CCCCC3)C2=O)c(Cl)c1)c1ccccn1 10.1021/jm200956q
137651515 164228 0 None 2 2 Human 4.8 pEC50 = 4.8 Functional
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 333 7 6 6 0.2 N[C@@H](CCP(=O)(O)C(O)c1ccc(O)c(C(=O)O)c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4079075 164228 0 None 2 2 Human 4.8 pEC50 = 4.8 Functional
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 333 7 6 6 0.2 N[C@@H](CCP(=O)(O)C(O)c1ccc(O)c(C(=O)O)c1)C(=O)O 10.1021/acs.jmedchem.7b01438
49862579 21873 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
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 Nc1cncc(/C=C/c2ccccc2)n1 10.1016/j.bmcl.2010.06.078
CHEMBL1209589 21873 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
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 Nc1cncc(/C=C/c2ccccc2)n1 10.1016/j.bmcl.2010.06.078
134190222 179269 0 None -12 2 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 283 2 2 5 3.3 Cc1noc2ccc(Nc3n[nH]c4cc(F)cnc34)cc12 10.1021/acs.jmedchem.8b00994
CHEMBL4483053 179269 0 None -12 2 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 283 2 2 5 3.3 Cc1noc2ccc(Nc3n[nH]c4cc(F)cnc34)cc12 10.1021/acs.jmedchem.8b00994
45111050 22614 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilization
ChEMBL 395 5 2 4 4.1 Cc1cc(C)c(NS(=O)(=O)c2ccc(NC(=O)c3ccccn3)cc2)c(C)c1 10.1016/j.bmcl.2010.07.007
CHEMBL1223014 22614 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilization
ChEMBL 395 5 2 4 4.1 Cc1cc(C)c(NS(=O)(=O)c2ccc(NC(=O)c3ccccn3)cc2)c(C)c1 10.1016/j.bmcl.2010.07.007
92044496 162746 0 None 2 4 Human 6.8 pEC50 = 6.8 Functional
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 324 7 4 7 0.7 N[C@@H](CCP(=O)(O)C(O)c1csc([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4061423 162746 0 None 2 4 Human 6.8 pEC50 = 6.8 Functional
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 324 7 4 7 0.7 N[C@@H](CCP(=O)(O)C(O)c1csc([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
145946669 174333 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 318 4 2 5 3.9 CCn1nc(C2CC2)c2ccc(Nc3n[nH]c4ncccc34)cc21 10.1016/j.bmcl.2018.06.034
CHEMBL4241662 174333 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 318 4 2 5 3.9 CCn1nc(C2CC2)c2ccc(Nc3n[nH]c4ncccc34)cc21 10.1016/j.bmcl.2018.06.034
CHEMBL4300337 174333 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 318 4 2 5 3.9 CCn1nc(C2CC2)c2ccc(Nc3n[nH]c4ncccc34)cc21 10.1016/j.bmcl.2018.06.034
89115789 162867 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 351 5 1 7 3.1 COCCOc1ccc2oc(-c3cc4cccn4cn3)c/c(=N\O)c2c1 10.1021/acs.jmedchem.7b00991
CHEMBL4062968 162867 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 351 5 1 7 3.1 COCCOc1ccc2oc(-c3cc4cccn4cn3)c/c(=N\O)c2c1 10.1021/acs.jmedchem.7b00991
57765531 163910 0 None 1 2 Human 5.8 pEC50 = 5.8 Functional
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 348 8 4 7 0.7 COc1ccc(C(O)P(=O)(O)CC[C@H](N)C(=O)O)cc1[N+](=O)[O-] 10.1021/acs.jmedchem.7b01438
CHEMBL4075070 163910 0 None 1 2 Human 5.8 pEC50 = 5.8 Functional
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 348 8 4 7 0.7 COc1ccc(C(O)P(=O)(O)CC[C@H](N)C(=O)O)cc1[N+](=O)[O-] 10.1021/acs.jmedchem.7b01438
57765572 164103 0 None 3 2 Human 5.8 pEC50 = 5.8 Functional
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 331 6 4 5 1.4 N[C@@H](CCP(=O)(O)C(O)c1ccc(C(F)(F)F)o1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4077371 164103 0 None 3 2 Human 5.8 pEC50 = 5.8 Functional
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 331 6 4 5 1.4 N[C@@H](CCP(=O)(O)C(O)c1ccc(C(F)(F)F)o1)C(=O)O 10.1021/acs.jmedchem.7b01438
49862523 21855 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 225 2 1 3 2.8 Cc1nc(N)nc(/C=C/c2ccccc2)c1C 10.1016/j.bmcl.2010.06.078
CHEMBL1209515 21855 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 225 2 1 3 2.8 Cc1nc(N)nc(/C=C/c2ccccc2)c1C 10.1016/j.bmcl.2010.06.078
49862527 21858 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 231 2 1 3 2.9 Nc1ncc(Cl)c(/C=C/c2ccccc2)n1 10.1016/j.bmcl.2010.06.078
CHEMBL1209520 21858 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 231 2 1 3 2.9 Nc1ncc(Cl)c(/C=C/c2ccccc2)n1 10.1016/j.bmcl.2010.06.078
51003282 64675 0 None 1 2 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 351 4 2 3 4.2 O=C(Nc1ccc(NC(=O)c2ccccc2Cl)cc1)c1ccccn1 10.1021/jm101271s
CHEMBL1672240 64675 0 None 1 2 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 351 4 2 3 4.2 O=C(Nc1ccc(NC(=O)c2ccccc2Cl)cc1)c1ccccn1 10.1021/jm101271s
54670500 154066 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 373 4 1 6 3.2 Cc1ccc(S(=O)(=O)c2sc(NC(=O)c3ccccn3)nc2C)cc1 nan
CHEMBL3928878 154066 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 373 4 1 6 3.2 Cc1ccc(S(=O)(=O)c2sc(NC(=O)c3ccccn3)nc2C)cc1 nan
52914665 147173 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 375 4 1 5 3.3 Cc1cc(S(=O)(=O)n2ccc(NC(=O)c3ccccn3)c2)ccc1Cl 10.1016/j.bmcl.2016.05.029
CHEMBL3808648 147173 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 375 4 1 5 3.3 Cc1cc(S(=O)(=O)n2ccc(NC(=O)c3ccccn3)c2)ccc1Cl 10.1016/j.bmcl.2016.05.029
52935623 158594 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 364 4 1 6 2.0 O=C(Nc1cnn(S(=O)(=O)c2ccc(F)cc2F)c1)c1ccccn1 nan
CHEMBL3965291 158594 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 364 4 1 6 2.0 O=C(Nc1cnn(S(=O)(=O)c2ccc(F)cc2F)c1)c1ccccn1 nan
127047343 146725 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 146725 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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
52934738 159621 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 342 4 1 6 2.1 Cc1cccc(S(=O)(=O)n2cc(NC(=O)c3ccccn3)cn2)c1 nan
CHEMBL3974101 159621 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 342 4 1 6 2.1 Cc1cccc(S(=O)(=O)n2cc(NC(=O)c3ccccn3)cn2)c1 nan
52914665 147173 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 375 4 1 5 3.3 Cc1cc(S(=O)(=O)n2ccc(NC(=O)c3ccccn3)c2)ccc1Cl 10.1016/j.bmcl.2016.05.029
CHEMBL3808648 147173 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 375 4 1 5 3.3 Cc1cc(S(=O)(=O)n2ccc(NC(=O)c3ccccn3)c2)ccc1Cl 10.1016/j.bmcl.2016.05.029
136503359 164153 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 372 2 1 5 4.8 O/N=c1\cc(-c2cc3ccccc3cn2)oc2ccc(OC(F)(F)F)cc12 10.1021/acs.jmedchem.7b00991
CHEMBL4078081 164153 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 372 2 1 5 4.8 O/N=c1\cc(-c2cc3ccccc3cn2)oc2ccc(OC(F)(F)F)cc12 10.1021/acs.jmedchem.7b00991
134191531 187390 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 332 5 2 5 4.1 CCN(CC)c1nccc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1016/j.bmcl.2018.10.050
CHEMBL4754632 187390 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 332 5 2 5 4.1 CCN(CC)c1nccc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1016/j.bmcl.2018.10.050
53375180 158166 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 258 2 2 3 3.7 Cc1cc(Nc2n[nH]c3cccnc23)ccc1Cl nan
CHEMBL3961520 158166 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 258 2 2 3 3.7 Cc1cc(Nc2n[nH]c3cccnc23)ccc1Cl nan
49862696 21906 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
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 198 2 1 4 1.6 Nc1nccc(/C=C/c2cccnc2)n1 10.1016/j.bmcl.2010.06.078
CHEMBL1209744 21906 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
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 198 2 1 4 1.6 Nc1nccc(/C=C/c2cccnc2)n1 10.1016/j.bmcl.2010.06.078
89106981 162817 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 447 6 1 8 3.4 CN(C)C1CCN(CCOc2ccc3oc(-c4cc5cccn5cn4)c/c(=N\O)c3c2)CC1 10.1021/acs.jmedchem.7b00991
CHEMBL4062426 162817 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 447 6 1 8 3.4 CN(C)C1CCN(CCOc2ccc3oc(-c4cc5cccn5cn4)c/c(=N\O)c3c2)CC1 10.1021/acs.jmedchem.7b00991
53374403 150504 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 258 2 2 3 3.7 Cc1ccc(Nc2n[nH]c3cccnc23)cc1Cl nan
CHEMBL3900600 150504 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 258 2 2 3 3.7 Cc1ccc(Nc2n[nH]c3cccnc23)cc1Cl nan
53324349 64683 0 None -1 2 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 393 3 1 4 4.8 O=C(Nc1ccc2c(ccn2C(=O)c2ccc(F)cc2Cl)c1)c1ccccn1 10.1021/jm101271s
CHEMBL1672256 64683 0 None -1 2 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 393 3 1 4 4.8 O=C(Nc1ccc2c(ccn2C(=O)c2ccc(F)cc2Cl)c1)c1ccccn1 10.1021/jm101271s
122197949 166615 0 None 15 3 Rat 5.8 pEC50 = 5.8 Functional
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 391 11 5 7 0.6 CCOc1cc(C(O)P(=O)(O)CC[C@@H](N)C(=O)O)ccc1OCC(=O)O nan
CHEMBL4106501 166615 0 None 15 3 Rat 5.8 pEC50 = 5.8 Functional
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 391 11 5 7 0.6 CCOc1cc(C(O)P(=O)(O)CC[C@@H](N)C(=O)O)ccc1OCC(=O)O nan
51003325 64680 0 None -1 2 Rat 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 403 4 2 3 5.0 O=C(Nc1ccc(NC(=O)c2ccc(F)cc2Cl)c(Cl)c1)c1ccccn1 10.1021/jm101271s
CHEMBL1672245 64680 0 None -1 2 Rat 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 403 4 2 3 5.0 O=C(Nc1ccc(NC(=O)c2ccc(F)cc2Cl)c(Cl)c1)c1ccccn1 10.1021/jm101271s
53373662 155216 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 240 3 2 4 2.7 COc1cccc(Nc2n[nH]c3cccnc23)c1 nan
CHEMBL3937846 155216 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 240 3 2 4 2.7 COc1cccc(Nc2n[nH]c3cccnc23)c1 nan
134191546 187178 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 330 3 2 5 3.9 c1cnc2c(Nc3ccc4c(N5CCCC5)nccc4c3)n[nH]c2c1 10.1016/j.bmcl.2018.10.050
CHEMBL4751992 187178 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 330 3 2 5 3.9 c1cnc2c(Nc3ccc4c(N5CCCC5)nccc4c3)n[nH]c2c1 10.1016/j.bmcl.2018.10.050
137644474 165177 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 457 4 1 9 4.4 O/N=c1\cc(-c2cc3sccc3cn2)oc2ccc(O[C@@H]3CCN(c4ccncn4)C3)cc12 10.1021/acs.jmedchem.7b00991
CHEMBL4090015 165177 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 457 4 1 9 4.4 O/N=c1\cc(-c2cc3sccc3cn2)oc2ccc(O[C@@H]3CCN(c4ccncn4)C3)cc12 10.1021/acs.jmedchem.7b00991
52935411 152196 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 358 5 1 7 1.8 COc1ccc(S(=O)(=O)n2cc(NC(=O)c3ccccn3)cn2)cc1 nan
CHEMBL3914060 152196 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 358 5 1 7 1.8 COc1ccc(S(=O)(=O)n2cc(NC(=O)c3ccccn3)cn2)cc1 nan
54670122 154750 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 395 5 1 6 3.0 O=C(Nc1ncc(S(=O)(=O)Cc2c(F)cccc2F)s1)c1ccccn1 nan
CHEMBL3934074 154750 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 395 5 1 6 3.0 O=C(Nc1ncc(S(=O)(=O)Cc2c(F)cccc2F)s1)c1ccccn1 nan
1408 7053 31 None 1 7 Human 5.8 pEC50 = 5.8 Functional
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 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O 10.1021/acs.jmedchem.7b01438
6604820 7053 31 None 1 7 Human 5.8 pEC50 = 5.8 Functional
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 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL285043 7053 31 None 1 7 Human 5.8 pEC50 = 5.8 Functional
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 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL288635 7053 31 None 1 7 Human 5.8 pEC50 = 5.8 Functional
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 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O 10.1021/acs.jmedchem.7b01438
137647077 164776 0 None 1 3 Human 5.8 pEC50 = 5.8 Functional
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 348 8 4 7 0.7 COc1ccc([C@H](O)P(=O)(O)CC[C@H](N)C(=O)O)cc1[N+](=O)[O-] 10.1021/acs.jmedchem.7b01438
CHEMBL4085327 164776 0 None 1 3 Human 5.8 pEC50 = 5.8 Functional
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 348 8 4 7 0.7 COc1ccc([C@H](O)P(=O)(O)CC[C@H](N)C(=O)O)cc1[N+](=O)[O-] 10.1021/acs.jmedchem.7b01438
135411610 10788 10 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 278 3 2 5 3.1 Oc1ccc(cc1)/C=N/Nc1nc2ccccc2nc1C 10.1021/jm200290z
135773804 10788 10 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 278 3 2 5 3.1 Oc1ccc(cc1)/C=N/Nc1nc2ccccc2nc1C 10.1021/jm200290z
6228 10788 10 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 278 3 2 5 3.1 Oc1ccc(cc1)/C=N/Nc1nc2ccccc2nc1C 10.1021/jm200290z
CHEMBL515763 10788 10 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 278 3 2 5 3.1 Oc1ccc(cc1)/C=N/Nc1nc2ccccc2nc1C 10.1021/jm200290z
1608415 14591 8 None 3 3 Rat 4.8 pEC50 = 4.8 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 239 7 4 4 -0.5 N[C@H](CCP(=O)(O)CCC(=O)O)C(=O)O 10.1021/jm901523t
44660046 14591 8 None 3 3 Rat 4.8 pEC50 = 4.8 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 239 7 4 4 -0.5 N[C@H](CCP(=O)(O)CCC(=O)O)C(=O)O 10.1021/jm901523t
CHEMBL1089514 14591 8 None 3 3 Rat 4.8 pEC50 = 4.8 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 239 7 4 4 -0.5 N[C@H](CCP(=O)(O)CCC(=O)O)C(=O)O 10.1021/jm901523t
87304250 165928 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 419 5 1 8 2.7 CN1CCN(CCOc2ccc3oc(-c4cc5cccn5cn4)c/c(=N\O)c3c2)CC1 10.1021/acs.jmedchem.7b00991
CHEMBL4098112 165928 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 419 5 1 8 2.7 CN1CCN(CCOc2ccc3oc(-c4cc5cccn5cn4)c/c(=N\O)c3c2)CC1 10.1021/acs.jmedchem.7b00991
136503360 166445 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 366 1 1 4 4.7 O/N=c1\cc(-c2cc3ccccc3cn2)oc2cc(Br)ccc12 10.1021/acs.jmedchem.7b00991
CHEMBL4103895 166445 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 366 1 1 4 4.7 O/N=c1\cc(-c2cc3ccccc3cn2)oc2cc(Br)ccc12 10.1021/acs.jmedchem.7b00991
54670963 149522 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 463 5 1 6 4.1 O=C(Nc1nc(C(F)(F)F)c(S(=O)(=O)Cc2ccc(F)cc2F)s1)c1ccccn1 nan
CHEMBL3892447 149522 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 463 5 1 6 4.1 O=C(Nc1nc(C(F)(F)F)c(S(=O)(=O)Cc2ccc(F)cc2F)s1)c1ccccn1 nan
51347212 147193 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 375 5 1 5 3.2 O=C(Nc1ccn(S(=O)(=O)Cc2ccccc2Cl)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
CHEMBL3808951 147193 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 375 5 1 5 3.2 O=C(Nc1ccn(S(=O)(=O)Cc2ccccc2Cl)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
51003372 74581 0 None 1 2 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 358 4 2 5 3.7 O=C(Nc1ccc(NC(=O)c2cncs2)c(Cl)c1)c1ccccn1 10.1021/jm101271s
CHEMBL1909433 74581 0 None 1 2 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 358 4 2 5 3.7 O=C(Nc1ccc(NC(=O)c2cncs2)c(Cl)c1)c1ccccn1 10.1021/jm101271s
162651504 187062 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 345 3 2 5 4.1 O=c1c2ccc(Nc3n[nH]c4cccnc34)cc2ccn1C1CCCC1 10.1016/j.bmcl.2018.10.050
CHEMBL4750744 187062 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 345 3 2 5 4.1 O=c1c2ccc(Nc3n[nH]c4cccnc34)cc2ccn1C1CCCC1 10.1016/j.bmcl.2018.10.050
53374000 157439 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 258 3 2 3 3.2 Clc1cccc(CNc2n[nH]c3cccnc23)c1 nan
CHEMBL3955656 157439 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 258 3 2 3 3.2 Clc1cccc(CNc2n[nH]c3cccnc23)c1 nan
51347212 147193 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 375 5 1 5 3.2 O=C(Nc1ccn(S(=O)(=O)Cc2ccccc2Cl)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
CHEMBL3808951 147193 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 375 5 1 5 3.2 O=C(Nc1ccn(S(=O)(=O)Cc2ccccc2Cl)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
135125802 176999 0 None 2 2 Rat 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 385 3 1 5 3.1 Cc1nnc2ccc(C(=O)NC3CN(c4ncc(F)cc4Cl)C3)cc2c1C 10.1016/j.bmcl.2019.126678
CHEMBL4445506 176999 0 None 2 2 Rat 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 385 3 1 5 3.1 Cc1nnc2ccc(C(=O)NC3CN(c4ncc(F)cc4Cl)C3)cc2c1C 10.1016/j.bmcl.2019.126678
1408 7053 31 None -1 7 Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O 10.1021/jm901523t
6604820 7053 31 None -1 7 Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O 10.1021/jm901523t
CHEMBL285043 7053 31 None -1 7 Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O 10.1021/jm901523t
CHEMBL288635 7053 31 None -1 7 Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O 10.1021/jm901523t
52934739 160315 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 364 4 1 6 2.0 O=C(Nc1cnn(S(=O)(=O)c2ccc(F)c(F)c2)c1)c1ccccn1 nan
CHEMBL3980020 160315 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 364 4 1 6 2.0 O=C(Nc1cnn(S(=O)(=O)c2ccc(F)c(F)c2)c1)c1ccccn1 nan
136503361 164573 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 392 4 1 4 5.7 O/N=c1\cc(-c2cc3ccccc3cn2)oc2cc(CCc3ccccc3)ccc12 10.1021/acs.jmedchem.7b00991
CHEMBL4083118 164573 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 392 4 1 4 5.7 O/N=c1\cc(-c2cc3ccccc3cn2)oc2cc(CCc3ccccc3)ccc12 10.1021/acs.jmedchem.7b00991
162672655 189914 0 None 7 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 399 3 1 5 3.9 Cc1nc(C(=O)Nc2cc(F)c(N3C(=O)C4=C(CCCC4)C3=O)cc2C)cs1 10.1016/j.bmcl.2020.127724
CHEMBL4795139 189914 0 None 7 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 399 3 1 5 3.9 Cc1nc(C(=O)Nc2cc(F)c(N3C(=O)C4=C(CCCC4)C3=O)cc2C)cs1 10.1016/j.bmcl.2020.127724
57765615 164346 0 None 1 2 Human 5.8 pEC50 = 5.8 Functional
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 363 8 4 8 0.6 N[C@@H](CCP(=O)(O)C(O)c1c([N+](=O)[O-])cccc1[N+](=O)[O-])C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4080400 164346 0 None 1 2 Human 5.8 pEC50 = 5.8 Functional
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 363 8 4 8 0.6 N[C@@H](CCP(=O)(O)C(O)c1c([N+](=O)[O-])cccc1[N+](=O)[O-])C(=O)O 10.1021/acs.jmedchem.7b01438
45111049 22615 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilization
ChEMBL 353 5 2 4 3.1 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1)c1ccccn1 10.1016/j.bmcl.2010.07.007
CHEMBL1223015 22615 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilization
ChEMBL 353 5 2 4 3.1 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1)c1ccccn1 10.1016/j.bmcl.2010.07.007
53373878 159858 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 238 2 2 3 3.3 Cc1cc(C)cc(Nc2n[nH]c3cccnc23)c1 nan
CHEMBL3976080 159858 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 238 2 2 3 3.3 Cc1cc(C)cc(Nc2n[nH]c3cccnc23)c1 nan
52935624 150763 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 382 4 1 6 2.2 O=C(Nc1cnn(S(=O)(=O)c2cc(F)c(F)cc2F)c1)c1ccccn1 nan
CHEMBL3902753 150763 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 382 4 1 6 2.2 O=C(Nc1cnn(S(=O)(=O)c2cc(F)c(F)cc2F)c1)c1ccccn1 nan
51003233 64670 0 None -1 2 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 382 5 2 5 3.6 COc1cc(NC(=O)c2cnccn2)ccc1NC(=O)c1ccccc1Cl 10.1021/jm101271s
CHEMBL1672235 64670 0 None -1 2 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 382 5 2 5 3.6 COc1cc(NC(=O)c2cnccn2)ccc1NC(=O)c1ccccc1Cl 10.1021/jm101271s
46853682 75559 0 None 1 2 Human 6.8 pEC50 = 6.8 Functional
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 416 3 1 7 1.6 O=C(Nc1ccc(N2S(=O)(=O)c3ccccc3S2(=O)=O)cc1)c1ccncn1 10.1021/jm200956q
CHEMBL1921950 75559 0 None 1 2 Human 6.8 pEC50 = 6.8 Functional
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 416 3 1 7 1.6 O=C(Nc1ccc(N2S(=O)(=O)c3ccccc3S2(=O)=O)cc1)c1ccncn1 10.1021/jm200956q
134191633 188160 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 329 2 2 4 4.3 FC(F)(F)c1nccc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1016/j.bmcl.2018.10.050
CHEMBL4763355 188160 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 329 2 2 4 4.3 FC(F)(F)c1nccc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1016/j.bmcl.2018.10.050
44361401 38115 0 None -398 5 Rat 5.8 pEC50 = 5.8 Functional
Metabotropic glutamate receptor 4 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 4 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 175 3 4 4 -1.9 N[C@H](C(=O)O)[C@H]1[C@@H](O)[C@@H]1C(=O)O 10.1021/jm030967o
CHEMBL140197 38115 0 None -398 5 Rat 5.8 pEC50 = 5.8 Functional
Metabotropic glutamate receptor 4 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 4 agonist activity to influence 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
70683517 80998 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 400 6 0 6 3.8 c1ccc(-n2cc(-c3ccnc4cc(OCCN5CCOCC5)ccc34)cn2)cc1 10.1016/j.bmcl.2012.03.032
CHEMBL2023470 80998 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 400 6 0 6 3.8 c1ccc(-n2cc(-c3ccnc4cc(OCCN5CCOCC5)ccc34)cn2)cc1 10.1016/j.bmcl.2012.03.032
46853659 75558 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 433 3 1 6 2.4 O=C(Nc1ccc(N2S(=O)(=O)c3ccccc3S2(=O)=O)cc1)c1cccc(F)n1 10.1021/jm200956q
CHEMBL1921948 75558 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 433 3 1 6 2.4 O=C(Nc1ccc(N2S(=O)(=O)c3ccccc3S2(=O)=O)cc1)c1cccc(F)n1 10.1021/jm200956q
46853732 75563 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 401 4 1 6 2.6 O=S1(=O)c2ccccc2S(=O)(=O)N1c1ccc(NCc2ccccn2)cc1 10.1021/jm200956q
CHEMBL1921955 75563 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 401 4 1 6 2.6 O=S1(=O)c2ccccc2S(=O)(=O)N1c1ccc(NCc2ccccn2)cc1 10.1021/jm200956q
24780084 14488 0 None 9 2 Rat 4.8 pEC50 = 4.8 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 281 7 5 5 -0.9 N[C@@H](CCP(=O)(O)C(O)C1CC1C(=O)O)C(=O)O 10.1021/jm901523t
CHEMBL1088873 14488 0 None 9 2 Rat 4.8 pEC50 = 4.8 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 281 7 5 5 -0.9 N[C@@H](CCP(=O)(O)C(O)C1CC1C(=O)O)C(=O)O 10.1021/jm901523t
CHEMBL1204419 14488 0 None 9 2 Rat 4.8 pEC50 = 4.8 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 281 7 5 5 -0.9 N[C@@H](CCP(=O)(O)C(O)C1CC1C(=O)O)C(=O)O 10.1021/jm901523t
54670780 159804 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 479 5 1 6 4.6 O=C(Nc1nc(C(F)(F)F)c(S(=O)(=O)Cc2ccc(Cl)cc2F)s1)c1ccccn1 nan
CHEMBL3975694 159804 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 479 5 1 6 4.6 O=C(Nc1nc(C(F)(F)F)c(S(=O)(=O)Cc2ccc(Cl)cc2F)s1)c1ccccn1 nan
16747848 92290 0 None 1 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at mGlu4 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate productionAgonist activity at mGlu4 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate production
ChEMBL 195 3 4 3 -1.0 N[C@@]1(C(=O)O)C[C@@H]1CP(=O)(O)O 10.1021/jm070262c
CHEMBL227288 92290 0 None 1 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at mGlu4 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate productionAgonist activity at mGlu4 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate production
ChEMBL 195 3 4 3 -1.0 N[C@@]1(C(=O)O)C[C@@H]1CP(=O)(O)O 10.1021/jm070262c
134189994 178258 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 265 2 2 5 3.2 Cc1noc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
CHEMBL4463609 178258 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 265 2 2 5 3.2 Cc1noc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
134189994 178258 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 265 2 2 5 3.2 Cc1noc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
CHEMBL4463609 178258 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 265 2 2 5 3.2 Cc1noc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
127046934 146425 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 146425 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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
162667269 189292 0 None -3 3 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 434 3 1 4 4.7 Cc1ccoc1C(=O)Nc1cc(F)c(N2C(=O)c3cccc(Cl)c3C2=O)c(F)c1F 10.1016/j.bmcl.2020.127724
CHEMBL4787053 189292 0 None -3 3 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 434 3 1 4 4.7 Cc1ccoc1C(=O)Nc1cc(F)c(N2C(=O)c3cccc(Cl)c3C2=O)c(F)c1F 10.1016/j.bmcl.2020.127724
71260327 147266 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 409 5 1 5 3.5 O=C(Nc1ccn(S(=O)(=O)Cc2ccc(C(F)(F)F)cc2)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
CHEMBL3809765 147266 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 409 5 1 5 3.5 O=C(Nc1ccn(S(=O)(=O)Cc2ccc(C(F)(F)F)cc2)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
134192002 172439 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 377 4 2 7 3.1 CN1CCC(Oc2nn(C)c3cc(Nc4n[nH]c5cccnc45)ccc23)CC1 10.1016/j.bmcl.2018.06.034
CHEMBL4244458 172439 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 377 4 2 7 3.1 CN1CCC(Oc2nn(C)c3cc(Nc4n[nH]c5cccnc45)ccc23)CC1 10.1016/j.bmcl.2018.06.034
54670965 147229 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 393 5 1 6 3.4 O=C(Nc1ncc(S(=O)(=O)Cc2ccccc2Cl)s1)c1ccccn1 10.1016/j.bmcl.2016.05.029
CHEMBL3809341 147229 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 393 5 1 6 3.4 O=C(Nc1ncc(S(=O)(=O)Cc2ccccc2Cl)s1)c1ccccn1 10.1016/j.bmcl.2016.05.029
137652776 165446 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 426 6 1 7 4.8 Cc1cc(CCCOc2ccc3oc(-c4cc5cccn5cn4)c/c(=N\O)c3c2)ccn1 10.1021/acs.jmedchem.7b00991
CHEMBL4092850 165446 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 426 6 1 7 4.8 Cc1cc(CCCOc2ccc3oc(-c4cc5cccn5cn4)c/c(=N\O)c3c2)ccn1 10.1021/acs.jmedchem.7b00991
46934289 22742 77 None - 1 Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilization
ChEMBL 421 5 2 4 4.4 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2Cl)c(Cl)c1)c1ccccn1 10.1016/j.bmcl.2010.07.007
CHEMBL1223381 22742 77 None - 1 Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilization
ChEMBL 421 5 2 4 4.4 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2Cl)c(Cl)c1)c1ccccn1 10.1016/j.bmcl.2010.07.007
134191937 172574 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 305 3 2 6 2.9 Cn1nc(C2CC2)c2ccc(Nc3n[nH]c4nccnc34)cc21 10.1016/j.bmcl.2018.06.034
CHEMBL4247943 172574 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 305 3 2 6 2.9 Cn1nc(C2CC2)c2ccc(Nc3n[nH]c4nccnc34)cc21 10.1016/j.bmcl.2018.06.034
92044496 162746 0 None 2 4 Human 6.7 pEC50 = 6.7 Functional
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 324 7 4 7 0.7 N[C@@H](CCP(=O)(O)C(O)c1csc([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4061423 162746 0 None 2 4 Human 6.7 pEC50 = 6.7 Functional
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 324 7 4 7 0.7 N[C@@H](CCP(=O)(O)C(O)c1csc([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
52913885 147241 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 377 5 1 5 2.8 O=C(Nc1ccn(S(=O)(=O)Cc2ccc(F)cc2F)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
CHEMBL3809468 147241 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 377 5 1 5 2.8 O=C(Nc1ccn(S(=O)(=O)Cc2ccc(F)cc2F)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
70691970 81016 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 398 3 0 5 5.1 O=C(Oc1ccc2c(-c3cnn(-c4ccccc4)c3)ccnc2c1)N1CCCCC1 10.1016/j.bmcl.2012.03.032
CHEMBL2023624 81016 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 398 3 0 5 5.1 O=C(Oc1ccc2c(-c3cnn(-c4ccccc4)c3)ccnc2c1)N1CCCCC1 10.1016/j.bmcl.2012.03.032
54670965 147229 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 393 5 1 6 3.4 O=C(Nc1ncc(S(=O)(=O)Cc2ccccc2Cl)s1)c1ccccn1 10.1016/j.bmcl.2016.05.029
CHEMBL3809341 147229 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 393 5 1 6 3.4 O=C(Nc1ncc(S(=O)(=O)Cc2ccccc2Cl)s1)c1ccccn1 10.1016/j.bmcl.2016.05.029
52913885 147241 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 377 5 1 5 2.8 O=C(Nc1ccn(S(=O)(=O)Cc2ccc(F)cc2F)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
CHEMBL3809468 147241 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 377 5 1 5 2.8 O=C(Nc1ccn(S(=O)(=O)Cc2ccc(F)cc2F)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
71260327 147266 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 409 5 1 5 3.5 O=C(Nc1ccn(S(=O)(=O)Cc2ccc(C(F)(F)F)cc2)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
CHEMBL3809765 147266 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 409 5 1 5 3.5 O=C(Nc1ccn(S(=O)(=O)Cc2ccc(C(F)(F)F)cc2)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
68012045 162960 0 None 1 2 Human 4.7 pEC50 = 4.7 Functional
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 348 8 4 7 0.9 COc1cc(CP(=O)(O)CC[C@H](N)C(=O)O)cc([N+](=O)[O-])c1O 10.1021/acs.jmedchem.7b01438
CHEMBL4063991 162960 0 None 1 2 Human 4.7 pEC50 = 4.7 Functional
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 348 8 4 7 0.9 COc1cc(CP(=O)(O)CC[C@H](N)C(=O)O)cc([N+](=O)[O-])c1O 10.1021/acs.jmedchem.7b01438
54670687 149229 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 425 5 1 6 3.9 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1c(F)cccc1Cl nan
CHEMBL3890158 149229 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 425 5 1 6 3.9 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1c(F)cccc1Cl nan
122196110 131022 0 None -13 2 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 394 4 1 5 3.8 COc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(F)c2C1=O 10.1016/j.bmcl.2015.10.013
CHEMBL3634432 131022 0 None -13 2 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 394 4 1 5 3.8 COc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(F)c2C1=O 10.1016/j.bmcl.2015.10.013
10135 10826 21 None -3 2 Rat 6.7 pEC50 = 6.7 Functional
Positive allosteric modulator activity at rat mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at rat mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 329 2 2 4 4.3 FC(c1nccc2c1ccc(c2)Nc1n[nH]c2c1cccn2)(F)F 10.1016/j.bmcl.2018.10.050
134191471 10826 21 None -3 2 Rat 6.7 pEC50 = 6.7 Functional
Positive allosteric modulator activity at rat mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at rat mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 329 2 2 4 4.3 FC(c1nccc2c1ccc(c2)Nc1n[nH]c2c1cccn2)(F)F 10.1016/j.bmcl.2018.10.050
CHEMBL4797139 10826 21 None -3 2 Rat 6.7 pEC50 = 6.7 Functional
Positive allosteric modulator activity at rat mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at rat mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 329 2 2 4 4.3 FC(c1nccc2c1ccc(c2)Nc1n[nH]c2c1cccn2)(F)F 10.1016/j.bmcl.2018.10.050
137650519 164124 0 None -1 4 Human 5.7 pEC50 = 5.7 Functional
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 352 7 5 7 0.5 N[C@@H](CCP(=O)(O)C(O)c1cc(F)c(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4077705 164124 0 None -1 4 Human 5.7 pEC50 = 5.7 Functional
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 352 7 5 7 0.5 N[C@@H](CCP(=O)(O)C(O)c1cc(F)c(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
54670225 156790 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 435 6 1 6 4.5 CC(C)c1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccccc1Cl nan
CHEMBL3950312 156790 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 435 6 1 6 4.5 CC(C)c1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccccc1Cl nan
1407 8860 42 None -117 7 Human 5.7 pEC50 = 5.7 Functional
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 239 4 4 4 0.2 N[C@@H](c1ccc(c(c1)C(=O)O)C(=O)O)C(=O)O 10.1021/acs.jmedchem.7b01438
16062593 8860 42 None -117 7 Human 5.7 pEC50 = 5.7 Functional
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 239 4 4 4 0.2 N[C@@H](c1ccc(c(c1)C(=O)O)C(=O)O)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL143210 8860 42 None -117 7 Human 5.7 pEC50 = 5.7 Functional
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 239 4 4 4 0.2 N[C@@H](c1ccc(c(c1)C(=O)O)C(=O)O)C(=O)O 10.1021/acs.jmedchem.7b01438
54670593 151781 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 403 6 1 7 3.1 COc1ccc(CS(=O)(=O)c2sc(NC(=O)c3ccccn3)nc2C)cc1 nan
CHEMBL3910945 151781 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 403 6 1 7 3.1 COc1ccc(CS(=O)(=O)c2sc(NC(=O)c3ccccn3)nc2C)cc1 nan
52934972 158520 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 396 4 1 6 3.1 O=C(Nc1cnn(S(=O)(=O)c2cc(Cl)ccc2Cl)c1)c1ccccn1 nan
CHEMBL3964592 158520 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 396 4 1 6 3.1 O=C(Nc1cnn(S(=O)(=O)c2cc(Cl)ccc2Cl)c1)c1ccccn1 nan
10135 10826 21 None -3 2 Rat 6.7 pEC50 = 6.7 Functional
Positive allosteric modulator activity at rat mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at rat mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 329 2 2 4 4.3 FC(c1nccc2c1ccc(c2)Nc1n[nH]c2c1cccn2)(F)F 10.1016/j.bmcl.2018.10.050
134191471 10826 21 None -3 2 Rat 6.7 pEC50 = 6.7 Functional
Positive allosteric modulator activity at rat mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at rat mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 329 2 2 4 4.3 FC(c1nccc2c1ccc(c2)Nc1n[nH]c2c1cccn2)(F)F 10.1016/j.bmcl.2018.10.050
CHEMBL4797139 10826 21 None -3 2 Rat 6.7 pEC50 = 6.7 Functional
Positive allosteric modulator activity at rat mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at rat mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 329 2 2 4 4.3 FC(c1nccc2c1ccc(c2)Nc1n[nH]c2c1cccn2)(F)F 10.1016/j.bmcl.2018.10.050
127025548 144453 0 None -4 2 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human mGlu4 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu4 receptor by cell based calcium mobilization
ChEMBL 395 3 1 5 4.0 Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3ncoc3C)cc1Cl)C2=O 10.1016/j.bmcl.2015.12.104
CHEMBL3758587 144453 0 None -4 2 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human mGlu4 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu4 receptor by cell based calcium mobilization
ChEMBL 395 3 1 5 4.0 Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3ncoc3C)cc1Cl)C2=O 10.1016/j.bmcl.2015.12.104
127026138 144411 0 None -38 2 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human mGlu4 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu4 receptor by cell based calcium mobilization
ChEMBL 431 3 1 5 4.8 Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3758216 144411 0 None -38 2 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human mGlu4 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu4 receptor by cell based calcium mobilization
ChEMBL 431 3 1 5 4.8 Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
122419063 182860 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 392 3 2 6 4.0 CC(=O)N1CCC(c2nsc3cc(Nc4n[nH]c5cccnc45)ccc23)CC1 10.1021/acs.jmedchem.8b00994
CHEMBL4591132 182860 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 392 3 2 6 4.0 CC(=O)N1CCC(c2nsc3cc(Nc4n[nH]c5cccnc45)ccc23)CC1 10.1021/acs.jmedchem.8b00994
127047638 146599 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
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 3.7 Nc1cccnc1C(=O)Nc1ccc(N2Cc3ccccc3CC2=O)c(Cl)c1 10.1016/j.bmcl.2016.04.041
CHEMBL3798945 146599 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
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 3.7 Nc1cccnc1C(=O)Nc1ccc(N2Cc3ccccc3CC2=O)c(Cl)c1 10.1016/j.bmcl.2016.04.041
127046254 146654 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
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 407 4 2 5 3.5 Nc1cccnc1C(=O)Nc1ccc(N2CC(c3cccnc3)CC2=O)c(Cl)c1 10.1016/j.bmcl.2016.04.041
CHEMBL3799281 146654 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
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 407 4 2 5 3.5 Nc1cccnc1C(=O)Nc1ccc(N2CC(c3cccnc3)CC2=O)c(Cl)c1 10.1016/j.bmcl.2016.04.041
127046933 146776 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
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 384 4 2 4 3.7 CC1(C2CC2)CC(=O)N(c2ccc(NC(=O)c3ncccc3N)cc2Cl)C1 10.1016/j.bmcl.2016.04.041
CHEMBL3799999 146776 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
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 384 4 2 4 3.7 CC1(C2CC2)CC(=O)N(c2ccc(NC(=O)c3ncccc3N)cc2Cl)C1 10.1016/j.bmcl.2016.04.041
46934289 22742 77 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 421 5 2 4 4.4 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2Cl)c(Cl)c1)c1ccccn1 10.1021/jm200290z
CHEMBL1223381 22742 77 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 421 5 2 4 4.4 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2Cl)c(Cl)c1)c1ccccn1 10.1021/jm200290z
122419063 182860 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 392 3 2 6 4.0 CC(=O)N1CCC(c2nsc3cc(Nc4n[nH]c5cccnc45)ccc23)CC1 10.1021/acs.jmedchem.8b00994
CHEMBL4591132 182860 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 392 3 2 6 4.0 CC(=O)N1CCC(c2nsc3cc(Nc4n[nH]c5cccnc45)ccc23)CC1 10.1021/acs.jmedchem.8b00994
49862522 21854 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 211 2 1 3 2.5 Cc1cnc(N)nc1/C=C/c1ccccc1 10.1016/j.bmcl.2010.06.078
CHEMBL1209514 21854 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 211 2 1 3 2.5 Cc1cnc(N)nc1/C=C/c1ccccc1 10.1016/j.bmcl.2010.06.078
136503356 164236 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 294 1 1 5 4.0 O/N=c1\cc(-c2cc3sccc3cn2)oc2ccccc12 10.1021/acs.jmedchem.7b00991
CHEMBL4079161 164236 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 294 1 1 5 4.0 O/N=c1\cc(-c2cc3sccc3cn2)oc2ccccc12 10.1021/acs.jmedchem.7b00991
137649749 164066 0 None 4 2 Human 5.7 pEC50 = 5.7 Functional
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 307 7 5 6 0.0 N[C@@H](CCP(=O)(O)C(O)c1coc(C(=O)O)c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4076894 164066 0 None 4 2 Human 5.7 pEC50 = 5.7 Functional
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 307 7 5 6 0.0 N[C@@H](CCP(=O)(O)C(O)c1coc(C(=O)O)c1)C(=O)O 10.1021/acs.jmedchem.7b01438
57765535 164583 0 None 1 3 Human 5.7 pEC50 = 5.7 Functional
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 352 7 4 6 1.3 N[C@@H](CCP(=O)(O)C(O)c1ccc(Cl)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4083240 164583 0 None 1 3 Human 5.7 pEC50 = 5.7 Functional
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 352 7 4 6 1.3 N[C@@H](CCP(=O)(O)C(O)c1ccc(Cl)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
137634883 162929 0 None 1 3 Human 5.7 pEC50 = 5.7 Functional
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 348 8 4 7 0.7 COc1ccc([C@@H](O)P(=O)(O)CC[C@H](N)C(=O)O)cc1[N+](=O)[O-] 10.1021/acs.jmedchem.7b01438
CHEMBL4063720 162929 0 None 1 3 Human 5.7 pEC50 = 5.7 Functional
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 348 8 4 7 0.7 COc1ccc([C@@H](O)P(=O)(O)CC[C@H](N)C(=O)O)cc1[N+](=O)[O-] 10.1021/acs.jmedchem.7b01438
45484614 203994 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Allosteric modulator activity at human mGlu4 receptor expressed in CHO cells coexpressing Gqi5 assessed as effect on calcium fluxAllosteric modulator activity at human mGlu4 receptor expressed in CHO cells coexpressing Gqi5 assessed as effect on calcium flux
ChEMBL 299 3 2 2 3.3 O=C(Nc1cc(F)cc(Cl)c1)[C@H]1CCCC[C@H]1C(=O)O 10.1016/j.bmcl.2009.07.072
CHEMBL568240 203994 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Allosteric modulator activity at human mGlu4 receptor expressed in CHO cells coexpressing Gqi5 assessed as effect on calcium fluxAllosteric modulator activity at human mGlu4 receptor expressed in CHO cells coexpressing Gqi5 assessed as effect on calcium flux
ChEMBL 299 3 2 2 3.3 O=C(Nc1cc(F)cc(Cl)c1)[C@H]1CCCC[C@H]1C(=O)O 10.1016/j.bmcl.2009.07.072
45484642 204447 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Allosteric modulator activity at human mGlu4 receptor expressed in CHO cells coexpressing Gqi5 assessed as effect on calcium fluxAllosteric modulator activity at human mGlu4 receptor expressed in CHO cells coexpressing Gqi5 assessed as effect on calcium flux
ChEMBL 296 2 1 2 4.3 N#C[C@@H]1CCCC[C@@H]1C(=O)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2009.07.072
CHEMBL571063 204447 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Allosteric modulator activity at human mGlu4 receptor expressed in CHO cells coexpressing Gqi5 assessed as effect on calcium fluxAllosteric modulator activity at human mGlu4 receptor expressed in CHO cells coexpressing Gqi5 assessed as effect on calcium flux
ChEMBL 296 2 1 2 4.3 N#C[C@@H]1CCCC[C@@H]1C(=O)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2009.07.072
13285567 21856 1 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 227 3 1 4 2.2 COc1cc(/C=C/c2ccccc2)nc(N)n1 10.1016/j.bmcl.2010.06.078
CHEMBL1209518 21856 1 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 227 3 1 4 2.2 COc1cc(/C=C/c2ccccc2)nc(N)n1 10.1016/j.bmcl.2010.06.078
46898088 9145 6 None -33 8 Rat 4.7 pEC50 = 4.7 Functional
Agonist activity at mGlu4 assessed as decrease in PF-induced presynaptic calcium amplitude in rat coronal slices by Fluo-4FF-AM dye based fluorescence assayAgonist activity at mGlu4 assessed as decrease in PF-induced presynaptic calcium amplitude in rat coronal slices by Fluo-4FF-AM dye based fluorescence assay
ChEMBL 364 8 5 8 0.4 COc1cc(cc(c1O)[N+](=O)[O-])C(P(=O)(CC[C@@H](C(=O)O)N)O)O 10.1021/acs.jmedchem.7b01438
6739 9145 6 None -33 8 Rat 4.7 pEC50 = 4.7 Functional
Agonist activity at mGlu4 assessed as decrease in PF-induced presynaptic calcium amplitude in rat coronal slices by Fluo-4FF-AM dye based fluorescence assayAgonist activity at mGlu4 assessed as decrease in PF-induced presynaptic calcium amplitude in rat coronal slices by Fluo-4FF-AM dye based fluorescence assay
ChEMBL 364 8 5 8 0.4 COc1cc(cc(c1O)[N+](=O)[O-])C(P(=O)(CC[C@@H](C(=O)O)N)O)O 10.1021/acs.jmedchem.7b01438
CHEMBL3114672 9145 6 None -33 8 Rat 4.7 pEC50 = 4.7 Functional
Agonist activity at mGlu4 assessed as decrease in PF-induced presynaptic calcium amplitude in rat coronal slices by Fluo-4FF-AM dye based fluorescence assayAgonist activity at mGlu4 assessed as decrease in PF-induced presynaptic calcium amplitude in rat coronal slices by Fluo-4FF-AM dye based fluorescence assay
ChEMBL 364 8 5 8 0.4 COc1cc(cc(c1O)[N+](=O)[O-])C(P(=O)(CC[C@@H](C(=O)O)N)O)O 10.1021/acs.jmedchem.7b01438
46197878 15210 0 None 3 2 Rat 4.7 pEC50 = 4.7 Functional
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 283 9 5 5 -0.9 N[C@@H](CCP(=O)(O)CC(CCO)C(=O)O)C(=O)O 10.1021/jm901523t
CHEMBL1093612 15210 0 None 3 2 Rat 4.7 pEC50 = 4.7 Functional
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 283 9 5 5 -0.9 N[C@@H](CCP(=O)(O)CC(CCO)C(=O)O)C(=O)O 10.1021/jm901523t
15078062 21874 15 None - 1 Human 4.7 pEC50 = 4.7 Functional
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 195 0 1 3 1.5 Nc1nccc(C#Cc2ccccc2)n1 10.1016/j.bmcl.2010.06.078
CHEMBL1209591 21874 15 None - 1 Human 4.7 pEC50 = 4.7 Functional
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 195 0 1 3 1.5 Nc1nccc(C#Cc2ccccc2)n1 10.1016/j.bmcl.2010.06.078
52935194 150716 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 396 4 1 6 3.1 O=C(Nc1cnn(S(=O)(=O)c2ccc(Cl)c(Cl)c2)c1)c1ccccn1 nan
CHEMBL3902298 150716 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 396 4 1 6 3.1 O=C(Nc1cnn(S(=O)(=O)c2ccc(Cl)c(Cl)c2)c1)c1ccccn1 nan
45111509 22638 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilization
ChEMBL 371 5 2 4 3.3 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2F)cc1)c1ccccn1 10.1016/j.bmcl.2010.07.007
CHEMBL1223084 22638 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilization
ChEMBL 371 5 2 4 3.3 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2F)cc1)c1ccccn1 10.1016/j.bmcl.2010.07.007
51003281 64674 0 None 1 2 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 419 4 2 3 5.3 O=C(Nc1ccc(NC(=O)c2ccccc2Cl)c(C(F)(F)F)c1)c1ccccn1 10.1021/jm101271s
CHEMBL1672239 64674 0 None 1 2 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 419 4 2 3 5.3 O=C(Nc1ccc(NC(=O)c2ccccc2Cl)c(C(F)(F)F)c1)c1ccccn1 10.1021/jm101271s
122197956 167250 0 None 5 3 Rat 6.7 pEC50 = 6.7 Functional
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 363 9 5 6 0.9 N[C@H](CCP(=O)(O)C(O)c1ccc(SCC(=O)O)cc1)C(=O)O nan
CHEMBL4111817 167250 0 None 5 3 Rat 6.7 pEC50 = 6.7 Functional
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 363 9 5 6 0.9 N[C@H](CCP(=O)(O)C(O)c1ccc(SCC(=O)O)cc1)C(=O)O nan
8403638 203274 4 None -1 2 Human 5.7 pEC50 = 5.7 Functional
Activity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilizationActivity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilization
ChEMBL 300 2 1 2 4.0 O=C(Nc1ccc(Cl)c(C(F)(F)F)c1)c1ccccn1 10.1021/jm9005065
CHEMBL563423 203274 4 None -1 2 Human 5.7 pEC50 = 5.7 Functional
Activity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilizationActivity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilization
ChEMBL 300 2 1 2 4.0 O=C(Nc1ccc(Cl)c(C(F)(F)F)c1)c1ccccn1 10.1021/jm9005065
70689779 80926 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 272 2 0 4 3.5 c1ccc(-n2cc(-c3ccnc4ccccc34)cn2)nc1 10.1016/j.bmcl.2012.03.032
CHEMBL2022872 80926 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 272 2 0 4 3.5 c1ccc(-n2cc(-c3ccnc4ccccc34)cn2)nc1 10.1016/j.bmcl.2012.03.032
145957424 168848 0 None -2 3 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assay
ChEMBL 407 4 0 4 5.2 CCc1nn2c(C(F)(F)F)cc(C)nc2c1-c1cc(F)c(OC(F)F)cc1F 10.1021/acsmedchemlett.7b00317
CHEMBL4160675 168848 0 None -2 3 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assay
ChEMBL 407 4 0 4 5.2 CCc1nn2c(C(F)(F)F)cc(C)nc2c1-c1cc(F)c(OC(F)F)cc1F 10.1021/acsmedchemlett.7b00317
51003328 74579 0 None - 1 Rat 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 387 4 2 3 4.5 O=C(Nc1ccc(NC(=O)c2ccc(F)cc2F)c(Cl)c1)c1ccccn1 10.1021/jm101271s
CHEMBL1909430 74579 0 None - 1 Rat 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 387 4 2 3 4.5 O=C(Nc1ccc(NC(=O)c2ccc(F)cc2F)c(Cl)c1)c1ccccn1 10.1021/jm101271s
10197984 9199 44 None -7762 5 Human 4.7 pEC50 = 4.7 Functional
Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR4aInhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR4a
ChEMBL 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10.1021/jm980616n
1394 9199 44 None -7762 5 Human 4.7 pEC50 = 4.7 Functional
Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR4aInhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR4a
ChEMBL 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10.1021/jm980616n
CHEMBL275079 9199 44 None -7762 5 Human 4.7 pEC50 = 4.7 Functional
Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR4aInhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR4a
ChEMBL 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10.1021/jm980616n
162677180 190308 0 None -5 3 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 400 3 1 4 4.1 Cc1ccoc1C(=O)Nc1c(F)cc(N2C(=O)c3ccccc3C2=O)c(F)c1F 10.1016/j.bmcl.2020.127724
CHEMBL4799902 190308 0 None -5 3 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 400 3 1 4 4.1 Cc1ccoc1C(=O)Nc1c(F)cc(N2C(=O)c3ccccc3C2=O)c(F)c1F 10.1016/j.bmcl.2020.127724
145957424 168848 0 None -2 3 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assay
ChEMBL 407 4 0 4 5.2 CCc1nn2c(C(F)(F)F)cc(C)nc2c1-c1cc(F)c(OC(F)F)cc1F 10.1021/acsmedchemlett.7b00317
CHEMBL4160675 168848 0 None -2 3 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assay
ChEMBL 407 4 0 4 5.2 CCc1nn2c(C(F)(F)F)cc(C)nc2c1-c1cc(F)c(OC(F)F)cc1F 10.1021/acsmedchemlett.7b00317
134191681 189894 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 344 3 2 5 4.2 c1cnc2c(Nc3ccc4c(N5CCCCC5)nccc4c3)n[nH]c2c1 10.1016/j.bmcl.2018.10.050
CHEMBL4794816 189894 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 344 3 2 5 4.2 c1cnc2c(Nc3ccc4c(N5CCCCC5)nccc4c3)n[nH]c2c1 10.1016/j.bmcl.2018.10.050
51003329 74580 0 None 1 2 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 419 4 2 3 5.5 O=C(Nc1ccc(NC(=O)c2ccccn2)cc1Cl)c1cc(Cl)cc(Cl)c1 10.1021/jm101271s
CHEMBL1909431 74580 0 None 1 2 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 419 4 2 3 5.5 O=C(Nc1ccc(NC(=O)c2ccccn2)cc1Cl)c1cc(Cl)cc(Cl)c1 10.1021/jm101271s
53373762 160778 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 312 2 2 3 4.4 FC(F)(F)c1ccc(Nc2n[nH]c3cccnc23)cc1Cl nan
CHEMBL3984012 160778 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 312 2 2 3 4.4 FC(F)(F)c1ccc(Nc2n[nH]c3cccnc23)cc1Cl nan
54670496 147312 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 439 6 1 6 4.1 CCc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccc(Cl)cc1F 10.1016/j.bmcl.2016.05.029
CHEMBL3810375 147312 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 439 6 1 6 4.1 CCc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccc(Cl)cc1F 10.1016/j.bmcl.2016.05.029
136015159 150660 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 260 2 3 4 3.1 Oc1ccc(Nc2n[nH]c3cccnc23)cc1Cl nan
CHEMBL3901833 150660 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 260 2 3 4 3.1 Oc1ccc(Nc2n[nH]c3cccnc23)cc1Cl nan
53374209 157993 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 296 2 2 3 3.9 Fc1cc(Nc2n[nH]c3cccnc23)cc(C(F)(F)F)c1 nan
CHEMBL3959958 157993 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 296 2 2 3 3.9 Fc1cc(Nc2n[nH]c3cccnc23)cc(C(F)(F)F)c1 nan
49865453 22745 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilization
ChEMBL 386 5 1 4 4.0 O=C(Nc1ccc(CS(=O)(=O)c2ccccc2Cl)cc1)c1ccccn1 10.1016/j.bmcl.2010.07.007
CHEMBL1223385 22745 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilization
ChEMBL 386 5 1 4 4.0 O=C(Nc1ccc(CS(=O)(=O)c2ccccc2Cl)cc1)c1ccccn1 10.1016/j.bmcl.2010.07.007
54670496 147312 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 439 6 1 6 4.1 CCc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccc(Cl)cc1F 10.1016/j.bmcl.2016.05.029
CHEMBL3810375 147312 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 439 6 1 6 4.1 CCc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccc(Cl)cc1F 10.1016/j.bmcl.2016.05.029
134190223 179137 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 283 2 2 5 3.3 Cc1noc2ccc(Nc3n[nH]c4ncc(F)cc34)cc12 10.1021/acs.jmedchem.8b00994
CHEMBL4475973 179137 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 283 2 2 5 3.3 Cc1noc2ccc(Nc3n[nH]c4ncc(F)cc34)cc12 10.1021/acs.jmedchem.8b00994
51003372 74581 0 None -1 2 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 358 4 2 5 3.7 O=C(Nc1ccc(NC(=O)c2cncs2)c(Cl)c1)c1ccccn1 10.1021/jm101271s
CHEMBL1909433 74581 0 None -1 2 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 358 4 2 5 3.7 O=C(Nc1ccc(NC(=O)c2cncs2)c(Cl)c1)c1ccccn1 10.1021/jm101271s
127047638 146599 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 3.7 Nc1cccnc1C(=O)Nc1ccc(N2Cc3ccccc3CC2=O)c(Cl)c1 10.1016/j.bmcl.2016.04.041
CHEMBL3798945 146599 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 3.7 Nc1cccnc1C(=O)Nc1ccc(N2Cc3ccccc3CC2=O)c(Cl)c1 10.1016/j.bmcl.2016.04.041
134190223 179137 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 283 2 2 5 3.3 Cc1noc2ccc(Nc3n[nH]c4ncc(F)cc34)cc12 10.1021/acs.jmedchem.8b00994
CHEMBL4475973 179137 0 None -1 2 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 283 2 2 5 3.3 Cc1noc2ccc(Nc3n[nH]c4ncc(F)cc34)cc12 10.1021/acs.jmedchem.8b00994
134190224 178517 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 284 2 2 6 2.7 Cc1noc2c(F)cc(Nc3n[nH]c4nccnc34)cc12 10.1021/acs.jmedchem.8b00994
CHEMBL4467229 178517 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 284 2 2 6 2.7 Cc1noc2c(F)cc(Nc3n[nH]c4nccnc34)cc12 10.1021/acs.jmedchem.8b00994
134190224 178517 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 284 2 2 6 2.7 Cc1noc2c(F)cc(Nc3n[nH]c4nccnc34)cc12 10.1021/acs.jmedchem.8b00994
CHEMBL4467229 178517 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 284 2 2 6 2.7 Cc1noc2c(F)cc(Nc3n[nH]c4nccnc34)cc12 10.1021/acs.jmedchem.8b00994
46700737 72299 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 269 2 2 5 2.8 c1ccc(Nc2nc3c(s2)CCc2n[nH]cc2-3)nc1 10.1021/jm200290z
CHEMBL1830698 72299 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 269 2 2 5 2.8 c1ccc(Nc2nc3c(s2)CCc2n[nH]cc2-3)nc1 10.1021/jm200290z
3525815 80921 3 None 4 3 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 271 2 0 3 4.1 c1ccc(-n2cc(-c3ccnc4ccccc34)cn2)cc1 10.1016/j.bmcl.2012.03.032
CHEMBL2022867 80921 3 None 4 3 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 271 2 0 3 4.1 c1ccc(-n2cc(-c3ccnc4ccccc34)cn2)cc1 10.1016/j.bmcl.2012.03.032
60150507 80991 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 301 3 0 4 4.1 COc1ccc2c(-c3cnn(-c4ccccc4)c3)ccnc2c1 10.1016/j.bmcl.2012.03.032
CHEMBL2023457 80991 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 301 3 0 4 4.1 COc1ccc2c(-c3cnn(-c4ccccc4)c3)ccnc2c1 10.1016/j.bmcl.2012.03.032
46898088 9145 6 None -11 8 Human 5.7 pEC50 = 5.7 Functional
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 364 8 5 8 0.4 COc1cc(cc(c1O)[N+](=O)[O-])C(P(=O)(CC[C@@H](C(=O)O)N)O)O 10.1021/acs.jmedchem.7b01438
6739 9145 6 None -11 8 Human 5.7 pEC50 = 5.7 Functional
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 364 8 5 8 0.4 COc1cc(cc(c1O)[N+](=O)[O-])C(P(=O)(CC[C@@H](C(=O)O)N)O)O 10.1021/acs.jmedchem.7b01438
CHEMBL3114672 9145 6 None -11 8 Human 5.7 pEC50 = 5.7 Functional
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 364 8 5 8 0.4 COc1cc(cc(c1O)[N+](=O)[O-])C(P(=O)(CC[C@@H](C(=O)O)N)O)O 10.1021/acs.jmedchem.7b01438
53387561 72300 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 268 2 2 4 3.4 c1ccc(Nc2nc3c(s2)CCc2n[nH]cc2-3)cc1 10.1021/jm200290z
CHEMBL1830701 72300 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 268 2 2 4 3.4 c1ccc(Nc2nc3c(s2)CCc2n[nH]cc2-3)cc1 10.1021/jm200290z
24779948 162758 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
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 317 7 5 5 0.4 N[C@@H](CCP(=O)(O)C(O)c1cccc(C(=O)O)c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4061539 162758 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
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 317 7 5 5 0.4 N[C@@H](CCP(=O)(O)C(O)c1cccc(C(=O)O)c1)C(=O)O 10.1021/acs.jmedchem.7b01438
52934970 158107 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 380 4 1 6 2.6 O=C(Nc1cnn(S(=O)(=O)c2cc(Cl)ccc2F)c1)c1ccccn1 nan
CHEMBL3961017 158107 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 380 4 1 6 2.6 O=C(Nc1cnn(S(=O)(=O)c2cc(Cl)ccc2F)c1)c1ccccn1 nan
122193176 130709 0 None -28 3 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of human mGlu4 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay
ChEMBL 414 3 1 4 4.9 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
CHEMBL3628112 130709 0 None -28 3 Human 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of human mGlu4 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay
ChEMBL 414 3 1 4 4.9 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
44572113 195677 4 None -1 2 Human 5.7 pEC50 = 5.7 Functional
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 294 2 2 4 2.7 O=C(Nc1ccccc1)[C@]12C[C@H]1/C(=N\O)c1ccccc1O2 10.1021/acs.jmedchem.7b00991
CHEMBL507522 195677 4 None -1 2 Human 5.7 pEC50 = 5.7 Functional
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 294 2 2 4 2.7 O=C(Nc1ccccc1)[C@]12C[C@H]1/C(=N\O)c1ccccc1O2 10.1021/acs.jmedchem.7b00991
4066845 75475 1 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 404 3 1 6 2.4 O=C(Nc1ccc(N2S(=O)(=O)c3ccccc3S2(=O)=O)cc1)c1ccco1 10.1021/jm200956q
CHEMBL1921852 75475 1 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 404 3 1 6 2.4 O=C(Nc1ccc(N2S(=O)(=O)c3ccccc3S2(=O)=O)cc1)c1ccco1 10.1021/jm200956q
51003282 64675 0 None -1 2 Rat 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 351 4 2 3 4.2 O=C(Nc1ccc(NC(=O)c2ccccc2Cl)cc1)c1ccccn1 10.1021/jm101271s
CHEMBL1672240 64675 0 None -1 2 Rat 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 351 4 2 3 4.2 O=C(Nc1ccc(NC(=O)c2ccccc2Cl)cc1)c1ccccn1 10.1021/jm101271s
134190173 178934 0 None -1 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 265 2 2 5 3.2 Cc1noc2ccc(Nc3n[nH]c4ncccc34)cc12 10.1021/acs.jmedchem.8b00994
CHEMBL4473211 178934 0 None -1 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 265 2 2 5 3.2 Cc1noc2ccc(Nc3n[nH]c4ncccc34)cc12 10.1021/acs.jmedchem.8b00994
162674612 190161 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 402 3 1 4 4.4 Cc1cc(N2C(=O)C3=C(CCCC3)C2=O)c(F)cc1NC(=O)c1ccc(Cl)o1 10.1016/j.bmcl.2020.127724
CHEMBL4797971 190161 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 402 3 1 4 4.4 Cc1cc(N2C(=O)C3=C(CCCC3)C2=O)c(F)cc1NC(=O)c1ccc(Cl)o1 10.1016/j.bmcl.2020.127724
134190173 178934 0 None -1 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 265 2 2 5 3.2 Cc1noc2ccc(Nc3n[nH]c4ncccc34)cc12 10.1021/acs.jmedchem.8b00994
CHEMBL4473211 178934 0 None -1 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 265 2 2 5 3.2 Cc1noc2ccc(Nc3n[nH]c4ncccc34)cc12 10.1021/acs.jmedchem.8b00994
122193176 130709 0 None -28 3 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of human mGlu4 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay
ChEMBL 414 3 1 4 4.9 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
CHEMBL3628112 130709 0 None -28 3 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of human mGlu4 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay
ChEMBL 414 3 1 4 4.9 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
135126573 176411 0 None -1 2 Rat 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 401 3 1 5 3.6 Cc1nnc2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cc2c1C 10.1016/j.bmcl.2019.126678
CHEMBL4437035 176411 0 None -1 2 Rat 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 401 3 1 5 3.6 Cc1nnc2ccc(C(=O)NC3CN(c4cc(Cl)ncc4Cl)C3)cc2c1C 10.1016/j.bmcl.2019.126678
46918015 162647 0 None 3 4 Human 5.6 pEC50 = 5.6 Functional
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 334 7 5 7 0.4 N[C@@H](CCP(=O)(O)C(O)c1ccc(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4060360 162647 0 None 3 4 Human 5.6 pEC50 = 5.6 Functional
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 334 7 5 7 0.4 N[C@@H](CCP(=O)(O)C(O)c1ccc(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
137642290 165013 0 None 8 2 Human 5.6 pEC50 = 5.6 Functional
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 334 7 5 7 0.4 N[C@@H](CCP(=O)(O)C(O)c1ccc([N+](=O)[O-])c(O)c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4088251 165013 0 None 8 2 Human 5.6 pEC50 = 5.6 Functional
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 334 7 5 7 0.4 N[C@@H](CCP(=O)(O)C(O)c1ccc([N+](=O)[O-])c(O)c1)C(=O)O 10.1021/acs.jmedchem.7b01438
70691972 81024 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 261 2 0 3 3.4 c1ccc(-n2cc(-c3ccnc4c3CCC4)cn2)cc1 10.1016/j.bmcl.2012.03.032
CHEMBL2023632 81024 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 261 2 0 3 3.4 c1ccc(-n2cc(-c3ccnc4c3CCC4)cn2)cc1 10.1016/j.bmcl.2012.03.032
57765607 166184 0 None -1 2 Human 4.6 pEC50 = 4.6 Functional
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 334 7 5 7 0.4 N[C@@H](CCP(=O)(O)C(O)c1cccc([N+](=O)[O-])c1O)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4100788 166184 0 None -1 2 Human 4.6 pEC50 = 4.6 Functional
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 334 7 5 7 0.4 N[C@@H](CCP(=O)(O)C(O)c1cccc([N+](=O)[O-])c1O)C(=O)O 10.1021/acs.jmedchem.7b01438
1377 8122 26 None -138 8 Rat 4.6 pEC50 = 4.6 Functional
Metabotropic glutamate receptor 4 antagonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 4 antagonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 203 4 4 4 -1.6 N[C@@H](C1[C@H]([C@@H]1C(=O)O)C(=O)O)C(=O)O 10.1021/jm030967o
5310979 8122 26 None -138 8 Rat 4.6 pEC50 = 4.6 Functional
Metabotropic glutamate receptor 4 antagonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 4 antagonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 203 4 4 4 -1.6 N[C@@H](C1[C@H]([C@@H]1C(=O)O)C(=O)O)C(=O)O 10.1021/jm030967o
CHEMBL284193 8122 26 None -138 8 Rat 4.6 pEC50 = 4.6 Functional
Metabotropic glutamate receptor 4 antagonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 4 antagonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 203 4 4 4 -1.6 N[C@@H](C1[C@H]([C@@H]1C(=O)O)C(=O)O)C(=O)O 10.1021/jm030967o
134192062 172201 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 336 5 2 6 3.6 CC(C)COc1nn(C)c2cc(Nc3n[nH]c4cccnc34)ccc12 10.1016/j.bmcl.2018.06.034
CHEMBL4238603 172201 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 336 5 2 6 3.6 CC(C)COc1nn(C)c2cc(Nc3n[nH]c4cccnc34)ccc12 10.1016/j.bmcl.2018.06.034
52935191 150536 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 382 4 1 6 2.2 O=C(Nc1cnn(S(=O)(=O)c2cc(F)c(F)c(F)c2)c1)c1ccccn1 nan
CHEMBL3900841 150536 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 382 4 1 6 2.2 O=C(Nc1cnn(S(=O)(=O)c2cc(F)c(F)c(F)c2)c1)c1ccccn1 nan
52934737 152152 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 348 4 1 7 2.1 Cc1cccc(S(=O)(=O)n2cc(NC(=O)c3nccs3)cn2)c1 nan
CHEMBL3913761 152152 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 348 4 1 7 2.1 Cc1cccc(S(=O)(=O)n2cc(NC(=O)c3nccs3)cn2)c1 nan
127046775 146495 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
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 146495 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
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
52934968 151204 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 360 4 1 6 2.2 Cc1cc(F)ccc1S(=O)(=O)n1cc(NC(=O)c2ccccn2)cn1 nan
CHEMBL3906337 151204 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 360 4 1 6 2.2 Cc1cc(F)ccc1S(=O)(=O)n1cc(NC(=O)c2ccccn2)cn1 nan
51003329 74580 0 None -1 2 Rat 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 419 4 2 3 5.5 O=C(Nc1ccc(NC(=O)c2ccccn2)cc1Cl)c1cc(Cl)cc(Cl)c1 10.1021/jm101271s
CHEMBL1909431 74580 0 None -1 2 Rat 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 419 4 2 3 5.5 O=C(Nc1ccc(NC(=O)c2ccccn2)cc1Cl)c1cc(Cl)cc(Cl)c1 10.1021/jm101271s
87304273 163582 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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 390 5 1 7 3.5 O/N=c1\cc(-c2cc3cccn3cn2)oc2ccc(OCCN3CCCC3)cc12 10.1021/acs.jmedchem.7b00991
CHEMBL4071064 163582 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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 390 5 1 7 3.5 O/N=c1\cc(-c2cc3cccn3cn2)oc2ccc(OCCN3CCCC3)cc12 10.1021/acs.jmedchem.7b00991
54670591 153174 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 425 5 1 6 3.9 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccc(F)c(Cl)c1 nan
CHEMBL3921666 153174 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 425 5 1 6 3.9 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccc(F)c(Cl)c1 nan
51003281 64674 0 None -1 2 Rat 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 419 4 2 3 5.3 O=C(Nc1ccc(NC(=O)c2ccccc2Cl)c(C(F)(F)F)c1)c1ccccn1 10.1021/jm101271s
CHEMBL1672239 64674 0 None -1 2 Rat 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 419 4 2 3 5.3 O=C(Nc1ccc(NC(=O)c2ccccc2Cl)c(C(F)(F)F)c1)c1ccccn1 10.1021/jm101271s
49865452 22744 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilization
ChEMBL 386 5 1 4 4.0 O=C(Nc1ccc(S(=O)(=O)Cc2ccccc2Cl)cc1)c1ccccn1 10.1016/j.bmcl.2010.07.007
CHEMBL1223384 22744 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilization
ChEMBL 386 5 1 4 4.0 O=C(Nc1ccc(S(=O)(=O)Cc2ccccc2Cl)cc1)c1ccccn1 10.1016/j.bmcl.2010.07.007
134191580 188924 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 341 3 2 6 3.7 Cc1ccn(-c2nccc3cc(Nc4n[nH]c5cccnc45)ccc23)n1 10.1016/j.bmcl.2018.10.050
CHEMBL4782314 188924 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 341 3 2 6 3.7 Cc1ccn(-c2nccc3cc(Nc4n[nH]c5cccnc45)ccc23)n1 10.1016/j.bmcl.2018.10.050
51003327 64682 0 None 1 2 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 369 4 2 3 4.4 O=C(Nc1ccc(NC(=O)c2ccccc2F)c(Cl)c1)c1ccccn1 10.1021/jm101271s
CHEMBL1672247 64682 0 None 1 2 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 369 4 2 3 4.4 O=C(Nc1ccc(NC(=O)c2ccccc2F)c(Cl)c1)c1ccccn1 10.1021/jm101271s
53373768 160721 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 330 3 2 6 2.6 Clc1cc(Nc2n[nH]c3cccnc23)cnc1N1CCOCC1 nan
CHEMBL3983519 160721 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 330 3 2 6 2.6 Clc1cc(Nc2n[nH]c3cccnc23)cnc1N1CCOCC1 nan
52935189 147291 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 396 4 1 6 2.8 O=C(Nc1cnn(S(=O)(=O)c2ccc(C(F)(F)F)cc2)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
CHEMBL3810136 147291 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 396 4 1 6 2.8 O=C(Nc1cnn(S(=O)(=O)c2ccc(C(F)(F)F)cc2)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
134190171 178055 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 319 3 2 5 4.5 c1cnc2[nH]nc(Nc3ccc4c(C5CCCC5)noc4c3)c2c1 10.1021/acs.jmedchem.8b00994
CHEMBL4460527 178055 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 319 3 2 5 4.5 c1cnc2[nH]nc(Nc3ccc4c(C5CCCC5)noc4c3)c2c1 10.1021/acs.jmedchem.8b00994
134191963 172548 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 319 3 2 6 3.0 Cn1nc(C2(C)CC2)c2ccc(Nc3n[nH]c4nccnc34)cc21 10.1016/j.bmcl.2018.06.034
CHEMBL4247139 172548 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 319 3 2 6 3.0 Cn1nc(C2(C)CC2)c2ccc(Nc3n[nH]c4nccnc34)cc21 10.1016/j.bmcl.2018.06.034
3956 10807 87 None -1 2 Human 6.6 pEC50 = 6.6 Functional
Activity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilizationActivity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilization
ChEMBL 262 3 1 3 3.0 COc1cc(ccc1Cl)NC(=O)c1ccccn1 10.1021/jm9005065
44191096 10807 87 None -1 2 Human 6.6 pEC50 = 6.6 Functional
Activity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilizationActivity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilization
ChEMBL 262 3 1 3 3.0 COc1cc(ccc1Cl)NC(=O)c1ccccn1 10.1021/jm9005065
CHEMBL562551 10807 87 None -1 2 Human 6.6 pEC50 = 6.6 Functional
Activity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilizationActivity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilization
ChEMBL 262 3 1 3 3.0 COc1cc(ccc1Cl)NC(=O)c1ccccn1 10.1021/jm9005065
3956 10807 87 None -1 2 Human 6.6 pEC50 = 6.6 Functional
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 262 3 1 3 3.0 COc1cc(ccc1Cl)NC(=O)c1ccccn1 10.1021/jm200290z
44191096 10807 87 None -1 2 Human 6.6 pEC50 = 6.6 Functional
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 262 3 1 3 3.0 COc1cc(ccc1Cl)NC(=O)c1ccccn1 10.1021/jm200290z
CHEMBL562551 10807 87 None -1 2 Human 6.6 pEC50 = 6.6 Functional
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 262 3 1 3 3.0 COc1cc(ccc1Cl)NC(=O)c1ccccn1 10.1021/jm200290z
136503384 163579 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
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 289 1 1 5 3.3 O/N=c1\cc(-c2cc3ncccc3cn2)oc2ccccc12 10.1021/acs.jmedchem.7b00991
