Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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name		 GPCRdb
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 Assay
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 Activity
Type		 Activity
Relation		 Activity
Value		 p-value
(-log)		 Fold
selectivity		 Tested
GPCRs		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
1392 73 None 32 Rat Functional pEC50 = 4 4.0 -323 4
Tested for the agonistic activity against Metabotropic glutamate receptor 1Tested for the agonistic activity against Metabotropic glutamate receptor 1
ChEMBL 174 2 4 4 -1.8 OC(=O)[C@@H]1NC[C@@](C1)(N)C(=O)O 10.1016/S0960-894X(97)00068-1
5310984 73 None 32 Rat Functional pEC50 = 4 4.0 -323 4
Tested for the agonistic activity against Metabotropic glutamate receptor 1Tested for the agonistic activity against Metabotropic glutamate receptor 1
ChEMBL 174 2 4 4 -1.8 OC(=O)[C@@H]1NC[C@@](C1)(N)C(=O)O 10.1016/S0960-894X(97)00068-1
CHEMBL40086 73 None 32 Rat Functional pEC50 = 4 4.0 -323 4
Tested for the agonistic activity against Metabotropic glutamate receptor 1Tested for the agonistic activity against Metabotropic glutamate receptor 1
ChEMBL 174 2 4 4 -1.8 OC(=O)[C@@H]1NC[C@@](C1)(N)C(=O)O 10.1016/S0960-894X(97)00068-1
44573737 192938 None 0 Rat Functional pEC50 = 7.0 7.0 - 1
Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology
ChEMBL 378 2 1 4 4.7 O=C(Nc1nc(C(F)(F)F)co1)C1c2ccccc2Oc2c(F)cccc21 10.1016/j.bmcl.2009.01.108
CHEMBL522161 192938 None 0 Rat Functional pEC50 = 7.0 7.0 - 1
Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology
ChEMBL 378 2 1 4 4.7 O=C(Nc1nc(C(F)(F)F)co1)C1c2ccccc2Oc2c(F)cccc21 10.1016/j.bmcl.2009.01.108
1310 2315 None 61 Human Functional pEC50 = 6.0 6.0 -741 17
Effect of compound on Metabotropic glutamate receptor 1 expressed in HEK 293 cells was determined by measuring IP production relative to glutamateEffect of compound on Metabotropic glutamate receptor 1 expressed in HEK 293 cells was determined by measuring IP production relative to glutamate
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/s0960-894x(99)00641-1
1369 2315 None 61 Human Functional pEC50 = 6.0 6.0 -741 17
Effect of compound on Metabotropic glutamate receptor 1 expressed in HEK 293 cells was determined by measuring IP production relative to glutamateEffect of compound on Metabotropic glutamate receptor 1 expressed in HEK 293 cells was determined by measuring IP production relative to glutamate
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/s0960-894x(99)00641-1
33032 2315 None 61 Human Functional pEC50 = 6.0 6.0 -741 17
Effect of compound on Metabotropic glutamate receptor 1 expressed in HEK 293 cells was determined by measuring IP production relative to glutamateEffect of compound on Metabotropic glutamate receptor 1 expressed in HEK 293 cells was determined by measuring IP production relative to glutamate
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/s0960-894x(99)00641-1
44272391 2315 None 61 Human Functional pEC50 = 6.0 6.0 -741 17
Effect of compound on Metabotropic glutamate receptor 1 expressed in HEK 293 cells was determined by measuring IP production relative to glutamateEffect of compound on Metabotropic glutamate receptor 1 expressed in HEK 293 cells was determined by measuring IP production relative to glutamate
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/s0960-894x(99)00641-1
88747398 2315 None 61 Human Functional pEC50 = 6.0 6.0 -741 17
Effect of compound on Metabotropic glutamate receptor 1 expressed in HEK 293 cells was determined by measuring IP production relative to glutamateEffect of compound on Metabotropic glutamate receptor 1 expressed in HEK 293 cells was determined by measuring IP production relative to glutamate
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/s0960-894x(99)00641-1
CHEMBL575060 2315 None 61 Human Functional pEC50 = 6.0 6.0 -741 17
Effect of compound on Metabotropic glutamate receptor 1 expressed in HEK 293 cells was determined by measuring IP production relative to glutamateEffect of compound on Metabotropic glutamate receptor 1 expressed in HEK 293 cells was determined by measuring IP production relative to glutamate
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/s0960-894x(99)00641-1
DB00142 2315 None 61 Human Functional pEC50 = 6.0 6.0 -741 17
Effect of compound on Metabotropic glutamate receptor 1 expressed in HEK 293 cells was determined by measuring IP production relative to glutamateEffect of compound on Metabotropic glutamate receptor 1 expressed in HEK 293 cells was determined by measuring IP production relative to glutamate
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/s0960-894x(99)00641-1
122196105 124307 None 0 Human Functional pEC50 = 7.0 7.0 22 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 448 3 1 4 5.3 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(C(F)(F)F)c1 10.1016/j.bmcl.2015.10.013
CHEMBL3634428 124307 None 0 Human Functional pEC50 = 7.0 7.0 22 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 448 3 1 4 5.3 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(C(F)(F)F)c1 10.1016/j.bmcl.2015.10.013
127032507 139111 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 380 3 1 3 5.0 Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(C)cccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
CHEMBL3785852 139111 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 380 3 1 3 5.0 Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(C)cccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
127032507 139111 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 380 3 1 3 5.0 Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(C)cccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
CHEMBL3785852 139111 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 380 3 1 3 5.0 Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(C)cccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
127026165 137782 None 4 Human Functional pEC50 = 7.9 7.9 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 378 3 1 4 4.1 Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3occc3C)c(F)c1)C2=O 10.1016/j.bmcl.2015.12.104
CHEMBL3758746 137782 None 4 Human Functional pEC50 = 7.9 7.9 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 378 3 1 4 4.1 Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3occc3C)c(F)c1)C2=O 10.1016/j.bmcl.2015.12.104
192790 71913 None 26 Rat Functional pEC50 = 5.0 5.0 4 2
Agonist activity in rat at mGlu1a receptor expressed in HEK293 cellsAgonist activity in rat at mGlu1a receptor expressed in HEK293 cells
ChEMBL 163 4 4 4 -1.8 N[C@@H](C[C@H](O)C(=O)O)C(=O)O 10.1016/s0960-894x(01)00158-5
44286641 71913 None 26 Rat Functional pEC50 = 5.0 5.0 4 2
Agonist activity in rat at mGlu1a receptor expressed in HEK293 cellsAgonist activity in rat at mGlu1a receptor expressed in HEK293 cells
ChEMBL 163 4 4 4 -1.8 N[C@@H](C[C@H](O)C(=O)O)C(=O)O 10.1016/s0960-894x(01)00158-5
CHEMBL197110 71913 None 26 Rat Functional pEC50 = 5.0 5.0 4 2
Agonist activity in rat at mGlu1a receptor expressed in HEK293 cellsAgonist activity in rat at mGlu1a receptor expressed in HEK293 cells
ChEMBL 163 4 4 4 -1.8 N[C@@H](C[C@H](O)C(=O)O)C(=O)O 10.1016/s0960-894x(01)00158-5
122193176 123998 None 0 Rat Functional pEC50 = 7.0 7.0 -1 3
Positive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay
ChEMBL 414 3 1 4 4.9 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
CHEMBL3628112 123998 None 0 Rat Functional pEC50 = 7.0 7.0 -1 3
Positive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay
ChEMBL 414 3 1 4 4.9 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
122193179 124001 None 0 Rat Functional pEC50 = 7.0 7.0 -1 2
Positive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay
ChEMBL 381 3 1 5 3.7 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccncc3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
CHEMBL3628115 124001 None 0 Rat Functional pEC50 = 7.0 7.0 -1 2
Positive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay
ChEMBL 381 3 1 5 3.7 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccncc3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
122193176 123998 None 0 Rat Functional pEC50 = 7.0 7.0 -1 3
Positive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay
ChEMBL 414 3 1 4 4.9 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
CHEMBL3628112 123998 None 0 Rat Functional pEC50 = 7.0 7.0 -1 3
Positive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay
ChEMBL 414 3 1 4 4.9 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
122193179 124001 None 0 Rat Functional pEC50 = 7.0 7.0 -1 2
Positive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay
ChEMBL 381 3 1 5 3.7 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccncc3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
CHEMBL3628115 124001 None 0 Rat Functional pEC50 = 7.0 7.0 -1 2
Positive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay
ChEMBL 381 3 1 5 3.7 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccncc3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
127030066 139126 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 434 3 1 3 5.7 Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(cccc3C(F)(F)F)C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
CHEMBL3785990 139126 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 434 3 1 3 5.7 Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(cccc3C(F)(F)F)C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
127026165 137782 None 4 Human Functional pEC50 = 4.9 4.9 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 378 3 1 4 4.1 Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3occc3C)c(F)c1)C2=O 10.1016/j.bmcl.2015.12.104
CHEMBL3758746 137782 None 4 Human Functional pEC50 = 4.9 4.9 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 378 3 1 4 4.1 Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3occc3C)c(F)c1)C2=O 10.1016/j.bmcl.2015.12.104
127030066 139126 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 434 3 1 3 5.7 Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(cccc3C(F)(F)F)C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
CHEMBL3785990 139126 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 434 3 1 3 5.7 Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(cccc3C(F)(F)F)C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
122196123 124324 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 364 3 1 4 3.8 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)cc1F 10.1016/j.bmcl.2016.03.031
CHEMBL3634445 124324 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 364 3 1 4 3.8 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)cc1F 10.1016/j.bmcl.2016.03.031
122196103 124305 None 0 Human Functional pEC50 = 6.9 6.9 53 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 414 3 1 4 4.7 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(C(F)(F)F)c1 10.1016/j.bmcl.2015.10.013
CHEMBL3634426 124305 None 0 Human Functional pEC50 = 6.9 6.9 53 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 414 3 1 4 4.7 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(C(F)(F)F)c1 10.1016/j.bmcl.2015.10.013
127029303 137879 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 380 3 2 4 3.4 Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3759563 137879 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 380 3 2 4 3.4 Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
44573779 187743 None 0 Rat Functional pEC50 = 6.9 6.9 - 1
Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay
ChEMBL 328 2 1 4 3.8 O=C(Nc1ncco1)C1c2cc(F)ccc2Oc2ccc(F)cc21 10.1016/j.bmcl.2009.01.108
CHEMBL494961 187743 None 0 Rat Functional pEC50 = 6.9 6.9 - 1
Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay
ChEMBL 328 2 1 4 3.8 O=C(Nc1ncco1)C1c2cc(F)ccc2Oc2ccc(F)cc21 10.1016/j.bmcl.2009.01.108
127029303 137879 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 380 3 2 4 3.4 Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3759563 137879 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 380 3 2 4 3.4 Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
127033422 139177 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 384 3 1 3 4.8 Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(Cl)cccc3C2=O)cc1F 10.1016/j.bmcl.2016.03.031
CHEMBL3786552 139177 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 384 3 1 3 4.8 Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(Cl)cccc3C2=O)cc1F 10.1016/j.bmcl.2016.03.031
127033422 139177 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 384 3 1 3 4.8 Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(Cl)cccc3C2=O)cc1F 10.1016/j.bmcl.2016.03.031
CHEMBL3786552 139177 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 384 3 1 3 4.8 Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(Cl)cccc3C2=O)cc1F 10.1016/j.bmcl.2016.03.031
127033432 139041 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 431 3 1 3 5.5 O=C(Nc1ccc(N2Cc3c(Cl)cccc3C2=O)c(Cl)c1)c1ncccc1Cl 10.1016/j.bmcl.2016.03.031
CHEMBL3785119 139041 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 431 3 1 3 5.5 O=C(Nc1ccc(N2Cc3c(Cl)cccc3C2=O)c(Cl)c1)c1ncccc1Cl 10.1016/j.bmcl.2016.03.031
127033432 139041 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 431 3 1 3 5.5 O=C(Nc1ccc(N2Cc3c(Cl)cccc3C2=O)c(Cl)c1)c1ncccc1Cl 10.1016/j.bmcl.2016.03.031
CHEMBL3785119 139041 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 431 3 1 3 5.5 O=C(Nc1ccc(N2Cc3c(Cl)cccc3C2=O)c(Cl)c1)c1ncccc1Cl 10.1016/j.bmcl.2016.03.031
127025550 137916 None 0 Human Functional pEC50 = 5.9 5.9 -1 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 415 3 1 5 4.3 Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3759867 137916 None 0 Human Functional pEC50 = 5.9 5.9 -1 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 415 3 1 5 4.3 Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
127034537 139056 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 380 3 1 3 5.1 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)CCc3ccccc32)c(Cl)c1 10.1016/j.bmcl.2016.03.031
CHEMBL3785267 139056 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 380 3 1 3 5.1 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)CCc3ccccc32)c(Cl)c1 10.1016/j.bmcl.2016.03.031
122196123 124324 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 364 3 1 4 3.8 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)cc1F 10.1016/j.bmcl.2015.10.013
CHEMBL3634445 124324 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 364 3 1 4 3.8 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)cc1F 10.1016/j.bmcl.2015.10.013
10362260 187742 None 0 Rat Functional pEC50 = 6.9 6.9 - 1
Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology
ChEMBL 378 2 1 4 4.7 O=C(Nc1ncc(C(F)(F)F)o1)C1c2ccccc2Oc2c(F)cccc21 10.1016/j.bmcl.2009.01.108
CHEMBL494960 187742 None 0 Rat Functional pEC50 = 6.9 6.9 - 1
Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology
ChEMBL 378 2 1 4 4.7 O=C(Nc1ncc(C(F)(F)F)o1)C1c2ccccc2Oc2c(F)cccc21 10.1016/j.bmcl.2009.01.108
127025550 137916 None 0 Human Functional pEC50 = 5.9 5.9 -1 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 415 3 1 5 4.3 Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3759867 137916 None 0 Human Functional pEC50 = 5.9 5.9 -1 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 415 3 1 5 4.3 Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
127034537 139056 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 380 3 1 3 5.1 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)CCc3ccccc32)c(Cl)c1 10.1016/j.bmcl.2016.03.031
CHEMBL3785267 139056 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 380 3 1 3 5.1 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)CCc3ccccc32)c(Cl)c1 10.1016/j.bmcl.2016.03.031
127033962 139129 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 366 3 1 3 5.1 Cc1ccoc1C(=O)Nc1ccc(N2CCc3ccccc3C2)c(Cl)c1 10.1016/j.bmcl.2016.03.031
CHEMBL3786032 139129 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 366 3 1 3 5.1 Cc1ccoc1C(=O)Nc1ccc(N2CCc3ccccc3C2)c(Cl)c1 10.1016/j.bmcl.2016.03.031
162643634 181861 None 0 Human Functional pEC50 = 6.9 6.9 -1 3
Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate 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 181861 None 0 Human Functional pEC50 = 6.9 6.9 -1 3
Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate 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
127033424 139070 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 411 3 1 3 5.1 Cc1cccnc1C(=O)Nc1ccc(N2Cc3c(Cl)cccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
CHEMBL3785387 139070 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 411 3 1 3 5.1 Cc1cccnc1C(=O)Nc1ccc(N2Cc3c(Cl)cccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
127026139 137784 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 431 3 1 5 4.8 Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3758756 137784 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 431 3 1 5 4.8 Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
127026139 137784 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 431 3 1 5 4.8 Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3758756 137784 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 431 3 1 5 4.8 Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
1310 2315 None 61 Rat Functional pEC50 = 4.9 4.9 -794 17
Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
1369 2315 None 61 Rat Functional pEC50 = 4.9 4.9 -794 17
Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
33032 2315 None 61 Rat Functional pEC50 = 4.9 4.9 -794 17
Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
44272391 2315 None 61 Rat Functional pEC50 = 4.9 4.9 -794 17
Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
88747398 2315 None 61 Rat Functional pEC50 = 4.9 4.9 -794 17
Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
CHEMBL575060 2315 None 61 Rat Functional pEC50 = 4.9 4.9 -794 17
Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
DB00142 2315 None 61 Rat Functional pEC50 = 4.9 4.9 -794 17
Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
44573779 187743 None 0 Rat Functional pEC50 = 6.9 6.9 - 1
Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology
ChEMBL 328 2 1 4 3.8 O=C(Nc1ncco1)C1c2cc(F)ccc2Oc2ccc(F)cc21 10.1016/j.bmcl.2009.01.108
CHEMBL494961 187743 None 0 Rat Functional pEC50 = 6.9 6.9 - 1
Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology
ChEMBL 328 2 1 4 3.8 O=C(Nc1ncco1)C1c2cc(F)ccc2Oc2ccc(F)cc21 10.1016/j.bmcl.2009.01.108
4125492 140179 None 9 Human Functional pEC50 = 5.9 5.9 2 2
Positive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 308 2 1 4 4.0 O=C(Nc1nccs1)C1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2016.03.044
CHEMBL3800589 140179 None 9 Human Functional pEC50 = 5.9 5.9 2 2
Positive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 308 2 1 4 4.0 O=C(Nc1nccs1)C1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2016.03.044
127025831 137856 None 0 Human Functional pEC50 = 6.9 6.9 4 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 399 3 1 5 3.8 Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3759381 137856 None 0 Human Functional pEC50 = 6.9 6.9 4 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 399 3 1 5 3.8 Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
127025831 137856 None 0 Human Functional pEC50 = 6.9 6.9 4 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 399 3 1 5 3.8 Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3759381 137856 None 0 Human Functional pEC50 = 6.9 6.9 4 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 399 3 1 5 3.8 Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
4125492 140179 None 9 Human Functional pEC50 = 5.9 5.9 2 2
Positive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 308 2 1 4 4.0 O=C(Nc1nccs1)C1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2016.03.044
CHEMBL3800589 140179 None 9 Human Functional pEC50 = 5.9 5.9 2 2
Positive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 308 2 1 4 4.0 O=C(Nc1nccs1)C1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2016.03.044
122196110 124311 None 0 Human Functional pEC50 = 6.8 6.8 13 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 394 4 1 5 3.8 COc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(F)c2C1=O 10.1016/j.bmcl.2015.10.013
CHEMBL3634432 124311 None 0 Human Functional pEC50 = 6.8 6.8 13 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 394 4 1 5 3.8 COc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(F)c2C1=O 10.1016/j.bmcl.2015.10.013
127033424 139070 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 411 3 1 3 5.1 Cc1cccnc1C(=O)Nc1ccc(N2Cc3c(Cl)cccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
CHEMBL3785387 139070 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 411 3 1 3 5.1 Cc1cccnc1C(=O)Nc1ccc(N2Cc3c(Cl)cccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
127029002 137849 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 381 3 1 5 3.7 Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3759321 137849 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 381 3 1 5 3.7 Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
127029002 137849 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 381 3 1 5 3.7 Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3759321 137849 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 381 3 1 5 3.7 Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
122196125 124326 None 0 Human Functional pEC50 = 7.8 7.8 40 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 360 3 1 4 3.9 Cc1cc(N2C(=O)c3ccccc3C2=O)ccc1NC(=O)c1occc1C 10.1016/j.bmcl.2015.10.013
CHEMBL3634447 124326 None 0 Human Functional pEC50 = 7.8 7.8 40 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 360 3 1 4 3.9 Cc1cc(N2C(=O)c3ccccc3C2=O)ccc1NC(=O)c1occc1C 10.1016/j.bmcl.2015.10.013
104766 33 None 30 Rat Functional pEC50 = 4.8 4.8 -8 14
Activity tested at cloned rat Metabotropic glutamate receptor 1 expressed in Chinese Hamster Ovary (CHO) cellsActivity tested at cloned rat Metabotropic glutamate receptor 1 expressed in Chinese Hamster Ovary (CHO) cells
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1021/jm0308085
1365 33 None 30 Rat Functional pEC50 = 4.8 4.8 -8 14
Activity tested at cloned rat Metabotropic glutamate receptor 1 expressed in Chinese Hamster Ovary (CHO) cellsActivity tested at cloned rat Metabotropic glutamate receptor 1 expressed in Chinese Hamster Ovary (CHO) cells
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1021/jm0308085
CHEMBL34453 33 None 30 Rat Functional pEC50 = 4.8 4.8 -8 14
Activity tested at cloned rat Metabotropic glutamate receptor 1 expressed in Chinese Hamster Ovary (CHO) cellsActivity tested at cloned rat Metabotropic glutamate receptor 1 expressed in Chinese Hamster Ovary (CHO) cells
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1021/jm0308085
127029000 137852 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 396 3 1 4 4.8 Cc1sccc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3759354 137852 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 396 3 1 4 4.8 Cc1sccc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
127029000 137852 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 396 3 1 4 4.8 Cc1sccc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3759354 137852 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 396 3 1 4 4.8 Cc1sccc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
127034513 139170 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 332 3 1 3 4.0 Cc1ccoc1C(=O)Nc1ccc(N2Cc3ccccc3C2=O)cc1 10.1016/j.bmcl.2016.03.031
CHEMBL3786494 139170 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 332 3 1 3 4.0 Cc1ccoc1C(=O)Nc1ccc(N2Cc3ccccc3C2=O)cc1 10.1016/j.bmcl.2016.03.031
122196106 124308 None 0 Human Functional pEC50 = 6.8 6.8 18 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 432 3 1 4 4.8 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(C(F)(F)F)c1 10.1016/j.bmcl.2015.10.013
CHEMBL3634429 124308 None 0 Human Functional pEC50 = 6.8 6.8 18 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 432 3 1 4 4.8 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(C(F)(F)F)c1 10.1016/j.bmcl.2015.10.013
127034513 139170 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 332 3 1 3 4.0 Cc1ccoc1C(=O)Nc1ccc(N2Cc3ccccc3C2=O)cc1 10.1016/j.bmcl.2016.03.031
CHEMBL3786494 139170 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 332 3 1 3 4.0 Cc1ccoc1C(=O)Nc1ccc(N2Cc3ccccc3C2=O)cc1 10.1016/j.bmcl.2016.03.031
1310 2315 None 61 Rat Functional pEC50 = 5.8 5.8 -794 17
Agonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
1369 2315 None 61 Rat Functional pEC50 = 5.8 5.8 -794 17
Agonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
33032 2315 None 61 Rat Functional pEC50 = 5.8 5.8 -794 17
Agonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
44272391 2315 None 61 Rat Functional pEC50 = 5.8 5.8 -794 17
Agonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
88747398 2315 None 61 Rat Functional pEC50 = 5.8 5.8 -794 17
Agonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
CHEMBL575060 2315 None 61 Rat Functional pEC50 = 5.8 5.8 -794 17
Agonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
DB00142 2315 None 61 Rat Functional pEC50 = 5.8 5.8 -794 17
Agonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
122196092 124294 None 0 Human Functional pEC50 = 7.8 7.8 21 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 360 3 1 4 3.9 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)cc1 10.1016/j.bmcl.2015.10.013
CHEMBL3634415 124294 None 0 Human Functional pEC50 = 7.8 7.8 21 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 360 3 1 4 3.9 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)cc1 10.1016/j.bmcl.2015.10.013
122196120 124321 None 0 Human Functional pEC50 = 7.8 7.8 26 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 410 3 1 4 5.1 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c2ccccc12 10.1016/j.bmcl.2015.10.013
CHEMBL3634442 124321 None 0 Human Functional pEC50 = 7.8 7.8 26 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 410 3 1 4 5.1 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c2ccccc12 10.1016/j.bmcl.2015.10.013
1310 2315 None 61 Rat Functional pEC50 = 5.8 5.8 -794 17
Agonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
1369 2315 None 61 Rat Functional pEC50 = 5.8 5.8 -794 17
Agonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
33032 2315 None 61 Rat Functional pEC50 = 5.8 5.8 -794 17
Agonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
44272391 2315 None 61 Rat Functional pEC50 = 5.8 5.8 -794 17
Agonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
88747398 2315 None 61 Rat Functional pEC50 = 5.8 5.8 -794 17
Agonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
CHEMBL575060 2315 None 61 Rat Functional pEC50 = 5.8 5.8 -794 17
Agonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
DB00142 2315 None 61 Rat Functional pEC50 = 5.8 5.8 -794 17
Agonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.5b01333
44573780 187746 None 0 Rat Functional pEC50 = 6.8 6.8 - 1
Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology
ChEMBL 396 2 1 4 4.8 O=C(Nc1nc(C(F)(F)F)co1)C1c2cccc(F)c2Oc2c(F)cccc21 10.1016/j.bmcl.2009.01.108
CHEMBL494967 187746 None 0 Rat Functional pEC50 = 6.8 6.8 - 1
Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology
ChEMBL 396 2 1 4 4.8 O=C(Nc1nc(C(F)(F)F)co1)C1c2cccc(F)c2Oc2c(F)cccc21 10.1016/j.bmcl.2009.01.108
44573738 187710 None 0 Rat Functional pEC50 = 6.8 6.8 - 1
Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology
ChEMBL 396 2 1 4 4.8 O=C(Nc1ncc(C(F)(F)F)o1)C1c2cccc(F)c2Oc2c(F)cccc21 10.1016/j.bmcl.2009.01.108
CHEMBL494766 187710 None 0 Rat Functional pEC50 = 6.8 6.8 - 1
Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology
ChEMBL 396 2 1 4 4.8 O=C(Nc1ncc(C(F)(F)F)o1)C1c2cccc(F)c2Oc2c(F)cccc21 10.1016/j.bmcl.2009.01.108
162650632 180192 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay
ChEMBL 392 3 1 4 4.0 Cc1cc(N2C(=O)Cc3ccccc3C2=O)c(F)cc1NC(=O)c1occc1C 10.1016/j.bmcl.2020.127724
CHEMBL4748116 180192 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay
ChEMBL 392 3 1 4 4.0 Cc1cc(N2C(=O)Cc3ccccc3C2=O)c(F)cc1NC(=O)c1occc1C 10.1016/j.bmcl.2020.127724
775428 140018 None 9 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 302 2 1 3 4.0 O=C(Nc1ccccn1)C1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2016.03.044
CHEMBL3799600 140018 None 9 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 302 2 1 3 4.0 O=C(Nc1ccccn1)C1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2016.03.044
127026137 137897 None 0 Human Functional pEC50 = 5.8 5.8 1 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 382 3 1 6 3.1 Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3cccnc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3759705 137897 None 0 Human Functional pEC50 = 5.8 5.8 1 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 382 3 1 6 3.1 Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3cccnc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
127026059 137918 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 399 3 1 5 3.8 Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3759878 137918 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 399 3 1 5 3.8 Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
775428 140018 None 9 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 302 2 1 3 4.0 O=C(Nc1ccccn1)C1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2016.03.044
CHEMBL3799600 140018 None 9 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 302 2 1 3 4.0 O=C(Nc1ccccn1)C1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2016.03.044
127026137 137897 None 0 Human Functional pEC50 = 5.8 5.8 1 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 382 3 1 6 3.1 Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3cccnc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3759705 137897 None 0 Human Functional pEC50 = 5.8 5.8 1 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 382 3 1 6 3.1 Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3cccnc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
127032499 139131 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 352 3 1 3 5.0 Cc1ccoc1C(=O)Nc1ccc(N2Cc3ccccc3C2)c(Cl)c1 10.1016/j.bmcl.2016.03.031
CHEMBL3786060 139131 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 352 3 1 3 5.0 Cc1ccoc1C(=O)Nc1ccc(N2Cc3ccccc3C2)c(Cl)c1 10.1016/j.bmcl.2016.03.031
127033963 139060 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 400 3 1 3 5.3 Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(Cl)cccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
CHEMBL3785321 139060 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 400 3 1 3 5.3 Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(Cl)cccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
127032499 139131 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 352 3 1 3 5.0 Cc1ccoc1C(=O)Nc1ccc(N2Cc3ccccc3C2)c(Cl)c1 10.1016/j.bmcl.2016.03.031
CHEMBL3786060 139131 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 352 3 1 3 5.0 Cc1ccoc1C(=O)Nc1ccc(N2Cc3ccccc3C2)c(Cl)c1 10.1016/j.bmcl.2016.03.031
122196109 124142 None 0 Human Functional pEC50 = 7.8 7.8 36 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 410 4 1 5 4.3 COc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(Cl)c2C1=O 10.1016/j.bmcl.2015.10.013
CHEMBL3632642 124142 None 0 Human Functional pEC50 = 7.8 7.8 36 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 410 4 1 5 4.3 COc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(Cl)c2C1=O 10.1016/j.bmcl.2015.10.013
127047993 139738 None 1 Rat Functional pEC50 = 5.8 5.8 -3 2
Positive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 333 2 1 5 3.9 N#Cc1csc(NC(=O)C2c3ccccc3Oc3ccccc32)n1 10.1016/j.bmcl.2016.03.044
CHEMBL3797793 139738 None 1 Rat Functional pEC50 = 5.8 5.8 -3 2
Positive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 333 2 1 5 3.9 N#Cc1csc(NC(=O)C2c3ccccc3Oc3ccccc32)n1 10.1016/j.bmcl.2016.03.044
127025563 137828 None 0 Human Functional pEC50 = 6.7 6.7 2 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 415 3 1 5 4.3 Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3759171 137828 None 0 Human Functional pEC50 = 6.7 6.7 2 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 415 3 1 5 4.3 Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
127047993 139738 None 1 Rat Functional pEC50 = 5.7 5.7 -3 2
Positive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 333 2 1 5 3.9 N#Cc1csc(NC(=O)C2c3ccccc3Oc3ccccc32)n1 10.1016/j.bmcl.2016.03.044
CHEMBL3797793 139738 None 1 Rat Functional pEC50 = 5.7 5.7 -3 2
Positive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 333 2 1 5 3.9 N#Cc1csc(NC(=O)C2c3ccccc3Oc3ccccc32)n1 10.1016/j.bmcl.2016.03.044
127025563 137828 None 0 Human Functional pEC50 = 6.7 6.7 2 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 415 3 1 5 4.3 Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3759171 137828 None 0 Human Functional pEC50 = 6.7 6.7 2 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 415 3 1 5 4.3 Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
127027100 137824 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 396 3 1 4 4.8 Cc1ccsc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3759137 137824 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 396 3 1 4 4.8 Cc1ccsc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
44573737 192938 None 0 Rat Functional pEC50 = 7.7 7.7 - 1
Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay
ChEMBL 378 2 1 4 4.7 O=C(Nc1nc(C(F)(F)F)co1)C1c2ccccc2Oc2c(F)cccc21 10.1016/j.bmcl.2009.01.108
CHEMBL522161 192938 None 0 Rat Functional pEC50 = 7.7 7.7 - 1
Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay
ChEMBL 378 2 1 4 4.7 O=C(Nc1nc(C(F)(F)F)co1)C1c2ccccc2Oc2c(F)cccc21 10.1016/j.bmcl.2009.01.108
127027101 137747 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 382 3 1 4 3.9 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)cc1F 10.1016/j.bmcl.2015.12.104
CHEMBL3758435 137747 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 382 3 1 4 3.9 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)cc1F 10.1016/j.bmcl.2015.12.104
127026386 137881 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 398 3 1 6 3.6 Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3cccnc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3759573 137881 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 398 3 1 6 3.6 Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3cccnc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
1310 2315 None 61 Human Functional pEC50 = 4.7 4.7 -741 17
Agonistic activity at mGlu1-alpha receptor expressed in CHO cellsAgonistic activity at mGlu1-alpha receptor expressed in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm9602569
1369 2315 None 61 Human Functional pEC50 = 4.7 4.7 -741 17
Agonistic activity at mGlu1-alpha receptor expressed in CHO cellsAgonistic activity at mGlu1-alpha receptor expressed in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm9602569
33032 2315 None 61 Human Functional pEC50 = 4.7 4.7 -741 17
Agonistic activity at mGlu1-alpha receptor expressed in CHO cellsAgonistic activity at mGlu1-alpha receptor expressed in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm9602569
44272391 2315 None 61 Human Functional pEC50 = 4.7 4.7 -741 17
Agonistic activity at mGlu1-alpha receptor expressed in CHO cellsAgonistic activity at mGlu1-alpha receptor expressed in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm9602569
88747398 2315 None 61 Human Functional pEC50 = 4.7 4.7 -741 17
Agonistic activity at mGlu1-alpha receptor expressed in CHO cellsAgonistic activity at mGlu1-alpha receptor expressed in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm9602569
CHEMBL575060 2315 None 61 Human Functional pEC50 = 4.7 4.7 -741 17
Agonistic activity at mGlu1-alpha receptor expressed in CHO cellsAgonistic activity at mGlu1-alpha receptor expressed in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm9602569
DB00142 2315 None 61 Human Functional pEC50 = 4.7 4.7 -741 17
Agonistic activity at mGlu1-alpha receptor expressed in CHO cellsAgonistic activity at mGlu1-alpha receptor expressed in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm9602569
127027100 137824 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 396 3 1 4 4.8 Cc1ccsc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3759137 137824 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 396 3 1 4 4.8 Cc1ccsc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
127026386 137881 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 398 3 1 6 3.6 Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3cccnc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3759573 137881 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 398 3 1 6 3.6 Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3cccnc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
127027101 137747 None 0 Human Functional pEC50 = 4.7 4.7 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 382 3 1 4 3.9 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)cc1F 10.1016/j.bmcl.2015.12.104
CHEMBL3758435 137747 None 0 Human Functional pEC50 = 4.7 4.7 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 382 3 1 4 3.9 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)cc1F 10.1016/j.bmcl.2015.12.104
122196114 124315 None 0 Human Functional pEC50 = 6.7 6.7 17 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 365 3 1 5 3.2 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)nc1 10.1016/j.bmcl.2015.10.013
CHEMBL3634436 124315 None 0 Human Functional pEC50 = 6.7 6.7 17 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 365 3 1 5 3.2 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)nc1 10.1016/j.bmcl.2015.10.013
162652796 180561 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay
ChEMBL 420 3 1 4 4.5 Cc1ccoc1C(=O)Nc1c(F)cc(N2C(=O)CC3(CCCC3)CC2=O)c(F)c1F 10.1016/j.bmcl.2020.127724
CHEMBL4752766 180561 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay
ChEMBL 420 3 1 4 4.5 Cc1ccoc1C(=O)Nc1c(F)cc(N2C(=O)CC3(CCCC3)CC2=O)c(F)c1F 10.1016/j.bmcl.2020.127724
10474765 193243 None 0 Rat Functional pEC50 = 7.7 7.7 - 1
Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay
ChEMBL 378 2 1 4 4.7 O=C(Nc1ncc(C(F)(F)F)o1)C1c2ccccc2Oc2ccc(F)cc21 10.1016/j.bmcl.2009.01.108
CHEMBL522875 193243 None 0 Rat Functional pEC50 = 7.7 7.7 - 1
Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay
ChEMBL 378 2 1 4 4.7 O=C(Nc1ncc(C(F)(F)F)o1)C1c2ccccc2Oc2ccc(F)cc21 10.1016/j.bmcl.2009.01.108
122196119 124320 None 0 Human Functional pEC50 = 7.7 7.7 17 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 396 3 1 4 4.8 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c2ccccc12 10.1016/j.bmcl.2015.10.013
CHEMBL3634441 124320 None 0 Human Functional pEC50 = 7.7 7.7 17 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 396 3 1 4 4.8 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c2ccccc12 10.1016/j.bmcl.2015.10.013
122196122 124323 None 0 Human Functional pEC50 = 7.7 7.7 41 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 414 3 1 4 4.9 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c2ccccc12 10.1016/j.bmcl.2015.10.013
CHEMBL3634444 124323 None 0 Human Functional pEC50 = 7.7 7.7 41 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 414 3 1 4 4.9 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c2ccccc12 10.1016/j.bmcl.2015.10.013
10338547 3340 None 29 Rat Functional pEC50 = 6.7 6.7 1 2
Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology
ChEMBL 360 2 1 4 4.6 O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F 10.1016/j.bmcl.2009.01.108
6204 3340 None 29 Rat Functional pEC50 = 6.7 6.7 1 2
Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology
ChEMBL 360 2 1 4 4.6 O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F 10.1016/j.bmcl.2009.01.108
CHEMBL521982 3340 None 29 Rat Functional pEC50 = 6.7 6.7 1 2
Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology
ChEMBL 360 2 1 4 4.6 O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F 10.1016/j.bmcl.2009.01.108
