Ligand source activities (1 row/activity)





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145422113 171011 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human mGlu7 expressed in CHO cells assessed as reduction in forskolin-induced cAMP productionAgonist activity at human mGlu7 expressed in CHO cells assessed as reduction in forskolin-induced cAMP production
ChEMBL 350 6 1 3 3.9 O=C(C[C@H](NCC1CC1)c1ccccc1)N1CCCOc2ccccc21 10.1039/C8MD00524A
CHEMBL4456545 171011 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human mGlu7 expressed in CHO cells assessed as reduction in forskolin-induced cAMP productionAgonist activity at human mGlu7 expressed in CHO cells assessed as reduction in forskolin-induced cAMP production
ChEMBL 350 6 1 3 3.9 O=C(C[C@H](NCC1CC1)c1ccccc1)N1CCCOc2ccccc21 10.1039/C8MD00524A
145952023 162782 0 None - 1 Rat 6.0 pEC50 = 6 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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)cc1F 10.1021/acsmedchemlett.7b00317
CHEMBL4172016 162782 0 None - 1 Rat 6.0 pEC50 = 6 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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)cc1F 10.1021/acsmedchemlett.7b00317
124425164 158015 0 None -41 4 Human 4.0 pEC50 = 4 Functional
Agonist activity at mGlu7 (unknown 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 mGlu7 (unknown 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 158015 0 None -41 4 Human 4.0 pEC50 = 4 Functional
Agonist activity at mGlu7 (unknown 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 mGlu7 (unknown 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
145952023 162782 0 None - 1 Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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)cc1F 10.1021/acsmedchemlett.7b00317
CHEMBL4172016 162782 0 None - 1 Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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)cc1F 10.1021/acsmedchemlett.7b00317
145952442 162733 0 None - 1 Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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 371 3 0 4 4.6 CCc1nn2c(C(F)(F)F)cc(C)nc2c1-c1ccc(OC)c(F)c1F 10.1021/acsmedchemlett.7b00317
CHEMBL4171274 162733 0 None - 1 Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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 371 3 0 4 4.6 CCc1nn2c(C(F)(F)F)cc(C)nc2c1-c1ccc(OC)c(F)c1F 10.1021/acsmedchemlett.7b00317
162654767 180572 0 None - 1 Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 362 3 0 5 3.6 COc1cccc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1021/acsmedchemlett.0c00432
CHEMBL4754102 180572 0 None - 1 Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 362 3 0 5 3.6 COc1cccc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1021/acsmedchemlett.0c00432
CHEMBL4776732 180572 0 None - 1 Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 362 3 0 5 3.6 COc1cccc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1021/acsmedchemlett.0c00432
145952442 162733 0 None - 1 Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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 371 3 0 4 4.6 CCc1nn2c(C(F)(F)F)cc(C)nc2c1-c1ccc(OC)c(F)c1F 10.1021/acsmedchemlett.7b00317
CHEMBL4171274 162733 0 None - 1 Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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 371 3 0 4 4.6 CCc1nn2c(C(F)(F)F)cc(C)nc2c1-c1ccc(OC)c(F)c1F 10.1021/acsmedchemlett.7b00317
162643634 181755 0 None -1 3 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human mGluR7 in presence of EC20 concentration of L-AP4 by calcium mobilization assayPositive allosteric modulation of human mGluR7 in presence of EC20 concentration of L-AP4 by calcium mobilization assay
ChEMBL 392 3 1 4 4.4 Cc1ccc2c(c1)C(=O)N(c1cc(C)c(NC(=O)c3occc3C)cc1F)C2=O 10.1016/j.bmcl.2020.127724
CHEMBL4777502 181755 0 None -1 3 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human mGluR7 in presence of EC20 concentration of L-AP4 by calcium mobilization assayPositive allosteric modulation of human mGluR7 in presence of EC20 concentration of L-AP4 by calcium mobilization assay
ChEMBL 392 3 1 4 4.4 Cc1ccc2c(c1)C(=O)N(c1cc(C)c(NC(=O)c3occc3C)cc1F)C2=O 10.1016/j.bmcl.2020.127724
155547657 173711 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Allosteric agonist activity at human mGlu7 expressed in CHO cells assessed as reduction in forskolin-induced cAMP production after 30 mins by cAMP reagent-based assayAllosteric agonist activity at human mGlu7 expressed in CHO cells assessed as reduction in forskolin-induced cAMP production after 30 mins by cAMP reagent-based assay
ChEMBL 337 7 2 3 2.9 CNCC[C@H](NCC(=O)N1CCCc2ccccc21)c1ccccc1 10.1039/C8MD00524A
CHEMBL4535940 173711 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Allosteric agonist activity at human mGlu7 expressed in CHO cells assessed as reduction in forskolin-induced cAMP production after 30 mins by cAMP reagent-based assayAllosteric agonist activity at human mGlu7 expressed in CHO cells assessed as reduction in forskolin-induced cAMP production after 30 mins by cAMP reagent-based assay
ChEMBL 337 7 2 3 2.9 CNCC[C@H](NCC(=O)N1CCCc2ccccc21)c1ccccc1 10.1039/C8MD00524A
162647803 179780 0 None - 1 Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 418 4 0 6 3.7 N#Cc1cnc2c(OC3CCOC3)cccc2c1N1CCN(c2ccccc2F)CC1 10.1021/acsmedchemlett.0c00432
CHEMBL4744634 179780 0 None - 1 Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 418 4 0 6 3.7 N#Cc1cnc2c(OC3CCOC3)cccc2c1N1CCN(c2ccccc2F)CC1 10.1021/acsmedchemlett.0c00432
162652580 180463 0 None - 1 Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 398 3 0 5 3.9 COc1c(F)c(F)cc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1021/acsmedchemlett.0c00432
CHEMBL4752850 180463 0 None - 1 Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 398 3 0 5 3.9 COc1c(F)c(F)cc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1021/acsmedchemlett.0c00432
162654767 180572 0 None - 1 Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 362 3 0 5 3.6 COc1cccc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1021/acsmedchemlett.0c00432
CHEMBL4754102 180572 0 None - 1 Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 362 3 0 5 3.6 COc1cccc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1021/acsmedchemlett.0c00432
CHEMBL4776732 180572 0 None - 1 Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 362 3 0 5 3.6 COc1cccc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1021/acsmedchemlett.0c00432
162663930 182101 0 None 1 2 Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 380 3 0 5 3.7 COc1cc(F)cc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1021/acsmedchemlett.0c00432
CHEMBL4761695 182101 0 None 1 2 Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 380 3 0 5 3.7 COc1cc(F)cc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1021/acsmedchemlett.0c00432
CHEMBL4781814 182101 0 None 1 2 Rat 6.0 pEC50 = 6.0 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 380 3 0 5 3.7 COc1cc(F)cc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1021/acsmedchemlett.0c00432
122197954 159935 0 None -42 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 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 159935 0 None -42 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 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
162661457 181434 0 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human mGluR7 in presence of EC20 concentration of L-AP4 by calcium mobilization assayPositive allosteric modulation of human mGluR7 in presence of EC20 concentration of L-AP4 by calcium mobilization assay
ChEMBL 396 3 1 4 4.2 Cc1cc(N2C(=O)c3cccc(F)c3C2=O)c(F)cc1NC(=O)c1occc1C 10.1016/j.bmcl.2020.127724
CHEMBL4764083 181434 0 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human mGluR7 in presence of EC20 concentration of L-AP4 by calcium mobilization assayPositive allosteric modulation of human mGluR7 in presence of EC20 concentration of L-AP4 by calcium mobilization assay
ChEMBL 396 3 1 4 4.2 Cc1cc(N2C(=O)c3cccc(F)c3C2=O)c(F)cc1NC(=O)c1occc1C 10.1016/j.bmcl.2020.127724
122197939 160694 0 None -89 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 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 160694 0 None -89 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 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
122197935 159852 0 None -114 4 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 377 10 5 7 0.2 COc1cc(C(O)P(=O)(O)CC[C@@H](N)C(=O)O)ccc1OCC(=O)O nan
CHEMBL4106637 159852 0 None -114 4 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 377 10 5 7 0.2 COc1cc(C(O)P(=O)(O)CC[C@@H](N)C(=O)O)ccc1OCC(=O)O nan
137643759 158426 0 None -1 3 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at mGlu7 (unknown 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 mGlu7 (unknown 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 158426 0 None -1 3 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at mGlu7 (unknown 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 mGlu7 (unknown 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
6706 2367 8 None -104 8 Rat 4.9 pEC50 = 4.9 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 347 9 5 6 0.2 OC(=O)COc1ccc(cc1)C(P(=O)(CC[C@@H](C(=O)O)N)O)O nan
71041983 2367 8 None -104 8 Rat 4.9 pEC50 = 4.9 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 347 9 5 6 0.2 OC(=O)COc1ccc(cc1)C(P(=O)(CC[C@@H](C(=O)O)N)O)O nan
CHEMBL3114673 2367 8 None -104 8 Rat 4.9 pEC50 = 4.9 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 347 9 5 6 0.2 OC(=O)COc1ccc(cc1)C(P(=O)(CC[C@@H](C(=O)O)N)O)O nan
1310 2315 110 None -309 17 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human mGlu7 receptor expressed in HEK293 assessed as inhibition of forskolin stimulated cAMP productionAgonist activity at human mGlu7 receptor expressed in HEK293 assessed as inhibition of forskolin stimulated cAMP production
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
1369 2315 110 None -309 17 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human mGlu7 receptor expressed in HEK293 assessed as inhibition of forskolin stimulated cAMP productionAgonist activity at human mGlu7 receptor expressed in HEK293 assessed as inhibition of forskolin stimulated cAMP production
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
33032 2315 110 None -309 17 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human mGlu7 receptor expressed in HEK293 assessed as inhibition of forskolin stimulated cAMP productionAgonist activity at human mGlu7 receptor expressed in HEK293 assessed as inhibition of forskolin stimulated cAMP production
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
44272391 2315 110 None -309 17 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human mGlu7 receptor expressed in HEK293 assessed as inhibition of forskolin stimulated cAMP productionAgonist activity at human mGlu7 receptor expressed in HEK293 assessed as inhibition of forskolin stimulated cAMP production
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
88747398 2315 110 None -309 17 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human mGlu7 receptor expressed in HEK293 assessed as inhibition of forskolin stimulated cAMP productionAgonist activity at human mGlu7 receptor expressed in HEK293 assessed as inhibition of forskolin stimulated cAMP production
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
CHEMBL575060 2315 110 None -309 17 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human mGlu7 receptor expressed in HEK293 assessed as inhibition of forskolin stimulated cAMP productionAgonist activity at human mGlu7 receptor expressed in HEK293 assessed as inhibition of forskolin stimulated cAMP production
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
DB00142 2315 110 None -309 17 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human mGlu7 receptor expressed in HEK293 assessed as inhibition of forskolin stimulated cAMP productionAgonist activity at human mGlu7 receptor expressed in HEK293 assessed as inhibition of forskolin stimulated cAMP production
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
162657893 181058 0 None - 1 Rat 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 390 4 0 5 4.4 CC(C)Oc1cccc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1021/acsmedchemlett.0c00432
CHEMBL4759638 181058 0 None - 1 Rat 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 390 4 0 5 4.4 CC(C)Oc1cccc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1021/acsmedchemlett.0c00432
162647576 179886 0 None - 1 Rat 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 417 3 0 6 3.4 N#Cc1cnc2c(N3CCOCC3)cccc2c1N1CCN(c2ccccc2F)CC1 10.1021/acsmedchemlett.0c00432
CHEMBL4745777 179886 0 None - 1 Rat 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 417 3 0 6 3.4 N#Cc1cnc2c(N3CCOCC3)cccc2c1N1CCN(c2ccccc2F)CC1 10.1021/acsmedchemlett.0c00432
162647803 179780 0 None - 1 Rat 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 418 4 0 6 3.7 N#Cc1cnc2c(OC3CCOC3)cccc2c1N1CCN(c2ccccc2F)CC1 10.1021/acsmedchemlett.0c00432
CHEMBL4744634 179780 0 None - 1 Rat 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 418 4 0 6 3.7 N#Cc1cnc2c(OC3CCOC3)cccc2c1N1CCN(c2ccccc2F)CC1 10.1021/acsmedchemlett.0c00432
162649074 179851 0 None - 1 Rat 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 432 5 0 6 4.0 N#Cc1cnc2c(OCC3CCOC3)cccc2c1N1CCN(c2ccccc2F)CC1 10.1021/acsmedchemlett.0c00432
CHEMBL4745281 179851 0 None - 1 Rat 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 432 5 0 6 4.0 N#Cc1cnc2c(OCC3CCOC3)cccc2c1N1CCN(c2ccccc2F)CC1 10.1021/acsmedchemlett.0c00432
162647576 179886 0 None - 1 Rat 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 417 3 0 6 3.4 N#Cc1cnc2c(N3CCOCC3)cccc2c1N1CCN(c2ccccc2F)CC1 10.1021/acsmedchemlett.0c00432
CHEMBL4745777 179886 0 None - 1 Rat 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 417 3 0 6 3.4 N#Cc1cnc2c(N3CCOCC3)cccc2c1N1CCN(c2ccccc2F)CC1 10.1021/acsmedchemlett.0c00432
122197956 160471 0 None -61 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 363 9 5 6 0.9 N[C@H](CCP(=O)(O)C(O)c1ccc(SCC(=O)O)cc1)C(=O)O nan
CHEMBL4111817 160471 0 None -61 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 363 9 5 6 0.9 N[C@H](CCP(=O)(O)C(O)c1ccc(SCC(=O)O)cc1)C(=O)O nan
162672655 183135 0 None -7 2 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human mGluR7 in presence of EC20 concentration of L-AP4 by calcium mobilization assayPositive allosteric modulation of human mGluR7 in presence of EC20 concentration of L-AP4 by calcium mobilization assay
ChEMBL 399 3 1 5 3.9 Cc1nc(C(=O)Nc2cc(F)c(N3C(=O)C4=C(CCCC4)C3=O)cc2C)cs1 10.1016/j.bmcl.2020.127724
CHEMBL4795139 183135 0 None -7 2 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human mGluR7 in presence of EC20 concentration of L-AP4 by calcium mobilization assayPositive allosteric modulation of human mGluR7 in presence of EC20 concentration of L-AP4 by calcium mobilization assay
ChEMBL 399 3 1 5 3.9 Cc1nc(C(=O)Nc2cc(F)c(N3C(=O)C4=C(CCCC4)C3=O)cc2C)cs1 10.1016/j.bmcl.2020.127724
162663930 182101 0 None 1 2 Rat 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 380 3 0 5 3.7 COc1cc(F)cc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1021/acsmedchemlett.0c00432
CHEMBL4761695 182101 0 None 1 2 Rat 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 380 3 0 5 3.7 COc1cc(F)cc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1021/acsmedchemlett.0c00432
CHEMBL4781814 182101 0 None 1 2 Rat 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 380 3 0 5 3.7 COc1cc(F)cc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1021/acsmedchemlett.0c00432
10239 4043 29 None -1 5 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat mGlu7 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 mGlu7 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 4043 29 None -1 5 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat mGlu7 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 mGlu7 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 4043 29 None -1 5 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat mGlu7 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 mGlu7 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 4043 29 None -1 5 Rat 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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 4043 29 None -1 5 Rat 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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 4043 29 None -1 5 Rat 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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
145972649 163021 0 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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 389 4 0 4 5.0 CCc1nn2c(C(F)(F)F)cc(C)nc2c1-c1ccc(OC(F)F)cc1F 10.1021/acsmedchemlett.7b00317
CHEMBL4175784 163021 0 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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 389 4 0 4 5.0 CCc1nn2c(C(F)(F)F)cc(C)nc2c1-c1ccc(OC(F)F)cc1F 10.1021/acsmedchemlett.7b00317
145972649 163021 0 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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 389 4 0 4 5.0 CCc1nn2c(C(F)(F)F)cc(C)nc2c1-c1ccc(OC(F)F)cc1F 10.1021/acsmedchemlett.7b00317
CHEMBL4175784 163021 0 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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 389 4 0 4 5.0 CCc1nn2c(C(F)(F)F)cc(C)nc2c1-c1ccc(OC(F)F)cc1F 10.1021/acsmedchemlett.7b00317
10238 4027 26 None -1 5 Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at rat mGlu7 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 mGlu7 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 4027 26 None -1 5 Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at rat mGlu7 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 mGlu7 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 4027 26 None -1 5 Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at rat mGlu7 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 mGlu7 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
10238 4027 26 None -1 5 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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 4027 26 None -1 5 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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 4027 26 None -1 5 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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
145962919 162373 0 None 1 2 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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 162373 0 None 1 2 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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
162654767 180572 0 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 362 3 0 5 3.6 COc1cccc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1021/acsmedchemlett.0c00432
CHEMBL4754102 180572 0 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 362 3 0 5 3.6 COc1cccc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1021/acsmedchemlett.0c00432
CHEMBL4776732 180572 0 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 362 3 0 5 3.6 COc1cccc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1021/acsmedchemlett.0c00432
122197952 160572 0 None -13 3 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 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 160572 0 None -13 3 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 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
145962919 162373 0 None 1 2 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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 162373 0 None 1 2 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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
122197955 160594 0 None -13 3 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 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 160594 0 None -13 3 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 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
162647803 179780 0 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 418 4 0 6 3.7 N#Cc1cnc2c(OC3CCOC3)cccc2c1N1CCN(c2ccccc2F)CC1 10.1021/acsmedchemlett.0c00432
CHEMBL4744634 179780 0 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 418 4 0 6 3.7 N#Cc1cnc2c(OC3CCOC3)cccc2c1N1CCN(c2ccccc2F)CC1 10.1021/acsmedchemlett.0c00432
1441 402 25 None 60 2 Human 6.8 pEC50 = 6.8 Functional
Allosteric agonist activity at human mGlu7 expressed in CHO cells assessed as reduction in forskolin-induced cAMP production after 30 mins by cAMP reagent-based assayAllosteric agonist activity at human mGlu7 expressed in CHO cells assessed as reduction in forskolin-induced cAMP production after 30 mins by cAMP reagent-based assay
ChEMBL 392 9 2 2 5.7 C(NC(c1ccccc1)c1ccccc1)CNC(c1ccccc1)c1ccccc1 10.1039/C8MD00524A
1894361 402 25 None 60 2 Human 6.8 pEC50 = 6.8 Functional
Allosteric agonist activity at human mGlu7 expressed in CHO cells assessed as reduction in forskolin-induced cAMP production after 30 mins by cAMP reagent-based assayAllosteric agonist activity at human mGlu7 expressed in CHO cells assessed as reduction in forskolin-induced cAMP production after 30 mins by cAMP reagent-based assay
ChEMBL 392 9 2 2 5.7 C(NC(c1ccccc1)c1ccccc1)CNC(c1ccccc1)c1ccccc1 10.1039/C8MD00524A
CHEMBL1387826 402 25 None 60 2 Human 6.8 pEC50 = 6.8 Functional
Allosteric agonist activity at human mGlu7 expressed in CHO cells assessed as reduction in forskolin-induced cAMP production after 30 mins by cAMP reagent-based assayAllosteric agonist activity at human mGlu7 expressed in CHO cells assessed as reduction in forskolin-induced cAMP production after 30 mins by cAMP reagent-based assay
ChEMBL 392 9 2 2 5.7 C(NC(c1ccccc1)c1ccccc1)CNC(c1ccccc1)c1ccccc1 10.1039/C8MD00524A
155518933 170346 0 None -2 3 Human 5.8 pEC50 = 5.8 Functional
Allosteric agonist activity at human mGlu7 expressed in CHO cells assessed as reduction in forskolin-induced cAMP production after 30 mins by cAMP reagent-based assayAllosteric agonist activity at human mGlu7 expressed in CHO cells assessed as reduction in forskolin-induced cAMP production after 30 mins by cAMP reagent-based assay
ChEMBL 421 6 1 3 4.3 CNC(=O)N1CCCC(CN2CCC(OC(c3ccccc3)c3ccccc3)CC2)C1 10.1039/C8MD00524A
CHEMBL4447269 170346 0 None -2 3 Human 5.8 pEC50 = 5.8 Functional
Allosteric agonist activity at human mGlu7 expressed in CHO cells assessed as reduction in forskolin-induced cAMP production after 30 mins by cAMP reagent-based assayAllosteric agonist activity at human mGlu7 expressed in CHO cells assessed as reduction in forskolin-induced cAMP production after 30 mins by cAMP reagent-based assay
ChEMBL 421 6 1 3 4.3 CNC(=O)N1CCCC(CN2CCC(OC(c3ccccc3)c3ccccc3)CC2)C1 10.1039/C8MD00524A
54815068 172307 4 None - 1 Human 5.8 pEC50 = 5.8 Functional
Allosteric agonist activity at human mGlu7 expressed in CHO cells assessed as reduction in forskolin-induced cAMP production after 30 mins by cAMP reagent-based assayAllosteric agonist activity at human mGlu7 expressed in CHO cells assessed as reduction in forskolin-induced cAMP production after 30 mins by cAMP reagent-based assay
ChEMBL 294 4 1 2 3.3 CC(NCC(=O)N1CCCc2ccccc21)c1ccccc1 10.1039/C8MD00524A
CHEMBL4475187 172307 4 None - 1 Human 5.8 pEC50 = 5.8 Functional
Allosteric agonist activity at human mGlu7 expressed in CHO cells assessed as reduction in forskolin-induced cAMP production after 30 mins by cAMP reagent-based assayAllosteric agonist activity at human mGlu7 expressed in CHO cells assessed as reduction in forskolin-induced cAMP production after 30 mins by cAMP reagent-based assay
ChEMBL 294 4 1 2 3.3 CC(NCC(=O)N1CCCc2ccccc21)c1ccccc1 10.1039/C8MD00524A
162663930 182101 0 None 1 2 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 380 3 0 5 3.7 COc1cc(F)cc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1021/acsmedchemlett.0c00432
CHEMBL4761695 182101 0 None 1 2 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 380 3 0 5 3.7 COc1cc(F)cc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1021/acsmedchemlett.0c00432
CHEMBL4781814 182101 0 None 1 2 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 380 3 0 5 3.7 COc1cc(F)cc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1021/acsmedchemlett.0c00432
122197962 160423 0 None -13 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 415 10 4 6 1.6 N[C@H](CCP(=O)(O)Cc1ccc(OCC(=O)O)c(OC(F)(F)F)c1)C(=O)O nan
CHEMBL4111386 160423 0 None -13 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 415 10 4 6 1.6 N[C@H](CCP(=O)(O)Cc1ccc(OCC(=O)O)c(OC(F)(F)F)c1)C(=O)O nan