CHEMBL4071024 163579 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
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 289 1 1 5 3.3 O/N=c1\cc(-c2cc3ncccc3cn2)oc2ccccc12 10.1021/acs.jmedchem.7b00991
57765556 163460 0 None 1 2 Human 5.6 pEC50 = 5.6 Functional
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 379 8 5 9 0.3 N[C@@H](CCP(=O)(O)C(O)c1cc([N+](=O)[O-])cc([N+](=O)[O-])c1O)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4069700 163460 0 None 1 2 Human 5.6 pEC50 = 5.6 Functional
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 379 8 5 9 0.3 N[C@@H](CCP(=O)(O)C(O)c1cc([N+](=O)[O-])cc([N+](=O)[O-])c1O)C(=O)O 10.1021/acs.jmedchem.7b01438
24779945 15013 0 None 3 3 Rat 5.6 pEC50 = 5.6 Functional
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 297 9 5 5 -0.8 N[C@@H](CCP(=O)(O)CC(CC(=O)O)C(=O)O)C(=O)O 10.1021/jm901523t
CHEMBL1092315 15013 0 None 3 3 Rat 5.6 pEC50 = 5.6 Functional
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 297 9 5 5 -0.8 N[C@@H](CCP(=O)(O)CC(CC(=O)O)C(=O)O)C(=O)O 10.1021/jm901523t
24779944 14640 0 None -2 3 Rat 5.6 pEC50 = 5.6 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 225 6 4 4 -0.9 N[C@@H](CCP(=O)(O)CC(=O)O)C(=O)O 10.1021/jm901523t
CHEMBL1089852 14640 0 None -2 3 Rat 5.6 pEC50 = 5.6 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 225 6 4 4 -0.9 N[C@@H](CCP(=O)(O)CC(=O)O)C(=O)O 10.1021/jm901523t
53387883 72306 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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 286 2 3 5 2.8 Cc1cc(Nc2nc3c(s2)CCCc2n[nH]cc2-3)n[nH]1 10.1021/jm200290z
CHEMBL1830713 72306 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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 286 2 3 5 2.8 Cc1cc(Nc2nc3c(s2)CCCc2n[nH]cc2-3)n[nH]1 10.1021/jm200290z
70683531 81023 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 260 2 1 3 3.4 c1ccc(-n2cc(-c3n[nH]c4ccccc34)cn2)cc1 10.1016/j.bmcl.2012.03.032
CHEMBL2023631 81023 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 260 2 1 3 3.4 c1ccc(-n2cc(-c3n[nH]c4ccccc34)cn2)cc1 10.1016/j.bmcl.2012.03.032
134190171 178055 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 319 3 2 5 4.5 c1cnc2[nH]nc(Nc3ccc4c(C5CCCC5)noc4c3)c2c1 10.1021/acs.jmedchem.8b00994
CHEMBL4460527 178055 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 319 3 2 5 4.5 c1cnc2[nH]nc(Nc3ccc4c(C5CCCC5)noc4c3)c2c1 10.1021/acs.jmedchem.8b00994
137646034 164555 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
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 0.9 N[C@@H](CCP(=O)(O)Cc1ccc(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4082813 164555 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
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 0.9 N[C@@H](CCP(=O)(O)Cc1ccc(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
52935189 147291 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 396 4 1 6 2.8 O=C(Nc1cnn(S(=O)(=O)c2ccc(C(F)(F)F)cc2)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
CHEMBL3810136 147291 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 396 4 1 6 2.8 O=C(Nc1cnn(S(=O)(=O)c2ccc(C(F)(F)F)cc2)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
137661528 166286 0 None -3 4 Human 5.6 pEC50 = 5.6 Functional
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 352 7 5 7 0.5 N[C@@H](CCP(=O)(O)[C@H](O)c1cc(F)c(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4101970 166286 0 None -3 4 Human 5.6 pEC50 = 5.6 Functional
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 352 7 5 7 0.5 N[C@@H](CCP(=O)(O)[C@H](O)c1cc(F)c(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
54670592 159484 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 441 5 1 6 4.1 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1cccc(C(F)(F)F)c1 nan
CHEMBL3972975 159484 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 441 5 1 6 4.1 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1cccc(C(F)(F)F)c1 nan
122196105 131018 0 None -22 2 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 448 3 1 4 5.3 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(C(F)(F)F)c1 10.1016/j.bmcl.2015.10.013
CHEMBL3634428 131018 0 None -22 2 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 448 3 1 4 5.3 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(C(F)(F)F)c1 10.1016/j.bmcl.2015.10.013
136503375 165021 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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 356 1 1 4 5.0 O/N=c1\cc(-c2cc3ccccc3cn2)oc2ccc(C(F)(F)F)cc12 10.1021/acs.jmedchem.7b00991
CHEMBL4088412 165021 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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 356 1 1 4 5.0 O/N=c1\cc(-c2cc3ccccc3cn2)oc2ccc(C(F)(F)F)cc12 10.1021/acs.jmedchem.7b00991
52935413 159672 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 356 5 1 6 2.3 CCc1ccc(S(=O)(=O)n2cc(NC(=O)c3ccccn3)cn2)cc1 nan
CHEMBL3974630 159672 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 356 5 1 6 2.3 CCc1ccc(S(=O)(=O)n2cc(NC(=O)c3ccccn3)cn2)cc1 nan
127030386 145819 0 None 7 3 Rat 5.6 pEC50 = 5.6 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 217 5 4 4 -1.0 N[C@@H](C[C@@]1(C(=O)O)C[C@@H]1C(=O)O)C(=O)O 10.1021/acs.jmedchem.5b01333
CHEMBL3786026 145819 0 None 7 3 Rat 5.6 pEC50 = 5.6 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 217 5 4 4 -1.0 N[C@@H](C[C@@]1(C(=O)O)C[C@@H]1C(=O)O)C(=O)O 10.1021/acs.jmedchem.5b01333
134191677 187342 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 366 3 2 5 4.1 FC1(F)CCN(c2nccc3cc(Nc4n[nH]c5cccnc45)ccc23)C1 10.1016/j.bmcl.2018.10.050
CHEMBL4754007 187342 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 366 3 2 5 4.1 FC1(F)CCN(c2nccc3cc(Nc4n[nH]c5cccnc45)ccc23)C1 10.1016/j.bmcl.2018.10.050
54670119 159218 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 417 6 1 6 3.8 O=C(Nc1nc(C2CC2)c(S(=O)(=O)Cc2ccccc2F)s1)c1ccccn1 nan
CHEMBL3970768 159218 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 417 6 1 6 3.8 O=C(Nc1nc(C2CC2)c(S(=O)(=O)Cc2ccccc2F)s1)c1ccccn1 nan
137659319 166120 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
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 441 5 1 6 5.3 O/N=c1\cc(-c2cc3sccc3cn2)oc2ccc(CCCN3CCC(F)(F)C3)cc12 10.1021/acs.jmedchem.7b00991
CHEMBL4100168 166120 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
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 441 5 1 6 5.3 O/N=c1\cc(-c2cc3sccc3cn2)oc2ccc(CCCN3CCC(F)(F)C3)cc12 10.1021/acs.jmedchem.7b00991
70687765 80995 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 359 7 0 5 4.5 COCCCOc1ccc2c(-c3cnn(-c4ccccc4)c3)ccnc2c1 10.1016/j.bmcl.2012.03.032
CHEMBL2023462 80995 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 359 7 0 5 4.5 COCCCOc1ccc2c(-c3cnn(-c4ccccc4)c3)ccnc2c1 10.1016/j.bmcl.2012.03.032
122197948 167229 0 None 5 2 Rat 5.6 pEC50 = 5.6 Functional
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 421 12 6 8 -0.3 N[C@H](CCP(=O)(O)C(O)c1ccc(OCC(=O)O)c(OCC(=O)O)c1)C(=O)O nan
CHEMBL4111698 167229 0 None 5 2 Rat 5.6 pEC50 = 5.6 Functional
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 421 12 6 8 -0.3 N[C@H](CCP(=O)(O)C(O)c1ccc(OCC(=O)O)c(OCC(=O)O)c1)C(=O)O nan
70687777 81022 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 259 2 1 2 4.0 c1ccc(-n2cc(-c3c[nH]c4ccccc34)cn2)cc1 10.1016/j.bmcl.2012.03.032
CHEMBL2023630 81022 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 259 2 1 2 4.0 c1ccc(-n2cc(-c3c[nH]c4ccccc34)cn2)cc1 10.1016/j.bmcl.2012.03.032
44572113 195677 4 None -1 2 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of recombinant human mGlu4 receptor expressed in HEK293 cells co-expressing chimeric G protein assessed as increase in EC20 glutamate-induced cAMP levelPositive allosteric modulation of recombinant human mGlu4 receptor expressed in HEK293 cells co-expressing chimeric G protein assessed as increase in EC20 glutamate-induced cAMP level
ChEMBL 294 2 2 4 2.7 O=C(Nc1ccccc1)[C@]12C[C@H]1/C(=N\O)c1ccccc1O2 10.1021/acs.jmedchem.7b00991
CHEMBL507522 195677 4 None -1 2 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of recombinant human mGlu4 receptor expressed in HEK293 cells co-expressing chimeric G protein assessed as increase in EC20 glutamate-induced cAMP levelPositive allosteric modulation of recombinant human mGlu4 receptor expressed in HEK293 cells co-expressing chimeric G protein assessed as increase in EC20 glutamate-induced cAMP level
ChEMBL 294 2 2 4 2.7 O=C(Nc1ccccc1)[C@]12C[C@H]1/C(=N\O)c1ccccc1O2 10.1021/acs.jmedchem.7b00991
137635566 163046 0 None -1 2 Human 4.6 pEC50 = 4.6 Functional
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 401 13 4 6 2.8 CCCCCCNC(c1cccc([N+](=O)[O-])c1)P(=O)(O)CC[C@H](N)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4065012 163046 0 None -1 2 Human 4.6 pEC50 = 4.6 Functional
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 401 13 4 6 2.8 CCCCCCNC(c1cccc([N+](=O)[O-])c1)P(=O)(O)CC[C@H](N)C(=O)O 10.1021/acs.jmedchem.7b01438
135125797 180432 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 374 4 1 6 2.5 Cc1nnc2ccc(C(=O)NC3CN(c4cnc(C5CC5)cn4)C3)cc2c1C 10.1016/j.bmcl.2019.126678
CHEMBL4534485 180432 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 374 4 1 6 2.5 Cc1nnc2ccc(C(=O)NC3CN(c4cnc(C5CC5)cn4)C3)cc2c1C 10.1016/j.bmcl.2019.126678
52913772 147231 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 359 5 1 5 2.7 O=C(Nc1ccn(S(=O)(=O)Cc2ccccc2F)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
CHEMBL3809364 147231 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 359 5 1 5 2.7 O=C(Nc1ccn(S(=O)(=O)Cc2ccccc2F)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
52913772 147231 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 359 5 1 5 2.7 O=C(Nc1ccn(S(=O)(=O)Cc2ccccc2F)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
CHEMBL3809364 147231 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 359 5 1 5 2.7 O=C(Nc1ccn(S(=O)(=O)Cc2ccccc2F)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
127046254 146654 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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 407 4 2 5 3.5 Nc1cccnc1C(=O)Nc1ccc(N2CC(c3cccnc3)CC2=O)c(Cl)c1 10.1016/j.bmcl.2016.04.041
CHEMBL3799281 146654 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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 407 4 2 5 3.5 Nc1cccnc1C(=O)Nc1ccc(N2CC(c3cccnc3)CC2=O)c(Cl)c1 10.1016/j.bmcl.2016.04.041
127026137 144588 0 None -1 2 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human mGlu4 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu4 receptor by cell based calcium mobilization
ChEMBL 382 3 1 6 3.1 Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3cccnc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3759705 144588 0 None -1 2 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human mGlu4 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu4 receptor by cell based calcium mobilization
ChEMBL 382 3 1 6 3.1 Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3cccnc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
122196117 131029 0 None -12 2 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 382 3 1 6 3.1 Cc1ccoc1C(=O)Nc1cnc(N2C(=O)c3cccc(Cl)c3C2=O)nc1 10.1016/j.bmcl.2015.10.013
CHEMBL3634439 131029 0 None -12 2 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 382 3 1 6 3.1 Cc1ccoc1C(=O)Nc1cnc(N2C(=O)c3cccc(Cl)c3C2=O)nc1 10.1016/j.bmcl.2015.10.013
137634489 162626 0 None 1 2 Human 4.6 pEC50 = 4.6 Functional
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 407 10 4 6 2.5 N[C@@H](CCP(=O)(O)C(NCc1ccccc1)c1cccc([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4060099 162626 0 None 1 2 Human 4.6 pEC50 = 4.6 Functional
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 407 10 4 6 2.5 N[C@@H](CCP(=O)(O)C(NCc1ccccc1)c1cccc([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
53375182 157081 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 276 4 2 4 3.3 FC(F)Oc1cccc(Nc2n[nH]c3cccnc23)c1 nan
CHEMBL3952838 157081 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 276 4 2 4 3.3 FC(F)Oc1cccc(Nc2n[nH]c3cccnc23)c1 nan
54670222 147236 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 425 5 1 6 3.9 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccc(Cl)cc1F nan
CHEMBL3809402 147236 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 425 5 1 6 3.9 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccc(Cl)cc1F nan
145986132 172234 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 264 2 2 5 2.6 Cn1ncc2ccc(Nc3n[nH]c4cccnc34)cc21 10.1016/j.bmcl.2018.06.034
CHEMBL4239399 172234 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 264 2 2 5 2.6 Cn1ncc2ccc(Nc3n[nH]c4cccnc34)cc21 10.1016/j.bmcl.2018.06.034
53374111 150149 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 238 3 2 3 3.3 CCc1cccc(Nc2n[nH]c3cccnc23)c1 nan
CHEMBL3897746 150149 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 238 3 2 3 3.3 CCc1cccc(Nc2n[nH]c3cccnc23)c1 nan
122419077 179599 0 None 3 2 Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 401 4 3 7 3.2 O=C(NC1CC(F)(F)C1)c1nsc2cc(Nc3n[nH]c4nccnc34)ccc12 10.1021/acs.jmedchem.8b00994
CHEMBL4514040 179599 0 None 3 2 Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 401 4 3 7 3.2 O=C(NC1CC(F)(F)C1)c1nsc2cc(Nc3n[nH]c4nccnc34)ccc12 10.1021/acs.jmedchem.8b00994
122419077 179599 0 None 3 2 Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 401 4 3 7 3.2 O=C(NC1CC(F)(F)C1)c1nsc2cc(Nc3n[nH]c4nccnc34)ccc12 10.1021/acs.jmedchem.8b00994
CHEMBL4514040 179599 0 None 3 2 Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 401 4 3 7 3.2 O=C(NC1CC(F)(F)C1)c1nsc2cc(Nc3n[nH]c4nccnc34)ccc12 10.1021/acs.jmedchem.8b00994
52935408 155893 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 392 5 1 7 2.4 COc1ccc(S(=O)(=O)n2cc(NC(=O)c3ccccn3)cn2)cc1Cl nan
CHEMBL3943225 155893 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 392 5 1 7 2.4 COc1ccc(S(=O)(=O)n2cc(NC(=O)c3ccccn3)cn2)cc1Cl nan
122197954 166714 0 None 6 3 Rat 6.6 pEC50 = 6.6 Functional
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 392 10 5 8 0.1 N[C@H](CCP(=O)(O)C(O)c1ccc(OCC(=O)O)c([N+](=O)[O-])c1)C(=O)O nan
CHEMBL4107228 166714 0 None 6 3 Rat 6.6 pEC50 = 6.6 Functional
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 392 10 5 8 0.1 N[C@H](CCP(=O)(O)C(O)c1ccc(OCC(=O)O)c([N+](=O)[O-])c1)C(=O)O nan
24780087 15129 0 None - 1 Rat 4.6 pEC50 = 4.6 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 307 7 4 4 0.5 N[C@@H](CCP(=O)(O)C(CC(=O)O)C(F)(F)F)C(=O)O 10.1021/jm901523t
CHEMBL1093010 15129 0 None - 1 Rat 4.6 pEC50 = 4.6 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 307 7 4 4 0.5 N[C@@H](CCP(=O)(O)C(CC(=O)O)C(F)(F)F)C(=O)O 10.1021/jm901523t
135126274 178288 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 435 3 1 5 3.9 Cc1nnc2ccc(C(=O)NC3CN(c4ncc(C(F)(F)F)cc4Cl)C3)cc2c1C 10.1016/j.bmcl.2019.126678
CHEMBL4463993 178288 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 435 3 1 5 3.9 Cc1nnc2ccc(C(=O)NC3CN(c4ncc(C(F)(F)F)cc4Cl)C3)cc2c1C 10.1016/j.bmcl.2019.126678
122196097 131010 0 None -9 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 398 3 1 4 4.4 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(F)c1 10.1016/j.bmcl.2015.10.013
CHEMBL3634420 131010 0 None -9 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 398 3 1 4 4.4 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(F)c1 10.1016/j.bmcl.2015.10.013
162665462 189127 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 277 2 3 4 2.5 O=c1[nH]ccc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1016/j.bmcl.2018.10.050
CHEMBL4784617 189127 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 277 2 3 4 2.5 O=c1[nH]ccc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1016/j.bmcl.2018.10.050
122196095 131008 0 None -12 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 364 3 1 4 3.8 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(F)c1 10.1016/j.bmcl.2015.10.013
CHEMBL3634418 131008 0 None -12 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 364 3 1 4 3.8 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(F)c1 10.1016/j.bmcl.2015.10.013
134198340 172665 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 332 3 2 5 4.5 Cc1nn(C2CCCC2)c2ccc(Nc3n[nH]c4cccnc34)cc12 10.1016/j.bmcl.2018.06.034
CHEMBL4249560 172665 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 332 3 2 5 4.5 Cc1nn(C2CCCC2)c2ccc(Nc3n[nH]c4cccnc34)cc12 10.1016/j.bmcl.2018.06.034
52935189 147291 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 396 4 1 6 2.8 O=C(Nc1cnn(S(=O)(=O)c2ccc(C(F)(F)F)cc2)c1)c1ccccn1 nan
CHEMBL3810136 147291 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 396 4 1 6 2.8 O=C(Nc1cnn(S(=O)(=O)c2ccc(C(F)(F)F)cc2)c1)c1ccccn1 nan
162670460 189674 0 None -4 3 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 382 3 1 4 4.0 Cc1cc(N2C(=O)C3=C(CCCC3)C2=O)c(F)cc1NC(=O)c1occc1C 10.1016/j.bmcl.2020.127724
CHEMBL4792152 189674 0 None -4 3 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 382 3 1 4 4.0 Cc1cc(N2C(=O)C3=C(CCCC3)C2=O)c(F)cc1NC(=O)c1occc1C 10.1016/j.bmcl.2020.127724
162648752 186731 0 None -4 3 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 418 3 1 4 4.2 Cc1ccoc1C(=O)Nc1cc(F)c(N2C(=O)c3cccc(F)c3C2=O)c(F)c1F 10.1016/j.bmcl.2020.127724
CHEMBL4746530 186731 0 None -4 3 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 418 3 1 4 4.2 Cc1ccoc1C(=O)Nc1cc(F)c(N2C(=O)c3cccc(F)c3C2=O)c(F)c1F 10.1016/j.bmcl.2020.127724
52914548 147221 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 359 4 1 5 2.8 Cc1cc(S(=O)(=O)n2ccc(NC(=O)c3ccccn3)c2)ccc1F 10.1016/j.bmcl.2016.05.029
CHEMBL3809272 147221 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 359 4 1 5 2.8 Cc1cc(S(=O)(=O)n2ccc(NC(=O)c3ccccn3)c2)ccc1F 10.1016/j.bmcl.2016.05.029
49865398 22720 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilization
ChEMBL 392 5 2 4 4.5 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2Cl)cc1)c1ccsc1 10.1016/j.bmcl.2010.07.007
CHEMBL1223313 22720 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilization
ChEMBL 392 5 2 4 4.5 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2Cl)cc1)c1ccsc1 10.1016/j.bmcl.2010.07.007
121485534 177770 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 337 3 2 5 4.9 CC(C)(C)Cc1nsc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
CHEMBL4456258 177770 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 337 3 2 5 4.9 CC(C)(C)Cc1nsc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
52914548 147221 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 359 4 1 5 2.8 Cc1cc(S(=O)(=O)n2ccc(NC(=O)c3ccccn3)c2)ccc1F 10.1016/j.bmcl.2016.05.029
CHEMBL3809272 147221 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 359 4 1 5 2.8 Cc1cc(S(=O)(=O)n2ccc(NC(=O)c3ccccn3)c2)ccc1F 10.1016/j.bmcl.2016.05.029
121485534 177770 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 337 3 2 5 4.9 CC(C)(C)Cc1nsc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
CHEMBL4456258 177770 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 337 3 2 5 4.9 CC(C)(C)Cc1nsc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
46182708 22637 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilization
ChEMBL 387 5 2 4 3.8 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2Cl)cc1)c1ccccn1 10.1016/j.bmcl.2010.07.007
CHEMBL1223083 22637 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilization
ChEMBL 387 5 2 4 3.8 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2Cl)cc1)c1ccccn1 10.1016/j.bmcl.2010.07.007
87305070 163295 0 None 2 2 Rat 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of rat 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 rat 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 406 5 1 8 2.7 O/N=c1\cc(-c2cc3cccn3cn2)oc2ccc(OCCN3CCOCC3)cc12 10.1021/acs.jmedchem.7b00991
CHEMBL4067875 163295 0 None 2 2 Rat 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of rat 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 rat 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 406 5 1 8 2.7 O/N=c1\cc(-c2cc3cccn3cn2)oc2ccc(OCCN3CCOCC3)cc12 10.1021/acs.jmedchem.7b00991
40605829 205323 1 None - 1 Human 5.6 pEC50 = 5.6 Functional
Allosteric modulator activity at human mGlu4 receptor expressed in CHO cells coexpressing Gqi5 assessed as effect on calcium fluxAllosteric modulator activity at human mGlu4 receptor expressed in CHO cells coexpressing Gqi5 assessed as effect on calcium flux
ChEMBL 313 3 2 2 3.6 O=C(Nc1cc(Cl)cc(Cl)c1)[C@H]1CC=CC[C@H]1C(=O)O 10.1016/j.bmcl.2009.07.072
CHEMBL578129 205323 1 None - 1 Human 5.6 pEC50 = 5.6 Functional
Allosteric modulator activity at human mGlu4 receptor expressed in CHO cells coexpressing Gqi5 assessed as effect on calcium fluxAllosteric modulator activity at human mGlu4 receptor expressed in CHO cells coexpressing Gqi5 assessed as effect on calcium flux
ChEMBL 313 3 2 2 3.6 O=C(Nc1cc(Cl)cc(Cl)c1)[C@H]1CC=CC[C@H]1C(=O)O 10.1016/j.bmcl.2009.07.072
53388193 72321 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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 313 3 3 6 2.7 OCc1cccc(Nc2nc3c(s2)CCCc2n[nH]cc2-3)n1 10.1021/jm200290z
CHEMBL1830909 72321 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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 313 3 3 6 2.7 OCc1cccc(Nc2nc3c(s2)CCCc2n[nH]cc2-3)n1 10.1021/jm200290z
57478075 81021 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 260 2 1 3 3.4 c1ccc(-n2cc(-c3ccnc4[nH]ccc34)cn2)cc1 10.1016/j.bmcl.2012.03.032
CHEMBL2023629 81021 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 260 2 1 3 3.4 c1ccc(-n2cc(-c3ccnc4[nH]ccc34)cn2)cc1 10.1016/j.bmcl.2012.03.032
54670967 161116 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 461 5 1 6 4.4 O=C(Nc1nc(C(F)(F)F)c(S(=O)(=O)Cc2ccccc2Cl)s1)c1ccccn1 nan
CHEMBL3986822 161116 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 461 5 1 6 4.4 O=C(Nc1nc(C(F)(F)F)c(S(=O)(=O)Cc2ccccc2Cl)s1)c1ccccn1 nan
134190227 177970 0 None -5 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 283 2 2 5 3.3 Cc1noc2c(F)cc(Nc3n[nH]c4cccnc34)cc12 10.1021/acs.jmedchem.8b00994
CHEMBL4459205 177970 0 None -5 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 283 2 2 5 3.3 Cc1noc2c(F)cc(Nc3n[nH]c4cccnc34)cc12 10.1021/acs.jmedchem.8b00994
50902540 83968 1 None - 1 Rat 4.6 pEC50 = 4.6 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells coexpressing Gq/Gi and EAAC1 assessed as intracellular calcium production measured every 1.5 secs for 60 secs by Fluo-4-AM based fluorometryAgonist activity at rat mGlu4 receptor expressed in HEK293 cells coexpressing Gq/Gi and EAAC1 assessed as intracellular calcium production measured every 1.5 secs for 60 secs by Fluo-4-AM based fluorometry
ChEMBL 229 3 5 4 -1.6 N[C@]1(C(=O)O)C[C@@]1(F)C(O)P(=O)(O)O 10.1016/j.bmc.2012.06.006
CHEMBL2058382 83968 1 None - 1 Rat 4.6 pEC50 = 4.6 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells coexpressing Gq/Gi and EAAC1 assessed as intracellular calcium production measured every 1.5 secs for 60 secs by Fluo-4-AM based fluorometryAgonist activity at rat mGlu4 receptor expressed in HEK293 cells coexpressing Gq/Gi and EAAC1 assessed as intracellular calcium production measured every 1.5 secs for 60 secs by Fluo-4-AM based fluorometry
ChEMBL 229 3 5 4 -1.6 N[C@]1(C(=O)O)C[C@@]1(F)C(O)P(=O)(O)O 10.1016/j.bmc.2012.06.006
CHEMBL2079098 83968 1 None - 1 Rat 4.6 pEC50 = 4.6 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells coexpressing Gq/Gi and EAAC1 assessed as intracellular calcium production measured every 1.5 secs for 60 secs by Fluo-4-AM based fluorometryAgonist activity at rat mGlu4 receptor expressed in HEK293 cells coexpressing Gq/Gi and EAAC1 assessed as intracellular calcium production measured every 1.5 secs for 60 secs by Fluo-4-AM based fluorometry
ChEMBL 229 3 5 4 -1.6 N[C@]1(C(=O)O)C[C@@]1(F)C(O)P(=O)(O)O 10.1016/j.bmc.2012.06.006
122419161 176997 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 380 3 2 7 2.8 O=C(c1nsc2cc(Nc3n[nH]c4cccnc34)ccc12)N1CCOCC1 10.1021/acs.jmedchem.8b00994
CHEMBL4445465 176997 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 380 3 2 7 2.8 O=C(c1nsc2cc(Nc3n[nH]c4cccnc34)ccc12)N1CCOCC1 10.1021/acs.jmedchem.8b00994
122419161 176997 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 380 3 2 7 2.8 O=C(c1nsc2cc(Nc3n[nH]c4cccnc34)ccc12)N1CCOCC1 10.1021/acs.jmedchem.8b00994
CHEMBL4445465 176997 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 380 3 2 7 2.8 O=C(c1nsc2cc(Nc3n[nH]c4cccnc34)ccc12)N1CCOCC1 10.1021/acs.jmedchem.8b00994
134190227 177970 0 None -5 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 283 2 2 5 3.3 Cc1noc2c(F)cc(Nc3n[nH]c4cccnc34)cc12 10.1021/acs.jmedchem.8b00994
CHEMBL4459205 177970 0 None -5 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 283 2 2 5 3.3 Cc1noc2c(F)cc(Nc3n[nH]c4cccnc34)cc12 10.1021/acs.jmedchem.8b00994
127026471 144585 0 None -4 2 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human mGlu4 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu4 receptor by cell based calcium mobilization
ChEMBL 394 3 2 4 3.7 Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3[nH]ncc3C)cc1Cl)C2=O 10.1016/j.bmcl.2015.12.104
CHEMBL3759656 144585 0 None -4 2 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human mGlu4 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu4 receptor by cell based calcium mobilization
ChEMBL 394 3 2 4 3.7 Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3[nH]ncc3C)cc1Cl)C2=O 10.1016/j.bmcl.2015.12.104
53374307 152256 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 322 4 2 6 3.4 Fc1cc(Nc2n[nH]c3cccnc23)ccc1Oc1ncccn1 nan
CHEMBL3914548 152256 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 322 4 2 6 3.4 Fc1cc(Nc2n[nH]c3cccnc23)ccc1Oc1ncccn1 nan
122197937 167087 0 None 13 3 Rat 6.6 pEC50 = 6.6 Functional
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 422 11 5 9 0.1 COc1cc(C(O)P(=O)(O)CC[C@@H](N)C(=O)O)cc([N+](=O)[O-])c1OCC(=O)O nan
CHEMBL4110535 167087 0 None 13 3 Rat 6.6 pEC50 = 6.6 Functional
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 422 11 5 9 0.1 COc1cc(C(O)P(=O)(O)CC[C@@H](N)C(=O)O)cc([N+](=O)[O-])c1OCC(=O)O nan
137642559 165124 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
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 277 1 1 5 3.0 O/N=c1\cc(-c2cn3cccc3cn2)oc2ccccc12 10.1021/acs.jmedchem.7b00991
CHEMBL4089473 165124 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
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 277 1 1 5 3.0 O/N=c1\cc(-c2cn3cccc3cn2)oc2ccccc12 10.1021/acs.jmedchem.7b00991
44191099 202781 6 None - 1 Human 5.6 pEC50 = 5.6 Functional
Activity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilizationActivity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilization
ChEMBL 267 2 1 3 3.0 O=C(Nc1ccc(Cl)c(Cl)c1)c1ccncn1 10.1021/jm9005065
CHEMBL560021 202781 6 None - 1 Human 5.6 pEC50 = 5.6 Functional
Activity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilizationActivity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilization
ChEMBL 267 2 1 3 3.0 O=C(Nc1ccc(Cl)c(Cl)c1)c1ccncn1 10.1021/jm9005065
57765525 166233 0 None -1 3 Human 5.6 pEC50 = 5.6 Functional
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 332 7 4 6 1.0 Cc1ccc(C(O)P(=O)(O)CC[C@H](N)C(=O)O)cc1[N+](=O)[O-] 10.1021/acs.jmedchem.7b01438
CHEMBL4101241 166233 0 None -1 3 Human 5.6 pEC50 = 5.6 Functional
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 332 7 4 6 1.0 Cc1ccc(C(O)P(=O)(O)CC[C@H](N)C(=O)O)cc1[N+](=O)[O-] 10.1021/acs.jmedchem.7b01438
70683515 80996 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 414 7 0 6 4.2 c1ccc(-n2cc(-c3ccnc4cc(OCCCN5CCOCC5)ccc34)cn2)cc1 10.1016/j.bmcl.2012.03.032
CHEMBL2023466 80996 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 414 7 0 6 4.2 c1ccc(-n2cc(-c3ccnc4cc(OCCCN5CCOCC5)ccc34)cn2)cc1 10.1016/j.bmcl.2012.03.032
137631886 163155 0 None -1 2 Human 4.6 pEC50 = 4.6 Functional
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 274 6 4 5 0.1 N[C@@H](CCP(=O)(O)C(O)c1ccncc1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4066249 163155 0 None -1 2 Human 4.6 pEC50 = 4.6 Functional
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 274 6 4 5 0.1 N[C@@H](CCP(=O)(O)C(O)c1ccncc1)C(=O)O 10.1021/acs.jmedchem.7b01438
134190028 178061 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 321 3 2 5 4.4 CC(C)(C)Cc1noc2cc(Nc3n[nH]c4ncccc34)ccc12 10.1021/acs.jmedchem.8b00994
CHEMBL4460568 178061 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 321 3 2 5 4.4 CC(C)(C)Cc1noc2cc(Nc3n[nH]c4ncccc34)ccc12 10.1021/acs.jmedchem.8b00994
127046933 146776 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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 384 4 2 4 3.7 CC1(C2CC2)CC(=O)N(c2ccc(NC(=O)c3ncccc3N)cc2Cl)C1 10.1016/j.bmcl.2016.04.041
CHEMBL3799999 146776 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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 384 4 2 4 3.7 CC1(C2CC2)CC(=O)N(c2ccc(NC(=O)c3ncccc3N)cc2Cl)C1 10.1016/j.bmcl.2016.04.041
52935412 158378 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 382 4 1 6 2.2 O=C(Nc1cnn(S(=O)(=O)c2ccc(F)c(F)c2F)c1)c1ccccn1 nan
CHEMBL3963484 158378 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 382 4 1 6 2.2 O=C(Nc1cnn(S(=O)(=O)c2ccc(F)c(F)c2F)c1)c1ccccn1 nan
53375181 151429 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 274 3 2 4 3.4 COc1ccc(Nc2n[nH]c3cccnc23)cc1Cl nan
CHEMBL3908181 151429 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 274 3 2 4 3.4 COc1ccc(Nc2n[nH]c3cccnc23)cc1Cl nan
134190028 178061 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 321 3 2 5 4.4 CC(C)(C)Cc1noc2cc(Nc3n[nH]c4ncccc34)ccc12 10.1021/acs.jmedchem.8b00994
CHEMBL4460568 178061 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 321 3 2 5 4.4 CC(C)(C)Cc1noc2cc(Nc3n[nH]c4ncccc34)ccc12 10.1021/acs.jmedchem.8b00994
44572113 195677 4 None 1 2 Rat 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 294 2 2 4 2.7 O=C(Nc1ccccc1)[C@]12C[C@H]1/C(=N\O)c1ccccc1O2 10.1021/jm101271s
CHEMBL507522 195677 4 None 1 2 Rat 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 294 2 2 4 2.7 O=C(Nc1ccccc1)[C@]12C[C@H]1/C(=N\O)c1ccccc1O2 10.1021/jm101271s
53373658 159041 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 245 2 2 4 2.8 Clc1ccnc(Nc2n[nH]c3cccnc23)c1 nan
CHEMBL3969118 159041 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 245 2 2 4 2.8 Clc1ccnc(Nc2n[nH]c3cccnc23)c1 nan
122196096 131009 0 None -10 2 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 378 3 1 4 4.1 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c(F)c1 10.1016/j.bmcl.2015.10.013
CHEMBL3634419 131009 0 None -10 2 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 378 3 1 4 4.1 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c(F)c1 10.1016/j.bmcl.2015.10.013
56649127 75568 0 None -1 2 Human 6.5 pEC50 = 6.5 Functional
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 407 3 1 4 3.7 O=C(Nc1ccc(N2C(=O)[C@H]3[C@@H]4C=C[C@@H](CC4)[C@H]3C2=O)c(Cl)c1)c1ccccn1 10.1021/jm200956q
CHEMBL1921962 75568 0 None -1 2 Human 6.5 pEC50 = 6.5 Functional
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 407 3 1 4 3.7 O=C(Nc1ccc(N2C(=O)[C@H]3[C@@H]4C=C[C@@H](CC4)[C@H]3C2=O)c(Cl)c1)c1ccccn1 10.1021/jm200956q
122196106 131019 0 None -18 2 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 432 3 1 4 4.8 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(C(F)(F)F)c1 10.1016/j.bmcl.2015.10.013
CHEMBL3634429 131019 0 None -18 2 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 432 3 1 4 4.8 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(C(F)(F)F)c1 10.1016/j.bmcl.2015.10.013
1310 9095 110 None -426 17 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells coexpressing Gq/Gi and EAAC1 assessed as intracellular calcium production measured every 1.5 secs for 60 secs by Fluo-4-AM based fluorometryAgonist activity at rat mGlu4 receptor expressed in HEK293 cells coexpressing Gq/Gi and EAAC1 assessed as intracellular calcium production measured every 1.5 secs for 60 secs by Fluo-4-AM based fluorometry
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2012.06.006
1369 9095 110 None -426 17 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells coexpressing Gq/Gi and EAAC1 assessed as intracellular calcium production measured every 1.5 secs for 60 secs by Fluo-4-AM based fluorometryAgonist activity at rat mGlu4 receptor expressed in HEK293 cells coexpressing Gq/Gi and EAAC1 assessed as intracellular calcium production measured every 1.5 secs for 60 secs by Fluo-4-AM based fluorometry
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2012.06.006
33032 9095 110 None -426 17 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells coexpressing Gq/Gi and EAAC1 assessed as intracellular calcium production measured every 1.5 secs for 60 secs by Fluo-4-AM based fluorometryAgonist activity at rat mGlu4 receptor expressed in HEK293 cells coexpressing Gq/Gi and EAAC1 assessed as intracellular calcium production measured every 1.5 secs for 60 secs by Fluo-4-AM based fluorometry
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2012.06.006
44272391 9095 110 None -426 17 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells coexpressing Gq/Gi and EAAC1 assessed as intracellular calcium production measured every 1.5 secs for 60 secs by Fluo-4-AM based fluorometryAgonist activity at rat mGlu4 receptor expressed in HEK293 cells coexpressing Gq/Gi and EAAC1 assessed as intracellular calcium production measured every 1.5 secs for 60 secs by Fluo-4-AM based fluorometry
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2012.06.006
88747398 9095 110 None -426 17 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells coexpressing Gq/Gi and EAAC1 assessed as intracellular calcium production measured every 1.5 secs for 60 secs by Fluo-4-AM based fluorometryAgonist activity at rat mGlu4 receptor expressed in HEK293 cells coexpressing Gq/Gi and EAAC1 assessed as intracellular calcium production measured every 1.5 secs for 60 secs by Fluo-4-AM based fluorometry
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2012.06.006
CHEMBL575060 9095 110 None -426 17 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells coexpressing Gq/Gi and EAAC1 assessed as intracellular calcium production measured every 1.5 secs for 60 secs by Fluo-4-AM based fluorometryAgonist activity at rat mGlu4 receptor expressed in HEK293 cells coexpressing Gq/Gi and EAAC1 assessed as intracellular calcium production measured every 1.5 secs for 60 secs by Fluo-4-AM based fluorometry
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2012.06.006
DB00142 9095 110 None -426 17 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells coexpressing Gq/Gi and EAAC1 assessed as intracellular calcium production measured every 1.5 secs for 60 secs by Fluo-4-AM based fluorometryAgonist activity at rat mGlu4 receptor expressed in HEK293 cells coexpressing Gq/Gi and EAAC1 assessed as intracellular calcium production measured every 1.5 secs for 60 secs by Fluo-4-AM based fluorometry
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2012.06.006
134198076 172300 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 397 3 2 6 3.1 Cn1nc(C(=O)N2CCC(F)(F)C2)c2ccc(Nc3n[nH]c4cccnc34)cc21 10.1016/j.bmcl.2018.06.034
CHEMBL4241027 172300 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 397 3 2 6 3.1 Cn1nc(C(=O)N2CCC(F)(F)C2)c2ccc(Nc3n[nH]c4cccnc34)cc21 10.1016/j.bmcl.2018.06.034
54670221 154458 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 441 5 1 6 4.4 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccc(Cl)cc1Cl nan
CHEMBL3931820 154458 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 441 5 1 6 4.4 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccc(Cl)cc1Cl nan
53388042 72319 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 327 4 2 6 3.6 CCOc1cccc(Nc2nc3c(s2)CCCc2n[nH]cc2-3)n1 10.1021/jm200290z
CHEMBL1830906 72319 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 327 4 2 6 3.6 CCOc1cccc(Nc2nc3c(s2)CCCc2n[nH]cc2-3)n1 10.1021/jm200290z
22037226 80925 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 289 2 0 3 4.2 Fc1ccc(-n2cc(-c3ccnc4ccccc34)cn2)cc1 10.1016/j.bmcl.2012.03.032
CHEMBL2022871 80925 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 289 2 0 3 4.2 Fc1ccc(-n2cc(-c3ccnc4ccccc34)cn2)cc1 10.1016/j.bmcl.2012.03.032
49862581 21741 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
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 215 2 1 3 2.4 Nc1nccc(/C=C/c2ccccc2F)n1 10.1016/j.bmcl.2010.06.078
CHEMBL1208800 21741 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
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 215 2 1 3 2.4 Nc1nccc(/C=C/c2ccccc2F)n1 10.1016/j.bmcl.2010.06.078
54752951 75567 3 None 1 4 Human 6.5 pEC50 = 6.5 Functional
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 393 3 1 4 3.3 O=C(Nc1ccc(N2C(=O)[C@H]3[C@H]4C=C[C@H](C4)[C@H]3C2=O)c(Cl)c1)c1ccccn1 10.1021/jm200956q
CHEMBL1921961 75567 3 None 1 4 Human 6.5 pEC50 = 6.5 Functional
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 393 3 1 4 3.3 O=C(Nc1ccc(N2C(=O)[C@H]3[C@H]4C=C[C@H](C4)[C@H]3C2=O)c(Cl)c1)c1ccccn1 10.1021/jm200956q
54670872 156434 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 453 6 1 6 4.7 CC(C)c1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccc(Cl)cc1F nan
CHEMBL3947399 156434 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 453 6 1 6 4.7 CC(C)c1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccc(Cl)cc1F nan
54670496 147312 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 439 6 1 6 4.1 CCc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccc(Cl)cc1F nan
CHEMBL3810375 147312 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 439 6 1 6 4.1 CCc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccc(Cl)cc1F nan
54670224 147295 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 409 5 1 6 3.4 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1c(F)cccc1F 10.1016/j.bmcl.2016.05.029
CHEMBL3810148 147295 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 409 5 1 6 3.4 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1c(F)cccc1F 10.1016/j.bmcl.2016.05.029
54670224 147295 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 409 5 1 6 3.4 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1c(F)cccc1F 10.1016/j.bmcl.2016.05.029
CHEMBL3810148 147295 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 409 5 1 6 3.4 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1c(F)cccc1F 10.1016/j.bmcl.2016.05.029
52913078 147238 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 355 5 1 5 3.1 CC(c1ccccc1)S(=O)(=O)n1ccc(NC(=O)c2ccccn2)c1 10.1016/j.bmcl.2016.05.029
CHEMBL3809420 147238 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 355 5 1 5 3.1 CC(c1ccccc1)S(=O)(=O)n1ccc(NC(=O)c2ccccn2)c1 10.1016/j.bmcl.2016.05.029
127047763 146655 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 370 5 2 7 3.1 CCc1cnc(Oc2ccc(NC(=O)c3nccnc3N)cc2Cl)nc1 10.1016/j.bmcl.2016.04.041
CHEMBL3799284 146655 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 370 5 2 7 3.1 CCc1cnc(Oc2ccc(NC(=O)c3nccnc3N)cc2Cl)nc1 10.1016/j.bmcl.2016.04.041
52913078 147238 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 355 5 1 5 3.1 CC(c1ccccc1)S(=O)(=O)n1ccc(NC(=O)c2ccccn2)c1 10.1016/j.bmcl.2016.05.029
CHEMBL3809420 147238 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 355 5 1 5 3.1 CC(c1ccccc1)S(=O)(=O)n1ccc(NC(=O)c2ccccn2)c1 10.1016/j.bmcl.2016.05.029
51003375 74584 0 None 1 2 Rat 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 404 4 2 4 4.7 Cn1c(C(=O)Nc2ccc(NC(=O)c3ccccn3)cc2Cl)cc2ccccc21 10.1021/jm101271s
CHEMBL1909436 74584 0 None 1 2 Rat 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 404 4 2 4 4.7 Cn1c(C(=O)Nc2ccc(NC(=O)c3ccccn3)cc2Cl)cc2ccccc21 10.1021/jm101271s
54670118 149938 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 433 6 1 6 4.3 O=C(Nc1nc(C2CC2)c(S(=O)(=O)Cc2ccccc2Cl)s1)c1ccccn1 nan
CHEMBL3895942 149938 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 433 6 1 6 4.3 O=C(Nc1nc(C2CC2)c(S(=O)(=O)Cc2ccccc2Cl)s1)c1ccccn1 nan
127046201 146550 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
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 4.3 CC1c2ccccc2C(=O)N1c1ccc(NC(=O)c2ncccc2N)cc1Cl 10.1016/j.bmcl.2016.04.041
CHEMBL3798583 146550 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
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 4.3 CC1c2ccccc2C(=O)N1c1ccc(NC(=O)c2ncccc2N)cc1Cl 10.1016/j.bmcl.2016.04.041
1410 9054 48 None -1 8 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.5b01333
1412 9054 48 None -1 8 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.5b01333
179394 9054 48 None -1 8 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.5b01333
57689795 9054 48 None -1 8 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.5b01333
CHEMBL33567 9054 48 None -1 8 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.5b01333
1410 9054 48 None -1 8 Rat 7.5 pEC50 = 7.5 Functional
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 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmcl.2015.04.043
1412 9054 48 None -1 8 Rat 7.5 pEC50 = 7.5 Functional
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 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmcl.2015.04.043
179394 9054 48 None -1 8 Rat 7.5 pEC50 = 7.5 Functional
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 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmcl.2015.04.043
57689795 9054 48 None -1 8 Rat 7.5 pEC50 = 7.5 Functional
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 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmcl.2015.04.043
CHEMBL33567 9054 48 None -1 8 Rat 7.5 pEC50 = 7.5 Functional
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 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmcl.2015.04.043
16747847 92617 1 None 11 4 Rat 7.5 pEC50 = 7.5 Functional
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 195 3 4 3 -1.0 N[C@@]1(C(=O)O)C[C@H]1CP(=O)(O)O 10.1016/j.bmcl.2015.04.043
CHEMBL229697 92617 1 None 11 4 Rat 7.5 pEC50 = 7.5 Functional
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 195 3 4 3 -1.0 N[C@@]1(C(=O)O)C[C@H]1CP(=O)(O)O 10.1016/j.bmcl.2015.04.043
57519364 125898 0 None 2 3 Rat 6.5 pEC50 = 6.5 Functional
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 125898 0 None 2 3 Rat 6.5 pEC50 = 6.5 Functional
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
46197778 14990 0 None -1 5 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
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 14990 0 None -1 5 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 237 6 4 4 -0.3 N[C@@H](CCP(=O)(O)/C=C/C(=O)O)C(=O)O 10.1021/jm901523t
4052597 10793 9 None - 1 Human 5.5 pEC50 = 5.5 Functional
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 342 3 1 2 5.2 Cc1ccc(cc1)N1C(Nc2c(C1=O)cccc2)C(c1ccccc1)C 10.1021/jm200290z
6229 10793 9 None - 1 Human 5.5 pEC50 = 5.5 Functional
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 342 3 1 2 5.2 Cc1ccc(cc1)N1C(Nc2c(C1=O)cccc2)C(c1ccccc1)C 10.1021/jm200290z
CHEMBL473806 10793 9 None - 1 Human 5.5 pEC50 = 5.5 Functional
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 342 3 1 2 5.2 Cc1ccc(cc1)N1C(Nc2c(C1=O)cccc2)C(c1ccccc1)C 10.1021/jm200290z
46836715 72307 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
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 286 2 2 6 2.5 Cn1ccc(Nc2nc3c(s2)CCCc2n[nH]cc2-3)n1 10.1021/jm200290z
CHEMBL1830714 72307 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
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 286 2 2 6 2.5 Cn1ccc(Nc2nc3c(s2)CCCc2n[nH]cc2-3)n1 10.1021/jm200290z
137652072 163988 0 None 1 2 Human 4.5 pEC50 = 4.5 Functional
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 274 6 4 5 0.1 N[C@@H](CCP(=O)(O)C(O)c1cccnc1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4076031 163988 0 None 1 2 Human 4.5 pEC50 = 4.5 Functional
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 274 6 4 5 0.1 N[C@@H](CCP(=O)(O)C(O)c1cccnc1)C(=O)O 10.1021/acs.jmedchem.7b01438
136503370 166212 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
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 362 5 1 6 4.0 COCCOc1ccc2/c(=N/O)cc(-c3cc4ccccc4cn3)oc2c1 10.1021/acs.jmedchem.7b00991
CHEMBL4101095 166212 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
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 362 5 1 6 4.0 COCCOc1ccc2/c(=N/O)cc(-c3cc4ccccc4cn3)oc2c1 10.1021/acs.jmedchem.7b00991
135125807 181561 0 None -2 2 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 392 3 1 6 2.8 Cc1nnc2ccc(C(=O)NC3CN(c4ncc(C#N)cc4Cl)C3)cc2c1C 10.1016/j.bmcl.2019.126678
CHEMBL4561636 181561 0 None -2 2 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 392 3 1 6 2.8 Cc1nnc2ccc(C(=O)NC3CN(c4ncc(C#N)cc4Cl)C3)cc2c1C 10.1016/j.bmcl.2019.126678
71526309 156767 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 346 2 2 3 4.7 FC(F)(F)c1cc(Nc2n[nH]c3cccnc23)cc(C(F)(F)F)c1 nan
CHEMBL3950113 156767 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 346 2 2 3 4.7 FC(F)(F)c1cc(Nc2n[nH]c3cccnc23)cc(C(F)(F)F)c1 nan
127026140 144499 0 None -4 2 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human mGlu4 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu4 receptor by cell based calcium mobilization
ChEMBL 415 3 1 5 4.3 Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3758967 144499 0 None -4 2 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human mGlu4 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu4 receptor by cell based calcium mobilization
ChEMBL 415 3 1 5 4.3 Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
134191673 186572 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 412 3 2 5 5.2 FC(F)(F)C1CCCCN1c1nccc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1016/j.bmcl.2018.10.050
CHEMBL4744787 186572 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 412 3 2 5 5.2 FC(F)(F)C1CCCCN1c1nccc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1016/j.bmcl.2018.10.050
53373765 159171 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 263 2 2 4 2.9 Fc1ccc(Nc2n[nH]c3cncnc23)cc1Cl nan
CHEMBL3970411 159171 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 263 2 2 4 2.9 Fc1ccc(Nc2n[nH]c3cncnc23)cc1Cl nan
122197964 167216 0 None 2 2 Rat 5.5 pEC50 = 5.5 Functional
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 379 10 4 6 0.9 COc1cc(CP(=O)(O)CC[C@@H](N)C(=O)O)cc(F)c1OCC(=O)O nan
CHEMBL4111568 167216 0 None 2 2 Rat 5.5 pEC50 = 5.5 Functional
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 379 10 4 6 0.9 COc1cc(CP(=O)(O)CC[C@@H](N)C(=O)O)cc(F)c1OCC(=O)O nan
136503347 164453 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 288 1 1 4 3.9 O/N=c1\cc(-c2cc3ccccc3cn2)oc2ccccc12 10.1021/acs.jmedchem.7b00991
CHEMBL4081595 164453 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 288 1 1 4 3.9 O/N=c1\cc(-c2cc3ccccc3cn2)oc2ccccc12 10.1021/acs.jmedchem.7b00991
45484623 203607 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Allosteric modulator activity at human mGlu4 receptor expressed in CHO cells coexpressing Gqi5 assessed as effect on calcium fluxAllosteric modulator activity at human mGlu4 receptor expressed in CHO cells coexpressing Gqi5 assessed as effect on calcium flux
ChEMBL 312 3 2 2 3.0 NC(=O)[C@@H]1CC=CC[C@@H]1C(=O)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2009.07.072
CHEMBL565748 203607 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Allosteric modulator activity at human mGlu4 receptor expressed in CHO cells coexpressing Gqi5 assessed as effect on calcium fluxAllosteric modulator activity at human mGlu4 receptor expressed in CHO cells coexpressing Gqi5 assessed as effect on calcium flux
ChEMBL 312 3 2 2 3.0 NC(=O)[C@@H]1CC=CC[C@@H]1C(=O)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2009.07.072
44572113 195677 4 None -1 2 Human 5.5 pEC50 = 5.5 Functional
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 294 2 2 4 2.7 O=C(Nc1ccccc1)[C@]12C[C@H]1/C(=N\O)c1ccccc1O2 10.1021/jm200290z
CHEMBL507522 195677 4 None -1 2 Human 5.5 pEC50 = 5.5 Functional
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 294 2 2 4 2.7 O=C(Nc1ccccc1)[C@]12C[C@H]1/C(=N\O)c1ccccc1O2 10.1021/jm200290z
70681379 80924 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 289 2 0 3 4.2 Fc1cccc(-n2cc(-c3ccnc4ccccc34)cn2)c1 10.1016/j.bmcl.2012.03.032
CHEMBL2022870 80924 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 289 2 0 3 4.2 Fc1cccc(-n2cc(-c3ccnc4ccccc34)cn2)c1 10.1016/j.bmcl.2012.03.032
53374494 159550 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 366 4 2 4 4.7 O=C(c1ccccc1F)c1ccc(Nc2n[nH]c3cccnc23)cc1Cl nan
CHEMBL3973565 159550 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 366 4 2 4 4.7 O=C(c1ccccc1F)c1ccc(Nc2n[nH]c3cccnc23)cc1Cl nan
54670871 159924 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 437 6 1 6 4.2 CC(C)c1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccc(F)cc1F nan
CHEMBL3976663 159924 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 437 6 1 6 4.2 CC(C)c1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccc(F)cc1F nan
54670224 147295 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 409 5 1 6 3.4 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1c(F)cccc1F nan
CHEMBL3810148 147295 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 409 5 1 6 3.4 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1c(F)cccc1F nan
53374500 156443 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 280 2 2 3 3.6 Fc1ccc2[nH]nc(Nc3ccc(F)c(Cl)c3)c2n1 nan
CHEMBL3947471 156443 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 280 2 2 3 3.6 Fc1ccc2[nH]nc(Nc3ccc(F)c(Cl)c3)c2n1 nan
53374404 154347 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 242 2 2 3 3.1 Cc1ccc(F)c(Nc2n[nH]c3cccnc23)c1 nan
CHEMBL3930906 154347 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 242 2 2 3 3.1 Cc1ccc(F)c(Nc2n[nH]c3cccnc23)c1 nan
54670318 154899 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 437 6 1 6 4.2 CC(C)c1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1c(F)cccc1F nan
CHEMBL3935314 154899 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 437 6 1 6 4.2 CC(C)c1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1c(F)cccc1F nan
127048133 146380 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 146380 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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
53374304 151397 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 262 2 2 3 3.5 Fc1cc(Cl)cc(Nc2n[nH]c3cccnc23)c1 nan
CHEMBL3907930 151397 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 262 2 2 3 3.5 Fc1cc(Cl)cc(Nc2n[nH]c3cccnc23)c1 nan
137642874 164813 0 None 4 3 Human 6.5 pEC50 = 6.5 Functional
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
CHEMBL4085750 164813 0 None 4 3 Human 6.5 pEC50 = 6.5 Functional
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
1410 9054 48 None -1 8 Rat 6.5 pEC50 = 6.5 Functional
Metabotropic glutamate receptor 4 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 4 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm030967o
1412 9054 48 None -1 8 Rat 6.5 pEC50 = 6.5 Functional
Metabotropic glutamate receptor 4 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 4 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm030967o
179394 9054 48 None -1 8 Rat 6.5 pEC50 = 6.5 Functional
Metabotropic glutamate receptor 4 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 4 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm030967o
57689795 9054 48 None -1 8 Rat 6.5 pEC50 = 6.5 Functional
Metabotropic glutamate receptor 4 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 4 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm030967o
CHEMBL33567 9054 48 None -1 8 Rat 6.5 pEC50 = 6.5 Functional
Metabotropic glutamate receptor 4 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 4 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm030967o
1410 9054 48 None -1 8 Rat 6.5 pEC50 = 6.5 Functional
Stimulation od [3H]phosphatidylinositol accumulation by rat Metabotropic glutamate receptor 4 co-expressed with Gqi9 protein in HEK 293 cellsStimulation od [3H]phosphatidylinositol accumulation by rat Metabotropic glutamate receptor 4 co-expressed with Gqi9 protein in HEK 293 cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm049092j
1412 9054 48 None -1 8 Rat 6.5 pEC50 = 6.5 Functional
Stimulation od [3H]phosphatidylinositol accumulation by rat Metabotropic glutamate receptor 4 co-expressed with Gqi9 protein in HEK 293 cellsStimulation od [3H]phosphatidylinositol accumulation by rat Metabotropic glutamate receptor 4 co-expressed with Gqi9 protein in HEK 293 cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm049092j
179394 9054 48 None -1 8 Rat 6.5 pEC50 = 6.5 Functional
Stimulation od [3H]phosphatidylinositol accumulation by rat Metabotropic glutamate receptor 4 co-expressed with Gqi9 protein in HEK 293 cellsStimulation od [3H]phosphatidylinositol accumulation by rat Metabotropic glutamate receptor 4 co-expressed with Gqi9 protein in HEK 293 cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm049092j
57689795 9054 48 None -1 8 Rat 6.5 pEC50 = 6.5 Functional
Stimulation od [3H]phosphatidylinositol accumulation by rat Metabotropic glutamate receptor 4 co-expressed with Gqi9 protein in HEK 293 cellsStimulation od [3H]phosphatidylinositol accumulation by rat Metabotropic glutamate receptor 4 co-expressed with Gqi9 protein in HEK 293 cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm049092j
CHEMBL33567 9054 48 None -1 8 Rat 6.5 pEC50 = 6.5 Functional
Stimulation od [3H]phosphatidylinositol accumulation by rat Metabotropic glutamate receptor 4 co-expressed with Gqi9 protein in HEK 293 cellsStimulation od [3H]phosphatidylinositol accumulation by rat Metabotropic glutamate receptor 4 co-expressed with Gqi9 protein in HEK 293 cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm049092j
1407 8860 42 None -117 7 Human 5.5 pEC50 = 5.5 Functional
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 239 4 4 4 0.2 N[C@@H](c1ccc(c(c1)C(=O)O)C(=O)O)C(=O)O 10.1021/acs.jmedchem.7b01438
16062593 8860 42 None -117 7 Human 5.5 pEC50 = 5.5 Functional
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 239 4 4 4 0.2 N[C@@H](c1ccc(c(c1)C(=O)O)C(=O)O)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL143210 8860 42 None -117 7 Human 5.5 pEC50 = 5.5 Functional
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 239 4 4 4 0.2 N[C@@H](c1ccc(c(c1)C(=O)O)C(=O)O)C(=O)O 10.1021/acs.jmedchem.7b01438
1310 9095 110 None -426 17 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP productionAgonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP production
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
1369 9095 110 None -426 17 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP productionAgonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP production
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
33032 9095 110 None -426 17 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP productionAgonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP production
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
44272391 9095 110 None -426 17 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP productionAgonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP production
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
88747398 9095 110 None -426 17 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP productionAgonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP production
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
CHEMBL575060 9095 110 None -426 17 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP productionAgonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP production
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
DB00142 9095 110 None -426 17 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP productionAgonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP production
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
1406 8854 38 None -22 7 Human 5.5 pEC50 = 5.5 Functional
Compound was evaluated for the inhibition of forskolin stimulated cAMP accumulation in CHO cells expressing hmGluR4aCompound was evaluated for the inhibition of forskolin stimulated cAMP accumulation in CHO cells expressing hmGluR4a
ChEMBL 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10.1016/s0960-894x(00)00197-9
4545574 8854 38 None -22 7 Human 5.5 pEC50 = 5.5 Functional
Compound was evaluated for the inhibition of forskolin stimulated cAMP accumulation in CHO cells expressing hmGluR4aCompound was evaluated for the inhibition of forskolin stimulated cAMP accumulation in CHO cells expressing hmGluR4a
ChEMBL 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10.1016/s0960-894x(00)00197-9
CHEMBL277475 8854 38 None -22 7 Human 5.5 pEC50 = 5.5 Functional
Compound was evaluated for the inhibition of forskolin stimulated cAMP accumulation in CHO cells expressing hmGluR4aCompound was evaluated for the inhibition of forskolin stimulated cAMP accumulation in CHO cells expressing hmGluR4a
ChEMBL 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10.1016/s0960-894x(00)00197-9
53387882 72305 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
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 272 2 3 5 2.5 c1cc(Nc2nc3c(s2)CCCc2n[nH]cc2-3)n[nH]1 10.1021/jm200290z
CHEMBL1830712 72305 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
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 272 2 3 5 2.5 c1cc(Nc2nc3c(s2)CCCc2n[nH]cc2-3)n[nH]1 10.1021/jm200290z
10238 10799 26 None -3 5 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assay
ChEMBL 436 7 1 6 4.8 COC(=O)c1ccc(cc1)n1c(C)cc(c1C)C(=O)CSc1ccc(cc1)NC(=O)C 10.1021/acsmedchemlett.7b00317
4043841 10799 26 None -3 5 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assay
ChEMBL 436 7 1 6 4.8 COC(=O)c1ccc(cc1)n1c(C)cc(c1C)C(=O)CSc1ccc(cc1)NC(=O)C 10.1021/acsmedchemlett.7b00317
CHEMBL1585091 10799 26 None -3 5 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assay
ChEMBL 436 7 1 6 4.8 COC(=O)c1ccc(cc1)n1c(C)cc(c1C)C(=O)CSc1ccc(cc1)NC(=O)C 10.1021/acsmedchemlett.7b00317
135126267 178668 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 392 5 1 7 2.4 Cc1nnc2ccc(C(=O)NC3CN(c4ncc(OC(C)C)cn4)C3)cc2c1C 10.1016/j.bmcl.2019.126678
CHEMBL4469593 178668 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 392 5 1 7 2.4 Cc1nnc2ccc(C(=O)NC3CN(c4ncc(OC(C)C)cn4)C3)cc2c1C 10.1016/j.bmcl.2019.126678
54670685 153870 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 427 5 1 6 3.5 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1cc(F)c(F)cc1F nan
CHEMBL3927279 153870 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 427 5 1 6 3.5 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1cc(F)c(F)cc1F nan
122193174 130707 0 None -5 2 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of human mGlu4 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay
ChEMBL 394 3 1 4 4.6 Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3occc3C)cc1Cl)C2=O 10.1021/acs.jmedchem.5b00727
CHEMBL3628110 130707 0 None -5 2 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of human mGlu4 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay
ChEMBL 394 3 1 4 4.6 Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3occc3C)cc1Cl)C2=O 10.1021/acs.jmedchem.5b00727
122193174 130707 0 None -5 2 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of human mGlu4 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay
ChEMBL 394 3 1 4 4.6 Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3occc3C)cc1Cl)C2=O 10.1021/acs.jmedchem.5b00727
CHEMBL3628110 130707 0 None -5 2 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of human mGlu4 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay
ChEMBL 394 3 1 4 4.6 Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3occc3C)cc1Cl)C2=O 10.1021/acs.jmedchem.5b00727
122419072 177279 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 323 2 2 5 4.6 CC(C)(C)c1nsc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
CHEMBL4449390 177279 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 323 2 2 5 4.6 CC(C)(C)c1nsc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
122419160 179782 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 408 3 2 7 3.6 CC1CN(C(=O)c2nsc3cc(Nc4n[nH]c5cccnc45)ccc23)CC(C)O1 10.1021/acs.jmedchem.8b00994
CHEMBL4518186 179782 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 408 3 2 7 3.6 CC1CN(C(=O)c2nsc3cc(Nc4n[nH]c5cccnc45)ccc23)CC(C)O1 10.1021/acs.jmedchem.8b00994
54670870 157071 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 421 5 1 6 4.3 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)C(C)c1ccccc1Cl nan
CHEMBL3952753 157071 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 421 5 1 6 4.3 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)C(C)c1ccccc1Cl nan
1310 9095 110 None -426 17 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP productionAgonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP production
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
1369 9095 110 None -426 17 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP productionAgonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP production
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
33032 9095 110 None -426 17 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP productionAgonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP production
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
44272391 9095 110 None -426 17 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP productionAgonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP production
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
88747398 9095 110 None -426 17 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP productionAgonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP production
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
CHEMBL575060 9095 110 None -426 17 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP productionAgonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP production
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
DB00142 9095 110 None -426 17 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP productionAgonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP production
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
67109801 154320 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 348 4 1 7 2.1 Cc1ccc(S(=O)(=O)n2cc(NC(=O)c3nccs3)cn2)cc1 nan
CHEMBL3930733 154320 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 348 4 1 7 2.1 Cc1ccc(S(=O)(=O)n2cc(NC(=O)c3nccs3)cn2)cc1 nan
122419072 177279 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 323 2 2 5 4.6 CC(C)(C)c1nsc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
CHEMBL4449390 177279 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 323 2 2 5 4.6 CC(C)(C)c1nsc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
122419160 179782 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 408 3 2 7 3.6 CC1CN(C(=O)c2nsc3cc(Nc4n[nH]c5cccnc45)ccc23)CC(C)O1 10.1021/acs.jmedchem.8b00994
CHEMBL4518186 179782 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 408 3 2 7 3.6 CC1CN(C(=O)c2nsc3cc(Nc4n[nH]c5cccnc45)ccc23)CC(C)O1 10.1021/acs.jmedchem.8b00994
49865230 22639 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilization
ChEMBL 389 5 2 4 3.4 O=C(Nc1ccc(S(=O)(=O)Nc2cc(F)ccc2F)cc1)c1ccccn1 10.1016/j.bmcl.2010.07.007
CHEMBL1223085 22639 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilization
ChEMBL 389 5 2 4 3.4 O=C(Nc1ccc(S(=O)(=O)Nc2cc(F)ccc2F)cc1)c1ccccn1 10.1016/j.bmcl.2010.07.007
53375080 146470 35 None - 1 Human 7.5 pEC50 = 7.5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 262 2 2 3 3.5 Fc1ccc(Nc2n[nH]c3cccnc23)cc1Cl nan
CHEMBL3798040 146470 35 None - 1 Human 7.5 pEC50 = 7.5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 262 2 2 3 3.5 Fc1ccc(Nc2n[nH]c3cccnc23)cc1Cl nan
122197958 167303 0 None 7 4 Rat 6.5 pEC50 = 6.5 Functional
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 383 9 5 6 0.5 N[C@H](CCP(=O)(O)C(O)c1cc(F)c(OCC(=O)O)c(F)c1)C(=O)O nan
CHEMBL4112299 167303 0 None 7 4 Rat 6.5 pEC50 = 6.5 Functional
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 383 9 5 6 0.5 N[C@H](CCP(=O)(O)C(O)c1cc(F)c(OCC(=O)O)c(F)c1)C(=O)O nan
57765525 166233 0 None -1 3 Human 5.5 pEC50 = 5.5 Functional
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 332 7 4 6 1.0 Cc1ccc(C(O)P(=O)(O)CC[C@H](N)C(=O)O)cc1[N+](=O)[O-] 10.1021/acs.jmedchem.7b01438
CHEMBL4101241 166233 0 None -1 3 Human 5.5 pEC50 = 5.5 Functional
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 332 7 4 6 1.0 Cc1ccc(C(O)P(=O)(O)CC[C@H](N)C(=O)O)cc1[N+](=O)[O-] 10.1021/acs.jmedchem.7b01438
45484641 205392 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Allosteric modulator activity at human mGlu4 receptor expressed in CHO cells coexpressing Gqi5 assessed as effect on calcium fluxAllosteric modulator activity at human mGlu4 receptor expressed in CHO cells coexpressing Gqi5 assessed as effect on calcium flux
ChEMBL 297 1 0 2 3.7 O=C1[C@H]2CCCC[C@H]2C(=O)N1c1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2009.07.072
CHEMBL578793 205392 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Allosteric modulator activity at human mGlu4 receptor expressed in CHO cells coexpressing Gqi5 assessed as effect on calcium fluxAllosteric modulator activity at human mGlu4 receptor expressed in CHO cells coexpressing Gqi5 assessed as effect on calcium flux
ChEMBL 297 1 0 2 3.7 O=C1[C@H]2CCCC[C@H]2C(=O)N1c1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2009.07.072
54670873 156493 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 469 6 1 6 5.2 CC(C)c1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccc(Cl)cc1Cl nan