122196117 124318 None 0 Human Functional pEC50 = 6.7 6.7 12 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 382 3 1 6 3.1 Cc1ccoc1C(=O)Nc1cnc(N2C(=O)c3cccc(Cl)c3C2=O)nc1 10.1016/j.bmcl.2015.10.013
CHEMBL3634439 124318 None 0 Human Functional pEC50 = 6.7 6.7 12 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 382 3 1 6 3.1 Cc1ccoc1C(=O)Nc1cnc(N2C(=O)c3cccc(Cl)c3C2=O)nc1 10.1016/j.bmcl.2015.10.013
127034504 139071 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 391 3 1 4 4.5 Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(C#N)cccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
CHEMBL3785392 139071 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 391 3 1 4 4.5 Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(C#N)cccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
10362260 187742 None 0 Rat Functional pEC50 = 7.7 7.7 - 1
Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay
ChEMBL 378 2 1 4 4.7 O=C(Nc1ncc(C(F)(F)F)o1)C1c2ccccc2Oc2c(F)cccc21 10.1016/j.bmcl.2009.01.108
CHEMBL494960 187742 None 0 Rat Functional pEC50 = 7.7 7.7 - 1
Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay
ChEMBL 378 2 1 4 4.7 O=C(Nc1ncc(C(F)(F)F)o1)C1c2ccccc2Oc2c(F)cccc21 10.1016/j.bmcl.2009.01.108
122196100 124302 None 0 Human Functional pEC50 = 7.7 7.7 19 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 374 3 1 4 4.3 Cc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(C)c2C1=O 10.1016/j.bmcl.2015.10.013
CHEMBL3634423 124302 None 0 Human Functional pEC50 = 7.7 7.7 19 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 374 3 1 4 4.3 Cc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(C)c2C1=O 10.1016/j.bmcl.2015.10.013
127025479 137817 None 0 Human Functional pEC50 = 7.7 7.7 51 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 411 3 1 5 4.5 Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3ncsc3C)cc1Cl)C2=O 10.1016/j.bmcl.2015.12.104
CHEMBL3759038 137817 None 0 Human Functional pEC50 = 7.7 7.7 51 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 411 3 1 5 4.5 Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3ncsc3C)cc1Cl)C2=O 10.1016/j.bmcl.2015.12.104
127033963 139060 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 400 3 1 3 5.3 Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(Cl)cccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
CHEMBL3785321 139060 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 400 3 1 3 5.3 Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(Cl)cccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
127034504 139071 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 391 3 1 4 4.5 Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(C#N)cccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
CHEMBL3785392 139071 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 391 3 1 4 4.5 Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(C#N)cccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
162669790 182736 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay
ChEMBL 412 3 1 4 4.7 Cc1cc(N2C(=O)c3ccc(Cl)cc3C2=O)c(F)cc1NC(=O)c1occc1C 10.1016/j.bmcl.2020.127724
CHEMBL4788523 182736 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay
ChEMBL 412 3 1 4 4.7 Cc1cc(N2C(=O)c3ccc(Cl)cc3C2=O)c(F)cc1NC(=O)c1occc1C 10.1016/j.bmcl.2020.127724
127025479 137817 None 0 Human Functional pEC50 = 7.7 7.7 51 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 411 3 1 5 4.5 Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3ncsc3C)cc1Cl)C2=O 10.1016/j.bmcl.2015.12.104
CHEMBL3759038 137817 None 0 Human Functional pEC50 = 7.7 7.7 51 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 411 3 1 5 4.5 Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3ncsc3C)cc1Cl)C2=O 10.1016/j.bmcl.2015.12.104
122196095 124297 None 0 Human Functional pEC50 = 7.7 7.7 12 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 364 3 1 4 3.8 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(F)c1 10.1016/j.bmcl.2015.10.013
CHEMBL3634418 124297 None 0 Human Functional pEC50 = 7.7 7.7 12 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 364 3 1 4 3.8 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(F)c1 10.1016/j.bmcl.2015.10.013
127026165 137782 None 4 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay
ChEMBL 378 3 1 4 4.1 Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3occc3C)c(F)c1)C2=O 10.1016/j.bmcl.2020.127724
CHEMBL3758746 137782 None 4 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay
ChEMBL 378 3 1 4 4.1 Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3occc3C)c(F)c1)C2=O 10.1016/j.bmcl.2020.127724
127027102 137749 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 382 3 1 4 3.9 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)cc1F 10.1016/j.bmcl.2015.12.104
CHEMBL3758465 137749 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 382 3 1 4 3.9 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)cc1F 10.1016/j.bmcl.2015.12.104
127025860 137815 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 398 3 2 4 3.6 Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3759028 137815 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 398 3 2 4 3.6 Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
44573698 1082 None 0 Rat Functional pEC50 = 6.7 6.7 - 1
Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology
ChEMBL 307 2 1 5 3.3 O=C(C1c2ccccc2Oc2c1cccc2)Nc1noc(n1)C 10.1016/j.bmcl.2009.01.108
6205 1082 None 0 Rat Functional pEC50 = 6.7 6.7 - 1
Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology
ChEMBL 307 2 1 5 3.3 O=C(C1c2ccccc2Oc2c1cccc2)Nc1noc(n1)C 10.1016/j.bmcl.2009.01.108
CHEMBL492378 1082 None 0 Rat Functional pEC50 = 6.7 6.7 - 1
Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology
ChEMBL 307 2 1 5 3.3 O=C(C1c2ccccc2Oc2c1cccc2)Nc1noc(n1)C 10.1016/j.bmcl.2009.01.108
162666895 182627 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Negative allosteric modulation of human mGluR1 by calcium mobilization assayNegative allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 335 3 1 4 2.5 CC1(C)C2C(=O)N(c3ccc(NC(=O)c4ccccn4)cc3)C(=O)C21 10.1016/j.bmcl.2020.127724
CHEMBL4787147 182627 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Negative allosteric modulation of human mGluR1 by calcium mobilization assayNegative allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 335 3 1 4 2.5 CC1(C)C2C(=O)N(c3ccc(NC(=O)c4ccccn4)cc3)C(=O)C21 10.1016/j.bmcl.2020.127724
127027102 137749 None 0 Human Functional pEC50 = 4.7 4.7 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 382 3 1 4 3.9 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)cc1F 10.1016/j.bmcl.2015.12.104
CHEMBL3758465 137749 None 0 Human Functional pEC50 = 4.7 4.7 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 382 3 1 4 3.9 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)cc1F 10.1016/j.bmcl.2015.12.104
127033436 139050 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 394 3 1 4 4.2 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)Cc3ccccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
CHEMBL3785245 139050 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 394 3 1 4 4.2 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)Cc3ccccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
127026067 137935 None 0 Human Functional pEC50 = 6.6 6.6 6 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 411 3 1 5 4.5 Cc1cccc2c1C(=O)N(c1ccc(NC(=O)c3ncsc3C)cc1Cl)C2=O 10.1016/j.bmcl.2015.12.104
CHEMBL3760018 137935 None 0 Human Functional pEC50 = 6.6 6.6 6 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 411 3 1 5 4.5 Cc1cccc2c1C(=O)N(c1ccc(NC(=O)c3ncsc3C)cc1Cl)C2=O 10.1016/j.bmcl.2015.12.104
122196121 124322 None 0 Human Functional pEC50 = 7.6 7.6 22 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 430 3 1 4 5.4 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c2ccccc12 10.1016/j.bmcl.2015.10.013
CHEMBL3634443 124322 None 0 Human Functional pEC50 = 7.6 7.6 22 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 430 3 1 4 5.4 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c2ccccc12 10.1016/j.bmcl.2015.10.013
122193178 124000 None 0 Human Functional pEC50 = 7.6 7.6 30 2
Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
ChEMBL 398 3 1 4 4.4 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
CHEMBL3628114 124000 None 0 Human Functional pEC50 = 7.6 7.6 30 2
Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
ChEMBL 398 3 1 4 4.4 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
1368 2290 None 30 Rat Functional pEC50 = 4.6 4.6 -60 11
Metabotropic glutamate receptor 1 agonist activity as basal [3H]- IP formation in ratMetabotropic glutamate receptor 1 agonist activity as basal [3H]- IP formation in rat
ChEMBL 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 10.1021/jm030967o
5310956 2290 None 30 Rat Functional pEC50 = 4.6 4.6 -60 11
Metabotropic glutamate receptor 1 agonist activity as basal [3H]- IP formation in ratMetabotropic glutamate receptor 1 agonist activity as basal [3H]- IP formation in rat
ChEMBL 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 10.1021/jm030967o
CHEMBL280563 2290 None 30 Rat Functional pEC50 = 4.6 4.6 -60 11
Metabotropic glutamate receptor 1 agonist activity as basal [3H]- IP formation in ratMetabotropic glutamate receptor 1 agonist activity as basal [3H]- IP formation in rat
ChEMBL 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 10.1021/jm030967o
1310 2315 None 61 Rat Functional pEC50 = 4.6 4.6 -794 17
Agonist activity at rat mGluR1 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR1 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2015.04.043
1369 2315 None 61 Rat Functional pEC50 = 4.6 4.6 -794 17
Agonist activity at rat mGluR1 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR1 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2015.04.043
33032 2315 None 61 Rat Functional pEC50 = 4.6 4.6 -794 17
Agonist activity at rat mGluR1 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR1 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2015.04.043
44272391 2315 None 61 Rat Functional pEC50 = 4.6 4.6 -794 17
Agonist activity at rat mGluR1 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR1 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2015.04.043
88747398 2315 None 61 Rat Functional pEC50 = 4.6 4.6 -794 17
Agonist activity at rat mGluR1 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR1 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2015.04.043
CHEMBL575060 2315 None 61 Rat Functional pEC50 = 4.6 4.6 -794 17
Agonist activity at rat mGluR1 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR1 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2015.04.043
DB00142 2315 None 61 Rat Functional pEC50 = 4.6 4.6 -794 17
Agonist activity at rat mGluR1 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR1 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2015.04.043
127026067 137935 None 0 Human Functional pEC50 = 6.6 6.6 6 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 411 3 1 5 4.5 Cc1cccc2c1C(=O)N(c1ccc(NC(=O)c3ncsc3C)cc1Cl)C2=O 10.1016/j.bmcl.2015.12.104
CHEMBL3760018 137935 None 0 Human Functional pEC50 = 6.6 6.6 6 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 411 3 1 5 4.5 Cc1cccc2c1C(=O)N(c1ccc(NC(=O)c3ncsc3C)cc1Cl)C2=O 10.1016/j.bmcl.2015.12.104
127046038 140028 None 0 Rat Functional pEC50 = 5.6 5.6 -4 2
Positive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 350 3 1 4 5.1 CC(C)c1csc(NC(=O)C2c3ccccc3Oc3ccccc32)n1 10.1016/j.bmcl.2016.03.044
CHEMBL3799685 140028 None 0 Rat Functional pEC50 = 5.6 5.6 -4 2
Positive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 350 3 1 4 5.1 CC(C)c1csc(NC(=O)C2c3ccccc3Oc3ccccc32)n1 10.1016/j.bmcl.2016.03.044
122193178 124000 None 0 Human Functional pEC50 = 7.6 7.6 30 2
Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
ChEMBL 398 3 1 4 4.4 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
CHEMBL3628114 124000 None 0 Human Functional pEC50 = 7.6 7.6 30 2
Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
ChEMBL 398 3 1 4 4.4 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
122193173 123995 None 0 Human Functional pEC50 = 7.6 7.6 25 2
Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
ChEMBL 394 3 1 4 4.6 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
CHEMBL3628109 123995 None 0 Human Functional pEC50 = 7.6 7.6 25 2
Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
ChEMBL 394 3 1 4 4.6 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
122193173 123995 None 0 Human Functional pEC50 = 7.6 7.6 25 2
Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
ChEMBL 394 3 1 4 4.6 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
CHEMBL3628109 123995 None 0 Human Functional pEC50 = 7.6 7.6 25 2
Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
ChEMBL 394 3 1 4 4.6 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
127046038 140028 None 0 Rat Functional pEC50 = 5.6 5.6 -4 2
Positive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 350 3 1 4 5.1 CC(C)c1csc(NC(=O)C2c3ccccc3Oc3ccccc32)n1 10.1016/j.bmcl.2016.03.044
CHEMBL3799685 140028 None 0 Rat Functional pEC50 = 5.6 5.6 -4 2
Positive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 350 3 1 4 5.1 CC(C)c1csc(NC(=O)C2c3ccccc3Oc3ccccc32)n1 10.1016/j.bmcl.2016.03.044
127026059 137918 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 399 3 1 5 3.8 Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3759878 137918 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 399 3 1 5 3.8 Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
127033436 139050 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 394 3 1 4 4.2 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)Cc3ccccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
CHEMBL3785245 139050 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 394 3 1 4 4.2 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)Cc3ccccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
127034514 139201 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 366 3 1 3 4.7 Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(Cl)cccc3C2=O)cc1 10.1016/j.bmcl.2016.03.031
CHEMBL3786739 139201 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 366 3 1 3 4.7 Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(Cl)cccc3C2=O)cc1 10.1016/j.bmcl.2016.03.031
10338547 3340 None 29 Human Functional pEC50 = 6.6 6.6 -1 2
Positive allosteric modulation of human mGlu1 receptor expressed in wild type T-Rex 293 cells assessed as increase in glutamate-induced calcium mobilization incubated for 2 mins before glutamate stimulation for 2.2 minsPositive allosteric modulation of human mGlu1 receptor expressed in wild type T-Rex 293 cells assessed as increase in glutamate-induced calcium mobilization incubated for 2 mins before glutamate stimulation for 2.2 mins
ChEMBL 360 2 1 4 4.6 O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F 10.1016/j.bmcl.2016.03.044
6204 3340 None 29 Human Functional pEC50 = 6.6 6.6 -1 2
Positive allosteric modulation of human mGlu1 receptor expressed in wild type T-Rex 293 cells assessed as increase in glutamate-induced calcium mobilization incubated for 2 mins before glutamate stimulation for 2.2 minsPositive allosteric modulation of human mGlu1 receptor expressed in wild type T-Rex 293 cells assessed as increase in glutamate-induced calcium mobilization incubated for 2 mins before glutamate stimulation for 2.2 mins
ChEMBL 360 2 1 4 4.6 O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F 10.1016/j.bmcl.2016.03.044
CHEMBL521982 3340 None 29 Human Functional pEC50 = 6.6 6.6 -1 2
Positive allosteric modulation of human mGlu1 receptor expressed in wild type T-Rex 293 cells assessed as increase in glutamate-induced calcium mobilization incubated for 2 mins before glutamate stimulation for 2.2 minsPositive allosteric modulation of human mGlu1 receptor expressed in wild type T-Rex 293 cells assessed as increase in glutamate-induced calcium mobilization incubated for 2 mins before glutamate stimulation for 2.2 mins
ChEMBL 360 2 1 4 4.6 O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F 10.1016/j.bmcl.2016.03.044
127034514 139201 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 366 3 1 3 4.7 Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(Cl)cccc3C2=O)cc1 10.1016/j.bmcl.2016.03.031
CHEMBL3786739 139201 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 366 3 1 3 4.7 Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(Cl)cccc3C2=O)cc1 10.1016/j.bmcl.2016.03.031
10338547 3340 None 29 Human Functional pEC50 = 6.6 6.6 -1 2
Positive allosteric modulation of human mGlu1 receptor expressed in wild type T-Rex 293 cells assessed as increase in glutamate-induced calcium mobilization incubated for 2 mins before glutamate stimulation for 2.2 minsPositive allosteric modulation of human mGlu1 receptor expressed in wild type T-Rex 293 cells assessed as increase in glutamate-induced calcium mobilization incubated for 2 mins before glutamate stimulation for 2.2 mins
ChEMBL 360 2 1 4 4.6 O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F 10.1016/j.bmcl.2016.03.044
6204 3340 None 29 Human Functional pEC50 = 6.6 6.6 -1 2
Positive allosteric modulation of human mGlu1 receptor expressed in wild type T-Rex 293 cells assessed as increase in glutamate-induced calcium mobilization incubated for 2 mins before glutamate stimulation for 2.2 minsPositive allosteric modulation of human mGlu1 receptor expressed in wild type T-Rex 293 cells assessed as increase in glutamate-induced calcium mobilization incubated for 2 mins before glutamate stimulation for 2.2 mins
ChEMBL 360 2 1 4 4.6 O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F 10.1016/j.bmcl.2016.03.044
CHEMBL521982 3340 None 29 Human Functional pEC50 = 6.6 6.6 -1 2
Positive allosteric modulation of human mGlu1 receptor expressed in wild type T-Rex 293 cells assessed as increase in glutamate-induced calcium mobilization incubated for 2 mins before glutamate stimulation for 2.2 minsPositive allosteric modulation of human mGlu1 receptor expressed in wild type T-Rex 293 cells assessed as increase in glutamate-induced calcium mobilization incubated for 2 mins before glutamate stimulation for 2.2 mins
ChEMBL 360 2 1 4 4.6 O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F 10.1016/j.bmcl.2016.03.044
127033962 139129 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 366 3 1 3 5.1 Cc1ccoc1C(=O)Nc1ccc(N2CCc3ccccc3C2)c(Cl)c1 10.1016/j.bmcl.2016.03.031
CHEMBL3786032 139129 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 366 3 1 3 5.1 Cc1ccoc1C(=O)Nc1ccc(N2CCc3ccccc3C2)c(Cl)c1 10.1016/j.bmcl.2016.03.031
44573738 187710 None 0 Rat Functional pEC50 = 7.6 7.6 - 1
Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay
ChEMBL 396 2 1 4 4.8 O=C(Nc1ncc(C(F)(F)F)o1)C1c2cccc(F)c2Oc2c(F)cccc21 10.1016/j.bmcl.2009.01.108
CHEMBL494766 187710 None 0 Rat Functional pEC50 = 7.6 7.6 - 1
Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay
ChEMBL 396 2 1 4 4.8 O=C(Nc1ncc(C(F)(F)F)o1)C1c2cccc(F)c2Oc2c(F)cccc21 10.1016/j.bmcl.2009.01.108
127026166 137729 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 378 3 1 4 4.1 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)cc1F 10.1016/j.bmcl.2015.12.104
CHEMBL3758305 137729 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 378 3 1 4 4.1 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)cc1F 10.1016/j.bmcl.2015.12.104
127026165 137782 None 4 Human Functional pEC50 = 7.6 7.6 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 378 3 1 4 4.1 Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3occc3C)c(F)c1)C2=O 10.1016/j.bmcl.2016.03.031
CHEMBL3758746 137782 None 4 Human Functional pEC50 = 7.6 7.6 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 378 3 1 4 4.1 Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3occc3C)c(F)c1)C2=O 10.1016/j.bmcl.2016.03.031
127025564 137877 None 0 Human Functional pEC50 = 6.6 6.6 2 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 394 3 1 5 3.4 Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3nccn3C)cc1Cl)C2=O 10.1016/j.bmcl.2015.12.104
CHEMBL3759555 137877 None 0 Human Functional pEC50 = 6.6 6.6 2 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 394 3 1 5 3.4 Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3nccn3C)cc1Cl)C2=O 10.1016/j.bmcl.2015.12.104
127025564 137877 None 0 Human Functional pEC50 = 6.6 6.6 2 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 394 3 1 5 3.4 Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3nccn3C)cc1Cl)C2=O 10.1016/j.bmcl.2015.12.104
CHEMBL3759555 137877 None 0 Human Functional pEC50 = 6.6 6.6 2 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 394 3 1 5 3.4 Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3nccn3C)cc1Cl)C2=O 10.1016/j.bmcl.2015.12.104
127026166 137729 None 0 Human Functional pEC50 = 4.6 4.6 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 378 3 1 4 4.1 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)cc1F 10.1016/j.bmcl.2015.12.104
CHEMBL3758305 137729 None 0 Human Functional pEC50 = 4.6 4.6 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 378 3 1 4 4.1 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)cc1F 10.1016/j.bmcl.2015.12.104
122196096 124298 None 0 Human Functional pEC50 = 7.6 7.6 10 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 378 3 1 4 4.1 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c(F)c1 10.1016/j.bmcl.2015.10.013
CHEMBL3634419 124298 None 0 Human Functional pEC50 = 7.6 7.6 10 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 378 3 1 4 4.1 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c(F)c1 10.1016/j.bmcl.2015.10.013
10045177 187410 None 0 Rat Functional pEC50 = 6.6 6.6 - 1
Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology
ChEMBL 378 2 1 4 4.7 O=C(Nc1nc(C(F)(F)F)co1)C1c2ccccc2Oc2cc(F)ccc21 10.1016/j.bmcl.2009.01.108
CHEMBL492979 187410 None 0 Rat Functional pEC50 = 6.6 6.6 - 1
Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology
ChEMBL 378 2 1 4 4.7 O=C(Nc1nc(C(F)(F)F)co1)C1c2ccccc2Oc2cc(F)ccc21 10.1016/j.bmcl.2009.01.108
127033960 139200 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 369 3 1 5 4.4 Cc1ccoc1C(=O)Nc1ccc(N2CCOc3ncccc32)c(Cl)c1 10.1016/j.bmcl.2016.03.031
CHEMBL3786721 139200 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 369 3 1 5 4.4 Cc1ccoc1C(=O)Nc1ccc(N2CCOc3ncccc32)c(Cl)c1 10.1016/j.bmcl.2016.03.031
127028298 137891 None 0 Human Functional pEC50 = 6.6 6.6 6 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 414 3 1 5 3.8 Cn1ccnc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3759647 137891 None 0 Human Functional pEC50 = 6.6 6.6 6 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 414 3 1 5 3.8 Cn1ccnc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
127033960 139200 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 369 3 1 5 4.4 Cc1ccoc1C(=O)Nc1ccc(N2CCOc3ncccc32)c(Cl)c1 10.1016/j.bmcl.2016.03.031
CHEMBL3786721 139200 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 369 3 1 5 4.4 Cc1ccoc1C(=O)Nc1ccc(N2CCOc3ncccc32)c(Cl)c1 10.1016/j.bmcl.2016.03.031
127028298 137891 None 0 Human Functional pEC50 = 6.6 6.6 6 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 414 3 1 5 3.8 Cn1ccnc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3759647 137891 None 0 Human Functional pEC50 = 6.6 6.6 6 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 414 3 1 5 3.8 Cn1ccnc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
127046020 139841 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 323 2 1 5 3.7 Cc1nsc(NC(=O)C2c3ccccc3Oc3ccccc32)n1 10.1016/j.bmcl.2016.03.044
CHEMBL3798489 139841 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 323 2 1 5 3.7 Cc1nsc(NC(=O)C2c3ccccc3Oc3ccccc32)n1 10.1016/j.bmcl.2016.03.044
127046020 139841 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 323 2 1 5 3.7 Cc1nsc(NC(=O)C2c3ccccc3Oc3ccccc32)n1 10.1016/j.bmcl.2016.03.044
CHEMBL3798489 139841 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Positive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 323 2 1 5 3.7 Cc1nsc(NC(=O)C2c3ccccc3Oc3ccccc32)n1 10.1016/j.bmcl.2016.03.044
10338547 3340 None 29 Rat Functional pEC50 = 6.6 6.6 1 2
Positive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 360 2 1 4 4.6 O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F 10.1016/j.bmcl.2016.03.044
6204 3340 None 29 Rat Functional pEC50 = 6.6 6.6 1 2
Positive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 360 2 1 4 4.6 O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F 10.1016/j.bmcl.2016.03.044
CHEMBL521982 3340 None 29 Rat Functional pEC50 = 6.6 6.6 1 2
Positive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 360 2 1 4 4.6 O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F 10.1016/j.bmcl.2016.03.044
10338547 3340 None 29 Rat Functional pEC50 = 6.6 6.6 1 2
Positive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 360 2 1 4 4.6 O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F 10.1016/j.bmcl.2016.03.044
6204 3340 None 29 Rat Functional pEC50 = 6.6 6.6 1 2
Positive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 360 2 1 4 4.6 O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F 10.1016/j.bmcl.2016.03.044
CHEMBL521982 3340 None 29 Rat Functional pEC50 = 6.6 6.6 1 2
Positive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 360 2 1 4 4.6 O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F 10.1016/j.bmcl.2016.03.044
122196097 124299 None 0 Human Functional pEC50 = 7.6 7.6 9 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 398 3 1 4 4.4 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(F)c1 10.1016/j.bmcl.2015.10.013
CHEMBL3634420 124299 None 0 Human Functional pEC50 = 7.6 7.6 9 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 398 3 1 4 4.4 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(F)c1 10.1016/j.bmcl.2015.10.013
122196093 124295 None 0 Human Functional pEC50 = 7.5 7.5 16 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 380 3 1 4 4.3 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)cc1 10.1016/j.bmcl.2015.10.013
CHEMBL3634416 124295 None 0 Human Functional pEC50 = 7.5 7.5 16 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 380 3 1 4 4.3 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)cc1 10.1016/j.bmcl.2015.10.013
122196124 124325 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 380 3 1 4 4.3 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)cc1Cl 10.1016/j.bmcl.2015.10.013
CHEMBL3634446 124325 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 380 3 1 4 4.3 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)cc1Cl 10.1016/j.bmcl.2015.10.013
122193310 124005 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
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/acs.jmedchem.5b00727
CHEMBL3628280 124005 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
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/acs.jmedchem.5b00727
1310 2315 None 61 Rat Functional pEC50 = 5.5 5.5 -794 17
Agonist activity in rat at Metabotropic glutamate receptor 1 expressed in HEK293 cellsAgonist activity in rat at Metabotropic glutamate receptor 1 expressed in HEK293 cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/s0960-894x(01)00158-5
1369 2315 None 61 Rat Functional pEC50 = 5.5 5.5 -794 17
Agonist activity in rat at Metabotropic glutamate receptor 1 expressed in HEK293 cellsAgonist activity in rat at Metabotropic glutamate receptor 1 expressed in HEK293 cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/s0960-894x(01)00158-5
33032 2315 None 61 Rat Functional pEC50 = 5.5 5.5 -794 17
Agonist activity in rat at Metabotropic glutamate receptor 1 expressed in HEK293 cellsAgonist activity in rat at Metabotropic glutamate receptor 1 expressed in HEK293 cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/s0960-894x(01)00158-5
44272391 2315 None 61 Rat Functional pEC50 = 5.5 5.5 -794 17
Agonist activity in rat at Metabotropic glutamate receptor 1 expressed in HEK293 cellsAgonist activity in rat at Metabotropic glutamate receptor 1 expressed in HEK293 cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/s0960-894x(01)00158-5
88747398 2315 None 61 Rat Functional pEC50 = 5.5 5.5 -794 17
Agonist activity in rat at Metabotropic glutamate receptor 1 expressed in HEK293 cellsAgonist activity in rat at Metabotropic glutamate receptor 1 expressed in HEK293 cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/s0960-894x(01)00158-5
CHEMBL575060 2315 None 61 Rat Functional pEC50 = 5.5 5.5 -794 17
Agonist activity in rat at Metabotropic glutamate receptor 1 expressed in HEK293 cellsAgonist activity in rat at Metabotropic glutamate receptor 1 expressed in HEK293 cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/s0960-894x(01)00158-5
DB00142 2315 None 61 Rat Functional pEC50 = 5.5 5.5 -794 17
Agonist activity in rat at Metabotropic glutamate receptor 1 expressed in HEK293 cellsAgonist activity in rat at Metabotropic glutamate receptor 1 expressed in HEK293 cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/s0960-894x(01)00158-5
162676671 183688 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay
ChEMBL 374 3 1 4 4.3 Cc1cc(N2C(=O)c3ccccc3C2=O)c(C)cc1NC(=O)c1occc1C 10.1016/j.bmcl.2020.127724
CHEMBL4800540 183688 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay
ChEMBL 374 3 1 4 4.3 Cc1cc(N2C(=O)c3ccccc3C2=O)c(C)cc1NC(=O)c1occc1C 10.1016/j.bmcl.2020.127724
122193177 123999 None 7 Human Functional pEC50 = 7.5 7.5 1 3
Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
ChEMBL 398 3 1 4 4.4 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
CHEMBL3628113 123999 None 7 Human Functional pEC50 = 7.5 7.5 1 3
Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
ChEMBL 398 3 1 4 4.4 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
122193177 123999 None 7 Human Functional pEC50 = 7.5 7.5 1 3
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 398 3 1 4 4.4 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
CHEMBL3628113 123999 None 7 Human Functional pEC50 = 7.5 7.5 1 3
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 398 3 1 4 4.4 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
122193177 123999 None 7 Human Functional pEC50 = 7.5 7.5 1 3
Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
ChEMBL 398 3 1 4 4.4 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
CHEMBL3628113 123999 None 7 Human Functional pEC50 = 7.5 7.5 1 3
Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
ChEMBL 398 3 1 4 4.4 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
1407 2079 None 36 Rat Functional pEC50 = 4.5 4.5 -1023 7
Metabotropic glutamate receptor 1 agonist activity as basal [3H]- IP formation in ratMetabotropic glutamate receptor 1 agonist activity as basal [3H]- IP formation in rat
ChEMBL 239 4 4 4 0.2 N[C@@H](c1ccc(c(c1)C(=O)O)C(=O)O)C(=O)O 10.1021/jm030967o
16062593 2079 None 36 Rat Functional pEC50 = 4.5 4.5 -1023 7
Metabotropic glutamate receptor 1 agonist activity as basal [3H]- IP formation in ratMetabotropic glutamate receptor 1 agonist activity as basal [3H]- IP formation in rat
ChEMBL 239 4 4 4 0.2 N[C@@H](c1ccc(c(c1)C(=O)O)C(=O)O)C(=O)O 10.1021/jm030967o
CHEMBL143210 2079 None 36 Rat Functional pEC50 = 4.5 4.5 -1023 7
Metabotropic glutamate receptor 1 agonist activity as basal [3H]- IP formation in ratMetabotropic glutamate receptor 1 agonist activity as basal [3H]- IP formation in rat
ChEMBL 239 4 4 4 0.2 N[C@@H](c1ccc(c(c1)C(=O)O)C(=O)O)C(=O)O 10.1021/jm030967o
122193175 123997 None 0 Human Functional pEC50 = 7.5 7.5 34 2
Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
ChEMBL 414 3 1 4 4.9 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
CHEMBL3628111 123997 None 0 Human Functional pEC50 = 7.5 7.5 34 2
Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
ChEMBL 414 3 1 4 4.9 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
122193175 123997 None 0 Human Functional pEC50 = 7.5 7.5 34 2
Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
ChEMBL 414 3 1 4 4.9 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
CHEMBL3628111 123997 None 0 Human Functional pEC50 = 7.5 7.5 34 2
Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
ChEMBL 414 3 1 4 4.9 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
122196127 124327 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 376 4 1 5 3.7 COc1cc(N2C(=O)c3ccccc3C2=O)ccc1NC(=O)c1occc1C 10.1016/j.bmcl.2015.10.013
CHEMBL3634449 124327 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 376 4 1 5 3.7 COc1cc(N2C(=O)c3ccccc3C2=O)ccc1NC(=O)c1occc1C 10.1016/j.bmcl.2015.10.013
127027327 137939 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 379 3 2 3 4.0 Cc1cc[nH]c1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3760068 137939 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 379 3 2 3 4.0 Cc1cc[nH]c1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
127027327 137939 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 379 3 2 3 4.0 Cc1cc[nH]c1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3760068 137939 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 379 3 2 3 4.0 Cc1cc[nH]c1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
122196098 124300 None 0 Human Functional pEC50 = 7.5 7.5 19 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 382 3 1 4 3.9 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(F)c1 10.1016/j.bmcl.2015.10.013
CHEMBL3634421 124300 None 0 Human Functional pEC50 = 7.5 7.5 19 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 382 3 1 4 3.9 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(F)c1 10.1016/j.bmcl.2015.10.013
122196113 124314 None 0 Human Functional pEC50 = 7.5 7.5 32 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 381 3 1 5 3.7 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)nc1 10.1016/j.bmcl.2015.10.013
CHEMBL3634435 124314 None 0 Human Functional pEC50 = 7.5 7.5 32 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 381 3 1 5 3.7 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)nc1 10.1016/j.bmcl.2015.10.013
127033437 139051 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 408 3 1 4 4.2 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)Cc3ccccc3CC2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
CHEMBL3785247 139051 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 408 3 1 4 4.2 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)Cc3ccccc3CC2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
127034515 139073 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 366 3 1 3 4.7 Cc1ccoc1C(=O)Nc1ccc(N2Cc3cccc(Cl)c3C2=O)cc1 10.1016/j.bmcl.2016.03.031
CHEMBL3785400 139073 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 366 3 1 3 4.7 Cc1ccoc1C(=O)Nc1ccc(N2Cc3cccc(Cl)c3C2=O)cc1 10.1016/j.bmcl.2016.03.031
127029302 137736 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 380 3 1 5 3.1 Cn1ccnc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3758364 137736 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 380 3 1 5 3.1 Cn1ccnc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
127034515 139073 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 366 3 1 3 4.7 Cc1ccoc1C(=O)Nc1ccc(N2Cc3cccc(Cl)c3C2=O)cc1 10.1016/j.bmcl.2016.03.031
CHEMBL3785400 139073 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 366 3 1 3 4.7 Cc1ccoc1C(=O)Nc1ccc(N2Cc3cccc(Cl)c3C2=O)cc1 10.1016/j.bmcl.2016.03.031
10009 4049 None 35 Rat Functional pEC50 = 6.5 6.5 -1 3
Positive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay
ChEMBL 445 3 1 4 5.1 Clc1cc(ccc1N1C(=O)c2c(C1=O)c(Cl)ccc2)NC(=O)c1ncccc1Cl 10.1021/acs.jmedchem.5b00727
91885483 4049 None 35 Rat Functional pEC50 = 6.5 6.5 -1 3
Positive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay
ChEMBL 445 3 1 4 5.1 Clc1cc(ccc1N1C(=O)c2c(C1=O)c(Cl)ccc2)NC(=O)c1ncccc1Cl 10.1021/acs.jmedchem.5b00727
CHEMBL3628116 4049 None 35 Rat Functional pEC50 = 6.5 6.5 -1 3
Positive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay
ChEMBL 445 3 1 4 5.1 Clc1cc(ccc1N1C(=O)c2c(C1=O)c(Cl)ccc2)NC(=O)c1ncccc1Cl 10.1021/acs.jmedchem.5b00727
4125492 140179 None 9 Rat Functional pEC50 = 5.4 5.4 -2 2
Positive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 308 2 1 4 4.0 O=C(Nc1nccs1)C1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2016.03.044
CHEMBL3800589 140179 None 9 Rat Functional pEC50 = 5.4 5.4 -2 2
Positive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 308 2 1 4 4.0 O=C(Nc1nccs1)C1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2016.03.044
127033694 139110 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 368 3 1 4 5.0 Cc1ccoc1C(=O)Nc1ccc(N2CCOc3ccccc32)c(Cl)c1 10.1016/j.bmcl.2016.03.031
CHEMBL3785850 139110 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 368 3 1 4 5.0 Cc1ccoc1C(=O)Nc1ccc(N2CCOc3ccccc32)c(Cl)c1 10.1016/j.bmcl.2016.03.031
127033437 139051 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 408 3 1 4 4.2 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)Cc3ccccc3CC2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
CHEMBL3785247 139051 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 408 3 1 4 4.2 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)Cc3ccccc3CC2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
127033694 139110 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 368 3 1 4 5.0 Cc1ccoc1C(=O)Nc1ccc(N2CCOc3ccccc32)c(Cl)c1 10.1016/j.bmcl.2016.03.031
CHEMBL3785850 139110 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 368 3 1 4 5.0 Cc1ccoc1C(=O)Nc1ccc(N2CCOc3ccccc32)c(Cl)c1 10.1016/j.bmcl.2016.03.031
4125492 140179 None 9 Rat Functional pEC50 = 5.4 5.4 -2 2
Positive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 308 2 1 4 4.0 O=C(Nc1nccs1)C1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2016.03.044
CHEMBL3800589 140179 None 9 Rat Functional pEC50 = 5.4 5.4 -2 2
Positive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 308 2 1 4 4.0 O=C(Nc1nccs1)C1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2016.03.044
127031257 139275 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 366 3 1 3 4.7 Cc1ccoc1C(=O)Nc1ccc(N2Cc3ccccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
CHEMBL3787619 139275 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 366 3 1 3 4.7 Cc1ccoc1C(=O)Nc1ccc(N2Cc3ccccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
127031257 139275 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 366 3 1 3 4.7 Cc1ccoc1C(=O)Nc1ccc(N2Cc3ccccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
CHEMBL3787619 139275 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 366 3 1 3 4.7 Cc1ccoc1C(=O)Nc1ccc(N2Cc3ccccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
127029302 137736 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 380 3 1 5 3.1 Cn1ccnc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3758364 137736 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 380 3 1 5 3.1 Cn1ccnc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
9975764 187745 None 0 Rat Functional pEC50 = 7.4 7.4 - 1
Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay
ChEMBL 360 2 1 4 4.6 O=C(Nc1ncc(C(F)(F)F)o1)C1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2009.01.108
CHEMBL494966 187745 None 0 Rat Functional pEC50 = 7.4 7.4 - 1
Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay
ChEMBL 360 2 1 4 4.6 O=C(Nc1ncc(C(F)(F)F)o1)C1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2009.01.108
122196111 124312 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 347 3 1 5 3.0 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)nc1 10.1016/j.bmcl.2015.10.013
CHEMBL3634433 124312 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 347 3 1 5 3.0 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)nc1 10.1016/j.bmcl.2015.10.013
127032809 139068 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 444 3 1 3 5.4 Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(Br)cccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
CHEMBL3785382 139068 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 444 3 1 3 5.4 Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(Br)cccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
10009 4049 None 35 Human Functional pEC50 = 6.4 6.4 -1 3
Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
ChEMBL 445 3 1 4 5.1 Clc1cc(ccc1N1C(=O)c2c(C1=O)c(Cl)ccc2)NC(=O)c1ncccc1Cl 10.1021/acs.jmedchem.5b00727
91885483 4049 None 35 Human Functional pEC50 = 6.4 6.4 -1 3
Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