145972181 163029 0 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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)c(F)c1 10.1021/acsmedchemlett.7b00317
CHEMBL4175868 163029 0 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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)c(F)c1 10.1021/acsmedchemlett.7b00317
145957196 162095 0 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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 335 3 0 4 4.3 CCc1nn2c(C(F)(F)F)cc(C)nc2c1-c1ccc(OC)cc1 10.1021/acsmedchemlett.7b00317
CHEMBL4161084 162095 0 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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 335 3 0 4 4.3 CCc1nn2c(C(F)(F)F)cc(C)nc2c1-c1ccc(OC)cc1 10.1021/acsmedchemlett.7b00317
145972181 163029 0 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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)c(F)c1 10.1021/acsmedchemlett.7b00317
CHEMBL4175868 163029 0 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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)c(F)c1 10.1021/acsmedchemlett.7b00317
145957196 162095 0 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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 335 3 0 4 4.3 CCc1nn2c(C(F)(F)F)cc(C)nc2c1-c1ccc(OC)cc1 10.1021/acsmedchemlett.7b00317
CHEMBL4161084 162095 0 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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 335 3 0 4 4.3 CCc1nn2c(C(F)(F)F)cc(C)nc2c1-c1ccc(OC)cc1 10.1021/acsmedchemlett.7b00317
162648102 179904 0 None -2 5 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human mGluR7 in presence of EC20 concentration of L-AP4 by calcium mobilization assayPositive allosteric modulation of human mGluR7 in presence of EC20 concentration of L-AP4 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 179904 0 None -2 5 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human mGluR7 in presence of EC20 concentration of L-AP4 by calcium mobilization assayPositive allosteric modulation of human mGluR7 in presence of EC20 concentration of L-AP4 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
162649929 180169 0 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 402 4 0 5 4.5 N#Cc1cnc2c(OC3CCC3)cccc2c1N1CCN(c2ccccc2F)CC1 10.1021/acsmedchemlett.0c00432
CHEMBL4749059 180169 0 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 402 4 0 5 4.5 N#Cc1cnc2c(OC3CCC3)cccc2c1N1CCN(c2ccccc2F)CC1 10.1021/acsmedchemlett.0c00432
162662952 181918 0 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 380 3 0 5 3.7 COc1c(F)ccc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1021/acsmedchemlett.0c00432
CHEMBL4779613 181918 0 None - 1 Rat 5.8 pEC50 = 5.8 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 380 3 0 5 3.7 COc1c(F)ccc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1021/acsmedchemlett.0c00432
162649074 179851 0 None - 1 Rat 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 432 5 0 6 4.0 N#Cc1cnc2c(OCC3CCOC3)cccc2c1N1CCN(c2ccccc2F)CC1 10.1021/acsmedchemlett.0c00432
CHEMBL4745281 179851 0 None - 1 Rat 5.7 pEC50 = 5.7 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 432 5 0 6 4.0 N#Cc1cnc2c(OCC3CCOC3)cccc2c1N1CCN(c2ccccc2F)CC1 10.1021/acsmedchemlett.0c00432
122197950 160313 0 None -32 3 Rat 5.7 pEC50 = 5.7 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 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 160313 0 None -32 3 Rat 5.7 pEC50 = 5.7 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 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
162667269 182513 0 None -3 3 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human mGluR7 in presence of EC20 concentration of L-AP4 by calcium mobilization assayPositive allosteric modulation of human mGluR7 in presence of EC20 concentration of L-AP4 by calcium mobilization assay
ChEMBL 434 3 1 4 4.7 Cc1ccoc1C(=O)Nc1cc(F)c(N2C(=O)c3cccc(Cl)c3C2=O)c(F)c1F 10.1016/j.bmcl.2020.127724
CHEMBL4787053 182513 0 None -3 3 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human mGluR7 in presence of EC20 concentration of L-AP4 by calcium mobilization assayPositive allosteric modulation of human mGluR7 in presence of EC20 concentration of L-AP4 by calcium mobilization assay
ChEMBL 434 3 1 4 4.7 Cc1ccoc1C(=O)Nc1cc(F)c(N2C(=O)c3cccc(Cl)c3C2=O)c(F)c1F 10.1016/j.bmcl.2020.127724
8595992 175406 2 None - 1 Human 6.7 pEC50 = 6.7 Functional
Allosteric agonist activity at human mGlu7 expressed in CHO cells assessed as reduction in forskolin-induced cAMP production after 30 mins by cAMP reagent-based assayAllosteric agonist activity at human mGlu7 expressed in CHO cells assessed as reduction in forskolin-induced cAMP production after 30 mins by cAMP reagent-based assay
ChEMBL 356 5 1 2 4.3 O=C(CNC(c1ccccc1)c1ccccc1)N1CCCc2ccccc21 10.1039/C8MD00524A
CHEMBL4575681 175406 2 None - 1 Human 6.7 pEC50 = 6.7 Functional
Allosteric agonist activity at human mGlu7 expressed in CHO cells assessed as reduction in forskolin-induced cAMP production after 30 mins by cAMP reagent-based assayAllosteric agonist activity at human mGlu7 expressed in CHO cells assessed as reduction in forskolin-induced cAMP production after 30 mins by cAMP reagent-based assay
ChEMBL 356 5 1 2 4.3 O=C(CNC(c1ccccc1)c1ccccc1)N1CCCc2ccccc21 10.1039/C8MD00524A
145949260 162800 0 None - 1 Rat 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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 355 2 0 4 4.7 COc1ccc(-c2c(C)nn3c(C(F)(F)F)cc(C)nc23)cc1Cl 10.1021/acsmedchemlett.7b00317
CHEMBL4172374 162800 0 None - 1 Rat 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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 355 2 0 4 4.7 COc1ccc(-c2c(C)nn3c(C(F)(F)F)cc(C)nc23)cc1Cl 10.1021/acsmedchemlett.7b00317
122197941 160748 0 None -60 2 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 415 9 5 6 1.5 N[C@H](CCP(=O)(O)C(O)c1cc(Cl)c(OCC(=O)O)c(Cl)c1)C(=O)O nan
CHEMBL4113972 160748 0 None -60 2 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 415 9 5 6 1.5 N[C@H](CCP(=O)(O)C(O)c1cc(Cl)c(OCC(=O)O)c(Cl)c1)C(=O)O nan
145949260 162800 0 None - 1 Rat 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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 355 2 0 4 4.7 COc1ccc(-c2c(C)nn3c(C(F)(F)F)cc(C)nc23)cc1Cl 10.1021/acsmedchemlett.7b00317
CHEMBL4172374 162800 0 None - 1 Rat 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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 355 2 0 4 4.7 COc1ccc(-c2c(C)nn3c(C(F)(F)F)cc(C)nc23)cc1Cl 10.1021/acsmedchemlett.7b00317
145960296 162308 0 None - 1 Rat 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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 3 0 4 4.6 Cc1cc(C(F)(F)F)n2nc(C)c(-c3ccc(OC(F)F)cc3)c2n1 10.1021/acsmedchemlett.7b00317
CHEMBL4164496 162308 0 None - 1 Rat 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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 3 0 4 4.6 Cc1cc(C(F)(F)F)n2nc(C)c(-c3ccc(OC(F)F)cc3)c2n1 10.1021/acsmedchemlett.7b00317
145960296 162308 0 None - 1 Rat 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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 3 0 4 4.6 Cc1cc(C(F)(F)F)n2nc(C)c(-c3ccc(OC(F)F)cc3)c2n1 10.1021/acsmedchemlett.7b00317
CHEMBL4164496 162308 0 None - 1 Rat 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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 3 0 4 4.6 Cc1cc(C(F)(F)F)n2nc(C)c(-c3ccc(OC(F)F)cc3)c2n1 10.1021/acsmedchemlett.7b00317
145955533 162596 0 None - 1 Rat 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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 335 2 0 4 4.3 COc1ccc(-c2c(C)nn3c(C(F)(F)F)cc(C)nc23)cc1C 10.1021/acsmedchemlett.7b00317
CHEMBL4169009 162596 0 None - 1 Rat 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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 335 2 0 4 4.3 COc1ccc(-c2c(C)nn3c(C(F)(F)F)cc(C)nc23)cc1C 10.1021/acsmedchemlett.7b00317
145955533 162596 0 None - 1 Rat 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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 335 2 0 4 4.3 COc1ccc(-c2c(C)nn3c(C(F)(F)F)cc(C)nc23)cc1C 10.1021/acsmedchemlett.7b00317
CHEMBL4169009 162596 0 None - 1 Rat 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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 335 2 0 4 4.3 COc1ccc(-c2c(C)nn3c(C(F)(F)F)cc(C)nc23)cc1C 10.1021/acsmedchemlett.7b00317
162677180 183529 0 None -7 3 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human mGluR7 in presence of EC20 concentration of L-AP4 by calcium mobilization assayPositive allosteric modulation of human mGluR7 in presence of EC20 concentration of L-AP4 by calcium mobilization assay
ChEMBL 400 3 1 4 4.1 Cc1ccoc1C(=O)Nc1c(F)cc(N2C(=O)c3ccccc3C2=O)c(F)c1F 10.1016/j.bmcl.2020.127724
CHEMBL4799902 183529 0 None -7 3 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human mGluR7 in presence of EC20 concentration of L-AP4 by calcium mobilization assayPositive allosteric modulation of human mGluR7 in presence of EC20 concentration of L-AP4 by calcium mobilization assay
ChEMBL 400 3 1 4 4.1 Cc1ccoc1C(=O)Nc1c(F)cc(N2C(=O)c3ccccc3C2=O)c(F)c1F 10.1016/j.bmcl.2020.127724
970725 88743 10 None - 1 Rat 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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 321 2 0 4 4.0 COc1ccc(-c2c(C)nn3c(C(F)(F)F)cc(C)nc23)cc1 10.1021/acsmedchemlett.7b00317
CHEMBL2361777 88743 10 None - 1 Rat 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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 321 2 0 4 4.0 COc1ccc(-c2c(C)nn3c(C(F)(F)F)cc(C)nc23)cc1 10.1021/acsmedchemlett.7b00317
970725 88743 10 None - 1 Rat 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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 321 2 0 4 4.0 COc1ccc(-c2c(C)nn3c(C(F)(F)F)cc(C)nc23)cc1 10.1021/acsmedchemlett.7b00317
CHEMBL2361777 88743 10 None - 1 Rat 5.5 pEC50 = 5.5 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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 321 2 0 4 4.0 COc1ccc(-c2c(C)nn3c(C(F)(F)F)cc(C)nc23)cc1 10.1021/acsmedchemlett.7b00317
122197946 160448 0 None -91 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 383 9 6 6 0.3 N[C@H](CCP(=O)(O)C(O)c1ccc(OCP(=O)(O)O)cc1)C(=O)O nan
CHEMBL4111679 160448 0 None -91 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 383 9 6 6 0.3 N[C@H](CCP(=O)(O)C(O)c1ccc(OCP(=O)(O)O)cc1)C(=O)O nan
122197938 160939 0 None -43 3 Rat 5.5 pEC50 = 5.5 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 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 160939 0 None -43 3 Rat 5.5 pEC50 = 5.5 Functional
Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.
ChEMBL 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
122197951 160734 0 None -39 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 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 160734 0 None -39 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 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
122197944 160223 0 None -38 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 345 9 5 5 0.8 N[C@H](CCP(=O)(O)C(O)c1ccc(CCC(=O)O)cc1)C(=O)O nan
CHEMBL4109748 160223 0 None -38 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 345 9 5 5 0.8 N[C@H](CCP(=O)(O)C(O)c1ccc(CCC(=O)O)cc1)C(=O)O nan
162670460 182895 0 None -6 3 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGluR7 in presence of EC20 concentration of L-AP4 by calcium mobilization assayPositive allosteric modulation of human mGluR7 in presence of EC20 concentration of L-AP4 by calcium mobilization assay
ChEMBL 382 3 1 4 4.0 Cc1cc(N2C(=O)C3=C(CCCC3)C2=O)c(F)cc1NC(=O)c1occc1C 10.1016/j.bmcl.2020.127724
CHEMBL4792152 182895 0 None -6 3 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGluR7 in presence of EC20 concentration of L-AP4 by calcium mobilization assayPositive allosteric modulation of human mGluR7 in presence of EC20 concentration of L-AP4 by calcium mobilization assay
ChEMBL 382 3 1 4 4.0 Cc1cc(N2C(=O)C3=C(CCCC3)C2=O)c(F)cc1NC(=O)c1occc1C 10.1016/j.bmcl.2020.127724
162657826 181127 0 None -4 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGluR7 in presence of EC20 concentration of L-AP4 by calcium mobilization assayPositive allosteric modulation of human mGluR7 in presence of EC20 concentration of L-AP4 by calcium mobilization assay
ChEMBL 368 3 1 4 3.7 Cc1cc(N2C(=O)C3=C(CCCC3)C2=O)c(F)cc1NC(=O)c1ccco1 10.1016/j.bmcl.2020.127724
CHEMBL4760570 181127 0 None -4 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGluR7 in presence of EC20 concentration of L-AP4 by calcium mobilization assayPositive allosteric modulation of human mGluR7 in presence of EC20 concentration of L-AP4 by calcium mobilization assay
ChEMBL 368 3 1 4 3.7 Cc1cc(N2C(=O)C3=C(CCCC3)C2=O)c(F)cc1NC(=O)c1ccco1 10.1016/j.bmcl.2020.127724
162664763 182174 0 None - 1 Rat 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 416 4 0 5 4.3 N#Cc1cnc2c(OC(F)F)cc(F)cc2c1N1CCN(c2ccccc2F)CC1 10.1021/acsmedchemlett.0c00432
CHEMBL4782643 182174 0 None - 1 Rat 5.4 pEC50 = 5.4 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 416 4 0 5 4.3 N#Cc1cnc2c(OC(F)F)cc(F)cc2c1N1CCN(c2ccccc2F)CC1 10.1021/acsmedchemlett.0c00432
122197958 160524 0 None -11 4 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 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 160524 0 None -11 4 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 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
137661528 159507 0 None -51 4 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at mGlu7 (unknown 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 mGlu7 (unknown 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 159507 0 None -51 4 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at mGlu7 (unknown 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 mGlu7 (unknown 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
162674612 183382 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGluR7 in presence of EC20 concentration of L-AP4 by calcium mobilization assayPositive allosteric modulation of human mGluR7 in presence of EC20 concentration of L-AP4 by calcium mobilization assay
ChEMBL 402 3 1 4 4.4 Cc1cc(N2C(=O)C3=C(CCCC3)C2=O)c(F)cc1NC(=O)c1ccc(Cl)o1 10.1016/j.bmcl.2020.127724
CHEMBL4797971 183382 0 None -1 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human mGluR7 in presence of EC20 concentration of L-AP4 by calcium mobilization assayPositive allosteric modulation of human mGluR7 in presence of EC20 concentration of L-AP4 by calcium mobilization assay
ChEMBL 402 3 1 4 4.4 Cc1cc(N2C(=O)C3=C(CCCC3)C2=O)c(F)cc1NC(=O)c1ccc(Cl)o1 10.1016/j.bmcl.2020.127724
1377 1340 26 None -239 8 Rat 4.4 pEC50 = 4.4 Functional
Metabotropic glutamate receptor 7 antagonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 7 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 1340 26 None -239 8 Rat 4.4 pEC50 = 4.4 Functional
Metabotropic glutamate receptor 7 antagonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 7 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 1340 26 None -239 8 Rat 4.4 pEC50 = 4.4 Functional
Metabotropic glutamate receptor 7 antagonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 7 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
46197778 8218 0 None -38 5 Rat 4.4 pEC50 = 4.4 Functional
Agonist activity at rat mGlu7 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 mGlu7 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 8218 0 None -38 5 Rat 4.4 pEC50 = 4.4 Functional
Agonist activity at rat mGlu7 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 mGlu7 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
1368 2290 37 None -123 11 Rat 4.3 pEC50 = 4.3 Functional
Metabotropic glutamate receptor 7 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 7 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 10.1021/jm030967o
5310956 2290 37 None -123 11 Rat 4.3 pEC50 = 4.3 Functional
Metabotropic glutamate receptor 7 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 7 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 10.1021/jm030967o
CHEMBL280563 2290 37 None -123 11 Rat 4.3 pEC50 = 4.3 Functional
Metabotropic glutamate receptor 7 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 7 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells
ChEMBL 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 10.1021/jm030967o
145957567 162288 0 None 1 2 Rat 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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 162288 0 None 1 2 Rat 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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
145957567 162288 0 None 1 2 Rat 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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 162288 0 None 1 2 Rat 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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
1406 2073 38 None -489 7 Human 4.3 pEC50 = 4.3 Functional
Compound was evaluated for the inhibition of forskolin stimulated cAMP accumulation in CHO cells expressing hmGluR7bCompound was evaluated for the inhibition of forskolin stimulated cAMP accumulation in CHO cells expressing hmGluR7b
ChEMBL 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10.1016/s0960-894x(00)00197-9
4545574 2073 38 None -489 7 Human 4.3 pEC50 = 4.3 Functional
Compound was evaluated for the inhibition of forskolin stimulated cAMP accumulation in CHO cells expressing hmGluR7bCompound was evaluated for the inhibition of forskolin stimulated cAMP accumulation in CHO cells expressing hmGluR7b
ChEMBL 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10.1016/s0960-894x(00)00197-9
CHEMBL277475 2073 38 None -489 7 Human 4.3 pEC50 = 4.3 Functional
Compound was evaluated for the inhibition of forskolin stimulated cAMP accumulation in CHO cells expressing hmGluR7bCompound was evaluated for the inhibition of forskolin stimulated cAMP accumulation in CHO cells expressing hmGluR7b
ChEMBL 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10.1016/s0960-894x(00)00197-9
162648752 179952 0 None -7 3 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human mGluR7 in presence of EC20 concentration of L-AP4 by calcium mobilization assayPositive allosteric modulation of human mGluR7 in presence of EC20 concentration of L-AP4 by calcium mobilization assay
ChEMBL 418 3 1 4 4.2 Cc1ccoc1C(=O)Nc1cc(F)c(N2C(=O)c3cccc(F)c3C2=O)c(F)c1F 10.1016/j.bmcl.2020.127724
CHEMBL4746530 179952 0 None -7 3 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human mGluR7 in presence of EC20 concentration of L-AP4 by calcium mobilization assayPositive allosteric modulation of human mGluR7 in presence of EC20 concentration of L-AP4 by calcium mobilization assay
ChEMBL 418 3 1 4 4.2 Cc1ccoc1C(=O)Nc1cc(F)c(N2C(=O)c3cccc(F)c3C2=O)c(F)c1F 10.1016/j.bmcl.2020.127724
162652009 180317 0 None - 1 Rat 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 436 4 0 6 3.9 N#Cc1cnc2c(OC3CCOC3)cc(F)cc2c1N1CCN(c2ccccc2F)CC1 10.1021/acsmedchemlett.0c00432
CHEMBL4751110 180317 0 None - 1 Rat 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 436 4 0 6 3.9 N#Cc1cnc2c(OC3CCOC3)cc(F)cc2c1N1CCN(c2ccccc2F)CC1 10.1021/acsmedchemlett.0c00432
137650519 157345 0 None -47 4 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at mGlu7 (unknown 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 mGlu7 (unknown 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 157345 0 None -47 4 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at mGlu7 (unknown 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 mGlu7 (unknown 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
122197942 160067 0 None -97 4 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 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 160067 0 None -97 4 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 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
46215704 80810 0 None -33 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human mGlu 7 expressed in HEK293 cells by Ca+2 assayAgonist activity at human mGlu 7 expressed in HEK293 cells by Ca+2 assay
ChEMBL 447 3 1 4 6.2 O[C@H]1CC[C@H](n2ccc3cc(-c4ccn5c(CC(F)(F)F)cnc5c4Cl)ccc32)CC1 10.1021/jm201561r
CHEMBL2152119 80810 0 None -33 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human mGlu 7 expressed in HEK293 cells by Ca+2 assayAgonist activity at human mGlu 7 expressed in HEK293 cells by Ca+2 assay
ChEMBL 447 3 1 4 6.2 O[C@H]1CC[C@H](n2ccc3cc(-c4ccn5c(CC(F)(F)F)cnc5c4Cl)ccc32)CC1 10.1021/jm201561r
46898088 2366 6 None -263 8 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at mGlu7 (unknown 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 mGlu7 (unknown 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 2366 6 None -263 8 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at mGlu7 (unknown 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 mGlu7 (unknown 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 2366 6 None -263 8 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at mGlu7 (unknown 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 mGlu7 (unknown 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
137655963 159023 0 None -5 4 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at mGlu7 (unknown 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 mGlu7 (unknown 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 159023 0 None -5 4 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at mGlu7 (unknown 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 mGlu7 (unknown 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
145955288 162577 0 None -1 4 Rat 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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 162577 0 None -1 4 Rat 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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
145955288 162577 0 None -1 4 Rat 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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 162577 0 None -1 4 Rat 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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
122197949 159836 0 None -36 3 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 391 11 5 7 0.6 CCOc1cc(C(O)P(=O)(O)CC[C@@H](N)C(=O)O)ccc1OCC(=O)O nan
CHEMBL4106501 159836 0 None -36 3 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 391 11 5 7 0.6 CCOc1cc(C(O)P(=O)(O)CC[C@@H](N)C(=O)O)ccc1OCC(=O)O nan
137639752 156915 0 None -123 4 Human 4.2 pEC50 = 4.2 Functional
Agonist activity at mGlu7 (unknown 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 mGlu7 (unknown 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 156915 0 None -123 4 Human 4.2 pEC50 = 4.2 Functional
Agonist activity at mGlu7 (unknown 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 mGlu7 (unknown 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
137645989 157694 0 None -87 4 Human 4.2 pEC50 = 4.2 Functional
Agonist activity at mGlu7 (unknown 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 mGlu7 (unknown 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 157694 0 None -87 4 Human 4.2 pEC50 = 4.2 Functional
Agonist activity at mGlu7 (unknown 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 mGlu7 (unknown 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
131954513 162078 38 None -1 5 Rat 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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 162078 38 None -1 5 Rat 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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
131954513 162078 38 None -1 5 Rat 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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 162078 38 None -1 5 Rat 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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
162650961 180326 0 None - 1 Rat 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 450 5 0 6 4.1 N#Cc1cnc2c(OCC3CCOC3)cc(F)cc2c1N1CCN(c2ccccc2F)CC1 10.1021/acsmedchemlett.0c00432
CHEMBL4751175 180326 0 None - 1 Rat 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 450 5 0 6 4.1 N#Cc1cnc2c(OCC3CCOC3)cc(F)cc2c1N1CCN(c2ccccc2F)CC1 10.1021/acsmedchemlett.0c00432
122197953 159953 0 None -16 3 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 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 159953 0 None -16 3 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 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
122197940 160007 0 None -43 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 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 160007 0 None -43 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 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