CHEMBL3947876 156493 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 469 6 1 6 5.2 CC(C)c1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccc(Cl)cc1Cl nan
137636549 162606 0 None -1 2 Human 4.5 pEC50 = 4.5 Functional
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 290 6 5 6 -0.2 N[C@@H](CCP(=O)(O)C(O)c1ccc(O)nc1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4059974 162606 0 None -1 2 Human 4.5 pEC50 = 4.5 Functional
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 290 6 5 6 -0.2 N[C@@H](CCP(=O)(O)C(O)c1ccc(O)nc1)C(=O)O 10.1021/acs.jmedchem.7b01438
122419157 179808 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 400 3 2 6 3.8 O=C(c1nsc2cc(Nc3n[nH]c4cccnc34)ccc12)N1CCC(F)(F)C1 10.1021/acs.jmedchem.8b00994
CHEMBL4518731 179808 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 400 3 2 6 3.8 O=C(c1nsc2cc(Nc3n[nH]c4cccnc34)ccc12)N1CCC(F)(F)C1 10.1021/acs.jmedchem.8b00994
122419157 179808 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 400 3 2 6 3.8 O=C(c1nsc2cc(Nc3n[nH]c4cccnc34)ccc12)N1CCC(F)(F)C1 10.1021/acs.jmedchem.8b00994
CHEMBL4518731 179808 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 400 3 2 6 3.8 O=C(c1nsc2cc(Nc3n[nH]c4cccnc34)ccc12)N1CCC(F)(F)C1 10.1021/acs.jmedchem.8b00994
51003376 74585 0 None - 1 Rat 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 417 5 2 4 5.5 O=C(Nc1ccc(NC(=O)c2ccc(-c3ccccc3)o2)c(Cl)c1)c1ccccn1 10.1021/jm101271s
CHEMBL1909437 74585 0 None - 1 Rat 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 417 5 2 4 5.5 O=C(Nc1ccc(NC(=O)c2ccc(-c3ccccc3)o2)c(Cl)c1)c1ccccn1 10.1021/jm101271s
53374501 159238 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 338 4 2 6 3.9 Clc1cc(Nc2n[nH]c3cccnc23)cnc1Oc1ccccn1 nan
CHEMBL3970929 159238 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 338 4 2 6 3.9 Clc1cc(Nc2n[nH]c3cccnc23)cnc1Oc1ccccn1 nan
135126261 176991 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 401 3 1 5 3.3 Cc1nnc2ccc(C(=O)NC3CN(c4cccc(C(F)(F)F)n4)C3)cc2c1C 10.1016/j.bmcl.2019.126678
CHEMBL4445362 176991 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 401 3 1 5 3.3 Cc1nnc2ccc(C(=O)NC3CN(c4cccc(C(F)(F)F)n4)C3)cc2c1C 10.1016/j.bmcl.2019.126678
127026472 144523 0 None -3 2 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of human mGlu4 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu4 receptor by cell based calcium mobilization
ChEMBL 414 3 2 4 4.1 Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3759211 144523 0 None -3 2 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of human mGlu4 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu4 receptor by cell based calcium mobilization
ChEMBL 414 3 2 4 4.1 Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
44189740 201709 0 None -1 2 Human 6.5 pEC50 = 6.5 Functional
Activity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilizationActivity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilization
ChEMBL 264 4 1 3 2.9 O=C(Nc1cccc(OC(F)F)c1)c1ccccn1 10.1021/jm9005065
CHEMBL541754 201709 0 None -1 2 Human 6.5 pEC50 = 6.5 Functional
Activity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilizationActivity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilization
ChEMBL 264 4 1 3 2.9 O=C(Nc1cccc(OC(F)F)c1)c1ccccn1 10.1021/jm9005065
50902542 82999 0 None - 1 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells coexpressing Gq/Gi and EAAC1 assessed as intracellular calcium production measured every 1.5 secs for 60 secs by Fluo-4-AM based fluorometryAgonist activity at rat mGlu4 receptor expressed in HEK293 cells coexpressing Gq/Gi and EAAC1 assessed as intracellular calcium production measured every 1.5 secs for 60 secs by Fluo-4-AM based fluorometry
ChEMBL 213 3 4 3 -0.9 N[C@]1(C(=O)O)C[C@@]1(F)CP(=O)(O)O 10.1016/j.bmc.2012.06.006
CHEMBL2058378 82999 0 None - 1 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells coexpressing Gq/Gi and EAAC1 assessed as intracellular calcium production measured every 1.5 secs for 60 secs by Fluo-4-AM based fluorometryAgonist activity at rat mGlu4 receptor expressed in HEK293 cells coexpressing Gq/Gi and EAAC1 assessed as intracellular calcium production measured every 1.5 secs for 60 secs by Fluo-4-AM based fluorometry
ChEMBL 213 3 4 3 -0.9 N[C@]1(C(=O)O)C[C@@]1(F)CP(=O)(O)O 10.1016/j.bmc.2012.06.006
53388195 72323 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 326 3 2 6 3.2 CN(C)c1cccc(Nc2nc3c(s2)CCCc2n[nH]cc2-3)n1 10.1021/jm200290z
CHEMBL1830911 72323 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 326 3 2 6 3.2 CN(C)c1cccc(Nc2nc3c(s2)CCCc2n[nH]cc2-3)n1 10.1021/jm200290z
137635378 162581 0 None 2 2 Human 5.5 pEC50 = 5.5 Functional
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 313 6 5 5 0.6 N[C@@H](CCP(=O)(O)C(O)c1c[nH]c2ncccc12)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4059673 162581 0 None 2 2 Human 5.5 pEC50 = 5.5 Functional
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 313 6 5 5 0.6 N[C@@H](CCP(=O)(O)C(O)c1c[nH]c2ncccc12)C(=O)O 10.1021/acs.jmedchem.7b01438
53387887 72312 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
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 297 2 2 5 3.5 Cc1cccnc1Nc1nc2c(s1)CCCc1n[nH]cc1-2 10.1021/jm200290z
CHEMBL1830898 72312 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
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 297 2 2 5 3.5 Cc1cccnc1Nc1nc2c(s1)CCCc1n[nH]cc1-2 10.1021/jm200290z
53374311 160772 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 280 2 2 3 3.6 Fc1cc(F)c(Nc2n[nH]c3cccnc23)cc1Cl nan
CHEMBL3983978 160772 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 280 2 2 3 3.6 Fc1cc(F)c(Nc2n[nH]c3cccnc23)cc1Cl nan
10238 10799 26 None -3 5 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human mGlu4 expressed in CHO cells co-expressing Gqi5 (unknown origin) assessed as reduction in intracellular Ca2+ levels by Fluo-4-AM dye based fluorescence assayAgonist activity at human mGlu4 expressed in CHO cells co-expressing Gqi5 (unknown origin) assessed as reduction in intracellular Ca2+ levels by Fluo-4-AM dye based fluorescence assay
ChEMBL 436 7 1 6 4.8 COC(=O)c1ccc(cc1)n1c(C)cc(c1C)C(=O)CSc1ccc(cc1)NC(=O)C 10.1039/C8MD00524A
4043841 10799 26 None -3 5 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human mGlu4 expressed in CHO cells co-expressing Gqi5 (unknown origin) assessed as reduction in intracellular Ca2+ levels by Fluo-4-AM dye based fluorescence assayAgonist activity at human mGlu4 expressed in CHO cells co-expressing Gqi5 (unknown origin) assessed as reduction in intracellular Ca2+ levels by Fluo-4-AM dye based fluorescence assay
ChEMBL 436 7 1 6 4.8 COC(=O)c1ccc(cc1)n1c(C)cc(c1C)C(=O)CSc1ccc(cc1)NC(=O)C 10.1039/C8MD00524A
CHEMBL1585091 10799 26 None -3 5 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human mGlu4 expressed in CHO cells co-expressing Gqi5 (unknown origin) assessed as reduction in intracellular Ca2+ levels by Fluo-4-AM dye based fluorescence assayAgonist activity at human mGlu4 expressed in CHO cells co-expressing Gqi5 (unknown origin) assessed as reduction in intracellular Ca2+ levels by Fluo-4-AM dye based fluorescence assay
ChEMBL 436 7 1 6 4.8 COC(=O)c1ccc(cc1)n1c(C)cc(c1C)C(=O)CSc1ccc(cc1)NC(=O)C 10.1039/C8MD00524A
68374351 147188 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 362 4 1 6 2.4 O=C(Nc1ccn(S(=O)(=O)c2ccc(Cl)cn2)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
CHEMBL3808889 147188 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 362 4 1 6 2.4 O=C(Nc1ccn(S(=O)(=O)c2ccc(Cl)cn2)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
134198077 172673 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 278 2 2 5 2.9 Cc1nn(C)c2ccc(Nc3n[nH]c4cccnc34)cc12 10.1016/j.bmcl.2018.06.034
CHEMBL4249753 172673 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 278 2 2 5 2.9 Cc1nn(C)c2ccc(Nc3n[nH]c4cccnc34)cc12 10.1016/j.bmcl.2018.06.034
68374351 147188 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 362 4 1 6 2.4 O=C(Nc1ccn(S(=O)(=O)c2ccc(Cl)cn2)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
CHEMBL3808889 147188 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 362 4 1 6 2.4 O=C(Nc1ccn(S(=O)(=O)c2ccc(Cl)cn2)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
136015189 156084 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 244 2 3 4 2.5 Oc1ccc(Nc2n[nH]c3cccnc23)cc1F nan
CHEMBL3944839 156084 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 244 2 3 4 2.5 Oc1ccc(Nc2n[nH]c3cccnc23)cc1F nan
136415554 162912 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
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 423 5 1 8 3.7 O/N=c1\cc(-c2cc3sccc3cn2)oc2ccc(OCCN3CCOCC3)cc12 10.1021/acs.jmedchem.7b00991
CHEMBL4063474 162912 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
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 423 5 1 8 3.7 O/N=c1\cc(-c2cc3sccc3cn2)oc2ccc(OCCN3CCOCC3)cc12 10.1021/acs.jmedchem.7b00991
137661688 166156 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
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 419 3 1 7 2.8 CN(C)C(=O)N1CC(Oc2ccc3oc(-c4cc5cccn5cn4)c/c(=N\O)c3c2)C1 10.1021/acs.jmedchem.7b00991
CHEMBL4100586 166156 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
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 419 3 1 7 2.8 CN(C)C(=O)N1CC(Oc2ccc3oc(-c4cc5cccn5cn4)c/c(=N\O)c3c2)C1 10.1021/acs.jmedchem.7b00991
122196092 131005 0 None -21 2 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 360 3 1 4 3.9 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)cc1 10.1016/j.bmcl.2015.10.013
CHEMBL3634415 131005 0 None -21 2 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 360 3 1 4 3.9 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)cc1 10.1016/j.bmcl.2015.10.013
57765531 163910 0 None 1 2 Human 5.5 pEC50 = 5.5 Functional
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 348 8 4 7 0.7 COc1ccc(C(O)P(=O)(O)CC[C@H](N)C(=O)O)cc1[N+](=O)[O-] 10.1021/acs.jmedchem.7b01438
CHEMBL4075070 163910 0 None 1 2 Human 5.5 pEC50 = 5.5 Functional
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 348 8 4 7 0.7 COc1ccc(C(O)P(=O)(O)CC[C@H](N)C(=O)O)cc1[N+](=O)[O-] 10.1021/acs.jmedchem.7b01438
70691971 81020 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 272 2 0 4 3.5 c1ccc(-n2cc(-c3ncnc4ccccc34)cn2)cc1 10.1016/j.bmcl.2012.03.032
CHEMBL2023628 81020 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 272 2 0 4 3.5 c1ccc(-n2cc(-c3ncnc4ccccc34)cn2)cc1 10.1016/j.bmcl.2012.03.032
53374211 150682 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 348 4 2 4 4.6 O=C(c1ccccc1)c1ccc(Nc2n[nH]c3cccnc23)cc1Cl nan
CHEMBL3901929 150682 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 348 4 2 4 4.6 O=C(c1ccccc1)c1ccc(Nc2n[nH]c3cccnc23)cc1Cl nan
122196119 131031 0 None -17 2 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 396 3 1 4 4.8 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c2ccccc12 10.1016/j.bmcl.2015.10.013
CHEMBL3634441 131031 0 None -17 2 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 396 3 1 4 4.8 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c2ccccc12 10.1016/j.bmcl.2015.10.013
56649042 75560 0 None -1 2 Human 6.5 pEC50 = 6.5 Functional
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 421 3 1 7 2.3 O=C(Nc1ccc(N2S(=O)(=O)c3ccccc3S2(=O)=O)cc1)c1nccs1 10.1021/jm200956q
CHEMBL1921951 75560 0 None -1 2 Human 6.5 pEC50 = 6.5 Functional
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 421 3 1 7 2.3 O=C(Nc1ccc(N2S(=O)(=O)c3ccccc3S2(=O)=O)cc1)c1nccs1 10.1021/jm200956q
53373659 158921 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 245 2 2 4 2.8 Clc1cncc(Nc2n[nH]c3cccnc23)c1 nan
CHEMBL3968018 158921 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 245 2 2 4 2.8 Clc1cncc(Nc2n[nH]c3cccnc23)c1 nan
54670410 152181 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 429 6 1 6 4.3 CCc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1c(C)cc(C)cc1C nan
CHEMBL3913983 152181 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 429 6 1 6 4.3 CCc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1c(C)cc(C)cc1C nan
122196114 131026 0 None -17 2 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 365 3 1 5 3.2 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)nc1 10.1016/j.bmcl.2015.10.013
CHEMBL3634436 131026 0 None -17 2 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 365 3 1 5 3.2 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)nc1 10.1016/j.bmcl.2015.10.013
135125813 182539 0 None 1 2 Rat 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 397 4 1 6 2.9 COc1cc(N2CC(NC(=O)c3ccc4nnc(C)c(C)c4c3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126678
CHEMBL4583516 182539 0 None 1 2 Rat 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 397 4 1 6 2.9 COc1cc(N2CC(NC(=O)c3ccc4nnc(C)c(C)c4c3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126678
53374105 172394 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 263 2 2 4 3.2 Cn1ccc2cc(Nc3n[nH]c4cccnc34)ccc21 10.1016/j.bmcl.2018.06.034
CHEMBL4243164 172394 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 263 2 2 4 3.2 Cn1ccc2cc(Nc3n[nH]c4cccnc34)ccc21 10.1016/j.bmcl.2018.06.034
121231185 160228 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 263 2 2 4 3.2 Cn1ccc2ccc(Nc3n[nH]c4cccnc34)cc21 nan
CHEMBL3979370 160228 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 263 2 2 4 3.2 Cn1ccc2ccc(Nc3n[nH]c4cccnc34)cc21 nan
134191665 188867 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 357 3 2 4 4.9 CC(c1nccc2cc(Nc3n[nH]c4cccnc34)ccc12)C(F)(F)F 10.1016/j.bmcl.2018.10.050
CHEMBL4781616 188867 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 357 3 2 4 4.9 CC(c1nccc2cc(Nc3n[nH]c4cccnc34)ccc12)C(F)(F)F 10.1016/j.bmcl.2018.10.050
134192044 172479 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 318 4 2 5 3.9 CCn1nc(C2CC2)c2ccc(Nc3n[nH]c4cccnc34)cc21 10.1016/j.bmcl.2018.06.034
CHEMBL4241223 172479 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 318 4 2 5 3.9 CCn1nc(C2CC2)c2ccc(Nc3n[nH]c4cccnc34)cc21 10.1016/j.bmcl.2018.06.034
CHEMBL4245437 172479 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 318 4 2 5 3.9 CCn1nc(C2CC2)c2ccc(Nc3n[nH]c4cccnc34)cc21 10.1016/j.bmcl.2018.06.034
51003324 64679 0 None 1 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 351 4 2 3 4.2 O=C(Nc1ccc(NC(=O)c2ccccn2)cc1Cl)c1ccccc1 10.1021/jm101271s
CHEMBL1672244 64679 0 None 1 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 351 4 2 3 4.2 O=C(Nc1ccc(NC(=O)c2ccccn2)cc1Cl)c1ccccc1 10.1021/jm101271s
54670964 155596 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 419 6 1 6 4.0 CC(C)c1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccccc1F nan
CHEMBL3940968 155596 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 419 6 1 6 4.0 CC(C)c1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccccc1F nan
134191960 172197 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 292 3 2 5 3.2 CCc1nn(C)c2cc(Nc3n[nH]c4cccnc34)ccc12 10.1016/j.bmcl.2018.06.034
CHEMBL4238452 172197 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 292 3 2 5 3.2 CCc1nn(C)c2cc(Nc3n[nH]c4cccnc34)ccc12 10.1016/j.bmcl.2018.06.034
122197946 167227 0 None 91 2 Rat 6.4 pEC50 = 6.4 Functional
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 383 9 6 6 0.3 N[C@H](CCP(=O)(O)C(O)c1ccc(OCP(=O)(O)O)cc1)C(=O)O nan
CHEMBL4111679 167227 0 None 91 2 Rat 6.4 pEC50 = 6.4 Functional
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 383 9 6 6 0.3 N[C@H](CCP(=O)(O)C(O)c1ccc(OCP(=O)(O)O)cc1)C(=O)O nan
56649125 75565 0 None 1 2 Human 6.4 pEC50 = 6.4 Functional
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 383 3 1 4 3.7 O=C(Nc1ccc(N2C(=O)[C@H]3CCCC[C@H]3C2=O)c(Cl)c1)c1ccccn1 10.1021/jm200956q
CHEMBL1921959 75565 0 None 1 2 Human 6.4 pEC50 = 6.4 Functional
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 383 3 1 4 3.7 O=C(Nc1ccc(N2C(=O)[C@H]3CCCC[C@H]3C2=O)c(Cl)c1)c1ccccn1 10.1021/jm200956q
26187503 22661 3 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilization
ChEMBL 359 4 1 4 2.8 CC1CCN(S(=O)(=O)c2ccc(NC(=O)c3ccccn3)cc2)CC1 10.1016/j.bmcl.2010.07.007
CHEMBL1223164 22661 3 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilization
ChEMBL 359 4 1 4 2.8 CC1CCN(S(=O)(=O)c2ccc(NC(=O)c3ccccn3)cc2)CC1 10.1016/j.bmcl.2010.07.007
135125813 182539 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 397 4 1 6 2.9 COc1cc(N2CC(NC(=O)c3ccc4nnc(C)c(C)c4c3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126678
CHEMBL4583516 182539 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 397 4 1 6 2.9 COc1cc(N2CC(NC(=O)c3ccc4nnc(C)c(C)c4c3)C2)c(Cl)cn1 10.1016/j.bmcl.2019.126678
88889540 155495 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 449 6 1 6 5.1 CC(C)c1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)C(C)c1ccccc1Cl nan
CHEMBL3940130 155495 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 449 6 1 6 5.1 CC(C)c1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)C(C)c1ccccc1Cl nan
51003231 64667 0 None 1 2 Rat 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 387 5 2 5 4.3 COc1cc(NC(=O)c2nccs2)ccc1NC(=O)c1ccccc1Cl 10.1021/jm101271s
CHEMBL1672232 64667 0 None 1 2 Rat 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 387 5 2 5 4.3 COc1cc(NC(=O)c2nccs2)ccc1NC(=O)c1ccccc1Cl 10.1021/jm101271s
57765622 162883 0 None 3 3 Human 6.4 pEC50 = 6.4 Functional
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 386 7 4 6 1.7 N[C@@H](CCP(=O)(O)C(O)c1ccc(C(F)(F)F)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4063142 162883 0 None 3 3 Human 6.4 pEC50 = 6.4 Functional
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 386 7 4 6 1.7 N[C@@H](CCP(=O)(O)C(O)c1ccc(C(F)(F)F)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
57765536 165050 0 None 1 3 Human 6.4 pEC50 = 6.4 Functional
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 318 7 4 6 0.7 N[C@@H](CCP(=O)(O)C(O)c1ccc([N+](=O)[O-])cc1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4088782 165050 0 None 1 3 Human 6.4 pEC50 = 6.4 Functional
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 318 7 4 6 0.7 N[C@@H](CCP(=O)(O)C(O)c1ccc([N+](=O)[O-])cc1)C(=O)O 10.1021/acs.jmedchem.7b01438
122197941 167527 0 None 60 2 Rat 6.4 pEC50 = 6.4 Functional
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 415 9 5 6 1.5 N[C@H](CCP(=O)(O)C(O)c1cc(Cl)c(OCC(=O)O)c(Cl)c1)C(=O)O nan
CHEMBL4113972 167527 0 None 60 2 Rat 6.4 pEC50 = 6.4 Functional
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 415 9 5 6 1.5 N[C@H](CCP(=O)(O)C(O)c1cc(Cl)c(OCC(=O)O)c(Cl)c1)C(=O)O nan
46197780 12354 0 None 4 4 Rat 5.4 pEC50 = 5.4 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
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 12354 0 None 4 4 Rat 5.4 pEC50 = 5.4 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 273 7 4 4 -0.2 N[C@@H](CCP(=O)(O)CC(Cl)C(=O)O)C(=O)O 10.1021/jm901523t
122196094 131007 0 None -8 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 364 3 1 4 3.8 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)cc1 10.1016/j.bmcl.2015.10.013
CHEMBL3634417 131007 0 None -8 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 364 3 1 4 3.8 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)cc1 10.1016/j.bmcl.2015.10.013
69938825 160874 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 296 2 2 3 3.9 Fc1ccc(Nc2n[nH]c3cccnc23)cc1C(F)(F)F nan
CHEMBL3984897 160874 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 296 2 2 3 3.9 Fc1ccc(Nc2n[nH]c3cccnc23)cc1C(F)(F)F nan
53373879 153094 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 416 4 2 4 5.6 O=C(c1cccc(C(F)(F)F)c1)c1ccc(Nc2n[nH]c3cccnc23)cc1Cl nan
CHEMBL3921007 153094 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 416 4 2 4 5.6 O=C(c1cccc(C(F)(F)F)c1)c1ccc(Nc2n[nH]c3cccnc23)cc1Cl nan
122419153 181888 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 418 4 2 6 4.4 O=C(C1CC1)N1CCC(c2nsc3cc(Nc4n[nH]c5cccnc45)ccc23)CC1 10.1021/acs.jmedchem.8b00994
CHEMBL4569169 181888 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 418 4 2 6 4.4 O=C(C1CC1)N1CCC(c2nsc3cc(Nc4n[nH]c5cccnc45)ccc23)CC1 10.1021/acs.jmedchem.8b00994
122419153 181888 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 418 4 2 6 4.4 O=C(C1CC1)N1CCC(c2nsc3cc(Nc4n[nH]c5cccnc45)ccc23)CC1 10.1021/acs.jmedchem.8b00994
CHEMBL4569169 181888 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 418 4 2 6 4.4 O=C(C1CC1)N1CCC(c2nsc3cc(Nc4n[nH]c5cccnc45)ccc23)CC1 10.1021/acs.jmedchem.8b00994
17759041 99636 8 None 1 3 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat mGluR4 receptor expressed HEK293 cells assessed as effect on inositol phosphate productionAgonist activity at rat mGluR4 receptor expressed HEK293 cells assessed as effect on inositol phosphate production
ChEMBL 199 4 4 3 -0.9 N[C@@H](CCP(O)(O)=S)C(=O)O 10.1021/jm070400y
CHEMBL243925 99636 8 None 1 3 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat mGluR4 receptor expressed HEK293 cells assessed as effect on inositol phosphate productionAgonist activity at rat mGluR4 receptor expressed HEK293 cells assessed as effect on inositol phosphate production
ChEMBL 199 4 4 3 -0.9 N[C@@H](CCP(O)(O)=S)C(=O)O 10.1021/jm070400y
155549892 180690 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 295 3 2 5 3.9 CCc1nsc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
CHEMBL4540386 180690 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 295 3 2 5 3.9 CCc1nsc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
53388194 72322 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
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 357 6 2 7 3.2 COCCOc1cccc(Nc2nc3c(s2)CCCc2n[nH]cc2-3)n1 10.1021/jm200290z
CHEMBL1830910 72322 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
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 357 6 2 7 3.2 COCCOc1cccc(Nc2nc3c(s2)CCCc2n[nH]cc2-3)n1 10.1021/jm200290z
70694004 80994 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 345 6 0 5 4.1 COCCOc1ccc2c(-c3cnn(-c4ccccc4)c3)ccnc2c1 10.1016/j.bmcl.2012.03.032
CHEMBL2023461 80994 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 345 6 0 5 4.1 COCCOc1ccc2c(-c3cnn(-c4ccccc4)c3)ccnc2c1 10.1016/j.bmcl.2012.03.032
70689822 81015 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 386 5 0 5 4.9 CCN(CC)C(=O)Oc1ccc2c(-c3cnn(-c4ccccc4)c3)ccnc2c1 10.1016/j.bmcl.2012.03.032
CHEMBL2023623 81015 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 386 5 0 5 4.9 CCN(CC)C(=O)Oc1ccc2c(-c3cnn(-c4ccccc4)c3)ccnc2c1 10.1016/j.bmcl.2012.03.032
52934969 158822 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 380 4 1 6 2.6 O=C(Nc1cnn(S(=O)(=O)c2ccc(Cl)c(F)c2)c1)c1ccccn1 nan
CHEMBL3967243 158822 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 380 4 1 6 2.6 O=C(Nc1cnn(S(=O)(=O)c2ccc(Cl)c(F)c2)c1)c1ccccn1 nan
137637239 162657 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
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 288 1 1 4 3.9 O/N=c1\cc(-c2cnc3ccccc3c2)oc2ccccc12 10.1021/acs.jmedchem.7b00991
CHEMBL4060429 162657 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
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 288 1 1 4 3.9 O/N=c1\cc(-c2cnc3ccccc3c2)oc2ccccc12 10.1021/acs.jmedchem.7b00991
52913077 147157 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 375 5 1 5 3.2 O=C(Nc1ccn(S(=O)(=O)Cc2ccc(Cl)cc2)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
CHEMBL3808534 147157 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 375 5 1 5 3.2 O=C(Nc1ccn(S(=O)(=O)Cc2ccc(Cl)cc2)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
122419141 177540 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 392 3 2 6 4.2 CC1CCN(C(=O)c2nsc3cc(Nc4n[nH]c5cccnc45)ccc23)CC1 10.1021/acs.jmedchem.8b00994
CHEMBL4452606 177540 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 392 3 2 6 4.2 CC1CCN(C(=O)c2nsc3cc(Nc4n[nH]c5cccnc45)ccc23)CC1 10.1021/acs.jmedchem.8b00994
54670120 151870 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 377 5 1 6 2.9 O=C(Nc1ncc(S(=O)(=O)Cc2ccccc2F)s1)c1ccccn1 nan
CHEMBL3911644 151870 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 377 5 1 6 2.9 O=C(Nc1ncc(S(=O)(=O)Cc2ccccc2F)s1)c1ccccn1 nan
52913077 147157 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 375 5 1 5 3.2 O=C(Nc1ccn(S(=O)(=O)Cc2ccc(Cl)cc2)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
CHEMBL3808534 147157 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 375 5 1 5 3.2 O=C(Nc1ccn(S(=O)(=O)Cc2ccc(Cl)cc2)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
122419141 177540 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 392 3 2 6 4.2 CC1CCN(C(=O)c2nsc3cc(Nc4n[nH]c5cccnc45)ccc23)CC1 10.1021/acs.jmedchem.8b00994
CHEMBL4452606 177540 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 392 3 2 6 4.2 CC1CCN(C(=O)c2nsc3cc(Nc4n[nH]c5cccnc45)ccc23)CC1 10.1021/acs.jmedchem.8b00994
127046201 146550 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
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 4.3 CC1c2ccccc2C(=O)N1c1ccc(NC(=O)c2ncccc2N)cc1Cl 10.1016/j.bmcl.2016.04.041
CHEMBL3798583 146550 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
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 4.3 CC1c2ccccc2C(=O)N1c1ccc(NC(=O)c2ncccc2N)cc1Cl 10.1016/j.bmcl.2016.04.041
137639864 163531 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
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 482 4 1 7 6.2 Cc1ncccc1N1CCC(Cc2ccc3oc(-c4cc5sccc5cn4)c/c(=N\O)c3c2)CC1 10.1021/acs.jmedchem.7b00991
CHEMBL4070594 163531 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
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 482 4 1 7 6.2 Cc1ncccc1N1CCC(Cc2ccc3oc(-c4cc5sccc5cn4)c/c(=N\O)c3c2)CC1 10.1021/acs.jmedchem.7b00991
137660178 165898 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
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 442 4 1 8 4.7 O/N=c1\cc(-c2cc3sccc3cn2)oc2ccc(OC3CN(c4cccnc4)C3)cc12 10.1021/acs.jmedchem.7b00991
CHEMBL4097743 165898 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
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 442 4 1 8 4.7 O/N=c1\cc(-c2cc3sccc3cn2)oc2ccc(OC3CN(c4cccnc4)C3)cc12 10.1021/acs.jmedchem.7b00991
155549892 180690 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 295 3 2 5 3.9 CCc1nsc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
CHEMBL4540386 180690 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 295 3 2 5 3.9 CCc1nsc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
57765616 164197 0 None 2 3 Human 6.4 pEC50 = 6.4 Functional
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 386 7 4 6 1.7 N[C@@H](CCP(=O)(O)C(O)c1ccc([N+](=O)[O-])c(C(F)(F)F)c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4078629 164197 0 None 2 3 Human 6.4 pEC50 = 6.4 Functional
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 386 7 4 6 1.7 N[C@@H](CCP(=O)(O)C(O)c1ccc([N+](=O)[O-])c(C(F)(F)F)c1)C(=O)O 10.1021/acs.jmedchem.7b01438
1368 9070 37 None -24 11 Rat 5.4 pEC50 = 5.4 Functional
Metabotropic glutamate receptor 4 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 4 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 10.1021/jm030967o
5310956 9070 37 None -24 11 Rat 5.4 pEC50 = 5.4 Functional
Metabotropic glutamate receptor 4 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 4 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 10.1021/jm030967o
CHEMBL280563 9070 37 None -24 11 Rat 5.4 pEC50 = 5.4 Functional
Metabotropic glutamate receptor 4 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 4 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 10.1021/jm030967o
122197953 166732 0 None 1 3 Rat 5.4 pEC50 = 5.4 Functional
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 391 10 6 7 -0.1 N[C@H](CCP(=O)(O)C(O)c1ccc(OCC(=O)O)c(C(=O)O)c1)C(=O)O nan
CHEMBL4107377 166732 0 None 1 3 Rat 5.4 pEC50 = 5.4 Functional
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 391 10 6 7 -0.1 N[C@H](CCP(=O)(O)C(O)c1ccc(OCC(=O)O)c(C(=O)O)c1)C(=O)O nan
4302961 11572 4 None - 1 Human 4.4 pEC50 = 4.4 Functional
Agonist activity against Metabotropic glutamate receptor 4 expressed in HEK 293 cells was evaluated by measuring total inositol phosphate accumulationAgonist activity against Metabotropic glutamate receptor 4 expressed in HEK 293 cells was evaluated by measuring total inositol phosphate accumulation
ChEMBL 217 3 4 4 -1.0 NC1(C(=O)O)CC(C(=O)O)C(C(=O)O)C1 10.1021/jm970207b
CHEMBL104116 11572 4 None - 1 Human 4.4 pEC50 = 4.4 Functional
Agonist activity against Metabotropic glutamate receptor 4 expressed in HEK 293 cells was evaluated by measuring total inositol phosphate accumulationAgonist activity against Metabotropic glutamate receptor 4 expressed in HEK 293 cells was evaluated by measuring total inositol phosphate accumulation
ChEMBL 217 3 4 4 -1.0 NC1(C(=O)O)CC(C(=O)O)C(C(=O)O)C1 10.1021/jm970207b
54670220 157739 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 445 5 1 6 3.9 O=C(Nc1nc(C(F)(F)F)c(S(=O)(=O)Cc2ccccc2F)s1)c1ccccn1 nan
CHEMBL3958116 157739 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 445 5 1 6 3.9 O=C(Nc1nc(C(F)(F)F)c(S(=O)(=O)Cc2ccccc2F)s1)c1ccccn1 nan
46843042 75476 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
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 414 3 1 5 2.8 O=C(Nc1ccc(N2S(=O)(=O)c3ccccc3S2(=O)=O)cc1)c1ccccc1 10.1021/jm200956q
CHEMBL1921853 75476 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
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 414 3 1 5 2.8 O=C(Nc1ccc(N2S(=O)(=O)c3ccccc3S2(=O)=O)cc1)c1ccccc1 10.1021/jm200956q
51003373 74582 0 None 1 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 358 4 2 5 3.7 O=C(Nc1ccc(NC(=O)c2nccs2)c(Cl)c1)c1ccccn1 10.1021/jm101271s
CHEMBL1909434 74582 0 None 1 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 358 4 2 5 3.7 O=C(Nc1ccc(NC(=O)c2nccs2)c(Cl)c1)c1ccccn1 10.1021/jm101271s
134191538 188142 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 260 2 2 3 3.9 c1ccc2cc(Nc3n[nH]c4cccnc34)ccc2c1 10.1016/j.bmcl.2018.10.050
CHEMBL4763214 188142 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 260 2 2 3 3.9 c1ccc2cc(Nc3n[nH]c4cccnc34)ccc2c1 10.1016/j.bmcl.2018.10.050
127028303 144536 0 None -7 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGlu4 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu4 receptor by cell based calcium mobilization
ChEMBL 415 3 1 5 4.3 Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3759289 144536 0 None -7 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGlu4 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu4 receptor by cell based calcium mobilization
ChEMBL 415 3 1 5 4.3 Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
6330803 98897 10 None -2 3 Rat 5.4 pEC50 = 5.4 Functional
Agonist activity at rat mGluR4 receptor expressed HEK293 cells assessed as effect on inositol phosphate productionAgonist activity at rat mGluR4 receptor expressed HEK293 cells assessed as effect on inositol phosphate production
ChEMBL 167 4 3 3 -0.7 N[C@@H](CC[PH](=O)O)C(=O)O 10.1021/jm070400y
CHEMBL241972 98897 10 None -2 3 Rat 5.4 pEC50 = 5.4 Functional
Agonist activity at rat mGluR4 receptor expressed HEK293 cells assessed as effect on inositol phosphate productionAgonist activity at rat mGluR4 receptor expressed HEK293 cells assessed as effect on inositol phosphate production
ChEMBL 167 4 3 3 -0.7 N[C@@H](CC[PH](=O)O)C(=O)O 10.1021/jm070400y
16748099 126641 1 None 1 2 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at mGlu4 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate productionAgonist activity at mGlu4 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate production
ChEMBL 195 3 4 3 -1.0 N[C@]1(C(=O)O)C[C@@H]1CP(=O)(O)O 10.1021/jm070262c
CHEMBL34880 126641 1 None 1 2 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at mGlu4 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate productionAgonist activity at mGlu4 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate production
ChEMBL 195 3 4 3 -1.0 N[C@]1(C(=O)O)C[C@@H]1CP(=O)(O)O 10.1021/jm070262c
46869944 65901 0 None -1 2 Human 7.4 pEC50 = 7.4 Functional
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 411 3 1 4 4.4 O=C(Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(Cl)c1)c1ccccn1 10.1021/jm200956q
CHEMBL1698378 65901 0 None -1 2 Human 7.4 pEC50 = 7.4 Functional
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 411 3 1 4 4.4 O=C(Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(Cl)c1)c1ccccn1 10.1021/jm200956q
42645487 7922 2 None - 1 Human 6.4 pEC50 = 6.4 Functional
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 243 3 2 5 2.7 c1ccc(nc1)Nc1scc(n1)c1c[nH]nc1 10.1021/jm200290z
6232 7922 2 None - 1 Human 6.4 pEC50 = 6.4 Functional
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 243 3 2 5 2.7 c1ccc(nc1)Nc1scc(n1)c1c[nH]nc1 10.1021/jm200290z
CHEMBL1830693 7922 2 None - 1 Human 6.4 pEC50 = 6.4 Functional
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 243 3 2 5 2.7 c1ccc(nc1)Nc1scc(n1)c1c[nH]nc1 10.1021/jm200290z
53374310 152205 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 258 2 2 3 3.7 Cc1ccc(Cl)cc1Nc1n[nH]c2cccnc12 nan
CHEMBL3914154 152205 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 258 2 2 3 3.7 Cc1ccc(Cl)cc1Nc1n[nH]c2cccnc12 nan
53373882 159982 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 296 2 2 3 4.1 Fc1c(Cl)cc(Nc2n[nH]c3cccnc23)cc1Cl nan
CHEMBL3977207 159982 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 296 2 2 3 4.1 Fc1c(Cl)cc(Nc2n[nH]c3cccnc23)cc1Cl nan
44572113 195677 4 None -1 2 Human 5.4 pEC50 = 5.4 Functional
Activity at human mGluR4 expressed in CHO coexpressing Gqi5 assessed as potentiation of glutamate-induced calcium flux by fluorescence assayActivity at human mGluR4 expressed in CHO coexpressing Gqi5 assessed as potentiation of glutamate-induced calcium flux by fluorescence assay
ChEMBL 294 2 2 4 2.7 O=C(Nc1ccccc1)[C@]12C[C@H]1/C(=N\O)c1ccccc1O2 10.1016/j.bmcl.2008.08.087
CHEMBL507522 195677 4 None -1 2 Human 5.4 pEC50 = 5.4 Functional
Activity at human mGluR4 expressed in CHO coexpressing Gqi5 assessed as potentiation of glutamate-induced calcium flux by fluorescence assayActivity at human mGluR4 expressed in CHO coexpressing Gqi5 assessed as potentiation of glutamate-induced calcium flux by fluorescence assay
ChEMBL 294 2 2 4 2.7 O=C(Nc1ccccc1)[C@]12C[C@H]1/C(=N\O)c1ccccc1O2 10.1016/j.bmcl.2008.08.087
836051 202450 18 None - 1 Human 5.4 pEC50 = 5.4 Functional
Activity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilizationActivity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilization
ChEMBL 333 2 1 2 4.6 O=C(Nc1ccc(Cl)c(Cl)c1)c1ccc(Br)o1 10.1021/jm9005065
CHEMBL556535 202450 18 None - 1 Human 5.4 pEC50 = 5.4 Functional
Activity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilizationActivity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilization
ChEMBL 333 2 1 2 4.6 O=C(Nc1ccc(Cl)c(Cl)c1)c1ccc(Br)o1 10.1021/jm9005065
49862693 21903 2 None - 1 Human 5.4 pEC50 = 5.4 Functional
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 203 2 1 4 2.3 Nc1nccc(/C=C/c2cccs2)n1 10.1016/j.bmcl.2010.06.078
CHEMBL1209741 21903 2 None - 1 Human 5.4 pEC50 = 5.4 Functional
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 203 2 1 4 2.3 Nc1nccc(/C=C/c2cccs2)n1 10.1016/j.bmcl.2010.06.078
101884456 128907 0 None - 1 Rat 5.4 pEC50 = 5.4 Functional
Positive allosteric modulator activity at rat mGlu4 receptor expressed in HEK293 cells assessed as effect on L-AP4-induced inositol phosphate accumulation incubated for 30 mins by florescence assayPositive allosteric modulator activity at rat mGlu4 receptor expressed in HEK293 cells assessed as effect on L-AP4-induced inositol phosphate accumulation incubated for 30 mins by florescence assay
ChEMBL 362 3 1 3 4.4 COc1cc(NC(=O)c2ccccn2)ccc1C#Cc1ccccc1Cl 10.1039/C4MD00208C
CHEMBL3596586 128907 0 None - 1 Rat 5.4 pEC50 = 5.4 Functional
Positive allosteric modulator activity at rat mGlu4 receptor expressed in HEK293 cells assessed as effect on L-AP4-induced inositol phosphate accumulation incubated for 30 mins by florescence assayPositive allosteric modulator activity at rat mGlu4 receptor expressed in HEK293 cells assessed as effect on L-AP4-induced inositol phosphate accumulation incubated for 30 mins by florescence assay
ChEMBL 362 3 1 3 4.4 COc1cc(NC(=O)c2ccccn2)ccc1C#Cc1ccccc1Cl 10.1039/C4MD00208C
137643079 165245 0 None - 1 Human 4.4 pEC50 = 4.4 Functional
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 298 6 4 5 0.6 N#Cc1cccc(C(O)P(=O)(O)CC[C@H](N)C(=O)O)c1 10.1021/acs.jmedchem.7b01438
CHEMBL4090699 165245 0 None - 1 Human 4.4 pEC50 = 4.4 Functional
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 298 6 4 5 0.6 N#Cc1cccc(C(O)P(=O)(O)CC[C@H](N)C(=O)O)c1 10.1021/acs.jmedchem.7b01438
134191965 172492 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 322 4 2 6 3.4 CC(C)Oc1nn(C)c2cc(Nc3n[nH]c4cccnc34)ccc12 10.1016/j.bmcl.2018.06.034
CHEMBL4245763 172492 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 322 4 2 6 3.4 CC(C)Oc1nn(C)c2cc(Nc3n[nH]c4cccnc34)ccc12 10.1016/j.bmcl.2018.06.034
54670222 147236 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 425 5 1 6 3.9 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccc(Cl)cc1F 10.1016/j.bmcl.2016.05.029
CHEMBL3809402 147236 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 425 5 1 6 3.9 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccc(Cl)cc1F 10.1016/j.bmcl.2016.05.029
52934740 149384 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 370 4 1 7 2.1 O=C(Nc1cnn(S(=O)(=O)c2ccc(F)c(F)c2)c1)c1nccs1 nan
CHEMBL3891422 149384 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 370 4 1 7 2.1 O=C(Nc1cnn(S(=O)(=O)c2ccc(F)c(F)c2)c1)c1nccs1 nan
52914203 147175 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 355 5 1 5 2.8 Cc1cccc(CS(=O)(=O)n2ccc(NC(=O)c3ccccn3)c2)c1 10.1016/j.bmcl.2016.05.029
CHEMBL3808698 147175 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 355 5 1 5 2.8 Cc1cccc(CS(=O)(=O)n2ccc(NC(=O)c3ccccn3)c2)c1 10.1016/j.bmcl.2016.05.029
54670222 147236 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 425 5 1 6 3.9 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccc(Cl)cc1F 10.1016/j.bmcl.2016.05.029
CHEMBL3809402 147236 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 425 5 1 6 3.9 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccc(Cl)cc1F 10.1016/j.bmcl.2016.05.029
52914203 147175 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 355 5 1 5 2.8 Cc1cccc(CS(=O)(=O)n2ccc(NC(=O)c3ccccn3)c2)c1 10.1016/j.bmcl.2016.05.029
CHEMBL3808698 147175 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 355 5 1 5 2.8 Cc1cccc(CS(=O)(=O)n2ccc(NC(=O)c3ccccn3)c2)c1 10.1016/j.bmcl.2016.05.029
58058372 162976 0 None 3 3 Human 6.4 pEC50 = 6.4 Functional
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 302 7 3 5 1.2 N[C@@H](CCP(=O)(O)Cc1cccc([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4064187 162976 0 None 3 3 Human 6.4 pEC50 = 6.4 Functional
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 302 7 3 5 1.2 N[C@@H](CCP(=O)(O)Cc1cccc([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
137651881 164063 0 None 1 2 Human 4.4 pEC50 = 4.4 Functional
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 290 6 5 6 -0.2 N[C@@H](CCP(=O)(O)C(O)c1ccnc(O)c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4076857 164063 0 None 1 2 Human 4.4 pEC50 = 4.4 Functional
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 290 6 5 6 -0.2 N[C@@H](CCP(=O)(O)C(O)c1ccnc(O)c1)C(=O)O 10.1021/acs.jmedchem.7b01438
122196100 131013 0 None -19 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 374 3 1 4 4.3 Cc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(C)c2C1=O 10.1016/j.bmcl.2015.10.013
CHEMBL3634423 131013 0 None -19 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 374 3 1 4 4.3 Cc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(C)c2C1=O 10.1016/j.bmcl.2015.10.013
51003284 64678 0 None 1 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 357 4 2 3 4.5 O=C(Nc1ccc(NC(=O)C2CCCCC2)c(Cl)c1)c1ccccn1 10.1021/jm101271s
CHEMBL1672243 64678 0 None 1 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 357 4 2 3 4.5 O=C(Nc1ccc(NC(=O)C2CCCCC2)c(Cl)c1)c1ccccn1 10.1021/jm101271s
53374407 154872 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 350 5 2 4 4.9 Clc1cc(Nc2n[nH]c3cccnc23)ccc1OCc1ccccc1 nan
CHEMBL3935108 154872 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 350 5 2 4 4.9 Clc1cc(Nc2n[nH]c3cccnc23)ccc1OCc1ccccc1 nan
51003326 64681 0 None 1 2 Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 317 4 2 3 3.6 CC(C)C(=O)Nc1ccc(NC(=O)c2ccccn2)cc1Cl 10.1021/jm101271s
CHEMBL1672246 64681 0 None 1 2 Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 317 4 2 3 3.6 CC(C)C(=O)Nc1ccc(NC(=O)c2ccccn2)cc1Cl 10.1021/jm101271s
122196120 131032 0 None -26 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 410 3 1 4 5.1 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c2ccccc12 10.1016/j.bmcl.2015.10.013
CHEMBL3634442 131032 0 None -26 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 410 3 1 4 5.1 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c2ccccc12 10.1016/j.bmcl.2015.10.013
134191934 172236 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 304 3 2 5 3.5 Cn1nc(C2CC2)c2ccc(Nc3n[nH]c4cccnc34)cc21 10.1021/acs.jmedchem.8b00994
CHEMBL4239430 172236 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 304 3 2 5 3.5 Cn1nc(C2CC2)c2ccc(Nc3n[nH]c4cccnc34)cc21 10.1021/acs.jmedchem.8b00994
134191934 172236 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 304 3 2 5 3.5 Cn1nc(C2CC2)c2ccc(Nc3n[nH]c4cccnc34)cc21 10.1016/j.bmcl.2018.06.034
CHEMBL4239430 172236 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 304 3 2 5 3.5 Cn1nc(C2CC2)c2ccc(Nc3n[nH]c4cccnc34)cc21 10.1016/j.bmcl.2018.06.034
53374215 157838 1 None - 1 Human 7.4 pEC50 = 7.4 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 278 2 2 3 4.0 Clc1cc(Cl)cc(Nc2n[nH]c3cccnc23)c1 nan
CHEMBL3958804 157838 1 None - 1 Human 7.4 pEC50 = 7.4 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 278 2 2 3 4.0 Clc1cc(Cl)cc(Nc2n[nH]c3cccnc23)c1 nan
134191938 172318 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 304 3 2 5 3.5 Cn1nc(C2CC2)c2ccc(Nc3n[nH]c4ncccc34)cc21 10.1016/j.bmcl.2018.06.034
CHEMBL4241489 172318 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 304 3 2 5 3.5 Cn1nc(C2CC2)c2ccc(Nc3n[nH]c4ncccc34)cc21 10.1016/j.bmcl.2018.06.034
58058356 165573 0 None 2 3 Human 5.4 pEC50 = 5.4 Functional
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 350 7 6 8 0.1 N[C@@H](CCP(=O)(O)C(O)c1cc(O)c(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4094241 165573 0 None 2 3 Human 5.4 pEC50 = 5.4 Functional
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 350 7 6 8 0.1 N[C@@H](CCP(=O)(O)C(O)c1cc(O)c(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
70681380 80927 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 277 2 0 4 4.1 c1csc(-n2cc(-c3ccnc4ccccc34)cn2)c1 10.1016/j.bmcl.2012.03.032
CHEMBL2022873 80927 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 277 2 0 4 4.1 c1csc(-n2cc(-c3ccnc4ccccc34)cn2)c1 10.1016/j.bmcl.2012.03.032
46869949 66207 1 None 1 2 Human 6.4 pEC50 = 6.4 Functional
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 3 1 4 3.1 CC1(C)[C@H]2C(=O)N(c3ccc(NC(=O)c4ccccn4)cc3Cl)C(=O)[C@H]21 10.1021/jm200956q
CHEMBL1711049 66207 1 None 1 2 Human 6.4 pEC50 = 6.4 Functional
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 3 1 4 3.1 CC1(C)[C@H]2C(=O)N(c3ccc(NC(=O)c4ccccn4)cc3Cl)C(=O)[C@H]21 10.1021/jm200956q
88957119 147270 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 362 4 1 6 2.4 O=C(Nc1ccn(S(=O)(=O)c2ccc(Cl)nc2)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
CHEMBL3809795 147270 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 362 4 1 6 2.4 O=C(Nc1ccn(S(=O)(=O)c2ccc(Cl)nc2)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
51003327 64682 0 None -1 2 Rat 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 369 4 2 3 4.4 O=C(Nc1ccc(NC(=O)c2ccccc2F)c(Cl)c1)c1ccccn1 10.1021/jm101271s
CHEMBL1672247 64682 0 None -1 2 Rat 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 369 4 2 3 4.4 O=C(Nc1ccc(NC(=O)c2ccccc2F)c(Cl)c1)c1ccccn1 10.1021/jm101271s
53495171 147279 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 411 5 1 6 3.6 O=C(Nc1ncc(S(=O)(=O)Cc2ccc(Cl)cc2F)s1)c1ccccn1 nan
CHEMBL3809990 147279 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 411 5 1 6 3.6 O=C(Nc1ncc(S(=O)(=O)Cc2ccc(Cl)cc2F)s1)c1ccccn1 nan
57765622 162883 0 None 3 3 Human 6.4 pEC50 = 6.4 Functional
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 386 7 4 6 1.7 N[C@@H](CCP(=O)(O)C(O)c1ccc(C(F)(F)F)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4063142 162883 0 None 3 3 Human 6.4 pEC50 = 6.4 Functional
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 386 7 4 6 1.7 N[C@@H](CCP(=O)(O)C(O)c1ccc(C(F)(F)F)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
57765613 165269 0 None 1 3 Human 6.4 pEC50 = 6.4 Functional
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 336 7 4 6 0.8 N[C@@H](CCP(=O)(O)C(O)c1ccc(F)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4091029 165269 0 None 1 3 Human 6.4 pEC50 = 6.4 Functional
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 336 7 4 6 0.8 N[C@@H](CCP(=O)(O)C(O)c1ccc(F)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
88957119 147270 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 362 4 1 6 2.4 O=C(Nc1ccn(S(=O)(=O)c2ccc(Cl)nc2)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
CHEMBL3809795 147270 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 362 4 1 6 2.4 O=C(Nc1ccn(S(=O)(=O)c2ccc(Cl)nc2)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
124425164 164794 0 None -1 4 Human 5.4 pEC50 = 5.4 Functional
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 364 8 5 8 0.4 COc1cc([C@H](O)P(=O)(O)CC[C@H](N)C(=O)O)cc([N+](=O)[O-])c1O 10.1021/acs.jmedchem.7b01438
CHEMBL4085558 164794 0 None -1 4 Human 5.4 pEC50 = 5.4 Functional
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 364 8 5 8 0.4 COc1cc([C@H](O)P(=O)(O)CC[C@H](N)C(=O)O)cc([N+](=O)[O-])c1O 10.1021/acs.jmedchem.7b01438
137643617 164927 0 None 1 2 Human 5.4 pEC50 = 5.4 Functional
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 421 11 4 6 2.5 N[C@@H](CCP(=O)(O)C(NCCc1ccccc1)c1cccc([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4087249 164927 0 None 1 2 Human 5.4 pEC50 = 5.4 Functional
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 421 11 4 6 2.5 N[C@@H](CCP(=O)(O)C(NCCc1ccccc1)c1cccc([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
54670596 153098 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 387 5 1 6 3.4 Cc1ccc(CS(=O)(=O)c2sc(NC(=O)c3ccccn3)nc2C)cc1 nan
CHEMBL3921043 153098 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 387 5 1 6 3.4 Cc1ccc(CS(=O)(=O)c2sc(NC(=O)c3ccccn3)nc2C)cc1 nan
54670123 147172 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 407 5 1 6 3.7 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccccc1Cl 10.1016/j.bmcl.2016.05.029
CHEMBL3808634 147172 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 407 5 1 6 3.7 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccccc1Cl 10.1016/j.bmcl.2016.05.029
122419143 182570 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 406 3 2 6 4.4 CC1CC(C)CN(C(=O)c2nsc3cc(Nc4n[nH]c5cccnc45)ccc23)C1 10.1021/acs.jmedchem.8b00994
CHEMBL4584171 182570 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 406 3 2 6 4.4 CC1CC(C)CN(C(=O)c2nsc3cc(Nc4n[nH]c5cccnc45)ccc23)C1 10.1021/acs.jmedchem.8b00994
122419143 182570 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 406 3 2 6 4.4 CC1CC(C)CN(C(=O)c2nsc3cc(Nc4n[nH]c5cccnc45)ccc23)C1 10.1021/acs.jmedchem.8b00994
CHEMBL4584171 182570 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 406 3 2 6 4.4 CC1CC(C)CN(C(=O)c2nsc3cc(Nc4n[nH]c5cccnc45)ccc23)C1 10.1021/acs.jmedchem.8b00994
122196116 131028 0 None -5 2 Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 362 3 1 6 2.7 Cc1ccoc1C(=O)Nc1cnc(N2C(=O)c3cccc(C)c3C2=O)nc1 10.1016/j.bmcl.2015.10.013
CHEMBL3634438 131028 0 None -5 2 Human 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 362 3 1 6 2.7 Cc1ccoc1C(=O)Nc1cnc(N2C(=O)c3cccc(C)c3C2=O)nc1 10.1016/j.bmcl.2015.10.013
54670123 147172 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 407 5 1 6 3.7 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccccc1Cl 10.1016/j.bmcl.2016.05.029
CHEMBL3808634 147172 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 407 5 1 6 3.7 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccccc1Cl 10.1016/j.bmcl.2016.05.029
134191470 186199 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 341 3 2 6 3.7 Cn1nccc1-c1nccc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1016/j.bmcl.2018.10.050
CHEMBL4740237 186199 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 341 3 2 6 3.7 Cn1nccc1-c1nccc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1016/j.bmcl.2018.10.050
134191605 187528 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 289 3 2 4 3.8 CCc1nccc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1016/j.bmcl.2018.10.050
CHEMBL4756046 187528 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 289 3 2 4 3.8 CCc1nccc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1016/j.bmcl.2018.10.050
134192169 172587 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 364 4 2 7 3.1 Cn1nc(OC2CCOCC2)c2ccc(Nc3n[nH]c4cccnc34)cc21 10.1016/j.bmcl.2018.06.034
CHEMBL4248273 172587 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 364 4 2 7 3.1 Cn1nc(OC2CCOCC2)c2ccc(Nc3n[nH]c4cccnc34)cc21 10.1016/j.bmcl.2018.06.034
54670411 155721 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 401 6 1 6 3.6 CCc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccc(C)cc1 nan
CHEMBL3941960 155721 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 401 6 1 6 3.6 CCc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccc(C)cc1 nan
137654697 165466 0 None 8 3 Human 5.4 pEC50 = 5.4 Functional
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 334 7 5 7 0.4 N[C@@H](CCP(=O)(O)[C@@H](O)c1ccc(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4093081 165466 0 None 8 3 Human 5.4 pEC50 = 5.4 Functional
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 334 7 5 7 0.4 N[C@@H](CCP(=O)(O)[C@@H](O)c1ccc(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
49862631 21888 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
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 215 2 1 3 2.4 Nc1nccc(/C=C/c2cccc(F)c2)n1 10.1016/j.bmcl.2010.06.078
CHEMBL1209660 21888 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
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 215 2 1 3 2.4 Nc1nccc(/C=C/c2cccc(F)c2)n1 10.1016/j.bmcl.2010.06.078
49862632 21889 6 None - 1 Human 5.4 pEC50 = 5.4 Functional
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 215 2 1 3 2.4 Nc1nccc(/C=C/c2ccc(F)cc2)n1 10.1016/j.bmcl.2010.06.078
CHEMBL1209661 21889 6 None - 1 Human 5.4 pEC50 = 5.4 Functional
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 215 2 1 3 2.4 Nc1nccc(/C=C/c2ccc(F)cc2)n1 10.1016/j.bmcl.2010.06.078
134192043 172343 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 290 3 3 4 3.5 c1cnc2c(Nc3ccc4c(C5CC5)n[nH]c4c3)n[nH]c2c1 10.1016/j.bmcl.2018.06.034
CHEMBL4242079 172343 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 290 3 3 4 3.5 c1cnc2c(Nc3ccc4c(C5CC5)n[nH]c4c3)n[nH]c2c1 10.1016/j.bmcl.2018.06.034
87305070 163295 0 None -2 2 Human 7.3 pEC50 = 7.3 Functional
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 406 5 1 8 2.7 O/N=c1\cc(-c2cc3cccn3cn2)oc2ccc(OCCN3CCOCC3)cc12 10.1021/acs.jmedchem.7b00991
CHEMBL4067875 163295 0 None -2 2 Human 7.3 pEC50 = 7.3 Functional
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 406 5 1 8 2.7 O/N=c1\cc(-c2cc3cccn3cn2)oc2ccc(OCCN3CCOCC3)cc12 10.1021/acs.jmedchem.7b00991
134198221 172321 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 332 4 2 5 4.2 Cc1nn(CC2CCC2)c2ccc(Nc3n[nH]c4cccnc34)cc12 10.1016/j.bmcl.2018.06.034
CHEMBL4241532 172321 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 332 4 2 5 4.2 Cc1nn(CC2CCC2)c2ccc(Nc3n[nH]c4cccnc34)cc12 10.1016/j.bmcl.2018.06.034
3260619 10791 24 None -1 4 Human 5.3 pEC50 = 5.3 Functional
Activity at human mGluR4 expressed in CHO coexpressing Gqi5 assessed as potentiation of glutamate-induced calcium flux by fluorescence assayActivity at human mGluR4 expressed in CHO coexpressing Gqi5 assessed as potentiation of glutamate-induced calcium flux by fluorescence assay
ChEMBL 321 2 0 5 3.7 CC1CCCN(C1)c1ncnc2c1cnn2c1ccc(cc1C)C 10.1016/j.bmcl.2008.08.087
6227 10791 24 None -1 4 Human 5.3 pEC50 = 5.3 Functional
Activity at human mGluR4 expressed in CHO coexpressing Gqi5 assessed as potentiation of glutamate-induced calcium flux by fluorescence assayActivity at human mGluR4 expressed in CHO coexpressing Gqi5 assessed as potentiation of glutamate-induced calcium flux by fluorescence assay
ChEMBL 321 2 0 5 3.7 CC1CCCN(C1)c1ncnc2c1cnn2c1ccc(cc1C)C 10.1016/j.bmcl.2008.08.087
CHEMBL477396 10791 24 None -1 4 Human 5.3 pEC50 = 5.3 Functional
Activity at human mGluR4 expressed in CHO coexpressing Gqi5 assessed as potentiation of glutamate-induced calcium flux by fluorescence assayActivity at human mGluR4 expressed in CHO coexpressing Gqi5 assessed as potentiation of glutamate-induced calcium flux by fluorescence assay
ChEMBL 321 2 0 5 3.7 CC1CCCN(C1)c1ncnc2c1cnn2c1ccc(cc1C)C 10.1016/j.bmcl.2008.08.087
24779945 15013 0 None 3 3 Rat 5.3 pEC50 = 5.3 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 297 9 5 5 -0.8 N[C@@H](CCP(=O)(O)CC(CC(=O)O)C(=O)O)C(=O)O 10.1021/jm901523t
CHEMBL1092315 15013 0 None 3 3 Rat 5.3 pEC50 = 5.3 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 297 9 5 5 -0.8 N[C@@H](CCP(=O)(O)CC(CC(=O)O)C(=O)O)C(=O)O 10.1021/jm901523t
17017653 72298 8 None - 1 Human 5.3 pEC50 = 5.3 Functional
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 321 2 0 5 3.7 Cc1cc(C)cc(-n2ncc3c(N4CCCC(C)C4)ncnc32)c1 10.1021/jm200290z
CHEMBL1830697 72298 8 None - 1 Human 5.3 pEC50 = 5.3 Functional
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 321 2 0 5 3.7 Cc1cc(C)cc(-n2ncc3c(N4CCCC(C)C4)ncnc32)c1 10.1021/jm200290z
57391520 75694 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as potentiation of EC20 glutamate-induced calcium mobilization after 2.5 minsPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as potentiation of EC20 glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 291 4 0 3 3.1 O=C(COc1ccccc1Br)c1ccccn1 10.1016/j.bmcl.2011.09.131
CHEMBL1922727 75694 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as potentiation of EC20 glutamate-induced calcium mobilization after 2.5 minsPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as potentiation of EC20 glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 291 4 0 3 3.1 O=C(COc1ccccc1Br)c1ccccn1 10.1016/j.bmcl.2011.09.131
54670324 157491 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 427 6 1 6 3.5 O=C(Nc1nc(CF)c(S(=O)(=O)Cc2c(F)cccc2F)s1)c1ccccn1 nan
CHEMBL3956107 157491 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 427 6 1 6 3.5 O=C(Nc1nc(CF)c(S(=O)(=O)Cc2c(F)cccc2F)s1)c1ccccn1 nan
135125802 176999 0 None -2 2 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 385 3 1 5 3.1 Cc1nnc2ccc(C(=O)NC3CN(c4ncc(F)cc4Cl)C3)cc2c1C 10.1016/j.bmcl.2019.126678
CHEMBL4445506 176999 0 None -2 2 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 385 3 1 5 3.1 Cc1nnc2ccc(C(=O)NC3CN(c4ncc(F)cc4Cl)C3)cc2c1C 10.1016/j.bmcl.2019.126678
122196115 131027 0 None -1 2 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 348 3 1 6 2.4 Cc1ccoc1C(=O)Nc1cnc(N2C(=O)c3ccccc3C2=O)nc1 10.1016/j.bmcl.2015.10.013
CHEMBL3634437 131027 0 None -1 2 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 348 3 1 6 2.4 Cc1ccoc1C(=O)Nc1cnc(N2C(=O)c3ccccc3C2=O)nc1 10.1016/j.bmcl.2015.10.013
134192017 172477 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 305 3 2 6 2.9 Cn1nc(C2CC2)c2ncc(Nc3n[nH]c4cccnc34)cc21 10.1016/j.bmcl.2018.06.034
CHEMBL4245399 172477 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 305 3 2 6 2.9 Cn1nc(C2CC2)c2ncc(Nc3n[nH]c4cccnc34)cc21 10.1016/j.bmcl.2018.06.034
135565465 165084 10 None 1 2 Rat 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of rat 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 rat 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 421 5 1 7 4.3 O/N=c1\cc(-c2cc3sccc3cn2)oc2ccc(CCCN3CCOCC3)cc12 10.1021/acs.jmedchem.7b00991
CHEMBL4089083 165084 10 None 1 2 Rat 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of rat 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 rat 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 421 5 1 7 4.3 O/N=c1\cc(-c2cc3sccc3cn2)oc2ccc(CCCN3CCOCC3)cc12 10.1021/acs.jmedchem.7b00991
57765535 164583 0 None 1 3 Human 5.3 pEC50 = 5.3 Functional
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 352 7 4 6 1.3 N[C@@H](CCP(=O)(O)C(O)c1ccc(Cl)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4083240 164583 0 None 1 3 Human 5.3 pEC50 = 5.3 Functional
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 352 7 4 6 1.3 N[C@@H](CCP(=O)(O)C(O)c1ccc(Cl)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
24779942 14993 0 None - 1 Rat 4.3 pEC50 = 4.3 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 283 8 5 5 -1.0 NC(CCP(=O)(O)C(CC(=O)O)C(=O)O)C(=O)O 10.1021/jm901523t
CHEMBL1092251 14993 0 None - 1 Rat 4.3 pEC50 = 4.3 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 283 8 5 5 -1.0 NC(CCP(=O)(O)C(CC(=O)O)C(=O)O)C(=O)O 10.1021/jm901523t
51003375 74584 0 None -1 2 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 404 4 2 4 4.7 Cn1c(C(=O)Nc2ccc(NC(=O)c3ccccn3)cc2Cl)cc2ccccc21 10.1021/jm101271s
CHEMBL1909436 74584 0 None -1 2 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 404 4 2 4 4.7 Cn1c(C(=O)Nc2ccc(NC(=O)c3ccccn3)cc2Cl)cc2ccccc21 10.1021/jm101271s
127025563 144519 0 None -2 2 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human mGlu4 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu4 receptor by cell based calcium mobilization
ChEMBL 415 3 1 5 4.3 Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3759171 144519 0 None -2 2 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human mGlu4 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu4 receptor by cell based calcium mobilization
ChEMBL 415 3 1 5 4.3 Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
44572113 195677 4 None -1 2 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 294 2 2 4 2.7 O=C(Nc1ccccc1)[C@]12C[C@H]1/C(=N\O)c1ccccc1O2 10.1021/jm101271s
CHEMBL507522 195677 4 None -1 2 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 294 2 2 4 2.7 O=C(Nc1ccccc1)[C@]12C[C@H]1/C(=N\O)c1ccccc1O2 10.1021/jm101271s
58058356 165573 0 None 2 3 Human 5.3 pEC50 = 5.3 Functional
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 350 7 6 8 0.1 N[C@@H](CCP(=O)(O)C(O)c1cc(O)c(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4094241 165573 0 None 2 3 Human 5.3 pEC50 = 5.3 Functional
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 350 7 6 8 0.1 N[C@@H](CCP(=O)(O)C(O)c1cc(O)c(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
49865352 22693 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilization
ChEMBL 388 5 2 5 3.2 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2Cl)cc1)c1ccncn1 10.1016/j.bmcl.2010.07.007
CHEMBL1223243 22693 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilization
ChEMBL 388 5 2 5 3.2 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2Cl)cc1)c1ccncn1 10.1016/j.bmcl.2010.07.007
54670869 160853 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 405 5 1 6 3.8 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)C(C)c1ccccc1F nan
CHEMBL3984753 160853 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 405 5 1 6 3.8 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)C(C)c1ccccc1F nan
122197943 167359 0 None 7 3 Rat 6.3 pEC50 = 6.3 Functional
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 343 8 5 5 0.8 N[C@H](CCP(=O)(O)C(O)c1ccc(/C=C/C(=O)O)cc1)C(=O)O nan
CHEMBL4112699 167359 0 None 7 3 Rat 6.3 pEC50 = 6.3 Functional
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 343 8 5 5 0.8 N[C@H](CCP(=O)(O)C(O)c1ccc(/C=C/C(=O)O)cc1)C(=O)O nan
70687762 80985 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 285 2 0 3 4.4 Cc1nn(-c2ccccc2)cc1-c1ccnc2ccccc12 10.1016/j.bmcl.2012.03.032
CHEMBL2023451 80985 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 285 2 0 3 4.4 Cc1nn(-c2ccccc2)cc1-c1ccnc2ccccc12 10.1016/j.bmcl.2012.03.032
6604704 108177 35 None -3 3 Human 4.3 pEC50 = 4.3 Functional
Agonist activity against Metabotropic glutamate receptor 4 expressed in HEK 293 cells was evaluated by measuring total inositol phosphate accumulationAgonist activity against Metabotropic glutamate receptor 4 expressed in HEK 293 cells was evaluated by measuring total inositol phosphate accumulation
ChEMBL 173 2 3 3 -0.3 N[C@@]1(C(=O)O)CC[C@H](C(=O)O)C1 10.1021/jm970207b
CHEMBL29726 108177 35 None -3 3 Human 4.3 pEC50 = 4.3 Functional
Agonist activity against Metabotropic glutamate receptor 4 expressed in HEK 293 cells was evaluated by measuring total inositol phosphate accumulationAgonist activity against Metabotropic glutamate receptor 4 expressed in HEK 293 cells was evaluated by measuring total inositol phosphate accumulation
ChEMBL 173 2 3 3 -0.3 N[C@@]1(C(=O)O)CC[C@H](C(=O)O)C1 10.1021/jm970207b
51003326 64681 0 None -1 2 Rat 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 317 4 2 3 3.6 CC(C)C(=O)Nc1ccc(NC(=O)c2ccccn2)cc1Cl 10.1021/jm101271s
CHEMBL1672246 64681 0 None -1 2 Rat 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 317 4 2 3 3.6 CC(C)C(=O)Nc1ccc(NC(=O)c2ccccn2)cc1Cl 10.1021/jm101271s
122196093 131006 0 None -16 2 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 380 3 1 4 4.3 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)cc1 10.1016/j.bmcl.2015.10.013
CHEMBL3634416 131006 0 None -16 2 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 380 3 1 4 4.3 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)cc1 10.1016/j.bmcl.2015.10.013
11565290 8461 11 None -1071 3 Rat 4.3 pEC50 = 4.3 Functional
Activity at rat mGluR4 receptor measured as intracellular calcium concentration in HEK293 cellsActivity at rat mGluR4 receptor measured as intracellular calcium concentration in HEK293 cells
ChEMBL 272 4 4 5 -1.9 OC(=O)/C=C/C(=O)N1C[C@](C[C@H]1C(=O)O)(N)C(=O)O 10.1016/j.bmcl.2006.06.062
1409 8461 11 None -1071 3 Rat 4.3 pEC50 = 4.3 Functional
Activity at rat mGluR4 receptor measured as intracellular calcium concentration in HEK293 cellsActivity at rat mGluR4 receptor measured as intracellular calcium concentration in HEK293 cells
ChEMBL 272 4 4 5 -1.9 OC(=O)/C=C/C(=O)N1C[C@](C[C@H]1C(=O)O)(N)C(=O)O 10.1016/j.bmcl.2006.06.062
CHEMBL212233 8461 11 None -1071 3 Rat 4.3 pEC50 = 4.3 Functional
Activity at rat mGluR4 receptor measured as intracellular calcium concentration in HEK293 cellsActivity at rat mGluR4 receptor measured as intracellular calcium concentration in HEK293 cells
ChEMBL 272 4 4 5 -1.9 OC(=O)/C=C/C(=O)N1C[C@](C[C@H]1C(=O)O)(N)C(=O)O 10.1016/j.bmcl.2006.06.062
52935409 152351 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 356 4 1 6 2.4 Cc1ccc(S(=O)(=O)n2cc(NC(=O)c3ccccn3)cn2)c(C)c1 nan
CHEMBL3915259 152351 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 356 4 1 6 2.4 Cc1ccc(S(=O)(=O)n2cc(NC(=O)c3ccccn3)cn2)c(C)c1 nan
54670689 151723 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 407 5 1 6 3.7 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccc(Cl)cc1 nan
CHEMBL3910418 151723 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 407 5 1 6 3.7 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccc(Cl)cc1 nan
54670590 159109 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 439 6 1 6 4.1 CCc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1cccc(Cl)c1F nan
CHEMBL3969803 159109 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 439 6 1 6 4.1 CCc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1cccc(Cl)c1F nan
54670121 155437 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 427 5 1 6 4.1 O=C(Nc1ncc(S(=O)(=O)Cc2ccc(Cl)cc2Cl)s1)c1ccccn1 nan
CHEMBL3939625 155437 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 427 5 1 6 4.1 O=C(Nc1ncc(S(=O)(=O)Cc2ccc(Cl)cc2Cl)s1)c1ccccn1 nan
57765633 165191 0 None 3 3 Human 6.3 pEC50 = 6.3 Functional
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 324 7 4 7 0.7 N[C@@H](CCP(=O)(O)C(O)c1ccc([N+](=O)[O-])s1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4090179 165191 0 None 3 3 Human 6.3 pEC50 = 6.3 Functional
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 324 7 4 7 0.7 N[C@@H](CCP(=O)(O)C(O)c1ccc([N+](=O)[O-])s1)C(=O)O 10.1021/acs.jmedchem.7b01438
24780225 162712 0 None 2 3 Human 5.3 pEC50 = 5.3 Functional
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 363 6 4 4 1.4 N[C@@H](CCP(=O)(O)C(O)c1c(F)c(F)c(F)c(F)c1F)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4061016 162712 0 None 2 3 Human 5.3 pEC50 = 5.3 Functional
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 363 6 4 4 1.4 N[C@@H](CCP(=O)(O)C(O)c1c(F)c(F)c(F)c(F)c1F)C(=O)O 10.1021/acs.jmedchem.7b01438
122197947 167166 0 None 5 2 Rat 5.3 pEC50 = 5.3 Functional
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 347 9 5 6 0.2 N[C@H](CCP(=O)(O)C(O)c1cccc(OCC(=O)O)c1)C(=O)O nan
CHEMBL4111192 167166 0 None 5 2 Rat 5.3 pEC50 = 5.3 Functional
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 347 9 5 6 0.2 N[C@H](CCP(=O)(O)C(O)c1cccc(OCC(=O)O)c1)C(=O)O nan
53388191 72320 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
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 308 2 2 6 3.0 N#Cc1cccc(Nc2nc3c(s2)CCCc2n[nH]cc2-3)n1 10.1021/jm200290z
CHEMBL1830907 72320 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
