Ligand source activities (1 row/activity)





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44361401 38115 0 None -2 5 Rat 8.0 pEC50 = 8 Functional
Metabotropic glutamate receptor 8 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 8 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 175 3 4 4 -1.9 N[C@H](C(=O)O)[C@H]1[C@@H](O)[C@@H]1C(=O)O 10.1021/jm030967o
CHEMBL140197 38115 0 None -2 5 Rat 8.0 pEC50 = 8 Functional
Metabotropic glutamate receptor 8 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 8 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 175 3 4 4 -1.9 N[C@H](C(=O)O)[C@H]1[C@@H](O)[C@@H]1C(=O)O 10.1021/jm030967o
58058372 162976 0 None -3 3 Human 6.0 pEC50 = 6 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 6.0 pEC50 = 6 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
1408 7053 31 None -1 7 Rat 5.0 pEC50 = 5 Functional
Activity at rat mGluR8 receptor measured as intracellular calcium concentration in HEK293 cellsActivity at rat mGluR8 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 5.0 pEC50 = 5 Functional
Activity at rat mGluR8 receptor measured as intracellular calcium concentration in HEK293 cellsActivity at rat mGluR8 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 5.0 pEC50 = 5 Functional
Activity at rat mGluR8 receptor measured as intracellular calcium concentration in HEK293 cellsActivity at rat mGluR8 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 5.0 pEC50 = 5 Functional
Activity at rat mGluR8 receptor measured as intracellular calcium concentration in HEK293 cellsActivity at rat mGluR8 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
53240406 130174 17 None -457 4 Human 5.0 pEC50 = 5 Functional
Agonist activity at human recombinant mGlu8 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assayAgonist activity at human recombinant mGlu8 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 284 4 4 6 -0.6 N[C@@]1(C(=O)O)C[C@@H](Sc2nnc[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
CHEMBL3616847 130174 17 None -457 4 Human 5.0 pEC50 = 5 Functional
Agonist activity at human recombinant mGlu8 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assayAgonist activity at human recombinant mGlu8 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assay
ChEMBL 284 4 4 6 -0.6 N[C@@]1(C(=O)O)C[C@@H](Sc2nnc[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/acs.jmedchem.5b01124
122197938 167718 0 None -128 3 Rat 5.0 pEC50 = 5.0 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 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 -128 3 Rat 5.0 pEC50 = 5.0 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 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
1410 9054 48 None 1 8 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat mGluR8 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR8 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 7.0 pEC50 = 7.0 Functional
Agonist activity at rat mGluR8 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR8 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 7.0 pEC50 = 7.0 Functional
Agonist activity at rat mGluR8 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR8 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 7.0 pEC50 = 7.0 Functional
Agonist activity at rat mGluR8 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR8 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 7.0 pEC50 = 7.0 Functional
Agonist activity at rat mGluR8 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR8 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
1393 8321 64 None -1047 6 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human mGluR8 assessed as effect on cAMP production in RGT cellsAgonist activity at human mGluR8 assessed as effect on cAMP production in RGT cells
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm060917u
1396 8321 64 None -1047 6 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human mGluR8 assessed as effect on cAMP production in RGT cellsAgonist activity at human mGluR8 assessed as effect on cAMP production in RGT cells
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm060917u
213056 8321 64 None -1047 6 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human mGluR8 assessed as effect on cAMP production in RGT cellsAgonist activity at human mGluR8 assessed as effect on cAMP production in RGT cells
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm060917u
CHEMBL8759 8321 64 None -1047 6 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human mGluR8 assessed as effect on cAMP production in RGT cellsAgonist activity at human mGluR8 assessed as effect on cAMP production in RGT cells
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm060917u
1393 8321 64 None -1047 6 Human 4.9 pEC50 = 4.9 Functional
Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR8Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR8
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm980616n
1396 8321 64 None -1047 6 Human 4.9 pEC50 = 4.9 Functional
Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR8Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR8
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm980616n
213056 8321 64 None -1047 6 Human 4.9 pEC50 = 4.9 Functional
Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR8Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR8
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm980616n
CHEMBL8759 8321 64 None -1047 6 Human 4.9 pEC50 = 4.9 Functional
Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR8Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR8
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm980616n
122197955 167373 0 None -10 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 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 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 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
46918013 165508 0 None -2 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 5.9 pEC50 = 5.9 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
46836872 7088 47 None -138 4 Rat 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux 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 -138 4 Rat 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux 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 -138 4 Rat 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux 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
122197956 167250 0 None -5 3 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 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 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 363 9 5 6 0.9 N[C@H](CCP(=O)(O)C(O)c1ccc(SCC(=O)O)cc1)C(=O)O nan
10239 10815 29 None -1 5 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat mGlu8 receptor expressed in HEK cell co-expressing Galpha15 (unknown origin) assessed as reduction in intracellular Ca2+ mobilization by Fluo-4-AM dye based fluorescence assayAgonist activity at rat mGlu8 receptor expressed in HEK cell co-expressing Galpha15 (unknown origin) assessed as reduction in intracellular Ca2+ mobilization 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 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat mGlu8 receptor expressed in HEK cell co-expressing Galpha15 (unknown origin) assessed as reduction in intracellular Ca2+ mobilization by Fluo-4-AM dye based fluorescence assayAgonist activity at rat mGlu8 receptor expressed in HEK cell co-expressing Galpha15 (unknown origin) assessed as reduction in intracellular Ca2+ mobilization 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 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat mGlu8 receptor expressed in HEK cell co-expressing Galpha15 (unknown origin) assessed as reduction in intracellular Ca2+ mobilization by Fluo-4-AM dye based fluorescence assayAgonist activity at rat mGlu8 receptor expressed in HEK cell co-expressing Galpha15 (unknown origin) assessed as reduction in intracellular Ca2+ mobilization 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 Rat 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux 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 Rat 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux 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 Rat 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux 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
137640190 163733 0 None -1 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 5.9 pEC50 = 5.9 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
57519364 125898 0 None -2 3 Rat 5.9 pEC50 = 5.9 Functional
Agonist activity at rat mGluR8 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR8 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 5.9 pEC50 = 5.9 Functional
Agonist activity at rat mGluR8 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR8 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
1410 9054 48 None 1 8 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity at rat mGluR8 receptor expressed HEK293 cells assessed as effect on inositol phosphate productionAgonist activity at rat mGluR8 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 6.9 pEC50 = 6.9 Functional
Agonist activity at rat mGluR8 receptor expressed HEK293 cells assessed as effect on inositol phosphate productionAgonist activity at rat mGluR8 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 6.9 pEC50 = 6.9 Functional
Agonist activity at rat mGluR8 receptor expressed HEK293 cells assessed as effect on inositol phosphate productionAgonist activity at rat mGluR8 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 6.9 pEC50 = 6.9 Functional
Agonist activity at rat mGluR8 receptor expressed HEK293 cells assessed as effect on inositol phosphate productionAgonist activity at rat mGluR8 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 6.9 pEC50 = 6.9 Functional
Agonist activity at rat mGluR8 receptor expressed HEK293 cells assessed as effect on inositol phosphate productionAgonist activity at rat mGluR8 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
57765613 165269 0 None -1 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 5.9 pEC50 = 5.9 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
137642874 164813 0 None -4 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 5.9 pEC50 = 5.9 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
10176324 121605 1 None -165 4 Rat 5.9 pEC50 = 5.9 Functional
Metabotropic glutamate receptor 8 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 8 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 173 3 3 3 -0.6 C[C@H]1[C@H](C(=O)O)[C@H]1[C@H](N)C(=O)O 10.1021/jm030967o
CHEMBL334160 121605 1 None -165 4 Rat 5.9 pEC50 = 5.9 Functional
Metabotropic glutamate receptor 8 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 8 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 173 3 3 3 -0.6 C[C@H]1[C@H](C(=O)O)[C@H]1[C@H](N)C(=O)O 10.1021/jm030967o
137631983 163325 0 None -1 2 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 4.9 pEC50 = 4.9 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
1310 9095 110 None -2187 17 Rat 4.9 pEC50 = 4.9 Functional
Agonist activity at rat mGlu8 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu8 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 -2187 17 Rat 4.9 pEC50 = 4.9 Functional
Agonist activity at rat mGlu8 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu8 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 -2187 17 Rat 4.9 pEC50 = 4.9 Functional
Agonist activity at rat mGlu8 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu8 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 -2187 17 Rat 4.9 pEC50 = 4.9 Functional
Agonist activity at rat mGlu8 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu8 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 -2187 17 Rat 4.9 pEC50 = 4.9 Functional
Agonist activity at rat mGlu8 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu8 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 -2187 17 Rat 4.9 pEC50 = 4.9 Functional
Agonist activity at rat mGlu8 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu8 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 -2187 17 Rat 4.9 pEC50 = 4.9 Functional
Agonist activity at rat mGlu8 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu8 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
122197948 167229 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 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 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 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
122197959 167163 0 None -15 2 Rat 4.8 pEC50 = 4.8 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 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 4.8 pEC50 = 4.8 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 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
46918013 165508 0 None -2 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 5.8 pEC50 = 5.8 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
57765622 162883 0 None -3 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 5.8 pEC50 = 5.8 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
122197954 166714 0 None -6 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 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 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 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
57765525 166233 0 None 1 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 5.8 pEC50 = 5.8 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
10197984 9199 44 None -630 5 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human mGluR8 assessed as effect on cAMP production in RGT cellsAgonist activity at human mGluR8 assessed as effect on cAMP production in RGT cells
ChEMBL 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10.1021/jm060917u
1394 9199 44 None -630 5 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human mGluR8 assessed as effect on cAMP production in RGT cellsAgonist activity at human mGluR8 assessed as effect on cAMP production in RGT cells
ChEMBL 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10.1021/jm060917u
CHEMBL275079 9199 44 None -630 5 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human mGluR8 assessed as effect on cAMP production in RGT cellsAgonist activity at human mGluR8 assessed as effect on cAMP production in RGT cells
ChEMBL 187 2 3 4 -1.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CO2)(N)C(=O)O 10.1021/jm060917u
10197984 9199 44 None -630 5 Human 5.8 pEC50 = 5.8 Functional
Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR8Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR8
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 -630 5 Human 5.8 pEC50 = 5.8 Functional
Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR8Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR8
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 -630 5 Human 5.8 pEC50 = 5.8 Functional
Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR8Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR8
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
137636549 162606 0 None 1 2 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 4.8 pEC50 = 4.8 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
137655963 165802 0 None -1 4 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 4.8 pEC50 = 4.8 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
6330803 98897 10 None 2 3 Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at rat mGluR8 receptor expressed HEK293 cells assessed as effect on inositol phosphate productionAgonist activity at rat mGluR8 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 5.8 pEC50 = 5.8 Functional
Agonist activity at rat mGluR8 receptor expressed HEK293 cells assessed as effect on inositol phosphate productionAgonist activity at rat mGluR8 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
69669747 190432 11 None -457 4 Human 5.8 pEC50 = 5.8 Functional