162657879 181047 0 None - 1 Rat 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 398 3 0 6 3.8 N#Cc1cnc2c(-n3ccnc3)cccc2c1N1CCN(c2ccccc2F)CC1 10.1021/acsmedchemlett.0c00432
CHEMBL4759480 181047 0 None - 1 Rat 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 398 3 0 6 3.8 N#Cc1cnc2c(-n3ccnc3)cccc2c1N1CCN(c2ccccc2F)CC1 10.1021/acsmedchemlett.0c00432
162653691 180496 0 None - 1 Rat 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 408 4 0 5 4.5 CC(C)Oc1cc(F)cc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1021/acsmedchemlett.0c00432
CHEMBL4753189 180496 0 None - 1 Rat 6.2 pEC50 = 6.2 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 408 4 0 5 4.5 CC(C)Oc1cc(F)cc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1021/acsmedchemlett.0c00432
46918015 155868 0 None -37 4 Human 4.2 pEC50 = 4.2 Functional
Agonist activity at mGlu7 (unknown 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 mGlu7 (unknown 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 155868 0 None -37 4 Human 4.2 pEC50 = 4.2 Functional
Agonist activity at mGlu7 (unknown 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 mGlu7 (unknown 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
162655830 180797 0 None - 1 Rat 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 431 3 0 6 3.8 CC1CN(c2cccc3c(N4CCN(c5ccccc5F)CC4)c(C#N)cnc23)CCO1 10.1021/acsmedchemlett.0c00432
CHEMBL4756462 180797 0 None - 1 Rat 5.2 pEC50 = 5.2 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 431 3 0 6 3.8 CC1CN(c2cccc3c(N4CCN(c5ccccc5F)CC4)c(C#N)cnc23)CCO1 10.1021/acsmedchemlett.0c00432
145957424 162069 0 None 1 3 Rat 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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 162069 0 None 1 3 Rat 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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 162069 0 None 1 3 Rat 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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 162069 0 None 1 3 Rat 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of rat mGlu7 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 mGlu7 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
162653691 180496 0 None - 1 Rat 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 408 4 0 5 4.5 CC(C)Oc1cc(F)cc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1021/acsmedchemlett.0c00432
CHEMBL4753189 180496 0 None - 1 Rat 6.1 pEC50 = 6.1 Functional
Positive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells co-expressing Gai5 assessed as potentiation of L-AP4-induced calcium mobilization preincubated for 140 secs and treated with EC20 L-AP4 for 125 secs and followed by subsequent addition of EC80 L-AP4 by Fluo-4-AM dye based fluorescence assay
ChEMBL 408 4 0 5 4.5 CC(C)Oc1cc(F)cc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1021/acsmedchemlett.0c00432
6348408 7820 1 None -14 8 Human 4.1 pEC50 = 4.1 Functional
Agonist activity at mGlu7 (unknown 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 mGlu7 (unknown 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 7820 1 None -14 8 Human 4.1 pEC50 = 4.1 Functional
Agonist activity at mGlu7 (unknown 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 mGlu7 (unknown 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
6348408 7820 1 None -14 8 Rat 4.1 pEC50 = 4.1 Functional
Agonist activity at rat mGlu7 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 mGlu7 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 7820 1 None -14 8 Rat 4.1 pEC50 = 4.1 Functional
Agonist activity at rat mGlu7 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 mGlu7 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
162674997 183390 0 None -1 3 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human mGluR7 in presence of EC20 concentration of L-AP4 by calcium mobilization assayPositive allosteric modulation of human mGluR7 in presence of EC20 concentration of L-AP4 by calcium mobilization assay
ChEMBL 412 3 1 4 4.7 Cc1cc(N2C(=O)c3cccc(Cl)c3C2=O)c(F)cc1NC(=O)c1occc1C 10.1016/j.bmcl.2020.127724
CHEMBL4798021 183390 0 None -1 3 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human mGluR7 in presence of EC20 concentration of L-AP4 by calcium mobilization assayPositive allosteric modulation of human mGluR7 in presence of EC20 concentration of L-AP4 by calcium mobilization assay
ChEMBL 412 3 1 4 4.7 Cc1cc(N2C(=O)c3cccc(Cl)c3C2=O)c(F)cc1NC(=O)c1occc1C 10.1016/j.bmcl.2020.127724
23579324 200137 0 None - 1 Rat 6.0 pIC50 = 6 Functional
Antagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPRAntagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPR
ChEMBL 303 2 0 5 3.3 Cn1c(-c2ccccc2)cc2onc(-c3ccccn3)c2c1=O 10.1016/j.bmcl.2009.11.070
CHEMBL596275 200137 0 None - 1 Rat 6.0 pIC50 = 6 Functional
Antagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPRAntagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPR
ChEMBL 303 2 0 5 3.3 Cn1c(-c2ccccc2)cc2onc(-c3ccccn3)c2c1=O 10.1016/j.bmcl.2009.11.070
168277688 190191 0 None - 1 Rat 6.0 pIC50 = 6 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 419 5 0 8 3.9 COc1ccc(-c2noc(-c3cc(Cl)cc(F)c3-n3cncn3)n2)c(F)c1OC 10.1016/j.bmcl.2022.128923
CHEMBL5174297 190191 0 None - 1 Rat 6.0 pIC50 = 6 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 419 5 0 8 3.9 COc1ccc(-c2noc(-c3cc(Cl)cc(F)c3-n3cncn3)n2)c(F)c1OC 10.1016/j.bmcl.2022.128923
168283516 191063 0 None 3 2 Rat 6.0 pIC50 = 6 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 448 7 1 7 4.4 COc1cc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OC1CCC1 10.1016/j.bmcl.2022.128923
CHEMBL5187341 191063 0 None 3 2 Rat 6.0 pIC50 = 6 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 448 7 1 7 4.4 COc1cc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OC1CCC1 10.1016/j.bmcl.2022.128923
168288994 191774 0 None 6 2 Rat 6.0 pIC50 = 6 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 383 5 0 8 3.7 COc1ccc(-c2noc(-c3cc(Cl)ccc3-n3cncn3)n2)cc1OC 10.1016/j.bmcl.2022.128923
CHEMBL5197933 191774 0 None 6 2 Rat 6.0 pIC50 = 6 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 383 5 0 8 3.7 COc1ccc(-c2noc(-c3cc(Cl)ccc3-n3cncn3)n2)cc1OC 10.1016/j.bmcl.2022.128923
23579326 199661 0 None - 1 Rat 7.0 pIC50 = 7 Functional
Antagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPRAntagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPR
ChEMBL 303 2 0 5 3.3 Cn1c(-c2ccccc2)cc2onc(-c3ccncc3)c2c1=O 10.1016/j.bmcl.2009.11.070
CHEMBL592956 199661 0 None - 1 Rat 7.0 pIC50 = 7 Functional
Antagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPRAntagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPR
ChEMBL 303 2 0 5 3.3 Cn1c(-c2ccccc2)cc2onc(-c3ccncc3)c2c1=O 10.1016/j.bmcl.2009.11.070
57338826 149627 0 None -229 5 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at recombinant human mGlu7 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 mGlu7 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 149627 0 None -229 5 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at recombinant human mGlu7 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 mGlu7 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
168288994 191774 0 None 6 2 Rat 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 383 5 0 8 3.7 COc1ccc(-c2noc(-c3cc(Cl)ccc3-n3cncn3)n2)cc1OC 10.1016/j.bmcl.2022.128923
CHEMBL5197933 191774 0 None 6 2 Rat 6.0 pIC50 = 6.0 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 383 5 0 8 3.7 COc1ccc(-c2noc(-c3cc(Cl)ccc3-n3cncn3)n2)cc1OC 10.1016/j.bmcl.2022.128923
155540837 172505 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assay
ChEMBL 442 9 1 8 3.8 COc1cc(F)c(OCCNc2cc(OC(F)(F)F)ccc2-n2cncn2)cc1OC 10.1021/acs.jmedchem.8b01810
CHEMBL4483431 172505 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assay
ChEMBL 442 9 1 8 3.8 COc1cc(F)c(OCCNc2cc(OC(F)(F)F)ccc2-n2cncn2)cc1OC 10.1021/acs.jmedchem.8b01810
155555306 174357 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 451 6 0 8 4.2 COc1ccc(-c2nnc(-c3cc(OC(F)(F)F)ccc3N3CCOCC3)o2)cc1OC 10.1016/j.bmcl.2019.03.016
CHEMBL4551424 174357 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 451 6 0 8 4.2 COc1ccc(-c2nnc(-c3cc(OC(F)(F)F)ccc3N3CCOCC3)o2)cc1OC 10.1016/j.bmcl.2019.03.016
23579328 199982 0 None - 1 Rat 7.9 pIC50 = 7.9 Functional
Antagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPRAntagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPR
ChEMBL 332 3 0 5 3.9 COc1cccc(-c2noc3cc(-c4ccccc4)n(C)c(=O)c23)c1 10.1016/j.bmcl.2009.11.070
CHEMBL595170 199982 0 None - 1 Rat 7.9 pIC50 = 7.9 Functional
Antagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPRAntagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPR
ChEMBL 332 3 0 5 3.9 COc1cccc(-c2noc3cc(-c4ccccc4)n(C)c(=O)c23)c1 10.1016/j.bmcl.2009.11.070
162651975 180212 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 416 7 0 6 4.9 CCOC(=O)c1cnc2c(OC)cccc2c1-c1ccn(Cc2ccccc2OC)c1 10.1016/j.bmcl.2020.127529
CHEMBL4749716 180212 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 416 7 0 6 4.9 CCOC(=O)c1cnc2c(OC)cccc2c1-c1ccn(Cc2ccccc2OC)c1 10.1016/j.bmcl.2020.127529
155540837 172505 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assay
ChEMBL 442 9 1 8 3.8 COc1cc(F)c(OCCNc2cc(OC(F)(F)F)ccc2-n2cncn2)cc1OC 10.1021/acs.jmedchem.8b01810
CHEMBL4483431 172505 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assay
ChEMBL 442 9 1 8 3.8 COc1cc(F)c(OCCNc2cc(OC(F)(F)F)ccc2-n2cncn2)cc1OC 10.1021/acs.jmedchem.8b01810
155558932 174817 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assay
ChEMBL 450 8 1 7 4.5 COc1cc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OCC(C)C 10.1021/acs.jmedchem.8b01810
CHEMBL4562432 174817 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assay
ChEMBL 450 8 1 7 4.5 COc1cc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OCC(C)C 10.1021/acs.jmedchem.8b01810
155558932 174817 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assay
ChEMBL 450 8 1 7 4.5 COc1cc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OCC(C)C 10.1021/acs.jmedchem.8b01810
CHEMBL4562432 174817 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assay
ChEMBL 450 8 1 7 4.5 COc1cc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OCC(C)C 10.1021/acs.jmedchem.8b01810
155534974 171984 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 446 6 0 8 4.7 COc1ccc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-c3ccnn3C)o2)cc1OC 10.1016/j.bmcl.2022.128923
CHEMBL4470938 171984 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 446 6 0 8 4.7 COc1ccc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-c3ccnn3C)o2)cc1OC 10.1016/j.bmcl.2022.128923
155534974 171984 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 446 6 0 8 4.7 COc1ccc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-c3ccnn3C)o2)cc1OC 10.1016/j.bmcl.2022.128923
CHEMBL4470938 171984 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 446 6 0 8 4.7 COc1ccc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-c3ccnn3C)o2)cc1OC 10.1016/j.bmcl.2022.128923
162660292 181215 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 435 6 0 7 4.1 CCOC(=O)c1cnc2c(OC)cccc2c1N1CCN(c2ccccc2OC)C(C)C1 10.1016/j.bmcl.2020.127529
CHEMBL4761295 181215 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 435 6 0 7 4.1 CCOC(=O)c1cnc2c(OC)cccc2c1N1CCN(c2ccccc2OC)C(C)C1 10.1016/j.bmcl.2020.127529
155544100 173311 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assay
ChEMBL 440 9 1 7 4.4 COc1cc(F)c(CCCNc2cc(OC(F)(F)F)ccc2-n2cncn2)cc1OC 10.1021/acs.jmedchem.8b01810
CHEMBL4526190 173311 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assay
ChEMBL 440 9 1 7 4.4 COc1cc(F)c(CCCNc2cc(OC(F)(F)F)ccc2-n2cncn2)cc1OC 10.1021/acs.jmedchem.8b01810
155518070 170249 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 473 8 0 9 4.7 COc1cc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-n3cncn3)o2)ccc1OCC1CC1 10.1016/j.bmcl.2019.03.016
CHEMBL4445828 170249 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 473 8 0 9 4.7 COc1cc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-n3cncn3)o2)ccc1OCC1CC1 10.1016/j.bmcl.2019.03.016
155544100 173311 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assay
ChEMBL 440 9 1 7 4.4 COc1cc(F)c(CCCNc2cc(OC(F)(F)F)ccc2-n2cncn2)cc1OC 10.1021/acs.jmedchem.8b01810
CHEMBL4526190 173311 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assay
ChEMBL 440 9 1 7 4.4 COc1cc(F)c(CCCNc2cc(OC(F)(F)F)ccc2-n2cncn2)cc1OC 10.1021/acs.jmedchem.8b01810
155534974 171984 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 446 6 0 8 4.7 COc1ccc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-c3ccnn3C)o2)cc1OC 10.1016/j.bmcl.2019.03.016
CHEMBL4470938 171984 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 446 6 0 8 4.7 COc1ccc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-c3ccnn3C)o2)cc1OC 10.1016/j.bmcl.2019.03.016
155564419 175267 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 433 6 0 9 3.9 COc1ccc(-c2noc(-c3cc(OC(F)(F)F)ccc3-n3cncn3)n2)cc1OC 10.1016/j.bmcl.2019.03.016
CHEMBL4572513 175267 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 433 6 0 9 3.9 COc1ccc(-c2noc(-c3cc(OC(F)(F)F)ccc3-n3cncn3)n2)cc1OC 10.1016/j.bmcl.2019.03.016
145951124 162722 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 462 7 1 7 4.7 COc1cc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OC1CCCC1 10.1021/acsmedchemlett.7b00429
CHEMBL4170997 162722 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 462 7 1 7 4.7 COc1cc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OC1CCCC1 10.1021/acsmedchemlett.7b00429
22137718 199662 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPRAntagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPR
ChEMBL 345 3 0 5 3.9 CN(C)c1ccc(-c2cc3onc(-c4ccccc4)c3c(=O)n2C)cc1 10.1016/j.bmcl.2009.11.070
CHEMBL592957 199662 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPRAntagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPR
ChEMBL 345 3 0 5 3.9 CN(C)c1ccc(-c2cc3onc(-c4ccccc4)c3c(=O)n2C)cc1 10.1016/j.bmcl.2009.11.070
145951124 162722 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 462 7 1 7 4.7 COc1cc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OC1CCCC1 10.1021/acsmedchemlett.7b00429
CHEMBL4170997 162722 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 462 7 1 7 4.7 COc1cc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OC1CCCC1 10.1021/acsmedchemlett.7b00429
155522547 170823 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assay
ChEMBL 462 8 1 7 4.6 COc1cc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OCC1CCC1 10.1021/acs.jmedchem.8b01810
CHEMBL4453525 170823 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assay
ChEMBL 462 8 1 7 4.6 COc1cc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OCC1CCC1 10.1021/acs.jmedchem.8b01810
155522547 170823 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assay
ChEMBL 462 8 1 7 4.6 COc1cc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OCC1CCC1 10.1021/acs.jmedchem.8b01810
CHEMBL4453525 170823 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assay
ChEMBL 462 8 1 7 4.6 COc1cc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OCC1CCC1 10.1021/acs.jmedchem.8b01810
22137720 200010 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
Antagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPRAntagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPR
ChEMBL 344 4 0 4 4.8 CCCc1ccc(-c2cc3onc(-c4ccccc4)c3c(=O)n2C)cc1 10.1016/j.bmcl.2009.11.070
CHEMBL595388 200010 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
Antagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPRAntagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPR
ChEMBL 344 4 0 4 4.8 CCCc1ccc(-c2cc3onc(-c4ccccc4)c3c(=O)n2C)cc1 10.1016/j.bmcl.2009.11.070
168293140 192125 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 382 5 1 6 4.5 COc1ccc(-c2nnc(-c3cc(Cl)ccc3-c3cn[nH]c3)o2)cc1OC 10.1016/j.bmcl.2022.128923
CHEMBL5203522 192125 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 382 5 1 6 4.5 COc1ccc(-c2nnc(-c3cc(Cl)ccc3-c3cn[nH]c3)o2)cc1OC 10.1016/j.bmcl.2022.128923
162652806 180468 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 422 6 0 8 3.2 CCOC(=O)c1cnc2c(OC)cccc2c1N1CCN(c2cccnc2OC)CC1 10.1016/j.bmcl.2020.127529
CHEMBL4752880 180468 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 422 6 0 8 3.2 CCOC(=O)c1cnc2c(OC)cccc2c1N1CCN(c2cccnc2OC)CC1 10.1016/j.bmcl.2020.127529
162670465 182896 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 442 7 0 6 5.9 CCOC(=O)c1cnc2c(OC)cccc2c1-c1ccc(-c2ccccc2OC(C)C)nc1 10.1016/j.bmcl.2020.127529
CHEMBL4792160 182896 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 442 7 0 6 5.9 CCOC(=O)c1cnc2c(OC)cccc2c1-c1ccc(-c2ccccc2OC(C)C)nc1 10.1016/j.bmcl.2020.127529
162676429 183472 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 435 6 0 7 4.1 CCOC(=O)c1cnc2c(OC)cccc2c1N1CCN(c2ccccc2OC)CC1C 10.1016/j.bmcl.2020.127529
CHEMBL4799243 183472 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 435 6 0 7 4.1 CCOC(=O)c1cnc2c(OC)cccc2c1N1CCN(c2ccccc2OC)CC1C 10.1016/j.bmcl.2020.127529
10456810 107879 0 None -123 5 Human 4.8 pIC50 = 4.8 Functional
Antagonistic activity against metabotropic glutamate receptor 7 (mGluR7) was evaluatedAntagonistic activity against metabotropic glutamate receptor 7 (mGluR7) 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 107879 0 None -123 5 Human 4.8 pIC50 = 4.8 Functional
Antagonistic activity against metabotropic glutamate receptor 7 (mGluR7) was evaluatedAntagonistic activity against metabotropic glutamate receptor 7 (mGluR7) 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
155526431 171124 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 473 7 0 9 4.8 COc1cc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-n3cncn3)o2)ccc1OC1CCC1 10.1016/j.bmcl.2019.03.016
CHEMBL4458158 171124 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 473 7 0 9 4.8 COc1cc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-n3cncn3)o2)ccc1OC1CCC1 10.1016/j.bmcl.2019.03.016
155531347 171639 0 None -1 2 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 433 6 0 9 3.9 COc1ccc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-n3cncn3)o2)cc1OC 10.1016/j.bmcl.2019.03.016
CHEMBL4465794 171639 0 None -1 2 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 433 6 0 9 3.9 COc1ccc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-n3cncn3)o2)cc1OC 10.1016/j.bmcl.2019.03.016
168293140 192125 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 382 5 1 6 4.5 COc1ccc(-c2nnc(-c3cc(Cl)ccc3-c3cn[nH]c3)o2)cc1OC 10.1016/j.bmcl.2022.128923
CHEMBL5203522 192125 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 382 5 1 6 4.5 COc1ccc(-c2nnc(-c3cc(Cl)ccc3-c3cn[nH]c3)o2)cc1OC 10.1016/j.bmcl.2022.128923
168295910 192390 0 None 1 2 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 396 5 0 7 4.5 COc1ccc(-c2nnc(-c3cc(Cl)ccc3-c3ccnn3C)o2)cc1OC 10.1016/j.bmcl.2022.128923
CHEMBL5207640 192390 0 None 1 2 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 396 5 0 7 4.5 COc1ccc(-c2nnc(-c3cc(Cl)ccc3-c3ccnn3C)o2)cc1OC 10.1016/j.bmcl.2022.128923
168295910 192390 0 None 1 2 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 396 5 0 7 4.5 COc1ccc(-c2nnc(-c3cc(Cl)ccc3-c3ccnn3C)o2)cc1OC 10.1016/j.bmcl.2022.128923
CHEMBL5207640 192390 0 None 1 2 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 396 5 0 7 4.5 COc1ccc(-c2nnc(-c3cc(Cl)ccc3-c3ccnn3C)o2)cc1OC 10.1016/j.bmcl.2022.128923
155530175 171486 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assay
ChEMBL 422 9 1 7 4.2 COc1ccc(CCCNc2cc(OC(F)(F)F)ccc2-n2cncn2)cc1OC 10.1021/acs.jmedchem.8b01810
CHEMBL4463654 171486 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assay
ChEMBL 422 9 1 7 4.2 COc1ccc(CCCNc2cc(OC(F)(F)F)ccc2-n2cncn2)cc1OC 10.1021/acs.jmedchem.8b01810
155530175 171486 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assay
ChEMBL 422 9 1 7 4.2 COc1ccc(CCCNc2cc(OC(F)(F)F)ccc2-n2cncn2)cc1OC 10.1021/acs.jmedchem.8b01810
CHEMBL4463654 171486 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assay
ChEMBL 422 9 1 7 4.2 COc1ccc(CCCNc2cc(OC(F)(F)F)ccc2-n2cncn2)cc1OC 10.1021/acs.jmedchem.8b01810
155555580 174384 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 432 6 0 8 4.5 COc1ccc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-n3cccn3)o2)cc1OC 10.1016/j.bmcl.2022.128923
CHEMBL4552061 174384 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 432 6 0 8 4.5 COc1ccc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-n3cccn3)o2)cc1OC 10.1016/j.bmcl.2022.128923
168276104 190271 0 None 2 2 Rat 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 382 5 0 7 4.3 COc1ccc(-c2coc(-c3cc(Cl)ccc3-n3cncn3)n2)cc1OC 10.1016/j.bmcl.2022.128923
CHEMBL5175583 190271 0 None 2 2 Rat 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 382 5 0 7 4.3 COc1ccc(-c2coc(-c3cc(Cl)ccc3-n3cncn3)n2)cc1OC 10.1016/j.bmcl.2022.128923
162660582 181349 0 None - 1 Rat 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 451 7 0 8 3.8 CCOC(=O)c1cnc2c(OC)cccc2c1N1CCN(c2ccc(OC)cc2OC)CC1 10.1016/j.bmcl.2020.127529
CHEMBL4763036 181349 0 None - 1 Rat 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 451 7 0 8 3.8 CCOC(=O)c1cnc2c(OC)cccc2c1N1CCN(c2ccc(OC)cc2OC)CC1 10.1016/j.bmcl.2020.127529
44329042 169083 0 None -257 5 Human 4.7 pIC50 = 4.7 Functional
Antagonistic activity against metabotropic glutamate receptor 7 (mGluR7) was evaluatedAntagonistic activity against metabotropic glutamate receptor 7 (mGluR7) 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 169083 0 None -257 5 Human 4.7 pIC50 = 4.7 Functional
Antagonistic activity against metabotropic glutamate receptor 7 (mGluR7) was evaluatedAntagonistic activity against metabotropic glutamate receptor 7 (mGluR7) 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
155531347 171639 0 None -1 2 Rat 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 433 6 0 9 3.9 COc1ccc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-n3cncn3)o2)cc1OC 10.1016/j.bmcl.2022.128923
CHEMBL4465794 171639 0 None -1 2 Rat 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 433 6 0 9 3.9 COc1ccc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-n3cncn3)o2)cc1OC 10.1016/j.bmcl.2022.128923
155532310 171737 0 None 2 2 Rat 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 432 6 1 7 4.7 COc1ccc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-c3cn[nH]c3)o2)cc1OC 10.1016/j.bmcl.2022.128923
CHEMBL4467224 171737 0 None 2 2 Rat 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 432 6 1 7 4.7 COc1ccc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-c3cn[nH]c3)o2)cc1OC 10.1016/j.bmcl.2022.128923
155555580 174384 0 None - 1 Rat 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 432 6 0 8 4.5 COc1ccc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-n3cccn3)o2)cc1OC 10.1016/j.bmcl.2022.128923
CHEMBL4552061 174384 0 None - 1 Rat 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 432 6 0 8 4.5 COc1ccc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-n3cccn3)o2)cc1OC 10.1016/j.bmcl.2022.128923
168276104 190271 0 None 2 2 Rat 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 382 5 0 7 4.3 COc1ccc(-c2coc(-c3cc(Cl)ccc3-n3cncn3)n2)cc1OC 10.1016/j.bmcl.2022.128923
CHEMBL5175583 190271 0 None 2 2 Rat 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 382 5 0 7 4.3 COc1ccc(-c2coc(-c3cc(Cl)ccc3-n3cncn3)n2)cc1OC 10.1016/j.bmcl.2022.128923
4250909 2476 21 None - 1 Rat 7.7 pIC50 = 7.7 Functional
Antagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPRAntagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPR
ChEMBL 302 2 0 4 3.9 Cn1c(cc2c(c1=O)c(no2)c1ccccc1)c1ccccc1 10.1016/j.bmcl.2009.11.070
6218 2476 21 None - 1 Rat 7.7 pIC50 = 7.7 Functional
Antagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPRAntagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPR
ChEMBL 302 2 0 4 3.9 Cn1c(cc2c(c1=O)c(no2)c1ccccc1)c1ccccc1 10.1016/j.bmcl.2009.11.070
CHEMBL595840 2476 21 None - 1 Rat 7.7 pIC50 = 7.7 Functional
Antagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPRAntagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPR
ChEMBL 302 2 0 4 3.9 Cn1c(cc2c(c1=O)c(no2)c1ccccc1)c1ccccc1 10.1016/j.bmcl.2009.11.070
155531347 171639 0 None -1 2 Rat 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 433 6 0 9 3.9 COc1ccc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-n3cncn3)o2)cc1OC 10.1016/j.bmcl.2022.128923
CHEMBL4465794 171639 0 None -1 2 Rat 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 433 6 0 9 3.9 COc1ccc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-n3cncn3)o2)cc1OC 10.1016/j.bmcl.2022.128923
