Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
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name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Potency)
# tested GPCRs
(Potency)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
145422113 177790 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 177790 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 169561 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 169561 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 164794 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 164794 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 169561 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 169561 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 169512 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 169512 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 187351 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 187351 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 187351 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 169512 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 169512 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 188534 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 188534 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 180490 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 180490 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 186559 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 186559 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 187242 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 187242 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 187351 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 187351 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 187351 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 188880 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 188880 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 188880 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 166714 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 166714 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 188213 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 188213 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 167473 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 167473 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 166631 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 166631 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 165205 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 165205 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 9146 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 9146 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 9146 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 187837 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 187837 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 186665 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 186665 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 186559 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 186559 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 186630 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 186630 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 186665 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 186665 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 167250 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 167250 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 189914 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 189914 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 188880 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 188880 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 188880 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 10815 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 10815 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 10815 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 10815 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 10815 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 10815 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 169800 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 169800 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 169800 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 169800 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 10799 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 10799 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 10799 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 10799 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 10799 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 10799 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 169152 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 169152 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 187351 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 187351 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 187351 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 167351 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 167351 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 169152 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 169152 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 167373 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 167373 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 186559 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 186559 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 7190 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 7190 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 7190 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 177125 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 177125 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 179086 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 179086 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 188880 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 188880 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 188880 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 167202 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 167202 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 169808 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 169808 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 168874 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 168874 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 169808 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 169808 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 168874 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 168874 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 186683 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 186683 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 186948 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 186948 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 188697 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 188697 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 186630 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 186630 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 167092 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 167092 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 189292 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 189292 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 182185 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 182185 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 169579 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 169579 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 167527 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 167527 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 169579 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 169579 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 169087 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 169087 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 169087 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 169087 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 169375 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 169375 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 169375 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 169375 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 190308 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 190308 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 95518 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 95518 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 95518 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 95518 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 167227 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 167227 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 167718 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 167718 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 167513 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 167513 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 167002 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 167002 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 189674 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 189674 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 187906 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 187906 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 188953 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 188953 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 167303 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 167303 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 166286 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 166286 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 190161 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 190161 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 8122 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 8122 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 8122 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 14990 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 14990 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 9070 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 9070 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 9070 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 169067 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 169067 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 169067 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 169067 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 8854 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 8854 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 8854 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 186731 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 186731 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 187096 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 187096 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 164124 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 164124 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 166846 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 166846 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 87585 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 87585 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 9145 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 9145 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 9145 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 165802 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 165802 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 169356 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 169356 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 169356 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 169356 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 166615 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 166615 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 163694 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 163694 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 164473 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 164473 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 168857 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 168857 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 168857 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 168857 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 187105 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 187105 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 166732 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 166732 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 166786 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 166786 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 187826 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 187826 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 187275 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 187275 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 162647 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 162647 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 187576 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 187576 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 168848 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 168848 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 168848 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 168848 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 187275 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 187275 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 14592 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 14592 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 14592 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 14592 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 190169 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 190169 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 206916 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 206916 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 196970 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 196970 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 197842 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 197842 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 198553 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 198553 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 206440 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 206440 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 156406 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 156406 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 198553 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 198553 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 179284 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 179284 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 181136 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 181136 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 206761 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 206761 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 186991 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 186991 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 179284 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 179284 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 181596 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 181596 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 181596 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 181596 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 178763 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 178763 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 178763 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 178763 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 187994 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 187994 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 180090 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 180090 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 177028 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 177028 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 180090 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 180090 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 178763 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 178763 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 182046 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 182046 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 169501 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 169501 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 206441 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 206441 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 169501 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 169501 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 177602 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 177602 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 177602 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 177602 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 206789 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 206789 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 198904 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 198904 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 187247 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 187247 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 189675 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 189675 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 190251 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 190251 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 114656 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 114656 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 177903 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 177903 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 178418 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 178418 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 198904 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 198904 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 199169 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 199169 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 199169 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 199169 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 178265 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 178265 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 178265 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 178265 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 181163 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 181163 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 197050 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 197050 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 188128 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 188128 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 175862 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 175862 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 178418 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 178418 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 178516 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 178516 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 181163 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 181163 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 197050 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 197050 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 9254 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 9254 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 9254 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 178418 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 178418 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 178516 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 178516 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 181163 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 181163 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 176822 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 176822 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 206791 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 206791 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 206671 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 206671 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 187112 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 187112 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 189916 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 189916 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 161443 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 161443 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 178516 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 178516 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 187153 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 187153 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 214830 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 214830 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 177150 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 177150 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 196985 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 196985 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 196985 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 196985 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 206915 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 206915 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 189134 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 189134 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 198074 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 198074 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 9362 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 9362 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 9362 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 9362 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 9362 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 9362 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 161444 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 161444 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 214759 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 214759 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 198867 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 198867 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 198867 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 198867 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 198074 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 198074 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 190212 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 190212 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 180951 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 180951 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 180951 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 180951 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 206439 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 206439 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 188813 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 188813 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 187646 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 187646 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 176993 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 176993 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 206606 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 206606 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 176993 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 176993 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 196824 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 196824 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 10828 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 10828 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 10828 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 10828 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 10828 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 10828 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 187055 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 187055 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 10828 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 10828 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 10828 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 177545 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 177545 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 196824 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 196824 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 189408 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 189408 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 186175 