ChEMBL 445 3 1 4 5.1 Clc1cc(ccc1N1C(=O)c2c(C1=O)c(Cl)ccc2)NC(=O)c1ncccc1Cl 10.1021/acs.jmedchem.5b00727
CHEMBL3628116 4049 None 35 Human Functional pEC50 = 6.4 6.4 -1 3
Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
ChEMBL 445 3 1 4 5.1 Clc1cc(ccc1N1C(=O)c2c(C1=O)c(Cl)ccc2)NC(=O)c1ncccc1Cl 10.1021/acs.jmedchem.5b00727
10009 4049 None 35 Human Functional pEC50 = 6.4 6.4 -1 3
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 445 3 1 4 5.1 Clc1cc(ccc1N1C(=O)c2c(C1=O)c(Cl)ccc2)NC(=O)c1ncccc1Cl 10.1016/j.bmcl.2016.03.031
91885483 4049 None 35 Human Functional pEC50 = 6.4 6.4 -1 3
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 445 3 1 4 5.1 Clc1cc(ccc1N1C(=O)c2c(C1=O)c(Cl)ccc2)NC(=O)c1ncccc1Cl 10.1016/j.bmcl.2016.03.031
CHEMBL3628116 4049 None 35 Human Functional pEC50 = 6.4 6.4 -1 3
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 445 3 1 4 5.1 Clc1cc(ccc1N1C(=O)c2c(C1=O)c(Cl)ccc2)NC(=O)c1ncccc1Cl 10.1016/j.bmcl.2016.03.031
127032809 139068 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 444 3 1 3 5.4 Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(Br)cccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
CHEMBL3785382 139068 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 444 3 1 3 5.4 Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(Br)cccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
9975764 187745 None 0 Rat Functional pEC50 = 6.4 6.4 - 1
Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology
ChEMBL 360 2 1 4 4.6 O=C(Nc1ncc(C(F)(F)F)o1)C1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2009.01.108
CHEMBL494966 187745 None 0 Rat Functional pEC50 = 6.4 6.4 - 1
Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology
ChEMBL 360 2 1 4 4.6 O=C(Nc1ncc(C(F)(F)F)o1)C1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2009.01.108
10407284 187343 None 0 Rat Functional pEC50 = 7.4 7.4 - 1
Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay
ChEMBL 378 2 1 4 4.7 O=C(Nc1nc(C(F)(F)F)co1)C1c2ccccc2Oc2ccc(F)cc21 10.1016/j.bmcl.2009.01.108
CHEMBL492570 187343 None 0 Rat Functional pEC50 = 7.4 7.4 - 1
Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay
ChEMBL 378 2 1 4 4.7 O=C(Nc1nc(C(F)(F)F)co1)C1c2ccccc2Oc2ccc(F)cc21 10.1016/j.bmcl.2009.01.108
10045177 187410 None 0 Rat Functional pEC50 = 7.4 7.4 - 1
Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay
ChEMBL 378 2 1 4 4.7 O=C(Nc1nc(C(F)(F)F)co1)C1c2ccccc2Oc2cc(F)ccc21 10.1016/j.bmcl.2009.01.108
CHEMBL492979 187410 None 0 Rat Functional pEC50 = 7.4 7.4 - 1
Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay
ChEMBL 378 2 1 4 4.7 O=C(Nc1nc(C(F)(F)F)co1)C1c2ccccc2Oc2cc(F)ccc21 10.1016/j.bmcl.2009.01.108
122193177 123999 None 7 Rat Functional pEC50 = 7.4 7.4 -1 3
Positive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay
ChEMBL 398 3 1 4 4.4 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
CHEMBL3628113 123999 None 7 Rat Functional pEC50 = 7.4 7.4 -1 3
Positive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay
ChEMBL 398 3 1 4 4.4 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
122193177 123999 None 7 Rat Functional pEC50 = 7.4 7.4 -1 3
Positive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay
ChEMBL 398 3 1 4 4.4 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
CHEMBL3628113 123999 None 7 Rat Functional pEC50 = 7.4 7.4 -1 3
Positive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay
ChEMBL 398 3 1 4 4.4 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
127025548 137762 None 0 Human Functional pEC50 = 7.4 7.4 4 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 395 3 1 5 4.0 Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3ncoc3C)cc1Cl)C2=O 10.1016/j.bmcl.2015.12.104
CHEMBL3758587 137762 None 0 Human Functional pEC50 = 7.4 7.4 4 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 395 3 1 5 4.0 Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3ncoc3C)cc1Cl)C2=O 10.1016/j.bmcl.2015.12.104
127025548 137762 None 0 Human Functional pEC50 = 7.4 7.4 4 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 395 3 1 5 4.0 Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3ncoc3C)cc1Cl)C2=O 10.1016/j.bmcl.2015.12.104
CHEMBL3758587 137762 None 0 Human Functional pEC50 = 7.4 7.4 4 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 395 3 1 5 4.0 Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3ncoc3C)cc1Cl)C2=O 10.1016/j.bmcl.2015.12.104
162677180 183635 None 0 Human Functional pEC50 = 7.4 7.4 5 3
Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate 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 183635 None 0 Human Functional pEC50 = 7.4 7.4 5 3
Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate 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
104766 33 None 30 Rat Functional pEC50 = 4.4 4.4 -8 14
Tested for the agonistic activity against Metabotropic glutamate receptor 1Tested for the agonistic activity against Metabotropic glutamate receptor 1
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1016/S0960-894X(97)00068-1
1365 33 None 30 Rat Functional pEC50 = 4.4 4.4 -8 14
Tested for the agonistic activity against Metabotropic glutamate receptor 1Tested for the agonistic activity against Metabotropic glutamate receptor 1
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1016/S0960-894X(97)00068-1
CHEMBL34453 33 None 30 Rat Functional pEC50 = 4.4 4.4 -8 14
Tested for the agonistic activity against Metabotropic glutamate receptor 1Tested for the agonistic activity against Metabotropic glutamate receptor 1
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1016/S0960-894X(97)00068-1
6603885 102256 None 18 Rat Functional pEC50 = 4.4 4.4 -4 5
Activity at rat cloned mGluR1a expressed in CHO cells assessed as effect on cAMP accumulationActivity at rat cloned mGluR1a expressed in CHO cells assessed as effect on cAMP accumulation
ChEMBL 158 2 3 5 -0.5 N[C@H](C(=O)O)c1cc(O)no1 10.1021/jm701394a
6971208 102256 None 18 Rat Functional pEC50 = 4.4 4.4 -4 5
Activity at rat cloned mGluR1a expressed in CHO cells assessed as effect on cAMP accumulationActivity at rat cloned mGluR1a expressed in CHO cells assessed as effect on cAMP accumulation
ChEMBL 158 2 3 5 -0.5 N[C@H](C(=O)O)c1cc(O)no1 10.1021/jm701394a
CHEMBL30285 102256 None 18 Rat Functional pEC50 = 4.4 4.4 -4 5
Activity at rat cloned mGluR1a expressed in CHO cells assessed as effect on cAMP accumulationActivity at rat cloned mGluR1a expressed in CHO cells assessed as effect on cAMP accumulation
ChEMBL 158 2 3 5 -0.5 N[C@H](C(=O)O)c1cc(O)no1 10.1021/jm701394a
12310764 1970 None 46 Rat Functional pEC50 = 4.4 4.4 -21 2
Compound was evaluated for agonistic activity against mGluR1 alpha metabotropic receptor subtype in rat cortical slice modelCompound was evaluated for agonistic activity against mGluR1 alpha metabotropic receptor subtype in rat cortical slice model
ChEMBL 158 2 3 4 -0.9 OC(=O)C(c1o[nH]c(=O)c1)N 10.1016/s0960-894x(98)00264-9
1233 1970 None 46 Rat Functional pEC50 = 4.4 4.4 -21 2
Compound was evaluated for agonistic activity against mGluR1 alpha metabotropic receptor subtype in rat cortical slice modelCompound was evaluated for agonistic activity against mGluR1 alpha metabotropic receptor subtype in rat cortical slice model
ChEMBL 158 2 3 4 -0.9 OC(=O)C(c1o[nH]c(=O)c1)N 10.1016/s0960-894x(98)00264-9
1371 1970 None 46 Rat Functional pEC50 = 4.4 4.4 -21 2
Compound was evaluated for agonistic activity against mGluR1 alpha metabotropic receptor subtype in rat cortical slice modelCompound was evaluated for agonistic activity against mGluR1 alpha metabotropic receptor subtype in rat cortical slice model
ChEMBL 158 2 3 4 -0.9 OC(=O)C(c1o[nH]c(=O)c1)N 10.1016/s0960-894x(98)00264-9
CHEMBL284895 1970 None 46 Rat Functional pEC50 = 4.4 4.4 -21 2
Compound was evaluated for agonistic activity against mGluR1 alpha metabotropic receptor subtype in rat cortical slice modelCompound was evaluated for agonistic activity against mGluR1 alpha metabotropic receptor subtype in rat cortical slice model
ChEMBL 158 2 3 4 -0.9 OC(=O)C(c1o[nH]c(=O)c1)N 10.1016/s0960-894x(98)00264-9
127028301 137870 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 394 3 2 4 3.7 Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3759530 137870 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 394 3 2 4 3.7 Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
9978023 187779 None 0 Rat Functional pEC50 = 7.4 7.4 - 1
Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay
ChEMBL 396 2 1 4 4.8 O=C(Nc1nc(C(F)(F)F)co1)C1c2cc(F)ccc2Oc2ccc(F)cc21 10.1016/j.bmcl.2009.01.108
CHEMBL495150 187779 None 0 Rat Functional pEC50 = 7.4 7.4 - 1
Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay
ChEMBL 396 2 1 4 4.8 O=C(Nc1nc(C(F)(F)F)co1)C1c2cc(F)ccc2Oc2ccc(F)cc21 10.1016/j.bmcl.2009.01.108
122196094 124296 None 0 Human Functional pEC50 = 7.4 7.4 8 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 364 3 1 4 3.8 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)cc1 10.1016/j.bmcl.2015.10.013
CHEMBL3634417 124296 None 0 Human Functional pEC50 = 7.4 7.4 8 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 364 3 1 4 3.8 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)cc1 10.1016/j.bmcl.2015.10.013
122193154 123993 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
ChEMBL 383 3 1 5 3.8 O=C(Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1)c1cscn1 10.1021/acs.jmedchem.5b00727
CHEMBL3628088 123993 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
ChEMBL 383 3 1 5 3.8 O=C(Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1)c1cscn1 10.1021/acs.jmedchem.5b00727
122193154 123993 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
ChEMBL 383 3 1 5 3.8 O=C(Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1)c1cscn1 10.1021/acs.jmedchem.5b00727
CHEMBL3628088 123993 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
ChEMBL 383 3 1 5 3.8 O=C(Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1)c1cscn1 10.1021/acs.jmedchem.5b00727
122196107 124309 None 0 Human Functional pEC50 = 7.3 7.3 25 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 376 4 1 5 3.7 COc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2ccccc2C1=O 10.1016/j.bmcl.2015.10.013
CHEMBL3634430 124309 None 0 Human Functional pEC50 = 7.3 7.3 25 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 376 4 1 5 3.7 COc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2ccccc2C1=O 10.1016/j.bmcl.2015.10.013
122196115 124316 None 0 Human Functional pEC50 = 5.3 5.3 1 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 348 3 1 6 2.4 Cc1ccoc1C(=O)Nc1cnc(N2C(=O)c3ccccc3C2=O)nc1 10.1016/j.bmcl.2015.10.013
CHEMBL3634437 124316 None 0 Human Functional pEC50 = 5.3 5.3 1 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 348 3 1 6 2.4 Cc1ccoc1C(=O)Nc1cnc(N2C(=O)c3ccccc3C2=O)nc1 10.1016/j.bmcl.2015.10.013
127025549 137860 None 0 Human Functional pEC50 = 6.3 6.3 1 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 395 3 1 5 4.0 Cc1cccc2c1C(=O)N(c1ccc(NC(=O)c3ncoc3C)cc1Cl)C2=O 10.1016/j.bmcl.2015.12.104
CHEMBL3759424 137860 None 0 Human Functional pEC50 = 6.3 6.3 1 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 395 3 1 5 4.0 Cc1cccc2c1C(=O)N(c1ccc(NC(=O)c3ncoc3C)cc1Cl)C2=O 10.1016/j.bmcl.2015.12.104
127033435 139251 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 417 3 1 4 5.2 Cc1scnc1C(=O)Nc1ccc(N2Cc3cccc(Cl)c3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
CHEMBL3787296 139251 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 417 3 1 4 5.2 Cc1scnc1C(=O)Nc1ccc(N2Cc3cccc(Cl)c3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
44573780 187746 None 0 Rat Functional pEC50 = 7.3 7.3 - 1
Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay
ChEMBL 396 2 1 4 4.8 O=C(Nc1nc(C(F)(F)F)co1)C1c2cccc(F)c2Oc2c(F)cccc21 10.1016/j.bmcl.2009.01.108
CHEMBL494967 187746 None 0 Rat Functional pEC50 = 7.3 7.3 - 1
Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay
ChEMBL 396 2 1 4 4.8 O=C(Nc1nc(C(F)(F)F)co1)C1c2cccc(F)c2Oc2c(F)cccc21 10.1016/j.bmcl.2009.01.108
127025549 137860 None 0 Human Functional pEC50 = 6.3 6.3 1 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 395 3 1 5 4.0 Cc1cccc2c1C(=O)N(c1ccc(NC(=O)c3ncoc3C)cc1Cl)C2=O 10.1016/j.bmcl.2015.12.104
CHEMBL3759424 137860 None 0 Human Functional pEC50 = 6.3 6.3 1 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 395 3 1 5 4.0 Cc1cccc2c1C(=O)N(c1ccc(NC(=O)c3ncoc3C)cc1Cl)C2=O 10.1016/j.bmcl.2015.12.104
2862916 40714 None 7 Human Functional pEC50 = 5.3 5.3 2 2
Positive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 358 2 1 4 5.2 O=C(Nc1nc2ccccc2s1)C1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2016.03.044
CHEMBL1484616 40714 None 7 Human Functional pEC50 = 5.3 5.3 2 2
Positive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 358 2 1 4 5.2 O=C(Nc1nc2ccccc2s1)C1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2016.03.044
127033435 139251 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 417 3 1 4 5.2 Cc1scnc1C(=O)Nc1ccc(N2Cc3cccc(Cl)c3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
CHEMBL3787296 139251 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 417 3 1 4 5.2 Cc1scnc1C(=O)Nc1ccc(N2Cc3cccc(Cl)c3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
122196091 124293 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 346 3 1 4 3.6 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)cc1 10.1016/j.bmcl.2015.10.013
CHEMBL3634414 124293 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 346 3 1 4 3.6 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)cc1 10.1016/j.bmcl.2015.10.013
2862916 40714 None 7 Human Functional pEC50 = 5.3 5.3 2 2
Positive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 358 2 1 4 5.2 O=C(Nc1nc2ccccc2s1)C1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2016.03.044
CHEMBL1484616 40714 None 7 Human Functional pEC50 = 5.3 5.3 2 2
Positive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 358 2 1 4 5.2 O=C(Nc1nc2ccccc2s1)C1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2016.03.044
127032506 139161 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 400 3 1 3 5.3 Cc1ccoc1C(=O)Nc1ccc(N2Cc3cccc(Cl)c3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
CHEMBL3786400 139161 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 400 3 1 3 5.3 Cc1ccoc1C(=O)Nc1ccc(N2Cc3cccc(Cl)c3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
127032506 139161 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 400 3 1 3 5.3 Cc1ccoc1C(=O)Nc1ccc(N2Cc3cccc(Cl)c3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
CHEMBL3786400 139161 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 400 3 1 3 5.3 Cc1ccoc1C(=O)Nc1ccc(N2Cc3cccc(Cl)c3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
122196101 124303 None 0 Human Functional pEC50 = 7.3 7.3 20 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 394 3 1 4 4.6 Cc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(Cl)c2C1=O 10.1016/j.bmcl.2015.10.013
CHEMBL3634424 124303 None 0 Human Functional pEC50 = 7.3 7.3 20 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 394 3 1 4 4.6 Cc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(Cl)c2C1=O 10.1016/j.bmcl.2015.10.013
122196102 124304 None 0 Human Functional pEC50 = 7.3 7.3 22 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 378 3 1 4 4.1 Cc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(F)c2C1=O 10.1016/j.bmcl.2015.10.013
CHEMBL3634425 124304 None 0 Human Functional pEC50 = 7.3 7.3 22 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 378 3 1 4 4.1 Cc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(F)c2C1=O 10.1016/j.bmcl.2015.10.013
122196108 124310 None 0 Human Functional pEC50 = 7.3 7.3 18 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 390 4 1 5 4.0 COc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(C)c2C1=O 10.1016/j.bmcl.2015.10.013
CHEMBL3634431 124310 None 0 Human Functional pEC50 = 7.3 7.3 18 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 390 4 1 5 4.0 COc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(C)c2C1=O 10.1016/j.bmcl.2015.10.013
127028301 137870 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 394 3 2 4 3.7 Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3759530 137870 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 394 3 2 4 3.7 Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
127026167 137921 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 398 3 1 4 4.4 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)cc1F 10.1016/j.bmcl.2015.12.104
CHEMBL3759901 137921 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 398 3 1 4 4.4 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)cc1F 10.1016/j.bmcl.2015.12.104
127026138 137720 None 0 Human Functional pEC50 = 7.3 7.3 38 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 431 3 1 5 4.8 Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3758216 137720 None 0 Human Functional pEC50 = 7.3 7.3 38 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 431 3 1 5 4.8 Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
162662674 182084 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay
ChEMBL 378 3 1 4 4.1 Cc1cc(N2C(=O)c3ccccc3C2=O)c(F)cc1NC(=O)c1occc1C 10.1016/j.bmcl.2020.127724
CHEMBL4780280 182084 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay
ChEMBL 378 3 1 4 4.1 Cc1cc(N2C(=O)c3ccccc3C2=O)c(F)cc1NC(=O)c1occc1C 10.1016/j.bmcl.2020.127724
127026138 137720 None 0 Human Functional pEC50 = 7.3 7.3 38 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 431 3 1 5 4.8 Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3758216 137720 None 0 Human Functional pEC50 = 7.3 7.3 38 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 431 3 1 5 4.8 Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
44573698 1082 None 0 Rat Functional pEC50 = 7.3 7.3 - 1
Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay
ChEMBL 307 2 1 5 3.3 O=C(C1c2ccccc2Oc2c1cccc2)Nc1noc(n1)C 10.1016/j.bmcl.2009.01.108
6205 1082 None 0 Rat Functional pEC50 = 7.3 7.3 - 1
Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay
ChEMBL 307 2 1 5 3.3 O=C(C1c2ccccc2Oc2c1cccc2)Nc1noc(n1)C 10.1016/j.bmcl.2009.01.108
CHEMBL492378 1082 None 0 Rat Functional pEC50 = 7.3 7.3 - 1
Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay
ChEMBL 307 2 1 5 3.3 O=C(C1c2ccccc2Oc2c1cccc2)Nc1noc(n1)C 10.1016/j.bmcl.2009.01.108
127027099 137806 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 379 3 1 4 3.7 Cn1cccc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3758942 137806 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 379 3 1 4 3.7 Cn1cccc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
127027099 137806 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 379 3 1 4 3.7 Cn1cccc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3758942 137806 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 379 3 1 4 3.7 Cn1cccc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
122196104 124306 None 0 Human Functional pEC50 = 6.3 6.3 10 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 428 3 1 4 5.0 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c(C(F)(F)F)c1 10.1016/j.bmcl.2015.10.013
CHEMBL3634427 124306 None 0 Human Functional pEC50 = 6.3 6.3 10 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 428 3 1 4 5.0 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c(C(F)(F)F)c1 10.1016/j.bmcl.2015.10.013
127026167 137921 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 398 3 1 4 4.4 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)cc1F 10.1016/j.bmcl.2015.12.104
CHEMBL3759901 137921 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 398 3 1 4 4.4 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)cc1F 10.1016/j.bmcl.2015.12.104
122196118 124319 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 366 3 1 6 2.6 Cc1ccoc1C(=O)Nc1cnc(N2C(=O)c3cccc(F)c3C2=O)nc1 10.1016/j.bmcl.2015.10.013
CHEMBL3634440 124319 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 366 3 1 6 2.6 Cc1ccoc1C(=O)Nc1cnc(N2C(=O)c3cccc(F)c3C2=O)nc1 10.1016/j.bmcl.2015.10.013
127028303 137845 None 0 Human Functional pEC50 = 7.3 7.3 7 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 415 3 1 5 4.3 Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3759289 137845 None 0 Human Functional pEC50 = 7.3 7.3 7 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 415 3 1 5 4.3 Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
122193174 123996 None 0 Human Functional pEC50 = 7.3 7.3 5 2
Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
ChEMBL 394 3 1 4 4.6 Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3occc3C)cc1Cl)C2=O 10.1021/acs.jmedchem.5b00727
CHEMBL3628110 123996 None 0 Human Functional pEC50 = 7.3 7.3 5 2
Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
ChEMBL 394 3 1 4 4.6 Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3occc3C)cc1Cl)C2=O 10.1021/acs.jmedchem.5b00727
127028303 137845 None 0 Human Functional pEC50 = 7.3 7.3 7 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 415 3 1 5 4.3 Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3759289 137845 None 0 Human Functional pEC50 = 7.3 7.3 7 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 415 3 1 5 4.3 Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
122193174 123996 None 0 Human Functional pEC50 = 7.3 7.3 5 2
Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
ChEMBL 394 3 1 4 4.6 Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3occc3C)cc1Cl)C2=O 10.1021/acs.jmedchem.5b00727
CHEMBL3628110 123996 None 0 Human Functional pEC50 = 7.3 7.3 5 2
Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
ChEMBL 394 3 1 4 4.6 Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3occc3C)cc1Cl)C2=O 10.1021/acs.jmedchem.5b00727
51116040 123992 None 3 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
ChEMBL 366 3 1 4 4.0 O=C(Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1)c1ccco1 10.1021/acs.jmedchem.5b00727
CHEMBL3628081 123992 None 3 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
ChEMBL 366 3 1 4 4.0 O=C(Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1)c1ccco1 10.1021/acs.jmedchem.5b00727
51116040 123992 None 3 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
ChEMBL 366 3 1 4 4.0 O=C(Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1)c1ccco1 10.1021/acs.jmedchem.5b00727
CHEMBL3628081 123992 None 3 Human Functional pEC50 = 6.3 6.3 - 1
Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
ChEMBL 366 3 1 4 4.0 O=C(Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1)c1ccco1 10.1021/acs.jmedchem.5b00727
127026471 137894 None 0 Human Functional pEC50 = 6.3 6.3 4 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 394 3 2 4 3.7 Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3[nH]ncc3C)cc1Cl)C2=O 10.1016/j.bmcl.2015.12.104
CHEMBL3759656 137894 None 0 Human Functional pEC50 = 6.3 6.3 4 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 394 3 2 4 3.7 Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3[nH]ncc3C)cc1Cl)C2=O 10.1016/j.bmcl.2015.12.104
10338547 3340 None 29 Rat Functional pEC50 = 7.3 7.3 1 2
Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay
ChEMBL 360 2 1 4 4.6 O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F 10.1016/j.bmcl.2009.01.108
6204 3340 None 29 Rat Functional pEC50 = 7.3 7.3 1 2
Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay
ChEMBL 360 2 1 4 4.6 O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F 10.1016/j.bmcl.2009.01.108
CHEMBL521982 3340 None 29 Rat Functional pEC50 = 7.3 7.3 1 2
Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay
ChEMBL 360 2 1 4 4.6 O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F 10.1016/j.bmcl.2009.01.108
127029301 137772 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 397 3 1 5 4.2 Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3758683 137772 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 397 3 1 5 4.2 Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
162667269 182619 None 0 Human Functional pEC50 = 7.3 7.3 3 3
Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate 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 182619 None 0 Human Functional pEC50 = 7.3 7.3 3 3
Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate 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
127026471 137894 None 0 Human Functional pEC50 = 6.3 6.3 4 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 394 3 2 4 3.7 Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3[nH]ncc3C)cc1Cl)C2=O 10.1016/j.bmcl.2015.12.104
CHEMBL3759656 137894 None 0 Human Functional pEC50 = 6.3 6.3 4 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 394 3 2 4 3.7 Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3[nH]ncc3C)cc1Cl)C2=O 10.1016/j.bmcl.2015.12.104
127033693 139047 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 352 3 1 3 5.2 Cc1ccoc1C(=O)Nc1ccc(N2CCc3ccccc32)c(Cl)c1 10.1016/j.bmcl.2016.03.031
CHEMBL3785210 139047 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 352 3 1 3 5.2 Cc1ccoc1C(=O)Nc1ccc(N2CCc3ccccc32)c(Cl)c1 10.1016/j.bmcl.2016.03.031
127033693 139047 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 352 3 1 3 5.2 Cc1ccoc1C(=O)Nc1ccc(N2CCc3ccccc32)c(Cl)c1 10.1016/j.bmcl.2016.03.031
CHEMBL3785210 139047 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 352 3 1 3 5.2 Cc1ccoc1C(=O)Nc1ccc(N2CCc3ccccc32)c(Cl)c1 10.1016/j.bmcl.2016.03.031
162670460 183001 None 0 Human Functional pEC50 = 7.2 7.2 4 3
Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate 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 183001 None 0 Human Functional pEC50 = 7.2 7.2 4 3
Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate 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
162674997 183496 None 0 Human Functional pEC50 = 7.2 7.2 1 3
Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate 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 183496 None 0 Human Functional pEC50 = 7.2 7.2 1 3
Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate 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
127029301 137772 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 397 3 1 5 4.2 Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3758683 137772 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 397 3 1 5 4.2 Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
162645938 179686 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay
ChEMBL 400 3 1 4 4.1 Cc1ccoc1C(=O)Nc1cc(F)c(N2C(=O)c3ccccc3C2=O)c(F)c1F 10.1016/j.bmcl.2020.127724
CHEMBL4742005 179686 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay
ChEMBL 400 3 1 4 4.1 Cc1ccoc1C(=O)Nc1cc(F)c(N2C(=O)c3ccccc3C2=O)c(F)c1F 10.1016/j.bmcl.2020.127724
127025860 137815 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 398 3 2 4 3.6 Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3759028 137815 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 398 3 2 4 3.6 Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
127026140 137808 None 0 Human Functional pEC50 = 7.2 7.2 4 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 415 3 1 5 4.3 Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3758967 137808 None 0 Human Functional pEC50 = 7.2 7.2 4 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 415 3 1 5 4.3 Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
162648752 180058 None 0 Human Functional pEC50 = 7.2 7.2 4 3
Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate 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 180058 None 0 Human Functional pEC50 = 7.2 7.2 4 3
Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate 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
127026140 137808 None 0 Human Functional pEC50 = 7.2 7.2 4 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 415 3 1 5 4.3 Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3758967 137808 None 0 Human Functional pEC50 = 7.2 7.2 4 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 415 3 1 5 4.3 Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
127026474 137855 None 0 Human Functional pEC50 = 6.2 6.2 9 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 398 3 2 4 3.6 Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3759376 137855 None 0 Human Functional pEC50 = 6.2 6.2 9 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 398 3 2 4 3.6 Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
127026474 137855 None 0 Human Functional pEC50 = 6.2 6.2 9 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 398 3 2 4 3.6 Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3759376 137855 None 0 Human Functional pEC50 = 6.2 6.2 9 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 398 3 2 4 3.6 Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
127032839 139279 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 434 3 1 3 6.0 Cc1ccoc1C(=O)Nc1ccc(N2Cc3cccc(Cl)c3C2=O)c(Cl)c1Cl 10.1016/j.bmcl.2016.03.031
CHEMBL3787654 139279 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 434 3 1 3 6.0 Cc1ccoc1C(=O)Nc1ccc(N2Cc3cccc(Cl)c3C2=O)c(Cl)c1Cl 10.1016/j.bmcl.2016.03.031
443586 146540 None 39 Human Functional pEC50 = 5.2 5.2 -16 3
Compound was tested for its agonist activity against Ser165 and Thr188 (Metabotropic glutamate receptor 1) receptor.Compound was tested for its agonist activity against Ser165 and Thr188 (Metabotropic glutamate receptor 1) receptor.
ChEMBL 183 2 4 4 0.2 N[C@H](C(=O)O)c1cc(O)cc(O)c1 10.1021/jm990353c
71668376 146540 None 39 Human Functional pEC50 = 5.2 5.2 -16 3
Compound was tested for its agonist activity against Ser165 and Thr188 (Metabotropic glutamate receptor 1) receptor.Compound was tested for its agonist activity against Ser165 and Thr188 (Metabotropic glutamate receptor 1) receptor.
ChEMBL 183 2 4 4 0.2 N[C@H](C(=O)O)c1cc(O)cc(O)c1 10.1021/jm990353c
CHEMBL39221 146540 None 39 Human Functional pEC50 = 5.2 5.2 -16 3
Compound was tested for its agonist activity against Ser165 and Thr188 (Metabotropic glutamate receptor 1) receptor.Compound was tested for its agonist activity against Ser165 and Thr188 (Metabotropic glutamate receptor 1) receptor.
ChEMBL 183 2 4 4 0.2 N[C@H](C(=O)O)c1cc(O)cc(O)c1 10.1021/jm990353c
127032839 139279 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 434 3 1 3 6.0 Cc1ccoc1C(=O)Nc1ccc(N2Cc3cccc(Cl)c3C2=O)c(Cl)c1Cl 10.1016/j.bmcl.2016.03.031
CHEMBL3787654 139279 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 434 3 1 3 6.0 Cc1ccoc1C(=O)Nc1ccc(N2Cc3cccc(Cl)c3C2=O)c(Cl)c1Cl 10.1016/j.bmcl.2016.03.031
10474765 193243 None 0 Rat Functional pEC50 = 7.2 7.2 - 1
Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology
ChEMBL 378 2 1 4 4.7 O=C(Nc1ncc(C(F)(F)F)o1)C1c2ccccc2Oc2ccc(F)cc21 10.1016/j.bmcl.2009.01.108
CHEMBL522875 193243 None 0 Rat Functional pEC50 = 7.2 7.2 - 1
Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology
ChEMBL 378 2 1 4 4.7 O=C(Nc1ncc(C(F)(F)F)o1)C1c2ccccc2Oc2ccc(F)cc21 10.1016/j.bmcl.2009.01.108
127025847 137813 None 0 Human Functional pEC50 = 6.2 6.2 1 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 398 3 1 5 3.3 Cn1ccnc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3758986 137813 None 0 Human Functional pEC50 = 6.2 6.2 1 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 398 3 1 5 3.3 Cn1ccnc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
127025847 137813 None 0 Human Functional pEC50 = 6.2 6.2 1 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 398 3 1 5 3.3 Cn1ccnc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3758986 137813 None 0 Human Functional pEC50 = 6.2 6.2 1 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 398 3 1 5 3.3 Cn1ccnc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
127034512 139222 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 394 3 1 3 5.4 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2(C)C)c(Cl)c1 10.1016/j.bmcl.2016.03.031
CHEMBL3786977 139222 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 394 3 1 3 5.4 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2(C)C)c(Cl)c1 10.1016/j.bmcl.2016.03.031
127034512 139222 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 394 3 1 3 5.4 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2(C)C)c(Cl)c1 10.1016/j.bmcl.2016.03.031
CHEMBL3786977 139222 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 394 3 1 3 5.4 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2(C)C)c(Cl)c1 10.1016/j.bmcl.2016.03.031
127047993 139738 None 1 Human Functional pEC50 = 6.2 6.2 3 2
Positive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 333 2 1 5 3.9 N#Cc1csc(NC(=O)C2c3ccccc3Oc3ccccc32)n1 10.1016/j.bmcl.2016.03.044
CHEMBL3797793 139738 None 1 Human Functional pEC50 = 6.2 6.2 3 2
Positive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 333 2 1 5 3.9 N#Cc1csc(NC(=O)C2c3ccccc3Oc3ccccc32)n1 10.1016/j.bmcl.2016.03.044
127047993 139738 None 1 Human Functional pEC50 = 6.1 6.1 3 2
Positive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 333 2 1 5 3.9 N#Cc1csc(NC(=O)C2c3ccccc3Oc3ccccc32)n1 10.1016/j.bmcl.2016.03.044
CHEMBL3797793 139738 None 1 Human Functional pEC50 = 6.1 6.1 3 2
Positive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 333 2 1 5 3.9 N#Cc1csc(NC(=O)C2c3ccccc3Oc3ccccc32)n1 10.1016/j.bmcl.2016.03.044
1310 2315 None 61 Rat Functional pEC50 = 5.1 5.1 -794 17
Activity at rat mGluR1 by measuring intracellular calcium concentration in CHO cellsActivity at rat mGluR1 by measuring intracellular calcium concentration in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2005.09.014
1369 2315 None 61 Rat Functional pEC50 = 5.1 5.1 -794 17
Activity at rat mGluR1 by measuring intracellular calcium concentration in CHO cellsActivity at rat mGluR1 by measuring intracellular calcium concentration in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2005.09.014
33032 2315 None 61 Rat Functional pEC50 = 5.1 5.1 -794 17
Activity at rat mGluR1 by measuring intracellular calcium concentration in CHO cellsActivity at rat mGluR1 by measuring intracellular calcium concentration in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2005.09.014
44272391 2315 None 61 Rat Functional pEC50 = 5.1 5.1 -794 17
Activity at rat mGluR1 by measuring intracellular calcium concentration in CHO cellsActivity at rat mGluR1 by measuring intracellular calcium concentration in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2005.09.014
88747398 2315 None 61 Rat Functional pEC50 = 5.1 5.1 -794 17
Activity at rat mGluR1 by measuring intracellular calcium concentration in CHO cellsActivity at rat mGluR1 by measuring intracellular calcium concentration in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2005.09.014
CHEMBL575060 2315 None 61 Rat Functional pEC50 = 5.1 5.1 -794 17
Activity at rat mGluR1 by measuring intracellular calcium concentration in CHO cellsActivity at rat mGluR1 by measuring intracellular calcium concentration in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2005.09.014
DB00142 2315 None 61 Rat Functional pEC50 = 5.1 5.1 -794 17
Activity at rat mGluR1 by measuring intracellular calcium concentration in CHO cellsActivity at rat mGluR1 by measuring intracellular calcium concentration in CHO cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmcl.2005.09.014
1310 2315 None 61 Rat Functional pEC50 = 5.1 5.1 -794 17
Activity at rat recombinant mGluR1 expressed in CHO cells assessed as intracellular calcium concentrationActivity at rat recombinant mGluR1 expressed in CHO cells assessed as intracellular calcium concentration
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2007.02.040
1369 2315 None 61 Rat Functional pEC50 = 5.1 5.1 -794 17
Activity at rat recombinant mGluR1 expressed in CHO cells assessed as intracellular calcium concentrationActivity at rat recombinant mGluR1 expressed in CHO cells assessed as intracellular calcium concentration
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2007.02.040
33032 2315 None 61 Rat Functional pEC50 = 5.1 5.1 -794 17
Activity at rat recombinant mGluR1 expressed in CHO cells assessed as intracellular calcium concentrationActivity at rat recombinant mGluR1 expressed in CHO cells assessed as intracellular calcium concentration
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2007.02.040
44272391 2315 None 61 Rat Functional pEC50 = 5.1 5.1 -794 17
Activity at rat recombinant mGluR1 expressed in CHO cells assessed as intracellular calcium concentrationActivity at rat recombinant mGluR1 expressed in CHO cells assessed as intracellular calcium concentration
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2007.02.040
88747398 2315 None 61 Rat Functional pEC50 = 5.1 5.1 -794 17
Activity at rat recombinant mGluR1 expressed in CHO cells assessed as intracellular calcium concentrationActivity at rat recombinant mGluR1 expressed in CHO cells assessed as intracellular calcium concentration
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2007.02.040
CHEMBL575060 2315 None 61 Rat Functional pEC50 = 5.1 5.1 -794 17
Activity at rat recombinant mGluR1 expressed in CHO cells assessed as intracellular calcium concentrationActivity at rat recombinant mGluR1 expressed in CHO cells assessed as intracellular calcium concentration
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2007.02.040
DB00142 2315 None 61 Rat Functional pEC50 = 5.1 5.1 -794 17
Activity at rat recombinant mGluR1 expressed in CHO cells assessed as intracellular calcium concentrationActivity at rat recombinant mGluR1 expressed in CHO cells assessed as intracellular calcium concentration
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2007.02.040
162648102 180010 None 0 Human Functional pEC50 = 7.1 7.1 1 5
Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate 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 180010 None 0 Human Functional pEC50 = 7.1 7.1 1 5
Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate 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
122196116 124317 None 0 Human Functional pEC50 = 6.1 6.1 5 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 362 3 1 6 2.7 Cc1ccoc1C(=O)Nc1cnc(N2C(=O)c3cccc(C)c3C2=O)nc1 10.1016/j.bmcl.2015.10.013
CHEMBL3634438 124317 None 0 Human Functional pEC50 = 6.1 6.1 5 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 362 3 1 6 2.7 Cc1ccoc1C(=O)Nc1cnc(N2C(=O)c3cccc(C)c3C2=O)nc1 10.1016/j.bmcl.2015.10.013
162661457 181540 None 0 Human Functional pEC50 = 7.1 7.1 1 3
Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate 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 181540 None 0 Human Functional pEC50 = 7.1 7.1 1 3
Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate 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
127033961 139052 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 380 3 1 3 4.7 Cc1ccoc1C(=O)Nc1ccc(N2CCc3ccccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
CHEMBL3785252 139052 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 380 3 1 3 4.7 Cc1ccoc1C(=O)Nc1ccc(N2CCc3ccccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
162674566 183388 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay
ChEMBL 382 3 1 4 3.9 Cc1ccoc1C(=O)Nc1cc(F)c(N2C(=O)c3ccccc3C2=O)cc1F 10.1016/j.bmcl.2020.127724
CHEMBL4796783 183388 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay
ChEMBL 382 3 1 4 3.9 Cc1ccoc1C(=O)Nc1cc(F)c(N2C(=O)c3ccccc3C2=O)cc1F 10.1016/j.bmcl.2020.127724
127033961 139052 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 380 3 1 3 4.7 Cc1ccoc1C(=O)Nc1ccc(N2CCc3ccccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
CHEMBL3785252 139052 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 380 3 1 3 4.7 Cc1ccoc1C(=O)Nc1ccc(N2CCc3ccccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
122193176 123998 None 0 Human Functional pEC50 = 7.1 7.1 1 3
Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
ChEMBL 414 3 1 4 4.9 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
CHEMBL3628112 123998 None 0 Human Functional pEC50 = 7.1 7.1 1 3
Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
ChEMBL 414 3 1 4 4.9 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
122193176 123998 None 0 Human Functional pEC50 = 7.1 7.1 1 3
Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
ChEMBL 414 3 1 4 4.9 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
CHEMBL3628112 123998 None 0 Human Functional pEC50 = 7.1 7.1 1 3
Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
ChEMBL 414 3 1 4 4.9 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
44450470 96139 None 1 Rat Functional pEC50 = 4.1 4.1 1 2