155532310 171737 0 None 2 2 Rat 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 432 6 1 7 4.7 COc1ccc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-c3cn[nH]c3)o2)cc1OC 10.1016/j.bmcl.2022.128923
CHEMBL4467224 171737 0 None 2 2 Rat 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 432 6 1 7 4.7 COc1ccc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-c3cn[nH]c3)o2)cc1OC 10.1016/j.bmcl.2022.128923
155555580 174384 0 None - 1 Rat 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 432 6 0 8 4.5 COc1ccc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-n3cccn3)o2)cc1OC 10.1016/j.bmcl.2019.03.016
CHEMBL4552061 174384 0 None - 1 Rat 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 432 6 0 8 4.5 COc1ccc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-n3cccn3)o2)cc1OC 10.1016/j.bmcl.2019.03.016
155516175 170043 0 None - 1 Rat 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 432 6 0 8 4.5 COc1ccc(-c2cnc(-c3cc(OC(F)(F)F)ccc3-n3cncn3)o2)cc1OC 10.1016/j.bmcl.2019.03.016
CHEMBL4442872 170043 0 None - 1 Rat 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 432 6 0 8 4.5 COc1ccc(-c2cnc(-c3cc(OC(F)(F)F)ccc3-n3cncn3)o2)cc1OC 10.1016/j.bmcl.2019.03.016
9884036 200012 32 None - 1 Rat 7.7 pIC50 = 7.7 Functional
Antagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPRAntagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPR
ChEMBL 332 3 0 5 3.9 COc1ccccc1-c1noc2cc(-c3ccccc3)n(C)c(=O)c12 10.1016/j.bmcl.2009.11.070
CHEMBL595402 200012 32 None - 1 Rat 7.7 pIC50 = 7.7 Functional
Antagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPRAntagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPR
ChEMBL 332 3 0 5 3.9 COc1ccccc1-c1noc2cc(-c3ccccc3)n(C)c(=O)c12 10.1016/j.bmcl.2009.11.070
22137728 199892 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPRAntagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPR
ChEMBL 350 3 0 5 4.0 COc1ccc(-c2cc3onc(-c4ccccc4)c3c(=O)n2C)cc1F 10.1016/j.bmcl.2009.11.070
CHEMBL594648 199892 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPRAntagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPR
ChEMBL 350 3 0 5 4.0 COc1ccc(-c2cc3onc(-c4ccccc4)c3c(=O)n2C)cc1F 10.1016/j.bmcl.2009.11.070
162651166 180333 0 None - 1 Rat 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 439 6 0 7 3.9 CCOC(=O)c1cnc2c(OC)cccc2c1N1CCN(c2cc(F)ccc2OC)CC1 10.1016/j.bmcl.2020.127529
CHEMBL4751217 180333 0 None - 1 Rat 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 439 6 0 7 3.9 CCOC(=O)c1cnc2c(OC)cccc2c1N1CCN(c2cc(F)ccc2OC)CC1 10.1016/j.bmcl.2020.127529
162672770 183137 0 None - 1 Rat 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 462 7 0 7 5.3 CCOC(=O)c1cnc2c(OC)cccc2c1-c1cc(F)c(-c2ccccc2OC)nc1OC 10.1016/j.bmcl.2020.127529
CHEMBL4795157 183137 0 None - 1 Rat 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 462 7 0 7 5.3 CCOC(=O)c1cnc2c(OC)cccc2c1-c1cc(F)c(-c2ccccc2OC)nc1OC 10.1016/j.bmcl.2020.127529
20304994 154664 0 None - 1 Rat 7.7 pIC50 = 7.7 Functional
Antagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPRAntagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPR
ChEMBL 332 3 0 5 3.9 COc1ccc(-c2cc3onc(-c4ccccc4)c3c(=O)n2C)cc1 10.1016/j.bmcl.2009.11.070
CHEMBL399602 154664 0 None - 1 Rat 7.7 pIC50 = 7.7 Functional
Antagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPRAntagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPR
ChEMBL 332 3 0 5 3.9 COc1ccc(-c2cc3onc(-c4ccccc4)c3c(=O)n2C)cc1 10.1016/j.bmcl.2009.11.070
155532310 171737 0 None 2 2 Rat 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 432 6 1 7 4.7 COc1ccc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-c3cn[nH]c3)o2)cc1OC 10.1016/j.bmcl.2019.03.016
CHEMBL4467224 171737 0 None 2 2 Rat 5.7 pIC50 = 5.7 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 432 6 1 7 4.7 COc1ccc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-c3cn[nH]c3)o2)cc1OC 10.1016/j.bmcl.2019.03.016
162652703 180374 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 449 7 0 7 4.5 CCOC(=O)c1cnc2c(OC)cccc2c1N1CCN(c2ccccc2OC(C)C)CC1 10.1016/j.bmcl.2020.127529
CHEMBL4751662 180374 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 449 7 0 7 4.5 CCOC(=O)c1cnc2c(OC)cccc2c1N1CCN(c2ccccc2OC(C)C)CC1 10.1016/j.bmcl.2020.127529
44328850 208051 0 None -22 4 Human 4.6 pIC50 = 4.6 Functional
Antagonistic activity against metabotropic glutamate receptor 7 (mGluR7) was evaluatedAntagonistic activity against metabotropic glutamate receptor 7 (mGluR7) 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 208051 0 None -22 4 Human 4.6 pIC50 = 4.6 Functional
Antagonistic activity against metabotropic glutamate receptor 7 (mGluR7) was evaluatedAntagonistic activity against metabotropic glutamate receptor 7 (mGluR7) 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
155519939 170371 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 433 6 0 9 3.9 COc1ccc(-c2nc(-c3cc(OC(F)(F)F)ccc3-n3cncn3)no2)cc1OC 10.1016/j.bmcl.2019.03.016
CHEMBL4447704 170371 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 433 6 0 9 3.9 COc1ccc(-c2nc(-c3cc(OC(F)(F)F)ccc3-n3cncn3)no2)cc1OC 10.1016/j.bmcl.2019.03.016
168275316 190206 0 None 1 2 Rat 5.6 pIC50 = 5.6 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 433 6 0 7 4.7 CCOC(=O)c1cnc2c(OC)cccc2c1-c1ccc(-c2cc(F)cnc2OC)nc1 10.1016/j.bmcl.2022.128923
CHEMBL5174531 190206 0 None 1 2 Rat 5.6 pIC50 = 5.6 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 433 6 0 7 4.7 CCOC(=O)c1cnc2c(OC)cccc2c1-c1ccc(-c2cc(F)cnc2OC)nc1 10.1016/j.bmcl.2022.128923
168275316 190206 0 None 1 2 Rat 5.6 pIC50 = 5.6 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 433 6 0 7 4.7 CCOC(=O)c1cnc2c(OC)cccc2c1-c1ccc(-c2cc(F)cnc2OC)nc1 10.1016/j.bmcl.2022.128923
CHEMBL5174531 190206 0 None 1 2 Rat 5.6 pIC50 = 5.6 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 433 6 0 7 4.7 CCOC(=O)c1cnc2c(OC)cccc2c1-c1ccc(-c2cc(F)cnc2OC)nc1 10.1016/j.bmcl.2022.128923
23579325 200136 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Antagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPRAntagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPR
ChEMBL 303 2 0 5 3.3 Cn1c(-c2ccccc2)cc2onc(-c3cccnc3)c2c1=O 10.1016/j.bmcl.2009.11.070
CHEMBL596274 200136 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Antagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPRAntagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPR
ChEMBL 303 2 0 5 3.3 Cn1c(-c2ccccc2)cc2onc(-c3cccnc3)c2c1=O 10.1016/j.bmcl.2009.11.070
162666795 182355 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 415 6 0 7 4.6 CCOC(=O)c1cnc2c(OC)cccc2c1-c1cnc(-c2ccccc2OC)nc1 10.1016/j.bmcl.2020.127529
CHEMBL4784728 182355 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 415 6 0 7 4.6 CCOC(=O)c1cnc2c(OC)cccc2c1-c1cnc(-c2ccccc2OC)nc1 10.1016/j.bmcl.2020.127529
168284838 191295 0 None -3 2 Rat 5.6 pIC50 = 5.6 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 401 5 0 8 3.8 COc1cc(-c2noc(-c3cc(Cl)ccc3-n3cncn3)n2)cc(F)c1OC 10.1016/j.bmcl.2022.128923
CHEMBL5190992 191295 0 None -3 2 Rat 5.6 pIC50 = 5.6 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 401 5 0 8 3.8 COc1cc(-c2noc(-c3cc(Cl)ccc3-n3cncn3)n2)cc(F)c1OC 10.1016/j.bmcl.2022.128923
3341 2584 38 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Allosteric antagonist activity at rat mGlu7 receptor expressed in CHO cell co-expressing Galpha15 (unknown origin) assessed as reduction in L-AP4-induced intracellular Ca2+ mobilizationAllosteric antagonist activity at rat mGlu7 receptor expressed in CHO cell co-expressing Galpha15 (unknown origin) assessed as reduction in L-AP4-induced intracellular Ca2+ mobilization
ChEMBL 333 3 0 6 3.3 COc1ccc(cc1)c1cc2onc(c2c(=O)n1C)c1ccncc1 10.1039/C8MD00524A
9945530 2584 38 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Allosteric antagonist activity at rat mGlu7 receptor expressed in CHO cell co-expressing Galpha15 (unknown origin) assessed as reduction in L-AP4-induced intracellular Ca2+ mobilizationAllosteric antagonist activity at rat mGlu7 receptor expressed in CHO cell co-expressing Galpha15 (unknown origin) assessed as reduction in L-AP4-induced intracellular Ca2+ mobilization
ChEMBL 333 3 0 6 3.3 COc1ccc(cc1)c1cc2onc(c2c(=O)n1C)c1ccncc1 10.1039/C8MD00524A
CHEMBL593489 2584 38 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Allosteric antagonist activity at rat mGlu7 receptor expressed in CHO cell co-expressing Galpha15 (unknown origin) assessed as reduction in L-AP4-induced intracellular Ca2+ mobilizationAllosteric antagonist activity at rat mGlu7 receptor expressed in CHO cell co-expressing Galpha15 (unknown origin) assessed as reduction in L-AP4-induced intracellular Ca2+ mobilization
ChEMBL 333 3 0 6 3.3 COc1ccc(cc1)c1cc2onc(c2c(=O)n1C)c1ccncc1 10.1039/C8MD00524A
3341 2584 38 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPRAntagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPR
ChEMBL 333 3 0 6 3.3 COc1ccc(cc1)c1cc2onc(c2c(=O)n1C)c1ccncc1 10.1016/j.bmcl.2009.11.070
9945530 2584 38 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPRAntagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPR
ChEMBL 333 3 0 6 3.3 COc1ccc(cc1)c1cc2onc(c2c(=O)n1C)c1ccncc1 10.1016/j.bmcl.2009.11.070
CHEMBL593489 2584 38 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPRAntagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPR
ChEMBL 333 3 0 6 3.3 COc1ccc(cc1)c1cc2onc(c2c(=O)n1C)c1ccncc1 10.1016/j.bmcl.2009.11.070
22015572 154665 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPRAntagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPR
ChEMBL 346 2 0 6 3.6 Cn1c(-c2ccc3c(c2)OCO3)cc2onc(-c3ccccc3)c2c1=O 10.1016/j.bmcl.2009.11.070
CHEMBL399603 154665 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPRAntagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPR
ChEMBL 346 2 0 6 3.6 Cn1c(-c2ccc3c(c2)OCO3)cc2onc(-c3ccccc3)c2c1=O 10.1016/j.bmcl.2009.11.070
44329033 207980 0 None -66 5 Human 5.6 pIC50 = 5.6 Functional
Antagonistic activity against metabotropic glutamate receptor 7 (mGluR7) was evaluatedAntagonistic activity against metabotropic glutamate receptor 7 (mGluR7) 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 207980 0 None -66 5 Human 5.6 pIC50 = 5.6 Functional
Antagonistic activity against metabotropic glutamate receptor 7 (mGluR7) was evaluatedAntagonistic activity against metabotropic glutamate receptor 7 (mGluR7) 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
168292732 192088 0 None 3 2 Rat 6.6 pIC50 = 6.6 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 480 9 1 9 3.0 COc1cc(OCC(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OC1COC1 10.1016/j.bmcl.2022.128923
CHEMBL5202961 192088 0 None 3 2 Rat 6.6 pIC50 = 6.6 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 480 9 1 9 3.0 COc1cc(OCC(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OC1COC1 10.1016/j.bmcl.2022.128923
168292732 192088 0 None 3 2 Rat 6.6 pIC50 = 6.6 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 480 9 1 9 3.0 COc1cc(OCC(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OC1COC1 10.1016/j.bmcl.2022.128923
CHEMBL5202961 192088 0 None 3 2 Rat 6.6 pIC50 = 6.6 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 480 9 1 9 3.0 COc1cc(OCC(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OC1COC1 10.1016/j.bmcl.2022.128923
168284838 191295 0 None -3 2 Rat 5.6 pIC50 = 5.6 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 401 5 0 8 3.8 COc1cc(-c2noc(-c3cc(Cl)ccc3-n3cncn3)n2)cc(F)c1OC 10.1016/j.bmcl.2022.128923
CHEMBL5190992 191295 0 None -3 2 Rat 5.6 pIC50 = 5.6 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 401 5 0 8 3.8 COc1cc(-c2noc(-c3cc(Cl)ccc3-n3cncn3)n2)cc(F)c1OC 10.1016/j.bmcl.2022.128923
162675680 183433 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 414 6 0 6 5.2 CCOC(=O)c1cnc2c(OC)cccc2c1-c1ccc(-c2ccccc2OC)cn1 10.1016/j.bmcl.2020.127529
CHEMBL4798689 183433 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 414 6 0 6 5.2 CCOC(=O)c1cnc2c(OC)cccc2c1-c1ccc(-c2ccccc2OC)cn1 10.1016/j.bmcl.2020.127529
155553348 174172 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assay
ChEMBL 476 8 1 7 5.0 COc1cc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OCC1CCCC1 10.1021/acs.jmedchem.8b01810
CHEMBL4547249 174172 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assay
ChEMBL 476 8 1 7 5.0 COc1cc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OCC1CCCC1 10.1021/acs.jmedchem.8b01810
155553348 174172 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assay
ChEMBL 476 8 1 7 5.0 COc1cc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OCC1CCCC1 10.1021/acs.jmedchem.8b01810
CHEMBL4547249 174172 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assay
ChEMBL 476 8 1 7 5.0 COc1cc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OCC1CCCC1 10.1021/acs.jmedchem.8b01810
20305061 199660 0 None - 1 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPRAntagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPR
ChEMBL 332 3 0 5 3.9 COc1ccc(-c2noc3cc(-c4ccccc4)n(C)c(=O)c23)cc1 10.1016/j.bmcl.2009.11.070
CHEMBL592954 199660 0 None - 1 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPRAntagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPR
ChEMBL 332 3 0 5 3.9 COc1ccc(-c2noc3cc(-c4ccccc4)n(C)c(=O)c23)cc1 10.1016/j.bmcl.2009.11.070
162662540 182034 0 None - 1 Rat 5.5 pIC50 = 5.5 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 413 6 0 5 5.8 CCOC(=O)c1cnc2c(OC)cccc2c1-c1ccc(-c2ccccc2OC)cc1 10.1016/j.bmcl.2020.127529
CHEMBL4780904 182034 0 None - 1 Rat 5.5 pIC50 = 5.5 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 413 6 0 5 5.8 CCOC(=O)c1cnc2c(OC)cccc2c1-c1ccc(-c2ccccc2OC)cc1 10.1016/j.bmcl.2020.127529
162657202 180867 0 None - 1 Rat 5.5 pIC50 = 5.5 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 423 6 0 9 2.5 CCOC(=O)c1cnc2c(OC)cccc2c1N1CCN(c2nccnc2OC)CC1 10.1016/j.bmcl.2020.127529
CHEMBL4757340 180867 0 None - 1 Rat 5.5 pIC50 = 5.5 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 423 6 0 9 2.5 CCOC(=O)c1cnc2c(OC)cccc2c1N1CCN(c2nccnc2OC)CC1 10.1016/j.bmcl.2020.127529
155517838 170214 0 None - 1 Rat 5.5 pIC50 = 5.5 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assay
ChEMBL 484 8 1 7 5.0 COc1cc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OCc1ccccc1 10.1021/acs.jmedchem.8b01810
CHEMBL4445412 170214 0 None - 1 Rat 5.5 pIC50 = 5.5 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assay
ChEMBL 484 8 1 7 5.0 COc1cc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OCc1ccccc1 10.1021/acs.jmedchem.8b01810
22137731 199827 0 None - 1 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPRAntagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPR
ChEMBL 345 3 0 5 3.9 CN(C)c1cccc(-c2cc3onc(-c4ccccc4)c3c(=O)n2C)c1 10.1016/j.bmcl.2009.11.070
CHEMBL594223 199827 0 None - 1 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPRAntagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPR
ChEMBL 345 3 0 5 3.9 CN(C)c1cccc(-c2cc3onc(-c4ccccc4)c3c(=O)n2C)c1 10.1016/j.bmcl.2009.11.070
155517838 170214 0 None - 1 Rat 5.5 pIC50 = 5.5 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assay
ChEMBL 484 8 1 7 5.0 COc1cc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OCc1ccccc1 10.1021/acs.jmedchem.8b01810
CHEMBL4445412 170214 0 None - 1 Rat 5.5 pIC50 = 5.5 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assay
ChEMBL 484 8 1 7 5.0 COc1cc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OCc1ccccc1 10.1021/acs.jmedchem.8b01810
168270781 190045 0 None -4 2 Rat 5.5 pIC50 = 5.5 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 419 5 0 8 3.9 COc1cc(F)c(-c2noc(-c3cc(Cl)ccc3-n3cncn3)n2)c(F)c1OC 10.1016/j.bmcl.2022.128923
CHEMBL5171986 190045 0 None -4 2 Rat 5.5 pIC50 = 5.5 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 419 5 0 8 3.9 COc1cc(F)c(-c2noc(-c3cc(Cl)ccc3-n3cncn3)n2)c(F)c1OC 10.1016/j.bmcl.2022.128923
10196 4056 25 None -1 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assay
ChEMBL 448 8 1 7 4.2 COc1cc(ccc1OCC1CC1)C(=O)Nc1cc(ccc1n1cncn1)OC(F)(F)F 10.1021/acs.jmedchem.8b01810
137321168 4056 25 None -1 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assay
ChEMBL 448 8 1 7 4.2 COc1cc(ccc1OCC1CC1)C(=O)Nc1cc(ccc1n1cncn1)OC(F)(F)F 10.1021/acs.jmedchem.8b01810
CHEMBL4445682 4056 25 None -1 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assay
ChEMBL 448 8 1 7 4.2 COc1cc(ccc1OCC1CC1)C(=O)Nc1cc(ccc1n1cncn1)OC(F)(F)F 10.1021/acs.jmedchem.8b01810
10196 4056 25 None -1 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 448 8 1 7 4.2 COc1cc(ccc1OCC1CC1)C(=O)Nc1cc(ccc1n1cncn1)OC(F)(F)F 10.1016/j.bmcl.2022.128923
137321168 4056 25 None -1 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 448 8 1 7 4.2 COc1cc(ccc1OCC1CC1)C(=O)Nc1cc(ccc1n1cncn1)OC(F)(F)F 10.1016/j.bmcl.2022.128923
CHEMBL4445682 4056 25 None -1 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 448 8 1 7 4.2 COc1cc(ccc1OCC1CC1)C(=O)Nc1cc(ccc1n1cncn1)OC(F)(F)F 10.1016/j.bmcl.2022.128923
162650841 180276 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 444 7 0 7 5.2 CCOC(=O)c1cnc2c(OC)cccc2c1-c1cnc(-c2ccccc2OC)c(OC)c1 10.1016/j.bmcl.2020.127529
CHEMBL4750685 180276 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 444 7 0 7 5.2 CCOC(=O)c1cnc2c(OC)cccc2c1-c1cnc(-c2ccccc2OC)c(OC)c1 10.1016/j.bmcl.2020.127529
10196 4056 25 None -1 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assay
ChEMBL 448 8 1 7 4.2 COc1cc(ccc1OCC1CC1)C(=O)Nc1cc(ccc1n1cncn1)OC(F)(F)F 10.1021/acs.jmedchem.8b01810
137321168 4056 25 None -1 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assay
ChEMBL 448 8 1 7 4.2 COc1cc(ccc1OCC1CC1)C(=O)Nc1cc(ccc1n1cncn1)OC(F)(F)F 10.1021/acs.jmedchem.8b01810
CHEMBL4445682 4056 25 None -1 2 Rat 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assay
ChEMBL 448 8 1 7 4.2 COc1cc(ccc1OCC1CC1)C(=O)Nc1cc(ccc1n1cncn1)OC(F)(F)F 10.1021/acs.jmedchem.8b01810
155522636 170766 0 None - 1 Rat 5.5 pIC50 = 5.5 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 449 6 0 8 5.4 COc1ccc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-c3cscn3)o2)cc1OC 10.1016/j.bmcl.2019.03.016
CHEMBL4452758 170766 0 None - 1 Rat 5.5 pIC50 = 5.5 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 449 6 0 8 5.4 COc1ccc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-c3cscn3)o2)cc1OC 10.1016/j.bmcl.2019.03.016
168270781 190045 0 None -4 2 Rat 5.4 pIC50 = 5.4 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 419 5 0 8 3.9 COc1cc(F)c(-c2noc(-c3cc(Cl)ccc3-n3cncn3)n2)c(F)c1OC 10.1016/j.bmcl.2022.128923
CHEMBL5171986 190045 0 None -4 2 Rat 5.4 pIC50 = 5.4 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 419 5 0 8 3.9 COc1cc(F)c(-c2noc(-c3cc(Cl)ccc3-n3cncn3)n2)c(F)c1OC 10.1016/j.bmcl.2022.128923
162669788 182629 0 None - 1 Rat 5.4 pIC50 = 5.4 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 418 6 0 6 4.7 CCOC(=O)c1cnc2c(OC)cccc2c1C1=CCN(c2ccccc2OC)CC1 10.1016/j.bmcl.2020.127529
CHEMBL4788520 182629 0 None - 1 Rat 5.4 pIC50 = 5.4 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 418 6 0 6 4.7 CCOC(=O)c1cnc2c(OC)cccc2c1C1=CCN(c2ccccc2OC)CC1 10.1016/j.bmcl.2020.127529
162644787 179396 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 428 7 0 6 5.5 CCOC(=O)c1cnc2c(OC)cccc2c1-c1ccc(-c2ccccc2OCC)nc1 10.1016/j.bmcl.2020.127529
CHEMBL4739931 179396 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 428 7 0 6 5.5 CCOC(=O)c1cnc2c(OC)cccc2c1-c1ccc(-c2ccccc2OCC)nc1 10.1016/j.bmcl.2020.127529
162648085 179872 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 430 6 0 6 5.9 CCOC(=O)c1cnc2c(OC)cccc2c1-c1ccc(-c2ccccc2SC)nc1 10.1016/j.bmcl.2020.127529
CHEMBL4745605 179872 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 430 6 0 6 5.9 CCOC(=O)c1cnc2c(OC)cccc2c1-c1ccc(-c2ccccc2SC)nc1 10.1016/j.bmcl.2020.127529
162644735 179424 0 None - 1 Rat 5.4 pIC50 = 5.4 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 416 5 0 7 3.6 CCOC(=O)c1cnc2c(OC)cccc2c1N1CCN(c2ccccc2C#N)CC1 10.1016/j.bmcl.2020.127529
CHEMBL4740263 179424 0 None - 1 Rat 5.4 pIC50 = 5.4 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 416 5 0 7 3.6 CCOC(=O)c1cnc2c(OC)cccc2c1N1CCN(c2ccccc2C#N)CC1 10.1016/j.bmcl.2020.127529
162669906 182614 0 None - 1 Rat 5.4 pIC50 = 5.4 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 341 5 0 6 2.6 CCOC(=O)c1cnccc1N1CCN(c2ccccc2OC)CC1 10.1016/j.bmcl.2020.127529
CHEMBL4788372 182614 0 None - 1 Rat 5.4 pIC50 = 5.4 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 341 5 0 6 2.6 CCOC(=O)c1cnccc1N1CCN(c2ccccc2OC)CC1 10.1016/j.bmcl.2020.127529
155524000 170844 0 None - 1 Rat 5.4 pIC50 = 5.4 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 434 6 0 10 3.3 COc1cc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-n3cncn3)o2)cnc1OC 10.1016/j.bmcl.2019.03.016
CHEMBL4453831 170844 0 None - 1 Rat 5.4 pIC50 = 5.4 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 434 6 0 10 3.3 COc1cc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-n3cncn3)o2)cnc1OC 10.1016/j.bmcl.2019.03.016
162656878 180842 0 None - 1 Rat 5.4 pIC50 = 5.4 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 423 9 0 7 4.0 CCOC(=O)c1cnc2c(OC)cccc2c1N(C)CCN(C)c1ccccc1OC 10.1016/j.bmcl.2020.127529
CHEMBL4757081 180842 0 None - 1 Rat 5.4 pIC50 = 5.4 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 423 9 0 7 4.0 CCOC(=O)c1cnc2c(OC)cccc2c1N(C)CCN(C)c1ccccc1OC 10.1016/j.bmcl.2020.127529
162661401 181528 0 None - 1 Rat 5.4 pIC50 = 5.4 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 397 5 0 7 3.8 CCOC(=O)c1cnc2ccsc2c1N1CCN(c2ccccc2OC)CC1 10.1016/j.bmcl.2020.127529
CHEMBL4765161 181528 0 None - 1 Rat 5.4 pIC50 = 5.4 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 397 5 0 7 3.8 CCOC(=O)c1cnc2ccsc2c1N1CCN(c2ccccc2OC)CC1 10.1016/j.bmcl.2020.127529
162676693 183502 0 None - 1 Rat 5.4 pIC50 = 5.4 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 397 5 0 7 3.8 CCOC(=O)c1cnc2sccc2c1N1CCN(c2ccccc2OC)CC1 10.1016/j.bmcl.2020.127529
CHEMBL4799651 183502 0 None - 1 Rat 5.4 pIC50 = 5.4 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 397 5 0 7 3.8 CCOC(=O)c1cnc2sccc2c1N1CCN(c2ccccc2OC)CC1 10.1016/j.bmcl.2020.127529
155538270 172393 0 None 5 2 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 432 6 0 8 4.5 COc1ccc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-n3ccnc3)o2)cc1OC 10.1016/j.bmcl.2022.128923
CHEMBL4476495 172393 0 None 5 2 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 432 6 0 8 4.5 COc1ccc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-n3ccnc3)o2)cc1OC 10.1016/j.bmcl.2022.128923
145953031 162602 0 None 3 2 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 422 7 1 7 3.8 CCOc1ccc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)cc1OC 10.1016/j.bmcl.2022.128923
CHEMBL4169114 162602 0 None 3 2 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 422 7 1 7 3.8 CCOc1ccc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)cc1OC 10.1016/j.bmcl.2022.128923
22015567 200072 1 None - 1 Rat 7.3 pIC50 = 7.3 Functional
Antagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPRAntagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPR
ChEMBL 316 2 0 4 4.2 Cc1ccc(-c2cc3onc(-c4ccccc4)c3c(=O)n2C)cc1 10.1016/j.bmcl.2009.11.070
CHEMBL595825 200072 1 None - 1 Rat 7.3 pIC50 = 7.3 Functional
Antagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPRAntagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPR
ChEMBL 316 2 0 4 4.2 Cc1ccc(-c2cc3onc(-c4ccccc4)c3c(=O)n2C)cc1 10.1016/j.bmcl.2009.11.070
145953031 162602 0 None 3 2 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 422 7 1 7 3.8 CCOc1ccc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)cc1OC 10.1021/acsmedchemlett.7b00429
CHEMBL4169114 162602 0 None 3 2 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 422 7 1 7 3.8 CCOc1ccc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)cc1OC 10.1021/acsmedchemlett.7b00429
162672067 182974 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 437 6 0 7 4.5 CCOC(=O)c1cnc2c(OC)cccc2c1N1CCN(c2ccccc2SC)CC1 10.1016/j.bmcl.2020.127529
CHEMBL4793197 182974 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 437 6 0 7 4.5 CCOC(=O)c1cnc2c(OC)cccc2c1N1CCN(c2ccccc2SC)CC1 10.1016/j.bmcl.2020.127529
162649213 179985 0 None - 1 Rat 5.3 pIC50 = 5.3 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 435 7 0 7 4.1 CCOC(=O)c1cnc2c(OC)cccc2c1N1CCN(c2ccccc2OCC)CC1 10.1016/j.bmcl.2020.127529
CHEMBL4746927 179985 0 None - 1 Rat 5.3 pIC50 = 5.3 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 435 7 0 7 4.1 CCOC(=O)c1cnc2c(OC)cccc2c1N1CCN(c2ccccc2OCC)CC1 10.1016/j.bmcl.2020.127529
145953031 162602 0 None 3 2 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 422 7 1 7 3.8 CCOc1ccc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)cc1OC 10.1021/acsmedchemlett.7b00429