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 308 2 2 6 3.0 N#Cc1cccc(Nc2nc3c(s2)CCCc2n[nH]cc2-3)n1 10.1021/jm200290z
44551744 21875 36 None - 1 Human 5.3 pEC50 = 5.3 Functional
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 211 1 1 4 2.5 Nc1nccc(-c2cc3ccccc3o2)n1 10.1016/j.bmcl.2010.06.078
CHEMBL1209593 21875 36 None - 1 Human 5.3 pEC50 = 5.3 Functional
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 211 1 1 4 2.5 Nc1nccc(-c2cc3ccccc3o2)n1 10.1016/j.bmcl.2010.06.078
44406221 79451 1 None -1 2 Rat 4.3 pEC50 = 4.3 Functional
Functional activity at rat mGluR4Functional activity at rat mGluR4
ChEMBL 195 3 4 3 -1.0 N[C@H](C(=O)O)[C@@H]1C[C@H]1P(=O)(O)O 10.1016/j.bmcl.2005.09.014
CHEMBL199626 79451 1 None -1 2 Rat 4.3 pEC50 = 4.3 Functional
Functional activity at rat mGluR4Functional activity at rat mGluR4
ChEMBL 195 3 4 3 -1.0 N[C@H](C(=O)O)[C@@H]1C[C@H]1P(=O)(O)O 10.1016/j.bmcl.2005.09.014
53374308 155803 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 389 4 2 5 5.0 Fc1cc(Nc2n[nH]c3cccnc23)ccc1Oc1cc(C(F)(F)F)ccn1 nan
CHEMBL3942548 155803 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 389 4 2 5 5.0 Fc1cc(Nc2n[nH]c3cccnc23)ccc1Oc1cc(C(F)(F)F)ccn1 nan
54670868 158155 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 495 5 1 6 5.1 O=C(Nc1nc(C(F)(F)F)c(S(=O)(=O)Cc2ccc(Cl)cc2Cl)s1)c1ccccn1 nan
CHEMBL3961434 158155 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 495 5 1 6 5.1 O=C(Nc1nc(C(F)(F)F)c(S(=O)(=O)Cc2ccc(Cl)cc2Cl)s1)c1ccccn1 nan
134198344 172602 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 411 3 2 6 3.5 Cn1nc(C(=O)N2CCC(F)(F)CC2)c2ccc(Nc3n[nH]c4cccnc34)cc21 10.1016/j.bmcl.2018.06.034
CHEMBL4248576 172602 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 411 3 2 6 3.5 Cn1nc(C(=O)N2CCC(F)(F)CC2)c2ccc(Nc3n[nH]c4cccnc34)cc21 10.1016/j.bmcl.2018.06.034
137631939 163238 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
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 277 1 2 4 3.3 O/N=c1\cc(-c2cc3cc[nH]c3cn2)oc2ccccc12 10.1021/acs.jmedchem.7b00991
CHEMBL4067271 163238 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
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 277 1 2 4 3.3 O/N=c1\cc(-c2cc3cc[nH]c3cn2)oc2ccccc12 10.1021/acs.jmedchem.7b00991
137639171 163670 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
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 412 6 1 7 4.4 O/N=c1\cc(-c2cc3cccn3cn2)oc2ccc(OCCCc3cccnc3)cc12 10.1021/acs.jmedchem.7b00991
CHEMBL4072094 163670 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
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 412 6 1 7 4.4 O/N=c1\cc(-c2cc3cccn3cn2)oc2ccc(OCCCc3cccnc3)cc12 10.1021/acs.jmedchem.7b00991
122419159 182747 15 None 1 2 Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 400 4 3 6 3.8 O=C(NC1CC(F)(F)C1)c1nsc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
CHEMBL4588443 182747 15 None 1 2 Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 400 4 3 6 3.8 O=C(NC1CC(F)(F)C1)c1nsc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
122419159 182747 15 None 1 2 Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 400 4 3 6 3.8 O=C(NC1CC(F)(F)C1)c1nsc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
CHEMBL4588443 182747 15 None 1 2 Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 400 4 3 6 3.8 O=C(NC1CC(F)(F)C1)c1nsc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
137639752 163694 0 None 7 4 Human 6.3 pEC50 = 6.3 Functional
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 334 7 5 7 0.4 N[C@@H](CCP(=O)(O)[C@H](O)c1ccc(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4072316 163694 0 None 7 4 Human 6.3 pEC50 = 6.3 Functional
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 334 7 5 7 0.4 N[C@@H](CCP(=O)(O)[C@H](O)c1ccc(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
122197936 167555 0 None 17 3 Rat 6.3 pEC50 = 6.3 Functional
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 407 11 5 8 0.2 COc1cc(C(O)P(=O)(O)CC[C@@H](N)C(=O)O)cc(OC)c1OCC(=O)O nan
CHEMBL4114200 167555 0 None 17 3 Rat 6.3 pEC50 = 6.3 Functional
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 407 11 5 8 0.2 COc1cc(C(O)P(=O)(O)CC[C@@H](N)C(=O)O)cc(OC)c1OCC(=O)O nan
70696137 81017 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 384 3 0 5 4.7 O=C(Oc1ccc2c(-c3cnn(-c4ccccc4)c3)ccnc2c1)N1CCCC1 10.1016/j.bmcl.2012.03.032
CHEMBL2023625 81017 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 384 3 0 5 4.7 O=C(Oc1ccc2c(-c3cnn(-c4ccccc4)c3)ccnc2c1)N1CCCC1 10.1016/j.bmcl.2012.03.032
127043558 147274 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 327 5 1 5 4.1 O=C(Nc1ncc(SCc2ccccc2)s1)c1ccccn1 10.1016/j.bmcl.2016.05.029
CHEMBL3809868 147274 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 327 5 1 5 4.1 O=C(Nc1ncc(SCc2ccccc2)s1)c1ccccn1 10.1016/j.bmcl.2016.05.029
122196112 131024 0 None -52 2 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 361 3 1 5 3.3 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)nc1 10.1016/j.bmcl.2015.10.013
CHEMBL3634434 131024 0 None -52 2 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 361 3 1 5 3.3 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)nc1 10.1016/j.bmcl.2015.10.013
49862698 21907 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
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 297 4 1 5 2.1 CCOC(=O)C(=O)Nc1nccc(/C=C/c2ccccc2)n1 10.1016/j.bmcl.2010.06.078
CHEMBL1209746 21907 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
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 297 4 1 5 2.1 CCOC(=O)C(=O)Nc1nccc(/C=C/c2ccccc2)n1 10.1016/j.bmcl.2010.06.078
44572113 195677 4 None -1 2 Human 5.3 pEC50 = 5.3 Functional
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 294 2 2 4 2.7 O=C(Nc1ccccc1)[C@]12C[C@H]1/C(=N\O)c1ccccc1O2 10.1016/j.bmcl.2010.06.078
CHEMBL507522 195677 4 None -1 2 Human 5.3 pEC50 = 5.3 Functional
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 294 2 2 4 2.7 O=C(Nc1ccccc1)[C@]12C[C@H]1/C(=N\O)c1ccccc1O2 10.1016/j.bmcl.2010.06.078
54670319 151782 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 395 5 1 5 5.4 O=C(Nc1ncc(SCc2ccc(Cl)cc2Cl)s1)c1ccccn1 nan
CHEMBL3910947 151782 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 395 5 1 5 5.4 O=C(Nc1ncc(SCc2ccc(Cl)cc2Cl)s1)c1ccccn1 nan
54670123 147172 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 407 5 1 6 3.7 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccccc1Cl nan
CHEMBL3808634 147172 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 407 5 1 6 3.7 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccccc1Cl nan
127025845 144413 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human mGlu4 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu4 receptor by cell based calcium mobilization
ChEMBL 394 3 1 5 3.4 Cc1cccc2c1C(=O)N(c1ccc(NC(=O)c3nccn3C)cc1Cl)C2=O 10.1016/j.bmcl.2015.12.104
CHEMBL3758228 144413 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human mGlu4 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu4 receptor by cell based calcium mobilization
ChEMBL 394 3 1 5 3.4 Cc1cccc2c1C(=O)N(c1ccc(NC(=O)c3nccn3C)cc1Cl)C2=O 10.1016/j.bmcl.2015.12.104
46836786 72325 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
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 298 2 2 6 2.9 Cc1ccnc(Nc2nc3c(s2)CCCc2n[nH]cc2-3)n1 10.1021/jm200290z
CHEMBL1830914 72325 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
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 298 2 2 6 2.9 Cc1ccnc(Nc2nc3c(s2)CCCc2n[nH]cc2-3)n1 10.1021/jm200290z
134191663 189100 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 330 2 2 5 3.7 FC(F)(F)c1nccc2cc(Nc3n[nH]c4nccnc34)ccc12 10.1016/j.bmcl.2018.10.050
CHEMBL4784310 189100 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 330 2 2 5 3.7 FC(F)(F)c1nccc2cc(Nc3n[nH]c4nccnc34)ccc12 10.1016/j.bmcl.2018.10.050
53373664 159231 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 224 2 2 3 3.0 Cc1cccc(Nc2n[nH]c3cccnc23)c1 nan
CHEMBL3970896 159231 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 224 2 2 3 3.0 Cc1cccc(Nc2n[nH]c3cccnc23)c1 nan
1410 9054 48 None -1 8 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity at rat recombinant mGluR4 expressed in BHK cellsAgonist activity at rat recombinant mGluR4 expressed in BHK cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmc.2007.02.040
1412 9054 48 None -1 8 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity at rat recombinant mGluR4 expressed in BHK cellsAgonist activity at rat recombinant mGluR4 expressed in BHK cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmc.2007.02.040
179394 9054 48 None -1 8 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity at rat recombinant mGluR4 expressed in BHK cellsAgonist activity at rat recombinant mGluR4 expressed in BHK cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmc.2007.02.040
57689795 9054 48 None -1 8 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity at rat recombinant mGluR4 expressed in BHK cellsAgonist activity at rat recombinant mGluR4 expressed in BHK cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmc.2007.02.040
CHEMBL33567 9054 48 None -1 8 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity at rat recombinant mGluR4 expressed in BHK cellsAgonist activity at rat recombinant mGluR4 expressed in BHK cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmc.2007.02.040
1410 9054 48 None -1 8 Rat 6.3 pEC50 = 6.3 Functional
Functional activity at rat mGluR4Functional activity at rat mGluR4
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmcl.2005.09.014
1412 9054 48 None -1 8 Rat 6.3 pEC50 = 6.3 Functional
Functional activity at rat mGluR4Functional activity at rat mGluR4
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmcl.2005.09.014
179394 9054 48 None -1 8 Rat 6.3 pEC50 = 6.3 Functional
Functional activity at rat mGluR4Functional activity at rat mGluR4
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmcl.2005.09.014
57689795 9054 48 None -1 8 Rat 6.3 pEC50 = 6.3 Functional
Functional activity at rat mGluR4Functional activity at rat mGluR4
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmcl.2005.09.014
CHEMBL33567 9054 48 None -1 8 Rat 6.3 pEC50 = 6.3 Functional
Functional activity at rat mGluR4Functional activity at rat mGluR4
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmcl.2005.09.014
137638288 163713 0 None 4 2 Human 5.3 pEC50 = 5.3 Functional
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 378 9 5 8 0.8 CCOc1cc([C@@H](O)P(=O)(O)CC[C@H](N)C(=O)O)cc([N+](=O)[O-])c1O 10.1021/acs.jmedchem.7b01438
CHEMBL4072587 163713 0 None 4 2 Human 5.3 pEC50 = 5.3 Functional
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 378 9 5 8 0.8 CCOc1cc([C@@H](O)P(=O)(O)CC[C@H](N)C(=O)O)cc([N+](=O)[O-])c1O 10.1021/acs.jmedchem.7b01438
24780084 14488 0 None 9 2 Rat 5.3 pEC50 = 5.3 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 281 7 5 5 -0.9 N[C@@H](CCP(=O)(O)C(O)C1CC1C(=O)O)C(=O)O 10.1021/jm901523t
CHEMBL1088873 14488 0 None 9 2 Rat 5.3 pEC50 = 5.3 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 281 7 5 5 -0.9 N[C@@H](CCP(=O)(O)C(O)C1CC1C(=O)O)C(=O)O 10.1021/jm901523t
CHEMBL1204419 14488 0 None 9 2 Rat 5.3 pEC50 = 5.3 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 281 7 5 5 -0.9 N[C@@H](CCP(=O)(O)C(O)C1CC1C(=O)O)C(=O)O 10.1021/jm901523t
70687778 81026 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 235 2 0 3 3.2 Cc1cnccc1-c1cnn(-c2ccccc2)c1 10.1016/j.bmcl.2012.03.032
CHEMBL2023634 81026 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 235 2 0 3 3.2 Cc1cnccc1-c1cnn(-c2ccccc2)c1 10.1016/j.bmcl.2012.03.032
134189978 177681 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 320 3 2 6 3.9 c1cnc2c(Nc3ccc4c(C5CCCC5)noc4c3)n[nH]c2n1 10.1021/acs.jmedchem.8b00994
CHEMBL4454698 177681 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 320 3 2 6 3.9 c1cnc2c(Nc3ccc4c(C5CCCC5)noc4c3)n[nH]c2n1 10.1021/acs.jmedchem.8b00994
122196121 131033 0 None -22 2 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 430 3 1 4 5.4 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c2ccccc12 10.1016/j.bmcl.2015.10.013
CHEMBL3634443 131033 0 None -22 2 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 430 3 1 4 5.4 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c2ccccc12 10.1016/j.bmcl.2015.10.013
134189978 177681 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 320 3 2 6 3.9 c1cnc2c(Nc3ccc4c(C5CCCC5)noc4c3)n[nH]c2n1 10.1021/acs.jmedchem.8b00994
CHEMBL4454698 177681 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 320 3 2 6 3.9 c1cnc2c(Nc3ccc4c(C5CCCC5)noc4c3)n[nH]c2n1 10.1021/acs.jmedchem.8b00994
46869941 64673 10 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 385 4 2 3 4.9 O=C(Nc1ccc(NC(=O)c2ccccc2Cl)c(Cl)c1)c1ccccn1 10.1021/jm101271s
CHEMBL1672238 64673 10 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 385 4 2 3 4.9 O=C(Nc1ccc(NC(=O)c2ccccc2Cl)c(Cl)c1)c1ccccn1 10.1021/jm101271s
51003324 64679 0 None -1 2 Rat 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 351 4 2 3 4.2 O=C(Nc1ccc(NC(=O)c2ccccn2)cc1Cl)c1ccccc1 10.1021/jm101271s
CHEMBL1672244 64679 0 None -1 2 Rat 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 351 4 2 3 4.2 O=C(Nc1ccc(NC(=O)c2ccccn2)cc1Cl)c1ccccc1 10.1021/jm101271s
127025549 144551 0 None -1 2 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human mGlu4 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu4 receptor by cell based calcium mobilization
ChEMBL 395 3 1 5 4.0 Cc1cccc2c1C(=O)N(c1ccc(NC(=O)c3ncoc3C)cc1Cl)C2=O 10.1016/j.bmcl.2015.12.104
CHEMBL3759424 144551 0 None -1 2 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human mGlu4 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu4 receptor by cell based calcium mobilization
ChEMBL 395 3 1 5 4.0 Cc1cccc2c1C(=O)N(c1ccc(NC(=O)c3ncoc3C)cc1Cl)C2=O 10.1016/j.bmcl.2015.12.104
46836872 7088 47 None 1 4 Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assay
ChEMBL 272 3 2 6 2.7 Cc1ccnc(n1)Nc1sc(c(n1)c1c[nH]nc1)C 10.1021/acsmedchemlett.7b00317
6238 7088 47 None 1 4 Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assay
ChEMBL 272 3 2 6 2.7 Cc1ccnc(n1)Nc1sc(c(n1)c1c[nH]nc1)C 10.1021/acsmedchemlett.7b00317
CHEMBL3609729 7088 47 None 1 4 Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assay
ChEMBL 272 3 2 6 2.7 Cc1ccnc(n1)Nc1sc(c(n1)c1c[nH]nc1)C 10.1021/acsmedchemlett.7b00317
122419163 179872 0 None 2 2 Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 414 3 2 6 4.2 O=C(c1nsc2cc(Nc3n[nH]c4cccnc34)ccc12)N1CCC(F)(F)CC1 10.1021/acs.jmedchem.8b00994
CHEMBL4520127 179872 0 None 2 2 Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 414 3 2 6 4.2 O=C(c1nsc2cc(Nc3n[nH]c4cccnc34)ccc12)N1CCC(F)(F)CC1 10.1021/acs.jmedchem.8b00994
122419163 179872 0 None 2 2 Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 414 3 2 6 4.2 O=C(c1nsc2cc(Nc3n[nH]c4cccnc34)ccc12)N1CCC(F)(F)CC1 10.1021/acs.jmedchem.8b00994
CHEMBL4520127 179872 0 None 2 2 Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 414 3 2 6 4.2 O=C(c1nsc2cc(Nc3n[nH]c4cccnc34)ccc12)N1CCC(F)(F)CC1 10.1021/acs.jmedchem.8b00994
1406 8854 38 None -22 7 Human 5.3 pEC50 = 5.3 Functional
Compound was evaluated for the inhibition of forskolin stimulated cAMP accumulation in CHO cells expressing hmGluR4aCompound was evaluated for the inhibition of forskolin stimulated cAMP accumulation in CHO cells expressing hmGluR4a
ChEMBL 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10.1016/s0960-894x(00)00197-9
4545574 8854 38 None -22 7 Human 5.3 pEC50 = 5.3 Functional
Compound was evaluated for the inhibition of forskolin stimulated cAMP accumulation in CHO cells expressing hmGluR4aCompound was evaluated for the inhibition of forskolin stimulated cAMP accumulation in CHO cells expressing hmGluR4a
ChEMBL 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10.1016/s0960-894x(00)00197-9
CHEMBL277475 8854 38 None -22 7 Human 5.3 pEC50 = 5.3 Functional
Compound was evaluated for the inhibition of forskolin stimulated cAMP accumulation in CHO cells expressing hmGluR4aCompound was evaluated for the inhibition of forskolin stimulated cAMP accumulation in CHO cells expressing hmGluR4a
ChEMBL 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10.1016/s0960-894x(00)00197-9
1406 8854 38 None -26 7 Rat 5.3 pEC50 = 5.3 Functional
Metabotropic glutamate receptor 4 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 4 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10.1021/jm030967o
4545574 8854 38 None -26 7 Rat 5.3 pEC50 = 5.3 Functional
Metabotropic glutamate receptor 4 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 4 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10.1021/jm030967o
CHEMBL277475 8854 38 None -26 7 Rat 5.3 pEC50 = 5.3 Functional
Metabotropic glutamate receptor 4 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 4 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10.1021/jm030967o
53373767 151443 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 258 3 2 3 3.6 CC(C)C1CCC(Nc2n[nH]c3cccnc23)CC1 nan
CHEMBL3908290 151443 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 258 3 2 3 3.6 CC(C)C1CCC(Nc2n[nH]c3cccnc23)CC1 nan
134190209 181958 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 321 5 2 5 4.7 CCC(CC)c1noc2cc(Nc3n[nH]c4ncccc34)ccc12 10.1021/acs.jmedchem.8b00994
CHEMBL4570505 181958 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 321 5 2 5 4.7 CCC(CC)c1noc2cc(Nc3n[nH]c4ncccc34)ccc12 10.1021/acs.jmedchem.8b00994
52934971 150665 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 380 4 1 6 2.6 O=C(Nc1cnn(S(=O)(=O)c2cccc(Cl)c2F)c1)c1ccccn1 nan
CHEMBL3901857 150665 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 380 4 1 6 2.6 O=C(Nc1cnn(S(=O)(=O)c2cccc(Cl)c2F)c1)c1ccccn1 nan
134190209 181958 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 321 5 2 5 4.7 CCC(CC)c1noc2cc(Nc3n[nH]c4ncccc34)ccc12 10.1021/acs.jmedchem.8b00994
CHEMBL4570505 181958 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 321 5 2 5 4.7 CCC(CC)c1noc2cc(Nc3n[nH]c4ncccc34)ccc12 10.1021/acs.jmedchem.8b00994
136353157 163721 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
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 443 6 2 7 4.0 CN1CCN(CCCNc2ccc3oc(-c4cc5ccccc5cn4)c/c(=N\O)c3c2)CC1 10.1021/acs.jmedchem.7b00991
CHEMBL4072639 163721 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
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 443 6 2 7 4.0 CN1CCN(CCCNc2ccc3oc(-c4cc5ccccc5cn4)c/c(=N\O)c3c2)CC1 10.1021/acs.jmedchem.7b00991
137635028 162783 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
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 470 4 2 9 4.9 O/N=c1\cc(-c2cc3sccc3cn2)oc2ccc(NC3CCN(c4ccncn4)CC3)cc12 10.1021/acs.jmedchem.7b00991
CHEMBL4061970 162783 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
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 470 4 2 9 4.9 O/N=c1\cc(-c2cc3sccc3cn2)oc2ccc(NC3CCN(c4ccncn4)CC3)cc12 10.1021/acs.jmedchem.7b00991
137646208 164404 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
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 407 3 1 7 3.6 CC(=O)N1CC(Oc2ccc3oc(-c4cc5sccc5cn4)c/c(=N\O)c3c2)C1 10.1021/acs.jmedchem.7b00991
CHEMBL4081211 164404 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
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 407 3 1 7 3.6 CC(=O)N1CC(Oc2ccc3oc(-c4cc5sccc5cn4)c/c(=N\O)c3c2)C1 10.1021/acs.jmedchem.7b00991
122197942 166846 0 None 34 4 Rat 6.3 pEC50 = 6.3 Functional
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 375 9 5 6 0.8 Cc1cc(C(O)P(=O)(O)CC[C@@H](N)C(=O)O)cc(C)c1OCC(=O)O nan
CHEMBL4108384 166846 0 None 34 4 Rat 6.3 pEC50 = 6.3 Functional
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 375 9 5 6 0.8 Cc1cc(C(O)P(=O)(O)CC[C@@H](N)C(=O)O)cc(C)c1OCC(=O)O nan
53373999 153429 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 230 3 2 3 3.0 c1cnc2c(NCC3CCCCC3)n[nH]c2c1 nan
CHEMBL3923616 153429 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 230 3 2 3 3.0 c1cnc2c(NCC3CCCCC3)n[nH]c2c1 nan
51003373 74582 0 None -1 2 Rat 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 358 4 2 5 3.7 O=C(Nc1ccc(NC(=O)c2nccs2)c(Cl)c1)c1ccccn1 10.1021/jm101271s
CHEMBL1909434 74582 0 None -1 2 Rat 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 358 4 2 5 3.7 O=C(Nc1ccc(NC(=O)c2nccs2)c(Cl)c1)c1ccccn1 10.1021/jm101271s
54670686 157891 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 425 5 1 6 3.9 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1cccc(Cl)c1F nan
CHEMBL3959217 157891 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 425 5 1 6 3.9 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1cccc(Cl)c1F nan
58058384 163705 0 None 4 2 Human 6.3 pEC50 = 6.3 Functional
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 317 7 4 6 0.6 NC(c1cccc([N+](=O)[O-])c1)P(=O)(O)CC[C@H](N)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4072409 163705 0 None 4 2 Human 6.3 pEC50 = 6.3 Functional
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 317 7 4 6 0.6 NC(c1cccc([N+](=O)[O-])c1)P(=O)(O)CC[C@H](N)C(=O)O 10.1021/acs.jmedchem.7b01438
46918013 165508 0 None 2 3 Human 6.3 pEC50 = 6.3 Functional
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 318 7 4 6 0.7 N[C@@H](CCP(=O)(O)C(O)c1cccc([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4093492 165508 0 None 2 3 Human 6.3 pEC50 = 6.3 Functional
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 318 7 4 6 0.7 N[C@@H](CCP(=O)(O)C(O)c1cccc([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
70691951 80992 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 315 4 0 4 4.5 CCOc1ccc2c(-c3cnn(-c4ccccc4)c3)ccnc2c1 10.1016/j.bmcl.2012.03.032
CHEMBL2023459 80992 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 315 4 0 4 4.5 CCOc1ccc2c(-c3cnn(-c4ccccc4)c3)ccnc2c1 10.1016/j.bmcl.2012.03.032
54670223 147284 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 409 5 1 6 3.4 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccc(F)cc1F 10.1016/j.bmcl.2016.05.029
CHEMBL3810046 147284 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 409 5 1 6 3.4 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccc(F)cc1F 10.1016/j.bmcl.2016.05.029
54670223 147284 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 409 5 1 6 3.4 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccc(F)cc1F 10.1016/j.bmcl.2016.05.029
CHEMBL3810046 147284 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 409 5 1 6 3.4 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccc(F)cc1F 10.1016/j.bmcl.2016.05.029
70694003 80989 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 339 2 0 3 5.1 FC(F)(F)c1ccc2c(-c3cnn(-c4ccccc4)c3)ccnc2c1 10.1016/j.bmcl.2012.03.032
CHEMBL2023455 80989 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 339 2 0 3 5.1 FC(F)(F)c1ccc2c(-c3cnn(-c4ccccc4)c3)ccnc2c1 10.1016/j.bmcl.2012.03.032
53373661 154023 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 245 2 2 4 2.8 Clc1ccc(Nc2n[nH]c3cccnc23)cn1 nan
CHEMBL3928501 154023 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 245 2 2 4 2.8 Clc1ccc(Nc2n[nH]c3cccnc23)cn1 nan
46869942 64676 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 369 4 2 3 4.4 O=C(Nc1ccc(NC(=O)c2ccccc2Cl)c(F)c1)c1ccccn1 10.1021/jm101271s
CHEMBL1672241 64676 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 369 4 2 3 4.4 O=C(Nc1ccc(NC(=O)c2ccccc2Cl)c(F)c1)c1ccccn1 10.1021/jm101271s
42644808 72297 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
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 257 3 2 5 3.0 Cc1n[nH]cc1-c1csc(Nc2ccccn2)n1 10.1021/jm200290z
CHEMBL1830695 72297 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
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 257 3 2 5 3.0 Cc1n[nH]cc1-c1csc(Nc2ccccn2)n1 10.1021/jm200290z
44191178 203038 0 None -2 2 Human 6.3 pEC50 = 6.3 Functional
Activity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilizationActivity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilization
ChEMBL 242 3 1 3 2.7 COc1cc(NC(=O)c2ccccn2)ccc1C 10.1021/jm9005065
CHEMBL561835 203038 0 None -2 2 Human 6.3 pEC50 = 6.3 Functional
Activity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilizationActivity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilization
ChEMBL 242 3 1 3 2.7 COc1cc(NC(=O)c2ccccn2)ccc1C 10.1021/jm9005065
24780225 162712 0 None 2 3 Human 5.3 pEC50 = 5.3 Functional
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 363 6 4 4 1.4 N[C@@H](CCP(=O)(O)C(O)c1c(F)c(F)c(F)c(F)c1F)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4061016 162712 0 None 2 3 Human 5.3 pEC50 = 5.3 Functional
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 363 6 4 4 1.4 N[C@@H](CCP(=O)(O)C(O)c1c(F)c(F)c(F)c(F)c1F)C(=O)O 10.1021/acs.jmedchem.7b01438
46869941 64673 10 None -1 2 Rat 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 385 4 2 3 4.9 O=C(Nc1ccc(NC(=O)c2ccccc2Cl)c(Cl)c1)c1ccccn1 10.1021/jm101271s
CHEMBL1672238 64673 10 None -1 2 Rat 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 385 4 2 3 4.9 O=C(Nc1ccc(NC(=O)c2ccccc2Cl)c(Cl)c1)c1ccccn1 10.1021/jm101271s
52913768 147254 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 359 5 1 5 2.7 O=C(Nc1ccn(S(=O)(=O)Cc2cccc(F)c2)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
CHEMBL3809562 147254 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 359 5 1 5 2.7 O=C(Nc1ccn(S(=O)(=O)Cc2cccc(F)c2)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
134190246 181121 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 293 3 2 5 4.0 CC(C)c1noc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
CHEMBL4551081 181121 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 293 3 2 5 4.0 CC(C)c1noc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
52913768 147254 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 359 5 1 5 2.7 O=C(Nc1ccn(S(=O)(=O)Cc2cccc(F)c2)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
CHEMBL3809562 147254 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 359 5 1 5 2.7 O=C(Nc1ccn(S(=O)(=O)Cc2cccc(F)c2)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
134190246 181121 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 293 3 2 5 4.0 CC(C)c1noc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
CHEMBL4551081 181121 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 293 3 2 5 4.0 CC(C)c1noc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
113447561 146382 1 None - 1 Human 6.2 pEC50 = 6.2 Functional
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 247 2 2 3 2.6 Nc1cccnc1C(=O)Nc1cccc(Cl)c1 10.1016/j.bmcl.2016.04.041
CHEMBL3797449 146382 1 None - 1 Human 6.2 pEC50 = 6.2 Functional
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 247 2 2 3 2.6 Nc1cccnc1C(=O)Nc1cccc(Cl)c1 10.1016/j.bmcl.2016.04.041
122196104 131017 0 None -10 2 Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 428 3 1 4 5.0 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c(C(F)(F)F)c1 10.1016/j.bmcl.2015.10.013
CHEMBL3634427 131017 0 None -10 2 Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 428 3 1 4 5.0 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c(C(F)(F)F)c1 10.1016/j.bmcl.2015.10.013
14842361 175969 1 None -4 2 Human 6.2 pEC50 = 6.2 Functional
Effective concentration which exhibit agonistic activity at metabotropic glutamate 4 receptor stably expressed in AV12 cellsEffective concentration which exhibit agonistic activity at metabotropic glutamate 4 receptor stably expressed in AV12 cells
ChEMBL 195 3 4 3 -1.0 NC1(C(=O)O)CC1CP(=O)(O)O 10.1016/j.bmcl.2004.10.040
CHEMBL440648 175969 1 None -4 2 Human 6.2 pEC50 = 6.2 Functional
Effective concentration which exhibit agonistic activity at metabotropic glutamate 4 receptor stably expressed in AV12 cellsEffective concentration which exhibit agonistic activity at metabotropic glutamate 4 receptor stably expressed in AV12 cells
ChEMBL 195 3 4 3 -1.0 NC1(C(=O)O)CC1CP(=O)(O)O 10.1016/j.bmcl.2004.10.040
14590355 21872 5 None - 1 Human 5.2 pEC50 = 5.2 Functional
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 196 2 1 2 2.8 Nc1cccc(/C=C/c2ccccc2)n1 10.1016/j.bmcl.2010.06.078
CHEMBL1209588 21872 5 None - 1 Human 5.2 pEC50 = 5.2 Functional
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 196 2 1 2 2.8 Nc1cccc(/C=C/c2ccccc2)n1 10.1016/j.bmcl.2010.06.078
53375081 150092 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 228 2 2 3 2.8 Fc1cccc(Nc2n[nH]c3cccnc23)c1 nan
CHEMBL3897174 150092 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 228 2 2 3 2.8 Fc1cccc(Nc2n[nH]c3cccnc23)c1 nan
113447561 146382 1 None - 1 Human 6.2 pEC50 = 6.2 Functional
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 247 2 2 3 2.6 Nc1cccnc1C(=O)Nc1cccc(Cl)c1 10.1016/j.bmcl.2016.04.041
CHEMBL3797449 146382 1 None - 1 Human 6.2 pEC50 = 6.2 Functional
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 247 2 2 3 2.6 Nc1cccnc1C(=O)Nc1cccc(Cl)c1 10.1016/j.bmcl.2016.04.041
45110131 66599 2 None 1 2 Human 7.2 pEC50 = 7.2 Functional
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 377 3 1 4 3.8 O=C(Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1)c1ccccn1 10.1021/jm200956q
CHEMBL1727966 66599 2 None 1 2 Human 7.2 pEC50 = 7.2 Functional
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 377 3 1 4 3.8 O=C(Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1)c1ccccn1 10.1021/jm200956q
70687763 80990 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 305 2 0 3 4.7 Clc1ccc2c(-c3cnn(-c4ccccc4)c3)ccnc2c1 10.1016/j.bmcl.2012.03.032
CHEMBL2023456 80990 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 305 2 0 3 4.7 Clc1ccc2c(-c3cnn(-c4ccccc4)c3)ccnc2c1 10.1016/j.bmcl.2012.03.032
24780092 165610 0 None - 1 Human 4.2 pEC50 = 4.2 Functional
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 351 7 4 6 0.2 CS(=O)(=O)c1ccc(C(O)P(=O)(O)CC[C@H](N)C(=O)O)cc1 10.1021/acs.jmedchem.7b01438
CHEMBL4094636 165610 0 None - 1 Human 4.2 pEC50 = 4.2 Functional
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 351 7 4 6 0.2 CS(=O)(=O)c1ccc(C(O)P(=O)(O)CC[C@H](N)C(=O)O)cc1 10.1021/acs.jmedchem.7b01438
16739372 153508 0 None -1 2 Rat 4.2 pEC50 = 4.2 Functional
Agonist activity at rat recombinant mGluR4 expressed in BHK cellsAgonist activity at rat recombinant mGluR4 expressed in BHK cells
ChEMBL 271 4 4 3 0.4 NC(C(=O)O)[C@@H]1[C@@H](P(=O)(O)O)[C@H]1c1ccccc1 10.1016/j.bmc.2007.02.040
CHEMBL392420 153508 0 None -1 2 Rat 4.2 pEC50 = 4.2 Functional
Agonist activity at rat recombinant mGluR4 expressed in BHK cellsAgonist activity at rat recombinant mGluR4 expressed in BHK cells
ChEMBL 271 4 4 3 0.4 NC(C(=O)O)[C@@H]1[C@@H](P(=O)(O)O)[C@H]1c1ccccc1 10.1016/j.bmc.2007.02.040
51003284 64678 0 None -1 2 Rat 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 357 4 2 3 4.5 O=C(Nc1ccc(NC(=O)C2CCCCC2)c(Cl)c1)c1ccccn1 10.1021/jm101271s
CHEMBL1672243 64678 0 None -1 2 Rat 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 357 4 2 3 4.5 O=C(Nc1ccc(NC(=O)C2CCCCC2)c(Cl)c1)c1ccccn1 10.1021/jm101271s
6348408 14592 1 None 1 8 Human 5.2 pEC50 = 5.2 Functional
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 239 7 4 4 -0.5 N[C@@H](CCP(=O)(O)CCC(=O)O)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL1089515 14592 1 None 1 8 Human 5.2 pEC50 = 5.2 Functional
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 239 7 4 4 -0.5 N[C@@H](CCP(=O)(O)CCC(=O)O)C(=O)O 10.1021/acs.jmedchem.7b01438
1012759 22613 16 None - 1 Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilization
ChEMBL 384 5 2 4 4.3 Cc1cc(C)c(NS(=O)(=O)c2ccc(NC(=O)c3ccco3)cc2)c(C)c1 10.1016/j.bmcl.2010.07.007
CHEMBL1223013 22613 16 None - 1 Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilization
ChEMBL 384 5 2 4 4.3 Cc1cc(C)c(NS(=O)(=O)c2ccc(NC(=O)c3ccco3)cc2)c(C)c1 10.1016/j.bmcl.2010.07.007
53373875 160044 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 263 2 2 4 2.9 Fc1ncc(Cl)cc1Nc1n[nH]c2cccnc12 nan
CHEMBL3977654 160044 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 263 2 2 4 2.9 Fc1ncc(Cl)cc1Nc1n[nH]c2cccnc12 nan
137656701 166573 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
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 449 4 1 7 4.6 CC(=O)N1CCC(COc2ccc3oc(-c4cc5sccc5cn4)c/c(=N\O)c3c2)CC1 10.1021/acs.jmedchem.7b00991
CHEMBL4105462 166573 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
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 449 4 1 7 4.6 CC(=O)N1CCC(COc2ccc3oc(-c4cc5sccc5cn4)c/c(=N\O)c3c2)CC1 10.1021/acs.jmedchem.7b00991
122197950 167092 0 None 32 3 Rat 7.2 pEC50 = 7.2 Functional
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 431 10 5 7 1.1 N[C@H](CCP(=O)(O)C(O)c1ccc(OCC(=O)O)c(OC(F)(F)F)c1)C(=O)O nan
CHEMBL4110560 167092 0 None 32 3 Rat 7.2 pEC50 = 7.2 Functional
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 431 10 5 7 1.1 N[C@H](CCP(=O)(O)C(O)c1ccc(OCC(=O)O)c(OC(F)(F)F)c1)C(=O)O nan
137631968 163294 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
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 490 5 1 8 4.9 CN1CCCC12CCN(CCOc1ccc3oc(-c4cc5sccc5cn4)c/c(=N\O)c3c1)CC2 10.1021/acs.jmedchem.7b00991
CHEMBL4067872 163294 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
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 490 5 1 8 4.9 CN1CCCC12CCN(CCOc1ccc3oc(-c4cc5sccc5cn4)c/c(=N\O)c3c1)CC2 10.1021/acs.jmedchem.7b00991
57765613 165269 0 None 1 3 Human 6.2 pEC50 = 6.2 Functional
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 336 7 4 6 0.8 N[C@@H](CCP(=O)(O)C(O)c1ccc(F)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4091029 165269 0 None 1 3 Human 6.2 pEC50 = 6.2 Functional
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 336 7 4 6 0.8 N[C@@H](CCP(=O)(O)C(O)c1ccc(F)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
46918013 165508 0 None 2 3 Human 6.2 pEC50 = 6.2 Functional
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(O)c1cccc([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4093492 165508 0 None 2 3 Human 6.2 pEC50 = 6.2 Functional
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(O)c1cccc([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
53388196 72324 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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 326 4 3 6 3.6 CCNc1cccc(Nc2nc3c(s2)CCCc2n[nH]cc2-3)n1 10.1021/jm200290z
CHEMBL1830912 72324 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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 326 4 3 6 3.6 CCNc1cccc(Nc2nc3c(s2)CCCc2n[nH]cc2-3)n1 10.1021/jm200290z
49862526 21857 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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 265 2 1 3 3.2 Nc1nc(/C=C/c2ccccc2)cc(C(F)(F)F)n1 10.1016/j.bmcl.2010.06.078
CHEMBL1209519 21857 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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 265 2 1 3 3.2 Nc1nc(/C=C/c2ccccc2)cc(C(F)(F)F)n1 10.1016/j.bmcl.2010.06.078
70691954 80997 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 398 6 0 5 5.0 c1ccc(-n2cc(-c3ccnc4cc(OCCN5CCCCC5)ccc34)cn2)cc1 10.1016/j.bmcl.2012.03.032
CHEMBL2023469 80997 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 398 6 0 5 5.0 c1ccc(-n2cc(-c3ccnc4cc(OCCN5CCCCC5)ccc34)cn2)cc1 10.1016/j.bmcl.2012.03.032
127025564 144568 0 None -2 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human mGlu4 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu4 receptor by cell based calcium mobilization
ChEMBL 394 3 1 5 3.4 Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3nccn3C)cc1Cl)C2=O 10.1016/j.bmcl.2015.12.104
CHEMBL3759555 144568 0 None -2 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human mGlu4 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu4 receptor by cell based calcium mobilization
ChEMBL 394 3 1 5 3.4 Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3nccn3C)cc1Cl)C2=O 10.1016/j.bmcl.2015.12.104
122196125 131037 0 None -40 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 360 3 1 4 3.9 Cc1cc(N2C(=O)c3ccccc3C2=O)ccc1NC(=O)c1occc1C 10.1016/j.bmcl.2015.10.013
CHEMBL3634447 131037 0 None -40 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 360 3 1 4 3.9 Cc1cc(N2C(=O)c3ccccc3C2=O)ccc1NC(=O)c1occc1C 10.1016/j.bmcl.2015.10.013
52914664 147160 4 None - 1 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 355 4 1 5 3.0 Cc1ccc(S(=O)(=O)n2ccc(NC(=O)c3ccccn3)c2)cc1C 10.1016/j.bmcl.2016.05.029
CHEMBL3808555 147160 4 None - 1 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 355 4 1 5 3.0 Cc1ccc(S(=O)(=O)n2ccc(NC(=O)c3ccccn3)c2)cc1C 10.1016/j.bmcl.2016.05.029
137638200 163596 0 None 6 2 Human 5.2 pEC50 = 5.2 Functional
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 429 15 4 6 3.6 CCCCCCCCNC(c1cccc([N+](=O)[O-])c1)P(=O)(O)CC[C@H](N)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4071200 163596 0 None 6 2 Human 5.2 pEC50 = 5.2 Functional
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 429 15 4 6 3.6 CCCCCCCCNC(c1cccc([N+](=O)[O-])c1)P(=O)(O)CC[C@H](N)C(=O)O 10.1021/acs.jmedchem.7b01438
1310 9095 110 None -426 17 Rat 5.2 pEC50 = 5.2 Functional
Agonist activity at rat recombinant mGluR4 expressed in BHK cellsAgonist activity at rat recombinant mGluR4 expressed in BHK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2007.02.040
1369 9095 110 None -426 17 Rat 5.2 pEC50 = 5.2 Functional
Agonist activity at rat recombinant mGluR4 expressed in BHK cellsAgonist activity at rat recombinant mGluR4 expressed in BHK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2007.02.040
33032 9095 110 None -426 17 Rat 5.2 pEC50 = 5.2 Functional
Agonist activity at rat recombinant mGluR4 expressed in BHK cellsAgonist activity at rat recombinant mGluR4 expressed in BHK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2007.02.040
44272391 9095 110 None -426 17 Rat 5.2 pEC50 = 5.2 Functional
Agonist activity at rat recombinant mGluR4 expressed in BHK cellsAgonist activity at rat recombinant mGluR4 expressed in BHK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2007.02.040
88747398 9095 110 None -426 17 Rat 5.2 pEC50 = 5.2 Functional
Agonist activity at rat recombinant mGluR4 expressed in BHK cellsAgonist activity at rat recombinant mGluR4 expressed in BHK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2007.02.040
CHEMBL575060 9095 110 None -426 17 Rat 5.2 pEC50 = 5.2 Functional
Agonist activity at rat recombinant mGluR4 expressed in BHK cellsAgonist activity at rat recombinant mGluR4 expressed in BHK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2007.02.040
DB00142 9095 110 None -426 17 Rat 5.2 pEC50 = 5.2 Functional
Agonist activity at rat recombinant mGluR4 expressed in BHK cellsAgonist activity at rat recombinant mGluR4 expressed in BHK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2007.02.040
1310 9095 110 None -426 17 Rat 5.2 pEC50 = 5.2 Functional
Functional activity at rat mGluR4Functional activity at rat mGluR4
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2005.09.014
1369 9095 110 None -426 17 Rat 5.2 pEC50 = 5.2 Functional
Functional activity at rat mGluR4Functional activity at rat mGluR4
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2005.09.014
33032 9095 110 None -426 17 Rat 5.2 pEC50 = 5.2 Functional
Functional activity at rat mGluR4Functional activity at rat mGluR4
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2005.09.014
44272391 9095 110 None -426 17 Rat 5.2 pEC50 = 5.2 Functional
Functional activity at rat mGluR4Functional activity at rat mGluR4
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2005.09.014
88747398 9095 110 None -426 17 Rat 5.2 pEC50 = 5.2 Functional
Functional activity at rat mGluR4Functional activity at rat mGluR4
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2005.09.014
CHEMBL575060 9095 110 None -426 17 Rat 5.2 pEC50 = 5.2 Functional
Functional activity at rat mGluR4Functional activity at rat mGluR4
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2005.09.014
DB00142 9095 110 None -426 17 Rat 5.2 pEC50 = 5.2 Functional
Functional activity at rat mGluR4Functional activity at rat mGluR4
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2005.09.014
6348408 14592 1 None -1 8 Rat 5.2 pEC50 = 5.2 Functional
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 239 7 4 4 -0.5 N[C@@H](CCP(=O)(O)CCC(=O)O)C(=O)O 10.1021/jm901523t
CHEMBL1089515 14592 1 None -1 8 Rat 5.2 pEC50 = 5.2 Functional
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 239 7 4 4 -0.5 N[C@@H](CCP(=O)(O)CCC(=O)O)C(=O)O 10.1021/jm901523t
122193173 130706 0 None -25 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of human mGlu4 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay
ChEMBL 394 3 1 4 4.6 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
CHEMBL3628109 130706 0 None -25 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of human mGlu4 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay
ChEMBL 394 3 1 4 4.6 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
52914664 147160 4 None - 1 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 355 4 1 5 3.0 Cc1ccc(S(=O)(=O)n2ccc(NC(=O)c3ccccn3)c2)cc1C 10.1016/j.bmcl.2016.05.029
CHEMBL3808555 147160 4 None - 1 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 355 4 1 5 3.0 Cc1ccc(S(=O)(=O)n2ccc(NC(=O)c3ccccn3)c2)cc1C 10.1016/j.bmcl.2016.05.029
122193173 130706 0 None -25 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of human mGlu4 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay
ChEMBL 394 3 1 4 4.6 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
CHEMBL3628109 130706 0 None -25 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of human mGlu4 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay
ChEMBL 394 3 1 4 4.6 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
122197965 166628 0 None 6 2 Rat 5.2 pEC50 = 5.2 Functional
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 395 10 4 6 1.4 COc1cc(CP(=O)(O)CC[C@@H](N)C(=O)O)cc(Cl)c1OCC(=O)O nan
CHEMBL4106594 166628 0 None 6 2 Rat 5.2 pEC50 = 5.2 Functional
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 395 10 4 6 1.4 COc1cc(CP(=O)(O)CC[C@@H](N)C(=O)O)cc(Cl)c1OCC(=O)O nan
127026474 144546 0 None -9 2 Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of human mGlu4 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu4 receptor by cell based calcium mobilization
ChEMBL 398 3 2 4 3.6 Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3759376 144546 0 None -9 2 Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of human mGlu4 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu4 receptor by cell based calcium mobilization
ChEMBL 398 3 2 4 3.6 Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
46869943 66086 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
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 329 3 1 4 2.6 O=C(Nc1ccc(N2C(=O)CCC2=O)c(Cl)c1)c1ccccn1 10.1021/jm200956q
CHEMBL1705559 66086 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
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 329 3 1 4 2.6 O=C(Nc1ccc(N2C(=O)CCC2=O)c(Cl)c1)c1ccccn1 10.1021/jm200956q
53373663 154520 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 262 2 2 3 3.5 Fc1c(Cl)cccc1Nc1n[nH]c2cccnc12 nan
CHEMBL3932339 154520 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 262 2 2 3 3.5 Fc1c(Cl)cccc1Nc1n[nH]c2cccnc12 nan
122197963 167461 0 None - 1 Rat 4.2 pEC50 = 4.2 Functional
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 399 9 4 5 1.7 N[C@H](CCP(=O)(O)Cc1ccc(OCC(=O)O)c(C(F)(F)F)c1)C(=O)O nan
CHEMBL4113484 167461 0 None - 1 Rat 4.2 pEC50 = 4.2 Functional
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 399 9 4 5 1.7 N[C@H](CCP(=O)(O)Cc1ccc(OCC(=O)O)c(C(F)(F)F)c1)C(=O)O nan
51003231 64667 0 None -1 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 387 5 2 5 4.3 COc1cc(NC(=O)c2nccs2)ccc1NC(=O)c1ccccc1Cl 10.1021/jm101271s
CHEMBL1672232 64667 0 None -1 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 387 5 2 5 4.3 COc1cc(NC(=O)c2nccs2)ccc1NC(=O)c1ccccc1Cl 10.1021/jm101271s
134191590 189310 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 327 3 2 6 3.4 c1cnc2c(Nc3ccc4c(-n5cccn5)nccc4c3)n[nH]c2c1 10.1016/j.bmcl.2018.10.050
CHEMBL4787268 189310 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 327 3 2 6 3.4 c1cnc2c(Nc3ccc4c(-n5cccn5)nccc4c3)n[nH]c2c1 10.1016/j.bmcl.2018.10.050
53373764 159539 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 243 2 2 2 4.0 Clc1cccc(Nc2c[nH]c3cccnc23)c1 nan
CHEMBL3973444 159539 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 243 2 2 2 4.0 Clc1cccc(Nc2c[nH]c3cccnc23)c1 nan
127047647 146537 0 None 22 2 Human 7.2 pEC50 = 7.2 Functional
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 146537 0 None 22 2 Human 7.2 pEC50 = 7.2 Functional
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
57765536 165050 0 None 1 3 Human 6.2 pEC50 = 6.2 Functional
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(O)c1ccc([N+](=O)[O-])cc1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4088782 165050 0 None 1 3 Human 6.2 pEC50 = 6.2 Functional
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(O)c1ccc([N+](=O)[O-])cc1)C(=O)O 10.1021/acs.jmedchem.7b01438
70687764 80993 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 377 5 0 4 5.7 c1ccc(COc2ccc3c(-c4cnn(-c5ccccc5)c4)ccnc3c2)cc1 10.1016/j.bmcl.2012.03.032
CHEMBL2023460 80993 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 377 5 0 4 5.7 c1ccc(COc2ccc3c(-c4cnn(-c5ccccc5)c4)ccnc3c2)cc1 10.1016/j.bmcl.2012.03.032
6348408 14592 1 None 1 8 Human 5.2 pEC50 = 5.2 Functional
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 239 7 4 4 -0.5 N[C@@H](CCP(=O)(O)CCC(=O)O)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL1089515 14592 1 None 1 8 Human 5.2 pEC50 = 5.2 Functional
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 239 7 4 4 -0.5 N[C@@H](CCP(=O)(O)CCC(=O)O)C(=O)O 10.1021/acs.jmedchem.7b01438
137632643 163196 0 None 1 2 Human 5.2 pEC50 = 5.2 Functional
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 378 9 5 8 0.8 CCOc1cc([C@H](O)P(=O)(O)CC[C@H](N)C(=O)O)cc([N+](=O)[O-])c1O 10.1021/acs.jmedchem.7b01438
CHEMBL4066711 163196 0 None 1 2 Human 5.2 pEC50 = 5.2 Functional
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 378 9 5 8 0.8 CCOc1cc([C@H](O)P(=O)(O)CC[C@H](N)C(=O)O)cc([N+](=O)[O-])c1O 10.1021/acs.jmedchem.7b01438
6348408 14592 1 None -1 8 Rat 5.2 pEC50 = 5.2 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 239 7 4 4 -0.5 N[C@@H](CCP(=O)(O)CCC(=O)O)C(=O)O 10.1021/jm901523t
CHEMBL1089515 14592 1 None -1 8 Rat 5.2 pEC50 = 5.2 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 239 7 4 4 -0.5 N[C@@H](CCP(=O)(O)CCC(=O)O)C(=O)O 10.1021/jm901523t
44189736 201658 2 None - 1 Human 5.2 pEC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Modulation of the Metabotropic Glutamate Receptor mGluR4: Calcium Assay. (Class of assay: confirmatory) [Related pubchem assays: 2180, 2199, 2193, 2179, 2182, 2183, 2191, 2181, 2190, 2188, 2185, 2197 ]PUBCHEM_BIOASSAY: Modulation of the Metabotropic Glutamate Receptor mGluR4: Calcium Assay. (Class of assay: confirmatory) [Related pubchem assays: 2180, 2199, 2193, 2179, 2182, 2183, 2191, 2181, 2190, 2188, 2185, 2197 ]
ChEMBL 263 3 1 4 2.4 COc1nc(NC(=O)c2ccccn2)ccc1Cl nan
CHEMBL540427 201658 2 None - 1 Human 5.2 pEC50 = 5.2 Functional
PUBCHEM_BIOASSAY: Modulation of the Metabotropic Glutamate Receptor mGluR4: Calcium Assay. (Class of assay: confirmatory) [Related pubchem assays: 2180, 2199, 2193, 2179, 2182, 2183, 2191, 2181, 2190, 2188, 2185, 2197 ]PUBCHEM_BIOASSAY: Modulation of the Metabotropic Glutamate Receptor mGluR4: Calcium Assay. (Class of assay: confirmatory) [Related pubchem assays: 2180, 2199, 2193, 2179, 2182, 2183, 2191, 2181, 2190, 2188, 2185, 2197 ]
ChEMBL 263 3 1 4 2.4 COc1nc(NC(=O)c2ccccn2)ccc1Cl nan
46853778 75564 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
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 427 4 1 6 3.1 O=S1(=O)c2ccccc2S(=O)(=O)N1c1ccc(NC2(c3ccccn3)CC2)cc1 10.1021/jm200956q
CHEMBL1921956 75564 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
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 427 4 1 6 3.1 O=S1(=O)c2ccccc2S(=O)(=O)N1c1ccc(NC2(c3ccccn3)CC2)cc1 10.1021/jm200956q
127025831 144547 0 None -4 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human mGlu4 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu4 receptor by cell based calcium mobilization
ChEMBL 399 3 1 5 3.8 Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3759381 144547 0 None -4 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human mGlu4 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu4 receptor by cell based calcium mobilization
ChEMBL 399 3 1 5 3.8 Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
69938272 152896 2 None - 1 Human 6.2 pEC50 = 6.2 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 246 2 2 3 3.0 Fc1ccc(Nc2n[nH]c3cccnc23)cc1F nan
CHEMBL3919518 152896 2 None - 1 Human 6.2 pEC50 = 6.2 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 246 2 2 3 3.0 Fc1ccc(Nc2n[nH]c3cccnc23)cc1F nan
53373998 149898 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 274 3 3 5 2.8 CNc1ncc(Nc2n[nH]c3cccnc23)cc1Cl nan
CHEMBL3895620 149898 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 274 3 3 5 2.8 CNc1ncc(Nc2n[nH]c3cccnc23)cc1Cl nan
122196109 130853 0 None -36 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 410 4 1 5 4.3 COc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(Cl)c2C1=O 10.1016/j.bmcl.2015.10.013
CHEMBL3632642 130853 0 None -36 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 410 4 1 5 4.3 COc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(Cl)c2C1=O 10.1016/j.bmcl.2015.10.013
135126262 176362 0 None -7 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 385 3 1 5 3.1 Cc1nnc2ccc(C(=O)NC3CN(c4ncc(Cl)cc4F)C3)cc2c1C 10.1016/j.bmcl.2019.126678
CHEMBL4436022 176362 0 None -7 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 385 3 1 5 3.1 Cc1nnc2ccc(C(=O)NC3CN(c4ncc(Cl)cc4F)C3)cc2c1C 10.1016/j.bmcl.2019.126678
46836714 72301 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
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 270 2 2 6 2.2 c1cnc(Nc2nc3c(s2)CCc2n[nH]cc2-3)nc1 10.1021/jm200290z
CHEMBL1830702 72301 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
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 270 2 2 6 2.2 c1cnc(Nc2nc3c(s2)CCc2n[nH]cc2-3)nc1 10.1021/jm200290z
162674997 190169 0 None -1 3 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 412 3 1 4 4.7 Cc1cc(N2C(=O)c3cccc(Cl)c3C2=O)c(F)cc1NC(=O)c1occc1C 10.1016/j.bmcl.2020.127724
CHEMBL4798021 190169 0 None -1 3 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 412 3 1 4 4.7 Cc1cc(N2C(=O)c3cccc(Cl)c3C2=O)c(F)cc1NC(=O)c1occc1C 10.1016/j.bmcl.2020.127724
10135 10826 21 None 3 2 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 329 2 2 4 4.3 FC(c1nccc2c1ccc(c2)Nc1n[nH]c2c1cccn2)(F)F 10.1016/j.bmcl.2018.10.050
134191471 10826 21 None 3 2 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 329 2 2 4 4.3 FC(c1nccc2c1ccc(c2)Nc1n[nH]c2c1cccn2)(F)F 10.1016/j.bmcl.2018.10.050
CHEMBL4797139 10826 21 None 3 2 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 329 2 2 4 4.3 FC(c1nccc2c1ccc(c2)Nc1n[nH]c2c1cccn2)(F)F 10.1016/j.bmcl.2018.10.050
46836635 72318 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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 313 3 2 6 3.2 COc1cccc(Nc2nc3c(s2)CCCc2n[nH]cc2-3)n1 10.1021/jm200290z
CHEMBL1830905 72318 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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 313 3 2 6 3.2 COc1cccc(Nc2nc3c(s2)CCCc2n[nH]cc2-3)n1 10.1021/jm200290z
137644345 164897 0 None 3 3 Human 5.2 pEC50 = 5.2 Functional
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 303 7 4 5 0.8 COc1ccc(C(O)P(=O)(O)CC[C@H](N)C(=O)O)cc1 10.1021/acs.jmedchem.7b01438
CHEMBL4086929 164897 0 None 3 3 Human 5.2 pEC50 = 5.2 Functional
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 303 7 4 5 0.8 COc1ccc(C(O)P(=O)(O)CC[C@H](N)C(=O)O)cc1 10.1021/acs.jmedchem.7b01438
52934967 152186 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 362 4 1 7 2.4 Cc1ccc(S(=O)(=O)n2cc(NC(=O)c3nccs3)cn2)cc1C nan
CHEMBL3914010 152186 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 362 4 1 7 2.4 Cc1ccc(S(=O)(=O)n2cc(NC(=O)c3nccs3)cn2)cc1C nan
134198074 172647 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 361 4 3 6 2.9 Cn1nc(C(=O)NC2CCC2)c2ccc(Nc3n[nH]c4cccnc34)cc21 10.1016/j.bmcl.2018.06.034
CHEMBL4249226 172647 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 361 4 3 6 2.9 Cn1nc(C(=O)NC2CCC2)c2ccc(Nc3n[nH]c4cccnc34)cc21 10.1016/j.bmcl.2018.06.034
162655927 187506 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 345 4 2 5 3.8 O=c1c2ccc(Nc3n[nH]c4cccnc34)cc2ccn1CC1CCC1 10.1016/j.bmcl.2018.10.050
CHEMBL4755785 187506 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 345 4 2 5 3.8 O=c1c2ccc(Nc3n[nH]c4cccnc34)cc2ccn1CC1CCC1 10.1016/j.bmcl.2018.10.050
122196103 131016 0 None -53 2 Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 414 3 1 4 4.7 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(C(F)(F)F)c1 10.1016/j.bmcl.2015.10.013
CHEMBL3634426 131016 0 None -53 2 Human 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 414 3 1 4 4.7 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(C(F)(F)F)c1 10.1016/j.bmcl.2015.10.013
135126257 179988 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 351 3 1 5 2.4 Cc1nnc2ccc(C(=O)NC3CN(c4cccc(F)n4)C3)cc2c1C 10.1016/j.bmcl.2019.126678
CHEMBL4522845 179988 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 351 3 1 5 2.4 Cc1nnc2ccc(C(=O)NC3CN(c4cccc(F)n4)C3)cc2c1C 10.1016/j.bmcl.2019.126678
53375080 146470 35 None - 1 Human 7.2 pEC50 = 7.2 Functional
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 262 2 2 3 3.5 Fc1ccc(Nc2n[nH]c3cccnc23)cc1Cl 10.1016/j.bmcl.2016.04.041
CHEMBL3798040 146470 35 None - 1 Human 7.2 pEC50 = 7.2 Functional
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 262 2 2 3 3.5 Fc1ccc(Nc2n[nH]c3cccnc23)cc1Cl 10.1016/j.bmcl.2016.04.041
122419058 178111 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 308 3 2 6 3.6 c1cnc2c(Nc3ccc4c(C5CC5)nsc4c3)n[nH]c2n1 10.1021/acs.jmedchem.8b00994
CHEMBL4461258 178111 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 308 3 2 6 3.6 c1cnc2c(Nc3ccc4c(C5CC5)nsc4c3)n[nH]c2n1 10.1021/acs.jmedchem.8b00994
122419145 180502 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 414 4 2 6 4.2 CN(C(=O)c1nsc2cc(Nc3n[nH]c4cccnc34)ccc12)C1CC(F)(F)C1 10.1021/acs.jmedchem.8b00994
CHEMBL4536224 180502 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 414 4 2 6 4.2 CN(C(=O)c1nsc2cc(Nc3n[nH]c4cccnc34)ccc12)C1CC(F)(F)C1 10.1021/acs.jmedchem.8b00994
53375080 146470 35 None - 1 Human 7.2 pEC50 = 7.2 Functional
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 262 2 2 3 3.5 Fc1ccc(Nc2n[nH]c3cccnc23)cc1Cl 10.1016/j.bmcl.2016.04.041
CHEMBL3798040 146470 35 None - 1 Human 7.2 pEC50 = 7.2 Functional
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 262 2 2 3 3.5 Fc1ccc(Nc2n[nH]c3cccnc23)cc1Cl 10.1016/j.bmcl.2016.04.041
134191951 172153 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 318 3 2 5 3.6 Cn1nc(C2(C)CC2)c2ccc(Nc3n[nH]c4cccnc34)cc21 10.1016/j.bmcl.2018.06.034
CHEMBL4237497 172153 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 318 3 2 5 3.6 Cn1nc(C2(C)CC2)c2ccc(Nc3n[nH]c4cccnc34)cc21 10.1016/j.bmcl.2018.06.034
70694002 80986 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 285 2 0 3 4.4 Cc1c(-c2ccnc3ccccc23)cnn1-c1ccccc1 10.1016/j.bmcl.2012.03.032
CHEMBL2023452 80986 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 285 2 0 3 4.4 Cc1c(-c2ccnc3ccccc23)cnn1-c1ccccc1 10.1016/j.bmcl.2012.03.032
122196098 131011 0 None -19 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 382 3 1 4 3.9 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(F)c1 10.1016/j.bmcl.2015.10.013
CHEMBL3634421 131011 0 None -19 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 382 3 1 4 3.9 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(F)c1 10.1016/j.bmcl.2015.10.013
45110765 65898 0 None -1 2 Human 6.2 pEC50 = 6.2 Functional
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 405 4 1 4 4.0 O=C(Nc1ccc(N2C(=O)CC(c3ccccc3)C2=O)c(Cl)c1)c1ccccn1 10.1021/jm200956q
CHEMBL1698322 65898 0 None -1 2 Human 6.2 pEC50 = 6.2 Functional
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 405 4 1 4 4.0 O=C(Nc1ccc(N2C(=O)CC(c3ccccc3)C2=O)c(Cl)c1)c1ccccn1 10.1021/jm200956q
134190146 178576 0 None 2 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 315 3 2 5 4.0 CC(F)(F)c1noc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
CHEMBL4468073 178576 0 None 2 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 315 3 2 5 4.0 CC(F)(F)c1noc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
134190146 178576 0 None 2 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 315 3 2 5 4.0 CC(F)(F)c1noc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
CHEMBL4468073 178576 0 None 2 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 315 3 2 5 4.0 CC(F)(F)c1noc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
53375080 146470 35 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human mGlu4 receptor assessed as increase in calcium fluxAgonist activity at human mGlu4 receptor assessed as increase in calcium flux
ChEMBL 262 2 2 3 3.5 Fc1ccc(Nc2n[nH]c3cccnc23)cc1Cl 10.1016/j.ejmech.2022.114378
CHEMBL3798040 146470 35 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human mGlu4 receptor assessed as increase in calcium fluxAgonist activity at human mGlu4 receptor assessed as increase in calcium flux
ChEMBL 262 2 2 3 3.5 Fc1ccc(Nc2n[nH]c3cccnc23)cc1Cl 10.1016/j.ejmech.2022.114378
122419058 178111 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 308 3 2 6 3.6 c1cnc2c(Nc3ccc4c(C5CC5)nsc4c3)n[nH]c2n1 10.1021/acs.jmedchem.8b00994
CHEMBL4461258 178111 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 308 3 2 6 3.6 c1cnc2c(Nc3ccc4c(C5CC5)nsc4c3)n[nH]c2n1 10.1021/acs.jmedchem.8b00994
53375080 146470 35 None - 1 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 262 2 2 3 3.5 Fc1ccc(Nc2n[nH]c3cccnc23)cc1Cl 10.1016/j.bmcl.2018.06.034
CHEMBL3798040 146470 35 None - 1 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 262 2 2 3 3.5 Fc1ccc(Nc2n[nH]c3cccnc23)cc1Cl 10.1016/j.bmcl.2018.06.034
53374402 154097 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 242 2 2 3 3.1 Cc1cc(Nc2n[nH]c3cccnc23)ccc1F nan
CHEMBL3929112 154097 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 242 2 2 3 3.1 Cc1cc(Nc2n[nH]c3cccnc23)ccc1F nan
122419145 180502 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 414 4 2 6 4.2 CN(C(=O)c1nsc2cc(Nc3n[nH]c4cccnc34)ccc12)C1CC(F)(F)C1 10.1021/acs.jmedchem.8b00994
CHEMBL4536224 180502 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 414 4 2 6 4.2 CN(C(=O)c1nsc2cc(Nc3n[nH]c4cccnc34)ccc12)C1CC(F)(F)C1 10.1021/acs.jmedchem.8b00994
54670323 153655 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 445 6 1 6 4.0 O=C(Nc1nc(C(F)F)c(S(=O)(=O)Cc2c(F)cccc2F)s1)c1ccccn1 nan
CHEMBL3925341 153655 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 445 6 1 6 4.0 O=C(Nc1nc(C(F)F)c(S(=O)(=O)Cc2c(F)cccc2F)s1)c1ccccn1 nan
53373996 151419 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 285 2 3 3 3.0 Cc1cc(NC(=O)Nc2n[nH]c3cccnc23)ccc1F nan
CHEMBL3908108 151419 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 285 2 3 3 3.0 Cc1cc(NC(=O)Nc2n[nH]c3cccnc23)ccc1F nan
162660130 188053 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 333 4 2 5 3.7 CC(C)Cn1ccc2cc(Nc3n[nH]c4cccnc34)ccc2c1=O 10.1016/j.bmcl.2018.10.050
CHEMBL4762098 188053 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 333 4 2 5 3.7 CC(C)Cn1ccc2cc(Nc3n[nH]c4cccnc34)ccc2c1=O 10.1016/j.bmcl.2018.10.050
49865400 22722 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilization
ChEMBL 407 5 1 5 3.9 CN(c1ccccc1Cl)S(=O)(=O)c1ccc(NC(=O)c2nccs2)cc1 10.1016/j.bmcl.2010.07.007
CHEMBL1223315 22722 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilization
ChEMBL 407 5 1 5 3.9 CN(c1ccccc1Cl)S(=O)(=O)c1ccc(NC(=O)c2nccs2)cc1 10.1016/j.bmcl.2010.07.007
1410 9054 48 None -1 8 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at mGlu4 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate productionAgonist activity at mGlu4 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate production
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm070262c
1412 9054 48 None -1 8 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at mGlu4 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate productionAgonist activity at mGlu4 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate production
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm070262c
179394 9054 48 None -1 8 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at mGlu4 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate productionAgonist activity at mGlu4 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate production
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm070262c
57689795 9054 48 None -1 8 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at mGlu4 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate productionAgonist activity at mGlu4 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate production
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm070262c
CHEMBL33567 9054 48 None -1 8 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at mGlu4 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate productionAgonist activity at mGlu4 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate production
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm070262c
70683518 80999 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 441 6 0 6 3.6 CC(=O)N1CCN(CCOc2ccc3c(-c4cnn(-c5ccccc5)c4)ccnc3c2)CC1 10.1016/j.bmcl.2012.03.032
CHEMBL2023471 80999 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 441 6 0 6 3.6 CC(=O)N1CCN(CCOc2ccc3c(-c4cnn(-c5ccccc5)c4)ccnc3c2)CC1 10.1016/j.bmcl.2012.03.032
136503365 165749 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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 366 1 1 4 4.7 O/N=c1\cc(-c2cc3ccccc3cn2)oc2ccc(Br)cc12 10.1021/acs.jmedchem.7b00991
CHEMBL4096136 165749 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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 366 1 1 4 4.7 O/N=c1\cc(-c2cc3ccccc3cn2)oc2ccc(Br)cc12 10.1021/acs.jmedchem.7b00991
13302355 21841 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
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 196 2 0 2 3.0 Cc1nccc(/C=C/c2ccccc2)n1 10.1016/j.bmcl.2010.06.078
CHEMBL1209435 21841 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
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 196 2 0 2 3.0 Cc1nccc(/C=C/c2ccccc2)n1 10.1016/j.bmcl.2010.06.078
127046558 146646 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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 146646 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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
54670501 154407 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 373 4 1 6 3.2 Cc1cccc(S(=O)(=O)c2sc(NC(=O)c3ccccn3)nc2C)c1 nan
CHEMBL3931345 154407 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 373 4 1 6 3.2 Cc1cccc(S(=O)(=O)c2sc(NC(=O)c3ccccn3)nc2C)c1 nan
137648363 164523 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
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 288 1 1 4 3.9 O/N=c1\cc(-c2ccc3ncccc3c2)oc2ccccc12 10.1021/acs.jmedchem.7b00991
CHEMBL4082331 164523 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
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 288 1 1 4 3.9 O/N=c1\cc(-c2ccc3ncccc3c2)oc2ccccc12 10.1021/acs.jmedchem.7b00991
46836713 72304 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
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 284 2 2 6 2.6 c1cnc(Nc2nc3c(s2)CCCc2n[nH]cc2-3)nc1 10.1021/jm200290z
CHEMBL1830711 72304 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
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 284 2 2 6 2.6 c1cnc(Nc2nc3c(s2)CCCc2n[nH]cc2-3)nc1 10.1021/jm200290z
87305070 163295 0 None -2 2 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of recombinant human mGlu4 receptor expressed in HEK293 cells co-expressing chimeric G protein assessed as increase in EC20 glutamate-induced cAMP levelPositive allosteric modulation of recombinant human mGlu4 receptor expressed in HEK293 cells co-expressing chimeric G protein assessed as increase in EC20 glutamate-induced cAMP level
ChEMBL 406 5 1 8 2.7 O/N=c1\cc(-c2cc3cccn3cn2)oc2ccc(OCCN3CCOCC3)cc12 10.1021/acs.jmedchem.7b00991
CHEMBL4067875 163295 0 None -2 2 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of recombinant human mGlu4 receptor expressed in HEK293 cells co-expressing chimeric G protein assessed as increase in EC20 glutamate-induced cAMP levelPositive allosteric modulation of recombinant human mGlu4 receptor expressed in HEK293 cells co-expressing chimeric G protein assessed as increase in EC20 glutamate-induced cAMP level
ChEMBL 406 5 1 8 2.7 O/N=c1\cc(-c2cc3cccn3cn2)oc2ccc(OCCN3CCOCC3)cc12 10.1021/acs.jmedchem.7b00991
134189979 176634 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 306 3 2 6 3.5 c1cnc2c(Nc3ccc4c(C5CCC5)noc4c3)n[nH]c2n1 10.1021/acs.jmedchem.8b00994
CHEMBL4440167 176634 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 306 3 2 6 3.5 c1cnc2c(Nc3ccc4c(C5CCC5)noc4c3)n[nH]c2n1 10.1021/acs.jmedchem.8b00994
134189979 176634 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 306 3 2 6 3.5 c1cnc2c(Nc3ccc4c(C5CCC5)noc4c3)n[nH]c2n1 10.1021/acs.jmedchem.8b00994
CHEMBL4440167 176634 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 306 3 2 6 3.5 c1cnc2c(Nc3ccc4c(C5CCC5)noc4c3)n[nH]c2n1 10.1021/acs.jmedchem.8b00994
53374001 152739 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 276 3 2 3 3.4 Fc1ccc(CNc2n[nH]c3cccnc23)cc1Cl nan