Activity at rat cloned mGluR1a expressed in CHO cells assessed as effect on cAMP accumulationActivity at rat cloned mGluR1a expressed in CHO cells assessed as effect on cAMP accumulation
ChEMBL 160 2 3 4 -0.9 N[C@H](C(=O)O)[C@H]1CC(O)=NO1 10.1021/jm701394a
CHEMBL260122 96139 None 1 Rat Functional pEC50 = 4.1 4.1 1 2
Activity at rat cloned mGluR1a expressed in CHO cells assessed as effect on cAMP accumulationActivity at rat cloned mGluR1a expressed in CHO cells assessed as effect on cAMP accumulation
ChEMBL 160 2 3 4 -0.9 N[C@H](C(=O)O)[C@H]1CC(O)=NO1 10.1021/jm701394a
127026472 137832 None 0 Human Functional pEC50 = 6.1 6.1 3 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 414 3 2 4 4.1 Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3759211 137832 None 0 Human Functional pEC50 = 6.1 6.1 3 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 414 3 2 4 4.1 Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
127026472 137832 None 0 Human Functional pEC50 = 6.1 6.1 3 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 414 3 2 4 4.1 Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
CHEMBL3759211 137832 None 0 Human Functional pEC50 = 6.1 6.1 3 2
Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization
ChEMBL 414 3 2 4 4.1 Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1 10.1016/j.bmcl.2015.12.104
127031845 139140 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 384 3 1 3 4.8 Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(F)cccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
CHEMBL3786160 139140 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 384 3 1 3 4.8 Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(F)cccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
122196099 124301 None 0 Human Functional pEC50 = 7.1 7.1 10 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 360 3 1 4 3.9 Cc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2ccccc2C1=O 10.1016/j.bmcl.2015.10.013
CHEMBL3634422 124301 None 0 Human Functional pEC50 = 7.1 7.1 10 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 360 3 1 4 3.9 Cc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2ccccc2C1=O 10.1016/j.bmcl.2015.10.013
127031845 139140 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 384 3 1 3 4.8 Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(F)cccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
CHEMBL3786160 139140 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 384 3 1 3 4.8 Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(F)cccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
9978023 187779 None 0 Rat Functional pEC50 = 7.1 7.1 - 1
Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology
ChEMBL 396 2 1 4 4.8 O=C(Nc1nc(C(F)(F)F)co1)C1c2cc(F)ccc2Oc2ccc(F)cc21 10.1016/j.bmcl.2009.01.108
CHEMBL495150 187779 None 0 Rat Functional pEC50 = 7.1 7.1 - 1
Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology
ChEMBL 396 2 1 4 4.8 O=C(Nc1nc(C(F)(F)F)co1)C1c2cc(F)ccc2Oc2ccc(F)cc21 10.1016/j.bmcl.2009.01.108
127046038 140028 None 0 Human Functional pEC50 = 6.1 6.1 4 2
Positive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 350 3 1 4 5.1 CC(C)c1csc(NC(=O)C2c3ccccc3Oc3ccccc32)n1 10.1016/j.bmcl.2016.03.044
CHEMBL3799685 140028 None 0 Human Functional pEC50 = 6.1 6.1 4 2
Positive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 350 3 1 4 5.1 CC(C)c1csc(NC(=O)C2c3ccccc3Oc3ccccc32)n1 10.1016/j.bmcl.2016.03.044
127046038 140028 None 0 Human Functional pEC50 = 6.0 6.0 4 2
Positive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 350 3 1 4 5.1 CC(C)c1csc(NC(=O)C2c3ccccc3Oc3ccccc32)n1 10.1016/j.bmcl.2016.03.044
CHEMBL3799685 140028 None 0 Human Functional pEC50 = 6.0 6.0 4 2
Positive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization
ChEMBL 350 3 1 4 5.1 CC(C)c1csc(NC(=O)C2c3ccccc3Oc3ccccc32)n1 10.1016/j.bmcl.2016.03.044
127030947 139185 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 398 5 3 4 4.4 Cc1ccoc1C(=O)Nc1ccc(NC(=O)c2ccccc2C(=O)O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
CHEMBL3786597 139185 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 398 5 3 4 4.4 Cc1ccoc1C(=O)Nc1ccc(NC(=O)c2ccccc2C(=O)O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
104766 33 None 30 Human Functional pEC50 = 5.0 5.0 -4 14
Agonist activity against Metabotropic glutamate receptor 1 expressed in HEK 293 cells was evaluated by measuring total inositol phosphate accumulationAgonist activity against Metabotropic glutamate receptor 1 expressed in HEK 293 cells was evaluated by measuring total inositol phosphate accumulation
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1021/jm970207b
1365 33 None 30 Human Functional pEC50 = 5.0 5.0 -4 14
Agonist activity against Metabotropic glutamate receptor 1 expressed in HEK 293 cells was evaluated by measuring total inositol phosphate accumulationAgonist activity against Metabotropic glutamate receptor 1 expressed in HEK 293 cells was evaluated by measuring total inositol phosphate accumulation
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1021/jm970207b
CHEMBL34453 33 None 30 Human Functional pEC50 = 5.0 5.0 -4 14
Agonist activity against Metabotropic glutamate receptor 1 expressed in HEK 293 cells was evaluated by measuring total inositol phosphate accumulationAgonist activity against Metabotropic glutamate receptor 1 expressed in HEK 293 cells was evaluated by measuring total inositol phosphate accumulation
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1021/jm970207b
127030947 139185 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 398 5 3 4 4.4 Cc1ccoc1C(=O)Nc1ccc(NC(=O)c2ccccc2C(=O)O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
CHEMBL3786597 139185 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 398 5 3 4 4.4 Cc1ccoc1C(=O)Nc1ccc(NC(=O)c2ccccc2C(=O)O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
122196112 124313 None 0 Human Functional pEC50 = 7.0 7.0 52 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 361 3 1 5 3.3 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)nc1 10.1016/j.bmcl.2015.10.013
CHEMBL3634434 124313 None 0 Human Functional pEC50 = 7.0 7.0 52 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 361 3 1 5 3.3 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)nc1 10.1016/j.bmcl.2015.10.013
127033434 139080 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 417 3 1 4 5.2 Cc1scnc1C(=O)Nc1ccc(N2Cc3c(Cl)cccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
CHEMBL3785499 139080 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 417 3 1 4 5.2 Cc1scnc1C(=O)Nc1ccc(N2Cc3c(Cl)cccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
127033434 139080 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 417 3 1 4 5.2 Cc1scnc1C(=O)Nc1ccc(N2Cc3c(Cl)cccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
CHEMBL3785499 139080 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 417 3 1 4 5.2 Cc1scnc1C(=O)Nc1ccc(N2Cc3c(Cl)cccc3C2=O)c(Cl)c1 10.1016/j.bmcl.2016.03.031
127030048 139039 None 0 Human Functional pEC50 = 5.0 5.0 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 353 3 1 4 4.4 Cc1ccoc1C(=O)Nc1ccc(N2Cc3cccnc3C2)c(Cl)c1 10.1016/j.bmcl.2016.03.031
CHEMBL3785114 139039 None 0 Human Functional pEC50 = 5.0 5.0 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 353 3 1 4 4.4 Cc1ccoc1C(=O)Nc1ccc(N2Cc3cccnc3C2)c(Cl)c1 10.1016/j.bmcl.2016.03.031
127030048 139039 None 0 Human Functional pEC50 = 5.0 5.0 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 353 3 1 4 4.4 Cc1ccoc1C(=O)Nc1ccc(N2Cc3cccnc3C2)c(Cl)c1 10.1016/j.bmcl.2016.03.031
CHEMBL3785114 139039 None 0 Human Functional pEC50 = 5.0 5.0 - 1
Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min
ChEMBL 353 3 1 4 4.4 Cc1ccoc1C(=O)Nc1ccc(N2Cc3cccnc3C2)c(Cl)c1 10.1016/j.bmcl.2016.03.031
52203651 123994 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
ChEMBL 380 3 1 4 4.3 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
CHEMBL3628104 123994 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
ChEMBL 380 3 1 4 4.3 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
52203651 123994 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
ChEMBL 380 3 1 4 4.3 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
CHEMBL3628104 123994 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
ChEMBL 380 3 1 4 4.3 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
122193179 124001 None 0 Human Functional pEC50 = 7.0 7.0 1 2
Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
ChEMBL 381 3 1 5 3.7 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccncc3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
CHEMBL3628115 124001 None 0 Human Functional pEC50 = 7.0 7.0 1 2
Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
ChEMBL 381 3 1 5 3.7 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccncc3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
122193179 124001 None 0 Human Functional pEC50 = 7 7.0 1 2
Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
ChEMBL 381 3 1 5 3.7 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccncc3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
CHEMBL3628115 124001 None 0 Human Functional pEC50 = 7 7.0 1 2
Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
ChEMBL 381 3 1 5 3.7 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccncc3C2=O)c(Cl)c1 10.1021/acs.jmedchem.5b00727
162664872 182281 None 0 Human Functional pEC50 = 7 7.0 - 1
Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay
ChEMBL 434 3 1 4 4.7 Cc1ccoc1C(=O)Nc1cc(F)c(N2C(=O)c3ccc(Cl)cc3C2=O)c(F)c1F 10.1016/j.bmcl.2020.127724
CHEMBL4782646 182281 None 0 Human Functional pEC50 = 7 7.0 - 1
Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay
ChEMBL 434 3 1 4 4.7 Cc1ccoc1C(=O)Nc1cc(F)c(N2C(=O)c3ccc(Cl)cc3C2=O)c(F)c1F 10.1016/j.bmcl.2020.127724
16659643 89990 None 0 Human Functional pIC50 = 9.4 9.4 - 1
Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay
ChEMBL 352 1 1 5 4.1 O=c1c2sc3ncc4cc[nH]c4c3c2ncn1-c1ccc(Cl)cc1 10.1021/jm070590c
CHEMBL238077 89990 None 0 Human Functional pIC50 = 9.4 9.4 - 1
Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay
ChEMBL 352 1 1 5 4.1 O=c1c2sc3ncc4cc[nH]c4c3c2ncn1-c1ccc(Cl)cc1 10.1021/jm070590c
16118680 70996 None 0 Human Functional pIC50 = 9.4 9.4 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 355 2 0 5 4.3 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951661 70996 None 0 Human Functional pIC50 = 9.4 9.4 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 355 2 0 5 4.3 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
16659645 148421 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay
ChEMBL 332 1 1 5 3.8 Cc1ccc(-n2cnc3c(sc4ncc5cc[nH]c5c43)c2=O)cc1 10.1021/jm070590c
CHEMBL393705 148421 None 0 Human Functional pIC50 = 9.2 9.2 - 1
Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay
ChEMBL 332 1 1 5 3.8 Cc1ccc(-n2cnc3c(sc4ncc5cc[nH]c5c43)c2=O)cc1 10.1021/jm070590c
15953801 71048 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 385 2 1 5 4.4 CNc1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951872 71048 None 0 Human Functional pIC50 = 9.1 9.1 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 385 2 1 5 4.4 CNc1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
23634171 976 None 1 Human Functional pIC50 = 9.1 9.1 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 366 3 1 6 3.7 C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)Cl 10.1016/j.bmcl.2009.04.104
6214 976 None 1 Human Functional pIC50 = 9.1 9.1 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 366 3 1 6 3.7 C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)Cl 10.1016/j.bmcl.2009.04.104
CHEMBL1783874 976 None 1 Human Functional pIC50 = 9.1 9.1 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 366 3 1 6 3.7 C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)Cl 10.1016/j.bmcl.2009.04.104
57404255 73237 None 1 Rat Functional pIC50 = 9.1 9.1 18 3
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 302 4 1 4 3.7 COc1ccc(-c2nsc(NC(=O)[C@@H]3C[C@H]3C)c2C)cc1 10.1016/j.bmcl.2012.02.003
CHEMBL2011870 73237 None 1 Rat Functional pIC50 = 9.1 9.1 18 3
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 302 4 1 4 3.7 COc1ccc(-c2nsc(NC(=O)[C@@H]3C[C@H]3C)c2C)cc1 10.1016/j.bmcl.2012.02.003
57559287 83855 None 0 Human Functional pIC50 = 9 9.0 10000 2
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 337 2 0 7 2.8 Cc1ccc(-n2cnc3c(sc4ncnc(N(C)C)c43)c2=O)cc1 10.1016/j.bmcl.2012.09.048
CHEMBL2205921 83855 None 0 Human Functional pIC50 = 9 9.0 10000 2
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 337 2 0 7 2.8 Cc1ccc(-n2cnc3c(sc4ncnc(N(C)C)c43)c2=O)cc1 10.1016/j.bmcl.2012.09.048
23634174 83856 None 0 Human Functional pIC50 = 9 9.0 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 357 2 0 7 3.1 CN(C)c1ncnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12 10.1016/j.bmcl.2012.09.048
CHEMBL2205922 83856 None 0 Human Functional pIC50 = 9 9.0 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 357 2 0 7 3.1 CN(C)c1ncnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12 10.1016/j.bmcl.2012.09.048
23634170 83857 None 0 Human Functional pIC50 = 9 9.0 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 401 2 0 7 3.2 CN(C)c1ncnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12 10.1016/j.bmcl.2012.09.048
CHEMBL2205923 83857 None 0 Human Functional pIC50 = 9 9.0 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 401 2 0 7 3.2 CN(C)c1ncnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12 10.1016/j.bmcl.2012.09.048
11537456 209 None 10 Human Functional pIC50 = 9 9.0 -3 3
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 342 2 0 6 4.0 CN(c1ccnc2c1c1ncn(c(=O)c1s2)C1CCCCCC1)C 10.1021/jm0504407
6354 209 None 10 Human Functional pIC50 = 9 9.0 -3 3
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 342 2 0 6 4.0 CN(c1ccnc2c1c1ncn(c(=O)c1s2)C1CCCCCC1)C 10.1021/jm0504407
CHEMBL225032 209 None 10 Human Functional pIC50 = 9 9.0 -3 3
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 342 2 0 6 4.0 CN(c1ccnc2c1c1ncn(c(=O)c1s2)C1CCCCCC1)C 10.1021/jm0504407
11559235 211 None 30 Rat Functional pIC50 = 9 9.0 4 3
Antagonist activity at rat mGluR1 expressed in 1321N1 cellsAntagonist activity at rat mGluR1 expressed in 1321N1 cells
ChEMBL 343 2 0 7 2.6 CN(c1ccnc2c1c1ncn(c(=O)c1s2)N1CCCCCC1)C 10.1016/j.bmcl.2006.06.053
3953 211 None 30 Rat Functional pIC50 = 9 9.0 4 3
Antagonist activity at rat mGluR1 expressed in 1321N1 cellsAntagonist activity at rat mGluR1 expressed in 1321N1 cells
ChEMBL 343 2 0 7 2.6 CN(c1ccnc2c1c1ncn(c(=O)c1s2)N1CCCCCC1)C 10.1016/j.bmcl.2006.06.053
CHEMBL386565 211 None 30 Rat Functional pIC50 = 9 9.0 4 3
Antagonist activity at rat mGluR1 expressed in 1321N1 cellsAntagonist activity at rat mGluR1 expressed in 1321N1 cells
ChEMBL 343 2 0 7 2.6 CN(c1ccnc2c1c1ncn(c(=O)c1s2)N1CCCCCC1)C 10.1016/j.bmcl.2006.06.053
23634254 62680 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 382 4 0 6 4.3 C=CCN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1783864 62680 None 0 Human Functional pIC50 = 9.0 9.0 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 382 4 0 6 4.3 C=CCN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
11313361 2134 None 44 Human Functional pIC50 = 8.9 8.9 3 2
Antagonist activity at human mGlu1 receptorAntagonist activity at human mGlu1 receptor
ChEMBL 325 3 0 4 3.9 COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1 10.1021/jm060950g
1385 2134 None 44 Human Functional pIC50 = 8.9 8.9 3 2
Antagonist activity at human mGlu1 receptorAntagonist activity at human mGlu1 receptor
ChEMBL 325 3 0 4 3.9 COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1 10.1021/jm060950g
CHEMBL174588 2134 None 44 Human Functional pIC50 = 8.9 8.9 3 2
Antagonist activity at human mGlu1 receptorAntagonist activity at human mGlu1 receptor
ChEMBL 325 3 0 4 3.9 COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1 10.1021/jm060950g
CHEMBL254574 2134 None 44 Human Functional pIC50 = 8.9 8.9 3 2
Antagonist activity at human mGlu1 receptorAntagonist activity at human mGlu1 receptor
ChEMBL 325 3 0 4 3.9 COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1 10.1021/jm060950g
16659802 1038 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay
ChEMBL 384 1 1 7 3.8 C[C@@H]1CNc2c(O1)cnc1c2c2ncn(c(=O)c2s1)c1ccc(cc1)Cl 10.1021/jm070590c
6348 1038 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay
ChEMBL 384 1 1 7 3.8 C[C@@H]1CNc2c(O1)cnc1c2c2ncn(c(=O)c2s1)c1ccc(cc1)Cl 10.1021/jm070590c
CHEMBL241327 1038 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay
ChEMBL 384 1 1 7 3.8 C[C@@H]1CNc2c(O1)cnc1c2c2ncn(c(=O)c2s1)c1ccc(cc1)Cl 10.1021/jm070590c
23634169 62690 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 346 3 1 6 3.3 C#CCNc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1783875 62690 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 346 3 1 6 3.3 C#CCNc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
44588464 175174 None 0 Mouse Functional pIC50 = 8.8 8.8 4 3
Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 359 2 0 6 3.1 Cc1c(C2=CCN(C(=O)OC(C)(C)C)CC2)nnn1-c1ncccc1F 10.1016/j.bmc.2008.09.060
CHEMBL456823 175174 None 0 Mouse Functional pIC50 = 8.8 8.8 4 3
Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 359 2 0 6 3.1 Cc1c(C2=CCN(C(=O)OC(C)(C)C)CC2)nnn1-c1ncccc1F 10.1016/j.bmc.2008.09.060
23634249 62764 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 410 3 1 6 3.8 C#CCNc1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784049 62764 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 410 3 1 6 3.8 C#CCNc1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
16660294 199834 None 2 Human Functional pIC50 = 8.7 8.7 4365 2
Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 343 4 1 6 3.1 CNc1cc(-c2csc(N(C)C(=O)c3ccc(F)cc3)n2)ncn1 10.1016/j.bmcl.2009.07.097
CHEMBL569270 199834 None 2 Human Functional pIC50 = 8.7 8.7 4365 2
Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 343 4 1 6 3.1 CNc1cc(-c2csc(N(C)C(=O)c3ccc(F)cc3)n2)ncn1 10.1016/j.bmcl.2009.07.097
23634325 62768 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 424 3 0 6 3.8 C#CCN(C)c1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784053 62768 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 424 3 0 6 3.8 C#CCN(C)c1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
11559235 211 None 30 Human Functional pIC50 = 8 8.0 -4 3
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 343 2 0 7 2.6 CN(c1ccnc2c1c1ncn(c(=O)c1s2)N1CCCCCC1)C 10.1021/jm0504407
3953 211 None 30 Human Functional pIC50 = 8 8.0 -4 3
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 343 2 0 7 2.6 CN(c1ccnc2c1c1ncn(c(=O)c1s2)N1CCCCCC1)C 10.1021/jm0504407
CHEMBL386565 211 None 30 Human Functional pIC50 = 8 8.0 -4 3
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 343 2 0 7 2.6 CN(c1ccnc2c1c1ncn(c(=O)c1s2)N1CCCCCC1)C 10.1021/jm0504407
16038338 199803 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 314 3 0 5 3.0 CN(C(=O)c1ccc(F)cc1)c1nc(-c2ccncn2)cs1 10.1016/j.bmcl.2009.07.097
CHEMBL568991 199803 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 314 3 0 5 3.0 CN(C(=O)c1ccc(F)cc1)c1nc(-c2ccncn2)cs1 10.1016/j.bmcl.2009.07.097
16118812 70998 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 346 2 0 6 3.5 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(C#N)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951663 70998 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 346 2 0 6 3.5 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(C#N)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
54585406 62685 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 378 5 1 7 4.0 C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1783869 62685 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 378 5 1 7 4.0 C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
54585404 62683 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 382 4 1 6 4.6 C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1783867 62683 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 382 4 1 6 4.6 C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
54582943 62776 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 367 4 1 7 3.5 C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc(F)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784061 62776 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 367 4 1 7 3.5 C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc(F)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
54584887 62767 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 376 4 0 7 3.1 C#CCN(C)c1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784052 62767 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 376 4 0 7 3.1 C#CCN(C)c1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
67181213 73242 None 0 Human Functional pIC50 = 7 7.0 - 1
Allosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assayAllosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assay
ChEMBL 290 3 1 3 3.9 Cc1c(-c2ccc(F)cc2)nsc1NC(=O)[C@@H]1C[C@H]1C 10.1016/j.bmcl.2012.02.003
CHEMBL2011875 73242 None 0 Human Functional pIC50 = 7 7.0 - 1
Allosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assayAllosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assay
ChEMBL 290 3 1 3 3.9 Cc1c(-c2ccc(F)cc2)nsc1NC(=O)[C@@H]1C[C@H]1C 10.1016/j.bmcl.2012.02.003
45486747 201104 None 0 Human Functional pIC50 = 7 7.0 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 313 3 0 4 3.6 CN(C(=O)c1cccc(F)c1)c1nc(-c2ccncc2)cs1 10.1016/j.bmcl.2009.07.097
CHEMBL579213 201104 None 0 Human Functional pIC50 = 7 7.0 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 313 3 0 4 3.6 CN(C(=O)c1cccc(F)c1)c1nc(-c2ccncc2)cs1 10.1016/j.bmcl.2009.07.097
44447970 155149 None 0 Human Functional pIC50 = 6 6.0 - 1
Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor
ChEMBL 369 4 3 4 3.2 NC(C(=O)O)(C1CC(C(=O)O)C1)C1c2ccccc2Sc2ccccc21 10.1021/jm060950g
CHEMBL401721 155149 None 0 Human Functional pIC50 = 6 6.0 - 1
Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor
ChEMBL 369 4 3 4 3.2 NC(C(=O)O)(C1CC(C(=O)O)C1)C1c2ccccc2Sc2ccccc21 10.1021/jm060950g
44588462 175655 None 0 Mouse Functional pIC50 = 6 6.0 -4 2
Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 327 2 0 6 2.7 CC(C)(C)OC(=O)N1CC=C(c2cn(-c3ccncc3)nn2)CC1 10.1016/j.bmc.2008.09.060
CHEMBL457873 175655 None 0 Mouse Functional pIC50 = 6 6.0 -4 2
Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 327 2 0 6 2.7 CC(C)(C)OC(=O)N1CC=C(c2cn(-c3ccncc3)nn2)CC1 10.1016/j.bmc.2008.09.060
72163585 92067 None 0 Human Functional pIC50 = 6 6.0 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 369 2 0 3 3.3 O=C(N1C[C@@H]2CN(c3ncccc3F)C[C@@H]2C1)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.07.029
CHEMBL2418382 92067 None 0 Human Functional pIC50 = 6 6.0 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 369 2 0 3 3.3 O=C(N1C[C@@H]2CN(c3ncccc3F)C[C@@H]2C1)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.07.029
1418 3449 None 40 Human Functional pIC50 = 5 5.0 -1 2
Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor
ChEMBL 195 3 3 3 0.5 N[C@@H](c1ccc(cc1)C(=O)O)C(=O)O 10.1021/jm060950g
5311459 3449 None 40 Human Functional pIC50 = 5 5.0 -1 2
Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor
ChEMBL 195 3 3 3 0.5 N[C@@H](c1ccc(cc1)C(=O)O)C(=O)O 10.1021/jm060950g
CHEMBL94990 3449 None 40 Human Functional pIC50 = 5 5.0 -1 2
Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor
ChEMBL 195 3 3 3 0.5 N[C@@H](c1ccc(cc1)C(=O)O)C(=O)O 10.1021/jm060950g
91618210 125189 None 0 Human Functional pIC50 = 5 5.0 -501 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 410 2 0 6 3.2 Cc1ccc(-c2ccnc3c2CCN2C(=O)CN=C(n4cnc(C5CC5)c4)C=C32)cn1 nan
CHEMBL3644418 125189 None 0 Human Functional pIC50 = 5 5.0 -501 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 410 2 0 6 3.2 Cc1ccc(-c2ccnc3c2CCN2C(=O)CN=C(n4cnc(C5CC5)c4)C=C32)cn1 nan
11654379 142158 None 0 Human Functional pIC50 = 7 7.0 1 3
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 406 6 0 6 5.0 CCCCc1nc2c(sc3nccc(N(C)C)c32)c(=O)n1-c1ccc(CC)cc1 10.1021/jm0504407
CHEMBL387976 142158 None 0 Human Functional pIC50 = 7 7.0 1 3
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 406 6 0 6 5.0 CCCCc1nc2c(sc3nccc(N(C)C)c32)c(=O)n1-c1ccc(CC)cc1 10.1021/jm0504407
44431061 86786 None 0 Rat Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay
ChEMBL 293 3 2 4 2.3 O=C1NN=CC2c3cc(OCc4ccccc4)ccc3NC12 10.1016/j.bmcl.2007.01.055
CHEMBL232013 86786 None 0 Rat Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay
ChEMBL 293 3 2 4 2.3 O=C1NN=CC2c3cc(OCc4ccccc4)ccc3NC12 10.1016/j.bmcl.2007.01.055
67425408 87551 None 0 Human Functional pIC50 = 6.0 6.0 -12 2
Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay
ChEMBL 439 5 1 6 5.3 C[C@@H]1C[C@H]1C(=O)Nc1snc(-c2ccc3nn(C)cc3c2)c1-c1cccc(C(F)F)n1 10.1016/j.bmcl.2013.01.009
CHEMBL2334975 87551 None 0 Human Functional pIC50 = 6.0 6.0 -12 2
Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay
ChEMBL 439 5 1 6 5.3 C[C@@H]1C[C@H]1C(=O)Nc1snc(-c2ccc3nn(C)cc3c2)c1-c1cccc(C(F)F)n1 10.1016/j.bmcl.2013.01.009
54582494 62687 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 396 5 1 7 4.1 C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc(OC)c(F)c4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1783871 62687 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 396 5 1 7 4.1 C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc(OC)c(F)c4)cnc3c12 10.1016/j.bmcl.2009.04.104
563298 92405 None 13 Rat Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay
ChEMBL 292 3 2 2 3.0 O=C1NCCc2c1[nH]c1ccc(OCc3ccccc3)cc21 10.1016/j.bmcl.2007.01.055
CHEMBL243043 92405 None 13 Rat Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay
ChEMBL 292 3 2 2 3.0 O=C1NCCc2c1[nH]c1ccc(OCc3ccccc3)cc21 10.1016/j.bmcl.2007.01.055
122196105 124307 None 0 Human Functional pIC50 = 7.0 7.0 22 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 448 3 1 4 5.3 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(C(F)(F)F)c1 10.1016/j.bmcl.2015.10.013
CHEMBL3634428 124307 None 0 Human Functional pIC50 = 7.0 7.0 22 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 448 3 1 4 5.3 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(C(F)(F)F)c1 10.1016/j.bmcl.2015.10.013
44431049 142430 None 0 Rat Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay
ChEMBL 305 2 3 2 2.7 O=C(Nc1ccccc1)c1ccc2[nH]c3c(c2c1)CCNC3=O 10.1016/j.bmcl.2007.01.055
CHEMBL388668 142430 None 0 Rat Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay
ChEMBL 305 2 3 2 2.7 O=C(Nc1ccccc1)c1ccc2[nH]c3c(c2c1)CCNC3=O 10.1016/j.bmcl.2007.01.055
24777698 94806 None 0 Rat Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 307 2 0 4 2.9 O=C1CCCc2nc(N3CCN(c4ccccc4)CC3)ccc21 10.1021/jm0611298
CHEMBL253145 94806 None 0 Rat Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 307 2 0 4 2.9 O=C1CCCc2nc(N3CCN(c4ccccc4)CC3)ccc21 10.1021/jm0611298
49788806 18128 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiologyAntagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiology
ChEMBL 531 18 5 5 3.9 NCCCNCCCCNCCCNC(=O)[C@H](CC1CCCCC1)NC(=O)CC12CC3CC(CC(C3)C1)C2 10.1021/jm100886h
CHEMBL1269127 18128 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiologyAntagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiology
ChEMBL 531 18 5 5 3.9 NCCCNCCCCNCCCNC(=O)[C@H](CC1CCCCC1)NC(=O)CC12CC3CC(CC(C3)C1)C2 10.1021/jm100886h
89979810 133172 None 0 Human Functional pIC50 = 6.0 6.0 -22 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 419 4 0 7 2.9 COCCc1cn(C2=NCC(=O)N3CCc4c(cccc4-c4nccs4)C3=C2)cn1 nan
CHEMBL3702444 133172 None 0 Human Functional pIC50 = 6.0 6.0 -22 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 419 4 0 7 2.9 COCCc1cn(C2=NCC(=O)N3CCc4c(cccc4-c4nccs4)C3=C2)cn1 nan
54583942 62763 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 391 3 1 9 2.2 C#CCNc1ncnc2sc3c(=O)n(-c4ccc5c(c4)OCCO5)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784048 62763 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 391 3 1 9 2.2 C#CCNc1ncnc2sc3c(=O)n(-c4ccc5c(c4)OCCO5)cnc3c12 10.1016/j.bmcl.2009.04.104
3115037 197641 None 5 Rat Functional pIC50 = 5.0 5.0 - 1
Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting
ChEMBL 282 4 0 3 3.8 CC(CC(=O)c1ccc2c(c1)OCCO2)c1ccccc1 10.1016/j.bmc.2009.05.072
CHEMBL550523 197641 None 5 Rat Functional pIC50 = 5.0 5.0 - 1
Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting
ChEMBL 282 4 0 3 3.8 CC(CC(=O)c1ccc2c(c1)OCCO2)c1ccccc1 10.1016/j.bmc.2009.05.072
118735959 118974 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay
ChEMBL 363 4 2 5 3.2 N#Cc1c(NCc2ccccc2)sc2c1CCN(C(=O)c1ccn[nH]1)C2 10.1016/j.ejmech.2015.04.060
CHEMBL3422875 118974 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay
ChEMBL 363 4 2 5 3.2 N#Cc1c(NCc2ccccc2)sc2c1CCN(C(=O)c1ccn[nH]1)C2 10.1016/j.ejmech.2015.04.060
49788655 18322 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiologyAntagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiology
ChEMBL 423 17 5 5 1.7 NCCCNCCCCNCCCNC(=O)[C@H](CC1CCCCC1)NC(=O)C1CC1 10.1021/jm100886h
CHEMBL1270718 18322 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiologyAntagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiology
ChEMBL 423 17 5 5 1.7 NCCCNCCCCNCCCNC(=O)[C@H](CC1CCCCC1)NC(=O)C1CC1 10.1021/jm100886h
46886138 8234 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 343 1 1 7 2.9 Cc1nc(N)c2c(n1)sc1c(=O)n(-c3ccc(Cl)cc3)cnc12 10.1016/j.bmcl.2010.03.004
CHEMBL1092277 8234 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 343 1 1 7 2.9 Cc1nc(N)c2c(n1)sc1c(=O)n(-c3ccc(Cl)cc3)cnc12 10.1016/j.bmcl.2010.03.004
54584442 62675 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 348 4 1 6 3.9 C=CCNc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1783859 62675 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 348 4 1 6 3.9 C=CCNc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
44588426 189311 None 0 Human Functional pIC50 = 8.0 8.0 5 3
Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 340 2 0 5 3.6 Cc1ccccc1-n1cc(C2=CCN(C(=O)OC(C)(C)C)CC2)nn1 10.1016/j.bmc.2008.09.060
CHEMBL511352 189311 None 0 Human Functional pIC50 = 8.0 8.0 5 3
Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 340 2 0 5 3.6 Cc1ccccc1-n1cc(C2=CCN(C(=O)OC(C)(C)C)CC2)nn1 10.1016/j.bmc.2008.09.060
45484929 199714 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL 318 2 0 5 3.4 Cc1c(-c2ccc3c(c2)CC(C)(C)C3=O)nnn1-c1cccnc1 10.1016/j.bmcl.2009.07.145
CHEMBL568451 199714 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL 318 2 0 5 3.4 Cc1c(-c2ccc3c(c2)CC(C)(C)C3=O)nnn1-c1cccnc1 10.1016/j.bmcl.2009.07.145
70691553 73238 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Allosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assayAllosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assay
ChEMBL 302 4 1 4 3.7 COc1ccc(-c2nsc(NC(=O)[C@H]3C[C@@H]3C)c2C)cc1 10.1016/j.bmcl.2012.02.003
CHEMBL2011871 73238 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Allosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assayAllosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assay
ChEMBL 302 4 1 4 3.7 COc1ccc(-c2nsc(NC(=O)[C@H]3C[C@@H]3C)c2C)cc1 10.1016/j.bmcl.2012.02.003
24777443 155034 None 0 Rat Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 375 2 0 4 4.5 CC1(C)CC(=O)c2cc(C#N)c(N3CC=C(c4ccc(F)cc4)CC3)nc2C1 10.1021/jm0611298
CHEMBL401096 155034 None 0 Rat Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 375 2 0 4 4.5 CC1(C)CC(=O)c2cc(C#N)c(N3CC=C(c4ccc(F)cc4)CC3)nc2C1 10.1021/jm0611298
44442432 154663 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay
ChEMBL 370 2 0 5 4.2 Cc1nc2c(cnn2-c2ccc(Cl)cc2)c(=O)n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2007.05.028
CHEMBL399127 154663 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay
ChEMBL 370 2 0 5 4.2 Cc1nc2c(cnn2-c2ccc(Cl)cc2)c(=O)n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2007.05.028
89979958 125167 None 0 Human Functional pIC50 = 6.0 6.0 -218 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 376 3 0 5 3.2 CO[C@@H](C)c1cn(C2=NCC(=O)N3CCc4c(cccc4C4CC4)C3=C2)cn1 nan
CHEMBL3644396 125167 None 0 Human Functional pIC50 = 6.0 6.0 -218 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 376 3 0 5 3.2 CO[C@@H](C)c1cn(C2=NCC(=O)N3CCc4c(cccc4C4CC4)C3=C2)cn1 nan
91618214 125203 None 0 Human Functional pIC50 = 6.0 6.0 -64 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 410 2 0 6 3.2 Cc1cnc(-c2cccc3c2CCN2C(=O)CN=C(n4cnc(C5CC5)c4)C=C32)cn1 nan
CHEMBL3644432 125203 None 0 Human Functional pIC50 = 6.0 6.0 -64 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 410 2 0 6 3.2 Cc1cnc(-c2cccc3c2CCN2C(=O)CN=C(n4cnc(C5CC5)c4)C=C32)cn1 nan
78320481 114403 None 4 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay
ChEMBL 318 2 0 4 4.4 Cc1ccc(-n2cnc3c(-c4ccccc4)csc3c2=O)cc1 10.1016/j.ejmech.2014.08.027
CHEMBL3330808 114403 None 4 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay
ChEMBL 318 2 0 4 4.4 Cc1ccc(-n2cnc3c(-c4ccccc4)csc3c2=O)cc1 10.1016/j.ejmech.2014.08.027
78320481 114403 None 4 Human Functional pIC50 = 7.0 7.0 - 1
FLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and diluteFLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and dilute
ChEMBL 318 2 0 4 4.4 Cc1ccc(-n2cnc3c(-c4ccccc4)csc3c2=O)cc1 nan
CHEMBL3330808 114403 None 4 Human Functional pIC50 = 7.0 7.0 - 1
FLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and diluteFLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and dilute
ChEMBL 318 2 0 4 4.4 Cc1ccc(-n2cnc3c(-c4ccccc4)csc3c2=O)cc1 nan
11682046 85188 None 0 Human Functional pIC50 = 7.0 7.0 1 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 362 3 0 6 3.8 CCc1ccc(-n2cnc3c(sc4nccc(N5CCC5)c43)c2=O)cc1 10.1021/jm0504407
CHEMBL225126 85188 None 0 Human Functional pIC50 = 7.0 7.0 1 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 362 3 0 6 3.8 CCc1ccc(-n2cnc3c(sc4nccc(N5CCC5)c43)c2=O)cc1 10.1021/jm0504407
71682959 91082 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 340 2 0 4 2.7 C[C@@H]1CN(c2cnccn2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
CHEMBL2397374 91082 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 340 2 0 4 2.7 C[C@@H]1CN(c2cnccn2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
72163835 92055 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 326 1 0 3 2.2 CC1(C)[C@H]2CN(C(=O)N3C[C@@H]4CN(c5ccccn5)C[C@@H]4C3)C[C@H]21 10.1016/j.bmcl.2013.07.029
CHEMBL2418357 92055 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 326 1 0 3 2.2 CC1(C)[C@H]2CN(C(=O)N3C[C@@H]4CN(c5ccccn5)C[C@@H]4C3)C[C@H]21 10.1016/j.bmcl.2013.07.029
57397023 71006 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 338 3 0 6 3.6 COc1cccc(-n2ccc3c(sc4nccc(OC)c43)c2=O)c1 10.1016/j.bmcl.2011.12.131
CHEMBL1951671 71006 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 338 3 0 6 3.6 COc1cccc(-n2ccc3c(sc4nccc(OC)c43)c2=O)c1 10.1016/j.bmcl.2011.12.131
71682959 91082 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 340 2 0 4 2.7 C[C@@H]1CN(c2cnccn2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
CHEMBL2397374 91082 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 340 2 0 4 2.7 C[C@@H]1CN(c2cnccn2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
72163835 92055 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 326 1 0 3 2.2 CC1(C)[C@H]2CN(C(=O)N3C[C@@H]4CN(c5ccccn5)C[C@@H]4C3)C[C@H]21 10.1016/j.bmcl.2013.07.029
CHEMBL2418357 92055 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 326 1 0 3 2.2 CC1(C)[C@H]2CN(C(=O)N3C[C@@H]4CN(c5ccccn5)C[C@@H]4C3)C[C@H]21 10.1016/j.bmcl.2013.07.029
89980424 125176 None 0 Human Functional pIC50 = 5.9 5.9 -169 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 374 2 1 5 2.4 O=C1CN=C(n2cnc(C3(O)CC3)c2)C=C2c3cccc(C4CC4)c3CCN12 nan
CHEMBL3644405 125176 None 0 Human Functional pIC50 = 5.9 5.9 -169 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 374 2 1 5 2.4 O=C1CN=C(n2cnc(C3(O)CC3)c2)C=C2c3cccc(C4CC4)c3CCN12 nan
89980085 133188 None 0 Human Functional pIC50 = 4.9 4.9 -117 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 414 2 0 6 3.0 O=C1CN=C(n2cnc(C3CC3)c2)C=C2c3cccc(-c4cnc(F)nc4)c3CCN12 nan
CHEMBL3702462 133188 None 0 Human Functional pIC50 = 4.9 4.9 -117 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 414 2 0 6 3.0 O=C1CN=C(n2cnc(C3CC3)c2)C=C2c3cccc(-c4cnc(F)nc4)c3CCN12 nan
57881707 83848 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 383 6 2 9 2.2 COc1ccc(-n2cnc3c(sc4ncnc(NCCCO)c43)c2=O)cc1 10.1016/j.bmcl.2012.09.048
CHEMBL2205913 83848 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 383 6 2 9 2.2 COc1ccc(-n2cnc3c(sc4ncnc(NCCCO)c43)c2=O)cc1 10.1016/j.bmcl.2012.09.048
16659805 148700 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay
ChEMBL 384 1 1 7 3.8 C[C@H]1COc2cnc3sc4c(=O)n(-c5ccc(Cl)cc5)cnc4c3c2N1 10.1021/jm070590c
CHEMBL393923 148700 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay
ChEMBL 384 1 1 7 3.8 C[C@H]1COc2cnc3sc4c(=O)n(-c5ccc(Cl)cc5)cnc4c3c2N1 10.1021/jm070590c
16118537 978 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 363 4 1 6 4.2 COc1ccc(cc1)n1ccc2c(c1=O)sc1c2c(ccn1)NC1CC1 10.1016/j.bmcl.2011.12.131
6357 978 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 363 4 1 6 4.2 COc1ccc(cc1)n1ccc2c(c1=O)sc1c2c(ccn1)NC1CC1 10.1016/j.bmcl.2011.12.131
CHEMBL1951683 978 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 363 4 1 6 4.2 COc1ccc(cc1)n1ccc2c(c1=O)sc1c2c(ccn1)NC1CC1 10.1016/j.bmcl.2011.12.131
16118817 71066 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 348 3 1 6 3.9 Cc1ccc(-n2ccc3c(sc4ncnc(NC5CC5)c43)c2=O)cc1 10.1016/j.bmcl.2011.12.131
CHEMBL1951890 71066 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 348 3 1 6 3.9 Cc1ccc(-n2ccc3c(sc4ncnc(NC5CC5)c43)c2=O)cc1 10.1016/j.bmcl.2011.12.131
44588463 173413 None 0 Mouse Functional pIC50 = 7.9 7.9 -4 3
Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 345 2 0 6 2.8 CC(C)(C)OC(=O)N1CC=C(c2cn(-c3ncccc3F)nn2)CC1 10.1016/j.bmc.2008.09.060
CHEMBL452618 173413 None 0 Mouse Functional pIC50 = 7.9 7.9 -4 3
Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 345 2 0 6 2.8 CC(C)(C)OC(=O)N1CC=C(c2cn(-c3ncccc3F)nn2)CC1 10.1016/j.bmc.2008.09.060
54582002 62770 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 363 4 1 7 3.7 C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784055 62770 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 363 4 1 7 3.7 C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
54585850 62765 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 380 4 1 7 3.2 C#CCNc1ccnc2sc3c(=O)n(-c4ccc(OC)c(F)c4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784050 62765 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 380 4 1 7 3.2 C#CCNc1ccnc2sc3c(=O)n(-c4ccc(OC)c(F)c4)cnc3c12 10.1016/j.bmcl.2009.04.104
122196123 124324 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 364 3 1 4 3.8 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)cc1F 10.1016/j.bmcl.2015.10.013
CHEMBL3634445 124324 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 364 3 1 4 3.8 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)cc1F 10.1016/j.bmcl.2015.10.013
54580485 62677 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 412 4 1 6 4.4 C=CCNc1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1783861 62677 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 412 4 1 6 4.4 C=CCNc1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
44588429 176938 None 0 Human Functional pIC50 = 6.9 6.9 1 2
Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 342 3 0 4 3.5 CC(C)(C)CC(=O)N1CC=C(c2cn(-c3ccccc3F)nn2)CC1 10.1016/j.bmc.2008.09.060
CHEMBL461035 176938 None 0 Human Functional pIC50 = 6.9 6.9 1 2
Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 342 3 0 4 3.5 CC(C)(C)CC(=O)N1CC=C(c2cn(-c3ccccc3F)nn2)CC1 10.1016/j.bmc.2008.09.060
44431044 88507 None 0 Rat Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay
ChEMBL 327 2 2 2 3.0 CC(N(C)C(=O)c1ccc2[nH]c3c(c2c1)CCNC3=O)C(C)(C)C 10.1016/j.bmcl.2007.01.055
CHEMBL234960 88507 None 0 Rat Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay
ChEMBL 327 2 2 2 3.0 CC(N(C)C(=O)c1ccc2[nH]c3c(c2c1)CCNC3=O)C(C)(C)C 10.1016/j.bmcl.2007.01.055
73335640 133149 None 0 Human Functional pIC50 = 5.9 5.9 -54 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 373 2 0 6 2.8 CCc1cn(C2=NCC(=O)N3CCc4c(cccc4-c4ncco4)C3=C2)cn1 nan