CHEMBL4169114 162602 0 None 3 2 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 422 7 1 7 3.8 CCOc1ccc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)cc1OC 10.1021/acsmedchemlett.7b00429
162646577 179645 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 415 6 0 7 4.6 CCOC(=O)c1cnc2c(OC)cccc2c1-c1cnc(-c2ccccc2OC)cn1 10.1016/j.bmcl.2020.127529
CHEMBL4743016 179645 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 415 6 0 7 4.6 CCOC(=O)c1cnc2c(OC)cccc2c1-c1cnc(-c2ccccc2OC)cn1 10.1016/j.bmcl.2020.127529
145953031 162602 0 None 3 2 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 422 7 1 7 3.8 CCOc1ccc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)cc1OC 10.1016/j.bmcl.2022.128923
CHEMBL4169114 162602 0 None 3 2 Rat 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 422 7 1 7 3.8 CCOc1ccc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)cc1OC 10.1016/j.bmcl.2022.128923
155538270 172393 0 None 5 2 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 432 6 0 8 4.5 COc1ccc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-n3ccnc3)o2)cc1OC 10.1016/j.bmcl.2019.03.016
CHEMBL4476495 172393 0 None 5 2 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 432 6 0 8 4.5 COc1ccc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-n3ccnc3)o2)cc1OC 10.1016/j.bmcl.2019.03.016
18084474 162080 5 None - 1 Rat 5.2 pIC50 = 5.2 Functional
Negative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 358 5 1 6 3.2 COc1ccc(C(=O)Nc2cc(Cl)ccc2-n2cncn2)cc1OC 10.1021/acsmedchemlett.7b00429
CHEMBL4160779 162080 5 None - 1 Rat 5.2 pIC50 = 5.2 Functional
Negative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 358 5 1 6 3.2 COc1ccc(C(=O)Nc2cc(Cl)ccc2-n2cncn2)cc1OC 10.1021/acsmedchemlett.7b00429
22137722 201665 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Antagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPRAntagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPR
ChEMBL 410 3 0 5 4.6 COc1ccc(-c2cc3onc(-c4ccccc4)c3c(=O)n2C)cc1Br 10.1016/j.bmcl.2009.11.070
CHEMBL606137 201665 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Antagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPRAntagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPR
ChEMBL 410 3 0 5 4.6 COc1ccc(-c2cc3onc(-c4ccccc4)c3c(=O)n2C)cc1Br 10.1016/j.bmcl.2009.11.070
18084474 162080 5 None - 1 Rat 5.2 pIC50 = 5.2 Functional
Negative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 358 5 1 6 3.2 COc1ccc(C(=O)Nc2cc(Cl)ccc2-n2cncn2)cc1OC 10.1021/acsmedchemlett.7b00429
CHEMBL4160779 162080 5 None - 1 Rat 5.2 pIC50 = 5.2 Functional
Negative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 358 5 1 6 3.2 COc1ccc(C(=O)Nc2cc(Cl)ccc2-n2cncn2)cc1OC 10.1021/acsmedchemlett.7b00429
155538549 173257 0 None - 1 Rat 5.2 pIC50 = 5.2 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 449 6 0 7 5.3 COc1ccc(-c2nnc(-c3cc(OC(F)(F)F)ccc3N3CCCCC3)o2)cc1OC 10.1016/j.bmcl.2019.03.016
CHEMBL4524757 173257 0 None - 1 Rat 5.2 pIC50 = 5.2 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 449 6 0 7 5.3 COc1ccc(-c2nnc(-c3cc(OC(F)(F)F)ccc3N3CCCCC3)o2)cc1OC 10.1016/j.bmcl.2019.03.016
155532116 171742 0 None - 1 Rat 5.2 pIC50 = 5.2 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assay
ChEMBL 394 7 1 7 3.8 COc1ccc(CNc2cc(OC(F)(F)F)ccc2-n2cncn2)cc1OC 10.1021/acs.jmedchem.8b01810
CHEMBL4467263 171742 0 None - 1 Rat 5.2 pIC50 = 5.2 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assay
ChEMBL 394 7 1 7 3.8 COc1ccc(CNc2cc(OC(F)(F)F)ccc2-n2cncn2)cc1OC 10.1021/acs.jmedchem.8b01810
155532116 171742 0 None - 1 Rat 5.2 pIC50 = 5.2 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assay
ChEMBL 394 7 1 7 3.8 COc1ccc(CNc2cc(OC(F)(F)F)ccc2-n2cncn2)cc1OC 10.1021/acs.jmedchem.8b01810
CHEMBL4467263 171742 0 None - 1 Rat 5.2 pIC50 = 5.2 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assay
ChEMBL 394 7 1 7 3.8 COc1ccc(CNc2cc(OC(F)(F)F)ccc2-n2cncn2)cc1OC 10.1021/acs.jmedchem.8b01810
162657265 180963 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 414 6 0 6 5.2 CCOC(=O)c1cnc2c(OC)cccc2c1-c1ccc(-c2ccccc2OC)nc1 10.1016/j.bmcl.2020.127529
CHEMBL4758459 180963 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 414 6 0 6 5.2 CCOC(=O)c1cnc2c(OC)cccc2c1-c1ccc(-c2ccccc2OC)nc1 10.1016/j.bmcl.2020.127529
17757064 45387 7 None - 1 Rat 5.2 pIC50 = 5.2 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 409 5 0 6 3.9 CCOC(=O)c1cnc2c(OC)cccc2c1N1CCN(c2ccccc2F)CC1 10.1016/j.bmcl.2020.127529
CHEMBL1527295 45387 7 None - 1 Rat 5.2 pIC50 = 5.2 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 409 5 0 6 3.9 CCOC(=O)c1cnc2c(OC)cccc2c1N1CCN(c2ccccc2F)CC1 10.1016/j.bmcl.2020.127529
44329031 108274 0 None -51 7 Human 5.2 pIC50 = 5.2 Functional
Antagonistic activity against metabotropic glutamate receptor 7 (mGluR7) was evaluatedAntagonistic activity against metabotropic glutamate receptor 7 (mGluR7) 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 108274 0 None -51 7 Human 5.2 pIC50 = 5.2 Functional
Antagonistic activity against metabotropic glutamate receptor 7 (mGluR7) was evaluatedAntagonistic activity against metabotropic glutamate receptor 7 (mGluR7) 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
53391766 299 22 None 5 2 Human 7.2 pIC50 = 7.2 Functional
Negative allosteric modulator activity at human mGlu7 assessed as reduction in Ca2+ mobilization by HTS assayNegative allosteric modulator activity at human mGlu7 assessed as reduction in Ca2+ mobilization by HTS assay
ChEMBL 269 2 0 3 3.8 CCc1nc2c(o1)CC(CC2=O)c1ccc(cc1C)C 10.1039/C8MD00524A
6217 299 22 None 5 2 Human 7.2 pIC50 = 7.2 Functional
Negative allosteric modulator activity at human mGlu7 assessed as reduction in Ca2+ mobilization by HTS assayNegative allosteric modulator activity at human mGlu7 assessed as reduction in Ca2+ mobilization by HTS assay
ChEMBL 269 2 0 3 3.8 CCc1nc2c(o1)CC(CC2=O)c1ccc(cc1C)C 10.1039/C8MD00524A
CHEMBL4174742 299 22 None 5 2 Human 7.2 pIC50 = 7.2 Functional
Negative allosteric modulator activity at human mGlu7 assessed as reduction in Ca2+ mobilization by HTS assayNegative allosteric modulator activity at human mGlu7 assessed as reduction in Ca2+ mobilization by HTS assay
ChEMBL 269 2 0 3 3.8 CCc1nc2c(o1)CC(CC2=O)c1ccc(cc1C)C 10.1039/C8MD00524A
155538270 172393 0 None 5 2 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 432 6 0 8 4.5 COc1ccc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-n3ccnc3)o2)cc1OC 10.1016/j.bmcl.2022.128923
CHEMBL4476495 172393 0 None 5 2 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 432 6 0 8 4.5 COc1ccc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-n3ccnc3)o2)cc1OC 10.1016/j.bmcl.2022.128923
3236309 25353 3 None 15 2 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 421 6 0 7 3.8 CCOC(=O)c1cnc2c(OC)cccc2c1N1CCN(c2ccccc2OC)CC1 10.1016/j.bmcl.2020.127529
CHEMBL1349403 25353 3 None 15 2 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 421 6 0 7 3.8 CCOC(=O)c1cnc2c(OC)cccc2c1N1CCN(c2ccccc2OC)CC1 10.1016/j.bmcl.2020.127529
53391766 299 22 None -5 2 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galphai5 assessed as decrease in glutamate-induced thallium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galphai5 assessed as decrease in glutamate-induced thallium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assay
ChEMBL 269 2 0 3 3.8 CCc1nc2c(o1)CC(CC2=O)c1ccc(cc1C)C 10.1021/acsmedchemlett.7b00317
6217 299 22 None -5 2 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galphai5 assessed as decrease in glutamate-induced thallium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galphai5 assessed as decrease in glutamate-induced thallium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assay
ChEMBL 269 2 0 3 3.8 CCc1nc2c(o1)CC(CC2=O)c1ccc(cc1C)C 10.1021/acsmedchemlett.7b00317
CHEMBL4174742 299 22 None -5 2 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galphai5 assessed as decrease in glutamate-induced thallium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galphai5 assessed as decrease in glutamate-induced thallium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assay
ChEMBL 269 2 0 3 3.8 CCc1nc2c(o1)CC(CC2=O)c1ccc(cc1C)C 10.1021/acsmedchemlett.7b00317
162666389 182383 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 451 7 0 8 3.8 CCOC(=O)c1cnc2c(OC)cc(OC)cc2c1N1CCN(c2ccccc2OC)CC1 10.1016/j.bmcl.2020.127529
CHEMBL4785180 182383 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 451 7 0 8 3.8 CCOC(=O)c1cnc2c(OC)cc(OC)cc2c1N1CCN(c2ccccc2OC)CC1 10.1016/j.bmcl.2020.127529
53391766 299 22 None -5 2 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 269 2 0 3 3.8 CCc1nc2c(o1)CC(CC2=O)c1ccc(cc1C)C 10.1021/acsmedchemlett.7b00429
6217 299 22 None -5 2 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 269 2 0 3 3.8 CCc1nc2c(o1)CC(CC2=O)c1ccc(cc1C)C 10.1021/acsmedchemlett.7b00429
CHEMBL4174742 299 22 None -5 2 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 269 2 0 3 3.8 CCc1nc2c(o1)CC(CC2=O)c1ccc(cc1C)C 10.1021/acsmedchemlett.7b00429
53391766 299 22 None -5 2 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 269 2 0 3 3.8 CCc1nc2c(o1)CC(CC2=O)c1ccc(cc1C)C 10.1021/acsmedchemlett.7b00429
6217 299 22 None -5 2 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 269 2 0 3 3.8 CCc1nc2c(o1)CC(CC2=O)c1ccc(cc1C)C 10.1021/acsmedchemlett.7b00429
CHEMBL4174742 299 22 None -5 2 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 269 2 0 3 3.8 CCc1nc2c(o1)CC(CC2=O)c1ccc(cc1C)C 10.1021/acsmedchemlett.7b00429
44329024 208358 0 None -346 3 Human 4.2 pIC50 = 4.2 Functional
Antagonistic activity against metabotropic glutamate receptor 7 (mGluR7) was evaluatedAntagonistic activity against metabotropic glutamate receptor 7 (mGluR7) 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 208358 0 None -346 3 Human 4.2 pIC50 = 4.2 Functional
Antagonistic activity against metabotropic glutamate receptor 7 (mGluR7) was evaluatedAntagonistic activity against metabotropic glutamate receptor 7 (mGluR7) 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
145958897 162053 2 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 434 7 1 7 4.0 COc1cc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OC1CC1 10.1021/acsmedchemlett.7b00429
CHEMBL4160395 162053 2 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 434 7 1 7 4.0 COc1cc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OC1CC1 10.1021/acsmedchemlett.7b00429
145958897 162053 2 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 434 7 1 7 4.0 COc1cc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OC1CC1 10.1021/acsmedchemlett.7b00429
CHEMBL4160395 162053 2 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 434 7 1 7 4.0 COc1cc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OC1CC1 10.1021/acsmedchemlett.7b00429
20305037 200073 1 None - 1 Rat 7.1 pIC50 = 7.1 Functional
Antagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPRAntagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPR
ChEMBL 320 2 0 4 4.0 Cn1c(-c2ccc(F)cc2)cc2onc(-c3ccccc3)c2c1=O 10.1016/j.bmcl.2009.11.070
CHEMBL595826 200073 1 None - 1 Rat 7.1 pIC50 = 7.1 Functional
Antagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPRAntagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPR
ChEMBL 320 2 0 4 4.0 Cn1c(-c2ccc(F)cc2)cc2onc(-c3ccccc3)c2c1=O 10.1016/j.bmcl.2009.11.070
131801162 4055 16 None -1 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 408 6 1 7 3.4 COc1ccc(cc1OC)C(=O)Nc1cc(ccc1n1ncnc1)OC(F)(F)F 10.1021/acsmedchemlett.7b00429
9703 4055 16 None -1 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 408 6 1 7 3.4 COc1ccc(cc1OC)C(=O)Nc1cc(ccc1n1ncnc1)OC(F)(F)F 10.1021/acsmedchemlett.7b00429
CHEMBL4176971 4055 16 None -1 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 408 6 1 7 3.4 COc1ccc(cc1OC)C(=O)Nc1cc(ccc1n1ncnc1)OC(F)(F)F 10.1021/acsmedchemlett.7b00429
131801162 4055 16 None -1 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assay
ChEMBL 408 6 1 7 3.4 COc1ccc(cc1OC)C(=O)Nc1cc(ccc1n1ncnc1)OC(F)(F)F 10.1021/acs.jmedchem.8b01810
9703 4055 16 None -1 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assay
ChEMBL 408 6 1 7 3.4 COc1ccc(cc1OC)C(=O)Nc1cc(ccc1n1ncnc1)OC(F)(F)F 10.1021/acs.jmedchem.8b01810
CHEMBL4176971 4055 16 None -1 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assay
ChEMBL 408 6 1 7 3.4 COc1ccc(cc1OC)C(=O)Nc1cc(ccc1n1ncnc1)OC(F)(F)F 10.1021/acs.jmedchem.8b01810
131801162 4055 16 None -1 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 408 6 1 7 3.4 COc1ccc(cc1OC)C(=O)Nc1cc(ccc1n1ncnc1)OC(F)(F)F 10.1016/j.bmcl.2022.128923
9703 4055 16 None -1 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 408 6 1 7 3.4 COc1ccc(cc1OC)C(=O)Nc1cc(ccc1n1ncnc1)OC(F)(F)F 10.1016/j.bmcl.2022.128923
CHEMBL4176971 4055 16 None -1 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 408 6 1 7 3.4 COc1ccc(cc1OC)C(=O)Nc1cc(ccc1n1ncnc1)OC(F)(F)F 10.1016/j.bmcl.2022.128923
131801162 4055 16 None -1 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 408 6 1 7 3.4 COc1ccc(cc1OC)C(=O)Nc1cc(ccc1n1ncnc1)OC(F)(F)F 10.1021/acsmedchemlett.7b00429
9703 4055 16 None -1 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 408 6 1 7 3.4 COc1ccc(cc1OC)C(=O)Nc1cc(ccc1n1ncnc1)OC(F)(F)F 10.1021/acsmedchemlett.7b00429
CHEMBL4176971 4055 16 None -1 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 408 6 1 7 3.4 COc1ccc(cc1OC)C(=O)Nc1cc(ccc1n1ncnc1)OC(F)(F)F 10.1021/acsmedchemlett.7b00429
131801162 4055 16 None -1 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assay
ChEMBL 408 6 1 7 3.4 COc1ccc(cc1OC)C(=O)Nc1cc(ccc1n1ncnc1)OC(F)(F)F 10.1021/acs.jmedchem.8b01810
9703 4055 16 None -1 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assay
ChEMBL 408 6 1 7 3.4 COc1ccc(cc1OC)C(=O)Nc1cc(ccc1n1ncnc1)OC(F)(F)F 10.1021/acs.jmedchem.8b01810
CHEMBL4176971 4055 16 None -1 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assay
ChEMBL 408 6 1 7 3.4 COc1ccc(cc1OC)C(=O)Nc1cc(ccc1n1ncnc1)OC(F)(F)F 10.1021/acs.jmedchem.8b01810
44329032 112544 0 None -75 5 Human 5.1 pIC50 = 5.1 Functional
Antagonistic activity against metabotropic glutamate receptor 7 (mGluR7) was evaluatedAntagonistic activity against metabotropic glutamate receptor 7 (mGluR7) 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 112544 0 None -75 5 Human 5.1 pIC50 = 5.1 Functional
Antagonistic activity against metabotropic glutamate receptor 7 (mGluR7) was evaluatedAntagonistic activity against metabotropic glutamate receptor 7 (mGluR7) 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
155511295 169570 0 None - 1 Rat 5.1 pIC50 = 5.1 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 432 6 0 8 4.5 COc1ccc(-c2coc(-c3cc(OC(F)(F)F)ccc3-n3cncn3)n2)cc1OC 10.1016/j.bmcl.2019.03.016
CHEMBL4435790 169570 0 None - 1 Rat 5.1 pIC50 = 5.1 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition for 120 secs followed by L-AP4 addition and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 432 6 0 8 4.5 COc1ccc(-c2coc(-c3cc(OC(F)(F)F)ccc3-n3cncn3)n2)cc1OC 10.1016/j.bmcl.2019.03.016
145958691 162146 0 None 1 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 436 8 1 7 4.2 CCCOc1ccc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)cc1OC 10.1021/acsmedchemlett.7b00429
CHEMBL4161847 162146 0 None 1 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 436 8 1 7 4.2 CCCOc1ccc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)cc1OC 10.1021/acsmedchemlett.7b00429
145955650 162399 0 None 6 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 436 7 1 7 4.2 COc1cc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OC(C)C 10.1021/acsmedchemlett.7b00429
CHEMBL4165849 162399 0 None 6 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 436 7 1 7 4.2 COc1cc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OC(C)C 10.1021/acsmedchemlett.7b00429
145958691 162146 0 None 1 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 436 8 1 7 4.2 CCCOc1ccc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)cc1OC 10.1021/acsmedchemlett.7b00429
CHEMBL4161847 162146 0 None 1 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 436 8 1 7 4.2 CCCOc1ccc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)cc1OC 10.1021/acsmedchemlett.7b00429
145955650 162399 0 None 6 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 436 7 1 7 4.2 COc1cc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OC(C)C 10.1021/acsmedchemlett.7b00429
CHEMBL4165849 162399 0 None 6 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 expressed in HEK cells co-expressing Galpha15 assessed as reduction in L-AP4-induced intracellular calcium flux pretreated for 142 secs followed by glutamate addition and subsequent stimulation of L-AP4 for 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 436 7 1 7 4.2 COc1cc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OC(C)C 10.1021/acsmedchemlett.7b00429
145958691 162146 0 None 1 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 436 8 1 7 4.2 CCCOc1ccc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)cc1OC 10.1016/j.bmcl.2022.128923
CHEMBL4161847 162146 0 None 1 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 436 8 1 7 4.2 CCCOc1ccc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)cc1OC 10.1016/j.bmcl.2022.128923
44329029 163521 0 None -3 6 Human 5.1 pIC50 = 5.1 Functional
Antagonistic activity against metabotropic glutamate receptor 7 (mGluR7) was evaluatedAntagonistic activity against metabotropic glutamate receptor 7 (mGluR7) 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 163521 0 None -3 6 Human 5.1 pIC50 = 5.1 Functional
Antagonistic activity against metabotropic glutamate receptor 7 (mGluR7) was evaluatedAntagonistic activity against metabotropic glutamate receptor 7 (mGluR7) 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
155516091 170055 0 None - 1 Rat 5.1 pIC50 = 5.1 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assay
ChEMBL 344 6 1 6 3.6 COc1ccc(CNc2cc(Cl)ccc2-n2cncn2)cc1OC 10.1021/acs.jmedchem.8b01810
CHEMBL4442991 170055 0 None - 1 Rat 5.1 pIC50 = 5.1 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assay
ChEMBL 344 6 1 6 3.6 COc1ccc(CNc2cc(Cl)ccc2-n2cncn2)cc1OC 10.1021/acs.jmedchem.8b01810
131801162 4055 16 None -1 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 408 6 1 7 3.4 COc1ccc(cc1OC)C(=O)Nc1cc(ccc1n1ncnc1)OC(F)(F)F 10.1016/j.bmcl.2022.128923
9703 4055 16 None -1 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 408 6 1 7 3.4 COc1ccc(cc1OC)C(=O)Nc1cc(ccc1n1ncnc1)OC(F)(F)F 10.1016/j.bmcl.2022.128923
CHEMBL4176971 4055 16 None -1 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 408 6 1 7 3.4 COc1ccc(cc1OC)C(=O)Nc1cc(ccc1n1ncnc1)OC(F)(F)F 10.1016/j.bmcl.2022.128923
145958691 162146 0 None 1 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 436 8 1 7 4.2 CCCOc1ccc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)cc1OC 10.1016/j.bmcl.2022.128923
CHEMBL4161847 162146 0 None 1 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 436 8 1 7 4.2 CCCOc1ccc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)cc1OC 10.1016/j.bmcl.2022.128923
145955650 162399 0 None 6 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 436 7 1 7 4.2 COc1cc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OC(C)C 10.1016/j.bmcl.2022.128923
CHEMBL4165849 162399 0 None 6 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 436 7 1 7 4.2 COc1cc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OC(C)C 10.1016/j.bmcl.2022.128923
155516091 170055 0 None - 1 Rat 5.1 pIC50 = 5.1 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assay
ChEMBL 344 6 1 6 3.6 COc1ccc(CNc2cc(Cl)ccc2-n2cncn2)cc1OC 10.1021/acs.jmedchem.8b01810
CHEMBL4442991 170055 0 None - 1 Rat 5.1 pIC50 = 5.1 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells harboring Ga15 assessed as reduction in L-AP4-induced calcium flux preincubated for 142 secs followed by agonist addition and measured after 120 secs by Fluo-4-AM-dye based fluorescence assay
ChEMBL 344 6 1 6 3.6 COc1ccc(CNc2cc(Cl)ccc2-n2cncn2)cc1OC 10.1021/acs.jmedchem.8b01810
162659630 181292 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 451 7 0 8 3.8 CCOC(=O)c1cnc2c(OC)cccc2c1N1CCN(c2c(OC)cccc2OC)CC1 10.1016/j.bmcl.2020.127529
CHEMBL4762262 181292 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 451 7 0 8 3.8 CCOC(=O)c1cnc2c(OC)cccc2c1N1CCN(c2c(OC)cccc2OC)CC1 10.1016/j.bmcl.2020.127529
162645718 179732 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 458 8 0 7 5.6 CCOC(=O)c1cnc2c(OC)cc(OC)cc2c1-c1ccc(-c2ccccc2OCC)nc1 10.1016/j.bmcl.2020.127529
CHEMBL4744070 179732 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 458 8 0 7 5.6 CCOC(=O)c1cnc2c(OC)cc(OC)cc2c1-c1ccc(-c2ccccc2OCC)nc1 10.1016/j.bmcl.2020.127529
162661367 181482 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 444 7 0 7 5.2 CCOC(=O)c1cnc2c(OC)cc(OC)cc2c1-c1ccc(-c2ccccc2OC)nc1 10.1016/j.bmcl.2020.127529
CHEMBL4764650 181482 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assayNegative allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galpha15 assessed as reduction in calcium mobilization incubated for 142 secs prior to glutamate addition and after 120 secs treated with L-AP4 and measured after 40 secs by Fluo-4 AM dye based fluorescence assay
ChEMBL 444 7 0 7 5.2 CCOC(=O)c1cnc2c(OC)cc(OC)cc2c1-c1ccc(-c2ccccc2OC)nc1 10.1016/j.bmcl.2020.127529
145955650 162399 0 None 6 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 436 7 1 7 4.2 COc1cc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OC(C)C 10.1016/j.bmcl.2022.128923
CHEMBL4165849 162399 0 None 6 2 Rat 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assayNegative allosteric modulation of rat mGlu7 in HEK cells expressing Galpha15 assessed as inhibition of L-AP4-induced response measured by calcium mobilization assay
ChEMBL 436 7 1 7 4.2 COc1cc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OC(C)C 10.1016/j.bmcl.2022.128923
46225494 200142 1 None - 1 Rat 6.0 pIC50 = 6.0 Functional
Antagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPRAntagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPR
ChEMBL 316 3 0 4 4.3 CCn1c(-c2ccccc2)cc2onc(-c3ccccc3)c2c1=O 10.1016/j.bmcl.2009.11.070
CHEMBL596305 200142 1 None - 1 Rat 6.0 pIC50 = 6.0 Functional
Antagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPRAntagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPR
ChEMBL 316 3 0 4 4.3 CCn1c(-c2ccccc2)cc2onc(-c3ccccc3)c2c1=O 10.1016/j.bmcl.2009.11.070
44328753 207754 0 None -323 6 Human 5.0 pIC50 = 5.0 Functional
Antagonistic activity against metabotropic glutamate receptor 7 (mGluR7) was evaluatedAntagonistic activity against metabotropic glutamate receptor 7 (mGluR7) 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 207754 0 None -323 6 Human 5.0 pIC50 = 5.0 Functional
Antagonistic activity against metabotropic glutamate receptor 7 (mGluR7) was evaluatedAntagonistic activity against metabotropic glutamate receptor 7 (mGluR7) 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
22137727 199856 0 None - 1 Rat 7.0 pIC50 = 7.0 Functional
Antagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPRAntagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPR
ChEMBL 370 2 0 4 4.9 Cn1c(-c2cccc(C(F)(F)F)c2)cc2onc(-c3ccccc3)c2c1=O 10.1016/j.bmcl.2009.11.070
CHEMBL594448 199856 0 None - 1 Rat 7.0 pIC50 = 7.0 Functional
Antagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPRAntagonist activity at rat mGluR7 expressed in CHO cells assessed as inhibition of LAP-induced intracellular calcium mobilization by FLIPR
ChEMBL 370 2 0 4 4.9 Cn1c(-c2cccc(C(F)(F)F)c2)cc2onc(-c3ccccc3)c2c1=O 10.1016/j.bmcl.2009.11.070
1378 2417 54 None -169 14 Human 6.0 pIC50 = 6 Functional
Antagonistic activity against metabotropic glutamate receptor 7 (mGluR7) was evaluatedAntagonistic activity against metabotropic glutamate receptor 7 (mGluR7) 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 2417 54 None -169 14 Human 6.0 pIC50 = 6 Functional
Antagonistic activity against metabotropic glutamate receptor 7 (mGluR7) was evaluatedAntagonistic activity against metabotropic glutamate receptor 7 (mGluR7) 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 2417 54 None -169 14 Human 6.0 pIC50 = 6 Functional
Antagonistic activity against metabotropic glutamate receptor 7 (mGluR7) was evaluatedAntagonistic activity against metabotropic glutamate receptor 7 (mGluR7) 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 2417 54 None -169 14 Human 6.0 pIC50 = 6 Functional
Antagonistic activity against metabotropic glutamate receptor 7 (mGluR7) was evaluatedAntagonistic activity against metabotropic glutamate receptor 7 (mGluR7) 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
1378 2417 54 None -169 14 Human 6.0 pKi = 6 Functional
Agonist potency against cloned Metabotropic glutamate receptor 7 (mGluR-7).Agonist potency against cloned Metabotropic glutamate receptor 7 (mGluR-7).