CHEMBL3918174 152739 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 276 3 2 3 3.4 Fc1ccc(CNc2n[nH]c3cccnc23)cc1Cl nan
54670775 149602 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 387 5 1 6 3.4 Cc1ccccc1CS(=O)(=O)c1sc(NC(=O)c2ccccn2)nc1C nan
CHEMBL3893029 149602 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 387 5 1 6 3.4 Cc1ccccc1CS(=O)(=O)c1sc(NC(=O)c2ccccn2)nc1C nan
134191684 187285 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 301 3 2 4 4.1 c1cnc2c(Nc3ccc4c(C5CC5)nccc4c3)n[nH]c2c1 10.1016/j.bmcl.2018.10.050
CHEMBL4753304 187285 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 301 3 2 4 4.1 c1cnc2c(Nc3ccc4c(C5CC5)nccc4c3)n[nH]c2c1 10.1016/j.bmcl.2018.10.050
3756397 15086 2 None 2 4 Rat 5.2 pEC50 = 5.2 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 239 7 4 4 -0.5 NC(CCP(=O)(O)CCC(=O)O)C(=O)O 10.1021/jm901523t
4041087 15086 2 None 2 4 Rat 5.2 pEC50 = 5.2 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 239 7 4 4 -0.5 NC(CCP(=O)(O)CCC(=O)O)C(=O)O 10.1021/jm901523t
CHEMBL1092727 15086 2 None 2 4 Rat 5.2 pEC50 = 5.2 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 239 7 4 4 -0.5 NC(CCP(=O)(O)CCC(=O)O)C(=O)O 10.1021/jm901523t
122193178 130711 0 None -30 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of human mGlu4 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay
ChEMBL 398 3 1 4 4.4 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
CHEMBL3628114 130711 0 None -30 2 Human 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of human mGlu4 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay
ChEMBL 398 3 1 4 4.4 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
137645989 164473 0 None 1 4 Human 6.1 pEC50 = 6.1 Functional
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 364 8 5 8 0.4 COc1cc([C@@H](O)P(=O)(O)CC[C@H](N)C(=O)O)cc([N+](=O)[O-])c1O 10.1021/acs.jmedchem.7b01438
CHEMBL4081842 164473 0 None 1 4 Human 6.1 pEC50 = 6.1 Functional
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 364 8 5 8 0.4 COc1cc([C@@H](O)P(=O)(O)CC[C@H](N)C(=O)O)cc([N+](=O)[O-])c1O 10.1021/acs.jmedchem.7b01438
16747847 92617 1 None -23 4 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at mGlu4 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate productionAgonist activity at mGlu4 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate production
ChEMBL 195 3 4 3 -1.0 N[C@@]1(C(=O)O)C[C@H]1CP(=O)(O)O 10.1021/jm070262c
CHEMBL229697 92617 1 None -23 4 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at mGlu4 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate productionAgonist activity at mGlu4 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate production
ChEMBL 195 3 4 3 -1.0 N[C@@]1(C(=O)O)C[C@H]1CP(=O)(O)O 10.1021/jm070262c
1408 7053 31 None -1 7 Rat 5.1 pEC50 = 5.1 Functional
Activity at rat mGluR4 receptor measured as intracellular calcium concentration in HEK293 cellsActivity at rat mGluR4 receptor measured as intracellular calcium concentration in HEK293 cells
ChEMBL 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O 10.1016/j.bmcl.2006.06.062
6604820 7053 31 None -1 7 Rat 5.1 pEC50 = 5.1 Functional
Activity at rat mGluR4 receptor measured as intracellular calcium concentration in HEK293 cellsActivity at rat mGluR4 receptor measured as intracellular calcium concentration in HEK293 cells
ChEMBL 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O 10.1016/j.bmcl.2006.06.062
CHEMBL285043 7053 31 None -1 7 Rat 5.1 pEC50 = 5.1 Functional
Activity at rat mGluR4 receptor measured as intracellular calcium concentration in HEK293 cellsActivity at rat mGluR4 receptor measured as intracellular calcium concentration in HEK293 cells
ChEMBL 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O 10.1016/j.bmcl.2006.06.062
CHEMBL288635 7053 31 None -1 7 Rat 5.1 pEC50 = 5.1 Functional
Activity at rat mGluR4 receptor measured as intracellular calcium concentration in HEK293 cellsActivity at rat mGluR4 receptor measured as intracellular calcium concentration in HEK293 cells
ChEMBL 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O 10.1016/j.bmcl.2006.06.062
1408 7053 31 None 1 7 Human 5.1 pEC50 = 5.1 Functional
Agonist activity against Metabotropic glutamate receptor 4 expressed in HEK 293 cells was evaluated by measuring total inositol phosphate accumulationAgonist activity against Metabotropic glutamate receptor 4 expressed in HEK 293 cells was evaluated by measuring total inositol phosphate accumulation
ChEMBL 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O 10.1021/jm970207b
6604820 7053 31 None 1 7 Human 5.1 pEC50 = 5.1 Functional
Agonist activity against Metabotropic glutamate receptor 4 expressed in HEK 293 cells was evaluated by measuring total inositol phosphate accumulationAgonist activity against Metabotropic glutamate receptor 4 expressed in HEK 293 cells was evaluated by measuring total inositol phosphate accumulation
ChEMBL 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O 10.1021/jm970207b
CHEMBL285043 7053 31 None 1 7 Human 5.1 pEC50 = 5.1 Functional
Agonist activity against Metabotropic glutamate receptor 4 expressed in HEK 293 cells was evaluated by measuring total inositol phosphate accumulationAgonist activity against Metabotropic glutamate receptor 4 expressed in HEK 293 cells was evaluated by measuring total inositol phosphate accumulation
ChEMBL 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O 10.1021/jm970207b
CHEMBL288635 7053 31 None 1 7 Human 5.1 pEC50 = 5.1 Functional
Agonist activity against Metabotropic glutamate receptor 4 expressed in HEK 293 cells was evaluated by measuring total inositol phosphate accumulationAgonist activity against Metabotropic glutamate receptor 4 expressed in HEK 293 cells was evaluated by measuring total inositol phosphate accumulation
ChEMBL 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O 10.1021/jm970207b
46197879 15014 0 None -2 2 Rat 5.1 pEC50 = 5.1 Functional
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 241 6 5 5 -1.5 N[C@@H](CCP(=O)(O)C(O)C(=O)O)C(=O)O 10.1021/jm901523t
CHEMBL1092316 15014 0 None -2 2 Rat 5.1 pEC50 = 5.1 Functional
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 241 6 5 5 -1.5 N[C@@H](CCP(=O)(O)C(O)C(=O)O)C(=O)O 10.1021/jm901523t
53373995 151232 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 312 2 2 3 4.7 Clc1cc(Nc2n[nH]c3cccnc23)cc(Cl)c1Cl nan
CHEMBL3906552 151232 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 312 2 2 3 4.7 Clc1cc(Nc2n[nH]c3cccnc23)cc(Cl)c1Cl nan
134189963 176461 0 None -1 2 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 319 3 2 5 4.5 c1cnc2c(Nc3ccc4c(C5CCCC5)noc4c3)n[nH]c2c1 10.1021/acs.jmedchem.8b00994
CHEMBL4437680 176461 0 None -1 2 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 319 3 2 5 4.5 c1cnc2c(Nc3ccc4c(C5CCCC5)noc4c3)n[nH]c2c1 10.1021/acs.jmedchem.8b00994
122193178 130711 0 None -30 2 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of human mGlu4 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay
ChEMBL 398 3 1 4 4.4 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
CHEMBL3628114 130711 0 None -30 2 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of human mGlu4 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay
ChEMBL 398 3 1 4 4.4 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
134189963 176461 0 None -1 2 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 319 3 2 5 4.5 c1cnc2c(Nc3ccc4c(C5CCCC5)noc4c3)n[nH]c2c1 10.1021/acs.jmedchem.8b00994
CHEMBL4437680 176461 0 None -1 2 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 319 3 2 5 4.5 c1cnc2c(Nc3ccc4c(C5CCCC5)noc4c3)n[nH]c2c1 10.1021/acs.jmedchem.8b00994
134191511 189195 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 355 3 2 6 4.1 Cc1cc(C)n(-c2nccc3cc(Nc4n[nH]c5cccnc45)ccc23)n1 10.1016/j.bmcl.2018.10.050
CHEMBL4785728 189195 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 355 3 2 6 4.1 Cc1cc(C)n(-c2nccc3cc(Nc4n[nH]c5cccnc45)ccc23)n1 10.1016/j.bmcl.2018.10.050
70689815 80988 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 289 2 0 3 4.2 Fc1ccc2c(-c3cnn(-c4ccccc4)c3)ccnc2c1 10.1016/j.bmcl.2012.03.032
CHEMBL2023454 80988 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 289 2 0 3 4.2 Fc1ccc2c(-c3cnn(-c4ccccc4)c3)ccnc2c1 10.1016/j.bmcl.2012.03.032
49865451 22743 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilization
ChEMBL 421 5 2 4 4.4 O=C(Nc1ccc(Cl)c(S(=O)(=O)Nc2ccccc2Cl)c1)c1ccccn1 10.1016/j.bmcl.2010.07.007
CHEMBL1223383 22743 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilization
ChEMBL 421 5 2 4 4.4 O=C(Nc1ccc(Cl)c(S(=O)(=O)Nc2ccccc2Cl)c1)c1ccccn1 10.1016/j.bmcl.2010.07.007
162668594 189363 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 261 2 2 4 3.3 c1cnc2ccc(Nc3n[nH]c4cccnc34)cc2c1 10.1016/j.bmcl.2018.10.050
CHEMBL4788007 189363 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 261 2 2 4 3.3 c1cnc2ccc(Nc3n[nH]c4cccnc34)cc2c1 10.1016/j.bmcl.2018.10.050
135126574 179108 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 368 3 1 4 3.1 Cc1nnc2ccc(C(=O)NC3CN(c4ccc(F)c(F)c4)C3)cc2c1C 10.1016/j.bmcl.2019.126678
CHEMBL4475472 179108 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 368 3 1 4 3.1 Cc1nnc2ccc(C(=O)NC3CN(c4ccc(F)c(F)c4)C3)cc2c1C 10.1016/j.bmcl.2019.126678
53373770 149774 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 225 2 2 4 2.4 Cc1cncc(Nc2n[nH]c3cccnc23)c1 nan
CHEMBL3894572 149774 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 225 2 2 4 2.4 Cc1cncc(Nc2n[nH]c3cccnc23)c1 nan
52914105 147212 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 395 4 1 5 3.4 O=C(Nc1ccn(S(=O)(=O)c2ccc(C(F)(F)F)cc2)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
CHEMBL3809183 147212 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 395 4 1 5 3.4 O=C(Nc1ccn(S(=O)(=O)c2ccc(C(F)(F)F)cc2)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
46869942 64676 0 None -1 2 Rat 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 369 4 2 3 4.4 O=C(Nc1ccc(NC(=O)c2ccccc2Cl)c(F)c1)c1ccccn1 10.1021/jm101271s
CHEMBL1672241 64676 0 None -1 2 Rat 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 369 4 2 3 4.4 O=C(Nc1ccc(NC(=O)c2ccccc2Cl)c(F)c1)c1ccccn1 10.1021/jm101271s
155557230 181353 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 338 3 2 6 4.3 CC(C)(C)Cc1nsc2cc(Nc3n[nH]c4cccnc34)cnc12 10.1021/acs.jmedchem.8b00994
CHEMBL4556685 181353 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 338 3 2 6 4.3 CC(C)(C)Cc1nsc2cc(Nc3n[nH]c4cccnc34)cnc12 10.1021/acs.jmedchem.8b00994
155557230 181353 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 338 3 2 6 4.3 CC(C)(C)Cc1nsc2cc(Nc3n[nH]c4cccnc34)cnc12 10.1021/acs.jmedchem.8b00994
CHEMBL4556685 181353 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 338 3 2 6 4.3 CC(C)(C)Cc1nsc2cc(Nc3n[nH]c4cccnc34)cnc12 10.1021/acs.jmedchem.8b00994
3323 10798 40 None - 1 Human 6.1 pEC50 = 6.1 Functional
Allosteric modulator activity at human mGlu4 receptor expressed in CHO cells coexpressing Gqi5 assessed as effect on calcium fluxAllosteric modulator activity at human mGlu4 receptor expressed in CHO cells coexpressing Gqi5 assessed as effect on calcium flux
ChEMBL 315 3 2 2 3.8 O=C([C@H]1CCCC[C@H]1C(=O)O)Nc1cc(Cl)cc(c1)Cl 10.1016/j.bmcl.2009.07.072
888023 10798 40 None - 1 Human 6.1 pEC50 = 6.1 Functional
Allosteric modulator activity at human mGlu4 receptor expressed in CHO cells coexpressing Gqi5 assessed as effect on calcium fluxAllosteric modulator activity at human mGlu4 receptor expressed in CHO cells coexpressing Gqi5 assessed as effect on calcium flux
ChEMBL 315 3 2 2 3.8 O=C([C@H]1CCCC[C@H]1C(=O)O)Nc1cc(Cl)cc(c1)Cl 10.1016/j.bmcl.2009.07.072
CHEMBL578988 10798 40 None - 1 Human 6.1 pEC50 = 6.1 Functional
Allosteric modulator activity at human mGlu4 receptor expressed in CHO cells coexpressing Gqi5 assessed as effect on calcium fluxAllosteric modulator activity at human mGlu4 receptor expressed in CHO cells coexpressing Gqi5 assessed as effect on calcium flux
ChEMBL 315 3 2 2 3.8 O=C([C@H]1CCCC[C@H]1C(=O)O)Nc1cc(Cl)cc(c1)Cl 10.1016/j.bmcl.2009.07.072
52914100 147277 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 345 4 1 5 2.5 O=C(Nc1ccn(S(=O)(=O)c2ccc(F)cc2)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
CHEMBL3809928 147277 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 345 4 1 5 2.5 O=C(Nc1ccn(S(=O)(=O)c2ccc(F)cc2)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
24779944 14640 0 None -2 3 Rat 5.1 pEC50 = 5.1 Functional
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 225 6 4 4 -0.9 N[C@@H](CCP(=O)(O)CC(=O)O)C(=O)O 10.1021/jm901523t
CHEMBL1089852 14640 0 None -2 3 Rat 5.1 pEC50 = 5.1 Functional
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 225 6 4 4 -0.9 N[C@@H](CCP(=O)(O)CC(=O)O)C(=O)O 10.1021/jm901523t
52914105 147212 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 395 4 1 5 3.4 O=C(Nc1ccn(S(=O)(=O)c2ccc(C(F)(F)F)cc2)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
CHEMBL3809183 147212 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 395 4 1 5 3.4 O=C(Nc1ccn(S(=O)(=O)c2ccc(C(F)(F)F)cc2)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
52914100 147277 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 345 4 1 5 2.5 O=C(Nc1ccn(S(=O)(=O)c2ccc(F)cc2)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
CHEMBL3809928 147277 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 345 4 1 5 2.5 O=C(Nc1ccn(S(=O)(=O)c2ccc(F)cc2)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
122197961 167624 0 None - 1 Rat 5.1 pEC50 = 5.1 Functional
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 361 10 4 6 0.7 COc1cc(CP(=O)(O)CC[C@@H](N)C(=O)O)ccc1OCC(=O)O nan
CHEMBL4114834 167624 0 None - 1 Rat 5.1 pEC50 = 5.1 Functional
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 361 10 4 6 0.7 COc1cc(CP(=O)(O)CC[C@@H](N)C(=O)O)ccc1OCC(=O)O nan
134190172 179977 0 None 1 2 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 265 2 2 5 3.2 Cc1noc2ccc(Nc3n[nH]c4cccnc34)cc12 10.1021/acs.jmedchem.8b00994
CHEMBL4522695 179977 0 None 1 2 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 265 2 2 5 3.2 Cc1noc2ccc(Nc3n[nH]c4cccnc34)cc12 10.1021/acs.jmedchem.8b00994
134190172 179977 0 None 1 2 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 265 2 2 5 3.2 Cc1noc2ccc(Nc3n[nH]c4cccnc34)cc12 10.1021/acs.jmedchem.8b00994
CHEMBL4522695 179977 0 None 1 2 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 265 2 2 5 3.2 Cc1noc2ccc(Nc3n[nH]c4cccnc34)cc12 10.1021/acs.jmedchem.8b00994
3323 10798 40 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 315 3 2 2 3.8 O=C([C@H]1CCCC[C@H]1C(=O)O)Nc1cc(Cl)cc(c1)Cl 10.1021/jm200290z
888023 10798 40 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 315 3 2 2 3.8 O=C([C@H]1CCCC[C@H]1C(=O)O)Nc1cc(Cl)cc(c1)Cl 10.1021/jm200290z
CHEMBL578988 10798 40 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 315 3 2 2 3.8 O=C([C@H]1CCCC[C@H]1C(=O)O)Nc1cc(Cl)cc(c1)Cl 10.1021/jm200290z
46836566 72315 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 301 2 2 5 3.3 Fc1ccc(Nc2nc3c(s2)CCCc2n[nH]cc2-3)nc1 10.1021/jm200290z
CHEMBL1830902 72315 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 301 2 2 5 3.3 Fc1ccc(Nc2nc3c(s2)CCCc2n[nH]cc2-3)nc1 10.1021/jm200290z
136503366 162964 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 362 5 1 6 4.0 COCCOc1ccc2oc(-c3cc4ccccc4cn3)c/c(=N\O)c2c1 10.1021/acs.jmedchem.7b00991
CHEMBL4064041 162964 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 362 5 1 6 4.0 COCCOc1ccc2oc(-c3cc4ccccc4cn3)c/c(=N\O)c2c1 10.1021/acs.jmedchem.7b00991
51003232 64668 0 None 1 2 Rat 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 387 5 2 5 4.3 COc1cc(NC(=O)c2cscn2)ccc1NC(=O)c1ccccc1Cl 10.1021/jm101271s
CHEMBL1672233 64668 0 None 1 2 Rat 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 387 5 2 5 4.3 COc1cc(NC(=O)c2cscn2)ccc1NC(=O)c1ccccc1Cl 10.1021/jm101271s
53373876 151291 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 412 3 2 5 4.2 CN1C(=O)N(c2ccc(Nc3n[nH]c4cccnc34)cc2Cl)C(=O)C1C(C)(C)C nan
CHEMBL3907055 151291 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 412 3 2 5 4.2 CN1C(=O)N(c2ccc(Nc3n[nH]c4cccnc34)cc2Cl)C(=O)C1C(C)(C)C nan
122419071 181870 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 337 3 2 5 4.9 CC(C)(C)Cc1nsc2cc(Nc3n[nH]c4ncccc34)ccc12 10.1021/acs.jmedchem.8b00994
CHEMBL4568745 181870 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 337 3 2 5 4.9 CC(C)(C)Cc1nsc2cc(Nc3n[nH]c4ncccc34)ccc12 10.1021/acs.jmedchem.8b00994
127047061 146453 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 146453 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
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
122419071 181870 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 337 3 2 5 4.9 CC(C)(C)Cc1nsc2cc(Nc3n[nH]c4ncccc34)ccc12 10.1021/acs.jmedchem.8b00994
CHEMBL4568745 181870 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 337 3 2 5 4.9 CC(C)(C)Cc1nsc2cc(Nc3n[nH]c4ncccc34)ccc12 10.1021/acs.jmedchem.8b00994
134191536 189016 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 261 2 2 4 3.3 c1cnc2c(Nc3ccc4cnccc4c3)n[nH]c2c1 10.1016/j.bmcl.2018.10.050
CHEMBL4783372 189016 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 261 2 2 4 3.3 c1cnc2c(Nc3ccc4cnccc4c3)n[nH]c2c1 10.1016/j.bmcl.2018.10.050
122197947 167166 0 None 5 2 Rat 5.1 pEC50 = 5.1 Functional
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 347 9 5 6 0.2 N[C@H](CCP(=O)(O)C(O)c1cccc(OCC(=O)O)c1)C(=O)O nan
CHEMBL4111192 167166 0 None 5 2 Rat 5.1 pEC50 = 5.1 Functional
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 347 9 5 6 0.2 N[C@H](CCP(=O)(O)C(O)c1cccc(OCC(=O)O)c1)C(=O)O nan
134198081 172146 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 379 3 2 6 2.8 Cn1nc(C(=O)N2CC[C@H](F)C2)c2ccc(Nc3n[nH]c4cccnc34)cc21 10.1016/j.bmcl.2018.06.034
CHEMBL4237293 172146 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 379 3 2 6 2.8 Cn1nc(C(=O)N2CC[C@H](F)C2)c2ccc(Nc3n[nH]c4cccnc34)cc21 10.1016/j.bmcl.2018.06.034
3586321 75477 1 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 3 1 5 3.1 O=C(Nc1ccc(N2S(=O)(=O)c3ccccc3S2(=O)=O)cc1)C1CCCCC1 10.1021/jm200956q
CHEMBL1921854 75477 1 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 3 1 5 3.1 O=C(Nc1ccc(N2S(=O)(=O)c3ccccc3S2(=O)=O)cc1)C1CCCCC1 10.1021/jm200956q
49865397 22719 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilization
ChEMBL 393 5 2 5 3.9 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2Cl)cc1)c1nccs1 10.1016/j.bmcl.2010.07.007
CHEMBL1223312 22719 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilization
ChEMBL 393 5 2 5 3.9 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2Cl)cc1)c1nccs1 10.1016/j.bmcl.2010.07.007
137634091 163087 0 None 3 2 Human 5.1 pEC50 = 5.1 Functional
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 289 6 5 5 0.5 N[C@@H](CCP(=O)(O)C(O)c1ccc(O)cc1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4065496 163087 0 None 3 2 Human 5.1 pEC50 = 5.1 Functional
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 289 6 5 5 0.5 N[C@@H](CCP(=O)(O)C(O)c1ccc(O)cc1)C(=O)O 10.1021/acs.jmedchem.7b01438
46869952 65932 0 None -1 2 Human 6.1 pEC50 = 6.1 Functional
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 419 4 1 4 4.2 CC1(c2ccccc2)CC(=O)N(c2ccc(NC(=O)c3ccccn3)cc2Cl)C1=O 10.1021/jm200956q
CHEMBL1699345 65932 0 None -1 2 Human 6.1 pEC50 = 6.1 Functional
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 419 4 1 4 4.2 CC1(c2ccccc2)CC(=O)N(c2ccc(NC(=O)c3ccccn3)cc2Cl)C1=O 10.1021/jm200956q
134191954 172692 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 278 2 2 5 2.9 Cc1nn(C)c2cc(Nc3n[nH]c4cccnc34)ccc12 10.1016/j.bmcl.2018.06.034
CHEMBL4250214 172692 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 278 2 2 5 2.9 Cc1nn(C)c2cc(Nc3n[nH]c4cccnc34)ccc12 10.1016/j.bmcl.2018.06.034
42644786 202110 2 None 2 2 Human 6.1 pEC50 = 6.1 Functional
Activity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilizationActivity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilization
ChEMBL 246 3 1 3 2.5 COc1cc(NC(=O)c2ccccn2)ccc1F 10.1021/jm9005065
CHEMBL551635 202110 2 None 2 2 Human 6.1 pEC50 = 6.1 Functional
Activity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilizationActivity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilization
ChEMBL 246 3 1 3 2.5 COc1cc(NC(=O)c2ccccn2)ccc1F 10.1021/jm9005065
137631983 163325 0 None 1 2 Human 5.1 pEC50 = 5.1 Functional
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 315 7 4 5 1.0 CC(=O)c1ccc(C(O)P(=O)(O)CC[C@H](N)C(=O)O)cc1 10.1021/acs.jmedchem.7b01438
CHEMBL4068205 163325 0 None 1 2 Human 5.1 pEC50 = 5.1 Functional
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 315 7 4 5 1.0 CC(=O)c1ccc(C(O)P(=O)(O)CC[C@H](N)C(=O)O)cc1 10.1021/acs.jmedchem.7b01438
5916431 21842 13 None - 1 Human 5.1 pEC50 = 5.1 Functional
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 214 2 1 3 2.9 Sc1nccc(/C=C/c2ccccc2)n1 10.1016/j.bmcl.2010.06.078
CHEMBL1209437 21842 13 None - 1 Human 5.1 pEC50 = 5.1 Functional
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 214 2 1 3 2.9 Sc1nccc(/C=C/c2ccccc2)n1 10.1016/j.bmcl.2010.06.078
53374109 155236 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 264 2 2 3 3.1 Fc1cc(F)c(F)c(Nc2n[nH]c3cccnc23)c1 nan
CHEMBL3937959 155236 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 264 2 2 3 3.1 Fc1cc(F)c(F)c(Nc2n[nH]c3cccnc23)c1 nan
53374108 158862 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 322 3 2 5 2.8 CS(=O)(=O)c1ccc(Nc2n[nH]c3cccnc23)cc1Cl nan
CHEMBL3967569 158862 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 322 3 2 5 2.8 CS(=O)(=O)c1ccc(Nc2n[nH]c3cccnc23)cc1Cl nan
135565465 165084 10 None -1 2 Human 7.1 pEC50 = 7.1 Functional
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 421 5 1 7 4.3 O/N=c1\cc(-c2cc3sccc3cn2)oc2ccc(CCCN3CCOCC3)cc12 10.1021/acs.jmedchem.7b00991
CHEMBL4089083 165084 10 None -1 2 Human 7.1 pEC50 = 7.1 Functional
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 421 5 1 7 4.3 O/N=c1\cc(-c2cc3sccc3cn2)oc2ccc(CCCN3CCOCC3)cc12 10.1021/acs.jmedchem.7b00991
137659207 165885 0 None 4 2 Human 5.1 pEC50 = 5.1 Functional
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 457 10 4 6 3.6 N[C@@H](CCP(=O)(O)C(NCc1cccc2ccccc12)c1cccc([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4097544 165885 0 None 4 2 Human 5.1 pEC50 = 5.1 Functional
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 457 10 4 6 3.6 N[C@@H](CCP(=O)(O)C(NCc1cccc2ccccc12)c1cccc([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
14842361 175969 1 None -4 2 Human 5.1 pEC50 = 5.1 Functional
Effective concentration which exhibit agonistic activity at metabotropic glutamate 4 receptor stably expressed in AV12 cellsEffective concentration which exhibit agonistic activity at metabotropic glutamate 4 receptor stably expressed in AV12 cells
ChEMBL 195 3 4 3 -1.0 NC1(C(=O)O)CC1CP(=O)(O)O 10.1016/j.bmcl.2004.10.040
CHEMBL440648 175969 1 None -4 2 Human 5.1 pEC50 = 5.1 Functional
Effective concentration which exhibit agonistic activity at metabotropic glutamate 4 receptor stably expressed in AV12 cellsEffective concentration which exhibit agonistic activity at metabotropic glutamate 4 receptor stably expressed in AV12 cells
ChEMBL 195 3 4 3 -1.0 NC1(C(=O)O)CC1CP(=O)(O)O 10.1016/j.bmcl.2004.10.040
53374208 149872 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 266 2 2 3 4.0 CC(C)(C)c1cccc(Nc2n[nH]c3cccnc23)c1 nan
CHEMBL3895394 149872 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 266 2 2 3 4.0 CC(C)(C)c1cccc(Nc2n[nH]c3cccnc23)c1 nan
121485558 182482 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 335 2 2 5 4.3 FC(F)(F)c1nsc2cc(Nc3n[nH]c4ncccc34)ccc12 10.1021/acs.jmedchem.8b00994
CHEMBL4582180 182482 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 335 2 2 5 4.3 FC(F)(F)c1nsc2cc(Nc3n[nH]c4ncccc34)ccc12 10.1021/acs.jmedchem.8b00994
134198078 172261 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 379 4 3 6 2.8 Cn1nc(C(=O)NC2CC(F)C2)c2ccc(Nc3n[nH]c4cccnc34)cc21 10.1016/j.bmcl.2018.06.034
CHEMBL4240046 172261 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 379 4 3 6 2.8 Cn1nc(C(=O)NC2CC(F)C2)c2ccc(Nc3n[nH]c4cccnc34)cc21 10.1016/j.bmcl.2018.06.034
121485558 182482 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 335 2 2 5 4.3 FC(F)(F)c1nsc2cc(Nc3n[nH]c4ncccc34)ccc12 10.1021/acs.jmedchem.8b00994
CHEMBL4582180 182482 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 335 2 2 5 4.3 FC(F)(F)c1nsc2cc(Nc3n[nH]c4ncccc34)ccc12 10.1021/acs.jmedchem.8b00994
134191669 188686 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 311 3 2 4 4.2 FC(F)c1nccc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1016/j.bmcl.2018.10.050
CHEMBL4779331 188686 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 311 3 2 4 4.2 FC(F)c1nccc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1016/j.bmcl.2018.10.050
1410 9054 48 None -1 8 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat mGluR4 receptor expressed HEK293 cells assessed as effect on inositol phosphate productionAgonist activity at rat mGluR4 receptor expressed HEK293 cells assessed as effect on inositol phosphate production
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm070400y
1412 9054 48 None -1 8 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat mGluR4 receptor expressed HEK293 cells assessed as effect on inositol phosphate productionAgonist activity at rat mGluR4 receptor expressed HEK293 cells assessed as effect on inositol phosphate production
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm070400y
179394 9054 48 None -1 8 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat mGluR4 receptor expressed HEK293 cells assessed as effect on inositol phosphate productionAgonist activity at rat mGluR4 receptor expressed HEK293 cells assessed as effect on inositol phosphate production
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm070400y
57689795 9054 48 None -1 8 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat mGluR4 receptor expressed HEK293 cells assessed as effect on inositol phosphate productionAgonist activity at rat mGluR4 receptor expressed HEK293 cells assessed as effect on inositol phosphate production
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm070400y
CHEMBL33567 9054 48 None -1 8 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat mGluR4 receptor expressed HEK293 cells assessed as effect on inositol phosphate productionAgonist activity at rat mGluR4 receptor expressed HEK293 cells assessed as effect on inositol phosphate production
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm070400y
122197938 167718 0 None 43 3 Rat 7.1 pEC50 = 7.1 Functional
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 395 10 5 7 0.4 COc1cc(C(O)P(=O)(O)CC[C@@H](N)C(=O)O)cc(F)c1OCC(=O)O nan
CHEMBL4115462 167718 0 None 43 3 Rat 7.1 pEC50 = 7.1 Functional
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 395 10 5 7 0.4 COc1cc(C(O)P(=O)(O)CC[C@@H](N)C(=O)O)cc(F)c1OCC(=O)O nan
58058372 162976 0 None 3 3 Human 6.1 pEC50 = 6.1 Functional
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 302 7 3 5 1.2 N[C@@H](CCP(=O)(O)Cc1cccc([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4064187 162976 0 None 3 3 Human 6.1 pEC50 = 6.1 Functional
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 302 7 3 5 1.2 N[C@@H](CCP(=O)(O)Cc1cccc([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
137649482 163976 0 None 2 2 Human 6.1 pEC50 = 6.1 Functional
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 323 7 4 7 0.7 NC(c1csc([N+](=O)[O-])c1)P(=O)(O)CC[C@H](N)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4075877 163976 0 None 2 2 Human 6.1 pEC50 = 6.1 Functional
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 323 7 4 7 0.7 NC(c1csc([N+](=O)[O-])c1)P(=O)(O)CC[C@H](N)C(=O)O 10.1021/acs.jmedchem.7b01438
13401655 21843 1 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 211 2 1 3 2.5 Cc1cc(/C=C/c2ccccc2)nc(N)n1 10.1016/j.bmcl.2010.06.078
CHEMBL1209438 21843 1 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 211 2 1 3 2.5 Cc1cc(/C=C/c2ccccc2)nc(N)n1 10.1016/j.bmcl.2010.06.078
24780088 165688 0 None 3 2 Human 5.1 pEC50 = 5.1 Functional
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 317 7 5 5 0.4 N[C@@H](CCP(=O)(O)C(O)c1ccc(C(=O)O)cc1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4095462 165688 0 None 3 2 Human 5.1 pEC50 = 5.1 Functional
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 317 7 5 5 0.4 N[C@@H](CCP(=O)(O)C(O)c1ccc(C(=O)O)cc1)C(=O)O 10.1021/acs.jmedchem.7b01438
53374406 158282 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 258 2 1 3 3.4 CN(c1cccc(Cl)c1)c1n[nH]c2cccnc12 nan
CHEMBL3962592 158282 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 258 2 1 3 3.4 CN(c1cccc(Cl)c1)c1n[nH]c2cccnc12 nan
122196122 131034 0 None -41 2 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 414 3 1 4 4.9 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c2ccccc12 10.1016/j.bmcl.2015.10.013
CHEMBL3634444 131034 0 None -41 2 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 414 3 1 4 4.9 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c2ccccc12 10.1016/j.bmcl.2015.10.013
122419056 179292 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 401 4 2 7 3.9 FC1(F)CCN(Cc2nsc3cc(Nc4n[nH]c5cccnc45)cnc23)CC1 10.1021/acs.jmedchem.8b00994
CHEMBL4483525 179292 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 401 4 2 7 3.9 FC1(F)CCN(Cc2nsc3cc(Nc4n[nH]c5cccnc45)cnc23)CC1 10.1021/acs.jmedchem.8b00994
122419073 179564 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 307 3 2 5 4.2 c1cnc2c(Nc3ccc4c(C5CC5)nsc4c3)n[nH]c2c1 10.1021/acs.jmedchem.8b00994
CHEMBL4513386 179564 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 307 3 2 5 4.2 c1cnc2c(Nc3ccc4c(C5CC5)nsc4c3)n[nH]c2c1 10.1021/acs.jmedchem.8b00994
122419056 179292 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 401 4 2 7 3.9 FC1(F)CCN(Cc2nsc3cc(Nc4n[nH]c5cccnc45)cnc23)CC1 10.1021/acs.jmedchem.8b00994
CHEMBL4483525 179292 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 401 4 2 7 3.9 FC1(F)CCN(Cc2nsc3cc(Nc4n[nH]c5cccnc45)cnc23)CC1 10.1021/acs.jmedchem.8b00994
122419073 179564 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 307 3 2 5 4.2 c1cnc2c(Nc3ccc4c(C5CC5)nsc4c3)n[nH]c2c1 10.1021/acs.jmedchem.8b00994
CHEMBL4513386 179564 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 307 3 2 5 4.2 c1cnc2c(Nc3ccc4c(C5CC5)nsc4c3)n[nH]c2c1 10.1021/acs.jmedchem.8b00994
134189970 179111 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 307 4 2 5 4.0 CC(C)Cc1noc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
CHEMBL4475516 179111 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 307 4 2 5 4.0 CC(C)Cc1noc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
134189970 179111 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 307 4 2 5 4.0 CC(C)Cc1noc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
CHEMBL4475516 179111 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 307 4 2 5 4.0 CC(C)Cc1noc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
53374107 158884 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 295 2 2 5 2.1 CN1C(=O)COc2ccc(Nc3n[nH]c4cccnc34)cc21 nan
CHEMBL3967727 158884 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 295 2 2 5 2.1 CN1C(=O)COc2ccc(Nc3n[nH]c4cccnc34)cc21 nan
134198103 172244 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 312 3 2 5 3.7 CCn1nc(Cl)c2cc(Nc3n[nH]c4cccnc34)ccc21 10.1016/j.bmcl.2018.06.034
CHEMBL4239644 172244 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 312 3 2 5 3.7 CCn1nc(Cl)c2cc(Nc3n[nH]c4cccnc34)ccc21 10.1016/j.bmcl.2018.06.034
135126262 176362 0 None 7 2 Rat 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 385 3 1 5 3.1 Cc1nnc2ccc(C(=O)NC3CN(c4ncc(Cl)cc4F)C3)cc2c1C 10.1016/j.bmcl.2019.126678
CHEMBL4436022 176362 0 None 7 2 Rat 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 385 3 1 5 3.1 Cc1nnc2ccc(C(=O)NC3CN(c4ncc(Cl)cc4F)C3)cc2c1C 10.1016/j.bmcl.2019.126678
54670320 157238 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 379 5 1 5 4.9 O=C(Nc1ncc(SCc2ccc(Cl)cc2F)s1)c1ccccn1 nan
CHEMBL3954184 157238 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 379 5 1 5 4.9 O=C(Nc1ncc(SCc2ccc(Cl)cc2F)s1)c1ccccn1 nan
134198072 172617 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 361 3 2 6 2.8 Cn1nc(C(=O)N2CCCC2)c2ccc(Nc3n[nH]c4cccnc34)cc21 10.1016/j.bmcl.2018.06.034
CHEMBL4248724 172617 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 361 3 2 6 2.8 Cn1nc(C(=O)N2CCCC2)c2ccc(Nc3n[nH]c4cccnc34)cc21 10.1016/j.bmcl.2018.06.034
53495171 147279 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 411 5 1 6 3.6 O=C(Nc1ncc(S(=O)(=O)Cc2ccc(Cl)cc2F)s1)c1ccccn1 10.1016/j.bmcl.2016.05.029
CHEMBL3809990 147279 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 411 5 1 6 3.6 O=C(Nc1ncc(S(=O)(=O)Cc2ccc(Cl)cc2F)s1)c1ccccn1 10.1016/j.bmcl.2016.05.029
53495171 147279 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 411 5 1 6 3.6 O=C(Nc1ncc(S(=O)(=O)Cc2ccc(Cl)cc2F)s1)c1ccccn1 10.1016/j.bmcl.2016.05.029
CHEMBL3809990 147279 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 411 5 1 6 3.6 O=C(Nc1ncc(S(=O)(=O)Cc2ccc(Cl)cc2F)s1)c1ccccn1 10.1016/j.bmcl.2016.05.029
121231186 150534 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 309 2 2 5 2.4 CC1Oc2ccc(Nc3n[nH]c4cccnc34)cc2N(C)C1=O nan
CHEMBL3900822 150534 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 309 2 2 5 2.4 CC1Oc2ccc(Nc3n[nH]c4cccnc34)cc2N(C)C1=O nan
52914310 147240 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 393 5 1 5 3.3 O=C(Nc1ccn(S(=O)(=O)Cc2ccc(F)cc2Cl)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
CHEMBL3809447 147240 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 393 5 1 5 3.3 O=C(Nc1ccn(S(=O)(=O)Cc2ccc(F)cc2Cl)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
70696128 80987 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 299 2 0 3 4.7 Cc1nn(-c2ccccc2)c(C)c1-c1ccnc2ccccc12 10.1016/j.bmcl.2012.03.032
CHEMBL2023453 80987 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 299 2 0 3 4.7 Cc1nn(-c2ccccc2)c(C)c1-c1ccnc2ccccc12 10.1016/j.bmcl.2012.03.032
51003232 64668 0 None -1 2 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 387 5 2 5 4.3 COc1cc(NC(=O)c2cscn2)ccc1NC(=O)c1ccccc1Cl 10.1021/jm101271s
CHEMBL1672233 64668 0 None -1 2 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 387 5 2 5 4.3 COc1cc(NC(=O)c2cscn2)ccc1NC(=O)c1ccccc1Cl 10.1021/jm101271s
52914310 147240 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 393 5 1 5 3.3 O=C(Nc1ccn(S(=O)(=O)Cc2ccc(F)cc2Cl)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
CHEMBL3809447 147240 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 393 5 1 5 3.3 O=C(Nc1ccn(S(=O)(=O)Cc2ccc(F)cc2Cl)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
134198051 172639 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 378 5 2 7 3.5 Cn1nc(OCC2CCCCO2)c2ccc(Nc3n[nH]c4cccnc34)cc21 10.1016/j.bmcl.2018.06.034
CHEMBL4249099 172639 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 378 5 2 7 3.5 Cn1nc(OCC2CCCCO2)c2ccc(Nc3n[nH]c4cccnc34)cc21 10.1016/j.bmcl.2018.06.034
46918017 165488 0 None 2 2 Human 5.1 pEC50 = 5.1 Functional
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 378 9 5 8 0.8 CCOc1cc(C(O)P(=O)(O)CC[C@H](N)C(=O)O)cc([N+](=O)[O-])c1O 10.1021/acs.jmedchem.7b01438
CHEMBL4093305 165488 0 None 2 2 Human 5.1 pEC50 = 5.1 Functional
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 378 9 5 8 0.8 CCOc1cc(C(O)P(=O)(O)CC[C@H](N)C(=O)O)cc([N+](=O)[O-])c1O 10.1021/acs.jmedchem.7b01438
46197776 15128 0 None 1 3 Rat 5.1 pEC50 = 5.1 Functional
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 253 8 4 4 -0.1 N[C@@H](CCP(=O)(O)CCCC(=O)O)C(=O)O 10.1021/jm901523t
CHEMBL1093009 15128 0 None 1 3 Rat 5.1 pEC50 = 5.1 Functional
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 253 8 4 4 -0.1 N[C@@H](CCP(=O)(O)CCCC(=O)O)C(=O)O 10.1021/jm901523t
134189980 176769 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 305 3 2 5 4.1 c1cnc2c(Nc3ccc4c(C5CCC5)noc4c3)n[nH]c2c1 10.1021/acs.jmedchem.8b00994
CHEMBL4442185 176769 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 305 3 2 5 4.1 c1cnc2c(Nc3ccc4c(C5CCC5)noc4c3)n[nH]c2c1 10.1021/acs.jmedchem.8b00994
134190027 176379 0 None -1 2 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 322 3 2 6 3.8 CC(C)(C)Cc1noc2cc(Nc3n[nH]c4nccnc34)ccc12 10.1021/acs.jmedchem.8b00994
CHEMBL4436346 176379 0 None -1 2 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 322 3 2 6 3.8 CC(C)(C)Cc1noc2cc(Nc3n[nH]c4nccnc34)ccc12 10.1021/acs.jmedchem.8b00994
134189980 176769 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 305 3 2 5 4.1 c1cnc2c(Nc3ccc4c(C5CCC5)noc4c3)n[nH]c2c1 10.1021/acs.jmedchem.8b00994
CHEMBL4442185 176769 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 305 3 2 5 4.1 c1cnc2c(Nc3ccc4c(C5CCC5)noc4c3)n[nH]c2c1 10.1021/acs.jmedchem.8b00994
50902625 83967 0 None - 1 Rat 4.1 pEC50 = 4.1 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells coexpressing Gq/Gi and EAAC1 assessed as intracellular calcium production measured every 1.5 secs for 60 secs by Fluo-4-AM based fluorometryAgonist activity at rat mGlu4 receptor expressed in HEK293 cells coexpressing Gq/Gi and EAAC1 assessed as intracellular calcium production measured every 1.5 secs for 60 secs by Fluo-4-AM based fluorometry
ChEMBL 213 3 3 4 -1.2 N[C@]1(C(=O)O)C[C@@]1(F)CS(=O)(=O)O 10.1016/j.bmc.2012.06.006
CHEMBL2058381 83967 0 None - 1 Rat 4.1 pEC50 = 4.1 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells coexpressing Gq/Gi and EAAC1 assessed as intracellular calcium production measured every 1.5 secs for 60 secs by Fluo-4-AM based fluorometryAgonist activity at rat mGlu4 receptor expressed in HEK293 cells coexpressing Gq/Gi and EAAC1 assessed as intracellular calcium production measured every 1.5 secs for 60 secs by Fluo-4-AM based fluorometry
ChEMBL 213 3 3 4 -1.2 N[C@]1(C(=O)O)C[C@@]1(F)CS(=O)(=O)O 10.1016/j.bmc.2012.06.006
CHEMBL2079097 83967 0 None - 1 Rat 4.1 pEC50 = 4.1 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells coexpressing Gq/Gi and EAAC1 assessed as intracellular calcium production measured every 1.5 secs for 60 secs by Fluo-4-AM based fluorometryAgonist activity at rat mGlu4 receptor expressed in HEK293 cells coexpressing Gq/Gi and EAAC1 assessed as intracellular calcium production measured every 1.5 secs for 60 secs by Fluo-4-AM based fluorometry
ChEMBL 213 3 3 4 -1.2 N[C@]1(C(=O)O)C[C@@]1(F)CS(=O)(=O)O 10.1016/j.bmc.2012.06.006
134190027 176379 0 None -1 2 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 322 3 2 6 3.8 CC(C)(C)Cc1noc2cc(Nc3n[nH]c4nccnc34)ccc12 10.1021/acs.jmedchem.8b00994
CHEMBL4436346 176379 0 None -1 2 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 322 3 2 6 3.8 CC(C)(C)Cc1noc2cc(Nc3n[nH]c4nccnc34)ccc12 10.1021/acs.jmedchem.8b00994
1092658 34936 11 None 1 2 Rat 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 386 5 2 4 4.9 COc1cc(NC(=O)c2cccs2)ccc1NC(=O)c1ccccc1Cl 10.1021/jm101271s
CHEMBL1373422 34936 11 None 1 2 Rat 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 386 5 2 4 4.9 COc1cc(NC(=O)c2cccs2)ccc1NC(=O)c1ccccc1Cl 10.1021/jm101271s
136503374 163331 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 291 1 1 5 3.3 Cn1ccc2cc(-c3c/c(=N\O)c4ccccc4o3)ncc21 10.1021/acs.jmedchem.7b00991
CHEMBL4068295 163331 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 291 1 1 5 3.3 Cn1ccc2cc(-c3c/c(=N\O)c4ccccc4o3)ncc21 10.1021/acs.jmedchem.7b00991
134191541 187958 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 330 4 3 5 4.2 c1cnc2c(Nc3ccc4c(NC5CCC5)nccc4c3)n[nH]c2c1 10.1016/j.bmcl.2018.10.050
CHEMBL4761011 187958 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assayPositive allosteric modulator activity at human mGlu4 receptor/Gqi5 in presence of EC20 glutamate by calcium mobilization assay
ChEMBL 330 4 3 5 4.2 c1cnc2c(Nc3ccc4c(NC5CCC5)nccc4c3)n[nH]c2c1 10.1016/j.bmcl.2018.10.050
134198363 172409 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 264 2 2 5 2.6 Cn1ncc2cc(Nc3n[nH]c4cccnc34)ccc21 10.1016/j.bmcl.2018.06.034
CHEMBL4243630 172409 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 264 2 2 5 2.6 Cn1ncc2cc(Nc3n[nH]c4cccnc34)ccc21 10.1016/j.bmcl.2018.06.034
53374309 149411 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 371 4 2 5 5.2 Clc1cccc(Oc2ccc(Nc3n[nH]c4cccnc34)cc2Cl)n1 nan
CHEMBL3891609 149411 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 371 4 2 5 5.2 Clc1cccc(Oc2ccc(Nc3n[nH]c4cccnc34)cc2Cl)n1 nan
54670498 153030 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 455 6 1 6 4.6 CCc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1c(Cl)cccc1Cl nan
CHEMBL3920531 153030 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 455 6 1 6 4.6 CCc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1c(Cl)cccc1Cl nan
10656383 119095 1 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity against Metabotropic glutamate receptor 4 expressed in HEK 293 cells was evaluated by measuring total inositol phosphate accumulationAgonist activity against Metabotropic glutamate receptor 4 expressed in HEK 293 cells was evaluated by measuring total inositol phosphate accumulation
ChEMBL 217 3 4 4 -1.0 NC1(C(=O)O)C[C@H](C(=O)O)[C@@H](C(=O)O)C1 10.1021/jm970207b
CHEMBL329236 119095 1 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity against Metabotropic glutamate receptor 4 expressed in HEK 293 cells was evaluated by measuring total inositol phosphate accumulationAgonist activity against Metabotropic glutamate receptor 4 expressed in HEK 293 cells was evaluated by measuring total inositol phosphate accumulation
ChEMBL 217 3 4 4 -1.0 NC1(C(=O)O)C[C@H](C(=O)O)[C@@H](C(=O)O)C1 10.1021/jm970207b
137643759 165205 0 None -1 3 Human 5.1 pEC50 = 5.1 Functional
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 288 6 5 5 0.3 Nc1ccc(C(O)P(=O)(O)CC[C@H](N)C(=O)O)cc1 10.1021/acs.jmedchem.7b01438
CHEMBL4090312 165205 0 None -1 3 Human 5.1 pEC50 = 5.1 Functional
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 288 6 5 5 0.3 Nc1ccc(C(O)P(=O)(O)CC[C@H](N)C(=O)O)cc1 10.1021/acs.jmedchem.7b01438
137643759 165205 0 None -1 3 Human 5.1 pEC50 = 5.1 Functional
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 288 6 5 5 0.3 Nc1ccc(C(O)P(=O)(O)CC[C@H](N)C(=O)O)cc1 10.1021/acs.jmedchem.7b01438
CHEMBL4090312 165205 0 None -1 3 Human 5.1 pEC50 = 5.1 Functional
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 288 6 5 5 0.3 Nc1ccc(C(O)P(=O)(O)CC[C@H](N)C(=O)O)cc1 10.1021/acs.jmedchem.7b01438
1407 8860 42 None -281 7 Rat 5.1 pEC50 = 5.1 Functional
Metabotropic glutamate receptor 4 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 4 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 239 4 4 4 0.2 N[C@@H](c1ccc(c(c1)C(=O)O)C(=O)O)C(=O)O 10.1021/jm030967o
16062593 8860 42 None -281 7 Rat 5.1 pEC50 = 5.1 Functional
Metabotropic glutamate receptor 4 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 4 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 239 4 4 4 0.2 N[C@@H](c1ccc(c(c1)C(=O)O)C(=O)O)C(=O)O 10.1021/jm030967o
CHEMBL143210 8860 42 None -281 7 Rat 5.1 pEC50 = 5.1 Functional
Metabotropic glutamate receptor 4 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 4 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 239 4 4 4 0.2 N[C@@H](c1ccc(c(c1)C(=O)O)C(=O)O)C(=O)O 10.1021/jm030967o
1407 8860 42 None -281 7 Rat 5.1 pEC50 = 5.1 Functional
Stimulation od [3H]phosphatidylinositol accumulation by rat Metabotropic glutamate receptor 4 co-expressed with Gqi9 protein in HEK 293 cellsStimulation od [3H]phosphatidylinositol accumulation by rat Metabotropic glutamate receptor 4 co-expressed with Gqi9 protein in HEK 293 cells
ChEMBL 239 4 4 4 0.2 N[C@@H](c1ccc(c(c1)C(=O)O)C(=O)O)C(=O)O 10.1021/jm049092j
16062593 8860 42 None -281 7 Rat 5.1 pEC50 = 5.1 Functional
Stimulation od [3H]phosphatidylinositol accumulation by rat Metabotropic glutamate receptor 4 co-expressed with Gqi9 protein in HEK 293 cellsStimulation od [3H]phosphatidylinositol accumulation by rat Metabotropic glutamate receptor 4 co-expressed with Gqi9 protein in HEK 293 cells
ChEMBL 239 4 4 4 0.2 N[C@@H](c1ccc(c(c1)C(=O)O)C(=O)O)C(=O)O 10.1021/jm049092j
CHEMBL143210 8860 42 None -281 7 Rat 5.1 pEC50 = 5.1 Functional
Stimulation od [3H]phosphatidylinositol accumulation by rat Metabotropic glutamate receptor 4 co-expressed with Gqi9 protein in HEK 293 cellsStimulation od [3H]phosphatidylinositol accumulation by rat Metabotropic glutamate receptor 4 co-expressed with Gqi9 protein in HEK 293 cells
ChEMBL 239 4 4 4 0.2 N[C@@H](c1ccc(c(c1)C(=O)O)C(=O)O)C(=O)O 10.1021/jm049092j
46884710 14991 0 None -1 2 Rat 4.1 pEC50 = 4.1 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 275 7 5 4 -0.8 N[C@@H](CCP(=O)(O)CCP(=O)(O)O)C(=O)O 10.1021/jm901523t
CHEMBL1092244 14991 0 None -1 2 Rat 4.1 pEC50 = 4.1 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 275 7 5 4 -0.8 N[C@@H](CCP(=O)(O)CCP(=O)(O)O)C(=O)O 10.1021/jm901523t
54670322 157522 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 425 6 2 7 2.5 O=C(Nc1nc(CO)c(S(=O)(=O)Cc2c(F)cccc2F)s1)c1ccccn1 nan
CHEMBL3956361 157522 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 425 6 2 7 2.5 O=C(Nc1nc(CO)c(S(=O)(=O)Cc2c(F)cccc2F)s1)c1ccccn1 nan
122196108 131021 0 None -18 2 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 390 4 1 5 4.0 COc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(C)c2C1=O 10.1016/j.bmcl.2015.10.013
CHEMBL3634431 131021 0 None -18 2 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 390 4 1 5 4.0 COc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(C)c2C1=O 10.1016/j.bmcl.2015.10.013
122196099 131012 0 None -10 2 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 360 3 1 4 3.9 Cc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2ccccc2C1=O 10.1016/j.bmcl.2015.10.013
CHEMBL3634422 131012 0 None -10 2 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 360 3 1 4 3.9 Cc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2ccccc2C1=O 10.1016/j.bmcl.2015.10.013
53375183 156954 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 306 5 2 5 3.3 COc1ccc(Nc2n[nH]c3cccnc23)cc1OC(F)F nan
CHEMBL3951739 156954 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 306 5 2 5 3.3 COc1ccc(Nc2n[nH]c3cccnc23)cc1OC(F)F nan
162657826 187906 0 None 4 2 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 368 3 1 4 3.7 Cc1cc(N2C(=O)C3=C(CCCC3)C2=O)c(F)cc1NC(=O)c1ccco1 10.1016/j.bmcl.2020.127724
CHEMBL4760570 187906 0 None 4 2 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 368 3 1 4 3.7 Cc1cc(N2C(=O)C3=C(CCCC3)C2=O)c(F)cc1NC(=O)c1ccco1 10.1016/j.bmcl.2020.127724
51003234 64671 0 None 1 2 Rat 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 382 5 2 5 3.6 COc1cc(NC(=O)c2ccncn2)ccc1NC(=O)c1ccccc1Cl 10.1021/jm101271s
CHEMBL1672236 64671 0 None 1 2 Rat 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 382 5 2 5 3.6 COc1cc(NC(=O)c2ccncn2)ccc1NC(=O)c1ccccc1Cl 10.1021/jm101271s
53373880 149596 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 212 2 2 5 1.5 c1cnc2c(Nc3cncnc3)n[nH]c2c1 nan
CHEMBL3892995 149596 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 212 2 2 5 1.5 c1cnc2c(Nc3cncnc3)n[nH]c2c1 nan
46836562 7818 32 None - 1 Human 8.1 pEC50 = 8.1 Functional
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 283 2 2 5 3.2 c1ccc(nc1)Nc1sc2c(n1)c1c[nH]nc1CCC2 10.1021/jm200290z
6231 7818 32 None - 1 Human 8.1 pEC50 = 8.1 Functional
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 283 2 2 5 3.2 c1ccc(nc1)Nc1sc2c(n1)c1c[nH]nc1CCC2 10.1021/jm200290z
CHEMBL1830707 7818 32 None - 1 Human 8.1 pEC50 = 8.1 Functional
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 283 2 2 5 3.2 c1ccc(nc1)Nc1sc2c(n1)c1c[nH]nc1CCC2 10.1021/jm200290z
136415539 164764 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
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 457 5 1 7 5.1 O/N=c1\cc(-c2cc3sccc3cn2)oc2ccc(OCCN3CCC(F)(F)CC3)cc12 10.1021/acs.jmedchem.7b00991
CHEMBL4085101 164764 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
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 457 5 1 7 5.1 O/N=c1\cc(-c2cc3sccc3cn2)oc2ccc(OCCN3CCC(F)(F)CC3)cc12 10.1021/acs.jmedchem.7b00991
57765594 166269 0 None 4 2 Human 6.1 pEC50 = 6.1 Functional
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 334 7 5 7 0.4 N[C@@H](CCP(=O)(O)C(O)c1cc([N+](=O)[O-])ccc1O)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4101745 166269 0 None 4 2 Human 6.1 pEC50 = 6.1 Functional
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 334 7 5 7 0.4 N[C@@H](CCP(=O)(O)C(O)c1cc([N+](=O)[O-])ccc1O)C(=O)O 10.1021/acs.jmedchem.7b01438
46898088 9145 6 None -11 8 Human 6.1 pEC50 = 6.1 Functional
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 364 8 5 8 0.4 COc1cc(cc(c1O)[N+](=O)[O-])C(P(=O)(CC[C@@H](C(=O)O)N)O)O 10.1021/acs.jmedchem.7b01438
6739 9145 6 None -11 8 Human 6.1 pEC50 = 6.1 Functional
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 364 8 5 8 0.4 COc1cc(cc(c1O)[N+](=O)[O-])C(P(=O)(CC[C@@H](C(=O)O)N)O)O 10.1021/acs.jmedchem.7b01438
CHEMBL3114672 9145 6 None -11 8 Human 6.1 pEC50 = 6.1 Functional
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 364 8 5 8 0.4 COc1cc(cc(c1O)[N+](=O)[O-])C(P(=O)(CC[C@@H](C(=O)O)N)O)O 10.1021/acs.jmedchem.7b01438
122197951 167513 0 None 7 3 Rat 6.1 pEC50 = 6.1 Functional
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 415 9 5 6 1.2 N[C@H](CCP(=O)(O)C(O)c1ccc(OCC(=O)O)c(C(F)(F)F)c1)C(=O)O nan
CHEMBL4113862 167513 0 None 7 3 Rat 6.1 pEC50 = 6.1 Functional
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 415 9 5 6 1.2 N[C@H](CCP(=O)(O)C(O)c1ccc(OCC(=O)O)c(C(F)(F)F)c1)C(=O)O nan
70696138 81018 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 400 3 0 6 3.9 O=C(Oc1ccc2c(-c3cnn(-c4ccccc4)c3)ccnc2c1)N1CCOCC1 10.1016/j.bmcl.2012.03.032
CHEMBL2023626 81018 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 400 3 0 6 3.9 O=C(Oc1ccc2c(-c3cnn(-c4ccccc4)c3)ccnc2c1)N1CCOCC1 10.1016/j.bmcl.2012.03.032
140838160 172557 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 379 3 2 6 2.8 Cn1nc(C(=O)N2CC[C@@H](F)C2)c2ccc(Nc3n[nH]c4cccnc34)cc21 10.1016/j.bmcl.2018.06.034
CHEMBL4247308 172557 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 379 3 2 6 2.8 Cn1nc(C(=O)N2CC[C@@H](F)C2)c2ccc(Nc3n[nH]c4cccnc34)cc21 10.1016/j.bmcl.2018.06.034
69938827 150351 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 416 5 1 8 4.5 Clc1cc(N(c2ncccn2)c2n[nH]c3cccnc23)ccc1Oc1ncccn1 nan
CHEMBL3899239 150351 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 416 5 1 8 4.5 Clc1cc(N(c2ncccn2)c2n[nH]c3cccnc23)ccc1Oc1ncccn1 nan
46836497 72302 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 283 2 2 5 3.1 Cc1cccc(Nc2nc3c(s2)CCc2n[nH]cc2-3)n1 10.1021/jm200290z
CHEMBL1830705 72302 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 283 2 2 5 3.1 Cc1cccc(Nc2nc3c(s2)CCc2n[nH]cc2-3)n1 10.1021/jm200290z
53374305 152110 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 306 3 2 5 2.2 CS(=O)(=O)c1cc(Nc2n[nH]c3cccnc23)ccc1F nan
CHEMBL3913382 152110 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 306 3 2 5 2.2 CS(=O)(=O)c1cc(Nc2n[nH]c3cccnc23)ccc1F nan
127047065 146386 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 146386 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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
51003283 64677 0 None 1 2 Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 365 4 2 3 4.5 Cc1ccccc1C(=O)Nc1ccc(NC(=O)c2ccccn2)cc1Cl 10.1021/jm101271s
CHEMBL1672242 64677 0 None 1 2 Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 365 4 2 3 4.5 Cc1ccccc1C(=O)Nc1ccc(NC(=O)c2ccccn2)cc1Cl 10.1021/jm101271s
53375178 156846 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 229 2 2 4 2.2 Fc1cncc(Nc2n[nH]c3cccnc23)c1 nan
CHEMBL3950739 156846 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 229 2 2 4 2.2 Fc1cncc(Nc2n[nH]c3cccnc23)c1 nan
162643634 188534 0 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 392 3 1 4 4.4 Cc1ccc2c(c1)C(=O)N(c1cc(C)c(NC(=O)c3occc3C)cc1F)C2=O 10.1016/j.bmcl.2020.127724
CHEMBL4777502 188534 0 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human mGluR4 by calcium mobilization assayPositive allosteric modulation of human mGluR4 by calcium mobilization assay
ChEMBL 392 3 1 4 4.4 Cc1ccc2c(c1)C(=O)N(c1cc(C)c(NC(=O)c3occc3C)cc1F)C2=O 10.1016/j.bmcl.2020.127724
53373666 156324 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 269 2 2 4 3.2 N#Cc1ccc(Nc2n[nH]c3cccnc23)cc1Cl nan
CHEMBL3946663 156324 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 269 2 2 4 3.2 N#Cc1ccc(Nc2n[nH]c3cccnc23)cc1Cl nan
54670594 154253 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 409 5 1 6 3.4 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccc(F)c(F)c1 nan
CHEMBL3930344 154253 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 409 5 1 6 3.4 Cc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccc(F)c(F)c1 nan
54670409 149937 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 455 6 1 6 4.6 CCc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccc(Cl)cc1Cl nan
CHEMBL3895941 149937 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 455 6 1 6 4.6 CCc1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)Cc1ccc(Cl)cc1Cl nan
11708219 176151 0 None 1 2 Rat 5.0 pEC50 = 5.0 Functional
Agonist activity at rat recombinant mGluR4 expressed in BHK cellsAgonist activity at rat recombinant mGluR4 expressed in BHK cells
ChEMBL 195 3 4 3 -1.0 NC(C(=O)O)[C@H]1C[C@@H]1P(=O)(O)O 10.1016/j.bmc.2007.02.040
CHEMBL442076 176151 0 None 1 2 Rat 5.0 pEC50 = 5.0 Functional
Agonist activity at rat recombinant mGluR4 expressed in BHK cellsAgonist activity at rat recombinant mGluR4 expressed in BHK cells
ChEMBL 195 3 4 3 -1.0 NC(C(=O)O)[C@H]1C[C@@H]1P(=O)(O)O 10.1016/j.bmc.2007.02.040
44406220 78948 1 None 1 2 Rat 5.0 pEC50 = 5.0 Functional
Functional activity at rat mGluR4Functional activity at rat mGluR4
ChEMBL 195 3 4 3 -1.0 N[C@H](C(=O)O)[C@H]1C[C@@H]1P(=O)(O)O 10.1016/j.bmcl.2005.09.014
CHEMBL197976 78948 1 None 1 2 Rat 5.0 pEC50 = 5.0 Functional
Functional activity at rat mGluR4Functional activity at rat mGluR4
ChEMBL 195 3 4 3 -1.0 N[C@H](C(=O)O)[C@H]1C[C@@H]1P(=O)(O)O 10.1016/j.bmcl.2005.09.014
49862694 21904 2 None - 1 Human 5.0 pEC50 = 5.0 Functional
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 187 2 1 4 1.8 Nc1nccc(/C=C/c2ccco2)n1 10.1016/j.bmcl.2010.06.078
CHEMBL1209742 21904 2 None - 1 Human 5.0 pEC50 = 5.0 Functional
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 187 2 1 4 1.8 Nc1nccc(/C=C/c2ccco2)n1 10.1016/j.bmcl.2010.06.078
1310 9095 110 None -426 17 Rat 5.0 pEC50 = 5.0 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
1369 9095 110 None -426 17 Rat 5.0 pEC50 = 5.0 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
33032 9095 110 None -426 17 Rat 5.0 pEC50 = 5.0 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
44272391 9095 110 None -426 17 Rat 5.0 pEC50 = 5.0 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
88747398 9095 110 None -426 17 Rat 5.0 pEC50 = 5.0 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
CHEMBL575060 9095 110 None -426 17 Rat 5.0 pEC50 = 5.0 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
DB00142 9095 110 None -426 17 Rat 5.0 pEC50 = 5.0 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
134191981 172369 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 292 3 2 5 3.4 CCn1nc(C)c2cc(Nc3n[nH]c4cccnc34)ccc21 10.1016/j.bmcl.2018.06.034
CHEMBL4242608 172369 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 292 3 2 5 3.4 CCn1nc(C)c2cc(Nc3n[nH]c4cccnc34)ccc21 10.1016/j.bmcl.2018.06.034
145985523 172472 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 346 3 2 5 3.7 Cn1nc(CC(F)(F)F)c2ccc(Nc3n[nH]c4cccnc34)cc21 10.1016/j.bmcl.2018.06.034
CHEMBL4245306 172472 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 346 3 2 5 3.7 Cn1nc(CC(F)(F)F)c2ccc(Nc3n[nH]c4cccnc34)cc21 10.1016/j.bmcl.2018.06.034
127046557 146505 3 None 42 2 Human 7.0 pEC50 = 7.0 Functional
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 146505 3 None 42 2 Human 7.0 pEC50 = 7.0 Functional
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
45101485 205354 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Allosteric modulator activity at human mGlu4 receptor expressed in CHO cells coexpressing Gqi5 assessed as effect on calcium fluxAllosteric modulator activity at human mGlu4 receptor expressed in CHO cells coexpressing Gqi5 assessed as effect on calcium flux
ChEMBL 314 3 2 2 3.2 NC(=O)[C@@H]1CCCC[C@@H]1C(=O)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2009.07.072
CHEMBL578358 205354 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Allosteric modulator activity at human mGlu4 receptor expressed in CHO cells coexpressing Gqi5 assessed as effect on calcium fluxAllosteric modulator activity at human mGlu4 receptor expressed in CHO cells coexpressing Gqi5 assessed as effect on calcium flux
ChEMBL 314 3 2 2 3.2 NC(=O)[C@@H]1CCCC[C@@H]1C(=O)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2009.07.072
122197959 167163 0 None 15 2 Rat 6.0 pEC50 = 6.0 Functional
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 361 9 5 6 0.6 CC(Oc1ccc(C(O)P(=O)(O)CC[C@@H](N)C(=O)O)cc1)C(=O)O nan
CHEMBL4111159 167163 0 None 15 2 Rat 6.0 pEC50 = 6.0 Functional
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 361 9 5 6 0.6 CC(Oc1ccc(C(O)P(=O)(O)CC[C@@H](N)C(=O)O)cc1)C(=O)O nan
70683529 81014 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 358 3 0 5 4.1 CN(C)C(=O)Oc1ccc2c(-c3cnn(-c4ccccc4)c3)ccnc2c1 10.1016/j.bmcl.2012.03.032
CHEMBL2023622 81014 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysisPositive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization by FLIPR analysis
ChEMBL 358 3 0 5 4.1 CN(C)C(=O)Oc1ccc2c(-c3cnn(-c4ccccc4)c3)ccnc2c1 10.1016/j.bmcl.2012.03.032
135126270 177385 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 367 3 1 5 2.9 Cc1nnc2ccc(C(=O)NC3CN(c4ncccc4Cl)C3)cc2c1C 10.1016/j.bmcl.2019.126678
CHEMBL4450773 177385 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization incubated with EC20 ACh for 140 secs and subsequent EC80 Ach addition further incubated for 120 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 367 3 1 5 2.9 Cc1nnc2ccc(C(=O)NC3CN(c4ncccc4Cl)C3)cc2c1C 10.1016/j.bmcl.2019.126678
54670406 151927 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 433 6 1 6 4.6 CC(C)c1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)C(C)c1ccccc1F nan
CHEMBL3912127 151927 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 433 6 1 6 4.6 CC(C)c1nc(NC(=O)c2ccccn2)sc1S(=O)(=O)C(C)c1ccccc1F nan
51003283 64677 0 None -1 2 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 365 4 2 3 4.5 Cc1ccccc1C(=O)Nc1ccc(NC(=O)c2ccccn2)cc1Cl 10.1021/jm101271s
CHEMBL1672242 64677 0 None -1 2 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 365 4 2 3 4.5 Cc1ccccc1C(=O)Nc1ccc(NC(=O)c2ccccn2)cc1Cl 10.1021/jm101271s
1410 9054 48 None -1 8 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm901523t
1412 9054 48 None -1 8 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm901523t
179394 9054 48 None -1 8 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm901523t
57689795 9054 48 None -1 8 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm901523t
CHEMBL33567 9054 48 None -1 8 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation countingAgonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm901523t
45484621 203998 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Allosteric modulator activity at human mGlu4 receptor expressed in CHO cells coexpressing Gqi5 assessed as effect on calcium fluxAllosteric modulator activity at human mGlu4 receptor expressed in CHO cells coexpressing Gqi5 assessed as effect on calcium flux
ChEMBL 356 5 2 2 4.3 CCCNC(=O)[C@@H]1CCCC[C@@H]1C(=O)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2009.07.072
CHEMBL568252 203998 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Allosteric modulator activity at human mGlu4 receptor expressed in CHO cells coexpressing Gqi5 assessed as effect on calcium fluxAllosteric modulator activity at human mGlu4 receptor expressed in CHO cells coexpressing Gqi5 assessed as effect on calcium flux
ChEMBL 356 5 2 2 4.3 CCCNC(=O)[C@@H]1CCCC[C@@H]1C(=O)Nc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2009.07.072
53373881 152383 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 261 2 2 4 3.3 c1ccc2ncc(Nc3n[nH]c4cccnc34)cc2c1 nan
CHEMBL3915530 152383 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 261 2 2 4 3.3 c1ccc2ncc(Nc3n[nH]c4cccnc34)cc2c1 nan
134190211 182580 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 322 5 2 6 4.1 CCC(CC)c1noc2cc(Nc3n[nH]c4nccnc34)ccc12 10.1021/acs.jmedchem.8b00994
CHEMBL4584387 182580 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 322 5 2 6 4.1 CCC(CC)c1noc2cc(Nc3n[nH]c4nccnc34)ccc12 10.1021/acs.jmedchem.8b00994
1092661 36328 12 None 1 2 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 370 5 2 4 4.4 COc1cc(NC(=O)c2ccco2)ccc1NC(=O)c1ccccc1Cl 10.1021/jm101271s
CHEMBL1385271 36328 12 None 1 2 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 370 5 2 4 4.4 COc1cc(NC(=O)c2ccco2)ccc1NC(=O)c1ccccc1Cl 10.1021/jm101271s
137655963 165802 0 None 1 4 Human 5.0 pEC50 = 5.0 Functional
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 352 7 5 7 0.5 N[C@@H](CCP(=O)(O)[C@@H](O)c1cc(F)c(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4096644 165802 0 None 1 4 Human 5.0 pEC50 = 5.0 Functional
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 352 7 5 7 0.5 N[C@@H](CCP(=O)(O)[C@@H](O)c1cc(F)c(O)c([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
134190211 182580 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 322 5 2 6 4.1 CCC(CC)c1noc2cc(Nc3n[nH]c4nccnc34)ccc12 10.1021/acs.jmedchem.8b00994
CHEMBL4584387 182580 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization preincubated for 142 secs followed by EC20 glutamate addition and subsequent EC80 glutamate addition after 147 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 322 5 2 6 4.1 CCC(CC)c1noc2cc(Nc3n[nH]c4nccnc34)ccc12 10.1021/acs.jmedchem.8b00994
122197944 167002 0 None 38 3 Rat 6.0 pEC50 = 6.0 Functional
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 345 9 5 5 0.8 N[C@H](CCP(=O)(O)C(O)c1ccc(CCC(=O)O)cc1)C(=O)O nan
CHEMBL4109748 167002 0 None 38 3 Rat 6.0 pEC50 = 6.0 Functional
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 345 9 5 5 0.8 N[C@H](CCP(=O)(O)C(O)c1ccc(CCC(=O)O)cc1)C(=O)O nan
137633977 163229 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 302 1 1 4 4.2 Cc1ccc2oc(-c3cc4ccccc4cn3)c/c(=N\O)c2c1 10.1021/acs.jmedchem.7b00991
CHEMBL4067152 163229 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 302 1 1 4 4.2 Cc1ccc2oc(-c3cc4ccccc4cn3)c/c(=N\O)c2c1 10.1021/acs.jmedchem.7b00991
127025550 144607 0 None 1 2 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human mGlu4 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu4 receptor by cell based calcium mobilization
ChEMBL 415 3 1 5 4.3 Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3759867 144607 0 None 1 2 Human 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of human mGlu4 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu4 receptor by cell based calcium mobilization
ChEMBL 415 3 1 5 4.3 Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
136415548 165493 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
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 430 5 1 7 3.6 CN1CCN(CCOc2ccc3oc(-c4cc5ccccc5cn4)c/c(=N\O)c3c2)CC1 10.1021/acs.jmedchem.7b00991
CHEMBL4093353 165493 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
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 430 5 1 7 3.6 CN1CCN(CCOc2ccc3oc(-c4cc5ccccc5cn4)c/c(=N\O)c3c2)CC1 10.1021/acs.jmedchem.7b00991
52934741 156861 0 None - 1 Human 5.0 pEC50 = 5 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 342 4 1 6 2.1 Cc1ccc(S(=O)(=O)n2cc(NC(=O)c3ccccn3)cn2)cc1 nan
CHEMBL3950853 156861 0 None - 1 Human 5.0 pEC50 = 5 Functional
Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Glutamate Receptor Activity: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 342 4 1 6 2.1 Cc1ccc(S(=O)(=O)n2cc(NC(=O)c3ccccn3)cn2)cc1 nan
134192068 172348 0 None - 1 Human 5.0 pEC50 = 5 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 306 3 2 5 3.9 Cc1nn(C(C)C)c2cc(Nc3n[nH]c4cccnc34)ccc12 10.1016/j.bmcl.2018.06.034
CHEMBL4242145 172348 0 None - 1 Human 5.0 pEC50 = 5 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 306 3 2 5 3.9 Cc1nn(C(C)C)c2cc(Nc3n[nH]c4cccnc34)ccc12 10.1016/j.bmcl.2018.06.034
46869940 64669 4 None -1 2 Human 7.0 pEC50 = 7 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 381 5 2 4 4.2 COc1cc(NC(=O)c2ccccn2)ccc1NC(=O)c1ccccc1Cl 10.1021/jm101271s
CHEMBL1672234 64669 4 None -1 2 Human 7.0 pEC50 = 7 Functional
Positive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilizationPositive allosteric modulation of human mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization
ChEMBL 381 5 2 4 4.2 COc1cc(NC(=O)c2ccccn2)ccc1NC(=O)c1ccccc1Cl 10.1021/jm101271s
49865399 22721 0 None - 1 Human 6.0 pEC50 = 6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilization
ChEMBL 402 5 1 5 3.2 CN(c1ccccc1Cl)S(=O)(=O)c1ccc(NC(=O)c2ccncn2)cc1 10.1016/j.bmcl.2010.07.007
CHEMBL1223314 22721 0 None - 1 Human 6.0 pEC50 = 6 Functional
Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu4 receptor expressed in CHO cells assessed as potentiation of glutamate-induced calcium mobilization
ChEMBL 402 5 1 5 3.2 CN(c1ccccc1Cl)S(=O)(=O)c1ccc(NC(=O)c2ccncn2)cc1 10.1016/j.bmcl.2010.07.007
88063541 159051 0 None - 1 Human 5.0 pEC50 = 5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 246 2 2 5 2.1 Clc1cncc(Nc2n[nH]c3cccnc23)n1 nan
CHEMBL3969227 159051 0 None - 1 Human 5.0 pEC50 = 5 Functional
Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured.