CHEMBL3702422 133149 None 0 Human Functional pIC50 = 5.9 5.9 -54 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 373 2 0 6 2.8 CCc1cn(C2=NCC(=O)N3CCc4c(cccc4-c4ncco4)C3=C2)cn1 nan
10523805 29056 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Inhibition of Quisqualate-Induced PI Hydrolysis measured in CHO Metabotropic glutamate receptor 1 Expressing CellsInhibition of Quisqualate-Induced PI Hydrolysis measured in CHO Metabotropic glutamate receptor 1 Expressing Cells
ChEMBL 380 5 2 6 1.9 COC(=O)[C@H](Cc1ccccc1)NC(=O)C12CC1/C(=N\O)c1ccccc1O2 10.1021/jm0009944
CHEMBL138082 29056 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Inhibition of Quisqualate-Induced PI Hydrolysis measured in CHO Metabotropic glutamate receptor 1 Expressing CellsInhibition of Quisqualate-Induced PI Hydrolysis measured in CHO Metabotropic glutamate receptor 1 Expressing Cells
ChEMBL 380 5 2 6 1.9 COC(=O)[C@H](Cc1ccccc1)NC(=O)C12CC1/C(=N\O)c1ccccc1O2 10.1021/jm0009944
44445058 94718 None 0 Rat Functional pIC50 = 4.9 4.9 - 1
Antagonist activity at rat mGluR1 by FLIPR assayAntagonist activity at rat mGluR1 by FLIPR assay
ChEMBL 409 4 1 5 5.3 CC1(C)CC(=O)c2cc([N+](=O)[O-])c(NC3CC=C(c4ccc(F)cc4)CC3)nc2C1 10.1021/jm0611298
CHEMBL252543 94718 None 0 Rat Functional pIC50 = 4.9 4.9 - 1
Antagonist activity at rat mGluR1 by FLIPR assayAntagonist activity at rat mGluR1 by FLIPR assay
ChEMBL 409 4 1 5 5.3 CC1(C)CC(=O)c2cc([N+](=O)[O-])c(NC3CC=C(c4ccc(F)cc4)CC3)nc2C1 10.1021/jm0611298
11537814 85228 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 362 2 1 7 2.9 CN(C)c1ccnc2sc3c(=O)n(-c4ccc5cn[nH]c5c4)cnc3c12 10.1021/jm0504407
CHEMBL225438 85228 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 362 2 1 7 2.9 CN(C)c1ccnc2sc3c(=O)n(-c4ccc5cn[nH]c5c4)cnc3c12 10.1021/jm0504407
118735953 118970 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay
ChEMBL 453 4 2 5 4.6 CC(C)c1cc(C(=O)N2CCc3c(sc(NC(=O)c4ccc(Cl)cc4)c3C#N)C2)[nH]n1 10.1016/j.ejmech.2015.04.060
CHEMBL3422869 118970 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay
ChEMBL 453 4 2 5 4.6 CC(C)c1cc(C(=O)N2CCc3c(sc(NC(=O)c4ccc(Cl)cc4)c3C#N)C2)[nH]n1 10.1016/j.ejmech.2015.04.060
122196103 124305 None 0 Human Functional pIC50 = 6.9 6.9 53 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 414 3 1 4 4.7 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(C(F)(F)F)c1 10.1016/j.bmcl.2015.10.013
CHEMBL3634426 124305 None 0 Human Functional pIC50 = 6.9 6.9 53 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 414 3 1 4 4.7 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(C(F)(F)F)c1 10.1016/j.bmcl.2015.10.013
57403924 71016 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 367 5 2 7 3.0 COc1ccc(-n2ccc3c(sc4nccc(NCCO)c43)c2=O)cc1 10.1016/j.bmcl.2011.12.131
CHEMBL1951684 71016 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 367 5 2 7 3.0 COc1ccc(-n2ccc3c(sc4nccc(NCCO)c43)c2=O)cc1 10.1016/j.bmcl.2011.12.131
118735967 118979 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay
ChEMBL 392 4 1 5 4.0 N#Cc1c(NCc2ccccc2)sc2c1CCN(C(=O)c1cnccc1F)C2 10.1016/j.ejmech.2015.04.060
CHEMBL3422883 118979 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay
ChEMBL 392 4 1 5 4.0 N#Cc1c(NCc2ccccc2)sc2c1CCN(C(=O)c1cnccc1F)C2 10.1016/j.ejmech.2015.04.060
23655076 93983 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay
ChEMBL 415 3 1 7 2.2 Cc1nc2c(cnn2-c2cccc(S(N)(=O)=O)c2)c(=O)n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2007.05.028
CHEMBL248233 93983 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay
ChEMBL 415 3 1 7 2.2 Cc1nc2c(cnn2-c2cccc(S(N)(=O)=O)c2)c(=O)n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2007.05.028
78320803 114406 None 4 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay
ChEMBL 330 3 0 4 4.8 C=Cc1ccc(-n2cnc3c(-c4ccccc4)csc3c2=O)cc1 10.1016/j.ejmech.2014.08.027
CHEMBL3330813 114406 None 4 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay
ChEMBL 330 3 0 4 4.8 C=Cc1ccc(-n2cnc3c(-c4ccccc4)csc3c2=O)cc1 10.1016/j.ejmech.2014.08.027
54580948 62784 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 363 4 1 8 2.4 C#CCNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784069 62784 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 363 4 1 8 2.4 C#CCNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
11515957 84843 None 1 Human Functional pIC50 = 7.9 7.9 1 3
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 356 2 0 6 4.4 CN(C)c1ccnc2sc3c(=O)n(C4CCCCCCC4)cnc3c12 10.1021/jm0504407
CHEMBL223399 84843 None 1 Human Functional pIC50 = 7.9 7.9 1 3
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 356 2 0 6 4.4 CN(C)c1ccnc2sc3c(=O)n(C4CCCCCCC4)cnc3c12 10.1021/jm0504407
11515679 85136 None 0 Human Functional pIC50 = 6.9 6.9 1 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 342 2 0 6 3.8 CC1CCCCC1n1cnc2c(sc3nccc(N(C)C)c32)c1=O 10.1021/jm0504407
CHEMBL224672 85136 None 0 Human Functional pIC50 = 6.9 6.9 1 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 342 2 0 6 3.8 CC1CCCCC1n1cnc2c(sc3nccc(N(C)C)c32)c1=O 10.1021/jm0504407
45486748 199561 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 313 3 0 4 3.6 CN(C(=O)c1ccccc1F)c1nc(-c2ccncc2)cs1 10.1016/j.bmcl.2009.07.097
CHEMBL567667 199561 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 313 3 0 4 3.6 CN(C(=O)c1ccccc1F)c1nc(-c2ccncc2)cs1 10.1016/j.bmcl.2009.07.097
24777318 94807 None 0 Rat Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 360 2 0 5 3.4 CC1(C)CC(=O)c2cc(C#N)c(N3CCN(c4ccccc4)CC3)nc2C1 10.1021/jm0611298
CHEMBL253146 94807 None 0 Rat Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 360 2 0 5 3.4 CC1(C)CC(=O)c2cc(C#N)c(N3CCN(c4ccccc4)CC3)nc2C1 10.1021/jm0611298
73335920 125145 None 0 Human Functional pIC50 = 5.9 5.9 -181 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 385 2 0 6 3.1 O=C1CN=C(n2cnc(C3CC3)c2)C=C2c3cccc(-c4ncco4)c3CCN12 nan
CHEMBL3644372 125145 None 0 Human Functional pIC50 = 5.9 5.9 -181 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 385 2 0 6 3.1 O=C1CN=C(n2cnc(C3CC3)c2)C=C2c3cccc(-c4ncco4)c3CCN12 nan
73335035 133093 None 0 Human Functional pIC50 = 5.9 5.9 -28 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 392 6 0 5 2.9 COCCOc1cccc(C2=NCC(=O)N3CCc4c(OC)cccc4C3=C2)c1 nan
CHEMBL3702366 133093 None 0 Human Functional pIC50 = 5.9 5.9 -28 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 392 6 0 5 2.9 COCCOc1cccc(C2=NCC(=O)N3CCc4c(OC)cccc4C3=C2)c1 nan
86711359 133110 None 0 Human Functional pIC50 = 5.9 5.9 -5 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 418 1 0 4 2.3 Cn1ccc(C2=NCC(=O)N3CCc4c(I)cccc4C3=C2)n1 nan
CHEMBL3702383 133110 None 0 Human Functional pIC50 = 5.9 5.9 -5 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 418 1 0 4 2.3 Cn1ccc(C2=NCC(=O)N3CCc4c(I)cccc4C3=C2)n1 nan
71561287 87550 None 0 Human Functional pIC50 = 5.9 5.9 -25 2
Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay
ChEMBL 421 5 1 6 4.8 C[C@@H]1C[C@H]1C(=O)Nc1snc(-c2ccc3nn(C)cc3c2)c1-c1cccc(CF)n1 10.1016/j.bmcl.2013.01.009
CHEMBL2334974 87550 None 0 Human Functional pIC50 = 5.9 5.9 -25 2
Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay
ChEMBL 421 5 1 6 4.8 C[C@@H]1C[C@H]1C(=O)Nc1snc(-c2ccc3nn(C)cc3c2)c1-c1cccc(CF)n1 10.1016/j.bmcl.2013.01.009
24777816 154934 None 0 Rat Functional pIC50 = 4.9 4.9 - 1
Antagonist activity at rat mGluR1 by FLIPR assayAntagonist activity at rat mGluR1 by FLIPR assay
ChEMBL 326 3 2 6 2.8 CC1(C)CC(=O)c2cc(-c3nn[nH]n3)c(NC3CCCC3)nc2C1 10.1021/jm0611298
CHEMBL400505 154934 None 0 Rat Functional pIC50 = 4.9 4.9 - 1
Antagonist activity at rat mGluR1 by FLIPR assayAntagonist activity at rat mGluR1 by FLIPR assay
ChEMBL 326 3 2 6 2.8 CC1(C)CC(=O)c2cc(-c3nn[nH]n3)c(NC3CCCC3)nc2C1 10.1021/jm0611298
71682961 91083 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 340 2 0 4 2.7 C[C@@H]1CN(c2ccncn2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
CHEMBL2397376 91083 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 340 2 0 4 2.7 C[C@@H]1CN(c2ccncn2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
57400362 71018 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 381 5 2 7 3.4 COc1ccc(-n2ccc3c(sc4nccc(NC[C@@H](C)O)c43)c2=O)cc1 10.1016/j.bmcl.2011.12.131
CHEMBL1951686 71018 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 381 5 2 7 3.4 COc1ccc(-n2ccc3c(sc4nccc(NC[C@@H](C)O)c43)c2=O)cc1 10.1016/j.bmcl.2011.12.131
71682961 91083 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 340 2 0 4 2.7 C[C@@H]1CN(c2ccncn2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
CHEMBL2397376 91083 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 340 2 0 4 2.7 C[C@@H]1CN(c2ccncn2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
87550873 122272 None 0 Rat Functional pIC50 = 5.9 5.9 -354 2
Negative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysisNegative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysis
ChEMBL 353 2 0 4 4.2 O=[N+]([O-])c1cccnc1N1CCC(=CC#Cc2cccc(Cl)c2)CC1 10.1016/j.bmc.2015.05.008
CHEMBL3597598 122272 None 0 Rat Functional pIC50 = 5.9 5.9 -354 2
Negative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysisNegative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysis
ChEMBL 353 2 0 4 4.2 O=[N+]([O-])c1cccnc1N1CCC(=CC#Cc2cccc(Cl)c2)CC1 10.1016/j.bmc.2015.05.008
78324865 114395 None 4 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay
ChEMBL 304 2 0 4 4.1 O=c1c2scc(-c3ccccc3)c2ncn1-c1ccccc1 10.1016/j.ejmech.2014.08.027
CHEMBL3330800 114395 None 4 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay
ChEMBL 304 2 0 4 4.1 O=c1c2scc(-c3ccccc3)c2ncn1-c1ccccc1 10.1016/j.ejmech.2014.08.027
54582006 62789 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 377 3 1 9 2.2 C#CCNc1ncnc2sc3c(=O)n(-c4ccc5c(c4)OCO5)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784074 62789 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 377 3 1 9 2.2 C#CCNc1ncnc2sc3c(=O)n(-c4ccc5c(c4)OCO5)cnc3c12 10.1016/j.bmcl.2009.04.104
136244237 73247 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Allosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assayAllosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assay
ChEMBL 288 3 2 4 3.4 Cc1c(-c2ccc(O)cc2)nsc1NC(=O)[C@@H]1C[C@H]1C 10.1016/j.bmcl.2012.02.003
CHEMBL2011880 73247 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Allosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assayAllosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assay
ChEMBL 288 3 2 4 3.4 Cc1c(-c2ccc(O)cc2)nsc1NC(=O)[C@@H]1C[C@H]1C 10.1016/j.bmcl.2012.02.003
71683128 91070 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 364 2 0 4 3.2 C[C@@H]1CN(c2cnccc2C#N)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
CHEMBL2397345 91070 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 364 2 0 4 3.2 C[C@@H]1CN(c2cnccc2C#N)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
11681681 85042 None 0 Human Functional pIC50 = 6.9 6.9 1 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 342 3 0 6 3.7 CN(C)c1ccnc2sc3c(=O)n(CC4CCCCC4)cnc3c12 10.1021/jm0504407
CHEMBL223868 85042 None 0 Human Functional pIC50 = 6.9 6.9 1 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 342 3 0 6 3.7 CN(C)c1ccnc2sc3c(=O)n(CC4CCCCC4)cnc3c12 10.1021/jm0504407
57559648 83859 None 0 Human Functional pIC50 = 7.9 7.9 707 2
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 407 3 0 8 3.4 CN(C)c1ncnc2sc3c(=O)n(-c4ccc(OC(F)(F)F)cc4)cnc3c12 10.1016/j.bmcl.2012.09.048
CHEMBL2205925 83859 None 0 Human Functional pIC50 = 7.9 7.9 707 2
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 407 3 0 8 3.4 CN(C)c1ncnc2sc3c(=O)n(-c4ccc(OC(F)(F)F)cc4)cnc3c12 10.1016/j.bmcl.2012.09.048
16118813 71002 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 369 3 0 6 3.8 COc1ccc(-n2ccc3c(sc4nccc(N(C)C)c43)c2=O)c(F)c1 10.1016/j.bmcl.2011.12.131
CHEMBL1951667 71002 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 369 3 0 6 3.8 COc1ccc(-n2ccc3c(sc4nccc(N(C)C)c43)c2=O)c(F)c1 10.1016/j.bmcl.2011.12.131
54584888 62772 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 427 4 1 7 4.1 C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784057 62772 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 427 4 1 7 4.1 C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
11493897 85097 None 0 Human Functional pIC50 = 6.9 6.9 1 3
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 342 2 0 6 3.8 CC1CCC(n2cnc3c(sc4nccc(N(C)C)c43)c2=O)CC1 10.1021/jm0504407
CHEMBL224315 85097 None 0 Human Functional pIC50 = 6.9 6.9 1 3
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 342 2 0 6 3.8 CC1CCC(n2cnc3c(sc4nccc(N(C)C)c43)c2=O)CC1 10.1021/jm0504407
75238115 124006 None 5 Human Functional pIC50 = 6.9 6.9 - 1
Negative allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisNegative allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
ChEMBL 369 3 1 4 3.1 CC1(C)C2C(=O)N(c3ccc(NC(=O)c4ccccn4)cc3Cl)C(=O)C21 10.1021/acs.jmedchem.5b00727
CHEMBL3628281 124006 None 5 Human Functional pIC50 = 6.9 6.9 - 1
Negative allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisNegative allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis
ChEMBL 369 3 1 4 3.1 CC1(C)C2C(=O)N(c3ccc(NC(=O)c4ccccn4)cc3Cl)C(=O)C21 10.1021/acs.jmedchem.5b00727
86711355 133109 None 0 Human Functional pIC50 = 5.9 5.9 -9 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 444 2 0 3 3.5 COc1cccc(C2=NCC(=O)N3CCc4c(I)cccc4C3=C2)c1 nan
CHEMBL3702382 133109 None 0 Human Functional pIC50 = 5.9 5.9 -9 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 444 2 0 3 3.5 COc1cccc(C2=NCC(=O)N3CCc4c(I)cccc4C3=C2)c1 nan
73335238 133111 None 0 Human Functional pIC50 = 5.9 5.9 -109 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 445 2 0 4 2.9 COc1cc(C2=NCC(=O)N3CCc4c(I)cccc4C3=C2)ccn1 nan
CHEMBL3702384 133111 None 0 Human Functional pIC50 = 5.9 5.9 -109 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 445 2 0 4 2.9 COc1cc(C2=NCC(=O)N3CCc4c(I)cccc4C3=C2)ccn1 nan
73335547 133142 None 0 Human Functional pIC50 = 5.9 5.9 -1 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 432 0 0 4 2.8 Cc1cn(C2=NCC(=O)N3CCc4c(I)cccc4C3=C2)c(C)n1 nan
CHEMBL3702415 133142 None 0 Human Functional pIC50 = 5.9 5.9 -1 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 432 0 0 4 2.8 Cc1cn(C2=NCC(=O)N3CCc4c(I)cccc4C3=C2)c(C)n1 nan
10714791 168400 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Inhibition of Quisqualate-Induced PI Hydrolysis measured in CHO Metabotropic glutamate receptor 1 Expressing CellsInhibition of Quisqualate-Induced PI Hydrolysis measured in CHO Metabotropic glutamate receptor 1 Expressing Cells
ChEMBL 380 5 2 6 1.9 COC(=O)[C@@H](Cc1ccccc1)NC(=O)C12CC1/C(=N\O)c1ccccc1O2 10.1021/jm0009944
CHEMBL434064 168400 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Inhibition of Quisqualate-Induced PI Hydrolysis measured in CHO Metabotropic glutamate receptor 1 Expressing CellsInhibition of Quisqualate-Induced PI Hydrolysis measured in CHO Metabotropic glutamate receptor 1 Expressing Cells
ChEMBL 380 5 2 6 1.9 COC(=O)[C@@H](Cc1ccccc1)NC(=O)C12CC1/C(=N\O)c1ccccc1O2 10.1021/jm0009944
71683128 91070 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 364 2 0 4 3.2 C[C@@H]1CN(c2cnccc2C#N)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
CHEMBL2397345 91070 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 364 2 0 4 3.2 C[C@@H]1CN(c2cnccc2C#N)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
76310874 105659 None 0 Human Functional pIC50 = 4.9 4.9 -3715 2
Negative allosteric modulation of human mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium flux after 16 to 24 hrs by FLIPR assayNegative allosteric modulation of human mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium flux after 16 to 24 hrs by FLIPR assay
ChEMBL 353 6 0 6 2.7 CCN(CC)C(=O)c1nn(C)c2nc(OCc3cccc(C)n3)ccc12 10.1021/jm401622k
CHEMBL3122223 105659 None 0 Human Functional pIC50 = 4.9 4.9 -3715 2
Negative allosteric modulation of human mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium flux after 16 to 24 hrs by FLIPR assayNegative allosteric modulation of human mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium flux after 16 to 24 hrs by FLIPR assay
ChEMBL 353 6 0 6 2.7 CCN(CC)C(=O)c1nn(C)c2nc(OCc3cccc(C)n3)ccc12 10.1021/jm401622k
44442431 1057 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay
ChEMBL 415 3 1 7 2.2 Clc1ccc(cc1)n1c(C)nc2c(c1=O)cnn2c1ccc(cc1)S(=O)(=O)N 10.1016/j.bmcl.2007.05.028
6342 1057 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay
ChEMBL 415 3 1 7 2.2 Clc1ccc(cc1)n1c(C)nc2c(c1=O)cnn2c1ccc(cc1)S(=O)(=O)N 10.1016/j.bmcl.2007.05.028
CHEMBL245990 1057 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay
ChEMBL 415 3 1 7 2.2 Clc1ccc(cc1)n1c(C)nc2c(c1=O)cnn2c1ccc(cc1)S(=O)(=O)N 10.1016/j.bmcl.2007.05.028
118735958 118973 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay
ChEMBL 377 4 2 5 3.5 Cc1cc(C(=O)N2CCc3c(sc(NCc4ccccc4)c3C#N)C2)[nH]n1 10.1016/j.ejmech.2015.04.060
CHEMBL3422874 118973 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay
ChEMBL 377 4 2 5 3.5 Cc1cc(C(=O)N2CCc3c(sc(NCc4ccccc4)c3C#N)C2)[nH]n1 10.1016/j.ejmech.2015.04.060
72163434 92063 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 365 3 0 3 3.6 O=C(CC12CC3CC(CC(C3)C1)C2)N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1 10.1016/j.bmcl.2013.07.029
CHEMBL2418374 92063 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 365 3 0 3 3.6 O=C(CC12CC3CC(CC(C3)C1)C2)N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1 10.1016/j.bmcl.2013.07.029
122196110 124311 None 0 Human Functional pIC50 = 6.8 6.8 13 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 394 4 1 5 3.8 COc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(F)c2C1=O 10.1016/j.bmcl.2015.10.013
CHEMBL3634432 124311 None 0 Human Functional pIC50 = 6.8 6.8 13 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 394 4 1 5 3.8 COc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(F)c2C1=O 10.1016/j.bmcl.2015.10.013
72163434 92063 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 365 3 0 3 3.6 O=C(CC12CC3CC(CC(C3)C1)C2)N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1 10.1016/j.bmcl.2013.07.029
CHEMBL2418374 92063 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 365 3 0 3 3.6 O=C(CC12CC3CC(CC(C3)C1)C2)N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1 10.1016/j.bmcl.2013.07.029
11652895 85102 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 334 3 0 6 3.2 CCc1ccc(-n2cnc3c(oc4nccc(N(C)C)c43)c2=O)cc1 10.1021/jm0504407
CHEMBL224377 85102 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 334 3 0 6 3.2 CCc1ccc(-n2cnc3c(oc4nccc(N(C)C)c43)c2=O)cc1 10.1021/jm0504407
127034284 139235 None 0 Rat Functional pIC50 = 6.8 6.8 15 2
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 319 2 1 5 3.7 c1ccn2nc3c(NC45CC6CC(CC(C6)C4)C5)ncnc3c2c1 10.1016/j.bmcl.2016.03.026
CHEMBL3787124 139235 None 0 Rat Functional pIC50 = 6.8 6.8 15 2
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 319 2 1 5 3.7 c1ccn2nc3c(NC45CC6CC(CC(C6)C4)C5)ncnc3c2c1 10.1016/j.bmcl.2016.03.026
127034284 139235 None 0 Rat Functional pIC50 = 6.8 6.8 15 2
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 319 2 1 5 3.7 c1ccn2nc3c(NC45CC6CC(CC(C6)C4)C5)ncnc3c2c1 10.1016/j.bmcl.2016.03.026
CHEMBL3787124 139235 None 0 Rat Functional pIC50 = 6.8 6.8 15 2
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 319 2 1 5 3.7 c1ccn2nc3c(NC45CC6CC(CC(C6)C4)C5)ncnc3c2c1 10.1016/j.bmcl.2016.03.026
73334761 125184 None 0 Human Functional pIC50 = 5.8 5.8 -18 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 385 2 0 7 2.0 O=C1CN=C(n2cnc(C3CC3)c2)C=C2c3cccc(-n4nccn4)c3CCN12 nan
CHEMBL3644413 125184 None 0 Human Functional pIC50 = 5.8 5.8 -18 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 385 2 0 7 2.0 O=C1CN=C(n2cnc(C3CC3)c2)C=C2c3cccc(-n4nccn4)c3CCN12 nan
57881945 83739 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 367 3 0 8 2.8 COc1ccc(-n2cnc3c(sc4ncnc(N(C)C)c43)c2=O)c(C)c1 10.1016/j.bmcl.2012.09.048
CHEMBL2205376 83739 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 367 3 0 8 2.8 COc1ccc(-n2cnc3c(sc4ncnc(N(C)C)c43)c2=O)c(C)c1 10.1016/j.bmcl.2012.09.048
16118536 71014 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 351 4 1 6 4.0 CCNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951681 71014 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 351 4 1 6 4.0 CCNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
16118816 71062 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 364 4 1 7 3.6 COc1ccc(-n2ccc3c(sc4ncnc(NC5CC5)c43)c2=O)cc1 10.1016/j.bmcl.2011.12.131
CHEMBL1951886 71062 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 364 4 1 7 3.6 COc1ccc(-n2ccc3c(sc4ncnc(NC5CC5)c43)c2=O)cc1 10.1016/j.bmcl.2011.12.131
16118942 71065 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 336 3 1 6 3.7 CCNc1ncnc2sc3c(=O)n(-c4ccc(C)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951889 71065 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 336 3 1 6 3.7 CCNc1ncnc2sc3c(=O)n(-c4ccc(C)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
73334942 133087 None 0 Human Functional pIC50 = 7.8 7.8 2 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 324 2 0 4 3.0 COc1cccc2c1CCN1C(=O)CN=C(c3cccs3)C=C21 nan
CHEMBL3702360 133087 None 0 Human Functional pIC50 = 7.8 7.8 2 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 324 2 0 4 3.0 COc1cccc2c1CCN1C(=O)CN=C(c3cccs3)C=C21 nan
73335337 133113 None 0 Human Functional pIC50 = 7.8 7.8 -1 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 446 2 0 4 3.3 CC(C)n1cc(C2=NCC(=O)N3CCc4c(I)cccc4C3=C2)cn1 nan
CHEMBL3702386 133113 None 0 Human Functional pIC50 = 7.8 7.8 -1 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 446 2 0 4 3.3 CC(C)n1cc(C2=NCC(=O)N3CCc4c(I)cccc4C3=C2)cn1 nan
122196125 124326 None 0 Human Functional pIC50 = 7.8 7.8 40 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 360 3 1 4 3.9 Cc1cc(N2C(=O)c3ccccc3C2=O)ccc1NC(=O)c1occc1C 10.1016/j.bmcl.2015.10.013
CHEMBL3634447 124326 None 0 Human Functional pIC50 = 7.8 7.8 40 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 360 3 1 4 3.9 Cc1cc(N2C(=O)c3ccccc3C2=O)ccc1NC(=O)c1occc1C 10.1016/j.bmcl.2015.10.013
44408491 141350 None 0 Rat Functional pIC50 = 7.8 7.8 - 1
Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method
ChEMBL 465 6 0 6 3.5 Cc1c(C(=O)OC(C)C(C)(C)C)cn2c1C(=O)N(CCCN1C(=O)c3ccccc3C1=O)CC2 10.1016/j.bmcl.2005.11.049
CHEMBL383107 141350 None 0 Rat Functional pIC50 = 7.8 7.8 - 1
Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method
ChEMBL 465 6 0 6 3.5 Cc1c(C(=O)OC(C)C(C)(C)C)cn2c1C(=O)N(CCCN1C(=O)c3ccccc3C1=O)CC2 10.1016/j.bmcl.2005.11.049
122196120 124321 None 0 Human Functional pIC50 = 7.8 7.8 26 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 410 3 1 4 5.1 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c2ccccc12 10.1016/j.bmcl.2015.10.013
CHEMBL3634442 124321 None 0 Human Functional pIC50 = 7.8 7.8 26 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 410 3 1 4 5.1 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c2ccccc12 10.1016/j.bmcl.2015.10.013
44588460 175653 None 0 Mouse Functional pIC50 = 6.8 6.8 -3 3
Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 327 2 0 6 2.7 CC(C)(C)OC(=O)N1CC=C(c2cn(-c3ccccn3)nn2)CC1 10.1016/j.bmc.2008.09.060
CHEMBL457872 175653 None 0 Mouse Functional pIC50 = 6.8 6.8 -3 3
Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 327 2 0 6 2.7 CC(C)(C)OC(=O)N1CC=C(c2cn(-c3ccccn3)nn2)CC1 10.1016/j.bmc.2008.09.060
73334941 133086 None 0 Human Functional pIC50 = 6.8 6.8 1 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 362 1 0 3 4.0 O=C1CN=C(c2cccs2)C=C2c3cccc(C(F)(F)F)c3CCN12 nan
CHEMBL3702359 133086 None 0 Human Functional pIC50 = 6.8 6.8 1 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 362 1 0 3 4.0 O=C1CN=C(c2cccs2)C=C2c3cccc(C(F)(F)F)c3CCN12 nan
45484850 200786 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL 307 2 0 6 3.6 Cc1nc2cc(-c3nnn(-c4cccnc4)c3C)ccc2s1 10.1016/j.bmcl.2009.07.145
CHEMBL576231 200786 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL 307 2 0 6 3.6 Cc1nc2cc(-c3nnn(-c4cccnc4)c3C)ccc2s1 10.1016/j.bmcl.2009.07.145
45486781 199692 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 325 4 0 5 3.5 COc1ccc(C(=O)N(C)c2nc(-c3ccncc3)cs2)cc1 10.1016/j.bmcl.2009.07.097
CHEMBL568321 199692 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 325 4 0 5 3.5 COc1ccc(C(=O)N(C)c2nc(-c3ccncc3)cs2)cc1 10.1016/j.bmcl.2009.07.097
45486816 201090 None 0 Human Functional pIC50 = 5.8 5.8 4 2
Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 314 3 0 5 3.0 CN(C(=O)c1ccc(F)cc1)c1nc(-c2cncnc2)cs1 10.1016/j.bmcl.2009.07.097
CHEMBL579011 201090 None 0 Human Functional pIC50 = 5.8 5.8 4 2
Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 314 3 0 5 3.0 CN(C(=O)c1ccc(F)cc1)c1nc(-c2cncnc2)cs1 10.1016/j.bmcl.2009.07.097
24777316 94770 None 0 Rat Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 331 1 0 4 3.7 CC1(C)CC(=O)c2cc(C#N)c(N3CCc4ccccc4C3)nc2C1 10.1021/jm0611298
CHEMBL252942 94770 None 0 Rat Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 331 1 0 4 3.7 CC1(C)CC(=O)c2cc(C#N)c(N3CCc4ccccc4C3)nc2C1 10.1021/jm0611298
86711404 125200 None 0 Human Functional pIC50 = 5.8 5.8 -758 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 362 2 1 5 2.5 CC(O)c1cn(C2=NCC(=O)N3CCc4c(cccc4C4CC4)C3=C2)cn1 nan
CHEMBL3644429 125200 None 0 Human Functional pIC50 = 5.8 5.8 -758 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 362 2 1 5 2.5 CC(O)c1cn(C2=NCC(=O)N3CCc4c(cccc4C4CC4)C3=C2)cn1 nan
89979743 133140 None 0 Human Functional pIC50 = 5.8 5.8 -7 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 434 1 1 5 1.7 O=C1CN=C(n2cnc(CO)c2)C=C2c3cccc(I)c3CCN12 nan
CHEMBL3702413 133140 None 0 Human Functional pIC50 = 5.8 5.8 -7 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 434 1 1 5 1.7 O=C1CN=C(n2cnc(CO)c2)C=C2c3cccc(I)c3CCN12 nan
91618209 133177 None 0 Human Functional pIC50 = 5.8 5.8 -151 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 336 3 1 4 2.7 CCCc1cccc2c1CCN1C(=O)CNC(n3cnc(C)c3)C=C21 nan
CHEMBL3702449 133177 None 0 Human Functional pIC50 = 5.8 5.8 -151 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 336 3 1 4 2.7 CCCc1cccc2c1CCN1C(=O)CNC(n3cnc(C)c3)C=C21 nan
89980574 133180 None 0 Human Functional pIC50 = 5.8 5.8 -501 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 363 3 0 6 2.0 COCc1ncn(C2=NCC(=O)N3CCc4c(cccc4C4CC4)C3=C2)n1 nan
CHEMBL3702452 133180 None 0 Human Functional pIC50 = 5.8 5.8 -501 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 363 3 0 6 2.0 COCc1ncn(C2=NCC(=O)N3CCc4c(cccc4C4CC4)C3=C2)n1 nan
10106002 78554 None 1 Human Functional pIC50 = 5.8 5.8 - 1
Inhibition of Quisqualate-Induced PI Hydrolysis measured in CHO Metabotropic glutamate receptor 1 Expressing CellsInhibition of Quisqualate-Induced PI Hydrolysis measured in CHO Metabotropic glutamate receptor 1 Expressing Cells
ChEMBL 247 2 1 5 1.6 CCOC(=O)[C@]12C[C@H]1/C(=N\O)c1ccccc1O2 10.1021/jm0009944
CHEMBL2111945 78554 None 1 Human Functional pIC50 = 5.8 5.8 - 1
Inhibition of Quisqualate-Induced PI Hydrolysis measured in CHO Metabotropic glutamate receptor 1 Expressing CellsInhibition of Quisqualate-Induced PI Hydrolysis measured in CHO Metabotropic glutamate receptor 1 Expressing Cells
ChEMBL 247 2 1 5 1.6 CCOC(=O)[C@]12C[C@H]1/C(=N\O)c1ccccc1O2 10.1021/jm0009944
24777817 167274 None 0 Rat Functional pIC50 = 4.8 4.8 - 1
Antagonist activity at rat mGluR1 by FLIPR assayAntagonist activity at rat mGluR1 by FLIPR assay
ChEMBL 435 3 0 5 4.5 CC1(C)CC(=O)c2cc(N3CCOCC3)c(N3CC=C(c4ccc(F)cc4)CC3)nc2C1 10.1021/jm0611298
CHEMBL429122 167274 None 0 Rat Functional pIC50 = 4.8 4.8 - 1
Antagonist activity at rat mGluR1 by FLIPR assayAntagonist activity at rat mGluR1 by FLIPR assay
ChEMBL 435 3 0 5 4.5 CC1(C)CC(=O)c2cc(N3CCOCC3)c(N3CC=C(c4ccc(F)cc4)CC3)nc2C1 10.1021/jm0611298
127032494 139043 None 0 Rat Functional pIC50 = 6.8 6.8 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 321 2 1 5 3.8 C[C@H]1[C@H](Nc2ncnc3c2nn2ccccc32)C[C@@H]2C[C@H]1C2(C)C 10.1016/j.bmcl.2016.03.026
CHEMBL3785139 139043 None 0 Rat Functional pIC50 = 6.8 6.8 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 321 2 1 5 3.8 C[C@H]1[C@H](Nc2ncnc3c2nn2ccccc32)C[C@@H]2C[C@H]1C2(C)C 10.1016/j.bmcl.2016.03.026
127032494 139043 None 0 Rat Functional pIC50 = 6.8 6.8 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 321 2 1 5 3.8 C[C@H]1[C@H](Nc2ncnc3c2nn2ccccc32)C[C@@H]2C[C@H]1C2(C)C 10.1016/j.bmcl.2016.03.026
CHEMBL3785139 139043 None 0 Rat Functional pIC50 = 6.8 6.8 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 321 2 1 5 3.8 C[C@H]1[C@H](Nc2ncnc3c2nn2ccccc32)C[C@@H]2C[C@H]1C2(C)C 10.1016/j.bmcl.2016.03.026
3342765 198232 None 9 Rat Functional pIC50 = 4.8 4.8 - 1
Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting
ChEMBL 302 4 0 2 5.3 Cc1ccc(C(=O)c2ccc(Oc3ccccc3)cc2)cc1C 10.1016/j.bmc.2009.05.072
CHEMBL557722 198232 None 9 Rat Functional pIC50 = 4.8 4.8 - 1
Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting
ChEMBL 302 4 0 2 5.3 Cc1ccc(C(=O)c2ccc(Oc3ccccc3)cc2)cc1C 10.1016/j.bmc.2009.05.072
57881822 83850 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 379 5 1 8 3.2 COc1ccc(-n2cnc3c(sc4ncnc(NCC5CC5)c43)c2=O)cc1 10.1016/j.bmcl.2012.09.048
CHEMBL2205916 83850 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 379 5 1 8 3.2 COc1ccc(-n2cnc3c(sc4ncnc(NCC5CC5)c43)c2=O)cc1 10.1016/j.bmcl.2012.09.048
122196106 124308 None 0 Human Functional pIC50 = 6.8 6.8 18 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 432 3 1 4 4.8 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(C(F)(F)F)c1 10.1016/j.bmcl.2015.10.013
CHEMBL3634429 124308 None 0 Human Functional pIC50 = 6.8 6.8 18 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 432 3 1 4 4.8 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(C(F)(F)F)c1 10.1016/j.bmcl.2015.10.013
67424813 89109 None 0 Human Functional pIC50 = 5.8 5.8 -25 2
Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay
ChEMBL 418 5 2 7 4.4 CNc1cccc(-c2c(-c3ccc4nn(C)cc4c3)nsc2NC(=O)[C@@H]2C[C@H]2C)n1 10.1016/j.bmcl.2013.01.009
CHEMBL2334978 89109 None 0 Human Functional pIC50 = 5.8 5.8 -25 2
Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay
ChEMBL 418 5 2 7 4.4 CNc1cccc(-c2c(-c3ccc4nn(C)cc4c3)nsc2NC(=O)[C@@H]2C[C@H]2C)n1 10.1016/j.bmcl.2013.01.009
CHEMBL2365133 89109 None 0 Human Functional pIC50 = 5.8 5.8 -25 2
Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay
ChEMBL 418 5 2 7 4.4 CNc1cccc(-c2c(-c3ccc4nn(C)cc4c3)nsc2NC(=O)[C@@H]2C[C@H]2C)n1 10.1016/j.bmcl.2013.01.009
46886135 7923 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 309 1 1 7 2.3 Cc1nc(N)c2c(n1)sc1c(=O)n(-c3ccccc3)cnc12 10.1016/j.bmcl.2010.03.004
CHEMBL1090247 7923 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 309 1 1 7 2.3 Cc1nc(N)c2c(n1)sc1c(=O)n(-c3ccccc3)cnc12 10.1016/j.bmcl.2010.03.004
54586818 62778 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 406 4 1 9 4.0 C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc5scnc5c4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784063 62778 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 406 4 1 9 4.0 C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc5scnc5c4)cnc3c12 10.1016/j.bmcl.2009.04.104
57559476 83860 None 0 Human Functional pIC50 = 7.8 7.8 630 2
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 391 2 0 7 3.5 CN(C)c1ncnc2sc3c(=O)n(-c4ccc(C(F)(F)F)cc4)cnc3c12 10.1016/j.bmcl.2012.09.048
CHEMBL2205926 83860 None 0 Human Functional pIC50 = 7.8 7.8 630 2
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 391 2 0 7 3.5 CN(C)c1ncnc2sc3c(=O)n(-c4ccc(C(F)(F)F)cc4)cnc3c12 10.1016/j.bmcl.2012.09.048
1069776 85256 None 8 Human Functional pIC50 = 7.8 7.8 1 3
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 356 2 0 6 3.7 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12 10.1021/jm0504407
CHEMBL225589 85256 None 8 Human Functional pIC50 = 7.8 7.8 1 3
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 356 2 0 6 3.7 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12 10.1021/jm0504407
44588425 176913 None 0 Human Functional pIC50 = 7.8 7.8 1 3
Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 344 2 0 5 3.4 CC(C)(C)OC(=O)N1CC=C(c2cn(-c3ccc(F)cc3)nn2)CC1 10.1016/j.bmc.2008.09.060
CHEMBL460827 176913 None 0 Human Functional pIC50 = 7.8 7.8 1 3
Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 344 2 0 5 3.4 CC(C)(C)OC(=O)N1CC=C(c2cn(-c3ccc(F)cc3)nn2)CC1 10.1016/j.bmc.2008.09.060
11716890 95051 None 16 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor
ChEMBL 328 2 2 5 3.5 Cc1c(C(=O)NC2CCCCC2)sc2nc3ccc(N)cc3n12 10.1021/jm060950g
CHEMBL1436386 95051 None 16 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor
ChEMBL 328 2 2 5 3.5 Cc1c(C(=O)NC2CCCCC2)sc2nc3ccc(N)cc3n12 10.1021/jm060950g
CHEMBL254777 95051 None 16 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor
ChEMBL 328 2 2 5 3.5 Cc1c(C(=O)NC2CCCCC2)sc2nc3ccc(N)cc3n12 10.1021/jm060950g
44588385 177000 None 0 Mouse Functional pIC50 = 7.8 7.8 -2 3
Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 344 2 0 5 3.4 CC(C)(C)OC(=O)N1CC=C(c2cn(-c3ccccc3F)nn2)CC1 10.1016/j.bmc.2008.09.060
CHEMBL461673 177000 None 0 Mouse Functional pIC50 = 7.8 7.8 -2 3
Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 344 2 0 5 3.4 CC(C)(C)OC(=O)N1CC=C(c2cn(-c3ccccc3F)nn2)CC1 10.1016/j.bmc.2008.09.060
1383 1449 None 0 Rat Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay
ChEMBL 309 5 1 4 3.8 CCCOC(=O)c1[nH]c(c(c1C)C(=O)O[C@H](C(C)(C)C)C)C 10.1016/j.bmcl.2007.01.055
44431042 1449 None 0 Rat Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay
ChEMBL 309 5 1 4 3.8 CCCOC(=O)c1[nH]c(c(c1C)C(=O)O[C@H](C(C)(C)C)C)C 10.1016/j.bmcl.2007.01.055
CHEMBL232052 1449 None 0 Rat Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay
ChEMBL 309 5 1 4 3.8 CCCOC(=O)c1[nH]c(c(c1C)C(=O)O[C@H](C(C)(C)C)C)C 10.1016/j.bmcl.2007.01.055
122196092 124294 None 0 Human Functional pIC50 = 7.8 7.8 21 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 360 3 1 4 3.9 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)cc1 10.1016/j.bmcl.2015.10.013
CHEMBL3634415 124294 None 0 Human Functional pIC50 = 7.8 7.8 21 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 360 3 1 4 3.9 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)cc1 10.1016/j.bmcl.2015.10.013
54585405 62684 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 362 4 1 6 4.3 C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1783868 62684 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 362 4 1 6 4.3 C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
16038352 90253 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay
ChEMBL 333 1 1 6 3.2 Cc1ccc(-n2cnc3c(sc4ncc5cn[nH]c5c43)c2=O)cc1 10.1021/jm070590c
CHEMBL238262 90253 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay
ChEMBL 333 1 1 6 3.2 Cc1ccc(-n2cnc3c(sc4ncc5cn[nH]c5c43)c2=O)cc1 10.1021/jm070590c
1381 581 None 25 Human Functional pIC50 = 6.8 6.8 -3 2
Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor
ChEMBL 278 2 0 2 3.9 C=C1C[C@H]2[C@](C1)(Cc1ccc3c(c1)cccc3)C(=O)OC2 10.1021/jm060950g
9903757 581 None 25 Human Functional pIC50 = 6.8 6.8 -3 2
Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor
ChEMBL 278 2 0 2 3.9 C=C1C[C@H]2[C@](C1)(Cc1ccc3c(c1)cccc3)C(=O)OC2 10.1021/jm060950g
CHEMBL254372 581 None 25 Human Functional pIC50 = 6.8 6.8 -3 2
Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor
ChEMBL 278 2 0 2 3.9 C=C1C[C@H]2[C@](C1)(Cc1ccc3c(c1)cccc3)C(=O)OC2 10.1021/jm060950g
44588429 176938 None 0 Mouse Functional pIC50 = 6.8 6.8 -1 2
Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 342 3 0 4 3.5 CC(C)(C)CC(=O)N1CC=C(c2cn(-c3ccccc3F)nn2)CC1 10.1016/j.bmc.2008.09.060
CHEMBL461035 176938 None 0 Mouse Functional pIC50 = 6.8 6.8 -1 2
Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 342 3 0 4 3.5 CC(C)(C)CC(=O)N1CC=C(c2cn(-c3ccccc3F)nn2)CC1 10.1016/j.bmc.2008.09.060
24777699 94876 None 0 Rat Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 378 2 0 5 3.6 CC1(C)CC(=O)c2cc(C#N)c(N3CCN(c4ccc(F)cc4)CC3)nc2C1 10.1021/jm0611298
CHEMBL253568 94876 None 0 Rat Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 378 2 0 5 3.6 CC1(C)CC(=O)c2cc(C#N)c(N3CCN(c4ccc(F)cc4)CC3)nc2C1 10.1021/jm0611298
44588427 176936 None 0 Mouse Functional pIC50 = 5.8 5.8 -2 3
Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 356 3 0 6 3.3 COc1ccccc1-n1cc(C2=CCN(C(=O)OC(C)(C)C)CC2)nn1 10.1016/j.bmc.2008.09.060
CHEMBL461033 176936 None 0 Mouse Functional pIC50 = 5.8 5.8 -2 3
Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 356 3 0 6 3.3 COc1ccccc1-n1cc(C2=CCN(C(=O)OC(C)(C)C)CC2)nn1 10.1016/j.bmc.2008.09.060
73335341 133117 None 0 Human Functional pIC50 = 5.8 5.8 -2 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 319 1 0 4 2.8 N#Cc1cccc2c1CCN1C(=O)CN=C(c3cccs3)C=C21 nan
CHEMBL3702390 133117 None 0 Human Functional pIC50 = 5.8 5.8 -2 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 319 1 0 4 2.8 N#Cc1cccc2c1CCN1C(=O)CN=C(c3cccs3)C=C21 nan
89980234 133137 None 0 Human Functional pIC50 = 5.8 5.8 -2 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 326 0 0 4 2.5 Cc1cn(C2=NCC(=O)N3CCc4c(Cl)cccc4C3=C2)cn1 nan
CHEMBL3702410 133137 None 0 Human Functional pIC50 = 5.8 5.8 -2 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 326 0 0 4 2.5 Cc1cn(C2=NCC(=O)N3CCc4c(Cl)cccc4C3=C2)cn1 nan
73335734 133160 None 0 Human Functional pIC50 = 5.8 5.8 -40 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 348 3 0 5 2.4 C=Cc1cccc2c1CCN1C(=O)CN=C(n3cnc(COC)c3)C=C21 nan
CHEMBL3702433 133160 None 0 Human Functional pIC50 = 5.8 5.8 -40 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 348 3 0 5 2.4 C=Cc1cccc2c1CCN1C(=O)CN=C(n3cnc(COC)c3)C=C21 nan
71682340 91074 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 339 2 0 3 3.3 C[C@@H]1CN(c2ccccn2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
CHEMBL2397349 91074 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 339 2 0 3 3.3 C[C@@H]1CN(c2ccccn2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
127030349 139114 None 0 Rat Functional pIC50 = 5.8 5.8 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 321 2 1 5 3.9 CC1(C)[C@@H]2CC[C@]1(C)[C@@H](Nc1ncnc3c1nn1ccccc31)C2 10.1016/j.bmcl.2016.03.026
CHEMBL3785862 139114 None 0 Rat Functional pIC50 = 5.8 5.8 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 321 2 1 5 3.9 CC1(C)[C@@H]2CC[C@]1(C)[C@@H](Nc1ncnc3c1nn1ccccc31)C2 10.1016/j.bmcl.2016.03.026
127034264 139123 None 0 Rat Functional pIC50 = 5.8 5.8 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 335 2 1 5 4.2 Cc1nc(N[C@H]2C[C@H]3CC[C@@]2(C)C3(C)C)c2nn3ccccc3c2n1 10.1016/j.bmcl.2016.03.026
CHEMBL3785977 139123 None 0 Rat Functional pIC50 = 5.8 5.8 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 335 2 1 5 4.2 Cc1nc(N[C@H]2C[C@H]3CC[C@@]2(C)C3(C)C)c2nn3ccccc3c2n1 10.1016/j.bmcl.2016.03.026
78324871 114400 None 4 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay
ChEMBL 338 2 0 4 4.8 O=c1c2scc(-c3ccccc3)c2ncn1-c1ccc(Cl)cc1 10.1016/j.ejmech.2014.08.027
CHEMBL3330805 114400 None 4 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay
ChEMBL 338 2 0 4 4.8 O=c1c2scc(-c3ccccc3)c2ncn1-c1ccc(Cl)cc1 10.1016/j.ejmech.2014.08.027
71682340 91074 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 339 2 0 3 3.3 C[C@@H]1CN(c2ccccn2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
CHEMBL2397349 91074 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 339 2 0 3 3.3 C[C@@H]1CN(c2ccccn2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
127030349 139114 None 0 Rat Functional pIC50 = 5.8 5.8 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 321 2 1 5 3.9 CC1(C)[C@@H]2CC[C@]1(C)[C@@H](Nc1ncnc3c1nn1ccccc31)C2 10.1016/j.bmcl.2016.03.026
CHEMBL3785862 139114 None 0 Rat Functional pIC50 = 5.8 5.8 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 321 2 1 5 3.9 CC1(C)[C@@H]2CC[C@]1(C)[C@@H](Nc1ncnc3c1nn1ccccc31)C2 10.1016/j.bmcl.2016.03.026
127034264 139123 None 0 Rat Functional pIC50 = 5.8 5.8 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 335 2 1 5 4.2 Cc1nc(N[C@H]2C[C@H]3CC[C@@]2(C)C3(C)C)c2nn3ccccc3c2n1 10.1016/j.bmcl.2016.03.026
CHEMBL3785977 139123 None 0 Rat Functional pIC50 = 5.8 5.8 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 335 2 1 5 4.2 Cc1nc(N[C@H]2C[C@H]3CC[C@@]2(C)C3(C)C)c2nn3ccccc3c2n1 10.1016/j.bmcl.2016.03.026
89979843 125173 None 0 Human Functional pIC50 = 5.8 5.8 -29 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 386 1 0 4 3.5 O=C1CN=C(n2cnc(C(F)(F)F)c2)C=C2c3cccc(C4CC4)c3CCN12 nan