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 186175 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 186651 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 186651 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 186203 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 186203 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 189393 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 189393 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 177623 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 177623 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 187621 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 187621 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 188307 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 188307 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 190281 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 190281 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 179172 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 179172 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 169381 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 169381 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 206851 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 206851 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 169381 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 169381 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 189753 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 189753 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 186764 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 186764 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 169381 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 169381 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 186424 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 186424 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 169381 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 169381 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 179172 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 179172 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 168859 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 168859 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 208444 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 208444 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 168859 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 168859 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 180036 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 180036 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 178521 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 178521 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 178521 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 178521 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 187742 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 187742 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 52161 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 52161 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 115051 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 115051 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 7087 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 7087 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 7087 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 179172 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 179172 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 32125 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 32125 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 7087 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 7087 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 7087 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 189162 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 189162 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 7087 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 7087 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 7087 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 7087 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 7087 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 7087 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 215137 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 215137 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 168832 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 168832 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 168832 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 168832 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 206852 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 206852 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 10827 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 10827 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 10827 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 10827 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 10827 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 10827 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 10827 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 10827 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 10827 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 10827 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 10827 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 10827 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 10827 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 10827 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 10827 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 119321 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 119321 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 176349 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 176349 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 168925 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 168925 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 169178 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 169178 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 168925 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 168925 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 169178 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 169178 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 168925 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 168925 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 170300 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 170300 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 176834 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 176834 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 10827 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 10827 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 10827 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 168925 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 168925 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 169178 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 169178 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 176834 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 176834 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 188071 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 188071 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 186511 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 186511 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 188261 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 188261 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 169178 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 169178 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 206921 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 206921 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 214533 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 214533 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 206635 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 206635 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 9195 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 9195 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 9195 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 9195 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 9195 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 9195 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 9195 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 9195 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 9140 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 9140 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 9140 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 9140 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 9140 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 9140 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9054 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 9054 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 9054 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 9054 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 9054 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 9145 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 9145 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 9145 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 9140 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 9140 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 9140 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 9140 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 9140 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 9140 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 9146 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 9146 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 9146 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 7190 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 7190 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 7190 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 10827 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 10827 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 10827 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 10828 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 10828 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 10828 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 9362 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 9362 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 9362 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 9362 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 9362 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 9362 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 7087 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 7087 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 7087 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 7087 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 7087 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 7087 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 9254 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 9254 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 9254 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 8854 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 8854 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 8854 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 8854 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 8854 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 8854 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




Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Affinity)
# tested GPCRs
(Affinity)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
134536725 177081 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 177081 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 181351 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 181351 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 186559 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 186559 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 188880 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 188880 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 188880 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 186559 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 186559 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 200499 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 201301 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 200540 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 200540 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 201220 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 201220 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 201108 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 201246 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 10815 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 10815 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 10815 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 200945 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 10799 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 10799 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 10799 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 200904 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 188880 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 188880 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 188880 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 200253 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 201185 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 201287 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 201287 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 200837 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 176894 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 176894 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 75567 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 75567 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 200374 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 201095 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 201095 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 201098 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 201230 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 200457 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 200457 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 201125 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 200891 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 201067 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 181351 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 181351 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 169356 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 169356 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 7190 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 7190 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 7190 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 168857 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 168857 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 168857 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 168857 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 200253 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 186665 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 186665 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 186665 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 186665 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 177044 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 177044 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 187275 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 187275 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 187275 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 187275 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 200801 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 187351 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 187351 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 187351 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 187351 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 187351 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 187351 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 188880 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 188880 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 188880 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 178418 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 178418 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 178418 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 178418 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 168925 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 168925 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 168925 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 168925 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 169381 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 169381 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 9195 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 9195 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 9195 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 9195 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 169381 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 169381 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 199169 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 199169 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 199169 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 199169 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 179172 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 179172 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 197842 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 197842 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 179172 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 179172 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 197842 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 197842 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 197050 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 197050 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 197050 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 197050 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 196985 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 196985 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 196985 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 196985 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 169178 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 169178 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 178516 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 178516 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 169178 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 169178 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 178516 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 178516 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 10827 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 10827 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 10827 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 198553 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 198553 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 198553 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 198553 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 10827 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 10827 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 10827 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 196824 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 196824 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 198074 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 198074 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 198867 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 198867 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 198867 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 198867 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 198074 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 198074 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 196824 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 196824 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 9195 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 9195 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 9195 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 9195 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 9307 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 9307 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 9307 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 10871 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 10871 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 9195 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 9195 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 9195 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 9195 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 33885 30 Functional -38 43 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
CHEMBL136560 33885 30 Functional -38 43 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
2207 106641 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 106641 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 140299 14 Functional -1778 45 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
CHEMBL370805 140299 14 Functional -1778 45 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
162265 209053 22 Functional -239 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
4786 209053 22 Functional -239 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
CHEMBL61006 209053 22 Functional -239 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
25137849 222958 0 Functional -4 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
71290 222958 0 Functional -4 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
None 223104 0 Functional -13 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 2 1 2 1.2 CC(C(=O)C1=CC=CC=C1)N None
1576 223105 0 Functional -16 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 163 3 1 2 1.5 CC(C(=O)C1=CC=CC=C1)NC None
None 223117 0 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 6822 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 6822 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 6822 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 6822 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 6822 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 6822 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9247 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 9247 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 9247 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 9253 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 9253 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 9253 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 9253 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 9253 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 9460 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 9460 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 9460 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 9054 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 9054 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 9054 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 9054 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 9054 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 9928 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 9928 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 9237 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 9237 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 9237 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 9392 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 9392 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 9392 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 9070 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 9070 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 9070 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 7153 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 7153 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 7153 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 9140 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 9140 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 9140 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 9140 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 9140 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 9140 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 8122 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 8122 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 8122 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 9195 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 9195 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 9195 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 9195 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