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 2417 54 None -169 14 Human 6.0 pKi = 6 Functional
Agonist potency against cloned Metabotropic glutamate receptor 7 (mGluR-7).Agonist potency against cloned Metabotropic glutamate receptor 7 (mGluR-7).
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 2417 54 None -169 14 Human 6.0 pKi = 6 Functional
Agonist potency against cloned Metabotropic glutamate receptor 7 (mGluR-7).Agonist potency against cloned Metabotropic glutamate receptor 7 (mGluR-7).
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 2417 54 None -169 14 Human 6.0 pKi = 6 Functional
Agonist potency against cloned Metabotropic glutamate receptor 7 (mGluR-7).Agonist potency against cloned Metabotropic glutamate receptor 7 (mGluR-7).
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/jm000007r
1411 2361 66 None -10 6 Human 8.4 pEC50 = 8.4 Functional
NoneNone
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
4120 2361 66 None -10 6 Human 8.4 pEC50 = 8.4 Functional
NoneNone
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
57689797 2361 66 None -10 6 Human 8.4 pEC50 = 8.4 Functional
NoneNone
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
68841 2361 66 None -10 6 Human 8.4 pEC50 = 8.4 Functional
NoneNone
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
CHEMBL284377 2361 66 None -10 6 Human 8.4 pEC50 = 8.4 Functional
NoneNone
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
DB04522 2361 66 None -10 6 Human 8.4 pEC50 = 8.4 Functional
NoneNone
Drug Central 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N None
1310 2315 110 None -309 17 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human mGlu7 receptor expressed in HEK293 assessed as inhibition of forskolin stimulated cAMP productionAgonist activity at human mGlu7 receptor expressed in HEK293 assessed as inhibition of forskolin stimulated cAMP production
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
1369 2315 110 None -309 17 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human mGlu7 receptor expressed in HEK293 assessed as inhibition of forskolin stimulated cAMP productionAgonist activity at human mGlu7 receptor expressed in HEK293 assessed as inhibition of forskolin stimulated cAMP production
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
33032 2315 110 None -309 17 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human mGlu7 receptor expressed in HEK293 assessed as inhibition of forskolin stimulated cAMP productionAgonist activity at human mGlu7 receptor expressed in HEK293 assessed as inhibition of forskolin stimulated cAMP production
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
44272391 2315 110 None -309 17 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human mGlu7 receptor expressed in HEK293 assessed as inhibition of forskolin stimulated cAMP productionAgonist activity at human mGlu7 receptor expressed in HEK293 assessed as inhibition of forskolin stimulated cAMP production
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
88747398 2315 110 None -309 17 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human mGlu7 receptor expressed in HEK293 assessed as inhibition of forskolin stimulated cAMP productionAgonist activity at human mGlu7 receptor expressed in HEK293 assessed as inhibition of forskolin stimulated cAMP production
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
CHEMBL575060 2315 110 None -309 17 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human mGlu7 receptor expressed in HEK293 assessed as inhibition of forskolin stimulated cAMP productionAgonist activity at human mGlu7 receptor expressed in HEK293 assessed as inhibition of forskolin stimulated cAMP production
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
DB00142 2315 110 None -309 17 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human mGlu7 receptor expressed in HEK293 assessed as inhibition of forskolin stimulated cAMP productionAgonist activity at human mGlu7 receptor expressed in HEK293 assessed as inhibition of forskolin stimulated cAMP production
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
1310 2315 110 None -309 17 Human 3.0 pEC50 = 3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
1369 2315 110 None -309 17 Human 3.0 pEC50 = 3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
33032 2315 110 None -309 17 Human 3.0 pEC50 = 3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
44272391 2315 110 None -309 17 Human 3.0 pEC50 = 3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
88747398 2315 110 None -309 17 Human 3.0 pEC50 = 3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
CHEMBL575060 2315 110 None -309 17 Human 3.0 pEC50 = 3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
DB00142 2315 110 None -309 17 Human 3.0 pEC50 = 3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
1410 2274 48 None -1000 8 Human 3.8 pEC50 = 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 9473604
1412 2274 48 None -1000 8 Human 3.8 pEC50 = 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 9473604
179394 2274 48 None -1000 8 Human 3.8 pEC50 = 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 9473604
57689795 2274 48 None -1000 8 Human 3.8 pEC50 = 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 9473604
CHEMBL33567 2274 48 None -1000 8 Human 3.8 pEC50 = 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 9473604
46898088 2366 6 None -263 8 Rat 4.3 pEC50 = 4.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 364 8 5 8 0.4 COc1cc(cc(c1O)[N+](=O)[O-])C(P(=O)(CC[C@@H](C(=O)O)N)O)O 19525404
6739 2366 6 None -263 8 Rat 4.3 pEC50 = 4.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 364 8 5 8 0.4 COc1cc(cc(c1O)[N+](=O)[O-])C(P(=O)(CC[C@@H](C(=O)O)N)O)O 19525404
CHEMBL3114672 2366 6 None -263 8 Rat 4.3 pEC50 = 4.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 364 8 5 8 0.4 COc1cc(cc(c1O)[N+](=O)[O-])C(P(=O)(CC[C@@H](C(=O)O)N)O)O 19525404
1411 2361 66 None -10 6 Human 4.5 pEC50 = 4.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 9473604
4120 2361 66 None -10 6 Human 4.5 pEC50 = 4.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 9473604
57689797 2361 66 None -10 6 Human 4.5 pEC50 = 4.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 9473604
68841 2361 66 None -10 6 Human 4.5 pEC50 = 4.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 9473604
CHEMBL284377 2361 66 None -10 6 Human 4.5 pEC50 = 4.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 9473604
DB04522 2361 66 None -10 6 Human 4.5 pEC50 = 4.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 9473604
6706 2367 8 None -104 8 Human 4.9 pEC50 = 4.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 347 9 5 6 0.2 OC(=O)COc1ccc(cc1)C(P(=O)(CC[C@@H](C(=O)O)N)O)O 22223752
71041983 2367 8 None -104 8 Human 4.9 pEC50 = 4.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 347 9 5 6 0.2 OC(=O)COc1ccc(cc1)C(P(=O)(CC[C@@H](C(=O)O)N)O)O 22223752
CHEMBL3114673 2367 8 None -104 8 Human 4.9 pEC50 = 4.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 347 9 5 6 0.2 OC(=O)COc1ccc(cc1)C(P(=O)(CC[C@@H](C(=O)O)N)O)O 22223752
1441 402 25 None 60 2 Human 6.7 pEC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 392 9 2 2 5.7 C(NC(c1ccccc1)c1ccccc1)CNC(c1ccccc1)c1ccccc1 16339898
1894361 402 25 None 60 2 Human 6.7 pEC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 392 9 2 2 5.7 C(NC(c1ccccc1)c1ccccc1)CNC(c1ccccc1)c1ccccc1 16339898
CHEMBL1387826 402 25 None 60 2 Human 6.7 pEC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 392 9 2 2 5.7 C(NC(c1ccccc1)c1ccccc1)CNC(c1ccccc1)c1ccccc1 16339898
131801162 4055 16 None -1 2 Rat 6.1 pIC50 = 6.1 Functional
IN a clacium mobilization assay using rat mGlu<sub>7</sub>/G<sub>&alpha;15</sub>/HEK cells activated by the agonist L-AP4.IN a clacium mobilization assay using rat mGlu<sub>7</sub>/G<sub>&alpha;15</sub>/HEK cells activated by the agonist L-AP4.
Guide to Pharmacology 408 6 1 7 3.4 COc1ccc(cc1OC)C(=O)Nc1cc(ccc1n1ncnc1)OC(F)(F)F 29259756
9703 4055 16 None -1 2 Rat 6.1 pIC50 = 6.1 Functional
IN a clacium mobilization assay using rat mGlu<sub>7</sub>/G<sub>&alpha;15</sub>/HEK cells activated by the agonist L-AP4.IN a clacium mobilization assay using rat mGlu<sub>7</sub>/G<sub>&alpha;15</sub>/HEK cells activated by the agonist L-AP4.
Guide to Pharmacology 408 6 1 7 3.4 COc1ccc(cc1OC)C(=O)Nc1cc(ccc1n1ncnc1)OC(F)(F)F 29259756
CHEMBL4176971 4055 16 None -1 2 Rat 6.1 pIC50 = 6.1 Functional
IN a clacium mobilization assay using rat mGlu<sub>7</sub>/G<sub>&alpha;15</sub>/HEK cells activated by the agonist L-AP4.IN a clacium mobilization assay using rat mGlu<sub>7</sub>/G<sub>&alpha;15</sub>/HEK cells activated by the agonist L-AP4.
Guide to Pharmacology 408 6 1 7 3.4 COc1ccc(cc1OC)C(=O)Nc1cc(ccc1n1ncnc1)OC(F)(F)F 29259756
10196 4056 25 None 1 2 Human 6.5 pIC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 448 8 1 7 4.2 COc1cc(ccc1OCC1CC1)C(=O)Nc1cc(ccc1n1cncn1)OC(F)(F)F 30608678
137321168 4056 25 None 1 2 Human 6.5 pIC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 448 8 1 7 4.2 COc1cc(ccc1OCC1CC1)C(=O)Nc1cc(ccc1n1cncn1)OC(F)(F)F 30608678
CHEMBL4445682 4056 25 None 1 2 Human 6.5 pIC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 448 8 1 7 4.2 COc1cc(ccc1OCC1CC1)C(=O)Nc1cc(ccc1n1cncn1)OC(F)(F)F 30608678
3341 2584 38 None - 1 Rat 6.9 pIC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 333 3 0 6 3.3 COc1ccc(cc1)c1cc2onc(c2c(=O)n1C)c1ccncc1 17609420
3341 2584 38 None - 1 Rat 6.9 pIC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 333 3 0 6 3.3 COc1ccc(cc1)c1cc2onc(c2c(=O)n1C)c1ccncc1 20026717
9945530 2584 38 None - 1 Rat 6.9 pIC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 333 3 0 6 3.3 COc1ccc(cc1)c1cc2onc(c2c(=O)n1C)c1ccncc1 17609420
9945530 2584 38 None - 1 Rat 6.9 pIC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 333 3 0 6 3.3 COc1ccc(cc1)c1cc2onc(c2c(=O)n1C)c1ccncc1 20026717
CHEMBL593489 2584 38 None - 1 Rat 6.9 pIC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 333 3 0 6 3.3 COc1ccc(cc1)c1cc2onc(c2c(=O)n1C)c1ccncc1 17609420
CHEMBL593489 2584 38 None - 1 Rat 6.9 pIC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 333 3 0 6 3.3 COc1ccc(cc1)c1cc2onc(c2c(=O)n1C)c1ccncc1 20026717
53391766 299 22 None -5 2 Rat 7.1 pIC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 269 2 0 3 3.8 CCc1nc2c(o1)CC(CC2=O)c1ccc(cc1C)C 23257312
6217 299 22 None -5 2 Rat 7.1 pIC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 269 2 0 3 3.8 CCc1nc2c(o1)CC(CC2=O)c1ccc(cc1C)C 23257312
CHEMBL4174742 299 22 None -5 2 Rat 7.1 pIC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 269 2 0 3 3.8 CCc1nc2c(o1)CC(CC2=O)c1ccc(cc1C)C 23257312
53391766 299 22 None 5 2 Human 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 269 2 0 3 3.8 CCc1nc2c(o1)CC(CC2=O)c1ccc(cc1C)C 23257312
6217 299 22 None 5 2 Human 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 269 2 0 3 3.8 CCc1nc2c(o1)CC(CC2=O)c1ccc(cc1C)C 23257312
CHEMBL4174742 299 22 None 5 2 Human 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 269 2 0 3 3.8 CCc1nc2c(o1)CC(CC2=O)c1ccc(cc1C)C 23257312
4250909 2476 21 None - 1 Rat 7.6 pIC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 302 2 0 4 3.9 Cn1c(cc2c(c1=O)c(no2)c1ccccc1)c1ccccc1 17609420
6218 2476 21 None - 1 Rat 7.6 pIC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 302 2 0 4 3.9 Cn1c(cc2c(c1=O)c(no2)c1ccccc1)c1ccccc1 17609420
CHEMBL595840 2476 21 None - 1 Rat 7.6 pIC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 302 2 0 4 3.9 Cn1c(cc2c(c1=O)c(no2)c1ccccc1)c1ccccc1 17609420
1406 2073 38 None -489 7 Human 3.7 pIC50 None 3.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10336568
1406 2073 38 None -489 7 Human 3.7 pIC50 None 3.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10866390
4545574 2073 38 None -489 7 Human 3.7 pIC50 None 3.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10336568
4545574 2073 38 None -489 7 Human 3.7 pIC50 None 3.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10866390
CHEMBL277475 2073 38 None -489 7 Human 3.7 pIC50 None 3.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10336568
CHEMBL277475 2073 38 None -489 7 Human 3.7 pIC50 None 3.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 231 3 4 3 -0.4 OC(=O)C(c1ccc(cc1)P(=O)(O)O)N 10866390




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DOI

134536725 170302 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Agonist activity at mGlu7 (unknown origin)Agonist activity at mGlu7 (unknown origin)
ChEMBL 315 3 2 3 2.5 C[C@H](C(=O)NC1COc2ccc(F)cc2C1O)c1ccccc1 10.1039/C8MD00524A
CHEMBL4446583 170302 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Agonist activity at mGlu7 (unknown origin)Agonist activity at mGlu7 (unknown origin)
ChEMBL 315 3 2 3 2.5 C[C@H](C(=O)NC1COc2ccc(F)cc2C1O)c1ccccc1 10.1039/C8MD00524A
134521675 174572 0 None - 0 Mouse 8.7 pEC50 = 8.7 Binding
Agonist activity at mouse mGlu7Agonist activity at mouse mGlu7
ChEMBL 377 4 1 4 2.6 C[C@H](C(=O)NC1COc2ccccc2C1S(C)(=O)=O)c1ccc(F)cc1 10.1039/C8MD00524A
CHEMBL4556629 174572 0 None - 0 Mouse 8.7 pEC50 = 8.7 Binding
Agonist activity at mouse mGlu7Agonist activity at mouse mGlu7
ChEMBL 377 4 1 4 2.6 C[C@H](C(=O)NC1COc2ccccc2C1S(C)(=O)=O)c1ccc(F)cc1 10.1039/C8MD00524A
162647803 179780 0 None - 0 Rat 6.0 pEC50 = 6 Binding
Positive allosteric modulation of rat mGlu7 expressed in HEK293 cells co- expressing GIRK assessed as potentiation of L-AP4-induced thallium flux incubated for 140 sec by FluoZin2-AM dye based fluorescence analysisPositive allosteric modulation of rat mGlu7 expressed in HEK293 cells co- expressing GIRK assessed as potentiation of L-AP4-induced thallium flux incubated for 140 sec by FluoZin2-AM dye based fluorescence analysis
ChEMBL 418 4 0 6 3.7 N#Cc1cnc2c(OC3CCOC3)cccc2c1N1CCN(c2ccccc2F)CC1 10.1021/acsmedchemlett.0c00432
CHEMBL4744634 179780 0 None - 0 Rat 6.0 pEC50 = 6 Binding
Positive allosteric modulation of rat mGlu7 expressed in HEK293 cells co- expressing GIRK assessed as potentiation of L-AP4-induced thallium flux incubated for 140 sec by FluoZin2-AM dye based fluorescence analysisPositive allosteric modulation of rat mGlu7 expressed in HEK293 cells co- expressing GIRK assessed as potentiation of L-AP4-induced thallium flux incubated for 140 sec by FluoZin2-AM dye based fluorescence analysis
ChEMBL 418 4 0 6 3.7 N#Cc1cnc2c(OC3CCOC3)cccc2c1N1CCN(c2ccccc2F)CC1 10.1021/acsmedchemlett.0c00432
162663930 182101 0 None - 0 Rat 6.0 pEC50 = 6 Binding
Positive allosteric modulation of rat mGlu7 expressed in HEK293 cells co- expressing GIRK assessed as potentiation of L-AP4-induced thallium flux incubated for 140 sec by FluoZin2-AM dye based fluorescence analysisPositive allosteric modulation of rat mGlu7 expressed in HEK293 cells co- expressing GIRK assessed as potentiation of L-AP4-induced thallium flux incubated for 140 sec by FluoZin2-AM dye based fluorescence analysis
ChEMBL 380 3 0 5 3.7 COc1cc(F)cc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1021/acsmedchemlett.0c00432
CHEMBL4761695 182101 0 None - 0 Rat 6.0 pEC50 = 6 Binding
Positive allosteric modulation of rat mGlu7 expressed in HEK293 cells co- expressing GIRK assessed as potentiation of L-AP4-induced thallium flux incubated for 140 sec by FluoZin2-AM dye based fluorescence analysisPositive allosteric modulation of rat mGlu7 expressed in HEK293 cells co- expressing GIRK assessed as potentiation of L-AP4-induced thallium flux incubated for 140 sec by FluoZin2-AM dye based fluorescence analysis
ChEMBL 380 3 0 5 3.7 COc1cc(F)cc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1021/acsmedchemlett.0c00432
CHEMBL4781814 182101 0 None - 0 Rat 6.0 pEC50 = 6 Binding
Positive allosteric modulation of rat mGlu7 expressed in HEK293 cells co- expressing GIRK assessed as potentiation of L-AP4-induced thallium flux incubated for 140 sec by FluoZin2-AM dye based fluorescence analysisPositive allosteric modulation of rat mGlu7 expressed in HEK293 cells co- expressing GIRK assessed as potentiation of L-AP4-induced thallium flux incubated for 140 sec by FluoZin2-AM dye based fluorescence analysis
ChEMBL 380 3 0 5 3.7 COc1cc(F)cc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1021/acsmedchemlett.0c00432
162647803 179780 0 None - 0 Rat 6.0 pEC50 = 6.0 Binding
Positive allosteric modulation of rat mGlu7 expressed in HEK293 cells co- expressing GIRK assessed as potentiation of L-AP4-induced thallium flux incubated for 140 sec by FluoZin2-AM dye based fluorescence analysisPositive allosteric modulation of rat mGlu7 expressed in HEK293 cells co- expressing GIRK assessed as potentiation of L-AP4-induced thallium flux incubated for 140 sec by FluoZin2-AM dye based fluorescence analysis
ChEMBL 418 4 0 6 3.7 N#Cc1cnc2c(OC3CCOC3)cccc2c1N1CCN(c2ccccc2F)CC1 10.1021/acsmedchemlett.0c00432
CHEMBL4744634 179780 0 None - 0 Rat 6.0 pEC50 = 6.0 Binding
Positive allosteric modulation of rat mGlu7 expressed in HEK293 cells co- expressing GIRK assessed as potentiation of L-AP4-induced thallium flux incubated for 140 sec by FluoZin2-AM dye based fluorescence analysisPositive allosteric modulation of rat mGlu7 expressed in HEK293 cells co- expressing GIRK assessed as potentiation of L-AP4-induced thallium flux incubated for 140 sec by FluoZin2-AM dye based fluorescence analysis
ChEMBL 418 4 0 6 3.7 N#Cc1cnc2c(OC3CCOC3)cccc2c1N1CCN(c2ccccc2F)CC1 10.1021/acsmedchemlett.0c00432
CHEMBL5272418 193720 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human mGluR7b expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human mGluR7b expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 324 6 1 3 2.9 CNC[C@@H](OCC(=O)N1CCCc2ccccc21)c1ccccc1 10.1021/acsmedchemlett.2c00529
CHEMBL5291195 194522 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human mGluR7 expressed in CHO cells expressing CRE-Luc reporter gene assessed as reduction in forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin stimulation and measured after 5 hrs by luminescence based Steady glo assayAgonist activity at human mGluR7 expressed in CHO cells expressing CRE-Luc reporter gene assessed as reduction in forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin stimulation and measured after 5 hrs by luminescence based Steady glo assay
ChEMBL 265 3 1 1 3.1 C[C@H](C(=O)NC1Cc2ccccc2C1)c1ccccc1 10.1021/acsmedchemlett.2c00529
CHEMBL5273386 193761 0 None - 0 Rat 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of rat mGluR7Positive allosteric modulation of rat mGluR7
ChEMBL 390 2 1 7 2.8 COc1cc(F)cc2c(N3CCN4c5ccccc5NCC4C3)c(C#N)nnc12 10.1016/j.bmcl.2022.129106
CHEMBL5273386 193761 0 None - 0 Rat 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of rat mGluR7Positive allosteric modulation of rat mGluR7
ChEMBL 390 2 1 7 2.8 COc1cc(F)cc2c(N3CCN4c5ccccc5NCC4C3)c(C#N)nnc12 10.1016/j.bmcl.2022.129106
CHEMBL5288733 194441 0 None - 0 Rat 5.9 pEC50 = 5.9 Binding
Positive allosteric modulation of rat mGluR7Positive allosteric modulation of rat mGluR7
ChEMBL 404 2 1 7 2.3 COc1cc(F)cc2c(N3CCN4c5ccccc5NC(=O)C4C3)c(C#N)nnc12 10.1016/j.bmcl.2022.129106
CHEMBL5288733 194441 0 None - 0 Rat 5.9 pEC50 = 5.9 Binding
Positive allosteric modulation of rat mGluR7Positive allosteric modulation of rat mGluR7
ChEMBL 404 2 1 7 2.3 COc1cc(F)cc2c(N3CCN4c5ccccc5NC(=O)C4C3)c(C#N)nnc12 10.1016/j.bmcl.2022.129106
CHEMBL5286074 194329 0 None - 0 Rat 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of rat mGluR7Positive allosteric modulation of rat mGluR7
ChEMBL 409 2 0 7 2.9 COc1cc(F)cc2c(N3CCN4c5c(F)cccc5OCC4C3)c(C#N)nnc12 10.1016/j.bmcl.2022.129106
CHEMBL5289481 194467 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human mGluR7 expressed in CHO cells expressing CRE-Luc reporter gene assessed as reduction in forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin stimulation and measured after 5 hrs by luminescence based Steady glo assayAgonist activity at human mGluR7 expressed in CHO cells expressing CRE-Luc reporter gene assessed as reduction in forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin stimulation and measured after 5 hrs by luminescence based Steady glo assay
ChEMBL 265 3 1 1 3.1 C[C@@H](C(=O)NC1Cc2ccccc2C1)c1ccccc1 10.1021/acsmedchemlett.2c00529
10239 4043 29 None - 0 Human 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of mGluR7 (unknown origin)Positive allosteric modulation of mGluR7 (unknown origin)
ChEMBL 359 4 1 4 4.8 Clc1ccc(nc1)Oc1ccc(cc1Cl)NC(=O)c1ccccn1 10.1016/j.bmcl.2022.129106
73058507 4043 29 None - 0 Human 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of mGluR7 (unknown origin)Positive allosteric modulation of mGluR7 (unknown origin)
ChEMBL 359 4 1 4 4.8 Clc1ccc(nc1)Oc1ccc(cc1Cl)NC(=O)c1ccccn1 10.1016/j.bmcl.2022.129106
CHEMBL4162576 4043 29 None - 0 Human 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of mGluR7 (unknown origin)Positive allosteric modulation of mGluR7 (unknown origin)
ChEMBL 359 4 1 4 4.8 Clc1ccc(nc1)Oc1ccc(cc1Cl)NC(=O)c1ccccn1 10.1016/j.bmcl.2022.129106
CHEMBL5282643 194166 0 None - 0 Rat 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of rat mGluR7Positive allosteric modulation of rat mGluR7
ChEMBL 409 2 0 7 2.9 COc1cc(F)cc2c(N3CCN4c5c(F)cccc5OC[C@@H]4C3)c(C#N)nnc12 10.1016/j.bmcl.2022.129106
10238 4027 26 None - 0 Human 5.8 pEC50 = 5.8 Binding
Positive allosteric modulation of mGluR7 (unknown origin)Positive allosteric modulation of mGluR7 (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 4027 26 None - 0 Human 5.8 pEC50 = 5.8 Binding
Positive allosteric modulation of mGluR7 (unknown origin)Positive allosteric modulation of mGluR7 (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 4027 26 None - 0 Human 5.8 pEC50 = 5.8 Binding
Positive allosteric modulation of mGluR7 (unknown origin)Positive allosteric modulation of mGluR7 (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
CHEMBL5281755 194125 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human mGluR7 expressed in CHO cells expressing CRE-Luc reporter gene assessed as reduction in forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin stimulation and measured after 5 hrs by luminescence based Steady glo assayAgonist activity at human mGluR7 expressed in CHO cells expressing CRE-Luc reporter gene assessed as reduction in forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin stimulation and measured after 5 hrs by luminescence based Steady glo assay
ChEMBL 285 3 1 1 3.2 O=C(Cc1ccc(Cl)cc1)NC1Cc2ccccc2C1 10.1021/acsmedchemlett.2c00529
162663930 182101 0 None - 0 Rat 5.8 pEC50 = 5.8 Binding
Positive allosteric modulation of rat mGluR7Positive allosteric modulation of rat mGluR7
ChEMBL 380 3 0 5 3.7 COc1cc(F)cc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1016/j.bmcl.2022.129106
CHEMBL4761695 182101 0 None - 0 Rat 5.8 pEC50 = 5.8 Binding
Positive allosteric modulation of rat mGluR7Positive allosteric modulation of rat mGluR7
ChEMBL 380 3 0 5 3.7 COc1cc(F)cc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1016/j.bmcl.2022.129106
CHEMBL4781814 182101 0 None - 0 Rat 5.8 pEC50 = 5.8 Binding
Positive allosteric modulation of rat mGluR7Positive allosteric modulation of rat mGluR7
ChEMBL 380 3 0 5 3.7 COc1cc(F)cc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1016/j.bmcl.2022.129106
CHEMBL5266235 193474 0 None - 0 Mouse 8.7 pEC50 = 8.7 Binding