Antagonist activity at human recombinant mGlu8 stably expressed in golden hamster AV12 cell membrane co-expressing Galpha15 assessed as reduction in glutamate-induced calcium influx incubated for 90 to 120 min by Fluo-4-AM dye based FLIPR assayAntagonist activity at human recombinant mGlu8 stably expressed in golden hamster AV12 cell membrane co-expressing Galpha15 assessed as reduction in glutamate-induced calcium influx incubated for 90 to 120 min by Fluo-4-AM dye based FLIPR assay
ChEMBL 359 5 4 5 0.8 N[C@@]1(C(=O)O)[C@H](CSc2ccc(F)c(F)c2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
CHEMBL4751065 190432 11 None -457 4 Human 5.8 pEC50 = 5.8 Functional
Antagonist activity at human recombinant mGlu8 stably expressed in golden hamster AV12 cell membrane co-expressing Galpha15 assessed as reduction in glutamate-induced calcium influx incubated for 90 to 120 min by Fluo-4-AM dye based FLIPR assayAntagonist activity at human recombinant mGlu8 stably expressed in golden hamster AV12 cell membrane co-expressing Galpha15 assessed as reduction in glutamate-induced calcium influx incubated for 90 to 120 min by Fluo-4-AM dye based FLIPR assay
ChEMBL 359 5 4 5 0.8 N[C@@]1(C(=O)O)[C@H](CSc2ccc(F)c(F)c2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
CHEMBL4802733 190432 11 None -457 4 Human 5.8 pEC50 = 5.8 Functional
Antagonist activity at human recombinant mGlu8 stably expressed in golden hamster AV12 cell membrane co-expressing Galpha15 assessed as reduction in glutamate-induced calcium influx incubated for 90 to 120 min by Fluo-4-AM dye based FLIPR assayAntagonist activity at human recombinant mGlu8 stably expressed in golden hamster AV12 cell membrane co-expressing Galpha15 assessed as reduction in glutamate-induced calcium influx incubated for 90 to 120 min by Fluo-4-AM dye based FLIPR assay
ChEMBL 359 5 4 5 0.8 N[C@@]1(C(=O)O)[C@H](CSc2ccc(F)c(F)c2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/acs.jmedchem.6b01119
137649482 163976 0 None -2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 5.8 pEC50 = 5.8 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
137645989 164473 0 None -24 4 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 -24 4 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
46197776 15128 0 None -1 3 Rat 4.8 pEC50 = 4.8 Functional
Agonist activity at rat mGlu8 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 mGlu8 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 4.8 pEC50 = 4.8 Functional
Agonist activity at rat mGlu8 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 mGlu8 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
122197935 166631 0 None -181 4 Rat 4.7 pEC50 = 4.7 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 -181 4 Rat 4.7 pEC50 = 4.7 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
24780225 162712 0 None -2 3 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 4.7 pEC50 = 4.7 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
162648102 186683 0 None -2 5 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of mGluR8 (unknown origin) by calcium mobilization assayPositive allosteric modulation of mGluR8 (unknown origin) 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 -2 5 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of mGluR8 (unknown origin) by calcium mobilization assayPositive allosteric modulation of mGluR8 (unknown origin) 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
57765633 165191 0 None -3 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 5.7 pEC50 = 5.7 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
46197776 15128 0 None -1 3 Rat 4.7 pEC50 = 4.7 Functional
Agonist activity at rat mGlu8 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 mGlu8 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 4.7 pEC50 = 4.7 Functional
Agonist activity at rat mGlu8 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 mGlu8 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
46898088 9145 6 None -177 8 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 -177 8 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 -177 8 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
137642290 165013 0 None -8 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 4.7 pEC50 = 4.7 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
145962919 169152 0 None -1 2 Rat 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assay
ChEMBL 339 2 0 4 4.2 COc1ccc(-c2c(C)nn3c(C(F)(F)F)cc(C)nc23)cc1F 10.1021/acsmedchemlett.7b00317
CHEMBL4165248 169152 0 None -1 2 Rat 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assay
ChEMBL 339 2 0 4 4.2 COc1ccc(-c2c(C)nn3c(C(F)(F)F)cc(C)nc23)cc1F 10.1021/acsmedchemlett.7b00317
46918017 165488 0 None -2 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 4.7 pEC50 = 4.7 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
3756397 15086 2 None -2 4 Rat 4.7 pEC50 = 4.7 Functional
Agonist activity at rat mGlu8 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 mGlu8 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 4.7 pEC50 = 4.7 Functional
Agonist activity at rat mGlu8 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 mGlu8 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 4.7 pEC50 = 4.7 Functional
Agonist activity at rat mGlu8 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 mGlu8 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
145962919 169152 0 None -1 2 Rat 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assay
ChEMBL 339 2 0 4 4.2 COc1ccc(-c2c(C)nn3c(C(F)(F)F)cc(C)nc23)cc1F 10.1021/acsmedchemlett.7b00317
CHEMBL4165248 169152 0 None -1 2 Rat 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assay
ChEMBL 339 2 0 4 4.2 COc1ccc(-c2c(C)nn3c(C(F)(F)F)cc(C)nc23)cc1F 10.1021/acsmedchemlett.7b00317
127030386 145819 0 None -8 3 Rat 4.7 pEC50 = 4.7 Functional
Agonist activity at rat mGlu8 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu8 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 -8 3 Rat 4.7 pEC50 = 4.7 Functional
Agonist activity at rat mGlu8 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu8 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
1406 8854 38 None -1 7 Rat 6.7 pEC50 = 6.7 Functional
Metabotropic glutamate receptor 8 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 8 agonist activity against 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 -1 7 Rat 6.7 pEC50 = 6.7 Functional
Metabotropic glutamate receptor 8 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 8 agonist activity against 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 -1 7 Rat 6.7 pEC50 = 6.7 Functional
Metabotropic glutamate receptor 8 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 8 agonist activity against 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
57765607 166184 0 None 1 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 4.7 pEC50 = 4.7 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
1310 9095 110 None -2187 17 Rat 4.7 pEC50 = 4.7 Functional
Agonist activity at rat mGluR8 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR8 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 -2187 17 Rat 4.7 pEC50 = 4.7 Functional
Agonist activity at rat mGluR8 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR8 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 -2187 17 Rat 4.7 pEC50 = 4.7 Functional
Agonist activity at rat mGluR8 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR8 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 -2187 17 Rat 4.7 pEC50 = 4.7 Functional
Agonist activity at rat mGluR8 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR8 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 -2187 17 Rat 4.7 pEC50 = 4.7 Functional
Agonist activity at rat mGluR8 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR8 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 -2187 17 Rat 4.7 pEC50 = 4.7 Functional
Agonist activity at rat mGluR8 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR8 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 -2187 17 Rat 4.7 pEC50 = 4.7 Functional
Agonist activity at rat mGluR8 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR8 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
16747848 92290 0 None -1 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at mGlu8 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate productionAgonist activity at mGlu8 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 mGlu8 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate productionAgonist activity at mGlu8 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
122197942 166846 0 None -41 4 Rat 4.7 pEC50 = 4.7 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 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 -41 4 Rat 4.7 pEC50 = 4.7 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 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
58058384 163705 0 None -4 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 5.7 pEC50 = 5.7 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
137647077 164776 0 None -1 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 5.7 pEC50 = 5.7 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
137638288 163713 0 None -4 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 4.7 pEC50 = 4.7 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
137635566 163046 0 None 1 2 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 mGlu8 (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 mGlu8 (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
1407 8860 42 None -1 7 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 -1 7 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 -1 7 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
137650519 164124 0 None -21 4 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 -21 4 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
1410 9054 48 None 1 8 Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat mGlu8 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 mGlu8 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 6.6 pEC50 = 6.6 Functional
Agonist activity at rat mGlu8 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 mGlu8 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 6.6 pEC50 = 6.6 Functional
Agonist activity at rat mGlu8 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 mGlu8 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 6.6 pEC50 = 6.6 Functional
Agonist activity at rat mGlu8 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 mGlu8 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 6.6 pEC50 = 6.6 Functional
Agonist activity at rat mGlu8 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 mGlu8 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
57765535 164583 0 None -1 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 5.6 pEC50 = 5.6 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 5.6 pEC50 = 5.6 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 5.6 pEC50 = 5.6 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
137634091 163087 0 None -3 2 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 4.6 pEC50 = 4.6 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
122197949 166615 0 None -15 3 Rat 4.6 pEC50 = 4.6 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 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 4.6 pEC50 = 4.6 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 391 11 5 7 0.6 CCOc1cc(C(O)P(=O)(O)CC[C@@H](N)C(=O)O)ccc1OCC(=O)O nan
131954513 168857 38 None -4 5 Rat 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assay
ChEMBL 357 2 0 4 4.3 COc1ccc(-c2c(C)nn3c(C(F)(F)F)cc(C)nc23)c(F)c1F 10.1021/acsmedchemlett.7b00317
CHEMBL4160748 168857 38 None -4 5 Rat 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assay
ChEMBL 357 2 0 4 4.3 COc1ccc(-c2c(C)nn3c(C(F)(F)F)cc(C)nc23)c(F)c1F 10.1021/acsmedchemlett.7b00317
124425164 164794 0 None -10 4 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 -10 4 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
137631886 163155 0 None 1 2 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 mGlu8 (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 mGlu8 (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
131954513 168857 38 None -4 5 Rat 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assay
ChEMBL 357 2 0 4 4.3 COc1ccc(-c2c(C)nn3c(C(F)(F)F)cc(C)nc23)c(F)c1F 10.1021/acsmedchemlett.7b00317
CHEMBL4160748 168857 38 None -4 5 Rat 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assay
ChEMBL 357 2 0 4 4.3 COc1ccc(-c2c(C)nn3c(C(F)(F)F)cc(C)nc23)c(F)c1F 10.1021/acsmedchemlett.7b00317
57765531 163910 0 None -1 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 5.6 pEC50 = 5.6 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
24779944 14640 0 None 2 3 Rat 5.6 pEC50 = 5.6 Functional
Agonist activity at rat mGlu8 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 mGlu8 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 5.6 pEC50 = 5.6 Functional
Agonist activity at rat mGlu8 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 mGlu8 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
122197936 167555 0 None -53 3 Rat 4.6 pEC50 = 4.6 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 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 -53 3 Rat 4.6 pEC50 = 4.6 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 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
122197958 167303 0 None -83 4 Rat 4.6 pEC50 = 4.6 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 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 -83 4 Rat 4.6 pEC50 = 4.6 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 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
68012045 162960 0 None -1 2 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 4.6 pEC50 = 4.6 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
137661492 166272 0 None -1 2 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 4.6 pEC50 = 4.6 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
122197940 166786 0 None -186 3 Rat 4.6 pEC50 = 4.6 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 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 -186 3 Rat 4.6 pEC50 = 4.6 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 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
122197945 167008 0 None -2 3 Rat 4.6 pEC50 = 4.6 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 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 4.6 pEC50 = 4.6 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 333 9 5 6 0.1 N[C@H](CCP(=O)(O)C(O)c1ccc(OCCO)cc1)C(=O)O nan
145955288 169356 0 None -4 4 Rat 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assay
ChEMBL 357 2 0 4 4.3 COc1cc(F)c(-c2c(C)nn3c(C(F)(F)F)cc(C)nc23)c(F)c1 10.1021/acsmedchemlett.7b00317
CHEMBL4168668 169356 0 None -4 4 Rat 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assay
ChEMBL 357 2 0 4 4.3 COc1cc(F)c(-c2c(C)nn3c(C(F)(F)F)cc(C)nc23)c(F)c1 10.1021/acsmedchemlett.7b00317
1410 9054 48 None -1 8 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 6.5 pEC50 = 6.5 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 6.5 pEC50 = 6.5 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 6.5 pEC50 = 6.5 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 6.5 pEC50 = 6.5 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
1410 9054 48 None -1 8 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 6.5 pEC50 = 6.5 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 6.5 pEC50 = 6.5 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 6.5 pEC50 = 6.5 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 6.5 pEC50 = 6.5 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
1443 8100 36 None -2 5 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 183 4 4 3 -1.0 OC(=O)[C@@H](CCP(=O)(O)O)N nan
1550579 8100 36 None -2 5 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 183 4 4 3 -1.0 OC(=O)[C@@H](CCP(=O)(O)O)N nan