CHEMBL3644402 125173 None 0 Human Functional pIC50 = 5.8 5.8 -29 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 386 1 0 4 3.5 O=C1CN=C(n2cnc(C(F)(F)F)c2)C=C2c3cccc(C4CC4)c3CCN12 nan
71682342 91076 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 339 2 0 3 3.3 C[C@@H]1CN(C(=O)C23CC4CC(CC(C4)C2)C3)CCN1c1ccccn1 10.1016/j.bmcl.2013.05.020
CHEMBL2397351 91076 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 339 2 0 3 3.3 C[C@@H]1CN(C(=O)C23CC4CC(CC(C4)C2)C3)CCN1c1ccccn1 10.1016/j.bmcl.2013.05.020
73355027 91079 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 327 2 0 3 3.3 C[C@@H]1CN(c2ccccn2)CCN1C(=O)C1CC2CCCC(C2)C1 10.1016/j.bmcl.2013.05.020
CHEMBL2397366 91079 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 327 2 0 3 3.3 C[C@@H]1CN(c2ccccn2)CCN1C(=O)C1CC2CCCC(C2)C1 10.1016/j.bmcl.2013.05.020
71682342 91076 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 339 2 0 3 3.3 C[C@@H]1CN(C(=O)C23CC4CC(CC(C4)C2)C3)CCN1c1ccccn1 10.1016/j.bmcl.2013.05.020
CHEMBL2397351 91076 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 339 2 0 3 3.3 C[C@@H]1CN(C(=O)C23CC4CC(CC(C4)C2)C3)CCN1c1ccccn1 10.1016/j.bmcl.2013.05.020
11666576 141815 None 0 Human Functional pIC50 = 6.8 6.8 1 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 300 2 0 6 2.8 CN(C)c1ccnc2sc3c(=O)n(C4CCC4)cnc3c12 10.1021/jm0504407
CHEMBL385776 141815 None 0 Human Functional pIC50 = 6.8 6.8 1 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 300 2 0 6 2.8 CN(C)c1ccnc2sc3c(=O)n(C4CCC4)cnc3c12 10.1021/jm0504407
11537767 141918 None 0 Human Functional pIC50 = 6.8 6.8 -5 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 359 2 0 7 2.6 C[N+](C)([O-])c1ccnc2sc3c(=O)n(N4CCCCCC4)cnc3c12 10.1021/jm0504407
CHEMBL386408 141918 None 0 Human Functional pIC50 = 6.8 6.8 -5 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 359 2 0 7 2.6 C[N+](C)([O-])c1ccnc2sc3c(=O)n(N4CCCCCC4)cnc3c12 10.1021/jm0504407
16739288 1033 None 0 Rat Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay
ChEMBL 306 3 2 2 3.3 Cc1cc2[nH]c3c(c2cc1OCc1ccccc1)CCNC3=O 10.1016/j.bmcl.2007.01.055
6358 1033 None 0 Rat Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay
ChEMBL 306 3 2 2 3.3 Cc1cc2[nH]c3c(c2cc1OCc1ccccc1)CCNC3=O 10.1016/j.bmcl.2007.01.055
CHEMBL396712 1033 None 0 Rat Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay
ChEMBL 306 3 2 2 3.3 Cc1cc2[nH]c3c(c2cc1OCc1ccccc1)CCNC3=O 10.1016/j.bmcl.2007.01.055
73355027 91079 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 327 2 0 3 3.3 C[C@@H]1CN(c2ccccn2)CCN1C(=O)C1CC2CCCC(C2)C1 10.1016/j.bmcl.2013.05.020
CHEMBL2397366 91079 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 327 2 0 3 3.3 C[C@@H]1CN(c2ccccn2)CCN1C(=O)C1CC2CCCC(C2)C1 10.1016/j.bmcl.2013.05.020
12988076 150358 None 0 Rat Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay
ChEMBL 294 3 2 3 2.7 O=C1NCCC2c3cc(OCc4ccccc4)ccc3NC12 10.1016/j.bmcl.2007.01.055
CHEMBL395256 150358 None 0 Rat Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay
ChEMBL 294 3 2 3 2.7 O=C1NCCC2c3cc(OCc4ccccc4)ccc3NC12 10.1016/j.bmcl.2007.01.055
54582944 62779 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 406 4 1 9 4.0 C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc5ncsc5c4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784064 62779 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 406 4 1 9 4.0 C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc5ncsc5c4)cnc3c12 10.1016/j.bmcl.2009.04.104
11688880 85099 None 0 Human Functional pIC50 = 7.8 7.8 1 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 350 2 0 6 3.7 Cc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)c(C)c1 10.1021/jm0504407
CHEMBL224356 85099 None 0 Human Functional pIC50 = 7.8 7.8 1 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 350 2 0 6 3.7 Cc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)c(C)c1 10.1021/jm0504407
16118539 71019 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 381 5 1 7 3.0 COc1ccc(-n2ccc3c(sc4nccc(N(C)CCO)c43)c2=O)cc1 10.1016/j.bmcl.2011.12.131
CHEMBL1951687 71019 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 381 5 1 7 3.0 COc1ccc(-n2ccc3c(sc4nccc(N(C)CCO)c43)c2=O)cc1 10.1016/j.bmcl.2011.12.131
45484897 201049 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL 292 4 0 5 3.2 CCC(=O)c1ccc(-c2nnn(-c3cccnc3)c2C)cc1 10.1016/j.bmcl.2009.07.145
CHEMBL578565 201049 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL 292 4 0 5 3.2 CCC(=O)c1ccc(-c2nnn(-c3cccnc3)c2C)cc1 10.1016/j.bmcl.2009.07.145
73335641 133150 None 0 Human Functional pIC50 = 6.8 6.8 -19 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 372 2 0 5 3.4 CCc1cn(C2=NCC(=O)N3CCc4c(cccc4-c4ccco4)C3=C2)cn1 nan
CHEMBL3702423 133150 None 0 Human Functional pIC50 = 6.8 6.8 -19 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 372 2 0 5 3.4 CCc1cn(C2=NCC(=O)N3CCc4c(cccc4-c4ccco4)C3=C2)cn1 nan
5766222 198368 None 11 Rat Functional pIC50 = 5.8 5.8 - 1
Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting
ChEMBL 307 3 0 2 5.1 Cc1ccc2nc(Cl)c(/C=C/C(=O)c3ccccc3)cc2c1 10.1016/j.bmc.2009.05.072
CHEMBL559243 198368 None 11 Rat Functional pIC50 = 5.8 5.8 - 1
Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting
ChEMBL 307 3 0 2 5.1 Cc1ccc2nc(Cl)c(/C=C/C(=O)c3ccccc3)cc2c1 10.1016/j.bmc.2009.05.072
24777696 94804 None 0 Rat Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 271 4 1 4 3.3 CCCCNc1nc2c(cc1C#N)C(=O)CC(C)(C)C2 10.1021/jm0611298
CHEMBL253143 94804 None 0 Rat Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 271 4 1 4 3.3 CCCCNc1nc2c(cc1C#N)C(=O)CC(C)(C)C2 10.1021/jm0611298
54582947 62795 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 374 3 1 6 4.1 C#CC(C)(C)Nc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784080 62795 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 374 3 1 6 4.1 C#CC(C)(C)Nc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
127034013 139179 None 0 Rat Functional pIC50 = 5.8 5.8 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 295 2 1 5 3.6 Cc1nc(N[C@H]2CC[C@H](C)CC2)c2nn3ccccc3c2n1 10.1016/j.bmcl.2016.03.026
CHEMBL3786560 139179 None 0 Rat Functional pIC50 = 5.8 5.8 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 295 2 1 5 3.6 Cc1nc(N[C@H]2CC[C@H](C)CC2)c2nn3ccccc3c2n1 10.1016/j.bmcl.2016.03.026
44588386 176866 None 0 Human Functional pIC50 = 7.8 7.8 2 3
Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 344 2 0 5 3.4 CC(C)(C)OC(=O)N1CC=C(c2cn(-c3cccc(F)c3)nn2)CC1 10.1016/j.bmc.2008.09.060
CHEMBL460391 176866 None 0 Human Functional pIC50 = 7.8 7.8 2 3
Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 344 2 0 5 3.4 CC(C)(C)OC(=O)N1CC=C(c2cn(-c3cccc(F)c3)nn2)CC1 10.1016/j.bmc.2008.09.060
16661728 199562 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 327 4 0 4 4.0 CCN(C(=O)c1ccc(F)cc1)c1nc(-c2ccccn2)cs1 10.1016/j.bmcl.2009.07.097
CHEMBL567668 199562 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 327 4 0 4 4.0 CCN(C(=O)c1ccc(F)cc1)c1nc(-c2ccccn2)cs1 10.1016/j.bmcl.2009.07.097
122196109 124142 None 0 Human Functional pIC50 = 7.7 7.7 36 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 410 4 1 5 4.3 COc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(Cl)c2C1=O 10.1016/j.bmcl.2015.10.013
CHEMBL3632642 124142 None 0 Human Functional pIC50 = 7.7 7.7 36 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 410 4 1 5 4.3 COc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(Cl)c2C1=O 10.1016/j.bmcl.2015.10.013
11530673 166208 None 0 Human Functional pIC50 = 6.8 6.8 1 3
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 364 4 0 6 4.0 CCCc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1 10.1021/jm0504407
CHEMBL426018 166208 None 0 Human Functional pIC50 = 6.8 6.8 1 3
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 364 4 0 6 4.0 CCCc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1 10.1021/jm0504407
44442429 154899 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay
ChEMBL 350 2 0 5 3.8 Cc1cccc(-n2ncc3c(=O)n(-c4ccc(Cl)cc4)c(C)nc32)c1 10.1016/j.bmcl.2007.05.028
CHEMBL400307 154899 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay
ChEMBL 350 2 0 5 3.8 Cc1cccc(-n2ncc3c(=O)n(-c4ccc(Cl)cc4)c(C)nc32)c1 10.1016/j.bmcl.2007.05.028
44588461 173670 None 0 Mouse Functional pIC50 = 6.8 6.8 -3 3
Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 327 2 0 6 2.7 CC(C)(C)OC(=O)N1CC=C(c2cn(-c3cccnc3)nn2)CC1 10.1016/j.bmc.2008.09.060
CHEMBL453249 173670 None 0 Mouse Functional pIC50 = 6.8 6.8 -3 3
Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 327 2 0 6 2.7 CC(C)(C)OC(=O)N1CC=C(c2cn(-c3cccnc3)nn2)CC1 10.1016/j.bmc.2008.09.060
11674352 175269 None 0 Mouse Functional pIC50 = 6.8 6.8 -4 3
Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 331 3 0 6 2.4 CC(C)OC(=O)N1CC=C(c2cn(-c3cccnc3F)nn2)CC1 10.1016/j.bmc.2008.09.060
CHEMBL457026 175269 None 0 Mouse Functional pIC50 = 6.8 6.8 -4 3
Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 331 3 0 6 2.4 CC(C)OC(=O)N1CC=C(c2cn(-c3cccnc3F)nn2)CC1 10.1016/j.bmc.2008.09.060
45484911 201384 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL 333 3 0 5 2.9 Cc1c(-c2ccc(C(=O)N3CCCC3)cc2)nnn1-c1cccnc1 10.1016/j.bmcl.2009.07.145
CHEMBL584610 201384 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL 333 3 0 5 2.9 Cc1c(-c2ccc(C(=O)N3CCCC3)cc2)nnn1-c1cccnc1 10.1016/j.bmcl.2009.07.145
91618212 125195 None 0 Human Functional pIC50 = 5.8 5.8 -177 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 385 2 0 6 3.1 O=C1CN=C(n2cnc(C3CC3)c2)C=C2c3cccc(-c4cocn4)c3CCN12 nan
CHEMBL3644424 125195 None 0 Human Functional pIC50 = 5.8 5.8 -177 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 385 2 0 6 3.1 O=C1CN=C(n2cnc(C3CC3)c2)C=C2c3cccc(-c4cocn4)c3CCN12 nan
127034013 139179 None 0 Rat Functional pIC50 = 5.8 5.8 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 295 2 1 5 3.6 Cc1nc(N[C@H]2CC[C@H](C)CC2)c2nn3ccccc3c2n1 10.1016/j.bmcl.2016.03.026
CHEMBL3786560 139179 None 0 Rat Functional pIC50 = 5.8 5.8 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 295 2 1 5 3.6 Cc1nc(N[C@H]2CC[C@H](C)CC2)c2nn3ccccc3c2n1 10.1016/j.bmcl.2016.03.026
44329032 112607 None 0 Human Functional pIC50 = 4.8 4.8 -177 5
Antagonistic activity against metabotropic glutamate receptor 1 (mGluR1) was evaluatedAntagonistic activity against metabotropic glutamate receptor 1 (mGluR1) 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 112607 None 0 Human Functional pIC50 = 4.8 4.8 -177 5
Antagonistic activity against metabotropic glutamate receptor 1 (mGluR1) was evaluatedAntagonistic activity against metabotropic glutamate receptor 1 (mGluR1) 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
118735971 118983 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay
ChEMBL 391 4 1 4 4.6 N#Cc1c(NCc2ccc(F)cc2)sc2c1CCN(C(=O)c1ccccc1)C2 10.1016/j.ejmech.2015.04.060
CHEMBL3422887 118983 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay
ChEMBL 391 4 1 4 4.6 N#Cc1c(NCc2ccc(F)cc2)sc2c1CCN(C(=O)c1ccccc1)C2 10.1016/j.ejmech.2015.04.060
89979990 133189 None 0 Human Functional pIC50 = 4.7 4.7 -83 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 413 2 0 5 3.6 O=C1CN=C(n2cnc(C3CC3)c2)C=C2c3cccc(-c4ccnc(F)c4)c3CCN12 nan
CHEMBL3702463 133189 None 0 Human Functional pIC50 = 4.7 4.7 -83 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 413 2 0 5 3.6 O=C1CN=C(n2cnc(C3CC3)c2)C=C2c3cccc(-c4ccnc(F)c4)c3CCN12 nan
11566478 85153 None 0 Human Functional pIC50 = 6.7 6.7 11 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 350 3 0 6 3.6 CCc1ccc(-n2cnc3c(sc4cncc(N(C)C)c43)c2=O)cc1 10.1021/jm0504407
CHEMBL224798 85153 None 0 Human Functional pIC50 = 6.7 6.7 11 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 350 3 0 6 3.6 CCc1ccc(-n2cnc3c(sc4cncc(N(C)C)c43)c2=O)cc1 10.1021/jm0504407
86729801 114402 None 4 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay
ChEMBL 318 2 0 4 4.4 Cc1cccc(-n2cnc3c(-c4ccccc4)csc3c2=O)c1 10.1016/j.ejmech.2014.08.027
CHEMBL3330807 114402 None 4 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay
ChEMBL 318 2 0 4 4.4 Cc1cccc(-n2cnc3c(-c4ccccc4)csc3c2=O)c1 10.1016/j.ejmech.2014.08.027
72163719 92068 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 375 2 0 3 3.7 N#Cc1ccccc1N1C[C@H]2CN(C(=O)C34CC5CC(CC(C5)C3)C4)C[C@H]2C1 10.1016/j.bmcl.2013.07.029
CHEMBL2418383 92068 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 375 2 0 3 3.7 N#Cc1ccccc1N1C[C@H]2CN(C(=O)C34CC5CC(CC(C5)C3)C4)C[C@H]2C1 10.1016/j.bmcl.2013.07.029
89980679 133174 None 0 Human Functional pIC50 = 5.7 5.7 -33 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 419 4 0 7 3.2 CCOCc1cn(C2=NCC(=O)N3CCc4c(cccc4-c4nccs4)C3=C2)cn1 nan
CHEMBL3702446 133174 None 0 Human Functional pIC50 = 5.7 5.7 -33 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 419 4 0 7 3.2 CCOCc1cn(C2=NCC(=O)N3CCc4c(cccc4-c4nccs4)C3=C2)cn1 nan
72163719 92068 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 375 2 0 3 3.7 N#Cc1ccccc1N1C[C@H]2CN(C(=O)C34CC5CC(CC(C5)C3)C4)C[C@H]2C1 10.1016/j.bmcl.2013.07.029
CHEMBL2418383 92068 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 375 2 0 3 3.7 N#Cc1ccccc1N1C[C@H]2CN(C(=O)C34CC5CC(CC(C5)C3)C4)C[C@H]2C1 10.1016/j.bmcl.2013.07.029
46886136 8232 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 339 2 1 8 2.3 COc1ccc(-n2cnc3c(sc4nc(C)nc(N)c43)c2=O)cc1 10.1016/j.bmcl.2010.03.004
CHEMBL1092275 8232 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 339 2 1 8 2.3 COc1ccc(-n2cnc3c(sc4nc(C)nc(N)c43)c2=O)cc1 10.1016/j.bmcl.2010.03.004
57881818 83737 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 383 4 1 8 3.1 COc1ccc(-n2cnc3c(sc4ncnc(NC5CC5)c43)c2=O)cc1F 10.1016/j.bmcl.2012.09.048
CHEMBL2205374 83737 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 383 4 1 8 3.1 COc1ccc(-n2cnc3c(sc4ncnc(NC5CC5)c43)c2=O)cc1F 10.1016/j.bmcl.2012.09.048
71455906 83845 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 367 5 1 8 3.2 CCCNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12 10.1016/j.bmcl.2012.09.048
CHEMBL2205910 83845 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 367 5 1 8 3.2 CCCNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12 10.1016/j.bmcl.2012.09.048
11702918 136929 None 0 Human Functional pIC50 = 7.7 7.7 42 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 343 2 0 7 3.4 CN(C)c1ccnc2sc3c(=O)n(C4CCCCCC4)nnc3c12 10.1021/jm0504407
CHEMBL374180 136929 None 0 Human Functional pIC50 = 7.7 7.7 42 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 343 2 0 7 3.4 CN(C)c1ccnc2sc3c(=O)n(C4CCCCCC4)nnc3c12 10.1021/jm0504407
122196122 124323 None 0 Human Functional pIC50 = 7.7 7.7 41 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 414 3 1 4 4.9 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c2ccccc12 10.1016/j.bmcl.2015.10.013
CHEMBL3634444 124323 None 0 Human Functional pIC50 = 7.7 7.7 41 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 414 3 1 4 4.9 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c2ccccc12 10.1016/j.bmcl.2015.10.013
44408468 75733 None 0 Rat Functional pIC50 = 7.7 7.7 - 1
Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method
ChEMBL 318 4 0 4 3.0 C=CCN1CCn2cc(C(=O)OC(C)C(C)(C)C)c(C)c2C1=O 10.1016/j.bmcl.2005.11.049
CHEMBL204802 75733 None 0 Rat Functional pIC50 = 7.7 7.7 - 1
Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method
ChEMBL 318 4 0 4 3.0 C=CCN1CCn2cc(C(=O)OC(C)C(C)(C)C)c(C)c2C1=O 10.1016/j.bmcl.2005.11.049
44408578 138603 None 0 Rat Functional pIC50 = 7.7 7.7 - 1
Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method
ChEMBL 324 4 0 4 2.8 Cc1c(C(=O)OC(C)C(C)(C)C)cn2c1C(=O)N(CCF)CC2 10.1016/j.bmcl.2005.11.049
CHEMBL377503 138603 None 0 Rat Functional pIC50 = 7.7 7.7 - 1
Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method
ChEMBL 324 4 0 4 2.8 Cc1c(C(=O)OC(C)C(C)(C)C)cn2c1C(=O)N(CCF)CC2 10.1016/j.bmcl.2005.11.049
44408599 170209 None 0 Rat Functional pIC50 = 7.7 7.7 - 1
Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method
ChEMBL 332 4 0 4 3.3 Cc1c(C(=O)OC(C)C(C)(C)C)cn2c1C(=O)N(CC1CC1)CC2 10.1016/j.bmcl.2005.11.049
CHEMBL444359 170209 None 0 Rat Functional pIC50 = 7.7 7.7 - 1
Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method
ChEMBL 332 4 0 4 3.3 Cc1c(C(=O)OC(C)C(C)(C)C)cn2c1C(=O)N(CC1CC1)CC2 10.1016/j.bmcl.2005.11.049
57908399 87552 None 0 Human Functional pIC50 = 6.7 6.7 -5 2
Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay
ChEMBL 419 5 1 7 4.4 COc1cccc(-c2c(-c3ccc4nn(C)cc4c3)nsc2NC(=O)[C@@H]2C[C@H]2C)n1 10.1016/j.bmcl.2013.01.009
CHEMBL2334977 87552 None 0 Human Functional pIC50 = 6.7 6.7 -5 2
Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay
ChEMBL 419 5 1 7 4.4 COc1cccc(-c2c(-c3ccc4nn(C)cc4c3)nsc2NC(=O)[C@@H]2C[C@H]2C)n1 10.1016/j.bmcl.2013.01.009
24777694 94769 None 0 Rat Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 331 2 1 4 3.7 CC1(C)CC(=O)c2cc(C#N)c(NC3Cc4ccccc4C3)nc2C1 10.1021/jm0611298
CHEMBL252941 94769 None 0 Rat Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 331 2 1 4 3.7 CC1(C)CC(=O)c2cc(C#N)c(NC3Cc4ccccc4C3)nc2C1 10.1021/jm0611298
1379 2420 None 35 Human Functional pIC50 = 4.7 4.7 - 1
Compound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysisCompound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysis
ChEMBL 209 3 3 3 0.8 OC(=O)c1ccc(c(c1)C)[C@@H](C(=O)O)N 10.1016/S0960-894X(97)10071-3
5311261 2420 None 35 Human Functional pIC50 = 4.7 4.7 - 1
Compound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysisCompound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysis
ChEMBL 209 3 3 3 0.8 OC(=O)c1ccc(c(c1)C)[C@@H](C(=O)O)N 10.1016/S0960-894X(97)10071-3
CHEMBL94631 2420 None 35 Human Functional pIC50 = 4.7 4.7 - 1
Compound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysisCompound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysis
ChEMBL 209 3 3 3 0.8 OC(=O)c1ccc(c(c1)C)[C@@H](C(=O)O)N 10.1016/S0960-894X(97)10071-3
73350719 92060 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 340 1 0 3 2.7 O=C(N1CC2CCCC(C2)C1)N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1 10.1016/j.bmcl.2013.07.029
CHEMBL2418363 92060 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 340 1 0 3 2.7 O=C(N1CC2CCCC(C2)C1)N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1 10.1016/j.bmcl.2013.07.029
73350719 92060 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 340 1 0 3 2.7 O=C(N1CC2CCCC(C2)C1)N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1 10.1016/j.bmcl.2013.07.029
CHEMBL2418363 92060 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 340 1 0 3 2.7 O=C(N1CC2CCCC(C2)C1)N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1 10.1016/j.bmcl.2013.07.029
89981446 125153 None 0 Human Functional pIC50 = 5.7 5.7 -83 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 414 2 0 7 3.2 Cc1nc(-c2cccc3c2CCN2C(=O)CN=C(n4cnc(C5CCC5)n4)C=C32)co1 nan
CHEMBL3644380 125153 None 0 Human Functional pIC50 = 5.7 5.7 -83 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 414 2 0 7 3.2 Cc1nc(-c2cccc3c2CCN2C(=O)CN=C(n4cnc(C5CCC5)n4)C=C32)co1 nan
57881851 83732 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 419 4 1 8 4.3 COc1ccc(-n2cnc3c(sc4ncnc(Nc5cccc(F)c5)c43)c2=O)cc1 10.1016/j.bmcl.2012.09.048
CHEMBL2205368 83732 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 419 4 1 8 4.3 COc1ccc(-n2cnc3c(sc4ncnc(Nc5cccc(F)c5)c43)c2=O)cc1 10.1016/j.bmcl.2012.09.048
57403925 71017 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 381 6 1 7 3.7 COCCNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951685 71017 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 381 6 1 7 3.7 COCCNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
73336124 133170 None 0 Human Functional pIC50 = 5.7 5.7 -19 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 396 2 0 6 2.9 O=C1CN=C(n2cnc(C3CC3)c2)C=C2c3cccc(-c4cnccn4)c3CCN12 nan
CHEMBL3702442 133170 None 0 Human Functional pIC50 = 5.7 5.7 -19 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 396 2 0 6 2.9 O=C1CN=C(n2cnc(C3CC3)c2)C=C2c3cccc(-c4cnccn4)c3CCN12 nan
54587386 62688 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 406 4 1 8 3.8 C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc5c(c4)OCCO5)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1783872 62688 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 406 4 1 8 3.8 C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc5c(c4)OCCO5)cnc3c12 10.1016/j.bmcl.2009.04.104
86729810 152631 None 0 Human Functional pIC50 = 5.7 5.7 - 1
FLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and diluteFLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and dilute
ChEMBL 378 3 0 7 3.9 COc1ccc(-n2cnc3c(-c4ccc5c(c4)OCO5)csc3c2=O)cc1 nan
CHEMBL3971614 152631 None 0 Human Functional pIC50 = 5.7 5.7 - 1
FLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and diluteFLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and dilute
ChEMBL 378 3 0 7 3.9 COc1ccc(-n2cnc3c(-c4ccc5c(c4)OCO5)csc3c2=O)cc1 nan
122196114 124315 None 0 Human Functional pIC50 = 6.7 6.7 17 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 365 3 1 5 3.2 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)nc1 10.1016/j.bmcl.2015.10.013
CHEMBL3634436 124315 None 0 Human Functional pIC50 = 6.7 6.7 17 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 365 3 1 5 3.2 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)nc1 10.1016/j.bmcl.2015.10.013
23634326 62674 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 364 5 1 7 3.6 C=CCNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1783858 62674 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 364 5 1 7 3.6 C=CCNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
57559313 83854 None 0 Human Functional pIC50 = 8.7 8.7 501 2
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 353 3 0 8 2.5 COc1ccc(-n2cnc3c(sc4ncnc(N(C)C)c43)c2=O)cc1 10.1016/j.bmcl.2012.09.048
CHEMBL2205920 83854 None 0 Human Functional pIC50 = 8.7 8.7 501 2
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 353 3 0 8 2.5 COc1ccc(-n2cnc3c(sc4ncnc(N(C)C)c43)c2=O)cc1 10.1016/j.bmcl.2012.09.048
16118540 71023 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 341 2 1 5 4.3 CNc1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951690 71023 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 341 2 1 5 4.3 CNc1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
16118685 71057 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 399 3 1 5 4.8 CCNc1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951881 71057 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 399 3 1 5 4.8 CCNc1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
23634102 977 None 2 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 362 4 1 7 3.0 C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)OC 10.1016/j.bmcl.2009.04.104
6215 977 None 2 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 362 4 1 7 3.0 C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)OC 10.1016/j.bmcl.2009.04.104
CHEMBL1783876 977 None 2 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 362 4 1 7 3.0 C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)OC 10.1016/j.bmcl.2009.04.104
46866191 1044 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 324 1 2 8 1.9 Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(N)nc(n1)N 10.1016/j.bmcl.2010.03.004
6209 1044 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 324 1 2 8 1.9 Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(N)nc(n1)N 10.1016/j.bmcl.2010.03.004
CHEMBL1093560 1044 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 324 1 2 8 1.9 Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(N)nc(n1)N 10.1016/j.bmcl.2010.03.004
16659803 1037 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay
ChEMBL 384 1 1 7 3.8 C[C@H]1CNc2c(O1)cnc1c2c2ncn(c(=O)c2s1)c1ccc(cc1)Cl 10.1021/jm070590c
6338 1037 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay
ChEMBL 384 1 1 7 3.8 C[C@H]1CNc2c(O1)cnc1c2c2ncn(c(=O)c2s1)c1ccc(cc1)Cl 10.1021/jm070590c
CHEMBL236180 1037 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay
ChEMBL 384 1 1 7 3.8 C[C@H]1CNc2c(O1)cnc1c2c2ncn(c(=O)c2s1)c1ccc(cc1)Cl 10.1021/jm070590c
16659966 88720 None 0 Human Functional pIC50 = 8.7 8.7 323 2
Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay
ChEMBL 350 1 1 7 3.1 Cc1ccc(-n2cnc3c(sc4ncc5c(c43)NCCO5)c2=O)cc1 10.1021/jm070590c
CHEMBL235975 88720 None 0 Human Functional pIC50 = 8.7 8.7 323 2
Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay
ChEMBL 350 1 1 7 3.1 Cc1ccc(-n2cnc3c(sc4ncc5c(c43)NCCO5)c2=O)cc1 10.1021/jm070590c
16118686 71058 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 411 3 1 5 4.9 O=c1c2sc3nccc(NC4CC4)c3c2ccn1-c1ccc(Br)cc1 10.1016/j.bmcl.2011.12.131
CHEMBL1951882 71058 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 411 3 1 5 4.9 O=c1c2sc3nccc(NC4CC4)c3c2ccn1-c1ccc(Br)cc1 10.1016/j.bmcl.2011.12.131
16660467 200951 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 329 3 1 6 2.6 CN(C(=O)c1ccc(F)cc1)c1nc(-c2cc(N)ncn2)cs1 10.1016/j.bmcl.2009.07.097
CHEMBL577729 200951 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 329 3 1 6 2.6 CN(C(=O)c1ccc(F)cc1)c1nc(-c2cc(N)ncn2)cs1 10.1016/j.bmcl.2009.07.097
23657393 88776 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay
ChEMBL 380 2 1 8 3.2 COc1ccc(-n2cnc3c(sc4ncc5c(c43)NC[C@@H](C)O5)c2=O)cc1 10.1021/jm070590c
CHEMBL236177 88776 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay
ChEMBL 380 2 1 8 3.2 COc1ccc(-n2cnc3c(sc4ncc5c(c43)NC[C@@H](C)O5)c2=O)cc1 10.1021/jm070590c
16659967 1035 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay
ChEMBL 366 2 1 8 2.8 COc1ccc(cc1)n1cnc2c(c1=O)sc1c2c2NCCOc2cn1 10.1021/jm070590c
6345 1035 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay
ChEMBL 366 2 1 8 2.8 COc1ccc(cc1)n1cnc2c(c1=O)sc1c2c2NCCOc2cn1 10.1021/jm070590c
CHEMBL393922 1035 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay
ChEMBL 366 2 1 8 2.8 COc1ccc(cc1)n1cnc2c(c1=O)sc1c2c2NCCOc2cn1 10.1021/jm070590c
44588463 173413 None 0 Human Functional pIC50 = 8.6 8.6 4 3
Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 345 2 0 6 2.8 CC(C)(C)OC(=O)N1CC=C(c2cn(-c3ncccc3F)nn2)CC1 10.1016/j.bmc.2008.09.060
CHEMBL452618 173413 None 0 Human Functional pIC50 = 8.6 8.6 4 3
Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 345 2 0 6 2.8 CC(C)(C)OC(=O)N1CC=C(c2cn(-c3ncccc3F)nn2)CC1 10.1016/j.bmc.2008.09.060
45484935 199315 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL 330 3 0 5 3.4 Cc1c(-c2ccc3c(c2)CC(C2CC2)C3=O)nnn1-c1cccnc1 10.1016/j.bmcl.2009.07.145
CHEMBL565943 199315 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL 330 3 0 5 3.4 Cc1c(-c2ccc3c(c2)CC(C2CC2)C3=O)nnn1-c1cccnc1 10.1016/j.bmcl.2009.07.145
16659801 1036 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay
ChEMBL 370 1 1 7 3.5 Clc1ccc(cc1)n1cnc2c(c1=O)sc1c2c2NCCOc2cn1 10.1021/jm070590c
6346 1036 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay
ChEMBL 370 1 1 7 3.5 Clc1ccc(cc1)n1cnc2c(c1=O)sc1c2c2NCCOc2cn1 10.1021/jm070590c
CHEMBL236994 1036 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay
ChEMBL 370 1 1 7 3.5 Clc1ccc(cc1)n1cnc2c(c1=O)sc1c2c2NCCOc2cn1 10.1021/jm070590c
57559504 83864 None 0 Human Functional pIC50 = 7.7 7.7 501 2
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 354 3 0 9 1.9 COc1ccc(-n2cnc3c(sc4ncnc(N(C)C)c43)c2=O)cn1 10.1016/j.bmcl.2012.09.048
CHEMBL2205930 83864 None 0 Human Functional pIC50 = 7.7 7.7 501 2
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 354 3 0 9 1.9 COc1ccc(-n2cnc3c(sc4ncnc(N(C)C)c43)c2=O)cn1 10.1016/j.bmcl.2012.09.048
699222 85126 None 8 Human Functional pIC50 = 7.7 7.7 1 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 322 2 0 6 3.1 CN(C)c1ccnc2sc3c(=O)n(-c4ccccc4)cnc3c12 10.1021/jm0504407
CHEMBL224615 85126 None 8 Human Functional pIC50 = 7.7 7.7 1 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 322 2 0 6 3.1 CN(C)c1ccnc2sc3c(=O)n(-c4ccccc4)cnc3c12 10.1021/jm0504407
122196119 124320 None 0 Human Functional pIC50 = 7.7 7.7 17 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 396 3 1 4 4.8 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c2ccccc12 10.1016/j.bmcl.2015.10.013
CHEMBL3634441 124320 None 0 Human Functional pIC50 = 7.7 7.7 17 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 396 3 1 4 4.8 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c2ccccc12 10.1016/j.bmcl.2015.10.013
45486758 200270 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 341 4 0 4 4.4 CC(C)N(C(=O)c1ccc(F)cc1)c1nc(-c2ccccn2)cs1 10.1016/j.bmcl.2009.07.097
CHEMBL572144 200270 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 341 4 0 4 4.4 CC(C)N(C(=O)c1ccc(F)cc1)c1nc(-c2ccccn2)cs1 10.1016/j.bmcl.2009.07.097
57391670 71049 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 332 2 1 6 3.5 CNc1ccnc2sc3c(=O)n(-c4ccc(C#N)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951873 71049 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 332 2 1 6 3.5 CNc1ccnc2sc3c(=O)n(-c4ccc(C#N)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
118735962 118976 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay
ChEMBL 381 4 2 5 3.3 N#Cc1c(NCc2ccc(F)cc2)sc2c1CCN(C(=O)c1ccn[nH]1)C2 10.1016/j.ejmech.2015.04.060
CHEMBL3422878 118976 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay
ChEMBL 381 4 2 5 3.3 N#Cc1c(NCc2ccc(F)cc2)sc2c1CCN(C(=O)c1ccn[nH]1)C2 10.1016/j.ejmech.2015.04.060
57559552 83863 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 324 2 0 8 1.9 CN(C)c1ncnc2sc3c(=O)n(-c4cccnc4)cnc3c12 10.1016/j.bmcl.2012.09.048
CHEMBL2205929 83863 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 324 2 0 8 1.9 CN(C)c1ncnc2sc3c(=O)n(-c4cccnc4)cnc3c12 10.1016/j.bmcl.2012.09.048
5766223 198106 None 18 Rat Functional pIC50 = 4.7 4.7 - 1
Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting
ChEMBL 337 4 0 3 5.1 COc1ccc(C(=O)/C=C/c2cc3cc(C)ccc3nc2Cl)cc1 10.1016/j.bmc.2009.05.072
CHEMBL556430 198106 None 18 Rat Functional pIC50 = 4.7 4.7 - 1
Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting
ChEMBL 337 4 0 3 5.1 COc1ccc(C(=O)/C=C/c2cc3cc(C)ccc3nc2Cl)cc1 10.1016/j.bmc.2009.05.072
86627336 122267 None 2 Rat Functional pIC50 = 6.7 6.7 -524 2
Negative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysisNegative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysis
ChEMBL 320 2 0 5 3.0 O=[N+]([O-])c1cccnc1N1CCC(=CC#Cc2ccccn2)CC1 10.1016/j.bmc.2015.05.008
CHEMBL3597593 122267 None 2 Rat Functional pIC50 = 6.7 6.7 -524 2
Negative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysisNegative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysis
ChEMBL 320 2 0 5 3.0 O=[N+]([O-])c1cccnc1N1CCC(=CC#Cc2ccccn2)CC1 10.1016/j.bmc.2015.05.008
86711408 125179 None 0 Human Functional pIC50 = 5.7 5.7 -33 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 376 2 0 6 2.2 COC(=O)c1cccc2c1CCN1C(=O)CN=C(n3cnc(C4CC4)c3)C=C21 nan
CHEMBL3644408 125179 None 0 Human Functional pIC50 = 5.7 5.7 -33 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 376 2 0 6 2.2 COC(=O)c1cccc2c1CCN1C(=O)CN=C(n3cnc(C4CC4)c3)C=C21 nan
89980392 125136 None 0 Human Functional pIC50 = 5.7 5.7 -346 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 394 3 0 5 3.3 CO[C@H](C)c1cn(C2=NCC(=O)N3CCc4c(ccc(F)c4C4CC4)C3=C2)cn1 nan
CHEMBL3644363 125136 None 0 Human Functional pIC50 = 5.7 5.7 -346 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 394 3 0 5 3.3 CO[C@H](C)c1cn(C2=NCC(=O)N3CCc4c(ccc(F)c4C4CC4)C3=C2)cn1 nan
122196117 124318 None 0 Human Functional pIC50 = 6.7 6.7 12 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 382 3 1 6 3.1 Cc1ccoc1C(=O)Nc1cnc(N2C(=O)c3cccc(Cl)c3C2=O)nc1 10.1016/j.bmcl.2015.10.013
CHEMBL3634439 124318 None 0 Human Functional pIC50 = 6.7 6.7 12 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 382 3 1 6 3.1 Cc1ccoc1C(=O)Nc1cnc(N2C(=O)c3cccc(Cl)c3C2=O)nc1 10.1016/j.bmcl.2015.10.013
54582946 62791 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 390 3 1 9 3.0 C#CCNc1ncnc2sc3c(=O)n(-c4ccc5ncsc5c4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784076 62791 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 390 3 1 9 3.0 C#CCNc1ncnc2sc3c(=O)n(-c4ccc5ncsc5c4)cnc3c12 10.1016/j.bmcl.2009.04.104
49788727 18323 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiologyAntagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiology
ChEMBL 465 17 5 5 2.8 NCCCNCCCCNCCCNC(=O)[C@H](CC1CCCCC1)NC(=O)C1CCCCC1 10.1021/jm100886h
CHEMBL1270719 18323 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiologyAntagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiology
ChEMBL 465 17 5 5 2.8 NCCCNCCCCNCCCNC(=O)[C@H](CC1CCCCC1)NC(=O)C1CCCCC1 10.1021/jm100886h
54583943 62792 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 373 3 1 8 3.2 C#CCNc1ncnc2sc3c(=O)n(-c4ccc5occc5c4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784077 62792 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 373 3 1 8 3.2 C#CCNc1ncnc2sc3c(=O)n(-c4ccc5occc5c4)cnc3c12 10.1016/j.bmcl.2009.04.104
11688952 80870 None 0 Rat Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at rat mGluR1 expressed in 1321N1 cellsAntagonist activity at rat mGluR1 expressed in 1321N1 cells
ChEMBL 354 2 0 6 3.5 Cc1ccc(-n2cnc3c(sc4cncc(N(C)C)c43)c2=O)cc1F 10.1016/j.bmcl.2006.06.053
CHEMBL215240 80870 None 0 Rat Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at rat mGluR1 expressed in 1321N1 cellsAntagonist activity at rat mGluR1 expressed in 1321N1 cells
ChEMBL 354 2 0 6 3.5 Cc1ccc(-n2cnc3c(sc4cncc(N(C)C)c43)c2=O)cc1F 10.1016/j.bmcl.2006.06.053
122196100 124302 None 0 Human Functional pIC50 = 7.7 7.7 19 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 374 3 1 4 4.3 Cc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(C)c2C1=O 10.1016/j.bmcl.2015.10.013
CHEMBL3634423 124302 None 0 Human Functional pIC50 = 7.7 7.7 19 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 374 3 1 4 4.3 Cc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(C)c2C1=O 10.1016/j.bmcl.2015.10.013
45484880 199316 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL 321 4 1 5 2.8 Cc1c(-c2ccc(C(=O)NC(C)C)cc2)nnn1-c1cccnc1 10.1016/j.bmcl.2009.07.145
CHEMBL565948 199316 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL 321 4 1 5 2.8 Cc1c(-c2ccc(C(=O)NC(C)C)cc2)nnn1-c1cccnc1 10.1016/j.bmcl.2009.07.145
45486764 199311 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 373 3 0 4 4.2 CN(C(=O)c1ccc(Br)cc1)c1nc(-c2ccncc2)cs1 10.1016/j.bmcl.2009.07.097
CHEMBL565934 199311 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 373 3 0 4 4.2 CN(C(=O)c1ccc(Br)cc1)c1nc(-c2ccncc2)cs1 10.1016/j.bmcl.2009.07.097
73334944 133089 None 0 Human Functional pIC50 = 6.7 6.7 -8 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 322 2 0 4 2.8 COc1cccc2c1CCN1C(=O)CN=C(c3ccc(C)o3)C=C21 nan
CHEMBL3702362 133089 None 0 Human Functional pIC50 = 6.7 6.7 -8 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 322 2 0 4 2.8 COc1cccc2c1CCN1C(=O)CN=C(c3ccc(C)o3)C=C21 nan
71561201 87876 None 0 Rat Functional pIC50 = 5.7 5.7 -35 2
Antagonist activity at rat mGluR1 expressed in HEK293 cells assessed as inhibition of Ca2+ mobilization by FLIPR assayAntagonist activity at rat mGluR1 expressed in HEK293 cells assessed as inhibition of Ca2+ mobilization by FLIPR assay
ChEMBL 374 4 2 2 4.0 O=C(N[C@@H]1CCC[C@@H](NC(=O)c2cccc(Cl)c2)C1)c1cccc(F)c1 10.1016/j.bmcl.2012.12.078
CHEMBL2338567 87876 None 0 Rat Functional pIC50 = 5.7 5.7 -35 2
Antagonist activity at rat mGluR1 expressed in HEK293 cells assessed as inhibition of Ca2+ mobilization by FLIPR assayAntagonist activity at rat mGluR1 expressed in HEK293 cells assessed as inhibition of Ca2+ mobilization by FLIPR assay
ChEMBL 374 4 2 2 4.0 O=C(N[C@@H]1CCC[C@@H](NC(=O)c2cccc(Cl)c2)C1)c1cccc(F)c1 10.1016/j.bmcl.2012.12.078
24777815 94996 None 0 Rat Functional pIC50 = 4.7 4.7 2 2
Antagonist activity at rat mGluR1 by FLIPR assayAntagonist activity at rat mGluR1 by FLIPR assay
ChEMBL 329 3 1 4 3.3 CN(C)C(=O)c1cc2c(nc1NC1CCCC1)CC(C)(C)CC2=O 10.1021/jm0611298
CHEMBL254429 94996 None 0 Rat Functional pIC50 = 4.7 4.7 2 2
Antagonist activity at rat mGluR1 by FLIPR assayAntagonist activity at rat mGluR1 by FLIPR assay
ChEMBL 329 3 1 4 3.3 CN(C)C(=O)c1cc2c(nc1NC1CCCC1)CC(C)(C)CC2=O 10.1021/jm0611298
11323495 94738 None 0 Rat Functional pIC50 = 4.7 4.7 -1 2
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 281 3 0 3 3.8 CC1(C)CC(=O)c2ccc(OCc3ccccc3)nc2C1 10.1021/jm0611298
CHEMBL1204390 94738 None 0 Rat Functional pIC50 = 4.7 4.7 -1 2
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 281 3 0 3 3.8 CC1(C)CC(=O)c2ccc(OCc3ccccc3)nc2C1 10.1021/jm0611298
CHEMBL252734 94738 None 0 Rat Functional pIC50 = 4.7 4.7 -1 2
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 281 3 0 3 3.8 CC1(C)CC(=O)c2ccc(OCc3ccccc3)nc2C1 10.1021/jm0611298
54585852 62786 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 381 4 1 8 2.6 C#CCNc1ncnc2sc3c(=O)n(-c4ccc(OC)c(F)c4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784071 62786 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 381 4 1 8 2.6 C#CCNc1ncnc2sc3c(=O)n(-c4ccc(OC)c(F)c4)cnc3c12 10.1016/j.bmcl.2009.04.104
127031562 139139 None 0 Rat Functional pIC50 = 5.7 5.7 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 334 2 2 6 3.1 Nc1nc(NC2C3CC4CC(C3)CC2C4)c2nn3ccccc3c2n1 10.1016/j.bmcl.2016.03.026
CHEMBL3786157 139139 None 0 Rat Functional pIC50 = 5.7 5.7 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 334 2 2 6 3.1 Nc1nc(NC2C3CC4CC(C3)CC2C4)c2nn3ccccc3c2n1 10.1016/j.bmcl.2016.03.026
127031562 139139 None 0 Rat Functional pIC50 = 5.7 5.7 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 334 2 2 6 3.1 Nc1nc(NC2C3CC4CC(C3)CC2C4)c2nn3ccccc3c2n1 10.1016/j.bmcl.2016.03.026
CHEMBL3786157 139139 None 0 Rat Functional pIC50 = 5.7 5.7 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 334 2 2 6 3.1 Nc1nc(NC2C3CC4CC(C3)CC2C4)c2nn3ccccc3c2n1 10.1016/j.bmcl.2016.03.026
54579959 62793 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 389 3 1 8 3.7 C#CCNc1ncnc2sc3c(=O)n(-c4ccc5sccc5c4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784078 62793 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 389 3 1 8 3.7 C#CCNc1ncnc2sc3c(=O)n(-c4ccc5sccc5c4)cnc3c12 10.1016/j.bmcl.2009.04.104
45484920 199744 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL 304 4 0 5 3.2 Cc1c(-c2ccc(C(=O)C3CC3)cc2)nnn1-c1cccnc1 10.1016/j.bmcl.2009.07.145
CHEMBL568648 199744 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL 304 4 0 5 3.2 Cc1c(-c2ccc(C(=O)C3CC3)cc2)nnn1-c1cccnc1 10.1016/j.bmcl.2009.07.145
73335340 133116 None 0 Human Functional pIC50 = 7.7 7.7 2 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 318 1 0 3 3.0 C#Cc1cccc2c1CCN1C(=O)CN=C(c3cccs3)C=C21 nan
CHEMBL3702389 133116 None 0 Human Functional pIC50 = 7.7 7.7 2 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 318 1 0 3 3.0 C#Cc1cccc2c1CCN1C(=O)CN=C(c3cccs3)C=C21 nan
122196095 124297 None 0 Human Functional pIC50 = 7.7 7.7 12 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 364 3 1 4 3.8 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(F)c1 10.1016/j.bmcl.2015.10.013
CHEMBL3634418 124297 None 0 Human Functional pIC50 = 7.7 7.7 12 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 364 3 1 4 3.8 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(F)c1 10.1016/j.bmcl.2015.10.013
122196121 124322 None 0 Human Functional pIC50 = 7.7 7.7 22 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 430 3 1 4 5.4 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c2ccccc12 10.1016/j.bmcl.2015.10.013
CHEMBL3634443 124322 None 0 Human Functional pIC50 = 7.7 7.7 22 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 430 3 1 4 5.4 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c2ccccc12 10.1016/j.bmcl.2015.10.013
44588462 175655 None 0 Human Functional pIC50 = 6.7 6.7 4 2
Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 327 2 0 6 2.7 CC(C)(C)OC(=O)N1CC=C(c2cn(-c3ccncc3)nn2)CC1 10.1016/j.bmc.2008.09.060
CHEMBL457873 175655 None 0 Human Functional pIC50 = 6.7 6.7 4 2
Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 327 2 0 6 2.7 CC(C)(C)OC(=O)N1CC=C(c2cn(-c3ccncc3)nn2)CC1 10.1016/j.bmc.2008.09.060
44442430 154714 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay
ChEMBL 370 2 0 5 4.2 Cc1nc2c(cnn2-c2cccc(Cl)c2)c(=O)n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2007.05.028
CHEMBL399309 154714 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay
ChEMBL 370 2 0 5 4.2 Cc1nc2c(cnn2-c2cccc(Cl)c2)c(=O)n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2007.05.028
73335826 133178 None 0 Human Functional pIC50 = 6.7 6.7 -24 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 376 3 0 5 3.0 COCc1cn(C2=NCC(=O)N3CCc4c(cccc4C4CCC4)C3=C2)cn1 nan