Agonist activity at mouse mGluR7 expressed in CHO cells expressing CRE-Luc reporter gene assessed as reduction in forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin stimulation and measured after 5 hrs by luminescence based Steady glo assayAgonist activity at mouse mGluR7 expressed in CHO cells expressing CRE-Luc reporter gene assessed as reduction in forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin stimulation and measured after 5 hrs by luminescence based Steady glo assay
ChEMBL 377 4 1 4 2.6 C[C@H](C(=O)N[C@H]1COc2ccccc2[C@@H]1S(C)(=O)=O)c1ccc(F)cc1 10.1021/acsmedchemlett.2c00529
CHEMBL5288109 194406 0 None - 0 Rat 6.6 pEC50 = 6.6 Binding
Positive allosteric modulation of rat mGluR7Positive allosteric modulation of rat mGluR7
ChEMBL 421 5 0 7 3.8 COc1cc(F)cc2c(N3CCN(c4ccccc4OC(C)C)CC3)c(C#N)nnc12 10.1016/j.bmcl.2022.129106
CHEMBL5290711 194508 0 None - 0 Rat 6.6 pEC50 = 6.6 Binding
Positive allosteric modulation of rat mGluR7Positive allosteric modulation of rat mGluR7
ChEMBL 391 2 0 7 2.7 COc1cc(F)cc2c(N3CCN4c5ccccc5OC[C@@H]4C3)c(C#N)nnc12 10.1016/j.bmcl.2022.129106
CHEMBL5290711 194508 0 None - 0 Rat 6.6 pEC50 = 6.6 Binding
Positive allosteric modulation of rat mGluR7Positive allosteric modulation of rat mGluR7
ChEMBL 391 2 0 7 2.7 COc1cc(F)cc2c(N3CCN4c5ccccc5OC[C@@H]4C3)c(C#N)nnc12 10.1016/j.bmcl.2022.129106
CHEMBL5280256 194058 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human mGluR7 expressed in CHO cells expressing CRE-Luc reporter gene assessed as reduction in forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin stimulation and measured after 5 hrs by luminescence based Steady glo assayAgonist activity at human mGluR7 expressed in CHO cells expressing CRE-Luc reporter gene assessed as reduction in forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin stimulation and measured after 5 hrs by luminescence based Steady glo assay
ChEMBL 375 4 1 3 3.1 C[C@H](C(=O)N[C@@H]1CCc2ccccc2[C@H]1S(C)(=O)=O)c1ccc(F)cc1 10.1021/acsmedchemlett.2c00529
134474664 170115 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at mGlu7 (unknown origin)Agonist activity at mGlu7 (unknown origin)
ChEMBL 352 5 1 2 3.0 O=C(NCc1ccccc1F)C1c2ccccc2CC(=O)N1CC1CC1 10.1039/C8MD00524A
CHEMBL4443735 170115 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at mGlu7 (unknown origin)Agonist activity at mGlu7 (unknown origin)
ChEMBL 352 5 1 2 3.0 O=C(NCc1ccccc1F)C1c2ccccc2CC(=O)N1CC1CC1 10.1039/C8MD00524A
54752951 68792 3 None - 0 Rat 5.5 pEC50 = 5.5 Binding
Positive allosteric modulator activity at rat mGlu7 receptor at 10 uM by thallium flux assayPositive allosteric modulator activity at rat mGlu7 receptor at 10 uM by thallium flux assay
ChEMBL 393 3 1 4 3.3 O=C(Nc1ccc(N2C(=O)[C@H]3[C@H]4C=C[C@H](C4)[C@H]3C2=O)c(Cl)c1)c1ccccn1 10.1021/jm200956q
CHEMBL1921961 68792 3 None - 0 Rat 5.5 pEC50 = 5.5 Binding
Positive allosteric modulator activity at rat mGlu7 receptor at 10 uM by thallium flux assayPositive allosteric modulator activity at rat mGlu7 receptor at 10 uM by thallium flux assay
ChEMBL 393 3 1 4 3.3 O=C(Nc1ccc(N2C(=O)[C@H]3[C@H]4C=C[C@H](C4)[C@H]3C2=O)c(Cl)c1)c1ccccn1 10.1021/jm200956q
CHEMBL5269255 193595 0 None - 0 Rat 6.5 pEC50 = 6.5 Binding
Positive allosteric modulation of rat mGluR7Positive allosteric modulation of rat mGluR7
ChEMBL 419 5 0 7 3.5 COc1cc(F)cc2c(N3CCN(c4ccccc4OC4CC4)CC3)c(C#N)nnc12 10.1016/j.bmcl.2022.129106
CHEMBL5285820 194316 0 None - 0 Rat 6.5 pEC50 = 6.5 Binding
Positive allosteric modulation of rat mGluR7Positive allosteric modulation of rat mGluR7
ChEMBL 441 2 0 7 3.6 COc1cc(C(F)(F)F)cc2c(N3CCN4c5ccccc5OC[C@H]4C3)c(C#N)nnc12 10.1016/j.bmcl.2022.129106
CHEMBL5285820 194316 0 None - 0 Rat 6.5 pEC50 = 6.5 Binding
Positive allosteric modulation of rat mGluR7Positive allosteric modulation of rat mGluR7
ChEMBL 441 2 0 7 3.6 COc1cc(C(F)(F)F)cc2c(N3CCN4c5ccccc5OC[C@H]4C3)c(C#N)nnc12 10.1016/j.bmcl.2022.129106
CHEMBL5285846 194319 0 None - 0 Rat 6.4 pEC50 = 6.4 Binding
Positive allosteric modulation of rat mGluR7Positive allosteric modulation of rat mGluR7
ChEMBL 381 3 0 6 3.1 COc1cc(F)cc2c(N3CCN(c4ccccc4F)CC3)c(C#N)nnc12 10.1016/j.bmcl.2022.129106
CHEMBL5288955 194451 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human mGluR7 expressed in CHO cells expressing CRE-Luc reporter gene assessed as reduction in forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin stimulation and measured after 5 hrs by luminescence based Steady glo assayAgonist activity at human mGluR7 expressed in CHO cells expressing CRE-Luc reporter gene assessed as reduction in forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin stimulation and measured after 5 hrs by luminescence based Steady glo assay
ChEMBL 361 4 1 3 2.8 C[C@H](C(=O)N[C@H]1Cc2ccccc2[C@@H]1S(C)(=O)=O)c1ccc(F)cc1 10.1021/acsmedchemlett.2c00529
CHEMBL5271313 193678 0 None - 0 Rat 7.4 pEC50 = 7.4 Binding
Positive allosteric modulation of rat mGluR7Positive allosteric modulation of rat mGluR7
ChEMBL 391 2 0 7 2.7 COc1cc(F)cc2c(N3CCN4c5ccccc5OC[C@H]4C3)c(C#N)nnc12 10.1016/j.bmcl.2022.129106
CHEMBL5271313 193678 0 None - 0 Rat 7.4 pEC50 = 7.4 Binding
Positive allosteric modulation of rat mGluR7Positive allosteric modulation of rat mGluR7
ChEMBL 391 2 0 7 2.7 COc1cc(F)cc2c(N3CCN4c5ccccc5OC[C@H]4C3)c(C#N)nnc12 10.1016/j.bmcl.2022.129106
CHEMBL5286456 194346 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human mGluR7 expressed in CHO cells expressing CRE-Luc reporter gene assessed as reduction in forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin stimulation and measured after 5 hrs by luminescence based Steady glo assayAgonist activity at human mGluR7 expressed in CHO cells expressing CRE-Luc reporter gene assessed as reduction in forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin stimulation and measured after 5 hrs by luminescence based Steady glo assay
ChEMBL 283 3 1 1 3.2 C[C@H](C(=O)NC1Cc2ccccc2C1)c1ccc(F)cc1 10.1021/acsmedchemlett.2c00529
CHEMBL5281472 194112 0 None - 0 Rat 7.3 pEC50 = 7.3 Binding
Positive allosteric modulation of rat mGluR7Positive allosteric modulation of rat mGluR7
ChEMBL 409 2 0 7 2.9 COc1cc(F)cc2c(N3CCN4c5c(F)cccc5OC[C@H]4C3)c(C#N)nnc12 10.1016/j.bmcl.2022.129106
CHEMBL5285249 194288 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at human mGluR7 expressed in CHO cells expressing CRE-Luc reporter gene assessed as reduction in forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin stimulation and measured after 5 hrs by luminescence based Steady glo assayAgonist activity at human mGluR7 expressed in CHO cells expressing CRE-Luc reporter gene assessed as reduction in forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin stimulation and measured after 5 hrs by luminescence based Steady glo assay
ChEMBL 361 4 1 3 2.8 C[C@H](C(=O)N[C@@H]1Cc2ccccc2[C@H]1S(C)(=O)=O)c1ccc(F)cc1 10.1021/acsmedchemlett.2c00529
134521675 174572 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at human mGlu7Agonist activity at human mGlu7
ChEMBL 377 4 1 4 2.6 C[C@H](C(=O)NC1COc2ccccc2C1S(C)(=O)=O)c1ccc(F)cc1 10.1039/C8MD00524A
CHEMBL4556629 174572 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at human mGlu7Agonist activity at human mGlu7
ChEMBL 377 4 1 4 2.6 C[C@H](C(=O)NC1COc2ccccc2C1S(C)(=O)=O)c1ccc(F)cc1 10.1039/C8MD00524A
145955288 162577 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at mGlu7 (unknown origin)Agonist activity at mGlu7 (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 162577 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at mGlu7 (unknown origin)Agonist activity at mGlu7 (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
1441 402 25 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human mGluR7b expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human mGluR7b expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 392 9 2 2 5.7 C(NC(c1ccccc1)c1ccccc1)CNC(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.2c00529
1894361 402 25 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human mGluR7b expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human mGluR7b expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 392 9 2 2 5.7 C(NC(c1ccccc1)c1ccccc1)CNC(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.2c00529
CHEMBL1387826 402 25 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human mGluR7b expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human mGluR7b expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 392 9 2 2 5.7 C(NC(c1ccccc1)c1ccccc1)CNC(c1ccccc1)c1ccccc1 10.1021/acsmedchemlett.2c00529
131954513 162078 38 None - 1 Human 6.2 pEC50 = 6.2 Binding
Positive allosteric modulation of mGluR7 (unknown origin)Positive allosteric modulation of mGluR7 (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 162078 38 None - 1 Human 6.2 pEC50 = 6.2 Binding
Positive allosteric modulation of mGluR7 (unknown origin)Positive allosteric modulation of mGluR7 (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
131954513 162078 38 None - 1 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at mGlu7 (unknown origin)Agonist activity at mGlu7 (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 162078 38 None - 1 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at mGlu7 (unknown origin)Agonist activity at mGlu7 (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
CHEMBL5266235 193474 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at human mGluR7 expressed in CHO cells expressing CRE-Luc reporter gene assessed as reduction in forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin stimulation and measured after 5 hrs by luminescence based Steady glo assayAgonist activity at human mGluR7 expressed in CHO cells expressing CRE-Luc reporter gene assessed as reduction in forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin stimulation and measured after 5 hrs by luminescence based Steady glo assay
ChEMBL 377 4 1 4 2.6 C[C@H](C(=O)N[C@H]1COc2ccccc2[C@@H]1S(C)(=O)=O)c1ccc(F)cc1 10.1021/acsmedchemlett.2c00529
162647576 179886 0 None - 0 Rat 6.2 pEC50 = 6.2 Binding
Positive allosteric modulation of rat mGlu7 expressed in HEK293 cells co- expressing GIRK assessed as potentiation of L-AP4-induced thallium flux incubated for 140 sec by FluoZin2-AM dye based fluorescence analysisPositive allosteric modulation of rat mGlu7 expressed in HEK293 cells co- expressing GIRK assessed as potentiation of L-AP4-induced thallium flux incubated for 140 sec by FluoZin2-AM dye based fluorescence analysis
ChEMBL 417 3 0 6 3.4 N#Cc1cnc2c(N3CCOCC3)cccc2c1N1CCN(c2ccccc2F)CC1 10.1021/acsmedchemlett.0c00432
CHEMBL4745777 179886 0 None - 0 Rat 6.2 pEC50 = 6.2 Binding
Positive allosteric modulation of rat mGlu7 expressed in HEK293 cells co- expressing GIRK assessed as potentiation of L-AP4-induced thallium flux incubated for 140 sec by FluoZin2-AM dye based fluorescence analysisPositive allosteric modulation of rat mGlu7 expressed in HEK293 cells co- expressing GIRK assessed as potentiation of L-AP4-induced thallium flux incubated for 140 sec by FluoZin2-AM dye based fluorescence analysis
ChEMBL 417 3 0 6 3.4 N#Cc1cnc2c(N3CCOCC3)cccc2c1N1CCN(c2ccccc2F)CC1 10.1021/acsmedchemlett.0c00432
162647576 179886 0 None - 0 Rat 6.2 pEC50 = 6.2 Binding
Positive allosteric modulation of rat mGlu7 expressed in HEK293 cells co- expressing GIRK assessed as potentiation of L-AP4-induced thallium flux incubated for 140 sec by FluoZin2-AM dye based fluorescence analysisPositive allosteric modulation of rat mGlu7 expressed in HEK293 cells co- expressing GIRK assessed as potentiation of L-AP4-induced thallium flux incubated for 140 sec by FluoZin2-AM dye based fluorescence analysis
ChEMBL 417 3 0 6 3.4 N#Cc1cnc2c(N3CCOCC3)cccc2c1N1CCN(c2ccccc2F)CC1 10.1021/acsmedchemlett.0c00432
CHEMBL4745777 179886 0 None - 0 Rat 6.2 pEC50 = 6.2 Binding
Positive allosteric modulation of rat mGlu7 expressed in HEK293 cells co- expressing GIRK assessed as potentiation of L-AP4-induced thallium flux incubated for 140 sec by FluoZin2-AM dye based fluorescence analysisPositive allosteric modulation of rat mGlu7 expressed in HEK293 cells co- expressing GIRK assessed as potentiation of L-AP4-induced thallium flux incubated for 140 sec by FluoZin2-AM dye based fluorescence analysis
ChEMBL 417 3 0 6 3.4 N#Cc1cnc2c(N3CCOCC3)cccc2c1N1CCN(c2ccccc2F)CC1 10.1021/acsmedchemlett.0c00432
155518354 170265 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at mGlu7 (unknown origin)Agonist activity at mGlu7 (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 170265 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at mGlu7 (unknown origin)Agonist activity at mGlu7 (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
162653691 180496 0 None - 0 Rat 6.1 pEC50 = 6.1 Binding
Positive allosteric modulation of rat mGlu7 expressed in HEK293 cells co- expressing GIRK assessed as potentiation of L-AP4-induced thallium flux incubated for 140 sec by FluoZin2-AM dye based fluorescence analysisPositive allosteric modulation of rat mGlu7 expressed in HEK293 cells co- expressing GIRK assessed as potentiation of L-AP4-induced thallium flux incubated for 140 sec by FluoZin2-AM dye based fluorescence analysis
ChEMBL 408 4 0 5 4.5 CC(C)Oc1cc(F)cc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1021/acsmedchemlett.0c00432
CHEMBL4753189 180496 0 None - 0 Rat 6.1 pEC50 = 6.1 Binding
Positive allosteric modulation of rat mGlu7 expressed in HEK293 cells co- expressing GIRK assessed as potentiation of L-AP4-induced thallium flux incubated for 140 sec by FluoZin2-AM dye based fluorescence analysisPositive allosteric modulation of rat mGlu7 expressed in HEK293 cells co- expressing GIRK assessed as potentiation of L-AP4-induced thallium flux incubated for 140 sec by FluoZin2-AM dye based fluorescence analysis
ChEMBL 408 4 0 5 4.5 CC(C)Oc1cc(F)cc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1021/acsmedchemlett.0c00432
162653691 180496 0 None - 0 Rat 6.1 pEC50 = 6.1 Binding
Positive allosteric modulation of rat mGlu7 expressed in HEK293 cells co- expressing GIRK assessed as potentiation of L-AP4-induced thallium flux incubated for 140 sec by FluoZin2-AM dye based fluorescence analysisPositive allosteric modulation of rat mGlu7 expressed in HEK293 cells co- expressing GIRK assessed as potentiation of L-AP4-induced thallium flux incubated for 140 sec by FluoZin2-AM dye based fluorescence analysis
ChEMBL 408 4 0 5 4.5 CC(C)Oc1cc(F)cc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1021/acsmedchemlett.0c00432
CHEMBL4753189 180496 0 None - 0 Rat 6.1 pEC50 = 6.1 Binding
Positive allosteric modulation of rat mGlu7 expressed in HEK293 cells co- expressing GIRK assessed as potentiation of L-AP4-induced thallium flux incubated for 140 sec by FluoZin2-AM dye based fluorescence analysisPositive allosteric modulation of rat mGlu7 expressed in HEK293 cells co- expressing GIRK assessed as potentiation of L-AP4-induced thallium flux incubated for 140 sec by FluoZin2-AM dye based fluorescence analysis
ChEMBL 408 4 0 5 4.5 CC(C)Oc1cc(F)cc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1021/acsmedchemlett.0c00432
CHEMBL5279292 194022 0 None - 0 Rat 6.1 pEC50 = 6.1 Binding
Positive allosteric modulation of rat mGluR7Positive allosteric modulation of rat mGluR7
ChEMBL 393 4 0 7 3.0 COc1ccccc1N1CCN(c2c(C#N)nnc3c(OC)cc(F)cc23)CC1 10.1016/j.bmcl.2022.129106
162654767 180572 0 None - 0 Rat 6.1 pEC50 = 6.1 Binding
Positive allosteric modulation of rat mGlu7 expressed in HEK293 cells co- expressing GIRK assessed as potentiation of L-AP4-induced thallium flux incubated for 140 sec by FluoZin2-AM dye based fluorescence analysisPositive allosteric modulation of rat mGlu7 expressed in HEK293 cells co- expressing GIRK assessed as potentiation of L-AP4-induced thallium flux incubated for 140 sec by FluoZin2-AM dye based fluorescence analysis
ChEMBL 362 3 0 5 3.6 COc1cccc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1021/acsmedchemlett.0c00432
CHEMBL4754102 180572 0 None - 0 Rat 6.1 pEC50 = 6.1 Binding
Positive allosteric modulation of rat mGlu7 expressed in HEK293 cells co- expressing GIRK assessed as potentiation of L-AP4-induced thallium flux incubated for 140 sec by FluoZin2-AM dye based fluorescence analysisPositive allosteric modulation of rat mGlu7 expressed in HEK293 cells co- expressing GIRK assessed as potentiation of L-AP4-induced thallium flux incubated for 140 sec by FluoZin2-AM dye based fluorescence analysis
ChEMBL 362 3 0 5 3.6 COc1cccc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1021/acsmedchemlett.0c00432
CHEMBL4776732 180572 0 None - 0 Rat 6.1 pEC50 = 6.1 Binding
Positive allosteric modulation of rat mGlu7 expressed in HEK293 cells co- expressing GIRK assessed as potentiation of L-AP4-induced thallium flux incubated for 140 sec by FluoZin2-AM dye based fluorescence analysisPositive allosteric modulation of rat mGlu7 expressed in HEK293 cells co- expressing GIRK assessed as potentiation of L-AP4-induced thallium flux incubated for 140 sec by FluoZin2-AM dye based fluorescence analysis
ChEMBL 362 3 0 5 3.6 COc1cccc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1021/acsmedchemlett.0c00432
162654767 180572 0 None - 0 Rat 6.1 pEC50 = 6.1 Binding
Positive allosteric modulation of rat mGlu7 expressed in HEK293 cells co- expressing GIRK assessed as potentiation of L-AP4-induced thallium flux incubated for 140 sec by FluoZin2-AM dye based fluorescence analysisPositive allosteric modulation of rat mGlu7 expressed in HEK293 cells co- expressing GIRK assessed as potentiation of L-AP4-induced thallium flux incubated for 140 sec by FluoZin2-AM dye based fluorescence analysis
ChEMBL 362 3 0 5 3.6 COc1cccc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1021/acsmedchemlett.0c00432
CHEMBL4754102 180572 0 None - 0 Rat 6.1 pEC50 = 6.1 Binding
Positive allosteric modulation of rat mGlu7 expressed in HEK293 cells co- expressing GIRK assessed as potentiation of L-AP4-induced thallium flux incubated for 140 sec by FluoZin2-AM dye based fluorescence analysisPositive allosteric modulation of rat mGlu7 expressed in HEK293 cells co- expressing GIRK assessed as potentiation of L-AP4-induced thallium flux incubated for 140 sec by FluoZin2-AM dye based fluorescence analysis
ChEMBL 362 3 0 5 3.6 COc1cccc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1021/acsmedchemlett.0c00432
CHEMBL4776732 180572 0 None - 0 Rat 6.1 pEC50 = 6.1 Binding
Positive allosteric modulation of rat mGlu7 expressed in HEK293 cells co- expressing GIRK assessed as potentiation of L-AP4-induced thallium flux incubated for 140 sec by FluoZin2-AM dye based fluorescence analysisPositive allosteric modulation of rat mGlu7 expressed in HEK293 cells co- expressing GIRK assessed as potentiation of L-AP4-induced thallium flux incubated for 140 sec by FluoZin2-AM dye based fluorescence analysis
ChEMBL 362 3 0 5 3.6 COc1cccc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1021/acsmedchemlett.0c00432
162663930 182101 0 None - 0 Rat 6.0 pEC50 = 6 Binding
Positive allosteric modulation of rat mGlu7 expressed in HEK293 cells co- expressing GIRK assessed as potentiation of L-AP4-induced thallium flux incubated for 140 sec by FluoZin2-AM dye based fluorescence analysisPositive allosteric modulation of rat mGlu7 expressed in HEK293 cells co- expressing GIRK assessed as potentiation of L-AP4-induced thallium flux incubated for 140 sec by FluoZin2-AM dye based fluorescence analysis
ChEMBL 380 3 0 5 3.7 COc1cc(F)cc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1021/acsmedchemlett.0c00432
CHEMBL4761695 182101 0 None - 0 Rat 6.0 pEC50 = 6 Binding
Positive allosteric modulation of rat mGlu7 expressed in HEK293 cells co- expressing GIRK assessed as potentiation of L-AP4-induced thallium flux incubated for 140 sec by FluoZin2-AM dye based fluorescence analysisPositive allosteric modulation of rat mGlu7 expressed in HEK293 cells co- expressing GIRK assessed as potentiation of L-AP4-induced thallium flux incubated for 140 sec by FluoZin2-AM dye based fluorescence analysis
ChEMBL 380 3 0 5 3.7 COc1cc(F)cc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1021/acsmedchemlett.0c00432
CHEMBL4781814 182101 0 None - 0 Rat 6.0 pEC50 = 6 Binding
Positive allosteric modulation of rat mGlu7 expressed in HEK293 cells co- expressing GIRK assessed as potentiation of L-AP4-induced thallium flux incubated for 140 sec by FluoZin2-AM dye based fluorescence analysisPositive allosteric modulation of rat mGlu7 expressed in HEK293 cells co- expressing GIRK assessed as potentiation of L-AP4-induced thallium flux incubated for 140 sec by FluoZin2-AM dye based fluorescence analysis
ChEMBL 380 3 0 5 3.7 COc1cc(F)cc2c(N3CCN(c4ccccc4F)CC3)c(C#N)cnc12 10.1021/acsmedchemlett.0c00432
155531347 171639 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 433 6 0 9 3.9 COc1ccc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-n3cncn3)o2)cc1OC 10.1016/j.bmcl.2022.128923
CHEMBL4465794 171639 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 433 6 0 9 3.9 COc1ccc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-n3cncn3)o2)cc1OC 10.1016/j.bmcl.2022.128923
155531347 171639 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 433 6 0 9 3.9 COc1ccc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-n3cncn3)o2)cc1OC 10.1016/j.bmcl.2022.128923
CHEMBL4465794 171639 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 433 6 0 9 3.9 COc1ccc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-n3cncn3)o2)cc1OC 10.1016/j.bmcl.2022.128923
145958691 162146 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 436 8 1 7 4.2 CCCOc1ccc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)cc1OC 10.1016/j.bmcl.2022.128923
CHEMBL4161847 162146 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 436 8 1 7 4.2 CCCOc1ccc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)cc1OC 10.1016/j.bmcl.2022.128923
145958691 162146 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 436 8 1 7 4.2 CCCOc1ccc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)cc1OC 10.1016/j.bmcl.2022.128923
CHEMBL4161847 162146 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 436 8 1 7 4.2 CCCOc1ccc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)cc1OC 10.1016/j.bmcl.2022.128923
145953031 162602 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 422 7 1 7 3.8 CCOc1ccc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)cc1OC 10.1016/j.bmcl.2022.128923
CHEMBL4169114 162602 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 422 7 1 7 3.8 CCOc1ccc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)cc1OC 10.1016/j.bmcl.2022.128923
1378 2417 54 None -123 10 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at mGluR7 (unknown origin) assessed as inhibition of L-AP4 stimulated decrease in forskolin induced cAMP response by CRE-Luc assayAntagonist activity at mGluR7 (unknown origin) assessed as inhibition of L-AP4 stimulated decrease in forskolin induced cAMP response by CRE-Luc assay
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/acsmedchemlett.2c00529
1399 2417 54 None -123 10 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at mGluR7 (unknown origin) assessed as inhibition of L-AP4 stimulated decrease in forskolin induced cAMP response by CRE-Luc assayAntagonist activity at mGluR7 (unknown origin) assessed as inhibition of L-AP4 stimulated decrease in forskolin induced cAMP response by CRE-Luc assay
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/acsmedchemlett.2c00529