ChEMBL 246 2 2 5 2.1 Clc1cncc(Nc2n[nH]c3cccnc23)n1 nan
44328753 214533 0 None -346 6 Human 5.0 pIC50 = 5 Functional
Antagonistic activity against metabotropic glutamate receptor 4 (mGluR4) was evaluatedAntagonistic activity against metabotropic glutamate receptor 4 (mGluR4) was evaluated
ChEMBL 409 8 3 4 4.2 CCCC[C@@H]1[C@H](C(=O)O)[C@H]1C(N)(CC1c2ccccc2Oc2ccccc21)C(=O)O 10.1016/s0960-894x(98)00510-1
CHEMBL95868 214533 0 None -346 6 Human 5.0 pIC50 = 5 Functional
Antagonistic activity against metabotropic glutamate receptor 4 (mGluR4) was evaluatedAntagonistic activity against metabotropic glutamate receptor 4 (mGluR4) was evaluated
ChEMBL 409 8 3 4 4.2 CCCC[C@@H]1[C@H](C(=O)O)[C@H]1C(N)(CC1c2ccccc2Oc2ccccc21)C(=O)O 10.1016/s0960-894x(98)00510-1
10456810 114656 0 None -91 5 Human 4.9 pIC50 = 4.9 Functional
Antagonistic activity against metabotropic glutamate receptor 4 (mGluR4) was evaluatedAntagonistic activity against metabotropic glutamate receptor 4 (mGluR4) was evaluated
ChEMBL 457 8 3 4 4.7 NC(CC1c2ccccc2Oc2ccccc21)(C(=O)O)[C@H]1[C@H](CCc2ccccc2)[C@@H]1C(=O)O 10.1016/s0960-894x(98)00510-1
CHEMBL319279 114656 0 None -91 5 Human 4.9 pIC50 = 4.9 Functional
Antagonistic activity against metabotropic glutamate receptor 4 (mGluR4) was evaluatedAntagonistic activity against metabotropic glutamate receptor 4 (mGluR4) was evaluated
ChEMBL 457 8 3 4 4.7 NC(CC1c2ccccc2Oc2ccccc21)(C(=O)O)[C@H]1[C@H](CCc2ccccc2)[C@@H]1C(=O)O 10.1016/s0960-894x(98)00510-1
44329031 115051 0 None -102 7 Human 4.9 pIC50 = 4.9 Functional
Antagonistic activity against metabotropic glutamate receptor 4 (mGluR4) was evaluatedAntagonistic activity against metabotropic glutamate receptor 4 (mGluR4) was evaluated
ChEMBL 437 10 3 4 5.0 CCCCCC[C@@H]1[C@H](C(=O)O)[C@H]1C(N)(CC1c2ccccc2Oc2ccccc21)C(=O)O 10.1016/s0960-894x(98)00510-1
CHEMBL319732 115051 0 None -102 7 Human 4.9 pIC50 = 4.9 Functional
Antagonistic activity against metabotropic glutamate receptor 4 (mGluR4) was evaluatedAntagonistic activity against metabotropic glutamate receptor 4 (mGluR4) was evaluated
ChEMBL 437 10 3 4 5.0 CCCCCC[C@@H]1[C@H](C(=O)O)[C@H]1C(N)(CC1c2ccccc2Oc2ccccc21)C(=O)O 10.1016/s0960-894x(98)00510-1
44329029 170300 0 None -9 6 Human 4.7 pIC50 = 4.7 Functional
Antagonistic activity against metabotropic glutamate receptor 4 (mGluR4) was evaluatedAntagonistic activity against metabotropic glutamate receptor 4 (mGluR4) was evaluated
ChEMBL 479 13 3 4 6.2 CCCCCCCCC[C@@H]1[C@H](C(=O)O)[C@H]1C(N)(CC1c2ccccc2Oc2ccccc21)C(=O)O 10.1016/s0960-894x(98)00510-1
CHEMBL420262 170300 0 None -9 6 Human 4.7 pIC50 = 4.7 Functional
Antagonistic activity against metabotropic glutamate receptor 4 (mGluR4) was evaluatedAntagonistic activity against metabotropic glutamate receptor 4 (mGluR4) was evaluated
ChEMBL 479 13 3 4 6.2 CCCCCCCCC[C@@H]1[C@H](C(=O)O)[C@H]1C(N)(CC1c2ccccc2Oc2ccccc21)C(=O)O 10.1016/s0960-894x(98)00510-1
1378 9195 54 None -2818 14 Human 4.7 pIC50 = 4.7 Functional
Antagonistic activity against metabotropic glutamate receptor 4 (mGluR4) was evaluatedAntagonistic activity against metabotropic glutamate receptor 4 (mGluR4) was evaluated
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1016/s0960-894x(98)00510-1
1399 9195 54 None -2818 14 Human 4.7 pIC50 = 4.7 Functional
Antagonistic activity against metabotropic glutamate receptor 4 (mGluR4) was evaluatedAntagonistic activity against metabotropic glutamate receptor 4 (mGluR4) was evaluated
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1016/s0960-894x(98)00510-1
9819927 9195 54 None -2818 14 Human 4.7 pIC50 = 4.7 Functional
Antagonistic activity against metabotropic glutamate receptor 4 (mGluR4) was evaluatedAntagonistic activity against metabotropic glutamate receptor 4 (mGluR4) was evaluated
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1016/s0960-894x(98)00510-1
CHEMBL432038 9195 54 None -2818 14 Human 4.7 pIC50 = 4.7 Functional
Antagonistic activity against metabotropic glutamate receptor 4 (mGluR4) was evaluatedAntagonistic activity against metabotropic glutamate receptor 4 (mGluR4) was evaluated
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1016/s0960-894x(98)00510-1
57393245 75697 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as inhibition of EC80 glutamate-induced calcium mobilization after 2.5 minsAntagonist activity at human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as inhibition of EC80 glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 315 4 0 3 4.0 O=C(COc1ccc(C(F)(F)F)cc1)c1ccc(Cl)nc1 10.1016/j.bmcl.2011.09.131
CHEMBL1922756 75697 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as inhibition of EC80 glutamate-induced calcium mobilization after 2.5 minsAntagonist activity at human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as inhibition of EC80 glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 315 4 0 3 4.0 O=C(COc1ccc(C(F)(F)F)cc1)c1ccc(Cl)nc1 10.1016/j.bmcl.2011.09.131
44329042 175862 0 None -794 5 Human 4.2 pIC50 = 4.2 Functional
Antagonistic activity against metabotropic glutamate receptor 4 (mGluR4) was evaluatedAntagonistic activity against metabotropic glutamate receptor 4 (mGluR4) was evaluated
ChEMBL 381 6 3 4 3.5 CC[C@@H]1[C@H](C(=O)O)[C@H]1C(N)(CC1c2ccccc2Oc2ccccc21)C(=O)O 10.1016/s0960-894x(98)00510-1
CHEMBL439775 175862 0 None -794 5 Human 4.2 pIC50 = 4.2 Functional
Antagonistic activity against metabotropic glutamate receptor 4 (mGluR4) was evaluatedAntagonistic activity against metabotropic glutamate receptor 4 (mGluR4) was evaluated
ChEMBL 381 6 3 4 3.5 CC[C@@H]1[C@H](C(=O)O)[C@H]1C(N)(CC1c2ccccc2Oc2ccccc21)C(=O)O 10.1016/s0960-894x(98)00510-1
44328850 214830 0 None -63 4 Human 4.2 pIC50 = 4.2 Functional
Antagonistic activity against metabotropic glutamate receptor 4 (mGluR4) was evaluatedAntagonistic activity against metabotropic glutamate receptor 4 (mGluR4) was evaluated
ChEMBL 367 5 3 4 3.1 C[C@@H]1[C@H](C(=O)O)[C@H]1C(N)(CC1c2ccccc2Oc2ccccc21)C(=O)O 10.1016/s0960-894x(98)00510-1
CHEMBL97574 214830 0 None -63 4 Human 4.2 pIC50 = 4.2 Functional
Antagonistic activity against metabotropic glutamate receptor 4 (mGluR4) was evaluatedAntagonistic activity against metabotropic glutamate receptor 4 (mGluR4) was evaluated
ChEMBL 367 5 3 4 3.1 C[C@@H]1[C@H](C(=O)O)[C@H]1C(N)(CC1c2ccccc2Oc2ccccc21)C(=O)O 10.1016/s0960-894x(98)00510-1
57391480 75696 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as inhibition of EC80 glutamate-induced calcium mobilization after 2.5 minsAntagonist activity at human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as inhibition of EC80 glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 325 4 0 3 3.8 O=C(COc1cccc(Br)c1)c1ccc(Cl)nc1 10.1016/j.bmcl.2011.09.131
CHEMBL1922750 75696 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as inhibition of EC80 glutamate-induced calcium mobilization after 2.5 minsAntagonist activity at human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as inhibition of EC80 glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 325 4 0 3 3.8 O=C(COc1cccc(Br)c1)c1ccc(Cl)nc1 10.1016/j.bmcl.2011.09.131
57396719 75698 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as inhibition of EC80 glutamate-induced calcium mobilization after 2.5 minsAntagonist activity at human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as inhibition of EC80 glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 324 5 0 4 4.1 O=C(COc1ccccc1-c1ccccn1)c1ccc(Cl)nc1 10.1016/j.bmcl.2011.09.131
CHEMBL1922760 75698 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as inhibition of EC80 glutamate-induced calcium mobilization after 2.5 minsAntagonist activity at human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as inhibition of EC80 glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 324 5 0 4 4.1 O=C(COc1ccccc1-c1ccccn1)c1ccc(Cl)nc1 10.1016/j.bmcl.2011.09.131
54764842 75695 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as inhibition of EC80 glutamate-induced calcium mobilization after 2.5 minsAntagonist activity at human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as inhibition of EC80 glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 325 4 0 3 3.8 O=C(COc1ccccc1Br)c1ccc(Cl)nc1 10.1016/j.bmcl.2011.09.131
CHEMBL1922728 75695 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as inhibition of EC80 glutamate-induced calcium mobilization after 2.5 minsAntagonist activity at human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as inhibition of EC80 glutamate-induced calcium mobilization after 2.5 mins
ChEMBL 325 4 0 3 3.8 O=C(COc1ccccc1Br)c1ccc(Cl)nc1 10.1016/j.bmcl.2011.09.131
44329033 214759 0 None -218 5 Human 5.1 pIC50 = 5.1 Functional
Antagonistic activity against metabotropic glutamate receptor 4 (mGluR4) was evaluatedAntagonistic activity against metabotropic glutamate receptor 4 (mGluR4) was evaluated
ChEMBL 409 7 3 4 4.1 CC(C)C[C@@H]1[C@H](C(=O)O)[C@H]1C(N)(CC1c2ccccc2Oc2ccccc21)C(=O)O 10.1016/s0960-894x(98)00510-1
CHEMBL97200 214759 0 None -218 5 Human 5.1 pIC50 = 5.1 Functional
Antagonistic activity against metabotropic glutamate receptor 4 (mGluR4) was evaluatedAntagonistic activity against metabotropic glutamate receptor 4 (mGluR4) was evaluated
ChEMBL 409 7 3 4 4.1 CC(C)C[C@@H]1[C@H](C(=O)O)[C@H]1C(N)(CC1c2ccccc2Oc2ccccc21)C(=O)O 10.1016/s0960-894x(98)00510-1
44329032 119321 0 None -93 5 Human 5.0 pIC50 = 5.0 Functional
Antagonistic activity against metabotropic glutamate receptor 4 (mGluR4) was evaluatedAntagonistic activity against metabotropic glutamate receptor 4 (mGluR4) was evaluated
ChEMBL 423 9 3 4 4.6 CCCCC[C@@H]1[C@H](C(=O)O)[C@H]1C(N)(CC1c2ccccc2Oc2ccccc21)C(=O)O 10.1016/s0960-894x(98)00510-1
CHEMBL329920 119321 0 None -93 5 Human 5.0 pIC50 = 5.0 Functional
Antagonistic activity against metabotropic glutamate receptor 4 (mGluR4) was evaluatedAntagonistic activity against metabotropic glutamate receptor 4 (mGluR4) was evaluated
ChEMBL 423 9 3 4 4.6 CCCCC[C@@H]1[C@H](C(=O)O)[C@H]1C(N)(CC1c2ccccc2Oc2ccccc21)C(=O)O 10.1016/s0960-894x(98)00510-1
1310 9095 110 None -1513 17 Human 4.8 pKi = 4.8 Functional
Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm000007r
1369 9095 110 None -1513 17 Human 4.8 pKi = 4.8 Functional
Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm000007r
33032 9095 110 None -1513 17 Human 4.8 pKi = 4.8 Functional
Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm000007r
44272391 9095 110 None -1513 17 Human 4.8 pKi = 4.8 Functional
Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm000007r
88747398 9095 110 None -1513 17 Human 4.8 pKi = 4.8 Functional
Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm000007r
CHEMBL575060 9095 110 None -1513 17 Human 4.8 pKi = 4.8 Functional
Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm000007r
DB00142 9095 110 None -1513 17 Human 4.8 pKi = 4.8 Functional
Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm000007r
10197984 9199 44 None -7762 5 Human 4.7 pKi = 4.7 Functional
Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)
ChEMBL 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10.1021/jm000007r
1394 9199 44 None -7762 5 Human 4.7 pKi = 4.7 Functional
Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)
ChEMBL 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10.1021/jm000007r
CHEMBL275079 9199 44 None -7762 5 Human 4.7 pKi = 4.7 Functional
Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)
ChEMBL 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10.1021/jm000007r
1378 9195 54 None -2818 14 Human 4.7 pKi = 4.7 Functional
Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/jm000007r
1399 9195 54 None -2818 14 Human 4.7 pKi = 4.7 Functional
Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/jm000007r
9819927 9195 54 None -2818 14 Human 4.7 pKi = 4.7 Functional
Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/jm000007r
CHEMBL432038 9195 54 None -2818 14 Human 4.7 pKi = 4.7 Functional
Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/jm000007r
44322840 119348 0 None - 0 Human 4.7 pKi = 4.7 Functional
Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)
ChEMBL 201 2 4 4 -1.5 N[C@]1(C(=O)O)C2C(C[C@H]1O)[C@@H]2C(=O)O 10.1021/jm000007r
CHEMBL330097 119348 0 None - 0 Human 4.7 pKi = 4.7 Functional
Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)
ChEMBL 201 2 4 4 -1.5 N[C@]1(C(=O)O)C2C(C[C@H]1O)[C@@H]2C(=O)O 10.1021/jm000007r
44322921 213616 1 None - 0 Human 4.6 pKi = 4.6 Functional
Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)
ChEMBL 185 2 3 3 -0.5 N[C@@]1(C(=O)O)CC2CC1[C@H]2C(=O)O 10.1021/jm000007r
CHEMBL90501 213616 1 None - 0 Human 4.6 pKi = 4.6 Functional
Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)
ChEMBL 185 2 3 3 -0.5 N[C@@]1(C(=O)O)CC2CC1[C@H]2C(=O)O 10.1021/jm000007r
1432 10374 45 None 3 4 Human 4.6 pKi = 4.6 Functional
Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)
ChEMBL 195 2 0 1 3.6 Cc1cccc(n1)/C=C/c1ccccc1 10.1021/jm000007r
5311432 10374 45 None 3 4 Human 4.6 pKi = 4.6 Functional
Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)
ChEMBL 195 2 0 1 3.6 Cc1cccc(n1)/C=C/c1ccccc1 10.1021/jm000007r
CHEMBL88612 10374 45 None 3 4 Human 4.6 pKi = 4.6 Functional
Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)
ChEMBL 195 2 0 1 3.6 Cc1cccc(n1)/C=C/c1ccccc1 10.1021/jm000007r
1368 9070 37 None - 11 Human 4.3 pKi = 4.3 Functional
Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)
ChEMBL 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 10.1021/jm000007r
5310956 9070 37 None - 11 Human 4.3 pKi = 4.3 Functional
Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)
ChEMBL 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 10.1021/jm000007r
CHEMBL280563 9070 37 None - 11 Human 4.3 pKi = 4.3 Functional
Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)
ChEMBL 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 10.1021/jm000007r
1406 8854 38 None -22 7 Human 5.3 pKi = 5.3 Functional
Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)
ChEMBL 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10.1021/jm000007r
4545574 8854 38 None -22 7 Human 5.3 pKi = 5.3 Functional
Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)
ChEMBL 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10.1021/jm000007r
CHEMBL277475 8854 38 None -22 7 Human 5.3 pKi = 5.3 Functional
Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)
ChEMBL 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10.1021/jm000007r
10656383 119095 1 None - 1 Human 5.1 pKi = 5.1 Functional
Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)
ChEMBL 217 3 4 4 -1.0 NC1(C(=O)O)C[C@H](C(=O)O)[C@@H](C(=O)O)C1 10.1021/jm000007r
CHEMBL329236 119095 1 None - 1 Human 5.1 pKi = 5.1 Functional
Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)
ChEMBL 217 3 4 4 -1.0 NC1(C(=O)O)C[C@H](C(=O)O)[C@@H](C(=O)O)C1 10.1021/jm000007r
18756981 105751 0 None - 0 Human 4.1 pKi = 4.1 Functional
Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)
ChEMBL 167 3 3 2 0.3 CC(C)(N)CCP(=O)(O)O 10.1021/jm000007r
CHEMBL279838 105751 0 None - 0 Human 4.1 pKi = 4.1 Functional
Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)
ChEMBL 167 3 3 2 0.3 CC(C)(N)CCP(=O)(O)O 10.1021/jm000007r
1410 9054 48 None -1 8 Human 6.0 pKi = 6.0 Functional
Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm000007r
1412 9054 48 None -1 8 Human 6.0 pKi = 6.0 Functional
Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm000007r
179394 9054 48 None -1 8 Human 6.0 pKi = 6.0 Functional
Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm000007r
57689795 9054 48 None -1 8 Human 6.0 pKi = 6.0 Functional
Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm000007r
CHEMBL33567 9054 48 None -1 8 Human 6.0 pKi = 6.0 Functional
Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm000007r
104766 6822 42 None -10 14 Human 4.0 pKi = 4.0 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1021/jm000007r
1365 6822 42 None -10 14 Human 4.0 pKi = 4.0 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1021/jm000007r
CHEMBL34453 6822 42 None -10 14 Human 4.0 pKi = 4.0 Functional
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1021/jm000007r
1310 9095 110 None -426 17 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
1369 9095 110 None -426 17 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
33032 9095 110 None -426 17 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
44272391 9095 110 None -426 17 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
88747398 9095 110 None -426 17 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
CHEMBL575060 9095 110 None -426 17 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
DB00142 9095 110 None -426 17 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
1411 9140 66 None -8 6 Rat 8.3 pEC50 = 8.3 Functional
Concentration for half maximal activation of metabotropic glutamate mGluR4a in ratConcentration for half maximal activation of metabotropic glutamate mGluR4a in rat
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
4120 9140 66 None -8 6 Rat 8.3 pEC50 = 8.3 Functional
Concentration for half maximal activation of metabotropic glutamate mGluR4a in ratConcentration for half maximal activation of metabotropic glutamate mGluR4a in rat
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
57689797 9140 66 None -8 6 Rat 8.3 pEC50 = 8.3 Functional
Concentration for half maximal activation of metabotropic glutamate mGluR4a in ratConcentration for half maximal activation of metabotropic glutamate mGluR4a in rat
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
68841 9140 66 None -8 6 Rat 8.3 pEC50 = 8.3 Functional
Concentration for half maximal activation of metabotropic glutamate mGluR4a in ratConcentration for half maximal activation of metabotropic glutamate mGluR4a in rat
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
CHEMBL284377 9140 66 None -8 6 Rat 8.3 pEC50 = 8.3 Functional
Concentration for half maximal activation of metabotropic glutamate mGluR4a in ratConcentration for half maximal activation of metabotropic glutamate mGluR4a in rat
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
DB04522 9140 66 None -8 6 Rat 8.3 pEC50 = 8.3 Functional
Concentration for half maximal activation of metabotropic glutamate mGluR4a in ratConcentration for half maximal activation of metabotropic glutamate mGluR4a in rat
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
1411 9140 66 None -8 6 Human 8.2 pEC50 = 8.2 Functional
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
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
4120 9140 66 None -8 6 Human 8.2 pEC50 = 8.2 Functional
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
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
57689797 9140 66 None -8 6 Human 8.2 pEC50 = 8.2 Functional
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
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
68841 9140 66 None -8 6 Human 8.2 pEC50 = 8.2 Functional
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
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
CHEMBL284377 9140 66 None -8 6 Human 8.2 pEC50 = 8.2 Functional
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
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
DB04522 9140 66 None -8 6 Human 8.2 pEC50 = 8.2 Functional
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
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
137222229 8456 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Calcium assay using human mGluR4.Calcium assay using human mGluR4.
Guide to Pharmacology 421 5 1 7 4.3 ON=c1cc(oc2c1cc(CCCN1CCOCC1)cc2)c1ncc2c(c1)scc2 None
9622 8456 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Calcium assay using human mGluR4.Calcium assay using human mGluR4.
Guide to Pharmacology 421 5 1 7 4.3 ON=c1cc(oc2c1cc(CCCN1CCOCC1)cc2)c1ncc2c(c1)scc2 None
1416 9867 41 None -13 4 Human 4.5 pEC50 = 4.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 294 2 2 4 2.7 O/N=C\1/c2ccccc2OC2(C1C2)C(=O)Nc1ccccc1 14573382
5866327 9867 41 None -13 4 Human 4.5 pEC50 = 4.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 294 2 2 4 2.7 O/N=C\1/c2ccccc2OC2(C1C2)C(=O)Nc1ccccc1 14573382
CHEMBL164770 9867 41 None -13 4 Human 4.5 pEC50 = 4.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 294 2 2 4 2.7 O/N=C\1/c2ccccc2OC2(C1C2)C(=O)Nc1ccccc1 14573382
1310 9095 110 None -1513 17 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
1369 9095 110 None -1513 17 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
33032 9095 110 None -1513 17 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
44272391 9095 110 None -1513 17 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
88747398 9095 110 None -1513 17 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
CHEMBL575060 9095 110 None -1513 17 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
DB00142 9095 110 None -1513 17 Human 5.1 pEC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
3260619 10791 24 None -1 4 Human 5.3 pEC50 = 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 321 2 0 5 3.7 CC1CCCN(C1)c1ncnc2c1cnn2c1ccc(cc1C)C 18793851
6227 10791 24 None -1 4 Human 5.3 pEC50 = 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 321 2 0 5 3.7 CC1CCCN(C1)c1ncnc2c1cnn2c1ccc(cc1C)C 18793851
CHEMBL477396 10791 24 None -1 4 Human 5.3 pEC50 = 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 321 2 0 5 3.7 CC1CCCN(C1)c1ncnc2c1cnn2c1ccc(cc1C)C 18793851
4052597 10793 9 None - 1 Human 5.6 pEC50 = 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 342 3 1 2 5.2 Cc1ccc(cc1)N1C(Nc2c(C1=O)cccc2)C(c1ccccc1)C 19097893
6229 10793 9 None - 1 Human 5.6 pEC50 = 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 342 3 1 2 5.2 Cc1ccc(cc1)N1C(Nc2c(C1=O)cccc2)C(c1ccccc1)C 19097893
CHEMBL473806 10793 9 None - 1 Human 5.6 pEC50 = 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 342 3 1 2 5.2 Cc1ccc(cc1)N1C(Nc2c(C1=O)cccc2)C(c1ccccc1)C 19097893
46898088 9145 6 None -33 8 Rat 5.7 pEC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 364 8 5 8 0.4 COc1cc(cc(c1O)[N+](=O)[O-])C(P(=O)(CC[C@@H](C(=O)O)N)O)O 19525404
6739 9145 6 None -33 8 Rat 5.7 pEC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 364 8 5 8 0.4 COc1cc(cc(c1O)[N+](=O)[O-])C(P(=O)(CC[C@@H](C(=O)O)N)O)O 19525404
CHEMBL3114672 9145 6 None -33 8 Rat 5.7 pEC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 364 8 5 8 0.4 COc1cc(cc(c1O)[N+](=O)[O-])C(P(=O)(CC[C@@H](C(=O)O)N)O)O 19525404
1411 9140 66 None -8 6 Human 5.9 pEC50 = 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 9473604
4120 9140 66 None -8 6 Human 5.9 pEC50 = 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 9473604
57689797 9140 66 None -8 6 Human 5.9 pEC50 = 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 9473604
68841 9140 66 None -8 6 Human 5.9 pEC50 = 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 9473604
CHEMBL284377 9140 66 None -8 6 Human 5.9 pEC50 = 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 9473604
DB04522 9140 66 None -8 6 Human 5.9 pEC50 = 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 9473604
46911068 7762 46 None 1 2 Human 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 197 2 1 3 2.2 Nc1nccc(n1)/C=C/c1ccccc1 20638279
6235 7762 46 None 1 2 Human 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 197 2 1 3 2.2 Nc1nccc(n1)/C=C/c1ccccc1 20638279
CHEMBL1209431 7762 46 None 1 2 Human 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 197 2 1 3 2.2 Nc1nccc(n1)/C=C/c1ccccc1 20638279
42645487 7922 2 None - 1 Human 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 243 3 2 5 2.7 c1ccc(nc1)Nc1scc(n1)c1c[nH]nc1 20638279
6232 7922 2 None - 1 Human 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 243 3 2 5 2.7 c1ccc(nc1)Nc1scc(n1)c1c[nH]nc1 20638279
CHEMBL1830693 7922 2 None - 1 Human 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 243 3 2 5 2.7 c1ccc(nc1)Nc1scc(n1)c1c[nH]nc1 20638279
6234 10810 68 None -3 2 Human 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 232 2 1 2 3.0 Clc1cccc(c1)NC(=O)c1ccccn1 22088953
836002 10810 68 None -3 2 Human 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 232 2 1 2 3.0 Clc1cccc(c1)NC(=O)c1ccccn1 22088953
CHEMBL556667 10810 68 None -3 2 Human 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 232 2 1 2 3.0 Clc1cccc(c1)NC(=O)c1ccccn1 22088953
3323 10798 40 None - 1 Human 6.1 pEC50 = 6.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 315 3 2 2 3.8 O=C([C@H]1CCCC[C@H]1C(=O)O)Nc1cc(Cl)cc(c1)Cl 18664603
888023 10798 40 None - 1 Human 6.1 pEC50 = 6.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 315 3 2 2 3.8 O=C([C@H]1CCCC[C@H]1C(=O)O)Nc1cc(Cl)cc(c1)Cl 18664603
CHEMBL578988 10798 40 None - 1 Human 6.1 pEC50 = 6.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 315 3 2 2 3.8 O=C([C@H]1CCCC[C@H]1C(=O)O)Nc1cc(Cl)cc(c1)Cl 18664603
135411610 10788 10 None - 1 Human 6.2 pEC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 278 3 2 5 3.1 Oc1ccc(cc1)/C=N/Nc1nc2ccccc2nc1C 19097893
135773804 10788 10 None - 1 Human 6.2 pEC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 278 3 2 5 3.1 Oc1ccc(cc1)/C=N/Nc1nc2ccccc2nc1C 19097893
6228 10788 10 None - 1 Human 6.2 pEC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 278 3 2 5 3.1 Oc1ccc(cc1)/C=N/Nc1nc2ccccc2nc1C 19097893
CHEMBL515763 10788 10 None - 1 Human 6.2 pEC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 278 3 2 5 3.1 Oc1ccc(cc1)/C=N/Nc1nc2ccccc2nc1C 19097893
6237 9155 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 316 4 2 3 3.6 NOC[C@@H]1CCCC[C@@H]1C(=O)Nc1ccc(c(c1)Cl)Cl 22491024
73755199 9155 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 316 4 2 3 3.6 NOC[C@@H]1CCCC[C@@H]1C(=O)Nc1ccc(c(c1)Cl)Cl 22491024
153640958 10805 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 295 2 2 5 2.1 O/N=C\1/c2ccccc2OC2(C1C2)C(=O)Nc1ccccn1 20582156
6230 10805 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 295 2 2 5 2.1 O/N=C\1/c2ccccc2OC2(C1C2)C(=O)Nc1ccccn1 20582156
73755197 10805 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 295 2 2 5 2.1 O/N=C\1/c2ccccc2OC2(C1C2)C(=O)Nc1ccccn1 20582156
46869947 10812 0 None -1 2 Rat 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 393 3 1 4 3.3 O=C1C2[C@H]3C=C[C@@H]([C@H]2C(=O)N1c1ccc(cc1Cl)NC(=O)c1ccccn1)C3 21966889
6233 10812 0 None -1 2 Rat 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 393 3 1 4 3.3 O=C1C2[C@H]3C=C[C@@H]([C@H]2C(=O)N1c1ccc(cc1Cl)NC(=O)c1ccccn1)C3 21966889
1426 9391 67 None -38 4 Human 6.5 pEC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 193 0 0 1 2.8 Cc1cccc(n1)C#Cc1ccccc1 12684257
3025961 9391 67 None -38 4 Human 6.5 pEC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 193 0 0 1 2.8 Cc1cccc(n1)C#Cc1ccccc1 12684257
CHEMBL66654 9391 67 None -38 4 Human 6.5 pEC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 193 0 0 1 2.8 Cc1cccc(n1)C#Cc1ccccc1 12684257
1410 9054 48 None -1 8 Human 6.5 pEC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 9473604
1412 9054 48 None -1 8 Human 6.5 pEC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 9473604
179394 9054 48 None -1 8 Human 6.5 pEC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 9473604
57689795 9054 48 None -1 8 Human 6.5 pEC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 9473604
CHEMBL33567 9054 48 None -1 8 Human 6.5 pEC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 9473604
6234 10810 68 None 3 2 Rat 6.5 pEC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 232 2 1 2 3.0 Clc1cccc(c1)NC(=O)c1ccccn1 22088953
836002 10810 68 None 3 2 Rat 6.5 pEC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 232 2 1 2 3.0 Clc1cccc(c1)NC(=O)c1ccccn1 22088953
CHEMBL556667 10810 68 None 3 2 Rat 6.5 pEC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 232 2 1 2 3.0 Clc1cccc(c1)NC(=O)c1ccccn1 22088953
46869947 10812 0 None 1 2 Human 6.5 pEC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 393 3 1 4 3.3 O=C1C2[C@H]3C=C[C@@H]([C@H]2C(=O)N1c1ccc(cc1Cl)NC(=O)c1ccccn1)C3 21966889
6233 10812 0 None 1 2 Human 6.5 pEC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 393 3 1 4 3.3 O=C1C2[C@H]3C=C[C@@H]([C@H]2C(=O)N1c1ccc(cc1Cl)NC(=O)c1ccccn1)C3 21966889
1432 10374 45 None 3 4 Human 6.6 pEC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 195 2 0 1 3.6 Cc1cccc(n1)/C=C/c1ccccc1 12684257
5311432 10374 45 None 3 4 Human 6.6 pEC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 195 2 0 1 3.6 Cc1cccc(n1)/C=C/c1ccccc1 12684257
CHEMBL88612 10374 45 None 3 4 Human 6.6 pEC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 195 2 0 1 3.6 Cc1cccc(n1)/C=C/c1ccccc1 12684257
3956 10807 87 None -1 2 Human 6.6 pEC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 262 3 1 3 3.0 COc1cc(ccc1Cl)NC(=O)c1ccccn1 19469556
44191096 10807 87 None -1 2 Human 6.6 pEC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 262 3 1 3 3.0 COc1cc(ccc1Cl)NC(=O)c1ccccn1 19469556
CHEMBL562551 10807 87 None -1 2 Human 6.6 pEC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 262 3 1 3 3.0 COc1cc(ccc1Cl)NC(=O)c1ccccn1 19469556
6236 7802 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 275 2 1 3 3.3 c1ccc(cc1)N1NCC(C1)c1ccnc2c1cccc2 22465637
73755198 7802 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 275 2 1 3 3.3 c1ccc(cc1)N1NCC(C1)c1ccnc2c1cccc2 22465637
6706 9146 8 None 1 8 Human 7.0 pEC50 = 7.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 347 9 5 6 0.2 OC(=O)COc1ccc(cc1)C(P(=O)(CC[C@@H](C(=O)O)N)O)O 22223752
71041983 9146 8 None 1 8 Human 7.0 pEC50 = 7.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 347 9 5 6 0.2 OC(=O)COc1ccc(cc1)C(P(=O)(CC[C@@H](C(=O)O)N)O)O 22223752
CHEMBL3114673 9146 8 None 1 8 Human 7.0 pEC50 = 7.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 347 9 5 6 0.2 OC(=O)COc1ccc(cc1)C(P(=O)(CC[C@@H](C(=O)O)N)O)O 22223752
10135 10826 21 None 3 2 Human 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 329 2 2 4 4.3 FC(c1nccc2c1ccc(c2)Nc1n[nH]c2c1cccn2)(F)F 30891122
134191471 10826 21 None 3 2 Human 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 329 2 2 4 4.3 FC(c1nccc2c1ccc(c2)Nc1n[nH]c2c1cccn2)(F)F 30891122
CHEMBL4797139 10826 21 None 3 2 Human 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 329 2 2 4 4.3 FC(c1nccc2c1ccc(c2)Nc1n[nH]c2c1cccn2)(F)F 30891122
11565290 8461 11 None 1071 3 Human 7.4 pEC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 272 4 4 5 -1.9 OC(=O)/C=C/C(=O)N1C[C@](C[C@H]1C(=O)O)(N)C(=O)O 17167031
1409 8461 11 None 1071 3 Human 7.4 pEC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 272 4 4 5 -1.9 OC(=O)/C=C/C(=O)N1C[C@](C[C@H]1C(=O)O)(N)C(=O)O 17167031
CHEMBL212233 8461 11 None 1071 3 Human 7.4 pEC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 272 4 4 5 -1.9 OC(=O)/C=C/C(=O)N1C[C@](C[C@H]1C(=O)O)(N)C(=O)O 17167031
46836872 7088 47 None -1 4 Rat 8.0 pEC50 = 8.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 272 3 2 6 2.7 Cc1ccnc(n1)Nc1sc(c(n1)c1c[nH]nc1)C 22787118
6238 7088 47 None -1 4 Rat 8.0 pEC50 = 8.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 272 3 2 6 2.7 Cc1ccnc(n1)Nc1sc(c(n1)c1c[nH]nc1)C 22787118
CHEMBL3609729 7088 47 None -1 4 Rat 8.0 pEC50 = 8.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 272 3 2 6 2.7 Cc1ccnc(n1)Nc1sc(c(n1)c1c[nH]nc1)C 22787118
46836562 7818 32 None - 1 Human 8.1 pEC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 283 2 2 5 3.2 c1ccc(nc1)Nc1sc2c(n1)c1c[nH]nc1CCC2 21688779
6231 7818 32 None - 1 Human 8.1 pEC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 283 2 2 5 3.2 c1ccc(nc1)Nc1sc2c(n1)c1c[nH]nc1CCC2 21688779
CHEMBL1830707 7818 32 None - 1 Human 8.1 pEC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 283 2 2 5 3.2 c1ccc(nc1)Nc1sc2c(n1)c1c[nH]nc1CCC2 21688779
46836872 7088 47 None 1 4 Human 8.5 pEC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 272 3 2 6 2.7 Cc1ccnc(n1)Nc1sc(c(n1)c1c[nH]nc1)C 22787118
6238 7088 47 None 1 4 Human 8.5 pEC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 272 3 2 6 2.7 Cc1ccnc(n1)Nc1sc(c(n1)c1c[nH]nc1)C 22787118
CHEMBL3609729 7088 47 None 1 4 Human 8.5 pEC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 272 3 2 6 2.7 Cc1ccnc(n1)Nc1sc(c(n1)c1c[nH]nc1)C 22787118
1408 7053 31 None -1 7 Rat 5.1 pEC50 None 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O 9301676
6604820 7053 31 None -1 7 Rat 5.1 pEC50 None 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O 9301676
CHEMBL285043 7053 31 None -1 7 Rat 5.1 pEC50 None 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O 9301676
CHEMBL288635 7053 31 None -1 7 Rat 5.1 pEC50 None 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O 9301676
1407 8860 42 None -117 7 Human 5.1 pEC50 None 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 239 4 4 4 0.2 N[C@@H](c1ccc(c(c1)C(=O)O)C(=O)O)C(=O)O 11166323
16062593 8860 42 None -117 7 Human 5.1 pEC50 None 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 239 4 4 4 0.2 N[C@@H](c1ccc(c(c1)C(=O)O)C(=O)O)C(=O)O 11166323
CHEMBL143210 8860 42 None -117 7 Human 5.1 pEC50 None 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 239 4 4 4 0.2 N[C@@H](c1ccc(c(c1)C(=O)O)C(=O)O)C(=O)O 11166323
1406 8854 38 None -22 7 Human 5.3 pEC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10336568
1406 8854 38 None -22 7 Human 5.3 pEC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10866390
4545574 8854 38 None -22 7 Human 5.3 pEC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10336568
4545574 8854 38 None -22 7 Human 5.3 pEC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10866390
CHEMBL277475 8854 38 None -22 7 Human 5.3 pEC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10336568
CHEMBL277475 8854 38 None -22 7 Human 5.3 pEC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10866390
1411 9140 66 None -8 6 Rat 5.8 pIC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 10187777
1411 9140 66 None -8 6 Rat 5.8 pIC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 8106006
1411 9140 66 None -8 6 Rat 5.8 pIC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 8463825
1411 9140 66 None -8 6 Rat 5.8 pIC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 8719808
1411 9140 66 None -8 6 Rat 5.8 pIC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 9144638
4120 9140 66 None -8 6 Rat 5.8 pIC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 10187777
4120 9140 66 None -8 6 Rat 5.8 pIC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 8106006
4120 9140 66 None -8 6 Rat 5.8 pIC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 8463825
4120 9140 66 None -8 6 Rat 5.8 pIC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 8719808
4120 9140 66 None -8 6 Rat 5.8 pIC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 9144638
57689797 9140 66 None -8 6 Rat 5.8 pIC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 10187777
57689797 9140 66 None -8 6 Rat 5.8 pIC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 8106006
57689797 9140 66 None -8 6 Rat 5.8 pIC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 8463825
57689797 9140 66 None -8 6 Rat 5.8 pIC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 8719808
57689797 9140 66 None -8 6 Rat 5.8 pIC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 9144638
68841 9140 66 None -8 6 Rat 5.8 pIC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 10187777
68841 9140 66 None -8 6 Rat 5.8 pIC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 8106006
68841 9140 66 None -8 6 Rat 5.8 pIC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 8463825
68841 9140 66 None -8 6 Rat 5.8 pIC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 8719808
68841 9140 66 None -8 6 Rat 5.8 pIC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 9144638
CHEMBL284377 9140 66 None -8 6 Rat 5.8 pIC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 10187777
CHEMBL284377 9140 66 None -8 6 Rat 5.8 pIC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 8106006
CHEMBL284377 9140 66 None -8 6 Rat 5.8 pIC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 8463825
CHEMBL284377 9140 66 None -8 6 Rat 5.8 pIC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 8719808
CHEMBL284377 9140 66 None -8 6 Rat 5.8 pIC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 9144638
DB04522 9140 66 None -8 6 Rat 5.8 pIC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 10187777
DB04522 9140 66 None -8 6 Rat 5.8 pIC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 8106006
DB04522 9140 66 None -8 6 Rat 5.8 pIC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 8463825
DB04522 9140 66 None -8 6 Rat 5.8 pIC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 8719808
DB04522 9140 66 None -8 6 Rat 5.8 pIC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 9144638
1368 9070 37 None -24 11 Rat 4.7 pIC50 None 4.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 1330184
5310956 9070 37 None -24 11 Rat 4.7 pIC50 None 4.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 1330184
CHEMBL280563 9070 37 None -24 11 Rat 4.7 pIC50 None 4.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 1330184
1378 9195 54 None -2818 14 Human 4.7 pIC50 None 4.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 8532170
1399 9195 54 None -2818 14 Human 4.7 pIC50 None 4.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 8532170
9819927 9195 54 None -2818 14 Human 4.7 pIC50 None 4.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 8532170
CHEMBL432038 9195 54 None -2818 14 Human 4.7 pIC50 None 4.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 8532170
1410 9054 48 None -1 8 Rat 6.2 pIC50 None 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10187777
1410 9054 48 None -1 8 Rat 6.2 pIC50 None 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 8463825
1410 9054 48 None -1 8 Rat 6.2 pIC50 None 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 8719808
1410 9054 48 None -1 8 Rat 6.2 pIC50 None 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 9144638
1412 9054 48 None -1 8 Rat 6.2 pIC50 None 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10187777
1412 9054 48 None -1 8 Rat 6.2 pIC50 None 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 8463825
1412 9054 48 None -1 8 Rat 6.2 pIC50 None 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 8719808
1412 9054 48 None -1 8 Rat 6.2 pIC50 None 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 9144638
179394 9054 48 None -1 8 Rat 6.2 pIC50 None 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10187777
179394 9054 48 None -1 8 Rat 6.2 pIC50 None 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 8463825
179394 9054 48 None -1 8 Rat 6.2 pIC50 None 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 8719808
179394 9054 48 None -1 8 Rat 6.2 pIC50 None 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 9144638
57689795 9054 48 None -1 8 Rat 6.2 pIC50 None 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10187777
57689795 9054 48 None -1 8 Rat 6.2 pIC50 None 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 8463825
57689795 9054 48 None -1 8 Rat 6.2 pIC50 None 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 8719808
57689795 9054 48 None -1 8 Rat 6.2 pIC50 None 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 9144638
CHEMBL33567 9054 48 None -1 8 Rat 6.2 pIC50 None 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10187777
CHEMBL33567 9054 48 None -1 8 Rat 6.2 pIC50 None 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 8463825
CHEMBL33567 9054 48 None -1 8 Rat 6.2 pIC50 None 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 8719808
CHEMBL33567 9054 48 None -1 8 Rat 6.2 pIC50 None 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 9144638




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44191180 202372 0 None - 0 Rat 6.0 pEC50 = 6 Binding
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 202372 0 None - 0 Rat 6.0 pEC50 = 6 Binding
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 9140 66 None - 1 Human 6.0 pEC50 = 6 Binding
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 9140 66 None - 1 Human 6.0 pEC50 = 6 Binding
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 9140 66 None - 1 Human 6.0 pEC50 = 6 Binding
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 9140 66 None - 1 Human 6.0 pEC50 = 6 Binding
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 9140 66 None - 1 Human 6.0 pEC50 = 6 Binding
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 9140 66 None - 1 Human 6.0 pEC50 = 6 Binding
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 7762 46 None - 0 Rat 6.0 pEC50 = 6 Binding
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 7762 46 None - 0 Rat 6.0 pEC50 = 6 Binding
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 7762 46 None - 0 Rat 6.0 pEC50 = 6 Binding
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 122923 0 None - 0 Human 7.0 pEC50 = 7 Binding
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 122923 0 None - 0 Human 7.0 pEC50 = 7 Binding
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 75561 0 None - 0 Rat 7.0 pEC50 = 7.0 Binding
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 75561 0 None - 0 Rat 7.0 pEC50 = 7.0 Binding
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 10815 29 None - 0 Human 7.0 pEC50 = 7.0 Binding
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 10815 29 None - 0 Human 7.0 pEC50 = 7.0 Binding
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 10815 29 None - 0 Human 7.0 pEC50 = 7.0 Binding
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 188835 0 None - 0 Rat 6.0 pEC50 = 6.0 Binding
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 188835 0 None - 0 Rat 6.0 pEC50 = 6.0 Binding
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 10807 87 None - 0 Rat 7.0 pEC50 = 7.0 Binding
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 10807 87 None - 0 Rat 7.0 pEC50 = 7.0 Binding
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 10807 87 None - 0 Rat 7.0 pEC50 = 7.0 Binding
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 31723 22 None - 0 Rat 6.0 pEC50 = 6.0 Binding
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 31723 22 None - 0 Rat 6.0 pEC50 = 6.0 Binding
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 188187 0 None - 0 Rat 6.9 pEC50 = 6.9 Binding
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 188187 0 None - 0 Rat 6.9 pEC50 = 6.9 Binding
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 10810 68 None - 0 Human 5.9 pEC50 = 5.9 Binding
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 10810 68 None - 0 Human 5.9 pEC50 = 5.9 Binding
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 10810 68 None - 0 Human 5.9 pEC50 = 5.9 Binding
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 9054 48 None -2 6 Rat 5.9 pEC50 = 5.9 Binding
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 9054 48 None -2 6 Rat 5.9 pEC50 = 5.9 Binding
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 9054 48 None -2 6 Rat 5.9 pEC50 = 5.9 Binding
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 9054 48 None -2 6 Rat 5.9 pEC50 = 5.9 Binding
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 9054 48 None -2 6 Rat 5.9 pEC50 = 5.9 Binding
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 9095 110 None -26 18 Rat 4.9 pEC50 = 4.9 Binding
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 9095 110 None -26 18 Rat 4.9 pEC50 = 4.9 Binding
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 9095 110 None -26 18 Rat 4.9 pEC50 = 4.9 Binding
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 9095 110 None -26 18 Rat 4.9 pEC50 = 4.9 Binding
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 9095 110 None -26 18 Rat 4.9 pEC50 = 4.9 Binding
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 9095 110 None -26 18 Rat 4.9 pEC50 = 4.9 Binding
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 9095 110 None -26 18 Rat 4.9 pEC50 = 4.9 Binding
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 211702 106 None - 5 Rat 4.9 pEC50 = 4.9 Binding
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 211702 106 None - 5 Rat 4.9 pEC50 = 4.9 Binding
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 211702 106 None - 5 Rat 4.9 pEC50 = 4.9 Binding
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 179269 0 None - 0 Rat 6.9 pEC50 = 6.9 Binding
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 179269 0 None - 0 Rat 6.9 pEC50 = 6.9 Binding
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 146505 3 None - 0 Rat 6.9 pEC50 = 6.9 Binding
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 146505 3 None - 0 Rat 6.9 pEC50 = 6.9 Binding
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 9140 66 None - 1 Human 5.9 pEC50 = 5.9 Binding
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
4120 9140 66 None - 1 Human 5.9 pEC50 = 5.9 Binding
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
57689797 9140 66 None - 1 Human 5.9 pEC50 = 5.9 Binding
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
68841 9140 66 None - 1 Human 5.9 pEC50 = 5.9 Binding
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
CHEMBL284377 9140 66 None - 1 Human 5.9 pEC50 = 5.9 Binding
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
DB04522 9140 66 None - 1 Human 5.9 pEC50 = 5.9 Binding
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
122419163 179872 0 None - 0 Rat 6.9 pEC50 = 6.9 Binding
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 414 3 2 6 4.2 O=C(c1nsc2cc(Nc3n[nH]c4cccnc34)ccc12)N1CCC(F)(F)CC1 10.1021/acs.jmedchem.8b00994
CHEMBL4520127 179872 0 None - 0 Rat 6.9 pEC50 = 6.9 Binding
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 414 3 2 6 4.2 O=C(c1nsc2cc(Nc3n[nH]c4cccnc34)ccc12)N1CCC(F)(F)CC1 10.1021/acs.jmedchem.8b00994
44572113 195677 4 None - 0 Human 5.9 pEC50 = 5.9 Binding
Positive allosteric modulator activity at mGlu4 receptor (unknown origin)Positive allosteric modulator activity at mGlu4 receptor (unknown origin)
ChEMBL 294 2 2 4 2.7 O=C(Nc1ccccc1)[C@]12C[C@H]1/C(=N\O)c1ccccc1O2 10.1016/j.bmcl.2015.07.031
CHEMBL507522 195677 4 None - 0 Human 5.9 pEC50 = 5.9 Binding
Positive allosteric modulator activity at mGlu4 receptor (unknown origin)Positive allosteric modulator activity at mGlu4 receptor (unknown origin)
ChEMBL 294 2 2 4 2.7 O=C(Nc1ccccc1)[C@]12C[C@H]1/C(=N\O)c1ccccc1O2 10.1016/j.bmcl.2015.07.031
162659228 188150 0 None - 0 Rat 6.8 pEC50 = 6.8 Binding
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 284 2 2 3 1.9 O=C1CCSC[C@@H](C(=O)Nc2cccc(Cl)c2)N1 10.1016/j.bmcl.2021.127838
CHEMBL4763297 188150 0 None - 0 Rat 6.8 pEC50 = 6.8 Binding
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 284 2 2 3 1.9 O=C1CCSC[C@@H](C(=O)Nc2cccc(Cl)c2)N1 10.1016/j.bmcl.2021.127838
46898088 9145 6 None - 0 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at human mGlu4 receptor by FLIPR assay relative to controlAgonist activity at human mGlu4 receptor by FLIPR assay relative to control
ChEMBL 364 8 5 8 0.4 COc1cc(cc(c1O)[N+](=O)[O-])C(P(=O)(CC[C@@H](C(=O)O)N)O)O 10.1021/ml400338f
6739 9145 6 None - 0 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at human mGlu4 receptor by FLIPR assay relative to controlAgonist activity at human mGlu4 receptor by FLIPR assay relative to control
ChEMBL 364 8 5 8 0.4 COc1cc(cc(c1O)[N+](=O)[O-])C(P(=O)(CC[C@@H](C(=O)O)N)O)O 10.1021/ml400338f
CHEMBL3114672 9145 6 None - 0 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at human mGlu4 receptor by FLIPR assay relative to controlAgonist activity at human mGlu4 receptor by FLIPR assay relative to control
ChEMBL 364 8 5 8 0.4 COc1cc(cc(c1O)[N+](=O)[O-])C(P(=O)(CC[C@@H](C(=O)O)N)O)O 10.1021/ml400338f
122419061 181852 0 None - 0 Rat 6.8 pEC50 = 6.8 Binding
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 339 3 2 7 3.7 CC(C)(C)Cc1nsc2cc(Nc3n[nH]c4nccnc34)cnc12 10.1021/acs.jmedchem.8b00994
CHEMBL4568302 181852 0 None - 0 Rat 6.8 pEC50 = 6.8 Binding
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 339 3 2 7 3.7 CC(C)(C)Cc1nsc2cc(Nc3n[nH]c4nccnc34)cnc12 10.1021/acs.jmedchem.8b00994
162663930 188880 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Positive allosteric modulation of mGluR4 (unknown origin)Positive allosteric modulation of mGluR4 (unknown origin)
ChEMBL 380 3 0 5 3.7 COc1cc(F)cc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1016/j.bmcl.2022.129106
CHEMBL4761695 188880 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Positive allosteric modulation of mGluR4 (unknown origin)Positive allosteric modulation of mGluR4 (unknown origin)
ChEMBL 380 3 0 5 3.7 COc1cc(F)cc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1016/j.bmcl.2022.129106
CHEMBL4781814 188880 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Positive allosteric modulation of mGluR4 (unknown origin)Positive allosteric modulation of mGluR4 (unknown origin)
ChEMBL 380 3 0 5 3.7 COc1cc(F)cc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1016/j.bmcl.2022.129106
134190146 178576 0 None - 0 Rat 5.8 pEC50 = 5.8 Binding
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 315 3 2 5 4.0 CC(F)(F)c1noc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
CHEMBL4468073 178576 0 None - 0 Rat 5.8 pEC50 = 5.8 Binding
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 315 3 2 5 4.0 CC(F)(F)c1noc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
46182708 22637 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of human mGlu4 receptorPositive allosteric modulation of human mGlu4 receptor
ChEMBL 387 5 2 4 3.8 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2Cl)cc1)c1ccccn1 10.1016/j.bmcl.2016.05.029
CHEMBL1223083 22637 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of human mGlu4 receptorPositive allosteric modulation of human mGlu4 receptor
ChEMBL 387 5 2 4 3.8 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2Cl)cc1)c1ccccn1 10.1016/j.bmcl.2016.05.029
46853681 75478 0 None - 0 Rat 6.8 pEC50 = 6.8 Binding
Positive allosteric modulator activity at rat mGlu4 receptor by thallium flux assayPositive allosteric modulator activity at rat mGlu4 receptor by thallium flux assay
ChEMBL 415 3 1 6 2.2 O=C(Nc1ccc(N2S(=O)(=O)c3ccccc3S2(=O)=O)cc1)c1ccccn1 10.1021/jm200956q
CHEMBL1921855 75478 0 None - 0 Rat 6.8 pEC50 = 6.8 Binding
Positive allosteric modulator activity at rat mGlu4 receptor by thallium flux assayPositive allosteric modulator activity at rat mGlu4 receptor by thallium flux assay
ChEMBL 415 3 1 6 2.2 O=C(Nc1ccc(N2S(=O)(=O)c3ccccc3S2(=O)=O)cc1)c1ccccn1 10.1021/jm200956q
122419063 182860 0 None - 0 Rat 6.8 pEC50 = 6.8 Binding
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 392 3 2 6 4.0 CC(=O)N1CCC(c2nsc3cc(Nc4n[nH]c5cccnc45)ccc23)CC1 10.1021/acs.jmedchem.8b00994
CHEMBL4591132 182860 0 None - 0 Rat 6.8 pEC50 = 6.8 Binding
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 392 3 2 6 4.0 CC(=O)N1CCC(c2nsc3cc(Nc4n[nH]c5cccnc45)ccc23)CC1 10.1021/acs.jmedchem.8b00994
134190225 182480 0 None - 0 Rat 6.8 pEC50 = 6.8 Binding
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 Cc1noc2c(F)cc(Nc3n[nH]c4ncccc34)cc12 10.1021/acs.jmedchem.8b00994
CHEMBL4582128 182480 0 None - 0 Rat 6.8 pEC50 = 6.8 Binding
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 Cc1noc2c(F)cc(Nc3n[nH]c4ncccc34)cc12 10.1021/acs.jmedchem.8b00994
135411610 10788 10 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activation of human mGluR4 expressed in CHO cells coexpressing Gqi5 protein assessed as potentiation of glutamate-induced responseActivation of human mGluR4 expressed in CHO cells coexpressing Gqi5 protein assessed as potentiation of glutamate-induced response
ChEMBL 278 3 2 5 3.1 Oc1ccc(cc1)/C=N/Nc1nc2ccccc2nc1C 10.1016/j.bmcl.2008.11.104
135773804 10788 10 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activation of human mGluR4 expressed in CHO cells coexpressing Gqi5 protein assessed as potentiation of glutamate-induced responseActivation of human mGluR4 expressed in CHO cells coexpressing Gqi5 protein assessed as potentiation of glutamate-induced response
ChEMBL 278 3 2 5 3.1 Oc1ccc(cc1)/C=N/Nc1nc2ccccc2nc1C 10.1016/j.bmcl.2008.11.104
6228 10788 10 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activation of human mGluR4 expressed in CHO cells coexpressing Gqi5 protein assessed as potentiation of glutamate-induced responseActivation of human mGluR4 expressed in CHO cells coexpressing Gqi5 protein assessed as potentiation of glutamate-induced response
ChEMBL 278 3 2 5 3.1 Oc1ccc(cc1)/C=N/Nc1nc2ccccc2nc1C 10.1016/j.bmcl.2008.11.104
CHEMBL515763 10788 10 None - 0 Human 5.8 pEC50 = 5.8 Binding
Activation of human mGluR4 expressed in CHO cells coexpressing Gqi5 protein assessed as potentiation of glutamate-induced responseActivation of human mGluR4 expressed in CHO cells coexpressing Gqi5 protein assessed as potentiation of glutamate-induced response
ChEMBL 278 3 2 5 3.1 Oc1ccc(cc1)/C=N/Nc1nc2ccccc2nc1C 10.1016/j.bmcl.2008.11.104
8403638 203274 4 None - 0 Rat 5.8 pEC50 = 5.8 Binding
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 300 2 1 2 4.0 O=C(Nc1ccc(Cl)c(C(F)(F)F)c1)c1ccccn1 10.1021/jm9005065
CHEMBL563423 203274 4 None - 0 Rat 5.8 pEC50 = 5.8 Binding
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 300 2 1 2 4.0 O=C(Nc1ccc(Cl)c(C(F)(F)F)c1)c1ccccn1 10.1021/jm9005065
10262421 119176 6 None - 0 Human 4.8 pEC50 = 4.8 Binding
Agonistic activity on Human mGlu4a receptor expressed in recombinant mammalian cells by GTPgammaS binding assayAgonistic activity on Human mGlu4a receptor expressed in recombinant mammalian cells by GTPgammaS binding assay
ChEMBL 207 2 4 3 -0.4 NC1(C(=O)O)CC=C(P(=O)(O)O)C1 10.1016/s0960-894x(00)00247-x
CHEMBL32972 119176 6 None - 0 Human 4.8 pEC50 = 4.8 Binding
Agonistic activity on Human mGlu4a receptor expressed in recombinant mammalian cells by GTPgammaS binding assayAgonistic activity on Human mGlu4a receptor expressed in recombinant mammalian cells by GTPgammaS binding assay
ChEMBL 207 2 4 3 -0.4 NC1(C(=O)O)CC=C(P(=O)(O)O)C1 10.1016/s0960-894x(00)00247-x
2306530 204501 9 None - 0 Rat 5.8 pEC50 = 5.8 Binding
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 266 2 1 2 3.4 O=C(Nc1cccc(C(F)(F)F)c1)c1ccccn1 10.1021/jm9005065
CHEMBL571453 204501 9 None - 0 Rat 5.8 pEC50 = 5.8 Binding
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 266 2 1 2 3.4 O=C(Nc1cccc(C(F)(F)F)c1)c1ccccn1 10.1021/jm9005065
46934289 22742 77 None - 0 Human 7.7 pEC50 = 7.7 Binding
Positive allosteric modulation of human mGlu4 receptorPositive allosteric modulation of human mGlu4 receptor
ChEMBL 421 5 2 4 4.4 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2Cl)c(Cl)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
CHEMBL1223381 22742 77 None - 0 Human 7.7 pEC50 = 7.7 Binding
Positive allosteric modulation of human mGlu4 receptorPositive allosteric modulation of human mGlu4 receptor
ChEMBL 421 5 2 4 4.4 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2Cl)c(Cl)c1)c1ccccn1 10.1016/j.bmcl.2016.05.029
134190223 179137 0 None - 0 Rat 6.7 pEC50 = 6.7 Binding
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]c4ncc(F)cc34)cc12 10.1021/acs.jmedchem.8b00994
CHEMBL4475973 179137 0 None - 0 Rat 6.7 pEC50 = 6.7 Binding
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]c4ncc(F)cc34)cc12 10.1021/acs.jmedchem.8b00994
10135 10826 21 None - 0 Rat 6.7 pEC50 = 6.7 Binding
Positive allosteric modulator activity at rat mGlu4 in human HEK cells co-expressing GRIK assessed as increase in by thallium flux preincubated for 2.5 mins followed by gluatamate addition and measured for 2 mins by thallium flux assayPositive allosteric modulator activity at rat mGlu4 in human HEK cells co-expressing GRIK assessed as increase in by thallium flux preincubated for 2.5 mins followed by gluatamate addition and measured for 2 mins by thallium flux assay
ChEMBL 329 2 2 4 4.3 FC(c1nccc2c1ccc(c2)Nc1n[nH]c2c1cccn2)(F)F 10.1021/acsmedchemlett.8b00426
134191471 10826 21 None - 0 Rat 6.7 pEC50 = 6.7 Binding
Positive allosteric modulator activity at rat mGlu4 in human HEK cells co-expressing GRIK assessed as increase in by thallium flux preincubated for 2.5 mins followed by gluatamate addition and measured for 2 mins by thallium flux assayPositive allosteric modulator activity at rat mGlu4 in human HEK cells co-expressing GRIK assessed as increase in by thallium flux preincubated for 2.5 mins followed by gluatamate addition and measured for 2 mins by thallium flux assay
ChEMBL 329 2 2 4 4.3 FC(c1nccc2c1ccc(c2)Nc1n[nH]c2c1cccn2)(F)F 10.1021/acsmedchemlett.8b00426
CHEMBL4797139 10826 21 None - 0 Rat 6.7 pEC50 = 6.7 Binding
Positive allosteric modulator activity at rat mGlu4 in human HEK cells co-expressing GRIK assessed as increase in by thallium flux preincubated for 2.5 mins followed by gluatamate addition and measured for 2 mins by thallium flux assayPositive allosteric modulator activity at rat mGlu4 in human HEK cells co-expressing GRIK assessed as increase in by thallium flux preincubated for 2.5 mins followed by gluatamate addition and measured for 2 mins by thallium flux assay
ChEMBL 329 2 2 4 4.3 FC(c1nccc2c1ccc(c2)Nc1n[nH]c2c1cccn2)(F)F 10.1021/acsmedchemlett.8b00426
10135 10826 21 None - 0 Rat 6.7 pEC50 = 6.7 Binding
Positive allosteric modulator activity at rat mGlu4 in human HEK cells co-expressing GRIK assessed as increase in by thallium flux preincubated for 2.5 mins followed by gluatamate addition and measured for 2 mins by thallium flux assayPositive allosteric modulator activity at rat mGlu4 in human HEK cells co-expressing GRIK assessed as increase in by thallium flux preincubated for 2.5 mins followed by gluatamate addition and measured for 2 mins by thallium flux assay
ChEMBL 329 2 2 4 4.3 FC(c1nccc2c1ccc(c2)Nc1n[nH]c2c1cccn2)(F)F 10.1021/acsmedchemlett.8b00426
134191471 10826 21 None - 0 Rat 6.7 pEC50 = 6.7 Binding
Positive allosteric modulator activity at rat mGlu4 in human HEK cells co-expressing GRIK assessed as increase in by thallium flux preincubated for 2.5 mins followed by gluatamate addition and measured for 2 mins by thallium flux assayPositive allosteric modulator activity at rat mGlu4 in human HEK cells co-expressing GRIK assessed as increase in by thallium flux preincubated for 2.5 mins followed by gluatamate addition and measured for 2 mins by thallium flux assay
ChEMBL 329 2 2 4 4.3 FC(c1nccc2c1ccc(c2)Nc1n[nH]c2c1cccn2)(F)F 10.1021/acsmedchemlett.8b00426
CHEMBL4797139 10826 21 None - 0 Rat 6.7 pEC50 = 6.7 Binding
Positive allosteric modulator activity at rat mGlu4 in human HEK cells co-expressing GRIK assessed as increase in by thallium flux preincubated for 2.5 mins followed by gluatamate addition and measured for 2 mins by thallium flux assayPositive allosteric modulator activity at rat mGlu4 in human HEK cells co-expressing GRIK assessed as increase in by thallium flux preincubated for 2.5 mins followed by gluatamate addition and measured for 2 mins by thallium flux assay
ChEMBL 329 2 2 4 4.3 FC(c1nccc2c1ccc(c2)Nc1n[nH]c2c1cccn2)(F)F 10.1021/acsmedchemlett.8b00426
46934289 22742 77 None - 0 Human 7.7 pEC50 = 7.7 Binding
Positive allosteric modulator activity at human mGlu4 receptorPositive allosteric modulator activity at human mGlu4 receptor
ChEMBL 421 5 2 4 4.4 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2Cl)c(Cl)c1)c1ccccn1 10.1016/j.bmcl.2015.07.031
CHEMBL1223381 22742 77 None - 0 Human 7.7 pEC50 = 7.7 Binding
Positive allosteric modulator activity at human mGlu4 receptorPositive allosteric modulator activity at human mGlu4 receptor
ChEMBL 421 5 2 4 4.4 O=C(Nc1ccc(S(=O)(=O)Nc2ccccc2Cl)c(Cl)c1)c1ccccn1 10.1016/j.bmcl.2015.07.031
46898088 9145 6 None - 0 Mouse 6.7 pEC50 = 6.7 Binding
Agonist activity at mGlu4 in C57/Bl6 mouse GP neurons assessed as inhibition of striatopallidal GABAergic inhibitory postsynaptic current amplitude by whole cell patch clamp assayAgonist activity at mGlu4 in C57/Bl6 mouse GP neurons assessed as inhibition of striatopallidal GABAergic inhibitory postsynaptic current amplitude by whole cell patch clamp assay
ChEMBL 364 8 5 8 0.4 COc1cc(cc(c1O)[N+](=O)[O-])C(P(=O)(CC[C@@H](C(=O)O)N)O)O 10.1021/acs.jmedchem.7b01438
6739 9145 6 None - 0 Mouse 6.7 pEC50 = 6.7 Binding
Agonist activity at mGlu4 in C57/Bl6 mouse GP neurons assessed as inhibition of striatopallidal GABAergic inhibitory postsynaptic current amplitude by whole cell patch clamp assayAgonist activity at mGlu4 in C57/Bl6 mouse GP neurons assessed as inhibition of striatopallidal GABAergic inhibitory postsynaptic current amplitude by whole cell patch clamp assay
ChEMBL 364 8 5 8 0.4 COc1cc(cc(c1O)[N+](=O)[O-])C(P(=O)(CC[C@@H](C(=O)O)N)O)O 10.1021/acs.jmedchem.7b01438
CHEMBL3114672 9145 6 None - 0 Mouse 6.7 pEC50 = 6.7 Binding
Agonist activity at mGlu4 in C57/Bl6 mouse GP neurons assessed as inhibition of striatopallidal GABAergic inhibitory postsynaptic current amplitude by whole cell patch clamp assayAgonist activity at mGlu4 in C57/Bl6 mouse GP neurons assessed as inhibition of striatopallidal GABAergic inhibitory postsynaptic current amplitude by whole cell patch clamp assay
ChEMBL 364 8 5 8 0.4 COc1cc(cc(c1O)[N+](=O)[O-])C(P(=O)(CC[C@@H](C(=O)O)N)O)O 10.1021/acs.jmedchem.7b01438
1410 9054 48 None -3 6 Human 6.7 pEC50 = 6.7 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR4a in humanConcentration for half maximal activation of metabotropic glutamate mGluR4a in human
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm00009a001
1412 9054 48 None -3 6 Human 6.7 pEC50 = 6.7 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR4a in humanConcentration for half maximal activation of metabotropic glutamate mGluR4a in human
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm00009a001
179394 9054 48 None -3 6 Human 6.7 pEC50 = 6.7 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR4a in humanConcentration for half maximal activation of metabotropic glutamate mGluR4a in human
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm00009a001
57689795 9054 48 None -3 6 Human 6.7 pEC50 = 6.7 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR4a in humanConcentration for half maximal activation of metabotropic glutamate mGluR4a in human