CHEMBL1319383 8100 36 None -2 5 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 183 4 4 3 -1.0 OC(=O)[C@@H](CCP(=O)(O)O)N nan
57765615 164346 0 None -1 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 5.5 pEC50 = 5.5 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
46197879 15014 0 None 2 2 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat mGlu8 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 mGlu8 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 5.5 pEC50 = 5.5 Functional
Agonist activity at rat mGlu8 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 mGlu8 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
145955288 169356 0 None -4 4 Rat 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assay
ChEMBL 357 2 0 4 4.3 COc1cc(F)c(-c2c(C)nn3c(C(F)(F)F)cc(C)nc23)c(F)c1 10.1021/acsmedchemlett.7b00317
CHEMBL4168668 169356 0 None -4 4 Rat 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assay
ChEMBL 357 2 0 4 4.3 COc1cc(F)c(-c2c(C)nn3c(C(F)(F)F)cc(C)nc23)c(F)c1 10.1021/acsmedchemlett.7b00317
6706 9146 8 None -263 8 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 -263 8 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 -263 8 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 -263 8 Rat 4.5 pEC50 = 4.5 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 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 -263 8 Rat 4.5 pEC50 = 4.5 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 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 -263 8 Rat 4.5 pEC50 = 4.5 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 347 9 5 6 0.2 OC(=O)COc1ccc(cc1)C(P(=O)(CC[C@@H](C(=O)O)N)O)O nan
122197947 167166 0 None -5 2 Rat 4.5 pEC50 = 4.5 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 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 4.5 pEC50 = 4.5 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 347 9 5 6 0.2 N[C@H](CCP(=O)(O)C(O)c1cccc(OCC(=O)O)c1)C(=O)O nan
137634489 162626 0 None -1 2 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 4.5 pEC50 = 4.5 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
16061421 163300 0 None -1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 6.5 pEC50 = 6.5 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
1410 9054 48 None 1 8 Rat 6.5 pEC50 = 6.5 Functional
Agonist activity at rat mGlu8 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 mGlu8 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 6.5 pEC50 = 6.5 Functional
Agonist activity at rat mGlu8 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 mGlu8 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 6.5 pEC50 = 6.5 Functional
Agonist activity at rat mGlu8 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 mGlu8 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 6.5 pEC50 = 6.5 Functional
Agonist activity at rat mGlu8 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 mGlu8 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 6.5 pEC50 = 6.5 Functional
Agonist activity at rat mGlu8 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 mGlu8 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
10353365 90022 1 None -2398 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human mGluR8 assessed as effect on cAMP production in RGT cellsAgonist activity at human mGluR8 assessed as effect on cAMP production in RGT cells
ChEMBL 219 2 3 4 -1.8 N[C@@]1(C(=O)O)C[S+]([O-])[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm060917u
CHEMBL218710 90022 1 None -2398 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human mGluR8 assessed as effect on cAMP production in RGT cellsAgonist activity at human mGluR8 assessed as effect on cAMP production in RGT cells
ChEMBL 219 2 3 4 -1.8 N[C@@]1(C(=O)O)C[S+]([O-])[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm060917u
1407 8860 42 None 1 7 Rat 7.5 pEC50 = 7.5 Functional
Metabotropic glutamate receptor 8 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 8 agonist activity against 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 1 7 Rat 7.5 pEC50 = 7.5 Functional
Metabotropic glutamate receptor 8 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 8 agonist activity against 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 1 7 Rat 7.5 pEC50 = 7.5 Functional
Metabotropic glutamate receptor 8 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 8 agonist activity against 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
137639752 163694 0 None -63 4 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 -63 4 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
1377 8122 26 None -190 8 Rat 4.5 pEC50 = 4.5 Functional
Metabotropic glutamate receptor 8 antagonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 8 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 -190 8 Rat 4.5 pEC50 = 4.5 Functional
Metabotropic glutamate receptor 8 antagonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 8 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 -190 8 Rat 4.5 pEC50 = 4.5 Functional
Metabotropic glutamate receptor 8 antagonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 8 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
58058356 165573 0 None -2 3 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 4.5 pEC50 = 4.5 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
58058380 164552 0 None -2 2 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 4.5 pEC50 = 4.5 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
16747847 92617 1 None -11 4 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at mGlu8 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate productionAgonist activity at mGlu8 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 -11 4 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at mGlu8 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate productionAgonist activity at mGlu8 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
24780091 163848 0 None -2 2 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 4.5 pEC50 = 4.5 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
122197952 167351 0 None -30 3 Rat 4.5 pEC50 = 4.5 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 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 -30 3 Rat 4.5 pEC50 = 4.5 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 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
137661528 166286 0 None -45 4 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 -45 4 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
24779945 15013 0 None -3 3 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat mGlu8 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 mGlu8 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 5.5 pEC50 = 5.5 Functional
Agonist activity at rat mGlu8 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 mGlu8 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
137659207 165885 0 None -4 2 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 4.5 pEC50 = 4.5 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
137652072 163988 0 None -1 2 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 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 4.4 pEC50 = 4.4 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 274 6 4 5 0.1 N[C@@H](CCP(=O)(O)C(O)c1cccnc1)C(=O)O 10.1021/acs.jmedchem.7b01438
122197947 167166 0 None -5 2 Rat 4.4 pEC50 = 4.4 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 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 4.4 pEC50 = 4.4 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 347 9 5 6 0.2 N[C@H](CCP(=O)(O)C(O)c1cccc(OCC(=O)O)c1)C(=O)O nan
122197937 167087 0 None -13 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 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 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 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
92044496 162746 0 None -2 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 6.4 pEC50 = 6.4 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
57765531 163910 0 None -1 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 5.4 pEC50 = 5.4 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
137638200 163596 0 None -6 2 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 4.4 pEC50 = 4.4 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
24779945 15013 0 None -3 3 Rat 4.4 pEC50 = 4.4 Functional
Agonist activity at rat mGlu8 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 mGlu8 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 4.4 pEC50 = 4.4 Functional
Agonist activity at rat mGlu8 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 mGlu8 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
122197965 166628 0 None -6 2 Rat 4.4 pEC50 = 4.4 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 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 4.4 pEC50 = 4.4 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 395 10 4 6 1.4 COc1cc(CP(=O)(O)CC[C@@H](N)C(=O)O)cc(Cl)c1OCC(=O)O nan
137654697 165466 0 None -8 3 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 4.4 pEC50 = 4.4 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
1368 9070 37 None -1 11 Rat 6.4 pEC50 = 6.4 Functional
Metabotropic glutamate receptor 8 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 8 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 10.1021/jm030967o
5310956 9070 37 None -1 11 Rat 6.4 pEC50 = 6.4 Functional
Metabotropic glutamate receptor 8 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 8 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 10.1021/jm030967o
CHEMBL280563 9070 37 None -1 11 Rat 6.4 pEC50 = 6.4 Functional
Metabotropic glutamate receptor 8 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 8 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 10.1021/jm030967o
137651515 164228 0 None -2 2 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 4.4 pEC50 = 4.4 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
57765594 166269 0 None -4 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 5.4 pEC50 = 5.4 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
46918015 162647 0 None -29 4 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 -29 4 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
1407 8860 42 None -1 7 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 -1 7 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 -1 7 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
58058372 162976 0 None -3 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 5.4 pEC50 = 5.4 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
122197939 167473 0 None -338 3 Rat 4.4 pEC50 = 4.4 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 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 -338 3 Rat 4.4 pEC50 = 4.4 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 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
57765556 163460 0 None -1 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 5.4 pEC50 = 5.4 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
57765529 162616 0 None -3 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 5.3 pEC50 = 5.3 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
9834591 144378 69 None -2041 3 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human mGluR8 assessed as effect on cAMP production in RGT cellsAgonist activity at human mGluR8 assessed as effect on cAMP production in RGT cells
ChEMBL 235 2 3 5 -2.1 N[C@@]1(C(=O)O)CS(=O)(=O)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm060917u
CHEMBL375611 144378 69 None -2041 3 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human mGluR8 assessed as effect on cAMP production in RGT cellsAgonist activity at human mGluR8 assessed as effect on cAMP production in RGT cells
ChEMBL 235 2 3 5 -2.1 N[C@@]1(C(=O)O)CS(=O)(=O)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm060917u
46884710 14991 0 None 1 2 Rat 4.3 pEC50 = 4.3 Functional
Agonist activity at rat mGlu8 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 mGlu8 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 4.3 pEC50 = 4.3 Functional
Agonist activity at rat mGlu8 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 mGlu8 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
122197944 167002 0 None -50 3 Rat 4.3 pEC50 = 4.3 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 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 -50 3 Rat 4.3 pEC50 = 4.3 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 345 9 5 5 0.8 N[C@H](CCP(=O)(O)C(O)c1ccc(CCC(=O)O)cc1)C(=O)O nan
145957567 169067 0 None -1 2 Rat 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assay
ChEMBL 373 2 0 4 4.8 COc1cc(F)c(-c2c(C)nn3c(C(F)(F)F)cc(C)nc23)cc1Cl 10.1021/acsmedchemlett.7b00317
CHEMBL4164141 169067 0 None -1 2 Rat 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assay
ChEMBL 373 2 0 4 4.8 COc1cc(F)c(-c2c(C)nn3c(C(F)(F)F)cc(C)nc23)cc1Cl 10.1021/acsmedchemlett.7b00317
57765536 165050 0 None -1 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 6.3 pEC50 = 6.3 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
145957567 169067 0 None -1 2 Rat 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assay
ChEMBL 373 2 0 4 4.8 COc1cc(F)c(-c2c(C)nn3c(C(F)(F)F)cc(C)nc23)cc1Cl 10.1021/acsmedchemlett.7b00317
CHEMBL4164141 169067 0 None -1 2 Rat 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assay
ChEMBL 373 2 0 4 4.8 COc1cc(F)c(-c2c(C)nn3c(C(F)(F)F)cc(C)nc23)cc1Cl 10.1021/acsmedchemlett.7b00317
57765535 164583 0 None -1 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 mGlu8 (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 mGlu8 (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
122197943 167359 0 None -102 3 Rat 4.3 pEC50 = 4.3 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 -102 3 Rat 4.3 pEC50 = 4.3 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
92044496 162746 0 None -2 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 6.3 pEC50 = 6.3 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
1408 7053 31 None -1 7 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 5.3 pEC50 = 5.3 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 5.3 pEC50 = 5.3 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 5.3 pEC50 = 5.3 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
46197778 14990 0 None -5 5 Rat 5.3 pEC50 = 5.3 Functional
Agonist activity at rat mGlu8 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 mGlu8 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 -5 5 Rat 5.3 pEC50 = 5.3 Functional
Agonist activity at rat mGlu8 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 mGlu8 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
1408 7053 31 None -1 7 Rat 5.3 pEC50 = 5.3 Functional
Agonist activity at rat mGlu8 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 mGlu8 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 5.3 pEC50 = 5.3 Functional
Agonist activity at rat mGlu8 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 mGlu8 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 5.3 pEC50 = 5.3 Functional
Agonist activity at rat mGlu8 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 mGlu8 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 5.3 pEC50 = 5.3 Functional
Agonist activity at rat mGlu8 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 mGlu8 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
57765572 164103 0 None -3 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 5.3 pEC50 = 5.3 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
57765536 165050 0 None -1 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 6.3 pEC50 = 6.3 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
46884751 15012 0 None -4 2 Rat 4.3 pEC50 = 4.3 Functional
Agonist activity at rat mGlu8 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 mGlu8 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 4.3 pEC50 = 4.3 Functional
Agonist activity at rat mGlu8 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 mGlu8 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