CHEMBL3702450 133178 None 0 Human Functional pIC50 = 6.7 6.7 -24 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 376 3 0 5 3.0 COCc1cn(C2=NCC(=O)N3CCc4c(cccc4C4CCC4)C3=C2)cn1 nan
73334852 125187 None 0 Human Functional pIC50 = 5.7 5.7 -23 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 348 3 0 4 2.9 COc1cccc(C2=NCC(=O)N3CCc4c(OC)cccc4C3=C2)c1 nan
CHEMBL3644416 125187 None 0 Human Functional pIC50 = 5.7 5.7 -23 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 348 3 0 4 2.9 COc1cccc(C2=NCC(=O)N3CCc4c(OC)cccc4C3=C2)c1 nan
89979353 133124 None 0 Human Functional pIC50 = 5.7 5.7 -8 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 322 2 1 5 1.1 Cn1cc(C2=NCC(=O)N3CCc4c(CO)cccc4C3=C2)cn1 nan
CHEMBL3702397 133124 None 0 Human Functional pIC50 = 5.7 5.7 -8 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 322 2 1 5 1.1 Cn1cc(C2=NCC(=O)N3CCc4c(CO)cccc4C3=C2)cn1 nan
78321442 114408 None 4 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay
ChEMBL 368 3 0 5 4.8 COc1ccc(-n2cnc3c(-c4ccccc4Cl)csc3c2=O)cc1 10.1016/j.ejmech.2014.08.027
CHEMBL3330820 114408 None 4 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay
ChEMBL 368 3 0 5 4.8 COc1ccc(-n2cnc3c(-c4ccccc4Cl)csc3c2=O)cc1 10.1016/j.ejmech.2014.08.027
78322062 114410 None 4 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay
ChEMBL 348 3 0 5 4.4 COc1ccc(-n2cnc3c(-c4cccc(C)c4)csc3c2=O)cc1 10.1016/j.ejmech.2014.08.027
CHEMBL3330824 114410 None 4 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay
ChEMBL 348 3 0 5 4.4 COc1ccc(-n2cnc3c(-c4cccc(C)c4)csc3c2=O)cc1 10.1016/j.ejmech.2014.08.027
67425734 89121 None 0 Human Functional pIC50 = 5.7 5.7 -48 2
Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay
ChEMBL 403 4 1 6 4.7 Cc1cccc(-c2c(-c3ccc4nn(C)cc4c3)nsc2NC(=O)[C@@H]2C[C@H]2C)n1 10.1016/j.bmcl.2013.01.009
CHEMBL2334973 89121 None 0 Human Functional pIC50 = 5.7 5.7 -48 2
Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay
ChEMBL 403 4 1 6 4.7 Cc1cccc(-c2c(-c3ccc4nn(C)cc4c3)nsc2NC(=O)[C@@H]2C[C@H]2C)n1 10.1016/j.bmcl.2013.01.009
CHEMBL2365251 89121 None 0 Human Functional pIC50 = 5.7 5.7 -48 2
Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay
ChEMBL 403 4 1 6 4.7 Cc1cccc(-c2c(-c3ccc4nn(C)cc4c3)nsc2NC(=O)[C@@H]2C[C@H]2C)n1 10.1016/j.bmcl.2013.01.009
127033450 139276 None 0 Rat Functional pIC50 = 6.7 6.7 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 281 2 1 5 3.4 c1ccn2nc3c(NC4CCCCCC4)ncnc3c2c1 10.1016/j.bmcl.2016.03.026
CHEMBL3787631 139276 None 0 Rat Functional pIC50 = 6.7 6.7 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 281 2 1 5 3.4 c1ccn2nc3c(NC4CCCCCC4)ncnc3c2c1 10.1016/j.bmcl.2016.03.026
127031256 139099 None 0 Rat Functional pIC50 = 5.7 5.7 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 295 3 1 5 3.7 C[C@H](Nc1ncnc2c1nn1ccccc21)C1CCCCC1 10.1016/j.bmcl.2016.03.026
CHEMBL3785675 139099 None 0 Rat Functional pIC50 = 5.7 5.7 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 295 3 1 5 3.7 C[C@H](Nc1ncnc2c1nn1ccccc21)C1CCCCC1 10.1016/j.bmcl.2016.03.026
127031256 139099 None 0 Rat Functional pIC50 = 5.7 5.7 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 295 3 1 5 3.7 C[C@H](Nc1ncnc2c1nn1ccccc21)C1CCCCC1 10.1016/j.bmcl.2016.03.026
CHEMBL3785675 139099 None 0 Rat Functional pIC50 = 5.7 5.7 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 295 3 1 5 3.7 C[C@H](Nc1ncnc2c1nn1ccccc21)C1CCCCC1 10.1016/j.bmcl.2016.03.026
127033450 139276 None 0 Rat Functional pIC50 = 6.7 6.7 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 281 2 1 5 3.4 c1ccn2nc3c(NC4CCCCCC4)ncnc3c2c1 10.1016/j.bmcl.2016.03.026
CHEMBL3787631 139276 None 0 Rat Functional pIC50 = 6.7 6.7 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 281 2 1 5 3.4 c1ccn2nc3c(NC4CCCCCC4)ncnc3c2c1 10.1016/j.bmcl.2016.03.026
3951963 199046 None 1 Rat Functional pIC50 = 4.7 4.7 - 1
Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting
ChEMBL 379 8 0 3 6.6 CCCCCc1ccc(-c2ccc(OC(=O)C3CCC(CC)CC3)cc2)nc1 10.1016/j.bmc.2009.05.072
CHEMBL564000 199046 None 1 Rat Functional pIC50 = 4.7 4.7 - 1
Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting
ChEMBL 379 8 0 3 6.6 CCCCCc1ccc(-c2ccc(OC(=O)C3CCC(CC)CC3)cc2)nc1 10.1016/j.bmc.2009.05.072
44431047 92404 None 0 Rat Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay
ChEMBL 323 2 3 2 2.4 O=C(NC1CC2CCC1C2)c1ccc2[nH]c3c(c2c1)CCNC3=O 10.1016/j.bmcl.2007.01.055
CHEMBL243020 92404 None 0 Rat Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay
ChEMBL 323 2 3 2 2.4 O=C(NC1CC2CCC1C2)c1ccc2[nH]c3c(c2c1)CCNC3=O 10.1016/j.bmcl.2007.01.055
89979891 125171 None 0 Human Functional pIC50 = 6.7 6.7 -28 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 359 2 0 5 2.7 O=C1CN=C(n2cnc(C3CC3)n2)C=C2c3cccc(C4CC4)c3CCN12 nan
CHEMBL3644400 125171 None 0 Human Functional pIC50 = 6.7 6.7 -28 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 359 2 0 5 2.7 O=C1CN=C(n2cnc(C3CC3)n2)C=C2c3cccc(C4CC4)c3CCN12 nan
159548 54725 None 13 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiologyAntagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiology
ChEMBL 435 18 6 6 1.0 CCCC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCCNCCCCNCCCN 10.1021/jm100886h
CHEMBL16117 54725 None 13 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiologyAntagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiology
ChEMBL 435 18 6 6 1.0 CCCC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCCNCCCCNCCCN 10.1021/jm100886h
11667270 85186 None 0 Human Functional pIC50 = 7.6 7.6 1 3
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 340 2 0 6 3.2 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(F)cc4)cnc3c12 10.1021/jm0504407
CHEMBL225124 85186 None 0 Human Functional pIC50 = 7.6 7.6 1 3
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 340 2 0 6 3.2 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(F)cc4)cnc3c12 10.1021/jm0504407
44442434 154664 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay
ChEMBL 337 2 0 6 2.9 Cc1nc2c(cnn2-c2cccnc2)c(=O)n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2007.05.028
CHEMBL399128 154664 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay
ChEMBL 337 2 0 6 2.9 Cc1nc2c(cnn2-c2cccnc2)c(=O)n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2007.05.028
45486755 200214 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 313 3 0 4 3.6 CN(C(=O)c1ccc(F)cc1)c1nc(-c2cccnc2)cs1 10.1016/j.bmcl.2009.07.097
CHEMBL571687 200214 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 313 3 0 4 3.6 CN(C(=O)c1ccc(F)cc1)c1nc(-c2cccnc2)cs1 10.1016/j.bmcl.2009.07.097
24777317 94771 None 0 Rat Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 257 3 1 4 2.9 CCCNc1nc2c(cc1C#N)C(=O)CC(C)(C)C2 10.1021/jm0611298
CHEMBL252943 94771 None 0 Rat Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 257 3 1 4 2.9 CCCNc1nc2c(cc1C#N)C(=O)CC(C)(C)C2 10.1021/jm0611298
86711394 125196 None 0 Human Functional pIC50 = 5.6 5.6 -19 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 378 2 0 4 3.5 CCc1cn(C2=NCC(=O)N3CCc4c(cccc4C4(F)CCC4)C3=C2)cn1 nan
CHEMBL3644425 125196 None 0 Human Functional pIC50 = 5.6 5.6 -19 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 378 2 0 4 3.5 CCc1cn(C2=NCC(=O)N3CCc4c(cccc4C4(F)CCC4)C3=C2)cn1 nan
89980108 133125 None 0 Human Functional pIC50 = 5.6 5.6 -66 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 360 3 0 4 3.1 COc1cccc(C2=NCC(=O)N3CCc4c(C(C)=O)cccc4C3=C2)c1 nan
CHEMBL3702398 133125 None 0 Human Functional pIC50 = 5.6 5.6 -66 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 360 3 0 4 3.1 COc1cccc(C2=NCC(=O)N3CCc4c(C(C)=O)cccc4C3=C2)c1 nan
24777814 94995 None 0 Rat Functional pIC50 = 4.6 4.6 - 1
Antagonist activity at rat mGluR1 by FLIPR assayAntagonist activity at rat mGluR1 by FLIPR assay
ChEMBL 302 3 2 4 3.3 CC1(C)CC(=O)c2cc(C(=O)O)c(NC3CCCC3)nc2C1 10.1021/jm0611298
CHEMBL254428 94995 None 0 Rat Functional pIC50 = 4.6 4.6 - 1
Antagonist activity at rat mGluR1 by FLIPR assayAntagonist activity at rat mGluR1 by FLIPR assay
ChEMBL 302 3 2 4 3.3 CC1(C)CC(=O)c2cc(C(=O)O)c(NC3CCCC3)nc2C1 10.1021/jm0611298
127033321 139142 None 0 Rat Functional pIC50 = 6.6 6.6 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 279 2 1 5 2.9 c1ccn2nc3c(N[C@H]4C[C@@H]5CC[C@H]4C5)ncnc3c2c1 10.1016/j.bmcl.2016.03.026
CHEMBL3786174 139142 None 0 Rat Functional pIC50 = 6.6 6.6 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 279 2 1 5 2.9 c1ccn2nc3c(N[C@H]4C[C@@H]5CC[C@H]4C5)ncnc3c2c1 10.1016/j.bmcl.2016.03.026
127031849 139210 None 0 Rat Functional pIC50 = 6.6 6.6 8 2
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 321 2 1 5 3.8 C[C@@H]1[C@@H](Nc2ncnc3c2nn2ccccc32)C[C@H]2C[C@@H]1C2(C)C 10.1016/j.bmcl.2016.03.026
CHEMBL3786866 139210 None 0 Rat Functional pIC50 = 6.6 6.6 8 2
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 321 2 1 5 3.8 C[C@@H]1[C@@H](Nc2ncnc3c2nn2ccccc32)C[C@H]2C[C@@H]1C2(C)C 10.1016/j.bmcl.2016.03.026
127033321 139142 None 0 Rat Functional pIC50 = 6.6 6.6 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 279 2 1 5 2.9 c1ccn2nc3c(N[C@H]4C[C@@H]5CC[C@H]4C5)ncnc3c2c1 10.1016/j.bmcl.2016.03.026
CHEMBL3786174 139142 None 0 Rat Functional pIC50 = 6.6 6.6 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 279 2 1 5 2.9 c1ccn2nc3c(N[C@H]4C[C@@H]5CC[C@H]4C5)ncnc3c2c1 10.1016/j.bmcl.2016.03.026
127031849 139210 None 0 Rat Functional pIC50 = 6.6 6.6 8 2
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 321 2 1 5 3.8 C[C@@H]1[C@@H](Nc2ncnc3c2nn2ccccc32)C[C@H]2C[C@@H]1C2(C)C 10.1016/j.bmcl.2016.03.026
CHEMBL3786866 139210 None 0 Rat Functional pIC50 = 6.6 6.6 8 2
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 321 2 1 5 3.8 C[C@@H]1[C@@H](Nc2ncnc3c2nn2ccccc32)C[C@H]2C[C@@H]1C2(C)C 10.1016/j.bmcl.2016.03.026
89979722 125170 None 0 Human Functional pIC50 = 5.6 5.6 -2344 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 385 2 0 6 3.1 O=C1CN=C(n2cnc(-c3ccno3)c2)C=C2c3cccc(C4CC4)c3CCN12 nan
CHEMBL3644399 125170 None 0 Human Functional pIC50 = 5.6 5.6 -2344 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 385 2 0 6 3.1 O=C1CN=C(n2cnc(-c3ccno3)c2)C=C2c3cccc(C4CC4)c3CCN12 nan
57908398 89128 None 0 Human Functional pIC50 = 6.6 6.6 -8 2
Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay
ChEMBL 389 4 1 6 4.4 C[C@@H]1C[C@H]1C(=O)Nc1snc(-c2ccc3nn(C)cc3c2)c1-c1ccccn1 10.1016/j.bmcl.2013.01.009
CHEMBL2334972 89128 None 0 Human Functional pIC50 = 6.6 6.6 -8 2
Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay
ChEMBL 389 4 1 6 4.4 C[C@@H]1C[C@H]1C(=O)Nc1snc(-c2ccc3nn(C)cc3c2)c1-c1ccccn1 10.1016/j.bmcl.2013.01.009
CHEMBL2365366 89128 None 0 Human Functional pIC50 = 6.6 6.6 -8 2
Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay
ChEMBL 389 4 1 6 4.4 C[C@@H]1C[C@H]1C(=O)Nc1snc(-c2ccc3nn(C)cc3c2)c1-c1ccccn1 10.1016/j.bmcl.2013.01.009
118735976 118986 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay
ChEMBL 409 4 1 4 4.7 N#Cc1c(NCc2cccc(F)c2)sc2c1CCN(C(=O)c1ccc(F)cc1)C2 10.1016/j.ejmech.2015.04.060
CHEMBL3422892 118986 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay
ChEMBL 409 4 1 4 4.7 N#Cc1c(NCc2cccc(F)c2)sc2c1CCN(C(=O)c1ccc(F)cc1)C2 10.1016/j.ejmech.2015.04.060
44431052 166602 None 0 Rat Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay
ChEMBL 286 2 2 2 3.3 CC(Oc1ccc2[nH]c3c(c2c1)CCNC3=O)C(C)(C)C 10.1016/j.bmcl.2007.01.055
CHEMBL427870 166602 None 0 Rat Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay
ChEMBL 286 2 2 2 3.3 CC(Oc1ccc2[nH]c3c(c2c1)CCNC3=O)C(C)(C)C 10.1016/j.bmcl.2007.01.055
3121216 198238 None 10 Rat Functional pIC50 = 4.6 4.6 - 1
Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting
ChEMBL 300 6 0 3 4.4 CCCCCCc1cc2c3c(c(=O)oc2cc1OC)CCC3 10.1016/j.bmc.2009.05.072
CHEMBL557769 198238 None 10 Rat Functional pIC50 = 4.6 4.6 - 1
Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting
ChEMBL 300 6 0 3 4.4 CCCCCCc1cc2c3c(c(=O)oc2cc1OC)CCC3 10.1016/j.bmc.2009.05.072
721080 198489 None 13 Rat Functional pIC50 = 4.6 4.6 - 1
Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting
ChEMBL 346 4 0 3 5.2 O=c1cc(-c2ccccc2)c2ccc(OCc3ccc(F)cc3)cc2o1 10.1016/j.bmc.2009.05.072
CHEMBL560273 198489 None 13 Rat Functional pIC50 = 4.6 4.6 - 1
Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting
ChEMBL 346 4 0 3 5.2 O=c1cc(-c2ccccc2)c2ccc(OCc3ccc(F)cc3)cc2o1 10.1016/j.bmc.2009.05.072
71682339 91073 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 339 2 0 3 3.3 C[C@H]1CN(c2ccccn2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
CHEMBL2397348 91073 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 339 2 0 3 3.3 C[C@H]1CN(c2ccccn2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
57559578 83846 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 407 4 1 8 3.4 COc1ccc(-n2cnc3c(sc4ncnc(NCC(F)(F)F)c43)c2=O)cc1 10.1016/j.bmcl.2012.09.048
CHEMBL2205911 83846 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 407 4 1 8 3.4 COc1ccc(-n2cnc3c(sc4ncnc(NCC(F)(F)F)c43)c2=O)cc1 10.1016/j.bmcl.2012.09.048
19705292 189312 None 0 Mouse Functional pIC50 = 7.6 7.6 -2 3
Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 326 2 0 5 3.3 CC(C)(C)OC(=O)N1CC=C(c2cn(-c3ccccc3)nn2)CC1 10.1016/j.bmc.2008.09.060
CHEMBL511355 189312 None 0 Mouse Functional pIC50 = 7.6 7.6 -2 3
Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 326 2 0 5 3.3 CC(C)(C)OC(=O)N1CC=C(c2cn(-c3ccccc3)nn2)CC1 10.1016/j.bmc.2008.09.060
16659804 88778 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay
ChEMBL 384 1 1 7 3.8 C[C@@H]1COc2cnc3sc4c(=O)n(-c5ccc(Cl)cc5)cnc4c3c2N1 10.1021/jm070590c
CHEMBL236178 88778 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay
ChEMBL 384 1 1 7 3.8 C[C@@H]1COc2cnc3sc4c(=O)n(-c5ccc(Cl)cc5)cnc4c3c2N1 10.1021/jm070590c
44442425 93654 None 0 Human Functional pIC50 = 6.6 6.6 15 2
Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay
ChEMBL 323 2 0 6 2.4 Cc1nc2c(cnn2-c2ccccc2)c(=O)n1N1CCCCCC1 10.1016/j.bmcl.2007.05.028
CHEMBL246609 93654 None 0 Human Functional pIC50 = 6.6 6.6 15 2
Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay
ChEMBL 323 2 0 6 2.4 Cc1nc2c(cnn2-c2ccccc2)c(=O)n1N1CCCCCC1 10.1016/j.bmcl.2007.05.028
15207262 93978 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay
ChEMBL 318 2 1 6 2.6 Cc1nc2c(cnn2-c2ccccc2)c(=O)n1-c1ccc(O)cc1 10.1016/j.bmcl.2007.05.028
CHEMBL248209 93978 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay
ChEMBL 318 2 1 6 2.6 Cc1nc2c(cnn2-c2ccccc2)c(=O)n1-c1ccc(O)cc1 10.1016/j.bmcl.2007.05.028
45484872 199672 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL 322 4 0 6 3.2 Cc1c(-c2cccc(C(=O)OC(C)C)c2)nnn1-c1cccnc1 10.1016/j.bmcl.2009.07.145
CHEMBL568241 199672 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL 322 4 0 6 3.2 Cc1c(-c2cccc(C(=O)OC(C)C)c2)nnn1-c1cccnc1 10.1016/j.bmcl.2009.07.145
89980695 133183 None 0 Human Functional pIC50 = 5.6 5.6 -169 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 427 2 0 5 4.0 O=C1CN=C(n2cnc(C3CCC3)c2)C=C2c3cccc(-c4cccnc4F)c3CCN12 nan
CHEMBL3702455 133183 None 0 Human Functional pIC50 = 5.6 5.6 -169 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 427 2 0 5 4.0 O=C1CN=C(n2cnc(C3CCC3)c2)C=C2c3cccc(-c4cccnc4F)c3CCN12 nan
54586363 62689 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 392 4 1 8 3.7 C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc5c(c4)OCO5)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1783873 62689 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 392 4 1 8 3.7 C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc5c(c4)OCO5)cnc3c12 10.1016/j.bmcl.2009.04.104
692972 93823 None 8 Human Functional pIC50 = 6.6 6.6 39 2
Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay
ChEMBL 336 2 0 5 3.5 Cc1nc2c(cnn2-c2ccccc2)c(=O)n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2007.05.028
CHEMBL247438 93823 None 8 Human Functional pIC50 = 6.6 6.6 39 2
Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay
ChEMBL 336 2 0 5 3.5 Cc1nc2c(cnn2-c2ccccc2)c(=O)n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2007.05.028
71682339 91073 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 339 2 0 3 3.3 C[C@H]1CN(c2ccccn2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
CHEMBL2397348 91073 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 339 2 0 3 3.3 C[C@H]1CN(c2ccccn2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
127034033 139118 None 0 Rat Functional pIC50 = 6.6 6.6 10 2
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 301 2 1 5 2.9 c1ccc2c(c1)CC(Nc1ncnc3c1nn1ccccc31)C2 10.1016/j.bmcl.2016.03.026
CHEMBL3785879 139118 None 0 Rat Functional pIC50 = 6.6 6.6 10 2
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 301 2 1 5 2.9 c1ccc2c(c1)CC(Nc1ncnc3c1nn1ccccc31)C2 10.1016/j.bmcl.2016.03.026
118735961 118975 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay
ChEMBL 395 4 2 5 3.6 Cc1cc(C(=O)N2CCc3c(sc(NCc4ccc(F)cc4)c3C#N)C2)[nH]n1 10.1016/j.ejmech.2015.04.060
CHEMBL3422877 118975 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay
ChEMBL 395 4 2 5 3.6 Cc1cc(C(=O)N2CCc3c(sc(NCc4ccc(F)cc4)c3C#N)C2)[nH]n1 10.1016/j.ejmech.2015.04.060
71683123 91085 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 363 2 0 3 3.8 C[C@@H]1CN(C(=O)C23CC4CC(CC(C4)C2)C3)CCN1c1ccccc1C#N 10.1016/j.bmcl.2013.05.020
CHEMBL2397379 91085 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 363 2 0 3 3.8 C[C@@H]1CN(C(=O)C23CC4CC(CC(C4)C2)C3)CCN1c1ccccc1C#N 10.1016/j.bmcl.2013.05.020
71683123 91085 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 363 2 0 3 3.8 C[C@@H]1CN(C(=O)C23CC4CC(CC(C4)C2)C3)CCN1c1ccccc1C#N 10.1016/j.bmcl.2013.05.020
CHEMBL2397379 91085 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 363 2 0 3 3.8 C[C@@H]1CN(C(=O)C23CC4CC(CC(C4)C2)C3)CCN1c1ccccc1C#N 10.1016/j.bmcl.2013.05.020
127034033 139118 None 0 Rat Functional pIC50 = 6.6 6.6 10 2
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 301 2 1 5 2.9 c1ccc2c(c1)CC(Nc1ncnc3c1nn1ccccc31)C2 10.1016/j.bmcl.2016.03.026
CHEMBL3785879 139118 None 0 Rat Functional pIC50 = 6.6 6.6 10 2
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 301 2 1 5 2.9 c1ccc2c(c1)CC(Nc1ncnc3c1nn1ccccc31)C2 10.1016/j.bmcl.2016.03.026
44408476 140425 None 0 Rat Functional pIC50 = 7.6 7.6 - 1
Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method
ChEMBL 342 4 0 4 3.1 Cc1c(C(=O)OC(C)C(C)(C)C)cn2c1C(=O)N(CC(F)F)CC2 10.1016/j.bmcl.2005.11.049
CHEMBL380698 140425 None 0 Rat Functional pIC50 = 7.6 7.6 - 1
Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method
ChEMBL 342 4 0 4 3.1 Cc1c(C(=O)OC(C)C(C)(C)C)cn2c1C(=O)N(CC(F)F)CC2 10.1016/j.bmcl.2005.11.049
45484964 200825 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL 275 2 1 4 3.1 Cc1c(-c2ccc3[nH]ccc3c2)nnn1-c1cccnc1 10.1016/j.bmcl.2009.07.145
CHEMBL576637 200825 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL 275 2 1 4 3.1 Cc1c(-c2ccc3[nH]ccc3c2)nnn1-c1cccnc1 10.1016/j.bmcl.2009.07.145
24777577 94690 None 0 Rat Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 305 3 1 4 3.7 CC1(C)CC(=O)c2cc(C#N)c(NCc3ccccc3)nc2C1 10.1021/jm0611298
CHEMBL252333 94690 None 0 Rat Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 305 3 1 4 3.7 CC1(C)CC(=O)c2cc(C#N)c(NCc3ccccc3)nc2C1 10.1021/jm0611298
3421 3544 None 30 Human Functional pIC50 = 4.6 4.6 1 3
Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor
ChEMBL 185 3 3 3 -0.3 OC(=O)[C@H](C12CC(C1)(C2)C(=O)O)N 10.1021/jm060950g
5311040 3544 None 30 Human Functional pIC50 = 4.6 4.6 1 3
Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor
ChEMBL 185 3 3 3 -0.3 OC(=O)[C@H](C12CC(C1)(C2)C(=O)O)N 10.1021/jm060950g
CHEMBL43412 3544 None 30 Human Functional pIC50 = 4.6 4.6 1 3
Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor
ChEMBL 185 3 3 3 -0.3 OC(=O)[C@H](C12CC(C1)(C2)C(=O)O)N 10.1021/jm060950g
24777578 94714 None 0 Rat Functional pIC50 = 4.6 4.6 3 2
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 291 3 0 4 3.1 CN(Cc1ccccc1)c1nc2c(cc1C#N)C(=O)CCC2 10.1021/jm0611298
CHEMBL252531 94714 None 0 Rat Functional pIC50 = 4.6 4.6 3 2
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 291 3 0 4 3.1 CN(Cc1ccccc1)c1nc2c(cc1C#N)C(=O)CCC2 10.1021/jm0611298
10444977 154853 None 5 Rat Functional pIC50 = 4.6 4.6 -13 2
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 253 3 0 3 3.2 O=C1CCCc2nc(OCc3ccccc3)ccc21 10.1021/jm0611298
CHEMBL400104 154853 None 5 Rat Functional pIC50 = 4.6 4.6 -13 2
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 253 3 0 3 3.2 O=C1CCCc2nc(OCc3ccccc3)ccc21 10.1021/jm0611298
22268047 46327 None 10 Human Functional pIC50 = 4.6 4.6 - 1
Compound was tested for its agonist activity against Ser165 and Thr188 (Metabotropic glutamate receptor 1) receptor.Compound was tested for its agonist activity against Ser165 and Thr188 (Metabotropic glutamate receptor 1) receptor.
ChEMBL 185 3 3 3 -0.3 NC(C(=O)O)C12CC(C(=O)O)(C1)C2 10.1021/jm990353c
CHEMBL153572 46327 None 10 Human Functional pIC50 = 4.6 4.6 - 1
Compound was tested for its agonist activity against Ser165 and Thr188 (Metabotropic glutamate receptor 1) receptor.Compound was tested for its agonist activity against Ser165 and Thr188 (Metabotropic glutamate receptor 1) receptor.
ChEMBL 185 3 3 3 -0.3 NC(C(=O)O)C12CC(C(=O)O)(C1)C2 10.1021/jm990353c
3421 3544 None 30 Human Functional pIC50 = 4.6 4.6 1 3
The compound was tested for inhibitory effect on second messenger formation in BHK cells expressing mGluR1aThe compound was tested for inhibitory effect on second messenger formation in BHK cells expressing mGluR1a
ChEMBL 185 3 3 3 -0.3 OC(=O)[C@H](C12CC(C1)(C2)C(=O)O)N 10.1021/jm960254o
5311040 3544 None 30 Human Functional pIC50 = 4.6 4.6 1 3
The compound was tested for inhibitory effect on second messenger formation in BHK cells expressing mGluR1aThe compound was tested for inhibitory effect on second messenger formation in BHK cells expressing mGluR1a
ChEMBL 185 3 3 3 -0.3 OC(=O)[C@H](C12CC(C1)(C2)C(=O)O)N 10.1021/jm960254o
CHEMBL43412 3544 None 30 Human Functional pIC50 = 4.6 4.6 1 3
The compound was tested for inhibitory effect on second messenger formation in BHK cells expressing mGluR1aThe compound was tested for inhibitory effect on second messenger formation in BHK cells expressing mGluR1a
ChEMBL 185 3 3 3 -0.3 OC(=O)[C@H](C12CC(C1)(C2)C(=O)O)N 10.1021/jm960254o
11501188 137630 None 0 Human Functional pIC50 = 6.6 6.6 1 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 350 3 0 6 3.6 CCc1ccccc1-n1cnc2c(sc3nccc(N(C)C)c32)c1=O 10.1021/jm0504407
CHEMBL375439 137630 None 0 Human Functional pIC50 = 6.6 6.6 1 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 350 3 0 6 3.6 CCc1ccccc1-n1cnc2c(sc3nccc(N(C)C)c32)c1=O 10.1021/jm0504407
44408492 75454 None 0 Rat Functional pIC50 = 6.6 6.6 - 1
Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method
ChEMBL 336 5 0 5 2.5 COCCN1CCn2cc(C(=O)OC(C)C(C)(C)C)c(C)c2C1=O 10.1016/j.bmcl.2005.11.049
CHEMBL204149 75454 None 0 Rat Functional pIC50 = 6.6 6.6 - 1
Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method
ChEMBL 336 5 0 5 2.5 COCCN1CCn2cc(C(=O)OC(C)C(C)(C)C)c(C)c2C1=O 10.1016/j.bmcl.2005.11.049
44408472 75589 None 0 Rat Functional pIC50 = 6.6 6.6 - 1
Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method
ChEMBL 368 4 0 4 4.0 Cc1c(C(=O)OC(C)C(C)(C)C)cn2c1C(=O)N(Cc1ccccc1)CC2 10.1016/j.bmcl.2005.11.049
CHEMBL204532 75589 None 0 Rat Functional pIC50 = 6.6 6.6 - 1
Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method
ChEMBL 368 4 0 4 4.0 Cc1c(C(=O)OC(C)C(C)(C)C)cn2c1C(=O)N(Cc1ccccc1)CC2 10.1016/j.bmcl.2005.11.049
71683124 91066 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 357 2 0 3 3.5 C[C@@H]1CN(c2cccc(F)n2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
CHEMBL2397341 91066 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 357 2 0 3 3.5 C[C@@H]1CN(c2cccc(F)n2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
78322065 114413 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay
ChEMBL 364 4 0 6 4.1 COc1ccc(-n2cnc3c(-c4cccc(OC)c4)csc3c2=O)cc1 10.1016/j.ejmech.2014.08.027
CHEMBL3330827 114413 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay
ChEMBL 364 4 0 6 4.1 COc1ccc(-n2cnc3c(-c4cccc(OC)c4)csc3c2=O)cc1 10.1016/j.ejmech.2014.08.027
71683124 91066 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 357 2 0 3 3.5 C[C@@H]1CN(c2cccc(F)n2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
CHEMBL2397341 91066 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 357 2 0 3 3.5 C[C@@H]1CN(c2cccc(F)n2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
11631279 141998 None 0 Human Functional pIC50 = 7.6 7.6 1 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 328 3 0 6 3.3 CN(C)c1ccnc2sc3c(=O)n(CC4CCCC4)cnc3c12 10.1021/jm0504407
CHEMBL386935 141998 None 0 Human Functional pIC50 = 7.6 7.6 1 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 328 3 0 6 3.3 CN(C)c1ccnc2sc3c(=O)n(CC4CCCC4)cnc3c12 10.1021/jm0504407
122196096 124298 None 0 Human Functional pIC50 = 7.6 7.6 10 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 378 3 1 4 4.1 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c(F)c1 10.1016/j.bmcl.2015.10.013
CHEMBL3634419 124298 None 0 Human Functional pIC50 = 7.6 7.6 10 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 378 3 1 4 4.1 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c(F)c1 10.1016/j.bmcl.2015.10.013
3260619 4019 None 24 Rat Functional pIC50 = 5.6 5.6 1 4
Antagonist activity at rat mGluR1 expressed in Syrian golden hamster BHK cells assessed as potentiation of glutamate-induced calcium flux by fluorescence assayAntagonist activity at rat mGluR1 expressed in Syrian golden hamster BHK cells assessed as potentiation of glutamate-induced calcium flux by fluorescence assay
ChEMBL 321 2 0 5 3.7 CC1CCCN(C1)c1ncnc2c1cnn2c1ccc(cc1C)C 10.1016/j.bmcl.2008.08.087
6227 4019 None 24 Rat Functional pIC50 = 5.6 5.6 1 4
Antagonist activity at rat mGluR1 expressed in Syrian golden hamster BHK cells assessed as potentiation of glutamate-induced calcium flux by fluorescence assayAntagonist activity at rat mGluR1 expressed in Syrian golden hamster BHK cells assessed as potentiation of glutamate-induced calcium flux by fluorescence assay
ChEMBL 321 2 0 5 3.7 CC1CCCN(C1)c1ncnc2c1cnn2c1ccc(cc1C)C 10.1016/j.bmcl.2008.08.087
CHEMBL477396 4019 None 24 Rat Functional pIC50 = 5.6 5.6 1 4
Antagonist activity at rat mGluR1 expressed in Syrian golden hamster BHK cells assessed as potentiation of glutamate-induced calcium flux by fluorescence assayAntagonist activity at rat mGluR1 expressed in Syrian golden hamster BHK cells assessed as potentiation of glutamate-induced calcium flux by fluorescence assay
ChEMBL 321 2 0 5 3.7 CC1CCCN(C1)c1ncnc2c1cnn2c1ccc(cc1C)C 10.1016/j.bmcl.2008.08.087
24777697 154452 None 0 Rat Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 299 6 1 4 4.1 CCCCCCNc1nc2c(cc1C#N)C(=O)CC(C)(C)C2 10.1021/jm0611298
CHEMBL398706 154452 None 0 Rat Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 299 6 1 4 4.1 CCCCCCNc1nc2c(cc1C#N)C(=O)CC(C)(C)C2 10.1021/jm0611298
89980646 125164 None 0 Human Functional pIC50 = 5.6 5.6 -109 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 376 3 0 5 3.3 C=C(C)c1cccc2c1CCN1C(=O)CN=C(n3cnc([C@H](C)OC)c3)C=C21 nan
CHEMBL3644393 125164 None 0 Human Functional pIC50 = 5.6 5.6 -109 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 376 3 0 5 3.3 C=C(C)c1cccc2c1CCN1C(=O)CN=C(n3cnc([C@H](C)OC)c3)C=C21 nan
71682963 91084 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 363 2 0 3 3.8 C[C@@H]1CN(c2ccccc2C#N)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
CHEMBL2397378 91084 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 363 2 0 3 3.8 C[C@@H]1CN(c2ccccc2C#N)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
71682963 91084 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 363 2 0 3 3.8 C[C@@H]1CN(c2ccccc2C#N)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
CHEMBL2397378 91084 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 363 2 0 3 3.8 C[C@@H]1CN(c2ccccc2C#N)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
127033449 139217 None 0 Rat Functional pIC50 = 5.6 5.6 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 267 2 1 5 3.0 c1ccn2nc3c(NC4CCCCC4)ncnc3c2c1 10.1016/j.bmcl.2016.03.026
CHEMBL3786959 139217 None 0 Rat Functional pIC50 = 5.6 5.6 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 267 2 1 5 3.0 c1ccn2nc3c(NC4CCCCC4)ncnc3c2c1 10.1016/j.bmcl.2016.03.026
46866192 1050 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 323 1 1 7 2.6 Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(N)nc(n1)C 10.1016/j.bmcl.2010.03.004
6210 1050 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 323 1 1 7 2.6 Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(N)nc(n1)C 10.1016/j.bmcl.2010.03.004
CHEMBL1093901 1050 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 323 1 1 7 2.6 Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(N)nc(n1)C 10.1016/j.bmcl.2010.03.004
16117046 71013 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 337 3 1 6 3.7 CNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951680 71013 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 337 3 1 6 3.7 CNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
73334939 133084 None 0 Human Functional pIC50 = 7.6 7.6 3 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 328 1 0 3 3.6 O=C1CN=C(c2cccs2)C=C2c3cccc(Cl)c3CCN12 nan
CHEMBL3702357 133084 None 0 Human Functional pIC50 = 7.6 7.6 3 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 328 1 0 3 3.6 O=C1CN=C(c2cccs2)C=C2c3cccc(Cl)c3CCN12 nan
122196097 124299 None 0 Human Functional pIC50 = 7.6 7.6 9 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 398 3 1 4 4.4 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(F)c1 10.1016/j.bmcl.2015.10.013
CHEMBL3634420 124299 None 0 Human Functional pIC50 = 7.6 7.6 9 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 398 3 1 4 4.4 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(F)c1 10.1016/j.bmcl.2015.10.013
10382361 122262 None 0 Rat Functional pIC50 = 6.6 6.6 -301 2
Negative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysisNegative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysis
ChEMBL 336 2 0 5 1.7 O=C(C#Cc1ccccc1)N1CCN(c2ncccc2[N+](=O)[O-])CC1 10.1016/j.bmc.2015.05.008
CHEMBL3597584 122262 None 0 Rat Functional pIC50 = 6.6 6.6 -301 2
Negative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysisNegative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysis
ChEMBL 336 2 0 5 1.7 O=C(C#Cc1ccccc1)N1CCN(c2ncccc2[N+](=O)[O-])CC1 10.1016/j.bmc.2015.05.008
127033449 139217 None 0 Rat Functional pIC50 = 5.6 5.6 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 267 2 1 5 3.0 c1ccn2nc3c(NC4CCCCC4)ncnc3c2c1 10.1016/j.bmcl.2016.03.026
CHEMBL3786959 139217 None 0 Rat Functional pIC50 = 5.6 5.6 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 267 2 1 5 3.0 c1ccn2nc3c(NC4CCCCC4)ncnc3c2c1 10.1016/j.bmcl.2016.03.026
57881896 83853 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 401 4 1 8 4.1 COc1ccc(-n2cnc3c(sc4ncnc(Nc5ccccc5)c43)c2=O)cc1 10.1016/j.bmcl.2012.09.048
CHEMBL2205919 83853 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 401 4 1 8 4.1 COc1ccc(-n2cnc3c(sc4ncnc(Nc5ccccc5)c43)c2=O)cc1 10.1016/j.bmcl.2012.09.048
44230992 89110 None 0 Human Functional pIC50 = 6.6 6.6 -28 2
Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay
ChEMBL 417 5 1 6 4.9 CCc1cccc(-c2c(-c3ccc4nn(C)cc4c3)nsc2NC(=O)[C@@H]2C[C@H]2C)n1 10.1016/j.bmcl.2013.01.009
CHEMBL2334976 89110 None 0 Human Functional pIC50 = 6.6 6.6 -28 2
Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay
ChEMBL 417 5 1 6 4.9 CCc1cccc(-c2c(-c3ccc4nn(C)cc4c3)nsc2NC(=O)[C@@H]2C[C@H]2C)n1 10.1016/j.bmcl.2013.01.009
CHEMBL2365134 89110 None 0 Human Functional pIC50 = 6.6 6.6 -28 2
Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay
ChEMBL 417 5 1 6 4.9 CCc1cccc(-c2c(-c3ccc4nn(C)cc4c3)nsc2NC(=O)[C@@H]2C[C@H]2C)n1 10.1016/j.bmcl.2013.01.009
3347 2423 None 10 Human Functional pIC50 = 7.6 7.6 - 1
Negative allosteric modulation activity at recombinant human mGluR1a expressed in CHO cells assessed as inhibition of L-glutamate-induced intracellular Ca2+ mobilizationNegative allosteric modulation activity at recombinant human mGluR1a expressed in CHO cells assessed as inhibition of L-glutamate-induced intracellular Ca2+ mobilization
ChEMBL 341 5 2 5 3.0 OCCSc1nc(NC2Cc3c(C2)cccc3)c2c(n1)CCCC2 10.1016/j.bmcl.2016.03.026
9840951 2423 None 10 Human Functional pIC50 = 7.6 7.6 - 1
Negative allosteric modulation activity at recombinant human mGluR1a expressed in CHO cells assessed as inhibition of L-glutamate-induced intracellular Ca2+ mobilizationNegative allosteric modulation activity at recombinant human mGluR1a expressed in CHO cells assessed as inhibition of L-glutamate-induced intracellular Ca2+ mobilization
ChEMBL 341 5 2 5 3.0 OCCSc1nc(NC2Cc3c(C2)cccc3)c2c(n1)CCCC2 10.1016/j.bmcl.2016.03.026
CHEMBL3786530 2423 None 10 Human Functional pIC50 = 7.6 7.6 - 1
Negative allosteric modulation activity at recombinant human mGluR1a expressed in CHO cells assessed as inhibition of L-glutamate-induced intracellular Ca2+ mobilizationNegative allosteric modulation activity at recombinant human mGluR1a expressed in CHO cells assessed as inhibition of L-glutamate-induced intracellular Ca2+ mobilization
ChEMBL 341 5 2 5 3.0 OCCSc1nc(NC2Cc3c(C2)cccc3)c2c(n1)CCCC2 10.1016/j.bmcl.2016.03.026
122196093 124295 None 0 Human Functional pIC50 = 7.5 7.5 16 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 380 3 1 4 4.3 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)cc1 10.1016/j.bmcl.2015.10.013
CHEMBL3634416 124295 None 0 Human Functional pIC50 = 7.5 7.5 16 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 380 3 1 4 4.3 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)cc1 10.1016/j.bmcl.2015.10.013
122196124 124325 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 380 3 1 4 4.3 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)cc1Cl 10.1016/j.bmcl.2015.10.013
CHEMBL3634446 124325 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 380 3 1 4 4.3 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)cc1Cl 10.1016/j.bmcl.2015.10.013
73335133 133100 None 0 Human Functional pIC50 = 5.6 5.6 -2 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 396 2 0 3 3.7 COc1cccc(C2=NCC(=O)N3CCc4c(Br)cccc4C3=C2)c1 nan
CHEMBL3702373 133100 None 0 Human Functional pIC50 = 5.6 5.6 -2 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 396 2 0 3 3.7 COc1cccc(C2=NCC(=O)N3CCc4c(Br)cccc4C3=C2)c1 nan
657896 142169 None 8 Human Functional pIC50 = 6.6 6.6 1 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 336 3 0 6 3.1 CN(C)c1ccnc2sc3c(=O)n(Cc4ccccc4)cnc3c12 10.1021/jm0504407
CHEMBL388087 142169 None 8 Human Functional pIC50 = 6.6 6.6 1 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 336 3 0 6 3.1 CN(C)c1ccnc2sc3c(=O)n(Cc4ccccc4)cnc3c12 10.1021/jm0504407
118735965 118977 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay
ChEMBL 373 4 1 4 4.4 N#Cc1c(NCc2ccccc2)sc2c1CCN(C(=O)c1ccccc1)C2 10.1016/j.ejmech.2015.04.060
CHEMBL3422881 118977 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay
ChEMBL 373 4 1 4 4.4 N#Cc1c(NCc2ccccc2)sc2c1CCN(C(=O)c1ccccc1)C2 10.1016/j.ejmech.2015.04.060
3483737 198305 None 2 Rat Functional pIC50 = 4.6 4.6 - 1
Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting
ChEMBL 386 7 0 4 6.7 CCCCOc1ccc(-c2nnc(-c3ccc(-c4ccccc4)cc3)s2)cc1 10.1016/j.bmc.2009.05.072
CHEMBL558521 198305 None 2 Rat Functional pIC50 = 4.6 4.6 - 1
Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting
ChEMBL 386 7 0 4 6.7 CCCCOc1ccc(-c2nnc(-c3ccc(-c4ccccc4)cc3)s2)cc1 10.1016/j.bmc.2009.05.072
44431056 152394 None 0 Rat Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay
ChEMBL 292 3 2 2 3.0 O=C1NCCc2c1[nH]c1cc(OCc3ccccc3)ccc21 10.1016/j.bmcl.2007.01.055
CHEMBL396956 152394 None 0 Rat Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay
ChEMBL 292 3 2 2 3.0 O=C1NCCc2c1[nH]c1cc(OCc3ccccc3)ccc21 10.1016/j.bmcl.2007.01.055
73336213 125192 None 0 Human Functional pIC50 = 6.5 6.5 -144 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 380 3 0 5 2.7 COCc1cn(C2=NCC(=O)N3CCc4c(ccc(F)c4C4CC4)C3=C2)cn1 nan
CHEMBL3644421 125192 None 0 Human Functional pIC50 = 6.5 6.5 -144 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 380 3 0 5 2.7 COCc1cn(C2=NCC(=O)N3CCc4c(ccc(F)c4C4CC4)C3=C2)cn1 nan
44588428 176937 None 0 Mouse Functional pIC50 = 6.5 6.5 -5 3
Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 343 2 1 4 3.0 CC(C)(C)NC(=O)N1CC=C(c2cn(-c3ccccc3F)nn2)CC1 10.1016/j.bmc.2008.09.060
CHEMBL461034 176937 None 0 Mouse Functional pIC50 = 6.5 6.5 -5 3
Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 343 2 1 4 3.0 CC(C)(C)NC(=O)N1CC=C(c2cn(-c3ccccc3F)nn2)CC1 10.1016/j.bmc.2008.09.060
118735968 118980 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay
ChEMBL 391 4 1 4 4.6 N#Cc1c(NCc2ccccc2)sc2c1CCN(C(=O)c1cccc(F)c1)C2 10.1016/j.ejmech.2015.04.060
CHEMBL3422884 118980 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay
ChEMBL 391 4 1 4 4.6 N#Cc1c(NCc2ccccc2)sc2c1CCN(C(=O)c1cccc(F)c1)C2 10.1016/j.ejmech.2015.04.060
72163837 92056 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 340 1 0 3 2.8 O=C(N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1)N1CCC2(CCCC2)C1 10.1016/j.bmcl.2013.07.029
CHEMBL2418359 92056 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 340 1 0 3 2.8 O=C(N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1)N1CCC2(CCCC2)C1 10.1016/j.bmcl.2013.07.029
72163837 92056 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 340 1 0 3 2.8 O=C(N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1)N1CCC2(CCCC2)C1 10.1016/j.bmcl.2013.07.029
CHEMBL2418359 92056 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 340 1 0 3 2.8 O=C(N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1)N1CCC2(CCCC2)C1 10.1016/j.bmcl.2013.07.029
5766228 198089 None 14 Rat Functional pIC50 = 5.5 5.5 - 1
Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting
ChEMBL 313 3 0 3 5.2 Cc1ccc2cc(/C=C/C(=O)c3cccs3)c(Cl)nc2c1 10.1016/j.bmc.2009.05.072
CHEMBL556293 198089 None 14 Rat Functional pIC50 = 5.5 5.5 - 1
Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting
ChEMBL 313 3 0 3 5.2 Cc1ccc2cc(/C=C/C(=O)c3cccs3)c(Cl)nc2c1 10.1016/j.bmc.2009.05.072
76321786 105661 None 0 Human Functional pIC50 = 4.5 4.5 -2041 2
Negative allosteric modulation of human mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium flux after 16 to 24 hrs by FLIPR assayNegative allosteric modulation of human mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium flux after 16 to 24 hrs by FLIPR assay
ChEMBL 351 4 0 6 2.6 C[C@@H]1CCCN1C(=O)c1nn(C)c2nc(OCc3ccccn3)ccc12 10.1021/jm401622k
CHEMBL3122225 105661 None 0 Human Functional pIC50 = 4.5 4.5 -2041 2
Negative allosteric modulation of human mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium flux after 16 to 24 hrs by FLIPR assayNegative allosteric modulation of human mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium flux after 16 to 24 hrs by FLIPR assay
ChEMBL 351 4 0 6 2.6 C[C@@H]1CCCN1C(=O)c1nn(C)c2nc(OCc3ccccn3)ccc12 10.1021/jm401622k
54584891 62782 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 367 3 1 7 3.1 C#CCNc1ncnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784067 62782 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 367 3 1 7 3.1 C#CCNc1ncnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
57881625 83734 None 0 Human Functional pIC50 = 8.5 8.5 3311 2
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 369 3 1 7 3.6 O=c1c2sc3ncnc(NC4CC4)c3c2ncn1-c1ccc(Cl)cc1 10.1016/j.bmcl.2012.09.048
CHEMBL2205371 83734 None 0 Human Functional pIC50 = 8.5 8.5 3311 2
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 369 3 1 7 3.6 O=c1c2sc3ncnc(NC4CC4)c3c2ncn1-c1ccc(Cl)cc1 10.1016/j.bmcl.2012.09.048
57559280 83843 None 0 Human Functional pIC50 = 8.5 8.5 3311 2
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 367 4 0 8 2.9 CCN(C)c1ncnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12 10.1016/j.bmcl.2012.09.048
CHEMBL2205909 83843 None 0 Human Functional pIC50 = 8.5 8.5 3311 2
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 367 4 0 8 2.9 CCN(C)c1ncnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12 10.1016/j.bmcl.2012.09.048
11530404 210 None 14 Human Functional pIC50 = 8.5 8.5 1 4
Antagonist activity at human mGluR1 expressed in 1321N1 cellsAntagonist activity at human mGluR1 expressed in 1321N1 cells
ChEMBL 350 3 0 6 3.6 CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C 10.1016/j.bmcl.2006.06.053