9819927 2417 54 None -123 10 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at mGluR7 (unknown origin) assessed as inhibition of L-AP4 stimulated decrease in forskolin induced cAMP response by CRE-Luc assayAntagonist activity at mGluR7 (unknown origin) assessed as inhibition of L-AP4 stimulated decrease in forskolin induced cAMP response by CRE-Luc assay
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/acsmedchemlett.2c00529
CHEMBL432038 2417 54 None -123 10 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at mGluR7 (unknown origin) assessed as inhibition of L-AP4 stimulated decrease in forskolin induced cAMP response by CRE-Luc assayAntagonist activity at mGluR7 (unknown origin) assessed as inhibition of L-AP4 stimulated decrease in forskolin induced cAMP response by CRE-Luc assay
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/acsmedchemlett.2c00529
145953031 162602 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 422 7 1 7 3.8 CCOc1ccc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)cc1OC 10.1016/j.bmcl.2022.128923
CHEMBL4169114 162602 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 422 7 1 7 3.8 CCOc1ccc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)cc1OC 10.1016/j.bmcl.2022.128923
168295910 192390 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 396 5 0 7 4.5 COc1ccc(-c2nnc(-c3cc(Cl)ccc3-c3ccnn3C)o2)cc1OC 10.1016/j.bmcl.2022.128923
CHEMBL5207640 192390 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 396 5 0 7 4.5 COc1ccc(-c2nnc(-c3cc(Cl)ccc3-c3ccnn3C)o2)cc1OC 10.1016/j.bmcl.2022.128923
168295910 192390 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 396 5 0 7 4.5 COc1ccc(-c2nnc(-c3cc(Cl)ccc3-c3ccnn3C)o2)cc1OC 10.1016/j.bmcl.2022.128923
CHEMBL5207640 192390 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 396 5 0 7 4.5 COc1ccc(-c2nnc(-c3cc(Cl)ccc3-c3ccnn3C)o2)cc1OC 10.1016/j.bmcl.2022.128923
155538270 172393 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 432 6 0 8 4.5 COc1ccc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-n3ccnc3)o2)cc1OC 10.1016/j.bmcl.2022.128923
CHEMBL4476495 172393 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 432 6 0 8 4.5 COc1ccc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-n3ccnc3)o2)cc1OC 10.1016/j.bmcl.2022.128923
168283516 191063 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 448 7 1 7 4.4 COc1cc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OC1CCC1 10.1016/j.bmcl.2022.128923
CHEMBL5187341 191063 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 448 7 1 7 4.4 COc1cc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OC1CCC1 10.1016/j.bmcl.2022.128923
155538270 172393 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 432 6 0 8 4.5 COc1ccc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-n3ccnc3)o2)cc1OC 10.1016/j.bmcl.2022.128923
CHEMBL4476495 172393 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 432 6 0 8 4.5 COc1ccc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-n3ccnc3)o2)cc1OC 10.1016/j.bmcl.2022.128923
168283516 191063 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 448 7 1 7 4.4 COc1cc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OC1CCC1 10.1016/j.bmcl.2022.128923
CHEMBL5187341 191063 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 448 7 1 7 4.4 COc1cc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OC1CCC1 10.1016/j.bmcl.2022.128923
168276104 190271 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 382 5 0 7 4.3 COc1ccc(-c2coc(-c3cc(Cl)ccc3-n3cncn3)n2)cc1OC 10.1016/j.bmcl.2022.128923
CHEMBL5175583 190271 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 382 5 0 7 4.3 COc1ccc(-c2coc(-c3cc(Cl)ccc3-n3cncn3)n2)cc1OC 10.1016/j.bmcl.2022.128923
168276104 190271 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 382 5 0 7 4.3 COc1ccc(-c2coc(-c3cc(Cl)ccc3-n3cncn3)n2)cc1OC 10.1016/j.bmcl.2022.128923
CHEMBL5175583 190271 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 382 5 0 7 4.3 COc1ccc(-c2coc(-c3cc(Cl)ccc3-n3cncn3)n2)cc1OC 10.1016/j.bmcl.2022.128923
168275316 190206 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 433 6 0 7 4.7 CCOC(=O)c1cnc2c(OC)cccc2c1-c1ccc(-c2cc(F)cnc2OC)nc1 10.1016/j.bmcl.2022.128923
CHEMBL5174531 190206 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 433 6 0 7 4.7 CCOC(=O)c1cnc2c(OC)cccc2c1-c1ccc(-c2cc(F)cnc2OC)nc1 10.1016/j.bmcl.2022.128923
168275316 190206 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 433 6 0 7 4.7 CCOC(=O)c1cnc2c(OC)cccc2c1-c1ccc(-c2cc(F)cnc2OC)nc1 10.1016/j.bmcl.2022.128923
CHEMBL5174531 190206 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 433 6 0 7 4.7 CCOC(=O)c1cnc2c(OC)cccc2c1-c1ccc(-c2cc(F)cnc2OC)nc1 10.1016/j.bmcl.2022.128923
145955650 162399 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 436 7 1 7 4.2 COc1cc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OC(C)C 10.1016/j.bmcl.2022.128923
CHEMBL4165849 162399 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 436 7 1 7 4.2 COc1cc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OC(C)C 10.1016/j.bmcl.2022.128923
155532310 171737 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 432 6 1 7 4.7 COc1ccc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-c3cn[nH]c3)o2)cc1OC 10.1016/j.bmcl.2022.128923
CHEMBL4467224 171737 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 432 6 1 7 4.7 COc1ccc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-c3cn[nH]c3)o2)cc1OC 10.1016/j.bmcl.2022.128923
145955650 162399 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 436 7 1 7 4.2 COc1cc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OC(C)C 10.1016/j.bmcl.2022.128923
CHEMBL4165849 162399 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 436 7 1 7 4.2 COc1cc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OC(C)C 10.1016/j.bmcl.2022.128923
155532310 171737 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 432 6 1 7 4.7 COc1ccc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-c3cn[nH]c3)o2)cc1OC 10.1016/j.bmcl.2022.128923
CHEMBL4467224 171737 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 432 6 1 7 4.7 COc1ccc(-c2nnc(-c3cc(OC(F)(F)F)ccc3-c3cn[nH]c3)o2)cc1OC 10.1016/j.bmcl.2022.128923
131801162 4055 16 None - 0 Human 6.2 pIC50 = 6.2 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 408 6 1 7 3.4 COc1ccc(cc1OC)C(=O)Nc1cc(ccc1n1ncnc1)OC(F)(F)F 10.1016/j.bmcl.2022.128923
9703 4055 16 None - 0 Human 6.2 pIC50 = 6.2 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 408 6 1 7 3.4 COc1ccc(cc1OC)C(=O)Nc1cc(ccc1n1ncnc1)OC(F)(F)F 10.1016/j.bmcl.2022.128923
CHEMBL4176971 4055 16 None - 0 Human 6.2 pIC50 = 6.2 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 408 6 1 7 3.4 COc1ccc(cc1OC)C(=O)Nc1cc(ccc1n1ncnc1)OC(F)(F)F 10.1016/j.bmcl.2022.128923
168288994 191774 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 383 5 0 8 3.7 COc1ccc(-c2noc(-c3cc(Cl)ccc3-n3cncn3)n2)cc1OC 10.1016/j.bmcl.2022.128923
CHEMBL5197933 191774 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 383 5 0 8 3.7 COc1ccc(-c2noc(-c3cc(Cl)ccc3-n3cncn3)n2)cc1OC 10.1016/j.bmcl.2022.128923
168288994 191774 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 383 5 0 8 3.7 COc1ccc(-c2noc(-c3cc(Cl)ccc3-n3cncn3)n2)cc1OC 10.1016/j.bmcl.2022.128923
CHEMBL5197933 191774 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 383 5 0 8 3.7 COc1ccc(-c2noc(-c3cc(Cl)ccc3-n3cncn3)n2)cc1OC 10.1016/j.bmcl.2022.128923
131801162 4055 16 None - 0 Human 6.2 pIC50 = 6.2 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 408 6 1 7 3.4 COc1ccc(cc1OC)C(=O)Nc1cc(ccc1n1ncnc1)OC(F)(F)F 10.1016/j.bmcl.2022.128923
9703 4055 16 None - 0 Human 6.2 pIC50 = 6.2 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 408 6 1 7 3.4 COc1ccc(cc1OC)C(=O)Nc1cc(ccc1n1ncnc1)OC(F)(F)F 10.1016/j.bmcl.2022.128923
CHEMBL4176971 4055 16 None - 0 Human 6.2 pIC50 = 6.2 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 408 6 1 7 3.4 COc1ccc(cc1OC)C(=O)Nc1cc(ccc1n1ncnc1)OC(F)(F)F 10.1016/j.bmcl.2022.128923
168270781 190045 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 419 5 0 8 3.9 COc1cc(F)c(-c2noc(-c3cc(Cl)ccc3-n3cncn3)n2)c(F)c1OC 10.1016/j.bmcl.2022.128923
CHEMBL5171986 190045 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 419 5 0 8 3.9 COc1cc(F)c(-c2noc(-c3cc(Cl)ccc3-n3cncn3)n2)c(F)c1OC 10.1016/j.bmcl.2022.128923
168284838 191295 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 401 5 0 8 3.8 COc1cc(-c2noc(-c3cc(Cl)ccc3-n3cncn3)n2)cc(F)c1OC 10.1016/j.bmcl.2022.128923
CHEMBL5190992 191295 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 401 5 0 8 3.8 COc1cc(-c2noc(-c3cc(Cl)ccc3-n3cncn3)n2)cc(F)c1OC 10.1016/j.bmcl.2022.128923
168292732 192088 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 480 9 1 9 3.0 COc1cc(OCC(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OC1COC1 10.1016/j.bmcl.2022.128923
CHEMBL5202961 192088 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 480 9 1 9 3.0 COc1cc(OCC(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OC1COC1 10.1016/j.bmcl.2022.128923
168292732 192088 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 480 9 1 9 3.0 COc1cc(OCC(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OC1COC1 10.1016/j.bmcl.2022.128923
CHEMBL5202961 192088 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 480 9 1 9 3.0 COc1cc(OCC(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OC1COC1 10.1016/j.bmcl.2022.128923
168284838 191295 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 401 5 0 8 3.8 COc1cc(-c2noc(-c3cc(Cl)ccc3-n3cncn3)n2)cc(F)c1OC 10.1016/j.bmcl.2022.128923
CHEMBL5190992 191295 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 401 5 0 8 3.8 COc1cc(-c2noc(-c3cc(Cl)ccc3-n3cncn3)n2)cc(F)c1OC 10.1016/j.bmcl.2022.128923
168270781 190045 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 419 5 0 8 3.9 COc1cc(F)c(-c2noc(-c3cc(Cl)ccc3-n3cncn3)n2)c(F)c1OC 10.1016/j.bmcl.2022.128923
CHEMBL5171986 190045 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Negative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assayNegative allosteric modulation of mGlu7 (unknown origin) in cells expressing G protein-regulated inwardly rectifying potassium channels (GIRKs) assessed as inhibition of L-AP4-induced response measured by thallium flux assay
ChEMBL 419 5 0 8 3.9 COc1cc(F)c(-c2noc(-c3cc(Cl)ccc3-n3cncn3)n2)c(F)c1OC 10.1016/j.bmcl.2022.128923
1378 2417 54 None -53 10 Rat 7.0 pKi = 7.0 Binding
Binding affinity towards metabotropic glutamate receptor 7 of rat expressed in CHO cells was determined by using [3H]MGS-0008Binding affinity towards metabotropic glutamate receptor 7 of rat expressed in CHO cells was determined by using [3H]MGS-0008
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/jm0400294
1399 2417 54 None -53 10 Rat 7.0 pKi = 7.0 Binding
Binding affinity towards metabotropic glutamate receptor 7 of rat expressed in CHO cells was determined by using [3H]MGS-0008Binding affinity towards metabotropic glutamate receptor 7 of rat expressed in CHO cells was determined by using [3H]MGS-0008
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/jm0400294
9819927 2417 54 None -53 10 Rat 7.0 pKi = 7.0 Binding
Binding affinity towards metabotropic glutamate receptor 7 of rat expressed in CHO cells was determined by using [3H]MGS-0008Binding affinity towards metabotropic glutamate receptor 7 of rat expressed in CHO cells was determined by using [3H]MGS-0008
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/jm0400294
CHEMBL432038 2417 54 None -53 10 Rat 7.0 pKi = 7.0 Binding
Binding affinity towards metabotropic glutamate receptor 7 of rat expressed in CHO cells was determined by using [3H]MGS-0008Binding affinity towards metabotropic glutamate receptor 7 of rat expressed in CHO cells was determined by using [3H]MGS-0008
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/jm0400294
1397 2529 15 None -301 5 Rat 6.2 pKi = 6.2 Binding
Binding affinity towards metabotropic glutamate receptor 7 of rat expressed in CHO cells was determined by using [3H]MGS-0008Binding affinity towards metabotropic glutamate receptor 7 of rat expressed in CHO cells was determined by using [3H]MGS-0008
ChEMBL 377 5 3 4 2.1 OC(=O)[C@]1(N)[C@H](OCc2ccc(c(c2)Cl)Cl)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O 10.1021/jm0400294
9886034 2529 15 None -301 5 Rat 6.2 pKi = 6.2 Binding
Binding affinity towards metabotropic glutamate receptor 7 of rat expressed in CHO cells was determined by using [3H]MGS-0008Binding affinity towards metabotropic glutamate receptor 7 of rat expressed in CHO cells was determined by using [3H]MGS-0008
ChEMBL 377 5 3 4 2.1 OC(=O)[C@]1(N)[C@H](OCc2ccc(c(c2)Cl)Cl)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O 10.1021/jm0400294
CHEMBL186453 2529 15 None -301 5 Rat 6.2 pKi = 6.2 Binding
Binding affinity towards metabotropic glutamate receptor 7 of rat expressed in CHO cells was determined by using [3H]MGS-0008Binding affinity towards metabotropic glutamate receptor 7 of rat expressed in CHO cells was determined by using [3H]MGS-0008
ChEMBL 377 5 3 4 2.1 OC(=O)[C@]1(N)[C@H](OCc2ccc(c(c2)Cl)Cl)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O 10.1021/jm0400294
5428913 4099 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of agonist-induced [<sup>35</sup>S]GTP&gamma;S binding.Inhibition of agonist-induced [<sup>35</sup>S]GTP&gamma;S binding.
Guide to Pharmacology 380 2 1 4 3.9 Ic1ccc(cc1)Oc1coc2c(c1=O)ccc(c2)O 24596089
8545 4099 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of agonist-induced [<sup>35</sup>S]GTP&gamma;S binding.Inhibition of agonist-induced [<sup>35</sup>S]GTP&gamma;S binding.
Guide to Pharmacology 380 2 1 4 3.9 Ic1ccc(cc1)Oc1coc2c(c1=O)ccc(c2)O 24596089
1378 2417 54 None -123 10 Human 7.1 pKd None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 11138847
1399 2417 54 None -123 10 Human 7.1 pKd None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 11138847
9819927 2417 54 None -123 10 Human 7.1 pKd None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 11138847
CHEMBL432038 2417 54 None -123 10 Human 7.1 pKd None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 11138847
1310 2315 110 Functional -389 18 Human 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 2315 110 Functional -389 18 Human 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 2315 110 Functional -389 18 Human 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 2315 110 Functional -389 18 Human 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 2315 110 Functional -389 18 Human 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 2315 110 Functional -389 18 Human 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 2315 110 Functional -389 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
10297 27112 30 Functional -38 42 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 27112 30 Functional -38 42 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
2207 99865 63 Functional -25 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 183 4 4 3 -1.0 NC(CCP(=O)(O)O)C(=O)O None
CHEMBL285843 99865 63 Functional -25 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 183 4 4 3 -1.0 NC(CCP(=O)(O)O)C(=O)O None
446220 133521 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 133521 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
162265 202274 22 Functional -239 43 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
4786 202274 22 Functional -239 43 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
CHEMBL61006 202274 22 Functional -239 43 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
25137849 216179 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 216179 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 216325 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 216326 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 216338 0 Functional -8 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 185 4 4 4 -1.5 C(C(C(=O)O)N)OP(=O)(O)O None
104766 33 42 None -562 11 Human 3.0 pKi None 3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 11138847
1365 33 42 None -562 11 Human 3.0 pKi None 3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 11138847
CHEMBL34453 33 42 None -562 11 Human 3.0 pKi None 3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 11138847
104766 33 42 None -562 11 Human 3.1 pKi None 3.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 11138847
1365 33 42 None -562 11 Human 3.1 pKi None 3.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 11138847
CHEMBL34453 33 42 None -562 11 Human 3.1 pKi None 3.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 11138847
1310 2315 110 None -389 18 Human 3.1 pKi None 3.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 11138847
1369 2315 110 None -389 18 Human 3.1 pKi None 3.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 11138847
33032 2315 110 None -389 18 Human 3.1 pKi None 3.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 11138847
44272391 2315 110 None -389 18 Human 3.1 pKi None 3.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 11138847
88747398 2315 110 None -389 18 Human 3.1 pKi None 3.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 11138847
CHEMBL575060 2315 110 None -389 18 Human 3.1 pKi None 3.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 11138847
DB00142 2315 110 None -389 18 Human 3.1 pKi None 3.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 11138847
1439 2469 15 None -7 2 Human 3.2 pKi None 3.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 173 3 3 3 -0.5 OC(=O)[C@H]1C[C@@H]1[C@@](C(=O)O)(N)C 11138847
5311457 2469 15 None -7 2 Human 3.2 pKi None 3.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 173 3 3 3 -0.5 OC(=O)[C@H]1C[C@@H]1[C@@](C(=O)O)(N)C 11138847
CHEMBL41013 2469 15 None -7 2 Human 3.2 pKi None 3.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 173 3 3 3 -0.5 OC(=O)[C@H]1C[C@@H]1[C@@](C(=O)O)(N)C 11138847
1373 2475 51 None -25 5 Human 3.2 pKi None 3.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 209 3 3 3 0.6 OC(=O)c1ccc(cc1)[C@@](C(=O)O)(N)C 11138847
139055582 2475 51 None -25 5 Human 3.2 pKi None 3.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 209 3 3 3 0.6 OC(=O)c1ccc(cc1)[C@@](C(=O)O)(N)C 11138847
446355 2475 51 None -25 5 Human 3.2 pKi None 3.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 209 3 3 3 0.6 OC(=O)c1ccc(cc1)[C@@](C(=O)O)(N)C 11138847
CHEMBL257626 2475 51 None -25 5 Human 3.2 pKi None 3.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 209 3 3 3 0.6 OC(=O)c1ccc(cc1)[C@@](C(=O)O)(N)C 11138847
DB04256 2475 51 None -25 5 Human 3.2 pKi None 3.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 209 3 3 3 0.6 OC(=O)c1ccc(cc1)[C@@](C(=O)O)(N)C 11138847
1440 2682 0 None - 1 Human 3.6 pKi None 3.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 275 6 3 5 1.0 OC(=O)C(COP(=O)(Oc1ccccc1)O)(N)C 11138847
5311463 2682 0 None - 1 Human 3.6 pKi None 3.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 275 6 3 5 1.0 OC(=O)C(COP(=O)(Oc1ccccc1)O)(N)C 11138847
CHEMBL1609272 2682 0 None - 1 Human 3.6 pKi None 3.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 275 6 3 5 1.0 OC(=O)C(COP(=O)(Oc1ccccc1)O)(N)C 11138847
1410 2274 48 None -1698 6 Human 3.7 pKi None 3.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 11138847
1412 2274 48 None -1698 6 Human 3.7 pKi None 3.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 11138847
179394 2274 48 None -1698 6 Human 3.7 pKi None 3.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 11138847
57689795 2274 48 None -1698 6 Human 3.7 pKi None 3.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 11138847
CHEMBL33567 2274 48 None -1698 6 Human 3.7 pKi None 3.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 4 4 3 -1.0 OC(=O)[C@H](CCP(=O)(O)O)N 11138847
1438 3154 0 None - 1 Human 3.7 pKi None 3.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 393 11 6 8 -1.5 NCCO/C=C/C(C(=O)O)NCC1=C(CNC(C1=O)C)COP(=O)(O)O 11138847
444843 3154 0 None - 1 Human 3.7 pKi None 3.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 393 11 6 8 -1.5 NCCO/C=C/C(C(=O)O)NCC1=C(CNC(C1=O)C)COP(=O)(O)O 11138847
1414 2459 0 None -6 2 Human 3.8 pKi None 3.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 197 4 4 3 -0.6 OC(=O)[C@](CCP(=O)(O)O)(N)C 11138847
1795545 2459 0 None -6 2 Human 3.8 pKi None 3.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 197 4 4 3 -0.6 OC(=O)[C@](CCP(=O)(O)O)(N)C 11138847
CHEMBL1488784 2459 0 None -6 2 Human 3.8 pKi None 3.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 197 4 4 3 -0.6 OC(=O)[C@](CCP(=O)(O)O)(N)C 11138847
1415 2614 41 None -14 3 Human 3.8 pKi None 3.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 245 3 4 3 -0.3 OC(=O)C(c1ccc(cc1)P(=O)(O)O)(N)C 11138847
3972752 2614 41 None -14 3 Human 3.8 pKi None 3.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 245 3 4 3 -0.3 OC(=O)C(c1ccc(cc1)P(=O)(O)O)(N)C 11138847
CHEMBL86508 2614 41 None -14 3 Human 3.8 pKi None 3.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 245 3 4 3 -0.3 OC(=O)C(c1ccc(cc1)P(=O)(O)O)(N)C 11138847
1368 2290 37 None -398 11 Human 4.3 pKi None 4.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 11138847
5310956 2290 37 None -398 11 Human 4.3 pKi None 4.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 11138847
CHEMBL280563 2290 37 None -398 11 Human 4.3 pKi None 4.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 11138847
1398 365 0 None -7 2 Human 4.4 pKi None 4.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 199 4 4 4 -1.1 OC(=O)C(COP(=O)(O)O)(N)C 11138847
3964633 365 0 None -7 2 Human 4.4 pKi None 4.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 199 4 4 4 -1.1 OC(=O)C(COP(=O)(O)O)(N)C 11138847
CHEMBL1437137 365 0 None -7 2 Human 4.4 pKi None 4.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 199 4 4 4 -1.1 OC(=O)C(COP(=O)(O)O)(N)C 11138847
1411 2361 66 None - 1 Human 4.4 pKi None 4.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 11138847
4120 2361 66 None - 1 Human 4.4 pKi None 4.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 11138847
57689797 2361 66 None - 1 Human 4.4 pKi None 4.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 11138847
68841 2361 66 None - 1 Human 4.4 pKi None 4.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 11138847
CHEMBL284377 2361 66 None - 1 Human 4.4 pKi None 4.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 11138847
DB04522 2361 66 None - 1 Human 4.4 pKi None 4.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 185 4 4 4 -1.5 OC(=O)[C@H](COP(=O)(O)O)N 11138847
1377 1340 26 None -316 6 Human 4.7 pKi None 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 4 4 4 -1.6 N[C@@H](C1[C@H]([C@@H]1C(=O)O)C(=O)O)C(=O)O 11138847
5310979 1340 26 None -316 6 Human 4.7 pKi None 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 4 4 4 -1.6 N[C@@H](C1[C@H]([C@@H]1C(=O)O)C(=O)O)C(=O)O 11138847
CHEMBL284193 1340 26 None -316 6 Human 4.7 pKi None 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 4 4 4 -1.6 N[C@@H](C1[C@H]([C@@H]1C(=O)O)C(=O)O)C(=O)O 11138847
1378 2417 54 None -123 10 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 11138847
1399 2417 54 None -123 10 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 11138847
9819927 2417 54 None -123 10 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 11138847
CHEMBL432038 2417 54 None -123 10 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 11138847