192790 78664 38 None -4 2 Rat 4.3 pEC50 = 4.3 Functional
Agonist activity in rat at mGlu8a receptor expressed in HEK293 cellsAgonist activity in rat at mGlu8a receptor expressed in HEK293 cells
ChEMBL 163 4 4 4 -1.8 N[C@@H](C[C@H](O)C(=O)O)C(=O)O 10.1016/s0960-894x(01)00158-5
44286641 78664 38 None -4 2 Rat 4.3 pEC50 = 4.3 Functional
Agonist activity in rat at mGlu8a receptor expressed in HEK293 cellsAgonist activity in rat at mGlu8a receptor expressed in HEK293 cells
ChEMBL 163 4 4 4 -1.8 N[C@@H](C[C@H](O)C(=O)O)C(=O)O 10.1016/s0960-894x(01)00158-5
CHEMBL197110 78664 38 None -4 2 Rat 4.3 pEC50 = 4.3 Functional
Agonist activity in rat at mGlu8a receptor expressed in HEK293 cellsAgonist activity in rat at mGlu8a receptor expressed in HEK293 cells
ChEMBL 163 4 4 4 -1.8 N[C@@H](C[C@H](O)C(=O)O)C(=O)O 10.1016/s0960-894x(01)00158-5
17759041 99636 8 None -1 3 Rat 7.3 pEC50 = 7.3 Functional
Agonist activity at rat mGluR8 receptor expressed HEK293 cells assessed as effect on inositol phosphate productionAgonist activity at rat mGluR8 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 7.3 pEC50 = 7.3 Functional
Agonist activity at rat mGluR8 receptor expressed HEK293 cells assessed as effect on inositol phosphate productionAgonist activity at rat mGluR8 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
58058356 165573 0 None -2 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 mGlu8 (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 mGlu8 (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
122197950 167092 0 None -933 3 Rat 4.3 pEC50 = 4.3 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 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 -933 3 Rat 4.3 pEC50 = 4.3 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 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
1410 9054 48 None -1 8 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at mGlu8 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate productionAgonist activity at mGlu8 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 6.3 pEC50 = 6.3 Functional
Agonist activity at mGlu8 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate productionAgonist activity at mGlu8 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 6.3 pEC50 = 6.3 Functional
Agonist activity at mGlu8 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate productionAgonist activity at mGlu8 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 6.3 pEC50 = 6.3 Functional
Agonist activity at mGlu8 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate productionAgonist activity at mGlu8 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 6.3 pEC50 = 6.3 Functional
Agonist activity at mGlu8 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate productionAgonist activity at mGlu8 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
57765525 166233 0 None 1 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 5.3 pEC50 = 5.3 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
11565290 8461 11 None -1258 3 Rat 4.3 pEC50 = 4.3 Functional
Activity at rat mGluR8 receptor measured as intracellular calcium concentration in HEK293 cellsActivity at rat mGluR8 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 -1258 3 Rat 4.3 pEC50 = 4.3 Functional
Activity at rat mGluR8 receptor measured as intracellular calcium concentration in HEK293 cellsActivity at rat mGluR8 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 -1258 3 Rat 4.3 pEC50 = 4.3 Functional
Activity at rat mGluR8 receptor measured as intracellular calcium concentration in HEK293 cellsActivity at rat mGluR8 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
1608415 14591 8 None -3 3 Rat 4.2 pEC50 = 4.2 Functional
Agonist activity at rat mGlu8 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 mGlu8 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 4.2 pEC50 = 4.2 Functional
Agonist activity at rat mGlu8 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 mGlu8 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 4.2 pEC50 = 4.2 Functional
Agonist activity at rat mGlu8 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 mGlu8 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
1410 9054 48 None 1 8 Rat 7.2 pEC50 = 7.2 Functional
Metabotropic glutamate receptor 8 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 8 agonist activity against 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 7.2 pEC50 = 7.2 Functional
Metabotropic glutamate receptor 8 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 8 agonist activity against 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 7.2 pEC50 = 7.2 Functional
Metabotropic glutamate receptor 8 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 8 agonist activity against 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 7.2 pEC50 = 7.2 Functional
Metabotropic glutamate receptor 8 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 8 agonist activity against 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 7.2 pEC50 = 7.2 Functional
Metabotropic glutamate receptor 8 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 8 agonist activity against 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
137644345 164897 0 None -9 3 Human 4.2 pEC50 = 4.2 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 -9 3 Human 4.2 pEC50 = 4.2 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
6348408 14592 1 None -1 8 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 mGlu8 (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 mGlu8 (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
137632643 163196 0 None -1 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 mGlu8 (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 mGlu8 (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
16748099 126641 1 None -1 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at mGlu8 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate productionAgonist activity at mGlu8 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 5.2 pEC50 = 5.2 Functional
Agonist activity at mGlu8 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate productionAgonist activity at mGlu8 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
57765613 165269 0 None -1 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 6.2 pEC50 = 6.2 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
87618914 165963 0 None -4 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 5.2 pEC50 = 5.2 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
6348408 14592 1 None -1 8 Rat 5.2 pEC50 = 5.2 Functional
Agonist activity at rat mGlu8 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 mGlu8 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 mGlu8 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 mGlu8 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
46898088 9145 6 None -177 8 Human 4.2 pEC50 = 4.2 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 -177 8 Human 4.2 pEC50 = 4.2 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 -177 8 Human 4.2 pEC50 = 4.2 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
127030387 145884 0 None -5 3 Rat 6.2 pEC50 = 6.2 Functional
Agonist activity at rat mGlu8 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu8 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 -5 3 Rat 6.2 pEC50 = 6.2 Functional
Agonist activity at rat mGlu8 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu8 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
122197951 167513 0 None -7 3 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 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 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 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
137635378 162581 0 None -2 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 5.2 pEC50 = 5.2 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
440854 141826 44 None - 1 Rat 4.2 pEC50 = 4.2 Functional
Agonist activity in rat at mGlu8a receptor expressed in HEK293 cellsAgonist activity in rat at mGlu8a receptor expressed in HEK293 cells
ChEMBL 163 4 4 4 -1.8 N[C@@H](C[C@@H](O)C(=O)O)C(=O)O 10.1016/s0960-894x(01)00158-5
44286856 141826 44 None - 1 Rat 4.2 pEC50 = 4.2 Functional
Agonist activity in rat at mGlu8a receptor expressed in HEK293 cellsAgonist activity in rat at mGlu8a receptor expressed in HEK293 cells
ChEMBL 163 4 4 4 -1.8 N[C@@H](C[C@@H](O)C(=O)O)C(=O)O 10.1016/s0960-894x(01)00158-5
CHEMBL371946 141826 44 None - 1 Rat 4.2 pEC50 = 4.2 Functional
Agonist activity in rat at mGlu8a receptor expressed in HEK293 cellsAgonist activity in rat at mGlu8a receptor expressed in HEK293 cells
ChEMBL 163 4 4 4 -1.8 N[C@@H](C[C@@H](O)C(=O)O)C(=O)O 10.1016/s0960-894x(01)00158-5
1410 9054 48 None 1 8 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat mGlu8 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu8 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 7.2 pEC50 = 7.2 Functional
Agonist activity at rat mGlu8 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu8 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 7.2 pEC50 = 7.2 Functional
Agonist activity at rat mGlu8 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu8 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 7.2 pEC50 = 7.2 Functional
Agonist activity at rat mGlu8 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu8 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 7.2 pEC50 = 7.2 Functional
Agonist activity at rat mGlu8 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu8 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
122197947 167166 0 None -5 2 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 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 4.2 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 347 9 5 6 0.2 N[C@H](CCP(=O)(O)C(O)c1cccc(OCC(=O)O)c1)C(=O)O nan
137643617 164927 0 None -1 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 5.1 pEC50 = 5.1 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
46197778 14990 0 None -5 5 Rat 5.1 pEC50 = 5.1 Functional
Agonist activity at rat mGlu8 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 mGlu8 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 -5 5 Rat 5.1 pEC50 = 5.1 Functional
Agonist activity at rat mGlu8 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 mGlu8 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
46918015 162647 0 None -29 4 Human 4.1 pEC50 = 4.1 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 -29 4 Human 4.1 pEC50 = 4.1 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
14376076 14538 0 None - 1 Rat 4.1 pEC50 = 4.1 Functional
Agonist activity at rat mGlu8 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 mGlu8 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 181 5 3 3 -0.4 N[C@@H](CCC[PH](=O)O)C(=O)O 10.1021/jm901523t
CHEMBL1089174 14538 0 None - 1 Rat 4.1 pEC50 = 4.1 Functional
Agonist activity at rat mGlu8 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 mGlu8 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 181 5 3 3 -0.4 N[C@@H](CCC[PH](=O)O)C(=O)O 10.1021/jm901523t
10198133 213287 12 None -1905 4 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human mGluR8 assessed as effect on cAMP production in RGT cellsAgonist activity at human mGluR8 assessed as effect on cAMP production in RGT cells
ChEMBL 203 2 3 4 -0.8 N[C@@]1(C(=O)O)CS[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm060917u
CHEMBL8839 213287 12 None -1905 4 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human mGluR8 assessed as effect on cAMP production in RGT cellsAgonist activity at human mGluR8 assessed as effect on cAMP production in RGT cells
ChEMBL 203 2 3 4 -0.8 N[C@@]1(C(=O)O)CS[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm060917u
10198133 213287 12 None -1905 4 Human 5.1 pEC50 = 5.1 Functional
Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR8Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR8
ChEMBL 203 2 3 4 -0.8 N[C@@]1(C(=O)O)CS[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm980616n
CHEMBL8839 213287 12 None -1905 4 Human 5.1 pEC50 = 5.1 Functional
Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR8Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR8
ChEMBL 203 2 3 4 -0.8 N[C@@]1(C(=O)O)CS[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm980616n
122197953 166732 0 None -1 3 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 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 5.1 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 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
24780225 162712 0 None -2 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 5.1 pEC50 = 5.1 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
46197878 15210 0 None -3 2 Rat 4.1 pEC50 = 4.1 Functional
Agonist activity at rat mGlu8 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 mGlu8 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 4.1 pEC50 = 4.1 Functional
Agonist activity at rat mGlu8 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 mGlu8 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
6348408 14592 1 None -1 8 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 5.1 pEC50 = 5.1 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
6348408 14592 1 None -1 8 Rat 5.1 pEC50 = 5.1 Functional
Agonist activity at rat mGlu8 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 mGlu8 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 5.1 pEC50 = 5.1 Functional
Agonist activity at rat mGlu8 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 mGlu8 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
1310 9095 110 None -2187 17 Rat 5.1 pEC50 = 5.1 Functional
Agonist activity in rat at Metabotropic glutamate receptor 8 expressed in HEK293 cellsAgonist activity in rat at Metabotropic glutamate receptor 8 expressed in HEK293 cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/s0960-894x(01)00158-5
1369 9095 110 None -2187 17 Rat 5.1 pEC50 = 5.1 Functional
Agonist activity in rat at Metabotropic glutamate receptor 8 expressed in HEK293 cellsAgonist activity in rat at Metabotropic glutamate receptor 8 expressed in HEK293 cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/s0960-894x(01)00158-5
33032 9095 110 None -2187 17 Rat 5.1 pEC50 = 5.1 Functional
Agonist activity in rat at Metabotropic glutamate receptor 8 expressed in HEK293 cellsAgonist activity in rat at Metabotropic glutamate receptor 8 expressed in HEK293 cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/s0960-894x(01)00158-5
44272391 9095 110 None -2187 17 Rat 5.1 pEC50 = 5.1 Functional
Agonist activity in rat at Metabotropic glutamate receptor 8 expressed in HEK293 cellsAgonist activity in rat at Metabotropic glutamate receptor 8 expressed in HEK293 cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/s0960-894x(01)00158-5
88747398 9095 110 None -2187 17 Rat 5.1 pEC50 = 5.1 Functional
Agonist activity in rat at Metabotropic glutamate receptor 8 expressed in HEK293 cellsAgonist activity in rat at Metabotropic glutamate receptor 8 expressed in HEK293 cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/s0960-894x(01)00158-5
CHEMBL575060 9095 110 None -2187 17 Rat 5.1 pEC50 = 5.1 Functional
Agonist activity in rat at Metabotropic glutamate receptor 8 expressed in HEK293 cellsAgonist activity in rat at Metabotropic glutamate receptor 8 expressed in HEK293 cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/s0960-894x(01)00158-5
DB00142 9095 110 None -2187 17 Rat 5.1 pEC50 = 5.1 Functional
Agonist activity in rat at Metabotropic glutamate receptor 8 expressed in HEK293 cellsAgonist activity in rat at Metabotropic glutamate receptor 8 expressed in HEK293 cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/s0960-894x(01)00158-5
46197780 12354 0 None -4 4 Rat 5.1 pEC50 = 5.1 Functional
Agonist activity at rat mGlu8 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 mGlu8 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 5.1 pEC50 = 5.1 Functional