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm00009a001
CHEMBL33567 9054 48 None -3 6 Human 6.7 pEC50 = 6.7 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR4a in humanConcentration for half maximal activation of metabotropic glutamate mGluR4a in human
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm00009a001
1410 9054 48 None -2 6 Rat 6.7 pEC50 = 6.7 Binding
Effective concentration against Metabotropic glutamate receptor 4Effective concentration against Metabotropic glutamate receptor 4
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm049092j
1412 9054 48 None -2 6 Rat 6.7 pEC50 = 6.7 Binding
Effective concentration against Metabotropic glutamate receptor 4Effective concentration against Metabotropic glutamate receptor 4
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm049092j
179394 9054 48 None -2 6 Rat 6.7 pEC50 = 6.7 Binding
Effective concentration against Metabotropic glutamate receptor 4Effective concentration against Metabotropic glutamate receptor 4
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm049092j
57689795 9054 48 None -2 6 Rat 6.7 pEC50 = 6.7 Binding
Effective concentration against Metabotropic glutamate receptor 4Effective concentration against Metabotropic glutamate receptor 4
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm049092j
CHEMBL33567 9054 48 None -2 6 Rat 6.7 pEC50 = 6.7 Binding
Effective concentration against Metabotropic glutamate receptor 4Effective concentration against Metabotropic glutamate receptor 4
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm049092j
1310 9095 110 None -4 18 Human 4.7 pEC50 = 4.7 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR4a in humanConcentration for half maximal activation of metabotropic glutamate mGluR4a in human
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
1369 9095 110 None -4 18 Human 4.7 pEC50 = 4.7 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR4a in humanConcentration for half maximal activation of metabotropic glutamate mGluR4a in human
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
33032 9095 110 None -4 18 Human 4.7 pEC50 = 4.7 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR4a in humanConcentration for half maximal activation of metabotropic glutamate mGluR4a in human
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
44272391 9095 110 None -4 18 Human 4.7 pEC50 = 4.7 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR4a in humanConcentration for half maximal activation of metabotropic glutamate mGluR4a in human
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
88747398 9095 110 None -4 18 Human 4.7 pEC50 = 4.7 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR4a in humanConcentration for half maximal activation of metabotropic glutamate mGluR4a in human
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
CHEMBL575060 9095 110 None -4 18 Human 4.7 pEC50 = 4.7 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR4a in humanConcentration for half maximal activation of metabotropic glutamate mGluR4a in human
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
DB00142 9095 110 None -4 18 Human 4.7 pEC50 = 4.7 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR4a in humanConcentration for half maximal activation of metabotropic glutamate mGluR4a in human
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
10198359 80733 9 None - 1 Human 4.7 pEC50 = 4.7 Binding
Concentration required to inhibit mGluR4a receptorConcentration required to inhibit mGluR4a receptor
ChEMBL 221 3 3 3 -0.8 N[C@H](C(=O)O)C12C3C4C1C1C2C3C41C(=O)O 10.1016/s0960-894x(98)00265-0
CHEMBL2021372 80733 9 None - 1 Human 4.7 pEC50 = 4.7 Binding
Concentration required to inhibit mGluR4a receptorConcentration required to inhibit mGluR4a receptor
ChEMBL 221 3 3 3 -0.8 N[C@H](C(=O)O)C12C3C4C1C1C2C3C41C(=O)O 10.1016/s0960-894x(98)00265-0
56649042 75560 0 None - 0 Rat 6.7 pEC50 = 6.7 Binding
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)c1nccs1 10.1021/jm200956q
CHEMBL1921951 75560 0 None - 0 Rat 6.7 pEC50 = 6.7 Binding
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)c1nccs1 10.1021/jm200956q
44572113 195677 4 None - 0 Rat 5.7 pEC50 = 5.7 Binding
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 294 2 2 4 2.7 O=C(Nc1ccccc1)[C@]12C[C@H]1/C(=N\O)c1ccccc1O2 10.1021/jm9005065
CHEMBL507522 195677 4 None - 0 Rat 5.7 pEC50 = 5.7 Binding
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 294 2 2 4 2.7 O=C(Nc1ccccc1)[C@]12C[C@H]1/C(=N\O)c1ccccc1O2 10.1021/jm9005065
134190173 178934 0 None - 0 Rat 6.7 pEC50 = 6.7 Binding
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 265 2 2 5 3.2 Cc1noc2ccc(Nc3n[nH]c4ncccc34)cc12 10.1021/acs.jmedchem.8b00994
CHEMBL4473211 178934 0 None - 0 Rat 6.7 pEC50 = 6.7 Binding
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 265 2 2 5 3.2 Cc1noc2ccc(Nc3n[nH]c4ncccc34)cc12 10.1021/acs.jmedchem.8b00994
44191178 203038 0 None - 0 Rat 6.7 pEC50 = 6.7 Binding
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 242 3 1 3 2.7 COc1cc(NC(=O)c2ccccn2)ccc1C 10.1021/jm9005065
CHEMBL561835 203038 0 None - 0 Rat 6.7 pEC50 = 6.7 Binding
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 242 3 1 3 2.7 COc1cc(NC(=O)c2ccccn2)ccc1C 10.1021/jm9005065
155518354 177044 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at mGlu4 (unknown origin)Agonist activity at mGlu4 (unknown origin)
ChEMBL 371 3 0 4 4.6 CCc1nn2c(C(F)(F)F)cc(C)nc2c1-c1cc(F)c(OC)cc1F 10.1039/C8MD00524A
CHEMBL4446107 177044 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at mGlu4 (unknown origin)Agonist activity at mGlu4 (unknown origin)
ChEMBL 371 3 0 4 4.6 CCc1nn2c(C(F)(F)F)cc(C)nc2c1-c1cc(F)c(OC)cc1F 10.1039/C8MD00524A
10846649 108008 4 None - 0 Human 4.6 pEC50 = 4.6 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 4Compound was tested for the inhibition of Metabotropic glutamate receptor 4
ChEMBL 185 2 3 3 -0.5 N[C@@]1(C(=O)O)C[C@@H]2C[C@H]1[C@H]2C(=O)O 10.1021/jm970719q
CHEMBL296054 108008 4 None - 0 Human 4.6 pEC50 = 4.6 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 4Compound was tested for the inhibition of Metabotropic glutamate receptor 4
ChEMBL 185 2 3 3 -0.5 N[C@@]1(C(=O)O)C[C@@H]2C[C@H]1[C@H]2C(=O)O 10.1021/jm970719q
49865452 22744 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Positive allosteric modulation of human mGlu4 receptorPositive allosteric modulation of human mGlu4 receptor
ChEMBL 386 5 1 4 4.0 O=C(Nc1ccc(S(=O)(=O)Cc2ccccc2Cl)cc1)c1ccccn1 10.1016/j.bmcl.2016.05.029
CHEMBL1223384 22744 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Positive allosteric modulation of human mGlu4 receptorPositive allosteric modulation of human mGlu4 receptor
ChEMBL 386 5 1 4 4.0 O=C(Nc1ccc(S(=O)(=O)Cc2ccccc2Cl)cc1)c1ccccn1 10.1016/j.bmcl.2016.05.029
39869221 186550 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Activation of human mGluR4 expressed in CHO cells coexpressing Gqi5 protein assessed as potentiation of glutamate-induced responseActivation of human mGluR4 expressed in CHO cells coexpressing Gqi5 protein assessed as potentiation of glutamate-induced response
ChEMBL 278 3 2 5 3.1 Cc1nc2ccccc2nc1N/N=C/c1cccc(O)c1 10.1016/j.bmcl.2008.11.104
CHEMBL474453 186550 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Activation of human mGluR4 expressed in CHO cells coexpressing Gqi5 protein assessed as potentiation of glutamate-induced responseActivation of human mGluR4 expressed in CHO cells coexpressing Gqi5 protein assessed as potentiation of glutamate-induced response
ChEMBL 278 3 2 5 3.1 Cc1nc2ccccc2nc1N/N=C/c1cccc(O)c1 10.1016/j.bmcl.2008.11.104
2447227 204613 14 None - 0 Rat 5.6 pEC50 = 5.6 Binding
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 258 4 1 4 2.4 COc1ccc(NC(=O)c2ccccn2)cc1OC 10.1021/jm9005065
CHEMBL572346 204613 14 None - 0 Rat 5.6 pEC50 = 5.6 Binding
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 258 4 1 4 2.4 COc1ccc(NC(=O)c2ccccn2)cc1OC 10.1021/jm9005065
46853682 75559 0 None - 0 Rat 6.6 pEC50 = 6.6 Binding
Positive allosteric modulator activity at rat mGlu4 receptor by thallium flux assayPositive allosteric modulator activity at rat mGlu4 receptor by thallium flux assay
ChEMBL 416 3 1 7 1.6 O=C(Nc1ccc(N2S(=O)(=O)c3ccccc3S2(=O)=O)cc1)c1ccncn1 10.1021/jm200956q
CHEMBL1921950 75559 0 None - 0 Rat 6.6 pEC50 = 6.6 Binding
Positive allosteric modulator activity at rat mGlu4 receptor by thallium flux assayPositive allosteric modulator activity at rat mGlu4 receptor by thallium flux assay
ChEMBL 416 3 1 7 1.6 O=C(Nc1ccc(N2S(=O)(=O)c3ccccc3S2(=O)=O)cc1)c1ccncn1 10.1021/jm200956q
56649127 75568 0 None - 0 Rat 6.6 pEC50 = 6.6 Binding
Positive allosteric modulator activity at rat mGlu4 receptor by thallium flux assayPositive allosteric modulator activity at rat mGlu4 receptor by thallium flux assay
ChEMBL 407 3 1 4 3.7 O=C(Nc1ccc(N2C(=O)[C@H]3[C@@H]4C=C[C@@H](CC4)[C@H]3C2=O)c(Cl)c1)c1ccccn1 10.1021/jm200956q
CHEMBL1921962 75568 0 None - 0 Rat 6.6 pEC50 = 6.6 Binding
Positive allosteric modulator activity at rat mGlu4 receptor by thallium flux assayPositive allosteric modulator activity at rat mGlu4 receptor by thallium flux assay
ChEMBL 407 3 1 4 3.7 O=C(Nc1ccc(N2C(=O)[C@H]3[C@@H]4C=C[C@@H](CC4)[C@H]3C2=O)c(Cl)c1)c1ccccn1 10.1021/jm200956q
44282403 119188 10 None - 0 Human 4.6 pEC50 = 4.6 Binding
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 209 2 4 3 -0.5 N[C@@]1(C(=O)O)CC[C@@H](P(=O)(O)O)C1 10.1016/s0960-894x(00)00247-x
CHEMBL32976 119188 10 None - 0 Human 4.6 pEC50 = 4.6 Binding
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 209 2 4 3 -0.5 N[C@@]1(C(=O)O)CC[C@@H](P(=O)(O)O)C1 10.1016/s0960-894x(00)00247-x
162643926 188576 0 None - 0 Rat 6.6 pEC50 = 6.6 Binding
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 318 2 2 3 2.6 O=C1CCSC[C@@H](C(=O)Nc2cc(Cl)cc(Cl)c2)N1 10.1016/j.bmcl.2021.127838
CHEMBL4777988 188576 0 None - 0 Rat 6.6 pEC50 = 6.6 Binding
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 318 2 2 3 2.6 O=C1CCSC[C@@H](C(=O)Nc2cc(Cl)cc(Cl)c2)N1 10.1016/j.bmcl.2021.127838
162660686 188104 0 None - 0 Rat 6.6 pEC50 = 6.6 Binding
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 302 2 2 3 2.0 O=C1CCSC[C@@H](C(=O)Nc2cc(F)cc(Cl)c2)N1 10.1016/j.bmcl.2021.127838
CHEMBL4762773 188104 0 None - 0 Rat 6.6 pEC50 = 6.6 Binding
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 302 2 2 3 2.0 O=C1CCSC[C@@H](C(=O)Nc2cc(F)cc(Cl)c2)N1 10.1016/j.bmcl.2021.127838
6234 10810 68 None - 0 Rat 6.5 pEC50 = 6.5 Binding
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 232 2 1 2 3.0 Clc1cccc(c1)NC(=O)c1ccccn1 10.1021/jm9005065
836002 10810 68 None - 0 Rat 6.5 pEC50 = 6.5 Binding
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 232 2 1 2 3.0 Clc1cccc(c1)NC(=O)c1ccccn1 10.1021/jm9005065
CHEMBL556667 10810 68 None - 0 Rat 6.5 pEC50 = 6.5 Binding
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 232 2 1 2 3.0 Clc1cccc(c1)NC(=O)c1ccccn1 10.1021/jm9005065
122187789 129849 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Positive allosteric modulator activity at human mGlu4 receptorPositive allosteric modulator activity at human mGlu4 receptor
ChEMBL 393 3 1 4 3.3 O=C(Nc1ccc(N2C(=O)C3C(C2=O)[C@H]2C=C[C@@H]3C2)c(Cl)c1)c1ccccn1 10.1016/j.bmcl.2015.07.031
CHEMBL3609730 129849 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Positive allosteric modulator activity at human mGlu4 receptorPositive allosteric modulator activity at human mGlu4 receptor
ChEMBL 393 3 1 4 3.3 O=C(Nc1ccc(N2C(=O)C3C(C2=O)[C@H]2C=C[C@@H]3C2)c(Cl)c1)c1ccccn1 10.1016/j.bmcl.2015.07.031
162647509 190416 0 None - 0 Rat 7.5 pEC50 = 7.5 Binding
Positive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glutamate by CODA-RET assayPositive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glutamate by CODA-RET assay
ChEMBL 1134 27 6 12 10.6 COc1cc(NC(=O)c2ccccn2)ccc1NC(=O)c1ccc(NC(=O)COCC(=O)NCCCCCCCNC(=O)COc2ccc(-c3cccc(COc4cc5c(c(C)c4C)C(=O)C(C4CCCC4)C5)c3)cc2C(=O)O)cc1Cl 10.1016/j.bmcl.2020.127212
CHEMBL4744407 190416 0 None - 0 Rat 7.5 pEC50 = 7.5 Binding
Positive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glutamate by CODA-RET assayPositive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glutamate by CODA-RET assay
ChEMBL 1134 27 6 12 10.6 COc1cc(NC(=O)c2ccccn2)ccc1NC(=O)c1ccc(NC(=O)COCC(=O)NCCCCCCCNC(=O)COc2ccc(-c3cccc(COc4cc5c(c(C)c4C)C(=O)C(C4CCCC4)C5)c3)cc2C(=O)O)cc1Cl 10.1016/j.bmcl.2020.127212
CHEMBL4802513 190416 0 None - 0 Rat 7.5 pEC50 = 7.5 Binding
Positive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glutamate by CODA-RET assayPositive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glutamate by CODA-RET assay
ChEMBL 1134 27 6 12 10.6 COc1cc(NC(=O)c2ccccn2)ccc1NC(=O)c1ccc(NC(=O)COCC(=O)NCCCCCCCNC(=O)COc2ccc(-c3cccc(COc4cc5c(c(C)c4C)C(=O)C(C4CCCC4)C5)c3)cc2C(=O)O)cc1Cl 10.1016/j.bmcl.2020.127212
4052597 10793 9 None - 0 Human 5.5 pEC50 = 5.5 Binding
Activation of human mGluR4 expressed in CHO cells coexpressing Gqi5 protein assessed as potentiation of glutamate-induced responseActivation of human mGluR4 expressed in CHO cells coexpressing Gqi5 protein assessed as potentiation of glutamate-induced response
ChEMBL 342 3 1 2 5.2 Cc1ccc(cc1)N1C(Nc2c(C1=O)cccc2)C(c1ccccc1)C 10.1016/j.bmcl.2008.11.104
6229 10793 9 None - 0 Human 5.5 pEC50 = 5.5 Binding
Activation of human mGluR4 expressed in CHO cells coexpressing Gqi5 protein assessed as potentiation of glutamate-induced responseActivation of human mGluR4 expressed in CHO cells coexpressing Gqi5 protein assessed as potentiation of glutamate-induced response
ChEMBL 342 3 1 2 5.2 Cc1ccc(cc1)N1C(Nc2c(C1=O)cccc2)C(c1ccccc1)C 10.1016/j.bmcl.2008.11.104
CHEMBL473806 10793 9 None - 0 Human 5.5 pEC50 = 5.5 Binding
Activation of human mGluR4 expressed in CHO cells coexpressing Gqi5 protein assessed as potentiation of glutamate-induced responseActivation of human mGluR4 expressed in CHO cells coexpressing Gqi5 protein assessed as potentiation of glutamate-induced response
ChEMBL 342 3 1 2 5.2 Cc1ccc(cc1)N1C(Nc2c(C1=O)cccc2)C(c1ccccc1)C 10.1016/j.bmcl.2008.11.104
1410 9054 48 None -3 6 Human 6.5 pEC50 = 6.5 Binding
Activation of human metabotropic glutamate 4 receptor expressed in golden hamster AV12-664 cellsActivation of human metabotropic glutamate 4 receptor expressed in golden hamster AV12-664 cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.8b01120
1412 9054 48 None -3 6 Human 6.5 pEC50 = 6.5 Binding
Activation of human metabotropic glutamate 4 receptor expressed in golden hamster AV12-664 cellsActivation of human metabotropic glutamate 4 receptor expressed in golden hamster AV12-664 cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.8b01120
179394 9054 48 None -3 6 Human 6.5 pEC50 = 6.5 Binding
Activation of human metabotropic glutamate 4 receptor expressed in golden hamster AV12-664 cellsActivation of human metabotropic glutamate 4 receptor expressed in golden hamster AV12-664 cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.8b01120
57689795 9054 48 None -3 6 Human 6.5 pEC50 = 6.5 Binding
Activation of human metabotropic glutamate 4 receptor expressed in golden hamster AV12-664 cellsActivation of human metabotropic glutamate 4 receptor expressed in golden hamster AV12-664 cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.8b01120
CHEMBL33567 9054 48 None -3 6 Human 6.5 pEC50 = 6.5 Binding
Activation of human metabotropic glutamate 4 receptor expressed in golden hamster AV12-664 cellsActivation of human metabotropic glutamate 4 receptor expressed in golden hamster AV12-664 cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/acs.jmedchem.8b01120
162646759 190411 0 None - 0 Rat 7.5 pEC50 = 7.5 Binding
Positive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glutamate by CODA-RET assayPositive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glutamate by CODA-RET assay
ChEMBL 1148 28 6 12 11.0 COc1cc(NC(=O)c2ccccn2)ccc1NC(=O)c1ccc(NC(=O)COCC(=O)NCCCCCCCCNC(=O)COc2ccc(-c3cccc(COc4cc5c(c(C)c4C)C(=O)C(C4CCCC4)C5)c3)cc2C(=O)O)cc1Cl 10.1016/j.bmcl.2020.127212
CHEMBL4740929 190411 0 None - 0 Rat 7.5 pEC50 = 7.5 Binding
Positive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glutamate by CODA-RET assayPositive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glutamate by CODA-RET assay
ChEMBL 1148 28 6 12 11.0 COc1cc(NC(=O)c2ccccn2)ccc1NC(=O)c1ccc(NC(=O)COCC(=O)NCCCCCCCCNC(=O)COc2ccc(-c3cccc(COc4cc5c(c(C)c4C)C(=O)C(C4CCCC4)C5)c3)cc2C(=O)O)cc1Cl 10.1016/j.bmcl.2020.127212
CHEMBL4802473 190411 0 None - 0 Rat 7.5 pEC50 = 7.5 Binding
Positive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glutamate by CODA-RET assayPositive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glutamate by CODA-RET assay
ChEMBL 1148 28 6 12 11.0 COc1cc(NC(=O)c2ccccn2)ccc1NC(=O)c1ccc(NC(=O)COCC(=O)NCCCCCCCCNC(=O)COc2ccc(-c3cccc(COc4cc5c(c(C)c4C)C(=O)C(C4CCCC4)C5)c3)cc2C(=O)O)cc1Cl 10.1016/j.bmcl.2020.127212
162660656 190485 0 None - 0 Rat 7.5 pEC50 = 7.5 Binding
Positive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glutamate by CODA-RET assayPositive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glutamate by CODA-RET assay
ChEMBL 1120 26 6 12 10.2 COc1cc(NC(=O)c2ccccn2)ccc1NC(=O)c1ccc(NC(=O)COCC(=O)NCCCCCCNC(=O)COc2ccc(-c3cccc(COc4cc5c(c(C)c4C)C(=O)C(C4CCCC4)C5)c3)cc2C(=O)O)cc1Cl 10.1016/j.bmcl.2020.127212
CHEMBL4762369 190485 0 None - 0 Rat 7.5 pEC50 = 7.5 Binding
Positive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glutamate by CODA-RET assayPositive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glutamate by CODA-RET assay
ChEMBL 1120 26 6 12 10.2 COc1cc(NC(=O)c2ccccn2)ccc1NC(=O)c1ccc(NC(=O)COCC(=O)NCCCCCCNC(=O)COc2ccc(-c3cccc(COc4cc5c(c(C)c4C)C(=O)C(C4CCCC4)C5)c3)cc2C(=O)O)cc1Cl 10.1016/j.bmcl.2020.127212
CHEMBL4803219 190485 0 None - 0 Rat 7.5 pEC50 = 7.5 Binding
Positive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glutamate by CODA-RET assayPositive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glutamate by CODA-RET assay
ChEMBL 1120 26 6 12 10.2 COc1cc(NC(=O)c2ccccn2)ccc1NC(=O)c1ccc(NC(=O)COCC(=O)NCCCCCCNC(=O)COc2ccc(-c3cccc(COc4cc5c(c(C)c4C)C(=O)C(C4CCCC4)C5)c3)cc2C(=O)O)cc1Cl 10.1016/j.bmcl.2020.127212
92044496 162746 0 None - 0 Rat 6.5 pEC50 = 6.5 Binding
Agonist activity at mGlu4 in Wistar rat striatum assessed as decrease in striatal GABAergic inhibitory post-synaptic potential by whole cell patch clamp assayAgonist activity at mGlu4 in Wistar rat striatum assessed as decrease in striatal GABAergic inhibitory post-synaptic potential by whole cell patch clamp assay
ChEMBL 324 7 4 7 0.7 N[C@@H](CCP(=O)(O)C(O)c1csc([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4061423 162746 0 None - 0 Rat 6.5 pEC50 = 6.5 Binding
Agonist activity at mGlu4 in Wistar rat striatum assessed as decrease in striatal GABAergic inhibitory post-synaptic potential by whole cell patch clamp assayAgonist activity at mGlu4 in Wistar rat striatum assessed as decrease in striatal GABAergic inhibitory post-synaptic potential by whole cell patch clamp assay
ChEMBL 324 7 4 7 0.7 N[C@@H](CCP(=O)(O)C(O)c1csc([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
1310 9095 110 None -4 18 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at human mGluR4 receptor expressed in HEK cellsAgonist activity at human mGluR4 receptor expressed in HEK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1039/C1MD00186H
1369 9095 110 None -4 18 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at human mGluR4 receptor expressed in HEK cellsAgonist activity at human mGluR4 receptor expressed in HEK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1039/C1MD00186H
33032 9095 110 None -4 18 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at human mGluR4 receptor expressed in HEK cellsAgonist activity at human mGluR4 receptor expressed in HEK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1039/C1MD00186H
44272391 9095 110 None -4 18 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at human mGluR4 receptor expressed in HEK cellsAgonist activity at human mGluR4 receptor expressed in HEK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1039/C1MD00186H
88747398 9095 110 None -4 18 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at human mGluR4 receptor expressed in HEK cellsAgonist activity at human mGluR4 receptor expressed in HEK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1039/C1MD00186H
CHEMBL575060 9095 110 None -4 18 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at human mGluR4 receptor expressed in HEK cellsAgonist activity at human mGluR4 receptor expressed in HEK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1039/C1MD00186H
DB00142 9095 110 None -4 18 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at human mGluR4 receptor expressed in HEK cellsAgonist activity at human mGluR4 receptor expressed in HEK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1039/C1MD00186H
1310 9095 110 None -26 18 Rat 5.5 pEC50 = 5.5 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR4a in ratConcentration for half maximal activation of metabotropic glutamate mGluR4a in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
1369 9095 110 None -26 18 Rat 5.5 pEC50 = 5.5 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR4a in ratConcentration for half maximal activation of metabotropic glutamate mGluR4a in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
33032 9095 110 None -26 18 Rat 5.5 pEC50 = 5.5 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR4a in ratConcentration for half maximal activation of metabotropic glutamate mGluR4a in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
44272391 9095 110 None -26 18 Rat 5.5 pEC50 = 5.5 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR4a in ratConcentration for half maximal activation of metabotropic glutamate mGluR4a in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
88747398 9095 110 None -26 18 Rat 5.5 pEC50 = 5.5 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR4a in ratConcentration for half maximal activation of metabotropic glutamate mGluR4a in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
CHEMBL575060 9095 110 None -26 18 Rat 5.5 pEC50 = 5.5 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR4a in ratConcentration for half maximal activation of metabotropic glutamate mGluR4a in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
DB00142 9095 110 None -26 18 Rat 5.5 pEC50 = 5.5 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR4a in ratConcentration for half maximal activation of metabotropic glutamate mGluR4a in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
10238 10799 26 None - 0 Human 5.5 pEC50 = 5.5 Binding
Positive allosteric modulation of mGluR4 (unknown origin)Positive allosteric modulation of mGluR4 (unknown origin)
ChEMBL 436 7 1 6 4.8 COC(=O)c1ccc(cc1)n1c(C)cc(c1C)C(=O)CSc1ccc(cc1)NC(=O)C 10.1016/j.bmcl.2022.129106
4043841 10799 26 None - 0 Human 5.5 pEC50 = 5.5 Binding
Positive allosteric modulation of mGluR4 (unknown origin)Positive allosteric modulation of mGluR4 (unknown origin)
ChEMBL 436 7 1 6 4.8 COC(=O)c1ccc(cc1)n1c(C)cc(c1C)C(=O)CSc1ccc(cc1)NC(=O)C 10.1016/j.bmcl.2022.129106
CHEMBL1585091 10799 26 None - 0 Human 5.5 pEC50 = 5.5 Binding
Positive allosteric modulation of mGluR4 (unknown origin)Positive allosteric modulation of mGluR4 (unknown origin)
ChEMBL 436 7 1 6 4.8 COC(=O)c1ccc(cc1)n1c(C)cc(c1C)C(=O)CSc1ccc(cc1)NC(=O)C 10.1016/j.bmcl.2022.129106
162656140 187717 0 None - 0 Rat 7.5 pEC50 = 7.5 Binding
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 362 2 2 3 2.7 O=C1CCSC[C@@H](C(=O)Nc2cc(Cl)cc(Br)c2)N1 10.1016/j.bmcl.2021.127838
CHEMBL4758183 187717 0 None - 0 Rat 7.5 pEC50 = 7.5 Binding
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 362 2 2 3 2.7 O=C1CCSC[C@@H](C(=O)Nc2cc(Cl)cc(Br)c2)N1 10.1016/j.bmcl.2021.127838
162666879 190512 0 None - 0 Rat 7.5 pEC50 = 7.5 Binding
Positive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glutamate by CODA-RET assayPositive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glutamate by CODA-RET assay
ChEMBL 1092 24 6 12 9.4 COc1cc(NC(=O)c2ccccn2)ccc1NC(=O)c1ccc(NC(=O)COCC(=O)NCCCCNC(=O)COc2ccc(-c3cccc(COc4cc5c(c(C)c4C)C(=O)C(C4CCCC4)C5)c3)cc2C(=O)O)cc1Cl 10.1016/j.bmcl.2020.127212
CHEMBL4786847 190512 0 None - 0 Rat 7.5 pEC50 = 7.5 Binding
Positive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glutamate by CODA-RET assayPositive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glutamate by CODA-RET assay
ChEMBL 1092 24 6 12 9.4 COc1cc(NC(=O)c2ccccn2)ccc1NC(=O)c1ccc(NC(=O)COCC(=O)NCCCCNC(=O)COc2ccc(-c3cccc(COc4cc5c(c(C)c4C)C(=O)C(C4CCCC4)C5)c3)cc2C(=O)O)cc1Cl 10.1016/j.bmcl.2020.127212
CHEMBL4803552 190512 0 None - 0 Rat 7.5 pEC50 = 7.5 Binding
Positive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glutamate by CODA-RET assayPositive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glutamate by CODA-RET assay
ChEMBL 1092 24 6 12 9.4 COc1cc(NC(=O)c2ccccn2)ccc1NC(=O)c1ccc(NC(=O)COCC(=O)NCCCCNC(=O)COc2ccc(-c3cccc(COc4cc5c(c(C)c4C)C(=O)C(C4CCCC4)C5)c3)cc2C(=O)O)cc1Cl 10.1016/j.bmcl.2020.127212
2207 106641 63 None - 7 Human 6.5 pEC50 = 6.5 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 4Compound was tested for the inhibition of Metabotropic glutamate receptor 4
ChEMBL 183 4 4 3 -1.0 NC(CCP(=O)(O)O)C(=O)O 10.1021/jm970719q
CHEMBL285843 106641 63 None - 7 Human 6.5 pEC50 = 6.5 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 4Compound was tested for the inhibition of Metabotropic glutamate receptor 4
ChEMBL 183 4 4 3 -1.0 NC(CCP(=O)(O)O)C(=O)O 10.1021/jm970719q
6234 10810 68 None - 0 Rat 6.5 pEC50 = 6.5 Binding
Positive allosteric modulator activity at rat mGlu4 receptorPositive allosteric modulator activity at rat mGlu4 receptor
ChEMBL 232 2 1 2 3.0 Clc1cccc(c1)NC(=O)c1ccccn1 10.1016/j.bmcl.2015.07.031
836002 10810 68 None - 0 Rat 6.5 pEC50 = 6.5 Binding
Positive allosteric modulator activity at rat mGlu4 receptorPositive allosteric modulator activity at rat mGlu4 receptor
ChEMBL 232 2 1 2 3.0 Clc1cccc(c1)NC(=O)c1ccccn1 10.1016/j.bmcl.2015.07.031
CHEMBL556667 10810 68 None - 0 Rat 6.5 pEC50 = 6.5 Binding
Positive allosteric modulator activity at rat mGlu4 receptorPositive allosteric modulator activity at rat mGlu4 receptor
ChEMBL 232 2 1 2 3.0 Clc1cccc(c1)NC(=O)c1ccccn1 10.1016/j.bmcl.2015.07.031
46869940 64669 4 None - 0 Rat 7.5 pEC50 = 7.5 Binding
Positive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glutamate by CODA-RET assayPositive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glutamate by CODA-RET assay
ChEMBL 381 5 2 4 4.2 COc1cc(NC(=O)c2ccccn2)ccc1NC(=O)c1ccccc1Cl 10.1016/j.bmcl.2020.127212
CHEMBL1672234 64669 4 None - 0 Rat 7.5 pEC50 = 7.5 Binding
Positive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glutamate by CODA-RET assayPositive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glutamate by CODA-RET assay
ChEMBL 381 5 2 4 4.2 COc1cc(NC(=O)c2ccccn2)ccc1NC(=O)c1ccccc1Cl 10.1016/j.bmcl.2020.127212
46869944 65901 0 None - 0 Rat 7.5 pEC50 = 7.5 Binding
Positive allosteric modulator activity at rat mGlu4 receptor by thallium flux assayPositive allosteric modulator activity at rat mGlu4 receptor by thallium flux assay
ChEMBL 411 3 1 4 4.4 O=C(Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(Cl)c1)c1ccccn1 10.1021/jm200956q
CHEMBL1698378 65901 0 None - 0 Rat 7.5 pEC50 = 7.5 Binding
Positive allosteric modulator activity at rat mGlu4 receptor by thallium flux assayPositive allosteric modulator activity at rat mGlu4 receptor by thallium flux assay
ChEMBL 411 3 1 4 4.4 O=C(Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(Cl)c1)c1ccccn1 10.1021/jm200956q
44189740 201709 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Positive allosteric modulator activity at human mGlu4 receptorPositive allosteric modulator activity at human mGlu4 receptor
ChEMBL 264 4 1 3 2.9 O=C(Nc1cccc(OC(F)F)c1)c1ccccn1 10.1016/j.bmcl.2015.07.031
CHEMBL541754 201709 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Positive allosteric modulator activity at human mGlu4 receptorPositive allosteric modulator activity at human mGlu4 receptor
ChEMBL 264 4 1 3 2.9 O=C(Nc1cccc(OC(F)F)c1)c1ccccn1 10.1016/j.bmcl.2015.07.031
162647308 186368 0 None - 0 Rat 7.5 pEC50 = 7.5 Binding
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 406 2 2 3 2.8 O=C1CCSC[C@@H](C(=O)Nc2cc(Br)cc(Br)c2)N1 10.1016/j.bmcl.2021.127838
CHEMBL4742127 186368 0 None - 0 Rat 7.5 pEC50 = 7.5 Binding
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 406 2 2 3 2.8 O=C1CCSC[C@@H](C(=O)Nc2cc(Br)cc(Br)c2)N1 10.1016/j.bmcl.2021.127838
162644103 190398 0 None - 0 Rat 7.5 pEC50 = 7.5 Binding
Positive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glutamate by CODA-RET assayPositive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glutamate by CODA-RET assay
ChEMBL 1106 25 6 12 9.8 COc1cc(NC(=O)c2ccccn2)ccc1NC(=O)c1ccc(NC(=O)COCC(=O)NCCCCCNC(=O)COc2ccc(-c3cccc(COc4cc5c(c(C)c4C)C(=O)C(C4CCCC4)C5)c3)cc2C(=O)O)cc1Cl 10.1016/j.bmcl.2020.127212
CHEMBL4777845 190398 0 None - 0 Rat 7.5 pEC50 = 7.5 Binding
Positive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glutamate by CODA-RET assayPositive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glutamate by CODA-RET assay
ChEMBL 1106 25 6 12 9.8 COc1cc(NC(=O)c2ccccn2)ccc1NC(=O)c1ccc(NC(=O)COCC(=O)NCCCCCNC(=O)COc2ccc(-c3cccc(COc4cc5c(c(C)c4C)C(=O)C(C4CCCC4)C5)c3)cc2C(=O)O)cc1Cl 10.1016/j.bmcl.2020.127212
CHEMBL4802343 190398 0 None - 0 Rat 7.5 pEC50 = 7.5 Binding
Positive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glutamate by CODA-RET assayPositive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glutamate by CODA-RET assay
ChEMBL 1106 25 6 12 9.8 COc1cc(NC(=O)c2ccccn2)ccc1NC(=O)c1ccc(NC(=O)COCC(=O)NCCCCCNC(=O)COc2ccc(-c3cccc(COc4cc5c(c(C)c4C)C(=O)C(C4CCCC4)C5)c3)cc2C(=O)O)cc1Cl 10.1016/j.bmcl.2020.127212
162650549 186927 0 None - 0 Rat 6.5 pEC50 = 6.5 Binding
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 346 2 2 3 2.1 O=C1CCSC[C@@H](C(=O)Nc2cc(F)cc(Br)c2)N1 10.1016/j.bmcl.2021.127838
CHEMBL4748883 186927 0 None - 0 Rat 6.5 pEC50 = 6.5 Binding
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 346 2 2 3 2.1 O=C1CCSC[C@@H](C(=O)Nc2cc(F)cc(Br)c2)N1 10.1016/j.bmcl.2021.127838
42644786 202110 2 None - 0 Rat 6.4 pEC50 = 6.4 Binding
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 246 3 1 3 2.5 COc1cc(NC(=O)c2ccccn2)ccc1F 10.1021/jm9005065
CHEMBL551635 202110 2 None - 0 Rat 6.4 pEC50 = 6.4 Binding
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 246 3 1 3 2.5 COc1cc(NC(=O)c2ccccn2)ccc1F 10.1021/jm9005065
122187789 129849 0 None - 0 Rat 6.4 pEC50 = 6.4 Binding
Positive allosteric modulator activity at rat mGlu4 receptorPositive allosteric modulator activity at rat mGlu4 receptor
ChEMBL 393 3 1 4 3.3 O=C(Nc1ccc(N2C(=O)C3C(C2=O)[C@H]2C=C[C@@H]3C2)c(Cl)c1)c1ccccn1 10.1016/j.bmcl.2015.07.031
CHEMBL3609730 129849 0 None - 0 Rat 6.4 pEC50 = 6.4 Binding
Positive allosteric modulator activity at rat mGlu4 receptorPositive allosteric modulator activity at rat mGlu4 receptor
ChEMBL 393 3 1 4 3.3 O=C(Nc1ccc(N2C(=O)C3C(C2=O)[C@H]2C=C[C@@H]3C2)c(Cl)c1)c1ccccn1 10.1016/j.bmcl.2015.07.031
54752951 75567 3 None - 0 Rat 6.4 pEC50 = 6.4 Binding
Positive allosteric modulator activity at rat mGlu4 receptor by thallium flux assayPositive allosteric modulator activity at rat mGlu4 receptor by thallium flux assay
ChEMBL 393 3 1 4 3.3 O=C(Nc1ccc(N2C(=O)[C@H]3[C@H]4C=C[C@H](C4)[C@H]3C2=O)c(Cl)c1)c1ccccn1 10.1021/jm200956q
CHEMBL1921961 75567 3 None - 0 Rat 6.4 pEC50 = 6.4 Binding
Positive allosteric modulator activity at rat mGlu4 receptor by thallium flux assayPositive allosteric modulator activity at rat mGlu4 receptor by thallium flux assay
ChEMBL 393 3 1 4 3.3 O=C(Nc1ccc(N2C(=O)[C@H]3[C@H]4C=C[C@H](C4)[C@H]3C2=O)c(Cl)c1)c1ccccn1 10.1021/jm200956q
162677305 190572 0 None - 0 Rat 7.4 pEC50 = 7.4 Binding
Positive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glutamate by CODA-RET assayPositive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glutamate by CODA-RET assay
ChEMBL 1078 23 6 12 9.0 COc1cc(NC(=O)c2ccccn2)ccc1NC(=O)c1ccc(NC(=O)COCC(=O)NCCCNC(=O)COc2ccc(-c3cccc(COc4cc5c(c(C)c4C)C(=O)C(C4CCCC4)C5)c3)cc2C(=O)O)cc1Cl 10.1016/j.bmcl.2020.127212
CHEMBL4800093 190572 0 None - 0 Rat 7.4 pEC50 = 7.4 Binding
Positive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glutamate by CODA-RET assayPositive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glutamate by CODA-RET assay
ChEMBL 1078 23 6 12 9.0 COc1cc(NC(=O)c2ccccn2)ccc1NC(=O)c1ccc(NC(=O)COCC(=O)NCCCNC(=O)COc2ccc(-c3cccc(COc4cc5c(c(C)c4C)C(=O)C(C4CCCC4)C5)c3)cc2C(=O)O)cc1Cl 10.1016/j.bmcl.2020.127212
CHEMBL4804159 190572 0 None - 0 Rat 7.4 pEC50 = 7.4 Binding
Positive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glutamate by CODA-RET assayPositive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glutamate by CODA-RET assay
ChEMBL 1078 23 6 12 9.0 COc1cc(NC(=O)c2ccccn2)ccc1NC(=O)c1ccc(NC(=O)COCC(=O)NCCCNC(=O)COc2ccc(-c3cccc(COc4cc5c(c(C)c4C)C(=O)C(C4CCCC4)C5)c3)cc2C(=O)O)cc1Cl 10.1016/j.bmcl.2020.127212
70682300 83396 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Positive allosteric modulation activity at mGlu4 receptorPositive allosteric modulation activity at mGlu4 receptor
ChEMBL 295 2 2 5 2.1 O=C(Nc1ccccn1)[C@]12C[C@H]1/C(=N\O)c1ccccc1O2 10.1021/jm201139r
CHEMBL2063423 83396 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Positive allosteric modulation activity at mGlu4 receptorPositive allosteric modulation activity at mGlu4 receptor
ChEMBL 295 2 2 5 2.1 O=C(Nc1ccccn1)[C@]12C[C@H]1/C(=N\O)c1ccccc1O2 10.1021/jm201139r
104766 6822 42 None -61 11 Human 4.4 pEC50 = 4.4 Binding
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 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1016/s0960-894x(00)00247-x
1365 6822 42 None -61 11 Human 4.4 pEC50 = 4.4 Binding
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 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1016/s0960-894x(00)00247-x
CHEMBL34453 6822 42 None -61 11 Human 4.4 pEC50 = 4.4 Binding
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 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1016/s0960-894x(00)00247-x
104766 6822 42 None - 11 Rat 4.4 pEC50 = 4.4 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR4a in ratConcentration for half maximal activation of metabotropic glutamate mGluR4a in rat
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1021/jm00009a001
1365 6822 42 None - 11 Rat 4.4 pEC50 = 4.4 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR4a in ratConcentration for half maximal activation of metabotropic glutamate mGluR4a in rat
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1021/jm00009a001
CHEMBL34453 6822 42 None - 11 Rat 4.4 pEC50 = 4.4 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR4a in ratConcentration for half maximal activation of metabotropic glutamate mGluR4a in rat
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1021/jm00009a001
46869951 66073 0 None - 0 Rat 6.4 pEC50 = 6.4 Binding
Positive allosteric modulator activity at rat mGlu4 receptor by thallium flux assayPositive allosteric modulator activity at rat mGlu4 receptor by thallium flux assay
ChEMBL 397 3 1 4 4.2 O=C(Nc1ccc(N2C(=O)CC3(CCCCC3)C2=O)c(Cl)c1)c1ccccn1 10.1021/jm200956q
CHEMBL1705230 66073 0 None - 0 Rat 6.4 pEC50 = 6.4 Binding
Positive allosteric modulator activity at rat mGlu4 receptor by thallium flux assayPositive allosteric modulator activity at rat mGlu4 receptor by thallium flux assay
ChEMBL 397 3 1 4 4.2 O=C(Nc1ccc(N2C(=O)CC3(CCCCC3)C2=O)c(Cl)c1)c1ccccn1 10.1021/jm200956q
46836872 7088 47 None - 1 Human 8.4 pEC50 = 8.4 Binding
Positive allosteric modulator activity at human mGlu4 receptorPositive allosteric modulator activity at human mGlu4 receptor
ChEMBL 272 3 2 6 2.7 Cc1ccnc(n1)Nc1sc(c(n1)c1c[nH]nc1)C 10.1016/j.bmcl.2015.07.031
6238 7088 47 None - 1 Human 8.4 pEC50 = 8.4 Binding
Positive allosteric modulator activity at human mGlu4 receptorPositive allosteric modulator activity at human mGlu4 receptor
ChEMBL 272 3 2 6 2.7 Cc1ccnc(n1)Nc1sc(c(n1)c1c[nH]nc1)C 10.1016/j.bmcl.2015.07.031
CHEMBL3609729 7088 47 None - 1 Human 8.4 pEC50 = 8.4 Binding
Positive allosteric modulator activity at human mGlu4 receptorPositive allosteric modulator activity at human mGlu4 receptor
ChEMBL 272 3 2 6 2.7 Cc1ccnc(n1)Nc1sc(c(n1)c1c[nH]nc1)C 10.1016/j.bmcl.2015.07.031
1411 9140 66 None - 1 Rat 5.4 pEC50 = 5.4 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR4a in ratConcentration for half maximal activation of metabotropic glutamate mGluR4a in rat
ChEMBL 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 10.1021/jm00009a001
4120 9140 66 None - 1 Rat 5.4 pEC50 = 5.4 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR4a in ratConcentration for half maximal activation of metabotropic glutamate mGluR4a in rat
ChEMBL 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 10.1021/jm00009a001
57689797 9140 66 None - 1 Rat 5.4 pEC50 = 5.4 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR4a in ratConcentration for half maximal activation of metabotropic glutamate mGluR4a in rat
ChEMBL 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 10.1021/jm00009a001
68841 9140 66 None - 1 Rat 5.4 pEC50 = 5.4 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR4a in ratConcentration for half maximal activation of metabotropic glutamate mGluR4a in rat
ChEMBL 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 10.1021/jm00009a001
CHEMBL284377 9140 66 None - 1 Rat 5.4 pEC50 = 5.4 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR4a in ratConcentration for half maximal activation of metabotropic glutamate mGluR4a in rat
ChEMBL 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 10.1021/jm00009a001
DB04522 9140 66 None - 1 Rat 5.4 pEC50 = 5.4 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR4a in ratConcentration for half maximal activation of metabotropic glutamate mGluR4a in rat
ChEMBL 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 10.1021/jm00009a001
135411506 187703 4 None - 0 Human 5.4 pEC50 = 5.4 Binding
Activation of human mGluR4 expressed in CHO cells coexpressing Gqi5 protein assessed as potentiation of glutamate-induced responseActivation of human mGluR4 expressed in CHO cells coexpressing Gqi5 protein assessed as potentiation of glutamate-induced response
ChEMBL 278 3 2 5 3.1 Cc1nc2ccccc2nc1N/N=C/c1ccccc1O 10.1016/j.bmcl.2008.11.104
CHEMBL475800 187703 4 None - 0 Human 5.4 pEC50 = 5.4 Binding
Activation of human mGluR4 expressed in CHO cells coexpressing Gqi5 protein assessed as potentiation of glutamate-induced responseActivation of human mGluR4 expressed in CHO cells coexpressing Gqi5 protein assessed as potentiation of glutamate-induced response
ChEMBL 278 3 2 5 3.1 Cc1nc2ccccc2nc1N/N=C/c1ccccc1O 10.1016/j.bmcl.2008.11.104
45110136 122920 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
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 391 3 1 4 4.1 Cc1cccc2c1C(=O)N(c1ccc(NC(=O)c3ccccn3)cc1Cl)C2=O 10.1021/jm501245b
CHEMBL3357575 122920 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
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 391 3 1 4 4.1 Cc1cccc2c1C(=O)N(c1ccc(NC(=O)c3ccccn3)cc1Cl)C2=O 10.1021/jm501245b
45110136 122920 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Positive allosteric modulator activity at human mGlu4 receptorPositive allosteric modulator activity at human mGlu4 receptor
ChEMBL 391 3 1 4 4.1 Cc1cccc2c1C(=O)N(c1ccc(NC(=O)c3ccccn3)cc1Cl)C2=O 10.1016/j.bmcl.2015.07.031
CHEMBL3357575 122920 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Positive allosteric modulator activity at human mGlu4 receptorPositive allosteric modulator activity at human mGlu4 receptor
ChEMBL 391 3 1 4 4.1 Cc1cccc2c1C(=O)N(c1ccc(NC(=O)c3ccccn3)cc1Cl)C2=O 10.1016/j.bmcl.2015.07.031
12104636 187706 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Activation of human mGluR4 expressed in CHO cells coexpressing Gqi5 protein assessed as potentiation of glutamate-induced responseActivation of human mGluR4 expressed in CHO cells coexpressing Gqi5 protein assessed as potentiation of glutamate-induced response
ChEMBL 262 3 1 4 3.4 Cc1nc2ccccc2nc1N/N=C/c1ccccc1 10.1016/j.bmcl.2008.11.104
CHEMBL475801 187706 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Activation of human mGluR4 expressed in CHO cells coexpressing Gqi5 protein assessed as potentiation of glutamate-induced responseActivation of human mGluR4 expressed in CHO cells coexpressing Gqi5 protein assessed as potentiation of glutamate-induced response
ChEMBL 262 3 1 4 3.4 Cc1nc2ccccc2nc1N/N=C/c1ccccc1 10.1016/j.bmcl.2008.11.104
126582 91059 9 None - 0 Human 5.4 pEC50 = 5.4 Binding
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 207 2 4 3 -0.4 NC1(C(=O)O)CC(=CP(=O)(O)O)C1 10.1016/s0960-894x(00)00247-x
CHEMBL22136 91059 9 None - 0 Human 5.4 pEC50 = 5.4 Binding
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 207 2 4 3 -0.4 NC1(C(=O)O)CC(=CP(=O)(O)O)C1 10.1016/s0960-894x(00)00247-x
126582 91059 9 None - 0 Rat 5.4 pEC50 = 5.4 Binding
Effective concentration against rat Metabotropic glutamate receptor 4Effective concentration against rat Metabotropic glutamate receptor 4
ChEMBL 207 2 4 3 -0.4 NC1(C(=O)O)CC(=CP(=O)(O)O)C1 10.1016/s0960-894x(00)00197-9
CHEMBL22136 91059 9 None - 0 Rat 5.4 pEC50 = 5.4 Binding
Effective concentration against rat Metabotropic glutamate receptor 4Effective concentration against rat Metabotropic glutamate receptor 4
ChEMBL 207 2 4 3 -0.4 NC1(C(=O)O)CC(=CP(=O)(O)O)C1 10.1016/s0960-894x(00)00197-9
127047647 146537 0 None - 0 Rat 7.3 pEC50 = 7.3 Binding
Positive allosteric modulator activity at rat mGlu4 receptorPositive allosteric modulator activity at rat mGlu4 receptor
ChEMBL 369 5 2 6 3.7 CCc1cnc(Oc2ccc(NC(=O)c3ncccc3N)cc2Cl)nc1 10.1016/j.bmcl.2016.04.041
CHEMBL3798517 146537 0 None - 0 Rat 7.3 pEC50 = 7.3 Binding
Positive allosteric modulator activity at rat mGlu4 receptorPositive allosteric modulator activity at rat mGlu4 receptor
ChEMBL 369 5 2 6 3.7 CCc1cnc(Oc2ccc(NC(=O)c3ncccc3N)cc2Cl)nc1 10.1016/j.bmcl.2016.04.041
1406 8854 38 None -25 3 Human 5.3 pEC50 = 5.3 Binding
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 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10.1016/s0960-894x(00)00247-x
4545574 8854 38 None -25 3 Human 5.3 pEC50 = 5.3 Binding
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 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10.1016/s0960-894x(00)00247-x
CHEMBL277475 8854 38 None -25 3 Human 5.3 pEC50 = 5.3 Binding
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 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10.1016/s0960-894x(00)00247-x
45110765 65898 0 None - 0 Rat 6.3 pEC50 = 6.3 Binding
Positive allosteric modulator activity at rat mGlu4 receptor by thallium flux assayPositive allosteric modulator activity at rat mGlu4 receptor by thallium flux assay
ChEMBL 405 4 1 4 4.0 O=C(Nc1ccc(N2C(=O)CC(c3ccccc3)C2=O)c(Cl)c1)c1ccccn1 10.1021/jm200956q
CHEMBL1698322 65898 0 None - 0 Rat 6.3 pEC50 = 6.3 Binding
Positive allosteric modulator activity at rat mGlu4 receptor by thallium flux assayPositive allosteric modulator activity at rat mGlu4 receptor by thallium flux assay
ChEMBL 405 4 1 4 4.0 O=C(Nc1ccc(N2C(=O)CC(c3ccccc3)C2=O)c(Cl)c1)c1ccccn1 10.1021/jm200956q
45110133 122919 1 None - 0 Human 7.3 pEC50 = 7.3 Binding
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 395 3 1 4 3.9 O=C(Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1)c1ccccn1 10.1021/jm501245b
CHEMBL3357574 122919 1 None - 0 Human 7.3 pEC50 = 7.3 Binding
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 395 3 1 4 3.9 O=C(Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1)c1ccccn1 10.1021/jm501245b
738280 203062 8 None - 0 Rat 6.3 pEC50 = 6.3 Binding
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 242 2 1 4 2.1 O=C(Nc1ccc2c(c1)OCO2)c1ccccn1 10.1021/jm9005065
CHEMBL562036 203062 8 None - 0 Rat 6.3 pEC50 = 6.3 Binding
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 242 2 1 4 2.1 O=C(Nc1ccc2c(c1)OCO2)c1ccccn1 10.1021/jm9005065
1410 9054 48 None -3 6 Human 6.3 pEC50 = 6.3 Binding
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 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/s0960-894x(00)00247-x
1412 9054 48 None -3 6 Human 6.3 pEC50 = 6.3 Binding
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 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/s0960-894x(00)00247-x
179394 9054 48 None -3 6 Human 6.3 pEC50 = 6.3 Binding
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 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/s0960-894x(00)00247-x
57689795 9054 48 None -3 6 Human 6.3 pEC50 = 6.3 Binding
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 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/s0960-894x(00)00247-x
CHEMBL33567 9054 48 None -3 6 Human 6.3 pEC50 = 6.3 Binding
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 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/s0960-894x(00)00247-x
1410 9054 48 None -2 6 Rat 6.3 pEC50 = 6.3 Binding
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 9054 48 None -2 6 Rat 6.3 pEC50 = 6.3 Binding
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 9054 48 None -2 6 Rat 6.3 pEC50 = 6.3 Binding
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 9054 48 None -2 6 Rat 6.3 pEC50 = 6.3 Binding
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 9054 48 None -2 6 Rat 6.3 pEC50 = 6.3 Binding
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
14842361 175969 1 None - 0 Rat 6.3 pEC50 = 6.3 Binding
Effective concentration against Metabotropic glutamate receptor 4Effective concentration against Metabotropic glutamate receptor 4
ChEMBL 195 3 4 3 -1.0 NC1(C(=O)O)CC1CP(=O)(O)O 10.1016/s0960-894x(00)00197-9
CHEMBL440648 175969 1 None - 0 Rat 6.3 pEC50 = 6.3 Binding
Effective concentration against Metabotropic glutamate receptor 4Effective concentration against Metabotropic glutamate receptor 4
ChEMBL 195 3 4 3 -1.0 NC1(C(=O)O)CC1CP(=O)(O)O 10.1016/s0960-894x(00)00197-9
1310 9095 110 None -26 18 Rat 5.3 pEC50 = 5.3 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR4a in ratConcentration for half maximal activation of metabotropic glutamate mGluR4a in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
1369 9095 110 None -26 18 Rat 5.3 pEC50 = 5.3 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR4a in ratConcentration for half maximal activation of metabotropic glutamate mGluR4a in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
33032 9095 110 None -26 18 Rat 5.3 pEC50 = 5.3 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR4a in ratConcentration for half maximal activation of metabotropic glutamate mGluR4a in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
44272391 9095 110 None -26 18 Rat 5.3 pEC50 = 5.3 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR4a in ratConcentration for half maximal activation of metabotropic glutamate mGluR4a in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
88747398 9095 110 None -26 18 Rat 5.3 pEC50 = 5.3 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR4a in ratConcentration for half maximal activation of metabotropic glutamate mGluR4a in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
CHEMBL575060 9095 110 None -26 18 Rat 5.3 pEC50 = 5.3 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR4a in ratConcentration for half maximal activation of metabotropic glutamate mGluR4a in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
DB00142 9095 110 None -26 18 Rat 5.3 pEC50 = 5.3 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR4a in ratConcentration for half maximal activation of metabotropic glutamate mGluR4a in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
6604704 108177 35 None - 0 Human 4.3 pEC50 = 4.3 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 4Compound was tested for the inhibition of Metabotropic glutamate receptor 4
ChEMBL 173 2 3 3 -0.3 N[C@@]1(C(=O)O)CC[C@H](C(=O)O)C1 10.1021/jm970719q
CHEMBL29726 108177 35 None - 0 Human 4.3 pEC50 = 4.3 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 4Compound was tested for the inhibition of Metabotropic glutamate receptor 4
ChEMBL 173 2 3 3 -0.3 N[C@@]1(C(=O)O)CC[C@H](C(=O)O)C1 10.1021/jm970719q
134190027 176379 0 None - 0 Rat 6.3 pEC50 = 6.3 Binding
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 322 3 2 6 3.8 CC(C)(C)Cc1noc2cc(Nc3n[nH]c4nccnc34)ccc12 10.1021/acs.jmedchem.8b00994
CHEMBL4436346 176379 0 None - 0 Rat 6.3 pEC50 = 6.3 Binding
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 322 3 2 6 3.8 CC(C)(C)Cc1noc2cc(Nc3n[nH]c4nccnc34)ccc12 10.1021/acs.jmedchem.8b00994
134189978 177681 0 None - 0 Rat 6.3 pEC50 = 6.3 Binding
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 320 3 2 6 3.9 c1cnc2c(Nc3ccc4c(C5CCCC5)noc4c3)n[nH]c2n1 10.1021/acs.jmedchem.8b00994
CHEMBL4454698 177681 0 None - 0 Rat 6.3 pEC50 = 6.3 Binding
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 320 3 2 6 3.9 c1cnc2c(Nc3ccc4c(C5CCCC5)noc4c3)n[nH]c2n1 10.1021/acs.jmedchem.8b00994
46836872 7088 47 None - 1 Human 7.3 pEC50 = 7.3 Binding
Positive allosteric modulation of mGluR4 (unknown origin)Positive allosteric modulation of mGluR4 (unknown origin)
ChEMBL 272 3 2 6 2.7 Cc1ccnc(n1)Nc1sc(c(n1)c1c[nH]nc1)C 10.1016/j.bmcl.2022.129106
6238 7088 47 None - 1 Human 7.3 pEC50 = 7.3 Binding
Positive allosteric modulation of mGluR4 (unknown origin)Positive allosteric modulation of mGluR4 (unknown origin)
ChEMBL 272 3 2 6 2.7 Cc1ccnc(n1)Nc1sc(c(n1)c1c[nH]nc1)C 10.1016/j.bmcl.2022.129106
CHEMBL3609729 7088 47 None - 1 Human 7.3 pEC50 = 7.3 Binding
Positive allosteric modulation of mGluR4 (unknown origin)Positive allosteric modulation of mGluR4 (unknown origin)
ChEMBL 272 3 2 6 2.7 Cc1ccnc(n1)Nc1sc(c(n1)c1c[nH]nc1)C 10.1016/j.bmcl.2022.129106
134190227 177970 0 None - 0 Rat 7.3 pEC50 = 7.3 Binding
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 Cc1noc2c(F)cc(Nc3n[nH]c4cccnc34)cc12 10.1021/acs.jmedchem.8b00994
CHEMBL4459205 177970 0 None - 0 Rat 7.3 pEC50 = 7.3 Binding
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 Cc1noc2c(F)cc(Nc3n[nH]c4cccnc34)cc12 10.1021/acs.jmedchem.8b00994
46869952 65932 0 None - 0 Rat 6.3 pEC50 = 6.3 Binding
Positive allosteric modulator activity at rat mGlu4 receptor by thallium flux assayPositive allosteric modulator activity at rat mGlu4 receptor by thallium flux assay
ChEMBL 419 4 1 4 4.2 CC1(c2ccccc2)CC(=O)N(c2ccc(NC(=O)c3ccccn3)cc2Cl)C1=O 10.1021/jm200956q
CHEMBL1699345 65932 0 None - 0 Rat 6.3 pEC50 = 6.3 Binding
Positive allosteric modulator activity at rat mGlu4 receptor by thallium flux assayPositive allosteric modulator activity at rat mGlu4 receptor by thallium flux assay
ChEMBL 419 4 1 4 4.2 CC1(c2ccccc2)CC(=O)N(c2ccc(NC(=O)c3ccccn3)cc2Cl)C1=O 10.1021/jm200956q
134189992 180657 0 None - 0 Rat 6.3 pEC50 = 6.3 Binding
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 321 3 2 5 4.4 CC(C)(C)Cc1noc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
CHEMBL4539629 180657 0 None - 0 Rat 6.3 pEC50 = 6.3 Binding
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 321 3 2 5 4.4 CC(C)(C)Cc1noc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
162651908 187094 0 None - 0 Rat 6.3 pEC50 = 6.3 Binding
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 394 2 2 3 2.0 O=C1CCSC[C@@H](C(=O)Nc2cc(F)cc(I)c2)N1 10.1016/j.bmcl.2021.127838
CHEMBL4751096 187094 0 None - 0 Rat 6.3 pEC50 = 6.3 Binding
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 394 2 2 3 2.0 O=C1CCSC[C@@H](C(=O)Nc2cc(F)cc(I)c2)N1 10.1016/j.bmcl.2021.127838
16748099 126641 1 None - 0 Human 6.2 pEC50 = 6.2 Binding
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 195 3 4 3 -1.0 N[C@]1(C(=O)O)C[C@@H]1CP(=O)(O)O 10.1016/s0960-894x(00)00247-x
CHEMBL34880 126641 1 None - 0 Human 6.2 pEC50 = 6.2 Binding
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 195 3 4 3 -1.0 N[C@]1(C(=O)O)C[C@@H]1CP(=O)(O)O 10.1016/s0960-894x(00)00247-x
95986374 187284 1 None - 0 Rat 5.2 pEC50 = 5.2 Binding
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 328 2 2 3 2.0 O=C1CCSC[C@@H](C(=O)Nc2cccc(Br)c2)N1 10.1016/j.bmcl.2021.127838
CHEMBL4753300 187284 1 None - 0 Rat 5.2 pEC50 = 5.2 Binding
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 328 2 2 3 2.0 O=C1CCSC[C@@H](C(=O)Nc2cccc(Br)c2)N1 10.1016/j.bmcl.2021.127838
162645569 186482 0 None - 0 Rat 7.2 pEC50 = 7.2 Binding
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 362 2 2 3 2.7 O=C1CCSC[C@H](C(=O)Nc2cc(Cl)cc(Br)c2)N1 10.1016/j.bmcl.2021.127838
CHEMBL4743836 186482 0 None - 0 Rat 7.2 pEC50 = 7.2 Binding
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 362 2 2 3 2.7 O=C1CCSC[C@H](C(=O)Nc2cc(Cl)cc(Br)c2)N1 10.1016/j.bmcl.2021.127838
10135 10826 21 None - 0 Human 7.2 pEC50 = 7.2 Binding
Positive allosteric modulator activity at human mGlu4 in Chinese hamster CHO cells co-expressing Gqi5 assessed as increase in calcium flux preincubated for 2.5 mins followed by gluatamate addition and measured for 2 mins by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulator activity at human mGlu4 in Chinese hamster CHO cells co-expressing Gqi5 assessed as increase in calcium flux preincubated for 2.5 mins followed by gluatamate addition and measured for 2 mins by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 329 2 2 4 4.3 FC(c1nccc2c1ccc(c2)Nc1n[nH]c2c1cccn2)(F)F 10.1021/acsmedchemlett.8b00426
134191471 10826 21 None - 0 Human 7.2 pEC50 = 7.2 Binding
Positive allosteric modulator activity at human mGlu4 in Chinese hamster CHO cells co-expressing Gqi5 assessed as increase in calcium flux preincubated for 2.5 mins followed by gluatamate addition and measured for 2 mins by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulator activity at human mGlu4 in Chinese hamster CHO cells co-expressing Gqi5 assessed as increase in calcium flux preincubated for 2.5 mins followed by gluatamate addition and measured for 2 mins by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 329 2 2 4 4.3 FC(c1nccc2c1ccc(c2)Nc1n[nH]c2c1cccn2)(F)F 10.1021/acsmedchemlett.8b00426
CHEMBL4797139 10826 21 None - 0 Human 7.2 pEC50 = 7.2 Binding
Positive allosteric modulator activity at human mGlu4 in Chinese hamster CHO cells co-expressing Gqi5 assessed as increase in calcium flux preincubated for 2.5 mins followed by gluatamate addition and measured for 2 mins by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulator activity at human mGlu4 in Chinese hamster CHO cells co-expressing Gqi5 assessed as increase in calcium flux preincubated for 2.5 mins followed by gluatamate addition and measured for 2 mins by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 329 2 2 4 4.3 FC(c1nccc2c1ccc(c2)Nc1n[nH]c2c1cccn2)(F)F 10.1021/acsmedchemlett.8b00426
10135 10826 21 None - 0 Human 7.2 pEC50 = 7.2 Binding
Positive allosteric modulator activity at human mGlu4 in Chinese hamster CHO cells co-expressing Gqi5 assessed as increase in calcium flux preincubated for 2.5 mins followed by gluatamate addition and measured for 2 mins by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulator activity at human mGlu4 in Chinese hamster CHO cells co-expressing Gqi5 assessed as increase in calcium flux preincubated for 2.5 mins followed by gluatamate addition and measured for 2 mins by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 329 2 2 4 4.3 FC(c1nccc2c1ccc(c2)Nc1n[nH]c2c1cccn2)(F)F 10.1021/acsmedchemlett.8b00426
134191471 10826 21 None - 0 Human 7.2 pEC50 = 7.2 Binding
Positive allosteric modulator activity at human mGlu4 in Chinese hamster CHO cells co-expressing Gqi5 assessed as increase in calcium flux preincubated for 2.5 mins followed by gluatamate addition and measured for 2 mins by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulator activity at human mGlu4 in Chinese hamster CHO cells co-expressing Gqi5 assessed as increase in calcium flux preincubated for 2.5 mins followed by gluatamate addition and measured for 2 mins by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 329 2 2 4 4.3 FC(c1nccc2c1ccc(c2)Nc1n[nH]c2c1cccn2)(F)F 10.1021/acsmedchemlett.8b00426
CHEMBL4797139 10826 21 None - 0 Human 7.2 pEC50 = 7.2 Binding
Positive allosteric modulator activity at human mGlu4 in Chinese hamster CHO cells co-expressing Gqi5 assessed as increase in calcium flux preincubated for 2.5 mins followed by gluatamate addition and measured for 2 mins by Fluo-4 AM dye based calcium mobilization assayPositive allosteric modulator activity at human mGlu4 in Chinese hamster CHO cells co-expressing Gqi5 assessed as increase in calcium flux preincubated for 2.5 mins followed by gluatamate addition and measured for 2 mins by Fluo-4 AM dye based calcium mobilization assay
ChEMBL 329 2 2 4 4.3 FC(c1nccc2c1ccc(c2)Nc1n[nH]c2c1cccn2)(F)F 10.1021/acsmedchemlett.8b00426
56649125 75565 0 None - 0 Rat 6.2 pEC50 = 6.2 Binding
Positive allosteric modulator activity at rat mGlu4 receptor by thallium flux assayPositive allosteric modulator activity at rat mGlu4 receptor by thallium flux assay
ChEMBL 383 3 1 4 3.7 O=C(Nc1ccc(N2C(=O)[C@H]3CCCC[C@H]3C2=O)c(Cl)c1)c1ccccn1 10.1021/jm200956q
CHEMBL1921959 75565 0 None - 0 Rat 6.2 pEC50 = 6.2 Binding
Positive allosteric modulator activity at rat mGlu4 receptor by thallium flux assayPositive allosteric modulator activity at rat mGlu4 receptor by thallium flux assay
ChEMBL 383 3 1 4 3.7 O=C(Nc1ccc(N2C(=O)[C@H]3CCCC[C@H]3C2=O)c(Cl)c1)c1ccccn1 10.1021/jm200956q
134190176 177475 0 None - 0 Rat 7.2 pEC50 = 7.2 Binding
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 266 2 2 6 2.5 Cc1noc2ccc(Nc3n[nH]c4nccnc34)cc12 10.1021/acs.jmedchem.8b00994
CHEMBL4451827 177475 0 None - 0 Rat 7.2 pEC50 = 7.2 Binding
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 266 2 2 6 2.5 Cc1noc2ccc(Nc3n[nH]c4nccnc34)cc12 10.1021/acs.jmedchem.8b00994
162650303 190427 0 None - 0 Rat 6.2 pEC50 = 6.2 Binding
Positive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glutamate by CODA-RET assayPositive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glutamate by CODA-RET assay
ChEMBL 1064 22 6 12 8.6 COc1cc(NC(=O)c2ccccn2)ccc1NC(=O)c1ccc(NC(=O)COCC(=O)NCCNC(=O)COc2ccc(-c3cccc(COc4cc5c(c(C)c4C)C(=O)C(C4CCCC4)C5)c3)cc2C(=O)O)cc1Cl 10.1016/j.bmcl.2020.127212
CHEMBL4748549 190427 0 None - 0 Rat 6.2 pEC50 = 6.2 Binding
Positive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glutamate by CODA-RET assayPositive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glutamate by CODA-RET assay
ChEMBL 1064 22 6 12 8.6 COc1cc(NC(=O)c2ccccn2)ccc1NC(=O)c1ccc(NC(=O)COCC(=O)NCCNC(=O)COc2ccc(-c3cccc(COc4cc5c(c(C)c4C)C(=O)C(C4CCCC4)C5)c3)cc2C(=O)O)cc1Cl 10.1016/j.bmcl.2020.127212
CHEMBL4802664 190427 0 None - 0 Rat 6.2 pEC50 = 6.2 Binding
Positive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glutamate by CODA-RET assayPositive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glutamate by CODA-RET assay
ChEMBL 1064 22 6 12 8.6 COc1cc(NC(=O)c2ccccn2)ccc1NC(=O)c1ccc(NC(=O)COCC(=O)NCCNC(=O)COc2ccc(-c3cccc(COc4cc5c(c(C)c4C)C(=O)C(C4CCCC4)C5)c3)cc2C(=O)O)cc1Cl 10.1016/j.bmcl.2020.127212
45110131 66599 2 None - 0 Rat 7.2 pEC50 = 7.2 Binding
Positive allosteric modulator activity at rat mGlu4 receptor by thallium flux assayPositive allosteric modulator activity at rat mGlu4 receptor by thallium flux assay
ChEMBL 377 3 1 4 3.8 O=C(Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1)c1ccccn1 10.1021/jm200956q
CHEMBL1727966 66599 2 None - 0 Rat 7.2 pEC50 = 7.2 Binding
Positive allosteric modulator activity at rat mGlu4 receptor by thallium flux assayPositive allosteric modulator activity at rat mGlu4 receptor by thallium flux assay
ChEMBL 377 3 1 4 3.8 O=C(Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1)c1ccccn1 10.1021/jm200956q
134189963 176461 0 None - 0 Rat 6.2 pEC50 = 6.2 Binding
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 319 3 2 5 4.5 c1cnc2c(Nc3ccc4c(C5CCCC5)noc4c3)n[nH]c2c1 10.1021/acs.jmedchem.8b00994
CHEMBL4437680 176461 0 None - 0 Rat 6.2 pEC50 = 6.2 Binding
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 319 3 2 5 4.5 c1cnc2c(Nc3ccc4c(C5CCCC5)noc4c3)n[nH]c2c1 10.1021/acs.jmedchem.8b00994
46869949 66207 1 None - 0 Rat 6.2 pEC50 = 6.2 Binding
Positive allosteric modulator activity at rat mGlu4 receptor by thallium flux assayPositive allosteric modulator activity at rat mGlu4 receptor by thallium flux assay
ChEMBL 369 3 1 4 3.1 CC1(C)[C@H]2C(=O)N(c3ccc(NC(=O)c4ccccn4)cc3Cl)C(=O)[C@H]21 10.1021/jm200956q
CHEMBL1711049 66207 1 None - 0 Rat 6.2 pEC50 = 6.2 Binding
Positive allosteric modulator activity at rat mGlu4 receptor by thallium flux assayPositive allosteric modulator activity at rat mGlu4 receptor by thallium flux assay
ChEMBL 369 3 1 4 3.1 CC1(C)[C@H]2C(=O)N(c3ccc(NC(=O)c4ccccn4)cc3Cl)C(=O)[C@H]21 10.1021/jm200956q
1408 7053 31 None - 0 Human 5.2 pEC50 = 5.2 Binding
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 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O 10.1016/s0960-894x(00)00247-x
6604820 7053 31 None - 0 Human 5.2 pEC50 = 5.2 Binding
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 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O 10.1016/s0960-894x(00)00247-x
CHEMBL285043 7053 31 None - 0 Human 5.2 pEC50 = 5.2 Binding
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 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O 10.1016/s0960-894x(00)00247-x
CHEMBL288635 7053 31 None - 0 Human 5.2 pEC50 = 5.2 Binding
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 217 3 4 4 -1.0 OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O 10.1016/s0960-894x(00)00247-x
2442621 203090 16 None - 0 Rat 6.1 pEC50 = 6.1 Binding
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 COc1ccc(NC(=O)c2ccccn2)cc1Cl 10.1021/jm9005065
CHEMBL562232 203090 16 None - 0 Rat 6.1 pEC50 = 6.1 Binding