Agonist activity at rat mGlu8 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 mGlu8 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
137651881 164063 0 None -1 2 Human 4.1 pEC50 = 4.1 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 4.1 pEC50 = 4.1 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
46197780 12354 0 None -4 4 Rat 5.1 pEC50 = 5.1 Functional
Agonist activity at rat mGlu8 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 mGlu8 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 5.1 pEC50 = 5.1 Functional
Agonist activity at rat mGlu8 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 mGlu8 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
137643759 165205 0 None 1 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 mGlu8 (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 mGlu8 (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 mGlu8 (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 mGlu8 (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 mGlu8 (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 mGlu8 (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
145957424 168848 0 None -1 3 Rat 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux 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 -1 3 Rat 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux 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
145957424 168848 0 None -1 3 Rat 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux 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 -1 3 Rat 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux 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
10238 10799 26 None 1 5 Rat 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux 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 1 5 Rat 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux 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 1 5 Rat 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux 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
24779944 14640 0 None 2 3 Rat 6.0 pEC50 = 6.0 Functional
Agonist activity at rat mGlu8 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 mGlu8 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 6.0 pEC50 = 6.0 Functional
Agonist activity at rat mGlu8 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 mGlu8 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
24780084 14488 0 None -9 2 Rat 4.0 pEC50 = 4.0 Functional
Agonist activity at rat mGlu8 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 mGlu8 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 4.0 pEC50 = 4.0 Functional
Agonist activity at rat mGlu8 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 mGlu8 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 4.0 pEC50 = 4.0 Functional
Agonist activity at rat mGlu8 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 mGlu8 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
122197964 167216 0 None -2 2 Rat 5.0 pEC50 = 5.0 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 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 5.0 pEC50 = 5.0 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 379 10 4 6 0.9 COc1cc(CP(=O)(O)CC[C@@H](N)C(=O)O)cc(F)c1OCC(=O)O nan
137649749 164066 0 None -4 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 5.0 pEC50 = 5.0 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
10238 10799 26 None 1 5 Rat 6.0 pEC50 = 6.0 Functional
Agonist activity at rat mGlu8 receptor expressed in HEK cell co-expressing Galpha15 (unknown origin) assessed as reduction in intracellular Ca2+ mobilization by Fluo-4-AM dye based fluorescence assayAgonist activity at rat mGlu8 receptor expressed in HEK cell co-expressing Galpha15 (unknown origin) assessed as reduction in intracellular Ca2+ mobilization 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 1 5 Rat 6.0 pEC50 = 6.0 Functional
Agonist activity at rat mGlu8 receptor expressed in HEK cell co-expressing Galpha15 (unknown origin) assessed as reduction in intracellular Ca2+ mobilization by Fluo-4-AM dye based fluorescence assayAgonist activity at rat mGlu8 receptor expressed in HEK cell co-expressing Galpha15 (unknown origin) assessed as reduction in intracellular Ca2+ mobilization 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 1 5 Rat 6.0 pEC50 = 6.0 Functional
Agonist activity at rat mGlu8 receptor expressed in HEK cell co-expressing Galpha15 (unknown origin) assessed as reduction in intracellular Ca2+ mobilization by Fluo-4-AM dye based fluorescence assayAgonist activity at rat mGlu8 receptor expressed in HEK cell co-expressing Galpha15 (unknown origin) assessed as reduction in intracellular Ca2+ mobilization 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
57765616 164197 0 None -2 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at mGlu8 (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 mGlu8 (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 6.0 pEC50 = 6.0 Functional
Agonist activity at mGlu8 (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 mGlu8 (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
44328850 214830 0 None -1 4 Human 5.9 pIC50 = 5.9 Functional
Antagonistic activity against metabotropic glutamate receptor 8 (mGluR8) was evaluatedAntagonistic activity against metabotropic glutamate receptor 8 (mGluR8) was evaluated
ChEMBL 367 5 3 4 3.1 C[C@@H]1[C@H](C(=O)O)[C@H]1C(N)(CC1c2ccccc2Oc2ccccc21)C(=O)O 10.1016/s0960-894x(98)00510-1
CHEMBL97574 214830 0 None -1 4 Human 5.9 pIC50 = 5.9 Functional
Antagonistic activity against metabotropic glutamate receptor 8 (mGluR8) was evaluatedAntagonistic activity against metabotropic glutamate receptor 8 (mGluR8) 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
1378 9195 54 None -21 14 Human 6.8 pIC50 = 6.8 Functional
Antagonistic activity against metabotropic glutamate receptor 8 (mGluR8) was evaluatedAntagonistic activity against metabotropic glutamate receptor 8 (mGluR8) 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 -21 14 Human 6.8 pIC50 = 6.8 Functional
Antagonistic activity against metabotropic glutamate receptor 8 (mGluR8) was evaluatedAntagonistic activity against metabotropic glutamate receptor 8 (mGluR8) 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 -21 14 Human 6.8 pIC50 = 6.8 Functional
Antagonistic activity against metabotropic glutamate receptor 8 (mGluR8) was evaluatedAntagonistic activity against metabotropic glutamate receptor 8 (mGluR8) 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 -21 14 Human 6.8 pIC50 = 6.8 Functional
Antagonistic activity against metabotropic glutamate receptor 8 (mGluR8) was evaluatedAntagonistic activity against metabotropic glutamate receptor 8 (mGluR8) 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
57338826 156406 0 None -41 5 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at recombinant human mGlu8 receptor expressed in hamster AV12 cells co-expressing human EAAT1/Galpha1s assessed as inhibition of Ca2+ flux by Fluo-3-AM dye based FLIPR assayAntagonist activity at recombinant human mGlu8 receptor expressed in hamster AV12 cells co-expressing human EAAT1/Galpha1s assessed as inhibition of Ca2+ flux by Fluo-3-AM dye based FLIPR assay
ChEMBL 375 5 4 5 1.0 N[C@@]1(C(=O)O)[C@H](OCc2ccc(Cl)c(Cl)c2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1016/j.bmcl.2016.10.067
CHEMBL3947221 156406 0 None -41 5 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at recombinant human mGlu8 receptor expressed in hamster AV12 cells co-expressing human EAAT1/Galpha1s assessed as inhibition of Ca2+ flux by Fluo-3-AM dye based FLIPR assayAntagonist activity at recombinant human mGlu8 receptor expressed in hamster AV12 cells co-expressing human EAAT1/Galpha1s assessed as inhibition of Ca2+ flux by Fluo-3-AM dye based FLIPR assay
ChEMBL 375 5 4 5 1.0 N[C@@]1(C(=O)O)[C@H](OCc2ccc(Cl)c(Cl)c2)[C@@H](O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1016/j.bmcl.2016.10.067
44329024 215137 0 None -11 3 Human 5.7 pIC50 = 5.7 Functional
Antagonistic activity against metabotropic glutamate receptor 8 (mGluR8) was evaluatedAntagonistic activity against metabotropic glutamate receptor 8 (mGluR8) was evaluated
ChEMBL 395 7 3 4 3.8 CCC[C@@H]1[C@H](C(=O)O)[C@H]1C(N)(CC1c2ccccc2Oc2ccccc21)C(=O)O 10.1016/s0960-894x(98)00510-1
CHEMBL99462 215137 0 None -11 3 Human 5.7 pIC50 = 5.7 Functional
Antagonistic activity against metabotropic glutamate receptor 8 (mGluR8) was evaluatedAntagonistic activity against metabotropic glutamate receptor 8 (mGluR8) was evaluated
ChEMBL 395 7 3 4 3.8 CCC[C@@H]1[C@H](C(=O)O)[C@H]1C(N)(CC1c2ccccc2Oc2ccccc21)C(=O)O 10.1016/s0960-894x(98)00510-1
44329042 175862 0 None -33 5 Human 5.6 pIC50 = 5.6 Functional
Antagonistic activity against metabotropic glutamate receptor 8 (mGluR8) was evaluatedAntagonistic activity against metabotropic glutamate receptor 8 (mGluR8) was evaluated
ChEMBL 381 6 3 4 3.5 CC[C@@H]1[C@H](C(=O)O)[C@H]1C(N)(CC1c2ccccc2Oc2ccccc21)C(=O)O 10.1016/s0960-894x(98)00510-1
CHEMBL439775 175862 0 None -33 5 Human 5.6 pIC50 = 5.6 Functional
Antagonistic activity against metabotropic glutamate receptor 8 (mGluR8) was evaluatedAntagonistic activity against metabotropic glutamate receptor 8 (mGluR8) 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
44329032 119321 0 None -3 5 Human 6.5 pIC50 = 6.5 Functional
Antagonistic activity against metabotropic glutamate receptor 8 (mGluR8) was evaluatedAntagonistic activity against metabotropic glutamate receptor 8 (mGluR8) was evaluated
ChEMBL 423 9 3 4 4.6 CCCCC[C@@H]1[C@H](C(=O)O)[C@H]1C(N)(CC1c2ccccc2Oc2ccccc21)C(=O)O 10.1016/s0960-894x(98)00510-1
CHEMBL329920 119321 0 None -3 5 Human 6.5 pIC50 = 6.5 Functional
Antagonistic activity against metabotropic glutamate receptor 8 (mGluR8) was evaluatedAntagonistic activity against metabotropic glutamate receptor 8 (mGluR8) 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
44329033 214759 0 None -9 5 Human 6.4 pIC50 = 6.4 Functional
Antagonistic activity against metabotropic glutamate receptor 8 (mGluR8) was evaluatedAntagonistic activity against metabotropic glutamate receptor 8 (mGluR8) was evaluated
ChEMBL 409 7 3 4 4.1 CC(C)C[C@@H]1[C@H](C(=O)O)[C@H]1C(N)(CC1c2ccccc2Oc2ccccc21)C(=O)O 10.1016/s0960-894x(98)00510-1
CHEMBL97200 214759 0 None -9 5 Human 6.4 pIC50 = 6.4 Functional
Antagonistic activity against metabotropic glutamate receptor 8 (mGluR8) was evaluatedAntagonistic activity against metabotropic glutamate receptor 8 (mGluR8) 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
44328753 214533 0 None -16 6 Human 6.3 pIC50 = 6.3 Functional
Antagonistic activity against metabotropic glutamate receptor 8 (mGluR8) was evaluatedAntagonistic activity against metabotropic glutamate receptor 8 (mGluR8) was evaluated
ChEMBL 409 8 3 4 4.2 CCCC[C@@H]1[C@H](C(=O)O)[C@H]1C(N)(CC1c2ccccc2Oc2ccccc21)C(=O)O 10.1016/s0960-894x(98)00510-1
CHEMBL95868 214533 0 None -16 6 Human 6.3 pIC50 = 6.3 Functional
Antagonistic activity against metabotropic glutamate receptor 8 (mGluR8) was evaluatedAntagonistic activity against metabotropic glutamate receptor 8 (mGluR8) 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
44329029 170300 0 None -2 6 Human 5.3 pIC50 = 5.3 Functional
Antagonistic activity against metabotropic glutamate receptor 8 (mGluR8) was evaluatedAntagonistic activity against metabotropic glutamate receptor 8 (mGluR8) 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 -2 6 Human 5.3 pIC50 = 5.3 Functional
Antagonistic activity against metabotropic glutamate receptor 8 (mGluR8) was evaluatedAntagonistic activity against metabotropic glutamate receptor 8 (mGluR8) 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
44329031 115051 0 None -6 7 Human 6.1 pIC50 = 6.1 Functional
Antagonistic activity against metabotropic glutamate receptor 8 (mGluR8) was evaluatedAntagonistic activity against metabotropic glutamate receptor 8 (mGluR8) was evaluated
ChEMBL 437 10 3 4 5.0 CCCCCC[C@@H]1[C@H](C(=O)O)[C@H]1C(N)(CC1c2ccccc2Oc2ccccc21)C(=O)O 10.1016/s0960-894x(98)00510-1
CHEMBL319732 115051 0 None -6 7 Human 6.1 pIC50 = 6.1 Functional
Antagonistic activity against metabotropic glutamate receptor 8 (mGluR8) was evaluatedAntagonistic activity against metabotropic glutamate receptor 8 (mGluR8) 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
10456810 114656 0 None -7 5 Human 6.0 pIC50 = 6 Functional
Antagonistic activity against metabotropic glutamate receptor 8 (mGluR8) was evaluatedAntagonistic activity against metabotropic glutamate receptor 8 (mGluR8) was evaluated
ChEMBL 457 8 3 4 4.7 NC(CC1c2ccccc2Oc2ccccc21)(C(=O)O)[C@H]1[C@H](CCc2ccccc2)[C@@H]1C(=O)O 10.1016/s0960-894x(98)00510-1
CHEMBL319279 114656 0 None -7 5 Human 6.0 pIC50 = 6 Functional
Antagonistic activity against metabotropic glutamate receptor 8 (mGluR8) was evaluatedAntagonistic activity against metabotropic glutamate receptor 8 (mGluR8) 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
1393 8321 64 None -1047 6 Human 4.9 pKi = 4.9 Functional
Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm000007r
1396 8321 64 None -1047 6 Human 4.9 pKi = 4.9 Functional
Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm000007r
213056 8321 64 None -1047 6 Human 4.9 pKi = 4.9 Functional
Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm000007r
CHEMBL8759 8321 64 None -1047 6 Human 4.9 pKi = 4.9 Functional
Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).
ChEMBL 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10.1021/jm000007r
44322840 119348 0 None - 0 Human 4.8 pKi = 4.8 Functional
Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).
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 4.8 pKi = 4.8 Functional
Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).
ChEMBL 201 2 4 4 -1.5 N[C@]1(C(=O)O)C2C(C[C@H]1O)[C@@H]2C(=O)O 10.1021/jm000007r
1378 9195 54 None -21 14 Human 6.8 pKi = 6.8 Functional
Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).
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 -21 14 Human 6.8 pKi = 6.8 Functional
Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).
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 -21 14 Human 6.8 pKi = 6.8 Functional
Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).
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 -21 14 Human 6.8 pKi = 6.8 Functional
Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/jm000007r
10197984 9199 44 None -630 5 Human 5.8 pKi = 5.8 Functional
Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).
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 -630 5 Human 5.8 pKi = 5.8 Functional
Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).
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 -630 5 Human 5.8 pKi = 5.8 Functional
Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).
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
1406 8854 38 None 1 7 Human 6.7 pKi = 6.7 Functional
Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).
ChEMBL 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10.1021/jm000007r
4545574 8854 38 None 1 7 Human 6.7 pKi = 6.7 Functional
Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).
ChEMBL 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10.1021/jm000007r
CHEMBL277475 8854 38 None 1 7 Human 6.7 pKi = 6.7 Functional
Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).
ChEMBL 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10.1021/jm000007r
1368 9070 37 None -1 11 Human 5.5 pKi = 5.5 Functional
Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).
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 -1 11 Human 5.5 pKi = 5.5 Functional
Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).
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 -1 11 Human 5.5 pKi = 5.5 Functional
Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).
ChEMBL 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 10.1021/jm000007r
104766 6822 42 None -11 14 Human 4.4 pKi = 4.4 Functional
Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).
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 -11 14 Human 4.4 pKi = 4.4 Functional
Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).
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 -11 14 Human 4.4 pKi = 4.4 Functional
Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1021/jm000007r
1410 9054 48 None -1 8 Human 7.2 pKi = 7.2 Functional
Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).
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 7.2 pKi = 7.2 Functional
Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).
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 7.2 pKi = 7.2 Functional
Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).
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 7.2 pKi = 7.2 Functional
Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).
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 7.2 pKi = 7.2 Functional
Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm000007r
10058694 213382 1 None - 0 Human 5.1 pKi = 5.1 Functional
Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).
ChEMBL 203 2 3 4 -0.8 N[C@@]1(C(=O)O)CSC2C1[C@H]2C(=O)O 10.1021/jm000007r
CHEMBL88999 213382 1 None - 0 Human 5.1 pKi = 5.1 Functional
Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).
ChEMBL 203 2 3 4 -0.8 N[C@@]1(C(=O)O)CSC2C1[C@H]2C(=O)O 10.1021/jm000007r
1310 9095 110 None -27 17 Human 5.0 pKi = 5.0 Functional
Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm000007r
1369 9095 110 None -27 17 Human 5.0 pKi = 5.0 Functional
Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm000007r
33032 9095 110 None -27 17 Human 5.0 pKi = 5.0 Functional
Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm000007r
44272391 9095 110 None -27 17 Human 5.0 pKi = 5.0 Functional
Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm000007r
88747398 9095 110 None -27 17 Human 5.0 pKi = 5.0 Functional
Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm000007r
CHEMBL575060 9095 110 None -27 17 Human 5.0 pKi = 5.0 Functional
Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm000007r
DB00142 9095 110 None -27 17 Human 5.0 pKi = 5.0 Functional
Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm000007r
1310 9095 110 None -2 17 Mouse 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
1369 9095 110 None -2 17 Mouse 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
33032 9095 110 None -2 17 Mouse 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
44272391 9095 110 None -2 17 Mouse 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
88747398 9095 110 None -2 17 Mouse 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
CHEMBL575060 9095 110 None -2 17 Mouse 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
DB00142 9095 110 None -2 17 Mouse 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
1310 9095 110 None -27 17 Human 5.3 pEC50 = 5.3 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 -27 17 Human 5.3 pEC50 = 5.3 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 -27 17 Human 5.3 pEC50 = 5.3 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 -27 17 Human 5.3 pEC50 = 5.3 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 -27 17 Human 5.3 pEC50 = 5.3 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 -27 17 Human 5.3 pEC50 = 5.3 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 -27 17 Human 5.3 pEC50 = 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
6216 7323 0 None 2 2 Human 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 391 7 1 2 5.8 CCC(c1ccc(cc1)NC(=O)CSCc1ccc(cc1)Br)C 20385173
73755190 7323 0 None 2 2 Human 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 391 7 1 2 5.8 CCC(c1ccc(cc1)NC(=O)CSCc1ccc(cc1)Br)C 20385173
1407 8860 42 None -1 7 Human 7.5 pEC50 = 7.5 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 -1 7 Human 7.5 pEC50 = 7.5 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 -1 7 Human 7.5 pEC50 = 7.5 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
104766 6822 42 None -14 14 Rat 4.3 pEC50 None 4.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 9016353
1365 6822 42 None -14 14 Rat 4.3 pEC50 None 4.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 9016353
CHEMBL34453 6822 42 None -14 14 Rat 4.3 pEC50 None 4.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 9016353
104766 6822 42 None -11 14 Human 4.4 pEC50 None 4.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 9473604
1365 6822 42 None -11 14 Human 4.4 pEC50 None 4.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 9473604
CHEMBL34453 6822 42 None -11 14 Human 4.4 pEC50 None 4.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 9473604
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 10771029
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 10771029
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 10771029
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 10771029
1393 8321 64 None -1047 6 Human 5.1 pEC50 None 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10216218
1396 8321 64 None -1047 6 Human 5.1 pEC50 None 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10216218
213056 8321 64 None -1047 6 Human 5.1 pEC50 None 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10216218
CHEMBL8759 8321 64 None -1047 6 Human 5.1 pEC50 None 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 2 3 3 -0.5 OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O 10216218
1443 8100 36 None -24 5 Human 5.5 pEC50 None 5.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@@H](CCP(=O)(O)O)N 9473604
1550579 8100 36 None -24 5 Human 5.5 pEC50 None 5.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@@H](CCP(=O)(O)O)N 9473604
CHEMBL1319383 8100 36 None -24 5 Human 5.5 pEC50 None 5.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@@H](CCP(=O)(O)O)N 9473604
1410 9054 48 None 1 8 Rat 6.2 pEC50 None 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 9016353
1412 9054 48 None 1 8 Rat 6.2 pEC50 None 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 9016353
179394 9054 48 None 1 8 Rat 6.2 pEC50 None 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 9016353
57689795 9054 48 None 1 8 Rat 6.2 pEC50 None 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 9016353
CHEMBL33567 9054 48 None 1 8 Rat 6.2 pEC50 None 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 9016353
1368 9070 37 None -1 11 Rat 6.2 pEC50 None 6.2 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 9016353
5310956 9070 37 None -1 11 Rat 6.2 pEC50 None 6.2 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 9016353
CHEMBL280563 9070 37 None -1 11 Rat 6.2 pEC50 None 6.2 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 9016353
1406 8854 38 None 1 7 Human 6.7 pEC50 None 6.7 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 1 7 Human 6.7 pEC50 None 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10866390
1406 8854 38 None 1 7 Human 6.7 pEC50 None 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 11166323
4545574 8854 38 None 1 7 Human 6.7 pEC50 None 6.7 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 1 7 Human 6.7 pEC50 None 6.7 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 1 7 Human 6.7 pEC50 None 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 11166323
CHEMBL277475 8854 38 None 1 7 Human 6.7 pEC50 None 6.7 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 1 7 Human 6.7 pEC50 None 6.7 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 1 7 Human 6.7 pEC50 None 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 11166323
1310 9095 110 None -27 17 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
1369 9095 110 None -27 17 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
33032 9095 110 None -27 17 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
44272391 9095 110 None -27 17 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
88747398 9095 110 None -27 17 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
CHEMBL575060 9095 110 None -27 17 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
DB00142 9095 110 None -27 17 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
1411 9140 66 None 1 6 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
4120 9140 66 None 1 6 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
57689797 9140 66 None 1 6 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
68841 9140 66 None 1 6 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
CHEMBL284377 9140 66 None 1 6 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
DB04522 9140 66 None 1 6 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
1415 9392 41 None 10 2 Human 4.3 pIC50 = 4.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 245 3 4 3 -0.3 OC(=O)C(c1ccc(cc1)P(=O)(O)O)(N)C 9473604
3972752 9392 41 None 10 2 Human 4.3 pIC50 = 4.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 245 3 4 3 -0.3 OC(=O)C(c1ccc(cc1)P(=O)(O)O)(N)C 9473604
CHEMBL86508 9392 41 None 10 2 Human 4.3 pIC50 = 4.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 245 3 4 3 -0.3 OC(=O)C(c1ccc(cc1)P(=O)(O)O)(N)C 9473604
1411 9140 66 None 1 6 Human 6.7 pIC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 10216218
1411 9140 66 None 1 6 Human 6.7 pIC50 = 6.7 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 1 6 Human 6.7 pIC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 10216218
4120 9140 66 None 1 6 Human 6.7 pIC50 = 6.7 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 1 6 Human 6.7 pIC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 10216218
57689797 9140 66 None 1 6 Human 6.7 pIC50 = 6.7 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 1 6 Human 6.7 pIC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 10216218
68841 9140 66 None 1 6 Human 6.7 pIC50 = 6.7 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 1 6 Human 6.7 pIC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 10216218
CHEMBL284377 9140 66 None 1 6 Human 6.7 pIC50 = 6.7 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 1 6 Human 6.7 pIC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 10216218
DB04522 9140 66 None 1 6 Human 6.7 pIC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 9473604
1410 9054 48 None -1 8 Human 7.1 pIC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10216218
1412 9054 48 None -1 8 Human 7.1 pIC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10216218
179394 9054 48 None -1 8 Human 7.1 pIC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10216218
57689795 9054 48 None -1 8 Human 7.1 pIC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10216218
CHEMBL33567 9054 48 None -1 8 Human 7.1 pIC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10216218
1398 7153 0 None 15 2 Rat 5.3 pIC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 199 4 4 4 -1.1 OC(=O)C(COP(=O)(O)O)(N)C 12769621
3964633 7153 0 None 15 2 Rat 5.3 pIC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 199 4 4 4 -1.1 OC(=O)C(COP(=O)(O)O)(N)C 12769621
CHEMBL1437137 7153 0 None 15 2 Rat 5.3 pIC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 199 4 4 4 -1.1 OC(=O)C(COP(=O)(O)O)(N)C 12769621
1310 9095 110 None -27 17 Human 5.4 pIC50 None 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10216218
1310 9095 110 None -27 17 Human 5.4 pIC50 None 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9473604
1369 9095 110 None -27 17 Human 5.4 pIC50 None 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10216218
1369 9095 110 None -27 17 Human 5.4 pIC50 None 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9473604
33032 9095 110 None -27 17 Human 5.4 pIC50 None 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10216218
33032 9095 110 None -27 17 Human 5.4 pIC50 None 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9473604
44272391 9095 110 None -27 17 Human 5.4 pIC50 None 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10216218
44272391 9095 110 None -27 17 Human 5.4 pIC50 None 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9473604
88747398 9095 110 None -27 17 Human 5.4 pIC50 None 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10216218
88747398 9095 110 None -27 17 Human 5.4 pIC50 None 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9473604
CHEMBL575060 9095 110 None -27 17 Human 5.4 pIC50 None 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10216218
CHEMBL575060 9095 110 None -27 17 Human 5.4 pIC50 None 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9473604
DB00142 9095 110 None -27 17 Human 5.4 pIC50 None 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10216218
DB00142 9095 110 None -27 17 Human 5.4 pIC50 None 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 9473604
1377 8122 26 None -19 8 Human 5.5 pIC50 None 5.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 203 4 4 4 -1.6 N[C@@H](C1[C@H]([C@@H]1C(=O)O)C(=O)O)C(=O)O 10216218
5310979 8122 26 None -19 8 Human 5.5 pIC50 None 5.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 203 4 4 4 -1.6 N[C@@H](C1[C@H]([C@@H]1C(=O)O)C(=O)O)C(=O)O 10216218
CHEMBL284193 8122 26 None -19 8 Human 5.5 pIC50 None 5.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 203 4 4 4 -1.6 N[C@@H](C1[C@H]([C@@H]1C(=O)O)C(=O)O)C(=O)O 10216218
1368 9070 37 None -1 11 Human 6.2 pIC50 None 6.2 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 10216218
5310956 9070 37 None -1 11 Human 6.2 pIC50 None 6.2 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 10216218
CHEMBL280563 9070 37 None -1 11 Human 6.2 pIC50 None 6.2 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 10216218
1414 9237 0 None 707 2 Rat 6.4 pIC50 None 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 197 4 4 3 -0.6 OC(=O)[C@](CCP(=O)(O)O)(N)C 10719229
1414 9237 0 None 707 2 Rat 6.4 pIC50 None 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 197 4 4 3 -0.6 OC(=O)[C@](CCP(=O)(O)O)(N)C 9016353
1795545 9237 0 None 707 2 Rat 6.4 pIC50 None 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 197 4 4 3 -0.6 OC(=O)[C@](CCP(=O)(O)O)(N)C 10719229
1795545 9237 0 None 707 2 Rat 6.4 pIC50 None 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 197 4 4 3 -0.6 OC(=O)[C@](CCP(=O)(O)O)(N)C 9016353
CHEMBL1488784 9237 0 None 707 2 Rat 6.4 pIC50 None 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 197 4 4 3 -0.6 OC(=O)[C@](CCP(=O)(O)O)(N)C 10719229