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 COc1ccc(NC(=O)c2ccccn2)cc1Cl 10.1021/jm9005065
162647048 186406 0 None - 0 Rat 7.1 pEC50 = 7.1 Binding
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 406 2 2 3 2.8 O=C1CCSC[C@H](C(=O)Nc2cc(Br)cc(Br)c2)N1 10.1016/j.bmcl.2021.127838
CHEMBL4742838 186406 0 None - 0 Rat 7.1 pEC50 = 7.1 Binding
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 406 2 2 3 2.8 O=C1CCSC[C@H](C(=O)Nc2cc(Br)cc(Br)c2)N1 10.1016/j.bmcl.2021.127838
125799 106912 7 None - 0 Human 5.1 pEC50 = 5.1 Binding
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 195 3 4 3 -1.0 N[C@]1(C(=O)O)C[C@H]1CP(=O)(O)O 10.1016/s0960-894x(00)00247-x
CHEMBL287703 106912 7 None - 0 Human 5.1 pEC50 = 5.1 Binding
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 195 3 4 3 -1.0 N[C@]1(C(=O)O)C[C@H]1CP(=O)(O)O 10.1016/s0960-894x(00)00247-x
44189740 201709 0 None - 0 Rat 7.1 pEC50 = 7.1 Binding
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 264 4 1 3 2.9 O=C(Nc1cccc(OC(F)F)c1)c1ccccn1 10.1021/jm9005065
CHEMBL541754 201709 0 None - 0 Rat 7.1 pEC50 = 7.1 Binding
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 264 4 1 3 2.9 O=C(Nc1cccc(OC(F)F)c1)c1ccccn1 10.1021/jm9005065
44189740 201709 0 None - 0 Rat 7.1 pEC50 = 7.1 Binding
Positive allosteric modulator activity at rat mGlu4 receptorPositive allosteric modulator activity at rat mGlu4 receptor
ChEMBL 264 4 1 3 2.9 O=C(Nc1cccc(OC(F)F)c1)c1ccccn1 10.1016/j.bmcl.2015.07.031
CHEMBL541754 201709 0 None - 0 Rat 7.1 pEC50 = 7.1 Binding
Positive allosteric modulator activity at rat mGlu4 receptorPositive allosteric modulator activity at rat mGlu4 receptor
ChEMBL 264 4 1 3 2.9 O=C(Nc1cccc(OC(F)F)c1)c1ccccn1 10.1016/j.bmcl.2015.07.031
122419077 179599 0 None - 0 Rat 7.1 pEC50 = 7.1 Binding
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 401 4 3 7 3.2 O=C(NC1CC(F)(F)C1)c1nsc2cc(Nc3n[nH]c4nccnc34)ccc12 10.1021/acs.jmedchem.8b00994
CHEMBL4514040 179599 0 None - 0 Rat 7.1 pEC50 = 7.1 Binding
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 401 4 3 7 3.2 O=C(NC1CC(F)(F)C1)c1nsc2cc(Nc3n[nH]c4nccnc34)ccc12 10.1021/acs.jmedchem.8b00994
122419159 182747 15 None - 0 Rat 7.1 pEC50 = 7.1 Binding
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 400 4 3 6 3.8 O=C(NC1CC(F)(F)C1)c1nsc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
CHEMBL4588443 182747 15 None - 0 Rat 7.1 pEC50 = 7.1 Binding
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 400 4 3 6 3.8 O=C(NC1CC(F)(F)C1)c1nsc2cc(Nc3n[nH]c4cccnc34)ccc12 10.1021/acs.jmedchem.8b00994
44282281 126896 1 None - 0 Human 4.1 pEC50 = 4.1 Binding
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 209 2 4 3 -0.5 N[C@@]1(C(=O)O)CC[C@H](P(=O)(O)O)C1 10.1016/s0960-894x(00)00247-x
CHEMBL35111 126896 1 None - 0 Human 4.1 pEC50 = 4.1 Binding
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 209 2 4 3 -0.5 N[C@@]1(C(=O)O)CC[C@H](P(=O)(O)O)C1 10.1016/s0960-894x(00)00247-x
162651551 186962 0 None - 0 Rat 5.1 pEC50 = 5.1 Binding
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 286 2 2 3 1.5 O=C1CCSC[C@@H](C(=O)Nc2cc(F)cc(F)c2)N1 10.1016/j.bmcl.2021.127838
CHEMBL4749281 186962 0 None - 0 Rat 5.1 pEC50 = 5.1 Binding
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 286 2 2 3 1.5 O=C1CCSC[C@@H](C(=O)Nc2cc(F)cc(F)c2)N1 10.1016/j.bmcl.2021.127838
46836713 72304 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Positive allosteric modulator activity at human mGlu4 receptorPositive allosteric modulator activity at human mGlu4 receptor
ChEMBL 284 2 2 6 2.6 c1cnc(Nc2nc3c(s2)CCCc2n[nH]cc2-3)nc1 10.1016/j.bmcl.2015.07.031
CHEMBL1830711 72304 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Positive allosteric modulator activity at human mGlu4 receptorPositive allosteric modulator activity at human mGlu4 receptor
ChEMBL 284 2 2 6 2.6 c1cnc(Nc2nc3c(s2)CCCc2n[nH]cc2-3)nc1 10.1016/j.bmcl.2015.07.031
46836872 7088 47 None - 1 Rat 8.1 pEC50 = 8.1 Binding
Positive allosteric modulator activity at rat mGlu4 receptorPositive allosteric modulator activity at rat mGlu4 receptor
ChEMBL 272 3 2 6 2.7 Cc1ccnc(n1)Nc1sc(c(n1)c1c[nH]nc1)C 10.1016/j.bmcl.2015.07.031
6238 7088 47 None - 1 Rat 8.1 pEC50 = 8.1 Binding
Positive allosteric modulator activity at rat mGlu4 receptorPositive allosteric modulator activity at rat mGlu4 receptor
ChEMBL 272 3 2 6 2.7 Cc1ccnc(n1)Nc1sc(c(n1)c1c[nH]nc1)C 10.1016/j.bmcl.2015.07.031
CHEMBL3609729 7088 47 None - 1 Rat 8.1 pEC50 = 8.1 Binding
Positive allosteric modulator activity at rat mGlu4 receptorPositive allosteric modulator activity at rat mGlu4 receptor
ChEMBL 272 3 2 6 2.7 Cc1ccnc(n1)Nc1sc(c(n1)c1c[nH]nc1)C 10.1016/j.bmcl.2015.07.031
6604819 115929 2 None - 0 Human 5.1 pEC50 = 5.1 Binding
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 217 3 4 4 -1.0 NC1(C(=O)O)C[C@@H](C(=O)O)[C@H](C(=O)O)C1 10.1016/s0960-894x(00)00247-x
CHEMBL32142 115929 2 None - 0 Human 5.1 pEC50 = 5.1 Binding
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 217 3 4 4 -1.0 NC1(C(=O)O)C[C@@H](C(=O)O)[C@H](C(=O)O)C1 10.1016/s0960-894x(00)00247-x
1410 9054 48 None -2 6 Rat 6.0 pEC50 = 6.0 Binding
Effect on Metabotropic glutamate receptor 4Effect on Metabotropic glutamate receptor 4
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm9703597
1412 9054 48 None -2 6 Rat 6.0 pEC50 = 6.0 Binding
Effect on Metabotropic glutamate receptor 4Effect on Metabotropic glutamate receptor 4
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm9703597
179394 9054 48 None -2 6 Rat 6.0 pEC50 = 6.0 Binding
Effect on Metabotropic glutamate receptor 4Effect on Metabotropic glutamate receptor 4
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm9703597
57689795 9054 48 None -2 6 Rat 6.0 pEC50 = 6.0 Binding
Effect on Metabotropic glutamate receptor 4Effect on Metabotropic glutamate receptor 4
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm9703597
CHEMBL33567 9054 48 None -2 6 Rat 6.0 pEC50 = 6.0 Binding
Effect on Metabotropic glutamate receptor 4Effect on Metabotropic glutamate receptor 4
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm9703597
92044496 162746 0 None - 0 Rat 5.0 pEC50 = 5.0 Binding
Agonist activity at mGlu4 in Wistar rat striatum assessed as decrease in corticostriatal glutamatergic excitatory post-synaptic potential by whole cell patch clamp assayAgonist activity at mGlu4 in Wistar rat striatum assessed as decrease in corticostriatal glutamatergic excitatory post-synaptic potential by whole cell patch clamp assay
ChEMBL 324 7 4 7 0.7 N[C@@H](CCP(=O)(O)C(O)c1csc([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
CHEMBL4061423 162746 0 None - 0 Rat 5.0 pEC50 = 5.0 Binding
Agonist activity at mGlu4 in Wistar rat striatum assessed as decrease in corticostriatal glutamatergic excitatory post-synaptic potential by whole cell patch clamp assayAgonist activity at mGlu4 in Wistar rat striatum assessed as decrease in corticostriatal glutamatergic excitatory post-synaptic potential by whole cell patch clamp assay
ChEMBL 324 7 4 7 0.7 N[C@@H](CCP(=O)(O)C(O)c1csc([N+](=O)[O-])c1)C(=O)O 10.1021/acs.jmedchem.7b01438
134190172 179977 0 None - 0 Rat 7.0 pEC50 = 7.0 Binding
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 265 2 2 5 3.2 Cc1noc2ccc(Nc3n[nH]c4cccnc34)cc12 10.1021/acs.jmedchem.8b00994
CHEMBL4522695 179977 0 None - 0 Rat 7.0 pEC50 = 7.0 Binding
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 265 2 2 5 3.2 Cc1noc2ccc(Nc3n[nH]c4cccnc34)cc12 10.1021/acs.jmedchem.8b00994
162654935 187372 0 None - 0 Rat 6.0 pEC50 = 6.0 Binding
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 386 2 2 3 3.3 O=C1CCSC[C@@H](C(=O)Nc2cc(C(F)(F)F)cc(C(F)(F)F)c2)N1 10.1016/j.bmcl.2021.127838
CHEMBL4754364 187372 0 None - 0 Rat 6.0 pEC50 = 6.0 Binding
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 386 2 2 3 3.3 O=C1CCSC[C@@H](C(=O)Nc2cc(C(F)(F)F)cc(C(F)(F)F)c2)N1 10.1016/j.bmcl.2021.127838
1310 9095 110 None -4 18 Human 5.0 pEC50 = 5.0 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 4Compound was tested for the inhibition of Metabotropic glutamate receptor 4
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm970719q
1369 9095 110 None -4 18 Human 5.0 pEC50 = 5.0 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 4Compound was tested for the inhibition of Metabotropic glutamate receptor 4
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm970719q
33032 9095 110 None -4 18 Human 5.0 pEC50 = 5.0 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 4Compound was tested for the inhibition of Metabotropic glutamate receptor 4
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm970719q
44272391 9095 110 None -4 18 Human 5.0 pEC50 = 5.0 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 4Compound was tested for the inhibition of Metabotropic glutamate receptor 4
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm970719q
88747398 9095 110 None -4 18 Human 5.0 pEC50 = 5.0 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 4Compound was tested for the inhibition of Metabotropic glutamate receptor 4
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm970719q
CHEMBL575060 9095 110 None -4 18 Human 5.0 pEC50 = 5.0 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 4Compound was tested for the inhibition of Metabotropic glutamate receptor 4
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm970719q
DB00142 9095 110 None -4 18 Human 5.0 pEC50 = 5.0 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 4Compound was tested for the inhibition of Metabotropic glutamate receptor 4
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm970719q
44189740 201709 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Displacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 264 4 1 3 2.9 O=C(Nc1cccc(OC(F)F)c1)c1ccccn1 10.1021/jm501245b
CHEMBL541754 201709 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Displacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 264 4 1 3 2.9 O=C(Nc1cccc(OC(F)F)c1)c1ccccn1 10.1021/jm501245b
2445811 129855 7 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 223 2 1 3 2.2 N#Cc1cccc(NC(=O)c2ccccn2)c1 10.1016/j.bmcl.2015.07.031
CHEMBL3609736 129855 7 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 223 2 1 3 2.2 N#Cc1cccc(NC(=O)c2ccccn2)c1 10.1016/j.bmcl.2015.07.031
2445811 129855 7 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 223 2 1 3 2.2 N#Cc1cccc(NC(=O)c2ccccn2)c1 10.1016/j.bmcl.2015.07.031
CHEMBL3609736 129855 7 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 223 2 1 3 2.2 N#Cc1cccc(NC(=O)c2ccccn2)c1 10.1016/j.bmcl.2015.07.031
45110136 122920 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
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 391 3 1 4 4.1 Cc1cccc2c1C(=O)N(c1ccc(NC(=O)c3ccccn3)cc1Cl)C2=O 10.1021/jm501245b
CHEMBL3357575 122920 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
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 391 3 1 4 4.1 Cc1cccc2c1C(=O)N(c1ccc(NC(=O)c3ccccn3)cc1Cl)C2=O 10.1021/jm501245b
118722304 122921 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 455 3 1 4 4.6 O=C(Nc1ccc(N2C(=O)c3cccc(Br)c3C2=O)c(Cl)c1)c1ccccn1 10.1021/jm501245b
CHEMBL3357576 122921 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 455 3 1 4 4.6 O=C(Nc1ccc(N2C(=O)c3cccc(Br)c3C2=O)c(Cl)c1)c1ccccn1 10.1021/jm501245b
118722304 122921 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 455 3 1 4 4.6 O=C(Nc1ccc(N2C(=O)c3cccc(Br)c3C2=O)c(Cl)c1)c1ccccn1 10.1021/jm501245b
CHEMBL3357576 122921 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 455 3 1 4 4.6 O=C(Nc1ccc(N2C(=O)c3cccc(Br)c3C2=O)c(Cl)c1)c1ccccn1 10.1021/jm501245b
45110506 122923 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
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 122923 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
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
3956 10807 87 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 262 3 1 3 3.0 COc1cc(ccc1Cl)NC(=O)c1ccccn1 10.1021/jm501245b
44191096 10807 87 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 262 3 1 3 3.0 COc1cc(ccc1Cl)NC(=O)c1ccccn1 10.1021/jm501245b
CHEMBL562551 10807 87 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 262 3 1 3 3.0 COc1cc(ccc1Cl)NC(=O)c1ccccn1 10.1021/jm501245b
3956 10807 87 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 262 3 1 3 3.0 COc1cc(ccc1Cl)NC(=O)c1ccccn1 10.1021/jm501245b
44191096 10807 87 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 262 3 1 3 3.0 COc1cc(ccc1Cl)NC(=O)c1ccccn1 10.1021/jm501245b
CHEMBL562551 10807 87 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 262 3 1 3 3.0 COc1cc(ccc1Cl)NC(=O)c1ccccn1 10.1021/jm501245b
22565221 129852 3 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 228 3 1 3 2.3 COc1cccc(NC(=O)c2ccccn2)c1 10.1016/j.bmcl.2015.07.031
CHEMBL3609733 129852 3 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 228 3 1 3 2.3 COc1cccc(NC(=O)c2ccccn2)c1 10.1016/j.bmcl.2015.07.031
22565221 129852 3 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 228 3 1 3 2.3 COc1cccc(NC(=O)c2ccccn2)c1 10.1016/j.bmcl.2015.07.031
CHEMBL3609733 129852 3 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 228 3 1 3 2.3 COc1cccc(NC(=O)c2ccccn2)c1 10.1016/j.bmcl.2015.07.031
122187791 129851 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 354 3 1 3 2.9 COc1cc(NC(=O)c2ccccn2)ccc1I 10.1016/j.bmcl.2015.07.031
CHEMBL3609732 129851 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 354 3 1 3 2.9 COc1cc(NC(=O)c2ccccn2)ccc1I 10.1016/j.bmcl.2015.07.031
122187791 129851 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 354 3 1 3 2.9 COc1cc(NC(=O)c2ccccn2)ccc1I 10.1016/j.bmcl.2015.07.031
CHEMBL3609732 129851 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 354 3 1 3 2.9 COc1cc(NC(=O)c2ccccn2)ccc1I 10.1016/j.bmcl.2015.07.031
122187793 129859 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 349 2 1 3 2.8 N#Cc1cc(NC(=O)c2ccccn2)ccc1I 10.1016/j.bmcl.2015.07.031
CHEMBL3609740 129859 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 349 2 1 3 2.8 N#Cc1cc(NC(=O)c2ccccn2)ccc1I 10.1016/j.bmcl.2015.07.031
122187793 129859 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 349 2 1 3 2.8 N#Cc1cc(NC(=O)c2ccccn2)ccc1I 10.1016/j.bmcl.2015.07.031
CHEMBL3609740 129859 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 349 2 1 3 2.8 N#Cc1cc(NC(=O)c2ccccn2)ccc1I 10.1016/j.bmcl.2015.07.031
1397 9307 15 None - 5 Rat 5.8 pIC50 = 5.8 Binding
Concentration required to inhibit metabotropic glutamate receptor 4 activity of rat expressed in CHO cellsConcentration required to inhibit metabotropic glutamate receptor 4 activity of rat expressed in CHO cells
ChEMBL 377 5 3 4 2.1 OC(=O)[C@]1(N)[C@H](OCc2ccc(c(c2)Cl)Cl)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O 10.1021/jm0400294
9886034 9307 15 None - 5 Rat 5.8 pIC50 = 5.8 Binding
Concentration required to inhibit metabotropic glutamate receptor 4 activity of rat expressed in CHO cellsConcentration required to inhibit metabotropic glutamate receptor 4 activity of rat expressed in CHO cells
ChEMBL 377 5 3 4 2.1 OC(=O)[C@]1(N)[C@H](OCc2ccc(c(c2)Cl)Cl)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O 10.1021/jm0400294
CHEMBL186453 9307 15 None - 5 Rat 5.8 pIC50 = 5.8 Binding
Concentration required to inhibit metabotropic glutamate receptor 4 activity of rat expressed in CHO cellsConcentration required to inhibit metabotropic glutamate receptor 4 activity of rat expressed in CHO cells
ChEMBL 377 5 3 4 2.1 OC(=O)[C@]1(N)[C@H](OCc2ccc(c(c2)Cl)Cl)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O 10.1021/jm0400294
118722305 122922 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 503 3 1 4 4.4 O=C(Nc1ccc(N2C(=O)c3cccc(I)c3C2=O)c(Cl)c1)c1ccccn1 10.1021/jm501245b
CHEMBL3357577 122922 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 503 3 1 4 4.4 O=C(Nc1ccc(N2C(=O)c3cccc(I)c3C2=O)c(Cl)c1)c1ccccn1 10.1021/jm501245b
1378 9195 54 None - 10 Rat 5.6 pIC50 = 5.6 Binding
Concentration required to inhibit metabotropic glutamate receptor 4 activity of rat expressed in CHO cellsConcentration required to inhibit metabotropic glutamate receptor 4 activity of rat expressed in CHO cells
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/jm0400294
1399 9195 54 None - 10 Rat 5.6 pIC50 = 5.6 Binding
Concentration required to inhibit metabotropic glutamate receptor 4 activity of rat expressed in CHO cellsConcentration required to inhibit metabotropic glutamate receptor 4 activity of rat expressed in CHO cells
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/jm0400294
9819927 9195 54 None - 10 Rat 5.6 pIC50 = 5.6 Binding
Concentration required to inhibit metabotropic glutamate receptor 4 activity of rat expressed in CHO cellsConcentration required to inhibit metabotropic glutamate receptor 4 activity of rat expressed in CHO cells
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/jm0400294
CHEMBL432038 9195 54 None - 10 Rat 5.6 pIC50 = 5.6 Binding
Concentration required to inhibit metabotropic glutamate receptor 4 activity of rat expressed in CHO cellsConcentration required to inhibit metabotropic glutamate receptor 4 activity of rat expressed in CHO cells
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/jm0400294
118722305 122922 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 503 3 1 4 4.4 O=C(Nc1ccc(N2C(=O)c3cccc(I)c3C2=O)c(Cl)c1)c1ccccn1 10.1021/jm501245b
CHEMBL3357577 122922 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 503 3 1 4 4.4 O=C(Nc1ccc(N2C(=O)c3cccc(I)c3C2=O)c(Cl)c1)c1ccccn1 10.1021/jm501245b
122187794 129860 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 280 4 1 3 3.3 O=C(Nc1ccc(Cl)c(OCF)c1)c1ccccn1 10.1016/j.bmcl.2015.07.031
CHEMBL3609741 129860 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 280 4 1 3 3.3 O=C(Nc1ccc(Cl)c(OCF)c1)c1ccccn1 10.1016/j.bmcl.2015.07.031
CHEMBL3609742 129860 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 280 4 1 3 3.3 O=C(Nc1ccc(Cl)c(OCF)c1)c1ccccn1 10.1016/j.bmcl.2015.07.031
122187794 129860 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 280 4 1 3 3.3 O=C(Nc1ccc(Cl)c(OCF)c1)c1ccccn1 10.1016/j.bmcl.2015.07.031
CHEMBL3609741 129860 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 280 4 1 3 3.3 O=C(Nc1ccc(Cl)c(OCF)c1)c1ccccn1 10.1016/j.bmcl.2015.07.031
CHEMBL3609742 129860 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 280 4 1 3 3.3 O=C(Nc1ccc(Cl)c(OCF)c1)c1ccccn1 10.1016/j.bmcl.2015.07.031
122187920 129869 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 246 4 1 3 2.6 O=C(Nc1cccc(OCF)c1)c1ccccn1 10.1016/j.bmcl.2015.07.031
CHEMBL3609743 129869 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 246 4 1 3 2.6 O=C(Nc1cccc(OCF)c1)c1ccccn1 10.1016/j.bmcl.2015.07.031
CHEMBL3609900 129869 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 246 4 1 3 2.6 O=C(Nc1cccc(OCF)c1)c1ccccn1 10.1016/j.bmcl.2015.07.031
122187920 129869 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 246 4 1 3 2.6 O=C(Nc1cccc(OCF)c1)c1ccccn1 10.1016/j.bmcl.2015.07.031
CHEMBL3609743 129869 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 246 4 1 3 2.6 O=C(Nc1cccc(OCF)c1)c1ccccn1 10.1016/j.bmcl.2015.07.031
CHEMBL3609900 129869 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 246 4 1 3 2.6 O=C(Nc1cccc(OCF)c1)c1ccccn1 10.1016/j.bmcl.2015.07.031
42644786 202110 2 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 246 3 1 3 2.5 COc1cc(NC(=O)c2ccccn2)ccc1F 10.1016/j.bmcl.2015.07.031
CHEMBL551635 202110 2 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 246 3 1 3 2.5 COc1cc(NC(=O)c2ccccn2)ccc1F 10.1016/j.bmcl.2015.07.031
42644786 202110 2 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 246 3 1 3 2.5 COc1cc(NC(=O)c2ccccn2)ccc1F 10.1016/j.bmcl.2015.07.031
CHEMBL551635 202110 2 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 246 3 1 3 2.5 COc1cc(NC(=O)c2ccccn2)ccc1F 10.1016/j.bmcl.2015.07.031
122187790 129850 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 306 3 1 3 3.1 COc1cc(NC(=O)c2ccccn2)ccc1Br 10.1016/j.bmcl.2015.07.031
CHEMBL3609731 129850 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 306 3 1 3 3.1 COc1cc(NC(=O)c2ccccn2)ccc1Br 10.1016/j.bmcl.2015.07.031
122187790 129850 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 306 3 1 3 3.1 COc1cc(NC(=O)c2ccccn2)ccc1Br 10.1016/j.bmcl.2015.07.031
CHEMBL3609731 129850 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 306 3 1 3 3.1 COc1cc(NC(=O)c2ccccn2)ccc1Br 10.1016/j.bmcl.2015.07.031
45110133 122919 1 None - 0 Human 7.4 pIC50 = 7.4 Binding
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 395 3 1 4 3.9 O=C(Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1)c1ccccn1 10.1021/jm501245b
CHEMBL3357574 122919 1 None - 0 Human 7.4 pIC50 = 7.4 Binding
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 395 3 1 4 3.9 O=C(Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1)c1ccccn1 10.1021/jm501245b
45110136 122920 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 391 3 1 4 4.1 Cc1cccc2c1C(=O)N(c1ccc(NC(=O)c3ccccn3)cc1Cl)C2=O 10.1021/jm501245b
CHEMBL3357575 122920 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 391 3 1 4 4.1 Cc1cccc2c1C(=O)N(c1ccc(NC(=O)c3ccccn3)cc1Cl)C2=O 10.1021/jm501245b
45110136 122920 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 391 3 1 4 4.1 Cc1cccc2c1C(=O)N(c1ccc(NC(=O)c3ccccn3)cc1Cl)C2=O 10.1021/jm501245b
CHEMBL3357575 122920 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 391 3 1 4 4.1 Cc1cccc2c1C(=O)N(c1ccc(NC(=O)c3ccccn3)cc1Cl)C2=O 10.1021/jm501245b
44189740 201709 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 264 4 1 3 2.9 O=C(Nc1cccc(OC(F)F)c1)c1ccccn1 10.1016/j.bmcl.2015.07.031
CHEMBL541754 201709 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 264 4 1 3 2.9 O=C(Nc1cccc(OC(F)F)c1)c1ccccn1 10.1016/j.bmcl.2015.07.031
44189740 201709 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 264 4 1 3 2.9 O=C(Nc1cccc(OC(F)F)c1)c1ccccn1 10.1016/j.bmcl.2015.07.031
CHEMBL541754 201709 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 264 4 1 3 2.9 O=C(Nc1cccc(OC(F)F)c1)c1ccccn1 10.1016/j.bmcl.2015.07.031
2441036 26412 6 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 244 3 1 3 3.1 CSc1cccc(NC(=O)c2ccccn2)c1 10.1016/j.bmcl.2015.07.031
CHEMBL1300476 26412 6 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 244 3 1 3 3.1 CSc1cccc(NC(=O)c2ccccn2)c1 10.1016/j.bmcl.2015.07.031
2441036 26412 6 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 244 3 1 3 3.1 CSc1cccc(NC(=O)c2ccccn2)c1 10.1016/j.bmcl.2015.07.031
CHEMBL1300476 26412 6 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 244 3 1 3 3.1 CSc1cccc(NC(=O)c2ccccn2)c1 10.1016/j.bmcl.2015.07.031
122187792 129858 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 301 2 1 3 3.0 N#Cc1cc(NC(=O)c2ccccn2)ccc1Br 10.1016/j.bmcl.2015.07.031
CHEMBL3609739 129858 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 301 2 1 3 3.0 N#Cc1cc(NC(=O)c2ccccn2)ccc1Br 10.1016/j.bmcl.2015.07.031
122187792 129858 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 301 2 1 3 3.0 N#Cc1cc(NC(=O)c2ccccn2)ccc1Br 10.1016/j.bmcl.2015.07.031
CHEMBL3609739 129858 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 301 2 1 3 3.0 N#Cc1cc(NC(=O)c2ccccn2)ccc1Br 10.1016/j.bmcl.2015.07.031
45110133 122919 1 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 395 3 1 4 3.9 O=C(Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1)c1ccccn1 10.1021/jm501245b
CHEMBL3357574 122919 1 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 395 3 1 4 3.9 O=C(Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1)c1ccccn1 10.1021/jm501245b
3956 10807 87 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 262 3 1 3 3.0 COc1cc(ccc1Cl)NC(=O)c1ccccn1 10.1016/j.bmcl.2015.07.031
44191096 10807 87 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 262 3 1 3 3.0 COc1cc(ccc1Cl)NC(=O)c1ccccn1 10.1016/j.bmcl.2015.07.031
CHEMBL562551 10807 87 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 262 3 1 3 3.0 COc1cc(ccc1Cl)NC(=O)c1ccccn1 10.1016/j.bmcl.2015.07.031
45110133 122919 1 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 395 3 1 4 3.9 O=C(Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1)c1ccccn1 10.1021/jm501245b
CHEMBL3357574 122919 1 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 395 3 1 4 3.9 O=C(Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1)c1ccccn1 10.1021/jm501245b
3956 10807 87 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 262 3 1 3 3.0 COc1cc(ccc1Cl)NC(=O)c1ccccn1 10.1016/j.bmcl.2015.07.031
44191096 10807 87 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 262 3 1 3 3.0 COc1cc(ccc1Cl)NC(=O)c1ccccn1 10.1016/j.bmcl.2015.07.031
CHEMBL562551 10807 87 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 262 3 1 3 3.0 COc1cc(ccc1Cl)NC(=O)c1ccccn1 10.1016/j.bmcl.2015.07.031
47131350 129857 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 257 2 1 3 2.9 N#Cc1cc(NC(=O)c2ccccn2)ccc1Cl 10.1016/j.bmcl.2015.07.031
CHEMBL3609738 129857 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 257 2 1 3 2.9 N#Cc1cc(NC(=O)c2ccccn2)ccc1Cl 10.1016/j.bmcl.2015.07.031
47131350 129857 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 257 2 1 3 2.9 N#Cc1cc(NC(=O)c2ccccn2)ccc1Cl 10.1016/j.bmcl.2015.07.031
CHEMBL3609738 129857 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 257 2 1 3 2.9 N#Cc1cc(NC(=O)c2ccccn2)ccc1Cl 10.1016/j.bmcl.2015.07.031
115497227 129853 1 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 282 4 1 3 3.1 O=C(Nc1cccc(OC(F)F)c1)c1cccc(F)n1 10.1016/j.bmcl.2015.07.031
CHEMBL3609734 129853 1 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 282 4 1 3 3.1 O=C(Nc1cccc(OC(F)F)c1)c1cccc(F)n1 10.1016/j.bmcl.2015.07.031
115497227 129853 1 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 282 4 1 3 3.1 O=C(Nc1cccc(OC(F)F)c1)c1cccc(F)n1 10.1016/j.bmcl.2015.07.031
CHEMBL3609734 129853 1 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 282 4 1 3 3.1 O=C(Nc1cccc(OC(F)F)c1)c1cccc(F)n1 10.1016/j.bmcl.2015.07.031
113943306 129744 2 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 280 3 1 3 3.1 COc1cc(NC(=O)c2cccc(F)n2)ccc1Cl 10.1016/j.bmcl.2015.07.031
CHEMBL3608323 129744 2 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 280 3 1 3 3.1 COc1cc(NC(=O)c2cccc(F)n2)ccc1Cl 10.1016/j.bmcl.2015.07.031
62316492 129856 2 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 241 2 1 3 2.3 N#Cc1cc(NC(=O)c2ccccn2)ccc1F 10.1016/j.bmcl.2015.07.031
CHEMBL3609737 129856 2 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 241 2 1 3 2.3 N#Cc1cc(NC(=O)c2ccccn2)ccc1F 10.1016/j.bmcl.2015.07.031
113943306 129744 2 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 280 3 1 3 3.1 COc1cc(NC(=O)c2cccc(F)n2)ccc1Cl 10.1016/j.bmcl.2015.07.031
CHEMBL3608323 129744 2 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 280 3 1 3 3.1 COc1cc(NC(=O)c2cccc(F)n2)ccc1Cl 10.1016/j.bmcl.2015.07.031
62316492 129856 2 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 241 2 1 3 2.3 N#Cc1cc(NC(=O)c2ccccn2)ccc1F 10.1016/j.bmcl.2015.07.031
CHEMBL3609737 129856 2 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 241 2 1 3 2.3 N#Cc1cc(NC(=O)c2ccccn2)ccc1F 10.1016/j.bmcl.2015.07.031
46898088 9145 6 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]-L-AP4 from human mGlu4 receptorDisplacement of [3H]-L-AP4 from human mGlu4 receptor
ChEMBL 364 8 5 8 0.4 COc1cc(cc(c1O)[N+](=O)[O-])C(P(=O)(CC[C@@H](C(=O)O)N)O)O 10.1021/ml400338f
6739 9145 6 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]-L-AP4 from human mGlu4 receptorDisplacement of [3H]-L-AP4 from human mGlu4 receptor
ChEMBL 364 8 5 8 0.4 COc1cc(cc(c1O)[N+](=O)[O-])C(P(=O)(CC[C@@H](C(=O)O)N)O)O 10.1021/ml400338f
CHEMBL3114672 9145 6 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]-L-AP4 from human mGlu4 receptorDisplacement of [3H]-L-AP4 from human mGlu4 receptor
ChEMBL 364 8 5 8 0.4 COc1cc(cc(c1O)[N+](=O)[O-])C(P(=O)(CC[C@@H](C(=O)O)N)O)O 10.1021/ml400338f
42644790 129854 1 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 264 3 1 3 2.6 COc1cc(NC(=O)c2cccc(F)n2)ccc1F 10.1016/j.bmcl.2015.07.031
CHEMBL3609735 129854 1 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 264 3 1 3 2.6 COc1cc(NC(=O)c2cccc(F)n2)ccc1F 10.1016/j.bmcl.2015.07.031
42644790 129854 1 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 264 3 1 3 2.6 COc1cc(NC(=O)c2cccc(F)n2)ccc1F 10.1016/j.bmcl.2015.07.031
CHEMBL3609735 129854 1 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodDisplacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
ChEMBL 264 3 1 3 2.6 COc1cc(NC(=O)c2cccc(F)n2)ccc1F 10.1016/j.bmcl.2015.07.031
44189740 201709 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Displacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 264 4 1 3 2.9 O=C(Nc1cccc(OC(F)F)c1)c1ccccn1 10.1021/jm501245b
CHEMBL541754 201709 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Displacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis
ChEMBL 264 4 1 3 2.9 O=C(Nc1cccc(OC(F)F)c1)c1ccccn1 10.1021/jm501245b
1310 9095 110 None -4 18 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]Quisqualate from human mGluR4 receptor expressed in BHK cellsDisplacement of [3H]Quisqualate from human mGluR4 receptor expressed in BHK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2008.11.015
1369 9095 110 None -4 18 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]Quisqualate from human mGluR4 receptor expressed in BHK cellsDisplacement of [3H]Quisqualate from human mGluR4 receptor expressed in BHK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2008.11.015
33032 9095 110 None -4 18 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]Quisqualate from human mGluR4 receptor expressed in BHK cellsDisplacement of [3H]Quisqualate from human mGluR4 receptor expressed in BHK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2008.11.015
44272391 9095 110 None -4 18 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]Quisqualate from human mGluR4 receptor expressed in BHK cellsDisplacement of [3H]Quisqualate from human mGluR4 receptor expressed in BHK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2008.11.015
88747398 9095 110 None -4 18 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]Quisqualate from human mGluR4 receptor expressed in BHK cellsDisplacement of [3H]Quisqualate from human mGluR4 receptor expressed in BHK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2008.11.015
CHEMBL575060 9095 110 None -4 18 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]Quisqualate from human mGluR4 receptor expressed in BHK cellsDisplacement of [3H]Quisqualate from human mGluR4 receptor expressed in BHK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2008.11.015
DB00142 9095 110 None -4 18 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]Quisqualate from human mGluR4 receptor expressed in BHK cellsDisplacement of [3H]Quisqualate from human mGluR4 receptor expressed in BHK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2008.11.015
1410 9054 48 None -2 6 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]L-AP4 from rat mGluR4 expressed in BHK cellsDisplacement of [3H]L-AP4 from rat mGluR4 expressed in BHK cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmcl.2005.09.014
1412 9054 48 None -2 6 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]L-AP4 from rat mGluR4 expressed in BHK cellsDisplacement of [3H]L-AP4 from rat mGluR4 expressed in BHK cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmcl.2005.09.014
179394 9054 48 None -2 6 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]L-AP4 from rat mGluR4 expressed in BHK cellsDisplacement of [3H]L-AP4 from rat mGluR4 expressed in BHK cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmcl.2005.09.014
57689795 9054 48 None -2 6 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]L-AP4 from rat mGluR4 expressed in BHK cellsDisplacement of [3H]L-AP4 from rat mGluR4 expressed in BHK cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmcl.2005.09.014
CHEMBL33567 9054 48 None -2 6 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]L-AP4 from rat mGluR4 expressed in BHK cellsDisplacement of [3H]L-AP4 from rat mGluR4 expressed in BHK cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmcl.2005.09.014
1410 9054 48 None -2 6 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]L-AP4 from rat recombinant mGluR4 expressed in BHK cells by SPA assayDisplacement of [3H]L-AP4 from rat recombinant mGluR4 expressed in BHK cells by SPA assay
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmc.2007.02.040
1412 9054 48 None -2 6 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]L-AP4 from rat recombinant mGluR4 expressed in BHK cells by SPA assayDisplacement of [3H]L-AP4 from rat recombinant mGluR4 expressed in BHK cells by SPA assay
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmc.2007.02.040
179394 9054 48 None -2 6 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]L-AP4 from rat recombinant mGluR4 expressed in BHK cells by SPA assayDisplacement of [3H]L-AP4 from rat recombinant mGluR4 expressed in BHK cells by SPA assay
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmc.2007.02.040
57689795 9054 48 None -2 6 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]L-AP4 from rat recombinant mGluR4 expressed in BHK cells by SPA assayDisplacement of [3H]L-AP4 from rat recombinant mGluR4 expressed in BHK cells by SPA assay
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmc.2007.02.040
CHEMBL33567 9054 48 None -2 6 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]L-AP4 from rat recombinant mGluR4 expressed in BHK cells by SPA assayDisplacement of [3H]L-AP4 from rat recombinant mGluR4 expressed in BHK cells by SPA assay
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmc.2007.02.040
1410 9054 48 None -3 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]Quisqualate from human mGluR4 receptor expressed in BHK cellsDisplacement of [3H]Quisqualate from human mGluR4 receptor expressed in BHK cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmc.2008.11.015
1412 9054 48 None -3 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]Quisqualate from human mGluR4 receptor expressed in BHK cellsDisplacement of [3H]Quisqualate from human mGluR4 receptor expressed in BHK cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmc.2008.11.015
179394 9054 48 None -3 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]Quisqualate from human mGluR4 receptor expressed in BHK cellsDisplacement of [3H]Quisqualate from human mGluR4 receptor expressed in BHK cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmc.2008.11.015
57689795 9054 48 None -3 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]Quisqualate from human mGluR4 receptor expressed in BHK cellsDisplacement of [3H]Quisqualate from human mGluR4 receptor expressed in BHK cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmc.2008.11.015
CHEMBL33567 9054 48 None -3 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]Quisqualate from human mGluR4 receptor expressed in BHK cellsDisplacement of [3H]Quisqualate from human mGluR4 receptor expressed in BHK cells
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1016/j.bmc.2008.11.015
1310 9095 110 None -4 18 Human 5.8 pKi = 5.8 Binding
Binding affinity at Metabotropic glutamate receptor 4Binding affinity at Metabotropic glutamate receptor 4
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm010323l
1369 9095 110 None -4 18 Human 5.8 pKi = 5.8 Binding
Binding affinity at Metabotropic glutamate receptor 4Binding affinity at Metabotropic glutamate receptor 4
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm010323l
33032 9095 110 None -4 18 Human 5.8 pKi = 5.8 Binding
Binding affinity at Metabotropic glutamate receptor 4Binding affinity at Metabotropic glutamate receptor 4
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm010323l
44272391 9095 110 None -4 18 Human 5.8 pKi = 5.8 Binding
Binding affinity at Metabotropic glutamate receptor 4Binding affinity at Metabotropic glutamate receptor 4
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm010323l
88747398 9095 110 None -4 18 Human 5.8 pKi = 5.8 Binding
Binding affinity at Metabotropic glutamate receptor 4Binding affinity at Metabotropic glutamate receptor 4
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm010323l
CHEMBL575060 9095 110 None -4 18 Human 5.8 pKi = 5.8 Binding
Binding affinity at Metabotropic glutamate receptor 4Binding affinity at Metabotropic glutamate receptor 4
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm010323l
DB00142 9095 110 None -4 18 Human 5.8 pKi = 5.8 Binding
Binding affinity at Metabotropic glutamate receptor 4Binding affinity at Metabotropic glutamate receptor 4
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm010323l
1310 9095 110 None -4 18 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LAP4 from mGluR4 receptor expressed in BHK cellsDisplacement of [3H]LAP4 from mGluR4 receptor expressed in BHK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm070322e
1369 9095 110 None -4 18 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LAP4 from mGluR4 receptor expressed in BHK cellsDisplacement of [3H]LAP4 from mGluR4 receptor expressed in BHK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm070322e
33032 9095 110 None -4 18 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LAP4 from mGluR4 receptor expressed in BHK cellsDisplacement of [3H]LAP4 from mGluR4 receptor expressed in BHK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm070322e
44272391 9095 110 None -4 18 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LAP4 from mGluR4 receptor expressed in BHK cellsDisplacement of [3H]LAP4 from mGluR4 receptor expressed in BHK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm070322e
88747398 9095 110 None -4 18 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LAP4 from mGluR4 receptor expressed in BHK cellsDisplacement of [3H]LAP4 from mGluR4 receptor expressed in BHK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm070322e
CHEMBL575060 9095 110 None -4 18 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LAP4 from mGluR4 receptor expressed in BHK cellsDisplacement of [3H]LAP4 from mGluR4 receptor expressed in BHK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm070322e
DB00142 9095 110 None -4 18 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LAP4 from mGluR4 receptor expressed in BHK cellsDisplacement of [3H]LAP4 from mGluR4 receptor expressed in BHK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm070322e
16739372 153508 0 None - 1 Rat 4.6 pKi = 4.6 Binding
Displacement of [3H]L-AP4 from rat recombinant mGluR4 expressed in BHK cells by SPA assayDisplacement of [3H]L-AP4 from rat recombinant mGluR4 expressed in BHK cells by SPA assay
ChEMBL 271 4 4 3 0.4 NC(C(=O)O)[C@@H]1[C@@H](P(=O)(O)O)[C@H]1c1ccccc1 10.1016/j.bmc.2007.02.040
CHEMBL392420 153508 0 None - 1 Rat 4.6 pKi = 4.6 Binding
Displacement of [3H]L-AP4 from rat recombinant mGluR4 expressed in BHK cells by SPA assayDisplacement of [3H]L-AP4 from rat recombinant mGluR4 expressed in BHK cells by SPA assay
ChEMBL 271 4 4 3 0.4 NC(C(=O)O)[C@@H]1[C@@H](P(=O)(O)O)[C@H]1c1ccccc1 10.1016/j.bmc.2007.02.040
1310 9095 110 None -4 18 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-L-AP4 from human mGluR4 receptor expressed in HEK cellsDisplacement of [3H]-L-AP4 from human mGluR4 receptor expressed in HEK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1039/C1MD00186H
1369 9095 110 None -4 18 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-L-AP4 from human mGluR4 receptor expressed in HEK cellsDisplacement of [3H]-L-AP4 from human mGluR4 receptor expressed in HEK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1039/C1MD00186H
33032 9095 110 None -4 18 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-L-AP4 from human mGluR4 receptor expressed in HEK cellsDisplacement of [3H]-L-AP4 from human mGluR4 receptor expressed in HEK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1039/C1MD00186H
44272391 9095 110 None -4 18 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-L-AP4 from human mGluR4 receptor expressed in HEK cellsDisplacement of [3H]-L-AP4 from human mGluR4 receptor expressed in HEK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1039/C1MD00186H
88747398 9095 110 None -4 18 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-L-AP4 from human mGluR4 receptor expressed in HEK cellsDisplacement of [3H]-L-AP4 from human mGluR4 receptor expressed in HEK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1039/C1MD00186H
CHEMBL575060 9095 110 None -4 18 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-L-AP4 from human mGluR4 receptor expressed in HEK cellsDisplacement of [3H]-L-AP4 from human mGluR4 receptor expressed in HEK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1039/C1MD00186H
DB00142 9095 110 None -4 18 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-L-AP4 from human mGluR4 receptor expressed in HEK cellsDisplacement of [3H]-L-AP4 from human mGluR4 receptor expressed in HEK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1039/C1MD00186H
1310 9095 110 None -26 18 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]L-AP4 from rat mGluR4 expressed in BHK cellsDisplacement of [3H]L-AP4 from rat mGluR4 expressed in BHK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2005.09.014
1369 9095 110 None -26 18 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]L-AP4 from rat mGluR4 expressed in BHK cellsDisplacement of [3H]L-AP4 from rat mGluR4 expressed in BHK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2005.09.014
33032 9095 110 None -26 18 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]L-AP4 from rat mGluR4 expressed in BHK cellsDisplacement of [3H]L-AP4 from rat mGluR4 expressed in BHK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2005.09.014
44272391 9095 110 None -26 18 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]L-AP4 from rat mGluR4 expressed in BHK cellsDisplacement of [3H]L-AP4 from rat mGluR4 expressed in BHK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2005.09.014
88747398 9095 110 None -26 18 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]L-AP4 from rat mGluR4 expressed in BHK cellsDisplacement of [3H]L-AP4 from rat mGluR4 expressed in BHK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2005.09.014
CHEMBL575060 9095 110 None -26 18 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]L-AP4 from rat mGluR4 expressed in BHK cellsDisplacement of [3H]L-AP4 from rat mGluR4 expressed in BHK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2005.09.014
DB00142 9095 110 None -26 18 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]L-AP4 from rat mGluR4 expressed in BHK cellsDisplacement of [3H]L-AP4 from rat mGluR4 expressed in BHK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2005.09.014
1310 9095 110 None -26 18 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]L-AP4 from rat recombinant mGluR4 expressed in BHK cells by SPA assayDisplacement of [3H]L-AP4 from rat recombinant mGluR4 expressed in BHK cells by SPA assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2007.02.040
1369 9095 110 None -26 18 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]L-AP4 from rat recombinant mGluR4 expressed in BHK cells by SPA assayDisplacement of [3H]L-AP4 from rat recombinant mGluR4 expressed in BHK cells by SPA assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2007.02.040
33032 9095 110 None -26 18 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]L-AP4 from rat recombinant mGluR4 expressed in BHK cells by SPA assayDisplacement of [3H]L-AP4 from rat recombinant mGluR4 expressed in BHK cells by SPA assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2007.02.040
44272391 9095 110 None -26 18 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]L-AP4 from rat recombinant mGluR4 expressed in BHK cells by SPA assayDisplacement of [3H]L-AP4 from rat recombinant mGluR4 expressed in BHK cells by SPA assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2007.02.040
88747398 9095 110 None -26 18 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]L-AP4 from rat recombinant mGluR4 expressed in BHK cells by SPA assayDisplacement of [3H]L-AP4 from rat recombinant mGluR4 expressed in BHK cells by SPA assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2007.02.040
CHEMBL575060 9095 110 None -26 18 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]L-AP4 from rat recombinant mGluR4 expressed in BHK cells by SPA assayDisplacement of [3H]L-AP4 from rat recombinant mGluR4 expressed in BHK cells by SPA assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2007.02.040
DB00142 9095 110 None -26 18 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]L-AP4 from rat recombinant mGluR4 expressed in BHK cells by SPA assayDisplacement of [3H]L-AP4 from rat recombinant mGluR4 expressed in BHK cells by SPA assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2007.02.040
1410 9054 48 None -3 6 Human 6.3 pKi = 6.3 Binding
Binding affinity at Metabotropic glutamate receptor 4Binding affinity at Metabotropic glutamate receptor 4
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm010323l
1412 9054 48 None -3 6 Human 6.3 pKi = 6.3 Binding
Binding affinity at Metabotropic glutamate receptor 4Binding affinity at Metabotropic glutamate receptor 4
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm010323l
179394 9054 48 None -3 6 Human 6.3 pKi = 6.3 Binding
Binding affinity at Metabotropic glutamate receptor 4Binding affinity at Metabotropic glutamate receptor 4
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm010323l
57689795 9054 48 None -3 6 Human 6.3 pKi = 6.3 Binding
Binding affinity at Metabotropic glutamate receptor 4Binding affinity at Metabotropic glutamate receptor 4
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm010323l
CHEMBL33567 9054 48 None -3 6 Human 6.3 pKi = 6.3 Binding
Binding affinity at Metabotropic glutamate receptor 4Binding affinity at Metabotropic glutamate receptor 4
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm010323l
3335 9789 4 None - 1 Human 4.3 pKi = 4.3 Binding
Binding affinity towards metabotropic glutamate receptor mGluR4aBinding affinity towards metabotropic glutamate receptor mGluR4a
ChEMBL 235 4 3 3 0.5 OC(=O)[C@H]([C@H]1[C@H]([C@@H]1C(=O)O)c1ccccc1)N 10.1021/jm960059+
5311344 9789 4 None - 1 Human 4.3 pKi = 4.3 Binding
Binding affinity towards metabotropic glutamate receptor mGluR4aBinding affinity towards metabotropic glutamate receptor mGluR4a
ChEMBL 235 4 3 3 0.5 OC(=O)[C@H]([C@H]1[C@H]([C@@H]1C(=O)O)c1ccccc1)N 10.1021/jm960059+
CHEMBL39573 9789 4 None - 1 Human 4.3 pKi = 4.3 Binding
Binding affinity towards metabotropic glutamate receptor mGluR4aBinding affinity towards metabotropic glutamate receptor mGluR4a
ChEMBL 235 4 3 3 0.5 OC(=O)[C@H]([C@H]1[C@H]([C@@H]1C(=O)O)c1ccccc1)N 10.1021/jm960059+
44406221 79451 1 None 1 2 Rat 4.3 pKi = 4.3 Binding
Displacement of [3H]L-AP4 from rat mGluR4 expressed in BHK cellsDisplacement of [3H]L-AP4 from rat mGluR4 expressed in BHK cells
ChEMBL 195 3 4 3 -1.0 N[C@H](C(=O)O)[C@@H]1C[C@H]1P(=O)(O)O 10.1016/j.bmcl.2005.09.014
CHEMBL199626 79451 1 None 1 2 Rat 4.3 pKi = 4.3 Binding
Displacement of [3H]L-AP4 from rat mGluR4 expressed in BHK cellsDisplacement of [3H]L-AP4 from rat mGluR4 expressed in BHK cells
ChEMBL 195 3 4 3 -1.0 N[C@H](C(=O)O)[C@@H]1C[C@H]1P(=O)(O)O 10.1016/j.bmcl.2005.09.014
177491 92864 42 None 1 3 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]LAP4 from mGluR4 receptor expressed in BHK cellsDisplacement of [3H]LAP4 from mGluR4 receptor expressed in BHK cells
ChEMBL 183 4 3 4 -1.3 N[C@@H](CCS(=O)(=O)O)C(=O)O 10.1021/jm070322e
CHEMBL230951 92864 42 None 1 3 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]LAP4 from mGluR4 receptor expressed in BHK cellsDisplacement of [3H]LAP4 from mGluR4 receptor expressed in BHK cells
ChEMBL 183 4 3 4 -1.3 N[C@@H](CCS(=O)(=O)O)C(=O)O 10.1021/jm070322e
44406220 78948 1 None 8 2 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]L-AP4 from rat mGluR4 expressed in BHK cellsDisplacement of [3H]L-AP4 from rat mGluR4 expressed in BHK cells
ChEMBL 195 3 4 3 -1.0 N[C@H](C(=O)O)[C@H]1C[C@@H]1P(=O)(O)O 10.1016/j.bmcl.2005.09.014
CHEMBL197976 78948 1 None 8 2 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]L-AP4 from rat mGluR4 expressed in BHK cellsDisplacement of [3H]L-AP4 from rat mGluR4 expressed in BHK cells
ChEMBL 195 3 4 3 -1.0 N[C@H](C(=O)O)[C@H]1C[C@@H]1P(=O)(O)O 10.1016/j.bmcl.2005.09.014
11708219 176151 0 None 8 2 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]L-AP4 from rat recombinant mGluR4 expressed in BHK cells by SPA assayDisplacement of [3H]L-AP4 from rat recombinant mGluR4 expressed in BHK cells by SPA assay
ChEMBL 195 3 4 3 -1.0 NC(C(=O)O)[C@H]1C[C@@H]1P(=O)(O)O 10.1016/j.bmc.2007.02.040
CHEMBL442076 176151 0 None 8 2 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]L-AP4 from rat recombinant mGluR4 expressed in BHK cells by SPA assayDisplacement of [3H]L-AP4 from rat recombinant mGluR4 expressed in BHK cells by SPA assay
ChEMBL 195 3 4 3 -1.0 NC(C(=O)O)[C@H]1C[C@@H]1P(=O)(O)O 10.1016/j.bmc.2007.02.040
1410 9054 48 None -2 6 Rat 6.3 pKd None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10187777
1412 9054 48 None -2 6 Rat 6.3 pKd None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10187777
179394 9054 48 None -2 6 Rat 6.3 pKd None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10187777
57689795 9054 48 None -2 6 Rat 6.3 pKd None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10187777
CHEMBL33567 9054 48 None -2 6 Rat 6.3 pKd None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10187777
12310764 8751 64 Functional -14 8 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 158 2 3 4 -0.9 OC(=O)C(c1o[nH]c(=O)c1)N None
1233 8751 64 Functional -14 8 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 158 2 3 4 -0.9 OC(=O)C(c1o[nH]c(=O)c1)N None
1371 8751 64 Functional -14 8 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 158 2 3 4 -0.9 OC(=O)C(c1o[nH]c(=O)c1)N None
CHEMBL284895 8751 64 Functional -14 8 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 158 2 3 4 -0.9 OC(=O)C(c1o[nH]c(=O)c1)N None
1310 9095 110 Functional -26 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
1369 9095 110 Functional -26 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
33032 9095 110 Functional -26 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
44272391 9095 110 Functional -26 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
88747398 9095 110 Functional -26 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
CHEMBL575060 9095 110 Functional -26 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
DB00142 9095 110 Functional -26 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
134 9292 24 Functional -8511 67 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 9292 24 Functional -8511 67 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 9292 24 Functional -8511 67 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 9292 24 Functional -8511 67 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 9292 24 Functional -8511 67 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
15897 9637 0 Functional -354 36 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 9637 0 Functional -354 36 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 9637 0 Functional -354 36 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
128563 10237 33 Functional -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
1666 10237 33 Functional -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
CHEMBL445332 10237 33 Functional -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
DB12327 10237 33 Functional -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
10297 33885 30 Functional -38 43 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
CHEMBL136560 33885 30 Functional -38 43 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
5115 118824 47 Functional -1 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 195 3 3 3 0.5 NC(C(=O)O)c1ccc(C(=O)O)cc1 None
5115 118824 47 3H-GLUTAMATE -1 5 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 195 3 3 3 0.5 NC(C(=O)O)c1ccc(C(=O)O)cc1 None
CHEMBL328984 118824 47 Functional -1 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 195 3 3 3 0.5 NC(C(=O)O)c1ccc(C(=O)O)cc1 None
CHEMBL328984 118824 47 3H-GLUTAMATE -1 5 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 195 3 3 3 0.5 NC(C(=O)O)c1ccc(C(=O)O)cc1 None
446220 140299 14 Functional -1778 45 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
CHEMBL370805 140299 14 Functional -1778 45 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
1615 174570 24 Functional -26 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
CHEMBL43048 174570 24 Functional -26 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
1297 177031 36 Functional 1 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 4 4 0.2 NC(C(=O)O)c1ccc(C(=O)O)c(O)c1 None
CHEMBL444589 177031 36 Functional 1 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 4 4 0.2 NC(C(=O)O)c1ccc(C(=O)O)c(O)c1 None
162265 209053 22 Functional -239 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
4786 209053 22 Functional -239 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
CHEMBL61006 209053 22 Functional -239 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
3337 213146 27 Functional -1513 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 213146 27 Functional -1513 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 213146 27 Functional -1513 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 213146 27 Functional -1513 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 213146 27 Functional -1513 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
11954224 222732 0 Functional -141253 59 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
None 222951 0 Functional -2 7 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 173 2 3 3 -0.3 C1CC(CC1C(=O)O)(C(=O)O)N None
25137849 222958 0 Functional -4 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
71290 222958 0 Functional -4 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
None 223095 0 Functional -1 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 3 3 3 -1.4 C(C(C(=O)O)N)S(=O)O None
None 223096 0 Functional -1 39 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 3 3 4 -1.7 C(C(C(=O)O)N)S(=O)(=O)O None
None 223104 0 Functional -13 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 2 1 2 1.2 CC(C(=O)C1=CC=CC=C1)N None
1576 223105 0 Functional -16 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 163 3 1 2 1.5 CC(C(=O)C1=CC=CC=C1)NC None
None 223142 0 Functional -1 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 245 3 3 4 0.2 CC(C1=CC=C(C=C1)S(=O)(=O)O)(C(=O)O)N None
None 223144 0 Functional -1 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 197 4 4 3 -0.6 CC(CCP(=O)(O)O)(C(=O)O)N None
None 223117 0 Functional -1 4 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 185 4 4 4 -1.5 C(C(C(=O)O)N)OP(=O)(O)O None
2207 106641 63 Functional -1 7 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 183 4 4 3 -1.0 NC(CCP(=O)(O)O)C(=O)O None
CHEMBL285843 106641 63 Functional -1 7 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 183 4 4 3 -1.0 NC(CCP(=O)(O)O)C(=O)O None
2207 106641 63 Functional -1 7 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 183 4 4 3 -1.0 NC(CCP(=O)(O)O)C(=O)O None
CHEMBL285843 106641 63 Functional -1 7 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 183 4 4 3 -1.0 NC(CCP(=O)(O)O)C(=O)O None
1310 9095 110 None -4 18 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Quisqualate from human mGluR4 receptor expressed in BHK cellsDisplacement of [3H]Quisqualate from human mGluR4 receptor expressed in BHK cells
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
1369 9095 110 None -4 18 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Quisqualate from human mGluR4 receptor expressed in BHK cellsDisplacement of [3H]Quisqualate from human mGluR4 receptor expressed in BHK cells
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
33032 9095 110 None -4 18 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Quisqualate from human mGluR4 receptor expressed in BHK cellsDisplacement of [3H]Quisqualate from human mGluR4 receptor expressed in BHK cells
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
44272391 9095 110 None -4 18 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Quisqualate from human mGluR4 receptor expressed in BHK cellsDisplacement of [3H]Quisqualate from human mGluR4 receptor expressed in BHK cells
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
88747398 9095 110 None -4 18 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Quisqualate from human mGluR4 receptor expressed in BHK cellsDisplacement of [3H]Quisqualate from human mGluR4 receptor expressed in BHK cells
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
CHEMBL575060 9095 110 None -4 18 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Quisqualate from human mGluR4 receptor expressed in BHK cellsDisplacement of [3H]Quisqualate from human mGluR4 receptor expressed in BHK cells
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
DB00142 9095 110 None -4 18 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Quisqualate from human mGluR4 receptor expressed in BHK cellsDisplacement of [3H]Quisqualate from human mGluR4 receptor expressed in BHK cells
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
1414 9237 0 None 6 2 Rat 4.6 pKi = 4.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 197 4 4 3 -0.6 OC(=O)[C@](CCP(=O)(O)O)(N)C 10187777
1795545 9237 0 None 6 2 Rat 4.6 pKi = 4.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 197 4 4 3 -0.6 OC(=O)[C@](CCP(=O)(O)O)(N)C 10187777
CHEMBL1488784 9237 0 None 6 2 Rat 4.6 pKi = 4.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 197 4 4 3 -0.6 OC(=O)[C@](CCP(=O)(O)O)(N)C 10187777
46836872 7088 47 None - 1 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 272 3 2 6 2.7 Cc1ccnc(n1)Nc1sc(c(n1)c1c[nH]nc1)C 22787118
6238 7088 47 None - 1 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 272 3 2 6 2.7 Cc1ccnc(n1)Nc1sc(c(n1)c1c[nH]nc1)C 22787118
CHEMBL3609729 7088 47 None - 1 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 272 3 2 6 2.7 Cc1ccnc(n1)Nc1sc(c(n1)c1c[nH]nc1)C 22787118
1415 9392 41 None -5 3 Rat 4.2 pKi None 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 245 3 4 3 -0.3 OC(=O)C(c1ccc(cc1)P(=O)(O)O)(N)C 10187777
3972752 9392 41 None -5 3 Rat 4.2 pKi None 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 245 3 4 3 -0.3 OC(=O)C(c1ccc(cc1)P(=O)(O)O)(N)C 10187777
CHEMBL86508 9392 41 None -5 3 Rat 4.2 pKi None 4.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 245 3 4 3 -0.3 OC(=O)C(c1ccc(cc1)P(=O)(O)O)(N)C 10187777
1413 7979 0 None -83 2 Rat 4.6 pKi None 4.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 271 4 4 3 0.1 OC(=O)C(c1ccc(cc1)P(=O)(O)O)(C1CC1)N 10187777
2878 7979 0 None -83 2 Rat 4.6 pKi None 4.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 271 4 4 3 0.1 OC(=O)C(c1ccc(cc1)P(=O)(O)O)(C1CC1)N 10187777
CHEMBL164642 7979 0 None -83 2 Rat 4.6 pKi None 4.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 271 4 4 3 0.1 OC(=O)C(c1ccc(cc1)P(=O)(O)O)(C1CC1)N 10187777
1310 9095 110 None -26 18 Rat 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10187777
1310 9095 110 None -26 18 Rat 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 1361913
1310 9095 110 None -26 18 Rat 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9144638
1310 9095 110 None -26 18 Rat 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9357538
1369 9095 110 None -26 18 Rat 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10187777
1369 9095 110 None -26 18 Rat 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 1361913
1369 9095 110 None -26 18 Rat 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9144638
1369 9095 110 None -26 18 Rat 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9357538
33032 9095 110 None -26 18 Rat 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10187777
33032 9095 110 None -26 18 Rat 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 1361913
33032 9095 110 None -26 18 Rat 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9144638
33032 9095 110 None -26 18 Rat 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9357538
44272391 9095 110 None -26 18 Rat 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10187777
44272391 9095 110 None -26 18 Rat 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 1361913
44272391 9095 110 None -26 18 Rat 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9144638
44272391 9095 110 None -26 18 Rat 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9357538
88747398 9095 110 None -26 18 Rat 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10187777
88747398 9095 110 None -26 18 Rat 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 1361913
88747398 9095 110 None -26 18 Rat 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9144638
88747398 9095 110 None -26 18 Rat 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9357538
CHEMBL575060 9095 110 None -26 18 Rat 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10187777
CHEMBL575060 9095 110 None -26 18 Rat 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 1361913
CHEMBL575060 9095 110 None -26 18 Rat 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9144638
CHEMBL575060 9095 110 None -26 18 Rat 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9357538
DB00142 9095 110 None -26 18 Rat 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10187777
DB00142 9095 110 None -26 18 Rat 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 1361913
DB00142 9095 110 None -26 18 Rat 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9144638
DB00142 9095 110 None -26 18 Rat 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9357538