CHEMBL1488784 9237 0 None 707 2 Rat 6.4 pIC50 None 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 197 4 4 3 -0.6 OC(=O)[C@](CCP(=O)(O)O)(N)C 9016353
1378 9195 54 None -21 14 Human 6.8 pIC50 None 6.8 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 9680254
1399 9195 54 None -21 14 Human 6.8 pIC50 None 6.8 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 9680254
9819927 9195 54 None -21 14 Human 6.8 pIC50 None 6.8 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 9680254
CHEMBL432038 9195 54 None -21 14 Human 6.8 pIC50 None 6.8 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 9680254
10238 10799 26 None -3 5 Human 5.0 pKB = 5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 436 7 1 6 4.8 COC(=O)c1ccc(cc1)n1c(C)cc(c1C)C(=O)CSc1ccc(cc1)NC(=O)C 25225882
4043841 10799 26 None -3 5 Human 5.0 pKB = 5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 436 7 1 6 4.8 COC(=O)c1ccc(cc1)n1c(C)cc(c1C)C(=O)CSc1ccc(cc1)NC(=O)C 25225882
CHEMBL1585091 10799 26 None -3 5 Human 5.0 pKB = 5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 436 7 1 6 4.8 COC(=O)c1ccc(cc1)n1c(C)cc(c1C)C(=O)CSc1ccc(cc1)NC(=O)C 25225882
6216 7323 0 None 2 2 Human 5.4 pKB = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 391 7 1 2 5.8 CCC(c1ccc(cc1)NC(=O)CSCc1ccc(cc1)Br)C 29514854
73755190 7323 0 None 2 2 Human 5.4 pKB = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 391 7 1 2 5.8 CCC(c1ccc(cc1)NC(=O)CSCc1ccc(cc1)Br)C 29514854
10239 10815 29 None -1 5 Human 6.7 pKB = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 359 4 1 4 4.8 Clc1ccc(nc1)Oc1ccc(cc1Cl)NC(=O)c1ccccn1 25225882
73058507 10815 29 None -1 5 Human 6.7 pKB = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 359 4 1 4 4.8 Clc1ccc(nc1)Oc1ccc(cc1Cl)NC(=O)c1ccccn1 25225882
CHEMBL4162576 10815 29 None -1 5 Human 6.7 pKB = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 359 4 1 4 4.8 Clc1ccc(nc1)Oc1ccc(cc1Cl)NC(=O)c1ccccn1 25225882




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DOI

139119037 96837 2 None - 0 Human 4.9 pEC50 = 4.9 Binding
Agonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 203 2 3 3 -0.5 N[C@@]1(C(=O)O)C[C@@H](F)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm4000165
15479143 96837 2 None - 0 Human 4.9 pEC50 = 4.9 Binding
Agonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 203 2 3 3 -0.5 N[C@@]1(C(=O)O)C[C@@H](F)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm4000165
CHEMBL2381652 96837 2 None - 0 Human 4.9 pEC50 = 4.9 Binding
Agonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 203 2 3 3 -0.5 N[C@@]1(C(=O)O)C[C@@H](F)[C@H]2[C@H](C(=O)O)[C@H]21 10.1021/jm4000165
46836872 7088 47 None - 1 Human 5.9 pEC50 = 5.9 Binding
Positive allosteric modulation of mGluR8 (unknown origin)Positive allosteric modulation of mGluR8 (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 5.9 pEC50 = 5.9 Binding
Positive allosteric modulation of mGluR8 (unknown origin)Positive allosteric modulation of mGluR8 (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 5.9 pEC50 = 5.9 Binding
Positive allosteric modulation of mGluR8 (unknown origin)Positive allosteric modulation of mGluR8 (unknown origin)
ChEMBL 272 3 2 6 2.7 Cc1ccnc(n1)Nc1sc(c(n1)c1c[nH]nc1)C 10.1016/j.bmcl.2022.129106
71681825 96830 0 None - 0 Human 4.9 pEC50 = 4.9 Binding
Agonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 226 3 3 4 -0.2 [N-]=[N+]=N[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/jm4000165
CHEMBL2381645 96830 0 None - 0 Human 4.9 pEC50 = 4.9 Binding
Agonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 226 3 3 4 -0.2 [N-]=[N+]=N[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/jm4000165
71681823 96829 0 None - 0 Human 4.9 pEC50 = 4.9 Binding
Agonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 226 3 3 4 -0.2 [N-]=[N+]=N[C@@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@@H]21 10.1021/jm4000165
CHEMBL2381644 96829 0 None - 0 Human 4.9 pEC50 = 4.9 Binding
Agonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 226 3 3 4 -0.2 [N-]=[N+]=N[C@@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@@H]21 10.1021/jm4000165
10239 10815 29 None - 0 Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of mGluR8 (unknown origin)Positive allosteric modulation of mGluR8 (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 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of mGluR8 (unknown origin)Positive allosteric modulation of mGluR8 (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 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of mGluR8 (unknown origin)Positive allosteric modulation of mGluR8 (unknown origin)
ChEMBL 359 4 1 4 4.8 Clc1ccc(nc1)Oc1ccc(cc1Cl)NC(=O)c1ccccn1 10.1016/j.bmcl.2022.129106
70051926 96826 2 None - 0 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 197 2 3 3 -0.3 C=C1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/jm4000165
CHEMBL2381641 96826 2 None - 0 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 197 2 3 3 -0.3 C=C1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/jm4000165
1310 9095 110 None - 18 Mouse 7.7 pEC50 = 7.7 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR8 in mouseConcentration for half maximal activation of metabotropic glutamate mGluR8 in mouse
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
1369 9095 110 None - 18 Mouse 7.7 pEC50 = 7.7 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR8 in mouseConcentration for half maximal activation of metabotropic glutamate mGluR8 in mouse
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
33032 9095 110 None - 18 Mouse 7.7 pEC50 = 7.7 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR8 in mouseConcentration for half maximal activation of metabotropic glutamate mGluR8 in mouse
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
44272391 9095 110 None - 18 Mouse 7.7 pEC50 = 7.7 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR8 in mouseConcentration for half maximal activation of metabotropic glutamate mGluR8 in mouse
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
88747398 9095 110 None - 18 Mouse 7.7 pEC50 = 7.7 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR8 in mouseConcentration for half maximal activation of metabotropic glutamate mGluR8 in mouse
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
CHEMBL575060 9095 110 None - 18 Mouse 7.7 pEC50 = 7.7 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR8 in mouseConcentration for half maximal activation of metabotropic glutamate mGluR8 in mouse
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
DB00142 9095 110 None - 18 Mouse 7.7 pEC50 = 7.7 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR8 in mouseConcentration for half maximal activation of metabotropic glutamate mGluR8 in mouse
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
131954513 168857 38 None - 1 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at mGlu8 (unknown origin)Agonist activity at mGlu8 (unknown origin)
ChEMBL 357 2 0 4 4.3 COc1ccc(-c2c(C)nn3c(C(F)(F)F)cc(C)nc23)c(F)c1F 10.1039/C8MD00524A
CHEMBL4160748 168857 38 None - 1 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at mGlu8 (unknown origin)Agonist activity at mGlu8 (unknown origin)
ChEMBL 357 2 0 4 4.3 COc1ccc(-c2c(C)nn3c(C(F)(F)F)cc(C)nc23)c(F)c1F 10.1039/C8MD00524A
131954513 168857 38 None - 1 Human 5.6 pEC50 = 5.6 Binding
Positive allosteric modulation of mGluR8 (unknown origin)Positive allosteric modulation of mGluR8 (unknown origin)
ChEMBL 357 2 0 4 4.3 COc1ccc(-c2c(C)nn3c(C(F)(F)F)cc(C)nc23)c(F)c1F 10.1016/j.bmcl.2022.129106
CHEMBL4160748 168857 38 None - 1 Human 5.6 pEC50 = 5.6 Binding
Positive allosteric modulation of mGluR8 (unknown origin)Positive allosteric modulation of mGluR8 (unknown origin)
ChEMBL 357 2 0 4 4.3 COc1ccc(-c2c(C)nn3c(C(F)(F)F)cc(C)nc23)c(F)c1F 10.1016/j.bmcl.2022.129106
145955288 169356 0 None - 0 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at mGlu8 (unknown origin)Agonist activity at mGlu8 (unknown origin)
ChEMBL 357 2 0 4 4.3 COc1cc(F)c(-c2c(C)nn3c(C(F)(F)F)cc(C)nc23)c(F)c1 10.1039/C8MD00524A
CHEMBL4168668 169356 0 None - 0 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at mGlu8 (unknown origin)Agonist activity at mGlu8 (unknown origin)
ChEMBL 357 2 0 4 4.3 COc1cc(F)c(-c2c(C)nn3c(C(F)(F)F)cc(C)nc23)c(F)c1 10.1039/C8MD00524A
1407 8860 42 None - 0 Human 7.5 pEC50 = 7.5 Binding
Activation of human metabotropic glutamate 8 receptor expressed in golden hamster AV12-664 cellsActivation of human metabotropic glutamate 8 receptor expressed in golden hamster AV12-664 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/acs.jmedchem.8b01120
16062593 8860 42 None - 0 Human 7.5 pEC50 = 7.5 Binding
Activation of human metabotropic glutamate 8 receptor expressed in golden hamster AV12-664 cellsActivation of human metabotropic glutamate 8 receptor expressed in golden hamster AV12-664 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/acs.jmedchem.8b01120
CHEMBL143210 8860 42 None - 0 Human 7.5 pEC50 = 7.5 Binding
Activation of human metabotropic glutamate 8 receptor expressed in golden hamster AV12-664 cellsActivation of human metabotropic glutamate 8 receptor expressed in golden hamster AV12-664 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/acs.jmedchem.8b01120
1410 9054 48 None - 6 Mouse 6.4 pEC50 = 6.4 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR8 in mouseConcentration for half maximal activation of metabotropic glutamate mGluR8 in mouse
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm00009a001
1412 9054 48 None - 6 Mouse 6.4 pEC50 = 6.4 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR8 in mouseConcentration for half maximal activation of metabotropic glutamate mGluR8 in mouse
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm00009a001
179394 9054 48 None - 6 Mouse 6.4 pEC50 = 6.4 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR8 in mouseConcentration for half maximal activation of metabotropic glutamate mGluR8 in mouse
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm00009a001
57689795 9054 48 None - 6 Mouse 6.4 pEC50 = 6.4 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR8 in mouseConcentration for half maximal activation of metabotropic glutamate mGluR8 in mouse
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm00009a001
CHEMBL33567 9054 48 None - 6 Mouse 6.4 pEC50 = 6.4 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR8 in mouseConcentration for half maximal activation of metabotropic glutamate mGluR8 in mouse
ChEMBL 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10.1021/jm00009a001
60096211 96834 0 None - 2 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 242 3 4 4 -1.4 CC(=O)N[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/jm4000165
CHEMBL2381649 96834 0 None - 2 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 242 3 4 4 -1.4 CC(=O)N[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12 10.1021/jm4000165
1410 9054 48 None 2 6 Human 7.2 pEC50 = 7.2 Binding
Activation of human metabotropic glutamate 8 receptor expressed in golden hamster AV12-664 cellsActivation of human metabotropic glutamate 8 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 2 6 Human 7.2 pEC50 = 7.2 Binding
Activation of human metabotropic glutamate 8 receptor expressed in golden hamster AV12-664 cellsActivation of human metabotropic glutamate 8 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 2 6 Human 7.2 pEC50 = 7.2 Binding
Activation of human metabotropic glutamate 8 receptor expressed in golden hamster AV12-664 cellsActivation of human metabotropic glutamate 8 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 2 6 Human 7.2 pEC50 = 7.2 Binding
Activation of human metabotropic glutamate 8 receptor expressed in golden hamster AV12-664 cellsActivation of human metabotropic glutamate 8 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 2 6 Human 7.2 pEC50 = 7.2 Binding
Activation of human metabotropic glutamate 8 receptor expressed in golden hamster AV12-664 cellsActivation of human metabotropic glutamate 8 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
9794208 96825 4 None - 0 Human 5.2 pEC50 = 5.2 Binding
Agonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 199 2 3 4 -1.3 N[C@@]1(C(=O)O)CC(=O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/jm4000165
CHEMBL2381640 96825 4 None - 0 Human 5.2 pEC50 = 5.2 Binding
Agonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay
ChEMBL 199 2 3 4 -1.3 N[C@@]1(C(=O)O)CC(=O)[C@@H]2[C@H]1[C@H]2C(=O)O 10.1021/jm4000165
155518354 177044 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at mGlu8 (unknown origin)Agonist activity at mGlu8 (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 6.1 pEC50 = 6.1 Binding
Agonist activity at mGlu8 (unknown origin)Agonist activity at mGlu8 (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
10238 10799 26 None - 0 Human 6.1 pEC50 = 6.1 Binding
Positive allosteric modulation of mGluR8 (unknown origin)Positive allosteric modulation of mGluR8 (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 6.1 pEC50 = 6.1 Binding
Positive allosteric modulation of mGluR8 (unknown origin)Positive allosteric modulation of mGluR8 (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 6.1 pEC50 = 6.1 Binding
Positive allosteric modulation of mGluR8 (unknown origin)Positive allosteric modulation of mGluR8 (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
2207 106641 63 None 1 7 Human 8.3 pIC50 = 8.3 Binding
Inhibitory concentration against [3H]1 binding to recombinant human Metabotropic glutamate receptor 8Inhibitory concentration against [3H]1 binding to recombinant human Metabotropic glutamate receptor 8
ChEMBL 183 4 4 3 -1.0 NC(CCP(=O)(O)O)C(=O)O 10.1016/j.bmcl.2004.10.093
CHEMBL285843 106641 63 None 1 7 Human 8.3 pIC50 = 8.3 Binding
Inhibitory concentration against [3H]1 binding to recombinant human Metabotropic glutamate receptor 8Inhibitory concentration against [3H]1 binding to recombinant human Metabotropic glutamate receptor 8
ChEMBL 183 4 4 3 -1.0 NC(CCP(=O)(O)O)C(=O)O 10.1016/j.bmcl.2004.10.093
1310 9095 110 None -1 18 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against [3H]1 binding to recombinant human Metabotropic glutamate receptor 8Inhibitory concentration against [3H]1 binding to recombinant human Metabotropic glutamate receptor 8
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2004.10.093
1369 9095 110 None -1 18 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against [3H]1 binding to recombinant human Metabotropic glutamate receptor 8Inhibitory concentration against [3H]1 binding to recombinant human Metabotropic glutamate receptor 8
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2004.10.093
33032 9095 110 None -1 18 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against [3H]1 binding to recombinant human Metabotropic glutamate receptor 8Inhibitory concentration against [3H]1 binding to recombinant human Metabotropic glutamate receptor 8
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2004.10.093
44272391 9095 110 None -1 18 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against [3H]1 binding to recombinant human Metabotropic glutamate receptor 8Inhibitory concentration against [3H]1 binding to recombinant human Metabotropic glutamate receptor 8
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2004.10.093
88747398 9095 110 None -1 18 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against [3H]1 binding to recombinant human Metabotropic glutamate receptor 8Inhibitory concentration against [3H]1 binding to recombinant human Metabotropic glutamate receptor 8
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2004.10.093
CHEMBL575060 9095 110 None -1 18 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against [3H]1 binding to recombinant human Metabotropic glutamate receptor 8Inhibitory concentration against [3H]1 binding to recombinant human Metabotropic glutamate receptor 8
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2004.10.093
DB00142 9095 110 None -1 18 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against [3H]1 binding to recombinant human Metabotropic glutamate receptor 8Inhibitory concentration against [3H]1 binding to recombinant human Metabotropic glutamate receptor 8
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2004.10.093
135544097 162444 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Displacement of [3H]-L-AP4 from rat mGluR8Displacement of [3H]-L-AP4 from rat mGluR8
ChEMBL 437 2 2 6 4.0 O=C1CC(c2cccc(-n3ccnn3)c2)=Nc2cc(O)c(C#Cc3ccc(F)cc3)cc2N1 10.1016/j.bmcl.2007.12.005
CHEMBL404886 162444 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Displacement of [3H]-L-AP4 from rat mGluR8Displacement of [3H]-L-AP4 from rat mGluR8
ChEMBL 437 2 2 6 4.0 O=C1CC(c2cccc(-n3ccnn3)c2)=Nc2cc(O)c(C#Cc3ccc(F)cc3)cc2N1 10.1016/j.bmcl.2007.12.005
44389027 70886 0 None - 1 Human 8.2 pKd = 8.2 Binding
Dissociation constant of radiolabeled compound against recombinant human Metabotropic glutamate receptor 8Dissociation constant of radiolabeled compound against recombinant human Metabotropic glutamate receptor 8
ChEMBL 189 4 4 4 -1.7 N[C@H](C(=O)O)[C@@H]1C(C(=O)O)[C@@H]1CO 10.1016/j.bmcl.2004.10.093
CHEMBL180822 70886 0 None - 1 Human 8.2 pKd = 8.2 Binding
Dissociation constant of radiolabeled compound against recombinant human Metabotropic glutamate receptor 8Dissociation constant of radiolabeled compound against recombinant human Metabotropic glutamate receptor 8
ChEMBL 189 4 4 4 -1.7 N[C@H](C(=O)O)[C@@H]1C(C(=O)O)[C@@H]1CO 10.1016/j.bmcl.2004.10.093
1410 9054 48 None -16 6 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]LY341495 from rat mGluR8 expressed in BHK cellsDisplacement of [3H]LY341495 from rat mGluR8 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 -16 6 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]LY341495 from rat mGluR8 expressed in BHK cellsDisplacement of [3H]LY341495 from rat mGluR8 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 -16 6 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]LY341495 from rat mGluR8 expressed in BHK cellsDisplacement of [3H]LY341495 from rat mGluR8 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 -16 6 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]LY341495 from rat mGluR8 expressed in BHK cellsDisplacement of [3H]LY341495 from rat mGluR8 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 -16 6 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]LY341495 from rat mGluR8 expressed in BHK cellsDisplacement of [3H]LY341495 from rat mGluR8 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 -16 6 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]LY341495 from rat recombinant mGluR8 expressed in BHK cells by SPA assayDisplacement of [3H]LY341495 from rat recombinant mGluR8 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 -16 6 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]LY341495 from rat recombinant mGluR8 expressed in BHK cells by SPA assayDisplacement of [3H]LY341495 from rat recombinant mGluR8 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 -16 6 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]LY341495 from rat recombinant mGluR8 expressed in BHK cells by SPA assayDisplacement of [3H]LY341495 from rat recombinant mGluR8 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 -16 6 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]LY341495 from rat recombinant mGluR8 expressed in BHK cells by SPA assayDisplacement of [3H]LY341495 from rat recombinant mGluR8 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 -16 6 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]LY341495 from rat recombinant mGluR8 expressed in BHK cells by SPA assayDisplacement of [3H]LY341495 from rat recombinant mGluR8 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
1310 9095 110 None -2 18 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]LY341495 from rat mGluR8 expressed in BHK cellsDisplacement of [3H]LY341495 from rat mGluR8 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 -2 18 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]LY341495 from rat mGluR8 expressed in BHK cellsDisplacement of [3H]LY341495 from rat mGluR8 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 -2 18 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]LY341495 from rat mGluR8 expressed in BHK cellsDisplacement of [3H]LY341495 from rat mGluR8 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 -2 18 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]LY341495 from rat mGluR8 expressed in BHK cellsDisplacement of [3H]LY341495 from rat mGluR8 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 -2 18 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]LY341495 from rat mGluR8 expressed in BHK cellsDisplacement of [3H]LY341495 from rat mGluR8 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 -2 18 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]LY341495 from rat mGluR8 expressed in BHK cellsDisplacement of [3H]LY341495 from rat mGluR8 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 -2 18 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]LY341495 from rat mGluR8 expressed in BHK cellsDisplacement of [3H]LY341495 from rat mGluR8 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 -2 18 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]LY341495 from rat recombinant mGluR8 expressed in BHK cells by SPA assayDisplacement of [3H]LY341495 from rat recombinant mGluR8 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 -2 18 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]LY341495 from rat recombinant mGluR8 expressed in BHK cells by SPA assayDisplacement of [3H]LY341495 from rat recombinant mGluR8 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 -2 18 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]LY341495 from rat recombinant mGluR8 expressed in BHK cells by SPA assayDisplacement of [3H]LY341495 from rat recombinant mGluR8 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 -2 18 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]LY341495 from rat recombinant mGluR8 expressed in BHK cells by SPA assayDisplacement of [3H]LY341495 from rat recombinant mGluR8 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 -2 18 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]LY341495 from rat recombinant mGluR8 expressed in BHK cells by SPA assayDisplacement of [3H]LY341495 from rat recombinant mGluR8 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 -2 18 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]LY341495 from rat recombinant mGluR8 expressed in BHK cells by SPA assayDisplacement of [3H]LY341495 from rat recombinant mGluR8 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 -2 18 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]LY341495 from rat recombinant mGluR8 expressed in BHK cells by SPA assayDisplacement of [3H]LY341495 from rat recombinant mGluR8 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
44406221 79451 1 None -1 2 Rat 4.3 pKi = 4.3 Binding
Displacement of [3H]LY341495 from rat mGluR8 expressed in BHK cellsDisplacement of [3H]LY341495 from rat mGluR8 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]LY341495 from rat mGluR8 expressed in BHK cellsDisplacement of [3H]LY341495 from rat mGluR8 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
44406220 78948 1 None -8 2 Rat 4.2 pKi = 4.2 Binding
Displacement of [3H]LY341495 from rat mGluR8 expressed in BHK cellsDisplacement of [3H]LY341495 from rat mGluR8 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 4.2 pKi = 4.2 Binding
Displacement of [3H]LY341495 from rat mGluR8 expressed in BHK cellsDisplacement of [3H]LY341495 from rat mGluR8 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 4.2 pKi = 4.2 Binding
Displacement of [3H]LY341495 from rat recombinant mGluR8 expressed in BHK cells by SPA assayDisplacement of [3H]LY341495 from rat recombinant mGluR8 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 4.2 pKi = 4.2 Binding
Displacement of [3H]LY341495 from rat recombinant mGluR8 expressed in BHK cells by SPA assayDisplacement of [3H]LY341495 from rat recombinant mGluR8 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 Human 6.7 pKd None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10216218
1412 9054 48 None 2 6 Human 6.7 pKd None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10216218
179394 9054 48 None 2 6 Human 6.7 pKd None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10216218
57689795 9054 48 None 2 6 Human 6.7 pKd None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10216218
CHEMBL33567 9054 48 None 2 6 Human 6.7 pKd None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 10216218
1310 9095 110 3H-CPPG -2 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 3H-CPPG -2 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 3H-CPPG -2 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 3H-CPPG -2 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 3H-CPPG -2 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 3H-CPPG -2 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 3H-CPPG -2 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
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
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
139054390 211702 106 3H-CPPG -1 5 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 N[C@H](CCC(=O)O)C(=O)O None
23327 211702 106 3H-CPPG -1 5 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 N[C@H](CCC(=O)O)C(=O)O None
CHEMBL76232 211702 106 3H-CPPG -1 5 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 N[C@H](CCC(=O)O)C(=O)O 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
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 223117 0 3H-CPPG 1 4 Rat 5.9 pKi = 5.9 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 -4 7 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 183 4 4 3 -1.0 NC(CCP(=O)(O)O)C(=O)O None
CHEMBL285843 106641 63 Functional -4 7 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 183 4 4 3 -1.0 NC(CCP(=O)(O)O)C(=O)O None
1413 7979 0 3H-CPPG 83 2 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 271 4 4 3 0.1 OC(=O)C(c1ccc(cc1)P(=O)(O)O)(C1CC1)N None
2878 7979 0 3H-CPPG 83 2 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 271 4 4 3 0.1 OC(=O)C(c1ccc(cc1)P(=O)(O)O)(C1CC1)N None
CHEMBL164642 7979 0 3H-CPPG 83 2 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 271 4 4 3 0.1 OC(=O)C(c1ccc(cc1)P(=O)(O)O)(C1CC1)N None
1310 9095 110 Functional -1 18 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
1369 9095 110 Functional -1 18 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
33032 9095 110 Functional -1 18 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
44272391 9095 110 Functional -1 18 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
88747398 9095 110 Functional -1 18 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
CHEMBL575060 9095 110 Functional -1 18 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
DB00142 9095 110 Functional -1 18 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
2207 106641 63 3H-CPPG -4 7 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 183 4 4 3 -1.0 NC(CCP(=O)(O)O)C(=O)O None
CHEMBL285843 106641 63 3H-CPPG -4 7 Rat 5.6 pKi = 5.6 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 Human 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 Human 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 -2 18 Rat 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
1369 9095 110 None -2 18 Rat 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
33032 9095 110 None -2 18 Rat 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
44272391 9095 110 None -2 18 Rat 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
88747398 9095 110 None -2 18 Rat 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
CHEMBL575060 9095 110 None -2 18 Rat 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
DB00142 9095 110 None -2 18 Rat 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
1413 7979 0 None 83 2 Rat 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 271 4 4 3 0.1 OC(=O)C(c1ccc(cc1)P(=O)(O)O)(C1CC1)N 10719229
2878 7979 0 None 83 2 Rat 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 271 4 4 3 0.1 OC(=O)C(c1ccc(cc1)P(=O)(O)O)(C1CC1)N 10719229
CHEMBL164642 7979 0 None 83 2 Rat 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 271 4 4 3 0.1 OC(=O)C(c1ccc(cc1)P(=O)(O)O)(C1CC1)N 10719229