6211 210 None 14 Human Functional pIC50 = 8.5 8.5 1 4
Antagonist activity at human mGluR1 expressed in 1321N1 cellsAntagonist activity at human mGluR1 expressed in 1321N1 cells
ChEMBL 350 3 0 6 3.6 CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C 10.1016/j.bmcl.2006.06.053
CHEMBL385336 210 None 14 Human Functional pIC50 = 8.5 8.5 1 4
Antagonist activity at human mGluR1 expressed in 1321N1 cellsAntagonist activity at human mGluR1 expressed in 1321N1 cells
ChEMBL 350 3 0 6 3.6 CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C 10.1016/j.bmcl.2006.06.053
11530404 210 None 14 Human Functional pIC50 = 8.5 8.5 1 4
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 350 3 0 6 3.6 CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C 10.1021/jm0504407
6211 210 None 14 Human Functional pIC50 = 8.5 8.5 1 4
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 350 3 0 6 3.6 CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C 10.1021/jm0504407
CHEMBL385336 210 None 14 Human Functional pIC50 = 8.5 8.5 1 4
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 350 3 0 6 3.6 CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C 10.1021/jm0504407
16118398 71055 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 355 3 1 5 4.7 CCNc1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951879 71055 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 355 3 1 5 4.7 CCNc1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
11530404 210 None 14 Human Functional pIC50 = 8.5 8.5 1 4
Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor
ChEMBL 350 3 0 6 3.6 CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C 10.1021/jm060950g
6211 210 None 14 Human Functional pIC50 = 8.5 8.5 1 4
Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor
ChEMBL 350 3 0 6 3.6 CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C 10.1021/jm060950g
CHEMBL385336 210 None 14 Human Functional pIC50 = 8.5 8.5 1 4
Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor
ChEMBL 350 3 0 6 3.6 CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C 10.1021/jm060950g
11772954 1034 None 0 Human Functional pIC50 = 8.5 8.5 1 2
Antagonist activity at mGluR1Antagonist activity at mGluR1
ChEMBL 365 8 3 7 2.0 OCCOCCNc1ncc2c(c1)c(ncn2)NC1Cc2c(C1)cccc2 10.1016/j.bmcl.2009.02.106
6349 1034 None 0 Human Functional pIC50 = 8.5 8.5 1 2
Antagonist activity at mGluR1Antagonist activity at mGluR1
ChEMBL 365 8 3 7 2.0 OCCOCCNc1ncc2c(c1)c(ncn2)NC1Cc2c(C1)cccc2 10.1016/j.bmcl.2009.02.106
CHEMBL469382 1034 None 0 Human Functional pIC50 = 8.5 8.5 1 2
Antagonist activity at mGluR1Antagonist activity at mGluR1
ChEMBL 365 8 3 7 2.0 OCCOCCNc1ncc2c(c1)c(ncn2)NC1Cc2c(C1)cccc2 10.1016/j.bmcl.2009.02.106
7442 2135 None 7 Rat Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 311 4 0 3 4.5 CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)C)CC 10.1021/jm0611298
9948645 2135 None 7 Rat Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 311 4 0 3 4.5 CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)C)CC 10.1021/jm0611298
CHEMBL188906 2135 None 7 Rat Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 311 4 0 3 4.5 CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)C)CC 10.1021/jm0611298
CHEMBL253345 2135 None 7 Rat Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 311 4 0 3 4.5 CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)C)CC 10.1021/jm0611298
46886140 8476 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 341 1 2 8 2.6 Cc1ccc(-n2cnc3c(sc4nc(S)nc(N)c43)c2=O)cc1 10.1016/j.bmcl.2010.03.004
CHEMBL1093869 8476 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 341 1 2 8 2.6 Cc1ccc(-n2cnc3c(sc4nc(S)nc(N)c43)c2=O)cc1 10.1016/j.bmcl.2010.03.004
16118124 71004 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 378 2 0 7 4.3 CN(C)c1ccnc2sc3c(=O)n(-c4ccc5ncsc5c4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951669 71004 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 378 2 0 7 4.3 CN(C)c1ccnc2sc3c(=O)n(-c4ccc5ncsc5c4)ccc3c12 10.1016/j.bmcl.2011.12.131
11245287 1697 None 29 Mouse Functional pIC50 = 8.5 8.5 1 4
Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 358 3 0 5 2.7 CC(N(C(=O)N1CCC(=CC1)c1nnn(c1C)c1cccnc1F)C)C 10.1016/j.bmc.2008.09.060
6363 1697 None 29 Mouse Functional pIC50 = 8.5 8.5 1 4
Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 358 3 0 5 2.7 CC(N(C(=O)N1CCC(=CC1)c1nnn(c1C)c1cccnc1F)C)C 10.1016/j.bmc.2008.09.060
CHEMBL502882 1697 None 29 Mouse Functional pIC50 = 8.5 8.5 1 4
Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 358 3 0 5 2.7 CC(N(C(=O)N1CCC(=CC1)c1nnn(c1C)c1cccnc1F)C)C 10.1016/j.bmc.2008.09.060
11772069 200970 None 1 Human Functional pIC50 = 8.5 8.5 331 2
Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL 337 3 0 5 2.8 CCN1Cc2cc(-c3nnn(-c4cccnc4F)c3C)ccc2C1=O 10.1016/j.bmcl.2009.07.145
CHEMBL577833 200970 None 1 Human Functional pIC50 = 8.5 8.5 331 2
Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL 337 3 0 5 2.8 CCN1Cc2cc(-c3nnn(-c4cccnc4F)c3C)ccc2C1=O 10.1016/j.bmcl.2009.07.145
11695894 174896 None 0 Mouse Functional pIC50 = 8.5 8.5 2 3
Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 345 3 0 6 2.7 Cc1c(C2=CCN(C(=O)OC(C)C)CC2)nnn1-c1cccnc1F 10.1016/j.bmc.2008.09.060
CHEMBL456196 174896 None 0 Mouse Functional pIC50 = 8.5 8.5 2 3
Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 345 3 0 6 2.7 Cc1c(C2=CCN(C(=O)OC(C)C)CC2)nnn1-c1cccnc1F 10.1016/j.bmc.2008.09.060
16118542 71020 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 321 2 1 5 4.0 CNc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951688 71020 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 321 2 1 5 4.0 CNc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
11175501 885 None 34 Human Functional pIC50 = 8.5 8.5 1819 2
Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL 349 3 0 5 2.9 O=C1N(Cc2c1ccc(c2)c1nnn(c1C)c1cccnc1F)C1CC1 10.1016/j.bmcl.2009.07.145
6341 885 None 34 Human Functional pIC50 = 8.5 8.5 1819 2
Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL 349 3 0 5 2.9 O=C1N(Cc2c1ccc(c2)c1nnn(c1C)c1cccnc1F)C1CC1 10.1016/j.bmcl.2009.07.145
CHEMBL578995 885 None 34 Human Functional pIC50 = 8.5 8.5 1819 2
Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL 349 3 0 5 2.9 O=C1N(Cc2c1ccc(c2)c1nnn(c1C)c1cccnc1F)C1CC1 10.1016/j.bmcl.2009.07.145
15985249 199711 None 0 Human Functional pIC50 = 8.4 8.4 776 2
Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL 351 4 0 5 3.1 CCCN1Cc2cc(-c3nnn(-c4cccnc4F)c3C)ccc2C1=O 10.1016/j.bmcl.2009.07.145
CHEMBL1645349 199711 None 0 Human Functional pIC50 = 8.4 8.4 776 2
Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL 351 4 0 5 3.1 CCCN1Cc2cc(-c3nnn(-c4cccnc4F)c3C)ccc2C1=O 10.1016/j.bmcl.2009.07.145
CHEMBL568443 199711 None 0 Human Functional pIC50 = 8.4 8.4 776 2
Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL 351 4 0 5 3.1 CCCN1Cc2cc(-c3nnn(-c4cccnc4F)c3C)ccc2C1=O 10.1016/j.bmcl.2009.07.145
15985251 2558 None 30 Rat Functional pIC50 = 8.4 8.4 1 2
Antagonist activity at rat mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at rat mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL 368 3 0 4 3.9 Fc1ccc(c(c1)F)n1nnc(c1C)c1ccc2c(c1)CN(C2=O)C(C)C 10.1016/j.bmcl.2009.07.145
6335 2558 None 30 Rat Functional pIC50 = 8.4 8.4 1 2
Antagonist activity at rat mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at rat mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL 368 3 0 4 3.9 Fc1ccc(c(c1)F)n1nnc(c1C)c1ccc2c(c1)CN(C2=O)C(C)C 10.1016/j.bmcl.2009.07.145
CHEMBL579062 2558 None 30 Rat Functional pIC50 = 8.4 8.4 1 2
Antagonist activity at rat mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at rat mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL 368 3 0 4 3.9 Fc1ccc(c(c1)F)n1nnc(c1C)c1ccc2c(c1)CN(C2=O)C(C)C 10.1016/j.bmcl.2009.07.145
16660140 199395 None 1 Human Functional pIC50 = 8.4 8.4 2454 2
Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 357 5 1 6 3.4 CCNc1cc(-c2csc(N(C)C(=O)c3ccc(F)cc3)n2)ncn1 10.1016/j.bmcl.2009.07.097
CHEMBL566374 199395 None 1 Human Functional pIC50 = 8.4 8.4 2454 2
Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 357 5 1 6 3.4 CCNc1cc(-c2csc(N(C)C(=O)c3ccc(F)cc3)n2)ncn1 10.1016/j.bmcl.2009.07.097
54586817 62766 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 380 3 0 6 3.7 C#CCN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784051 62766 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 380 3 0 6 3.7 C#CCN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
54582004 62783 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 347 3 1 7 2.7 C#CCNc1ncnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784068 62783 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 347 3 1 7 2.7 C#CCNc1ncnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
16118682 71001 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 369 3 0 6 3.8 COc1ccc(-n2ccc3c(sc4nccc(N(C)C)c43)c2=O)cc1F 10.1016/j.bmcl.2011.12.131
CHEMBL1951666 71001 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 369 3 0 6 3.8 COc1ccc(-n2ccc3c(sc4nccc(N(C)C)c43)c2=O)cc1F 10.1016/j.bmcl.2011.12.131
57881773 83738 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 383 4 1 8 3.1 COc1ccc(-n2cnc3c(sc4ncnc(NC5CC5)c43)c2=O)c(F)c1 10.1016/j.bmcl.2012.09.048
CHEMBL2205375 83738 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 383 4 1 8 3.1 COc1ccc(-n2cnc3c(sc4ncnc(NC5CC5)c43)c2=O)c(F)c1 10.1016/j.bmcl.2012.09.048
76955645 150692 None 4 Human Functional pIC50 = 7.5 7.5 - 1
FLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and diluteFLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and dilute
ChEMBL 356 2 0 4 4.9 O=c1c2scc(-c3ccccc3F)c2ncn1-c1ccc(Cl)cc1 nan
CHEMBL3955218 150692 None 4 Human Functional pIC50 = 7.5 7.5 - 1
FLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and diluteFLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and dilute
ChEMBL 356 2 0 4 4.9 O=c1c2scc(-c3ccccc3F)c2ncn1-c1ccc(Cl)cc1 nan
45484973 199550 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL 286 2 0 4 3.8 Cc1c(-c2ccc3ccccc3c2)nnn1-c1cccnc1 10.1016/j.bmcl.2009.07.145
CHEMBL567584 199550 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL 286 2 0 4 3.8 Cc1c(-c2ccc3ccccc3c2)nnn1-c1cccnc1 10.1016/j.bmcl.2009.07.145
10851012 188184 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at mGluR1Antagonist activity at mGluR1
ChEMBL 289 2 2 5 3.1 Nc1cc2c(Nc3ccc(F)c(Cl)c3)ncnc2cn1 10.1016/j.bmcl.2009.02.106
CHEMBL497917 188184 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at mGluR1Antagonist activity at mGluR1
ChEMBL 289 2 2 5 3.1 Nc1cc2c(Nc3ccc(F)c(Cl)c3)ncnc2cn1 10.1016/j.bmcl.2009.02.106
24777580 94740 None 0 Rat Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 269 2 1 4 3.2 N#Cc1cc2c(nc1NC1CCCCC1)CCCC2=O 10.1021/jm0611298
CHEMBL252736 94740 None 0 Rat Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 269 2 1 4 3.2 N#Cc1cc2c(nc1NC1CCCCC1)CCCC2=O 10.1021/jm0611298
5761323 198287 None 3 Rat Functional pIC50 = 4.5 4.5 - 1
Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting
ChEMBL 334 5 0 2 6.0 O=C(/C=C/c1ccc(Cl)cc1)c1ccc(Oc2ccccc2)cc1 10.1016/j.bmc.2009.05.072
CHEMBL558321 198287 None 3 Rat Functional pIC50 = 4.5 4.5 - 1
Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting
ChEMBL 334 5 0 2 6.0 O=C(/C=C/c1ccc(Cl)cc1)c1ccc(Oc2ccccc2)cc1 10.1016/j.bmc.2009.05.072
1893077 94689 None 12 Rat Functional pIC50 = 4.5 4.5 -6 3
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 294 3 0 4 3.8 N#Cc1cc2c(nc1SCc1ccccc1)CCCC2=O 10.1021/jm0611298
CHEMBL252332 94689 None 12 Rat Functional pIC50 = 4.5 4.5 -6 3
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 294 3 0 4 3.8 N#Cc1cc2c(nc1SCc1ccccc1)CCCC2=O 10.1021/jm0611298
73334943 133088 None 0 Human Functional pIC50 = 5.5 5.5 -39 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 353 2 0 4 3.0 COc1cc(C2=NCC(=O)N3CCc4c(Cl)cccc4C3=C2)ccn1 nan
CHEMBL3702361 133088 None 0 Human Functional pIC50 = 5.5 5.5 -39 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 353 2 0 4 3.0 COc1cc(C2=NCC(=O)N3CCc4c(Cl)cccc4C3=C2)ccn1 nan
72165213 105648 None 14 Human Functional pIC50 = 4.5 4.5 -12022 2
Negative allosteric modulation of human mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium flux after 16 to 24 hrs by FLIPR assayNegative allosteric modulation of human mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium flux after 16 to 24 hrs by FLIPR assay
ChEMBL 332 4 0 7 2.7 Cc1ccncc1-c1nn(C)c2nc(OCc3ccccn3)cnc12 10.1021/jm401622k
CHEMBL3122212 105648 None 14 Human Functional pIC50 = 4.5 4.5 -12022 2
Negative allosteric modulation of human mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium flux after 16 to 24 hrs by FLIPR assayNegative allosteric modulation of human mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium flux after 16 to 24 hrs by FLIPR assay
ChEMBL 332 4 0 7 2.7 Cc1ccncc1-c1nn(C)c2nc(OCc3ccccn3)cnc12 10.1021/jm401622k
11639210 144237 None 0 Human Functional pIC50 = 6.5 6.5 1 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 366 3 0 6 3.6 CCc1ccc(-n2cnc3c(sc4nccc([N+](C)(C)[O-])c43)c2=O)cc1 10.1021/jm0504407
CHEMBL390391 144237 None 0 Human Functional pIC50 = 6.5 6.5 1 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 366 3 0 6 3.6 CCc1ccc(-n2cnc3c(sc4nccc([N+](C)(C)[O-])c43)c2=O)cc1 10.1021/jm0504407
118735981 118988 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay
ChEMBL 421 5 1 5 4.6 COc1cccc(CNc2sc3c(c2C#N)CCN(C(=O)c2ccc(F)cc2)C3)c1 10.1016/j.ejmech.2015.04.060
CHEMBL3422897 118988 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay
ChEMBL 421 5 1 5 4.6 COc1cccc(CNc2sc3c(c2C#N)CCN(C(=O)c2ccc(F)cc2)C3)c1 10.1016/j.ejmech.2015.04.060
16117434 71064 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 322 2 1 6 3.3 CNc1ncnc2sc3c(=O)n(-c4ccc(C)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951888 71064 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 322 2 1 6 3.3 CNc1ncnc2sc3c(=O)n(-c4ccc(C)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
44588425 176913 None 0 Mouse Functional pIC50 = 7.5 7.5 -1 3
Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 344 2 0 5 3.4 CC(C)(C)OC(=O)N1CC=C(c2cn(-c3ccc(F)cc3)nn2)CC1 10.1016/j.bmc.2008.09.060
CHEMBL460827 176913 None 0 Mouse Functional pIC50 = 7.5 7.5 -1 3
Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 344 2 0 5 3.4 CC(C)(C)OC(=O)N1CC=C(c2cn(-c3ccc(F)cc3)nn2)CC1 10.1016/j.bmc.2008.09.060
73335545 133136 None 0 Human Functional pIC50 = 5.5 5.5 -8 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 350 2 0 5 2.7 COc1cccc2c1CCN1C(=O)CN=C(n3cnc(C(C)C)c3)C=C21 nan
CHEMBL3702409 133136 None 0 Human Functional pIC50 = 5.5 5.5 -8 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 350 2 0 5 2.7 COc1cccc2c1CCN1C(=O)CN=C(n3cnc(C(C)C)c3)C=C21 nan
71717644 89127 None 0 Human Functional pIC50 = 5.5 5.5 -85 2
Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay
ChEMBL 403 5 2 5 4.9 CCc1cccc(-c2c(-c3ccc4n[nH]cc4c3)nsc2NC(=O)[C@@H]2C[C@H]2C)n1 10.1016/j.bmcl.2013.01.009
CHEMBL2334986 89127 None 0 Human Functional pIC50 = 5.5 5.5 -85 2
Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay
ChEMBL 403 5 2 5 4.9 CCc1cccc(-c2c(-c3ccc4n[nH]cc4c3)nsc2NC(=O)[C@@H]2C[C@H]2C)n1 10.1016/j.bmcl.2013.01.009
CHEMBL2365364 89127 None 0 Human Functional pIC50 = 5.5 5.5 -85 2
Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay
ChEMBL 403 5 2 5 4.9 CCc1cccc(-c2c(-c3ccc4n[nH]cc4c3)nsc2NC(=O)[C@@H]2C[C@H]2C)n1 10.1016/j.bmcl.2013.01.009
44431048 93357 None 0 Rat Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay
ChEMBL 377 3 3 2 3.4 O=C(NCC12CC3CC(CC(C3)C1)C2)c1ccc2[nH]c3c(c2c1)CCNC3=O 10.1016/j.bmcl.2007.01.055
CHEMBL245176 93357 None 0 Rat Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay
ChEMBL 377 3 3 2 3.4 O=C(NCC12CC3CC(CC(C3)C1)C2)c1ccc2[nH]c3c(c2c1)CCNC3=O 10.1016/j.bmcl.2007.01.055
54580949 62794 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 360 3 1 6 3.7 C#CC(C)Nc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784079 62794 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 360 3 1 6 3.7 C#CC(C)Nc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
118735970 118982 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay
ChEMBL 387 4 1 4 4.7 Cc1cccc(C(=O)N2CCc3c(sc(NCc4ccccc4)c3C#N)C2)c1 10.1016/j.ejmech.2015.04.060
CHEMBL3422886 118982 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay
ChEMBL 387 4 1 4 4.7 Cc1cccc(C(=O)N2CCc3c(sc(NCc4ccccc4)c3C#N)C2)c1 10.1016/j.ejmech.2015.04.060
44408692 75059 None 0 Rat Functional pIC50 = 5.5 5.5 - 1
Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method
ChEMBL 454 7 0 6 3.4 Cc1c(C(=O)OC(C)C(C)(C)C)cn2c1C(=O)N(CCCN(C)C(=O)c1ccncc1)CC2 10.1016/j.bmcl.2005.11.049
CHEMBL203461 75059 None 0 Rat Functional pIC50 = 5.5 5.5 - 1
Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method
ChEMBL 454 7 0 6 3.4 Cc1c(C(=O)OC(C)C(C)(C)C)cn2c1C(=O)N(CCCN(C)C(=O)c1ccncc1)CC2 10.1016/j.bmcl.2005.11.049
44408600 75951 None 0 Rat Functional pIC50 = 5.5 5.5 - 1
Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method
ChEMBL 363 3 0 6 2.1 Cc1c(C(=O)OC(C)C(C)(C)C)cn2c1C(=O)N(N1CCOCC1)CC2 10.1016/j.bmcl.2005.11.049
CHEMBL205075 75951 None 0 Rat Functional pIC50 = 5.5 5.5 - 1
Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method
ChEMBL 363 3 0 6 2.1 Cc1c(C(=O)OC(C)C(C)(C)C)cn2c1C(=O)N(N1CCOCC1)CC2 10.1016/j.bmcl.2005.11.049
57404255 73237 None 1 Human Functional pIC50 = 7.5 7.5 -18 3
Allosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assayAllosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assay
ChEMBL 302 4 1 4 3.7 COc1ccc(-c2nsc(NC(=O)[C@@H]3C[C@H]3C)c2C)cc1 10.1016/j.bmcl.2012.02.003
CHEMBL2011870 73237 None 1 Human Functional pIC50 = 7.5 7.5 -18 3
Allosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assayAllosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assay
ChEMBL 302 4 1 4 3.7 COc1ccc(-c2nsc(NC(=O)[C@@H]3C[C@H]3C)c2C)cc1 10.1016/j.bmcl.2012.02.003
52941697 18308 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiologyAntagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiology
ChEMBL 425 18 5 5 2.1 CCCC(=O)N[C@@H](CC1CCCCC1)C(=O)NCCCNCCCCNCCCN 10.1021/jm100886h
CHEMBL1270621 18308 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiologyAntagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiology
ChEMBL 425 18 5 5 2.1 CCCC(=O)N[C@@H](CC1CCCCC1)C(=O)NCCCNCCCCNCCCN 10.1021/jm100886h
11560185 85101 None 0 Human Functional pIC50 = 7.5 7.5 1 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 390 2 0 6 4.1 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(C(F)(F)F)cc4)cnc3c12 10.1021/jm0504407
CHEMBL224375 85101 None 0 Human Functional pIC50 = 7.5 7.5 1 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 390 2 0 6 4.1 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(C(F)(F)F)cc4)cnc3c12 10.1021/jm0504407
73335546 133138 None 0 Human Functional pIC50 = 5.5 5.5 -5 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 472 0 0 4 3.2 O=C1CN=C(n2cnc(C(F)(F)F)c2)C=C2c3cccc(I)c3CCN12 nan
CHEMBL3702411 133138 None 0 Human Functional pIC50 = 5.5 5.5 -5 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 472 0 0 4 3.2 O=C1CN=C(n2cnc(C(F)(F)F)c2)C=C2c3cccc(I)c3CCN12 nan
89980768 133192 None 0 Human Functional pIC50 = 5.5 5.5 -457 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 394 3 0 5 3.3 CO[C@H](C)c1cn(C2=NCC(=O)N3CCc4c(C5CC5)ccc(F)c4C3=C2)cn1 nan
CHEMBL3702466 133192 None 0 Human Functional pIC50 = 5.5 5.5 -457 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 394 3 0 5 3.3 CO[C@H](C)c1cn(C2=NCC(=O)N3CCc4c(C5CC5)ccc(F)c4C3=C2)cn1 nan
46886120 8487 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 349 2 1 7 3.2 Cc1ccc(-n2cnc3c(sc4nc(C5CC5)nc(N)c43)c2=O)cc1 10.1016/j.bmcl.2010.03.004
CHEMBL1093987 8487 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 349 2 1 7 3.2 Cc1ccc(-n2cnc3c(sc4nc(C5CC5)nc(N)c43)c2=O)cc1 10.1016/j.bmcl.2010.03.004
54580947 62781 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 407 4 1 9 3.2 C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc5c(c4)OCCO5)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784066 62781 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 407 4 1 9 3.2 C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc5c(c4)OCCO5)cnc3c12 10.1016/j.bmcl.2009.04.104
45484871 199712 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL 322 4 0 6 3.2 Cc1c(-c2ccc(C(=O)OC(C)C)cc2)nnn1-c1cccnc1 10.1016/j.bmcl.2009.07.145
CHEMBL568449 199712 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL 322 4 0 6 3.2 Cc1c(-c2ccc(C(=O)OC(C)C)cc2)nnn1-c1cccnc1 10.1016/j.bmcl.2009.07.145
11537767 141918 None 0 Rat Functional pIC50 = 7.5 7.5 5 2
Antagonist activity at rat mGluR1 expressed in 1321N1 cellsAntagonist activity at rat mGluR1 expressed in 1321N1 cells
ChEMBL 359 2 0 7 2.6 C[N+](C)([O-])c1ccnc2sc3c(=O)n(N4CCCCCC4)cnc3c12 10.1016/j.bmcl.2006.06.053
CHEMBL386408 141918 None 0 Rat Functional pIC50 = 7.5 7.5 5 2
Antagonist activity at rat mGluR1 expressed in 1321N1 cellsAntagonist activity at rat mGluR1 expressed in 1321N1 cells
ChEMBL 359 2 0 7 2.6 C[N+](C)([O-])c1ccnc2sc3c(=O)n(N4CCCCCC4)cnc3c12 10.1016/j.bmcl.2006.06.053
86711401 125175 None 0 Human Functional pIC50 = 5.5 5.5 -660 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 388 3 0 5 3.4 CCC(=O)c1cccc2c1CCN1C(=O)CN=C(n3cnc(C4CCC4)c3)C=C21 nan
CHEMBL3644404 125175 None 0 Human Functional pIC50 = 5.5 5.5 -660 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 388 3 0 5 3.4 CCC(=O)c1cccc2c1CCN1C(=O)CN=C(n3cnc(C4CCC4)c3)C=C21 nan
86711388 125194 None 0 Human Functional pIC50 = 5.5 5.5 -186 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 399 2 0 6 3.4 Cc1nc(-c2cccc3c2CCN2C(=O)CN=C(n4cnc(C5CC5)c4)C=C32)co1 nan
CHEMBL3644423 125194 None 0 Human Functional pIC50 = 5.5 5.5 -186 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 399 2 0 6 3.4 Cc1nc(-c2cccc3c2CCN2C(=O)CN=C(n4cnc(C5CC5)c4)C=C32)co1 nan
122196127 124327 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 376 4 1 5 3.7 COc1cc(N2C(=O)c3ccccc3C2=O)ccc1NC(=O)c1occc1C 10.1016/j.bmcl.2015.10.013
CHEMBL3634449 124327 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 376 4 1 5 3.7 COc1cc(N2C(=O)c3ccccc3C2=O)ccc1NC(=O)c1occc1C 10.1016/j.bmcl.2015.10.013
86711405 125178 None 0 Human Functional pIC50 = 5.5 5.5 -123 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 388 3 1 5 2.9 O=C1CN=C(n2cnc(C(O)C3CC3)c2)C=C2c3cccc(C4CC4)c3CCN12 nan
CHEMBL3644407 125178 None 0 Human Functional pIC50 = 5.5 5.5 -123 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 388 3 1 5 2.9 O=C1CN=C(n2cnc(C(O)C3CC3)c2)C=C2c3cccc(C4CC4)c3CCN12 nan
11594849 85032 None 0 Human Functional pIC50 = 6.5 6.5 1 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 316 4 0 6 3.4 CCC(CC)n1cnc2c(sc3nccc(N(C)C)c32)c1=O 10.1021/jm0504407
CHEMBL223819 85032 None 0 Human Functional pIC50 = 6.5 6.5 1 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 316 4 0 6 3.4 CCC(CC)n1cnc2c(sc3nccc(N(C)C)c32)c1=O 10.1021/jm0504407
127033447 139127 None 0 Rat Functional pIC50 = 6.5 6.5 10 2
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 269 3 1 5 3.1 CC(C)(C)CCNc1ncnc2c1nn1ccccc21 10.1016/j.bmcl.2016.03.026
CHEMBL3786024 139127 None 0 Rat Functional pIC50 = 6.5 6.5 10 2
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 269 3 1 5 3.1 CC(C)(C)CCNc1ncnc2c1nn1ccccc21 10.1016/j.bmcl.2016.03.026
16117432 71061 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 352 4 1 7 3.4 CCNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951885 71061 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 352 4 1 7 3.4 CCNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
122196098 124300 None 0 Human Functional pIC50 = 7.5 7.5 19 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 382 3 1 4 3.9 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(F)c1 10.1016/j.bmcl.2015.10.013
CHEMBL3634421 124300 None 0 Human Functional pIC50 = 7.5 7.5 19 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 382 3 1 4 3.9 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(F)c1 10.1016/j.bmcl.2015.10.013
122196113 124314 None 0 Human Functional pIC50 = 7.5 7.5 32 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 381 3 1 5 3.7 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)nc1 10.1016/j.bmcl.2015.10.013
CHEMBL3634435 124314 None 0 Human Functional pIC50 = 7.5 7.5 32 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 381 3 1 5 3.7 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)nc1 10.1016/j.bmcl.2015.10.013
89980374 125188 None 0 Human Functional pIC50 = 5.5 5.5 -47 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 350 3 0 5 2.4 COC(C)c1cccc2c1CCN1C(=O)CN=C(c3ccn(C)n3)C=C21 nan
CHEMBL3644417 125188 None 0 Human Functional pIC50 = 5.5 5.5 -47 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 350 3 0 5 2.4 COC(C)c1cccc2c1CCN1C(=O)CN=C(c3ccn(C)n3)C=C21 nan
73335440 133120 None 0 Human Functional pIC50 = 5.5 5.5 -107 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 386 3 0 6 2.9 CC(C)n1cc(C2=NCC(=O)N3CCc4c(cccc4-n4cccn4)C3=C2)cn1 nan
CHEMBL3702393 133120 None 0 Human Functional pIC50 = 5.5 5.5 -107 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 386 3 0 6 2.9 CC(C)n1cc(C2=NCC(=O)N3CCc4c(cccc4-n4cccn4)C3=C2)cn1 nan
1382 1190 None 28 Human Functional pIC50 = 5.5 5.5 -1 3
Inhibition of Quisqualate-Induced PI Hydrolysis measured in CHO Metabotropic glutamate receptor 1 Expressing CellsInhibition of Quisqualate-Induced PI Hydrolysis measured in CHO Metabotropic glutamate receptor 1 Expressing Cells
ChEMBL 247 2 1 5 1.6 CCOC(=O)C12CC2/C(=N\O)/c2c(O1)cccc2 10.1021/jm0009944
6278000 1190 None 28 Human Functional pIC50 = 5.5 5.5 -1 3
Inhibition of Quisqualate-Induced PI Hydrolysis measured in CHO Metabotropic glutamate receptor 1 Expressing CellsInhibition of Quisqualate-Induced PI Hydrolysis measured in CHO Metabotropic glutamate receptor 1 Expressing Cells
ChEMBL 247 2 1 5 1.6 CCOC(=O)C12CC2/C(=N\O)/c2c(O1)cccc2 10.1021/jm0009944
CHEMBL327783 1190 None 28 Human Functional pIC50 = 5.5 5.5 -1 3
Inhibition of Quisqualate-Induced PI Hydrolysis measured in CHO Metabotropic glutamate receptor 1 Expressing CellsInhibition of Quisqualate-Induced PI Hydrolysis measured in CHO Metabotropic glutamate receptor 1 Expressing Cells
ChEMBL 247 2 1 5 1.6 CCOC(=O)C12CC2/C(=N\O)/c2c(O1)cccc2 10.1021/jm0009944
127033447 139127 None 0 Rat Functional pIC50 = 6.5 6.5 10 2
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 269 3 1 5 3.1 CC(C)(C)CCNc1ncnc2c1nn1ccccc21 10.1016/j.bmcl.2016.03.026
CHEMBL3786024 139127 None 0 Rat Functional pIC50 = 6.5 6.5 10 2
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 269 3 1 5 3.1 CC(C)(C)CCNc1ncnc2c1nn1ccccc21 10.1016/j.bmcl.2016.03.026
71683127 91069 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 364 2 0 4 3.2 C[C@@H]1CN(c2ncccc2C#N)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
CHEMBL2397344 91069 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 364 2 0 4 3.2 C[C@@H]1CN(c2ncccc2C#N)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
71683127 91069 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 364 2 0 4 3.2 C[C@@H]1CN(c2ncccc2C#N)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
CHEMBL2397344 91069 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 364 2 0 4 3.2 C[C@@H]1CN(c2ncccc2C#N)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
16118943 71009 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 336 3 0 5 4.2 CCc1ccc(-n2ccc3c(sc4nccc(OC)c43)c2=O)cc1 10.1016/j.bmcl.2011.12.131
CHEMBL1951675 71009 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 336 3 0 5 4.2 CCc1ccc(-n2ccc3c(sc4nccc(OC)c43)c2=O)cc1 10.1016/j.bmcl.2011.12.131
86711359 133110 None 0 Human Functional pIC50 = 7.5 7.5 -5 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 418 1 0 4 2.3 Cn1ccc(C2=NCC(=O)N3CCc4c(I)cccc4C3=C2)n1 nan
CHEMBL3702383 133110 None 0 Human Functional pIC50 = 7.5 7.5 -5 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 418 1 0 4 2.3 Cn1ccc(C2=NCC(=O)N3CCc4c(I)cccc4C3=C2)n1 nan
44442428 93656 None 0 Human Functional pIC50 = 6.5 6.5 27 2
Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay
ChEMBL 350 2 0 5 3.8 Cc1ccccc1-n1ncc2c(=O)n(-c3ccc(Cl)cc3)c(C)nc21 10.1016/j.bmcl.2007.05.028
CHEMBL246611 93656 None 0 Human Functional pIC50 = 6.5 6.5 27 2
Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay
ChEMBL 350 2 0 5 3.8 Cc1ccccc1-n1ncc2c(=O)n(-c3ccc(Cl)cc3)c(C)nc21 10.1016/j.bmcl.2007.05.028
73335130 133096 None 0 Human Functional pIC50 = 5.5 5.5 -1 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 386 2 0 3 3.9 COc1cccc2c1CCN1C(=O)CN=C(c3cccc(C(F)(F)F)c3)C=C21 nan
CHEMBL3702369 133096 None 0 Human Functional pIC50 = 5.5 5.5 -1 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 386 2 0 3 3.9 COc1cccc2c1CCN1C(=O)CN=C(c3cccc(C(F)(F)F)c3)C=C21 nan
76325411 105657 None 0 Human Functional pIC50 = 4.5 4.5 -1548 2
Negative allosteric modulation of human mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium flux after 16 to 24 hrs by FLIPR assayNegative allosteric modulation of human mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium flux after 16 to 24 hrs by FLIPR assay
ChEMBL 353 6 1 6 2.8 CCC(C)NC(=O)c1nn(C)c2nc(OCc3cccc(C)n3)ccc12 10.1021/jm401622k
CHEMBL3122221 105657 None 0 Human Functional pIC50 = 4.5 4.5 -1548 2
Negative allosteric modulation of human mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium flux after 16 to 24 hrs by FLIPR assayNegative allosteric modulation of human mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium flux after 16 to 24 hrs by FLIPR assay
ChEMBL 353 6 1 6 2.8 CCC(C)NC(=O)c1nn(C)c2nc(OCc3cccc(C)n3)ccc12 10.1021/jm401622k
54582007 62796 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 402 5 1 6 4.9 C#CC(CC)(CC)Nc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784081 62796 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 402 5 1 6 4.9 C#CC(CC)(CC)Nc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
71682645 91078 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 343 2 0 3 4.0 C[C@@H]1CN(c2ccccn2)CCN1C(=O)[C@H]1CC[C@H](C(C)(C)C)CC1 10.1016/j.bmcl.2013.05.020
CHEMBL2397364 91078 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 343 2 0 3 4.0 C[C@@H]1CN(c2ccccn2)CCN1C(=O)[C@H]1CC[C@H](C(C)(C)C)CC1 10.1016/j.bmcl.2013.05.020
72163839 92058 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 368 1 0 3 3.6 O=C(N1CCC2(CCCCC2)CC1)N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1 10.1016/j.bmcl.2013.07.029
CHEMBL2418361 92058 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 368 1 0 3 3.6 O=C(N1CCC2(CCCCC2)CC1)N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1 10.1016/j.bmcl.2013.07.029
71682645 91078 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 343 2 0 3 4.0 C[C@@H]1CN(c2ccccn2)CCN1C(=O)[C@H]1CC[C@H](C(C)(C)C)CC1 10.1016/j.bmcl.2013.05.020
CHEMBL2397364 91078 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 343 2 0 3 4.0 C[C@@H]1CN(c2ccccn2)CCN1C(=O)[C@H]1CC[C@H](C(C)(C)C)CC1 10.1016/j.bmcl.2013.05.020
72163839 92058 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 368 1 0 3 3.6 O=C(N1CCC2(CCCCC2)CC1)N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1 10.1016/j.bmcl.2013.07.029
CHEMBL2418361 92058 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 368 1 0 3 3.6 O=C(N1CCC2(CCCCC2)CC1)N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1 10.1016/j.bmcl.2013.07.029
11639176 84881 None 0 Human Functional pIC50 = 7.4 7.4 1 3
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 364 4 0 6 4.0 CCc1ccc(-n2cnc3c(sc4nccc(N(C)CC)c43)c2=O)cc1 10.1021/jm0504407
CHEMBL223543 84881 None 0 Human Functional pIC50 = 7.4 7.4 1 3
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 364 4 0 6 4.0 CCc1ccc(-n2cnc3c(sc4nccc(N(C)CC)c43)c2=O)cc1 10.1021/jm0504407
16659642 90254 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay
ChEMBL 353 1 1 6 3.5 O=c1c2sc3ncc4cn[nH]c4c3c2ncn1-c1ccc(Cl)cc1 10.1021/jm070590c
CHEMBL238263 90254 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay
ChEMBL 353 1 1 6 3.5 O=c1c2sc3ncc4cn[nH]c4c3c2ncn1-c1ccc(Cl)cc1 10.1021/jm070590c
78324870 114399 None 4 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay
ChEMBL 338 2 0 4 4.8 O=c1c2scc(-c3ccccc3)c2ncn1-c1cccc(Cl)c1 10.1016/j.ejmech.2014.08.027
CHEMBL3330804 114399 None 4 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay
ChEMBL 338 2 0 4 4.8 O=c1c2scc(-c3ccccc3)c2ncn1-c1cccc(Cl)c1 10.1016/j.ejmech.2014.08.027
44431055 166695 None 0 Rat Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay
ChEMBL 306 3 2 2 3.6 CC(Oc1ccc2[nH]c3c(c2c1)CCNC3=O)c1ccccc1 10.1016/j.bmcl.2007.01.055
CHEMBL428040 166695 None 0 Rat Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay
ChEMBL 306 3 2 2 3.6 CC(Oc1ccc2[nH]c3c(c2c1)CCNC3=O)c1ccccc1 10.1016/j.bmcl.2007.01.055
73336123 133169 None 0 Human Functional pIC50 = 5.4 5.4 -114 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 415 2 0 6 3.9 Cc1ncc(-c2cccc3c2CCN2C(=O)CN=C(n4cnc(C5CC5)c4)C=C32)s1 nan
CHEMBL3702441 133169 None 0 Human Functional pIC50 = 5.4 5.4 -114 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 415 2 0 6 3.9 Cc1ncc(-c2cccc3c2CCN2C(=O)CN=C(n4cnc(C5CC5)c4)C=C32)s1 nan
122196111 124312 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 347 3 1 5 3.0 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)nc1 10.1016/j.bmcl.2015.10.013
CHEMBL3634433 124312 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 347 3 1 5 3.0 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)nc1 10.1016/j.bmcl.2015.10.013
67180972 73245 None 0 Human Functional pIC50 = 7.4 7.4 169 2
Allosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assayAllosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assay
ChEMBL 340 3 1 3 5.0 Cc1c(-c2ccc(Cl)c(Cl)c2)nsc1NC(=O)[C@@H]1C[C@H]1C 10.1016/j.bmcl.2012.02.003
CHEMBL2011878 73245 None 0 Human Functional pIC50 = 7.4 7.4 169 2
Allosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assayAllosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assay
ChEMBL 340 3 1 3 5.0 Cc1c(-c2ccc(Cl)c(Cl)c2)nsc1NC(=O)[C@@H]1C[C@H]1C 10.1016/j.bmcl.2012.02.003
11717319 143581 None 0 Human Functional pIC50 = 7.4 7.4 1 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 353 3 0 8 2.5 COc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cn1 10.1021/jm0504407
CHEMBL389870 143581 None 0 Human Functional pIC50 = 7.4 7.4 1 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 353 3 0 8 2.5 COc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cn1 10.1021/jm0504407
11674352 175269 None 0 Human Functional pIC50 = 7.4 7.4 4 3
Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 331 3 0 6 2.4 CC(C)OC(=O)N1CC=C(c2cn(-c3cccnc3F)nn2)CC1 10.1016/j.bmc.2008.09.060
CHEMBL457026 175269 None 0 Human Functional pIC50 = 7.4 7.4 4 3
Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 331 3 0 6 2.4 CC(C)OC(=O)N1CC=C(c2cn(-c3cccnc3F)nn2)CC1 10.1016/j.bmc.2008.09.060
44588386 176866 None 0 Mouse Functional pIC50 = 7.4 7.4 -2 3
Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 344 2 0 5 3.4 CC(C)(C)OC(=O)N1CC=C(c2cn(-c3cccc(F)c3)nn2)CC1 10.1016/j.bmc.2008.09.060
CHEMBL460391 176866 None 0 Mouse Functional pIC50 = 7.4 7.4 -2 3
Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 344 2 0 5 3.4 CC(C)(C)OC(=O)N1CC=C(c2cn(-c3cccc(F)c3)nn2)CC1 10.1016/j.bmc.2008.09.060
25183673 122266 None 0 Rat Functional pIC50 = 7.4 7.4 -13 2
Negative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysisNegative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysis
ChEMBL 319 2 0 4 3.6 O=[N+]([O-])c1cccnc1N1CCC(=CC#Cc2ccccc2)CC1 10.1016/j.bmc.2015.05.008
CHEMBL3597592 122266 None 0 Rat Functional pIC50 = 7.4 7.4 -13 2
Negative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysisNegative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysis
ChEMBL 319 2 0 4 3.6 O=[N+]([O-])c1cccnc1N1CCC(=CC#Cc2ccccc2)CC1 10.1016/j.bmc.2015.05.008
44408471 166095 None 0 Rat Functional pIC50 = 7.4 7.4 - 1
Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method
ChEMBL 320 4 0 4 3.3 CCCN1CCn2cc(C(=O)OC(C)C(C)(C)C)c(C)c2C1=O 10.1016/j.bmcl.2005.11.049
CHEMBL425405 166095 None 0 Rat Functional pIC50 = 7.4 7.4 - 1
Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method
ChEMBL 320 4 0 4 3.3 CCCN1CCn2cc(C(=O)OC(C)C(C)(C)C)c(C)c2C1=O 10.1016/j.bmcl.2005.11.049
45484928 199713 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL 340 4 0 5 3.9 Cc1c(-c2ccc(C(=O)c3ccccc3)cc2)nnn1-c1cccnc1 10.1016/j.bmcl.2009.07.145
CHEMBL568450 199713 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL 340 4 0 5 3.9 Cc1c(-c2ccc(C(=O)c3ccccc3)cc2)nnn1-c1cccnc1 10.1016/j.bmcl.2009.07.145
5752613 198644 None 8 Rat Functional pIC50 = 4.4 4.4 - 1
Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting
ChEMBL 337 4 0 3 5.1 COc1ccc(C(=O)/C=C/c2cc3ccc(C)cc3nc2Cl)cc1 10.1016/j.bmc.2009.05.072
CHEMBL561391 198644 None 8 Rat Functional pIC50 = 4.4 4.4 - 1
Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting
ChEMBL 337 4 0 3 5.1 COc1ccc(C(=O)/C=C/c2cc3ccc(C)cc3nc2Cl)cc1 10.1016/j.bmc.2009.05.072
67424364 89099 None 0 Human Functional pIC50 = 6.4 6.4 -10 2
Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay
ChEMBL 417 5 1 6 5.2 CC(C)c1cccc(-c2c(-c3ccc4nn(C)cc4c3)nsc2NC(=O)C2CC2)n1 10.1016/j.bmcl.2013.01.009
CHEMBL2334989 89099 None 0 Human Functional pIC50 = 6.4 6.4 -10 2
Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay
ChEMBL 417 5 1 6 5.2 CC(C)c1cccc(-c2c(-c3ccc4nn(C)cc4c3)nsc2NC(=O)C2CC2)n1 10.1016/j.bmcl.2013.01.009
CHEMBL2365000 89099 None 0 Human Functional pIC50 = 6.4 6.4 -10 2
Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay
ChEMBL 417 5 1 6 5.2 CC(C)c1cccc(-c2c(-c3ccc4nn(C)cc4c3)nsc2NC(=O)C2CC2)n1 10.1016/j.bmcl.2013.01.009
720635 5865 None 7 Rat Functional pIC50 = 6.4 6.4 -1 2
Antagonist activity at rat mGluR1 expressed in BHK cells by calcium mobilization assayAntagonist activity at rat mGluR1 expressed in BHK cells by calcium mobilization assay
ChEMBL 333 2 1 3 4.8 Clc1cccc(Nc2ncnc3ccc(Br)cc23)c1 10.1016/j.bmcl.2009.10.024
CHEMBL1079374 5865 None 7 Rat Functional pIC50 = 6.4 6.4 -1 2
Antagonist activity at rat mGluR1 expressed in BHK cells by calcium mobilization assayAntagonist activity at rat mGluR1 expressed in BHK cells by calcium mobilization assay
ChEMBL 333 2 1 3 4.8 Clc1cccc(Nc2ncnc3ccc(Br)cc23)c1 10.1016/j.bmcl.2009.10.024
71680758 91071 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 364 2 0 4 3.2 C[C@@H]1CN(c2ccncc2C#N)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
CHEMBL2397346 91071 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 364 2 0 4 3.2 C[C@@H]1CN(c2ccncc2C#N)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
44408605 74458 None 0 Rat Functional pIC50 = 6.4 6.4 - 1
Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method
ChEMBL 421 5 1 6 3.4 Cc1c(C(=O)OC(C)C(C)(C)C)cn2c1C(=O)N(CCNC(=O)OC(C)(C)C)CC2 10.1016/j.bmcl.2005.11.049
CHEMBL202683 74458 None 0 Rat Functional pIC50 = 6.4 6.4 - 1
Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method
ChEMBL 421 5 1 6 3.4 Cc1c(C(=O)OC(C)C(C)(C)C)cn2c1C(=O)N(CCNC(=O)OC(C)(C)C)CC2 10.1016/j.bmcl.2005.11.049
44408568 75277 None 0 Rat Functional pIC50 = 6.4 6.4 - 1
Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method
ChEMBL 406 7 2 5 2.6 CCNC(=O)NCCCN1CCn2cc(C(=O)OC(C)C(C)(C)C)c(C)c2C1=O 10.1016/j.bmcl.2005.11.049
CHEMBL203688 75277 None 0 Rat Functional pIC50 = 6.4 6.4 - 1
Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method
ChEMBL 406 7 2 5 2.6 CCNC(=O)NCCCN1CCn2cc(C(=O)OC(C)C(C)(C)C)c(C)c2C1=O 10.1016/j.bmcl.2005.11.049
44408569 139895 None 0 Rat Functional pIC50 = 6.4 6.4 - 1
Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method
ChEMBL 440 7 1 6 3.1 Cc1c(C(=O)OC(C)C(C)(C)C)cn2c1C(=O)N(CCCNC(=O)c1ccncc1)CC2 10.1016/j.bmcl.2005.11.049
CHEMBL379882 139895 None 0 Rat Functional pIC50 = 6.4 6.4 - 1
Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method
ChEMBL 440 7 1 6 3.1 Cc1c(C(=O)OC(C)C(C)(C)C)cn2c1C(=O)N(CCCNC(=O)c1ccncc1)CC2 10.1016/j.bmcl.2005.11.049
71680758 91071 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 364 2 0 4 3.2 C[C@@H]1CN(c2ccncc2C#N)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
CHEMBL2397346 91071 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 364 2 0 4 3.2 C[C@@H]1CN(c2ccncc2C#N)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
44431057 87869 None 0 Rat Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay
ChEMBL 292 3 2 2 3.0 O=C1NCCc2c1[nH]c1cccc(OCc3ccccc3)c21 10.1016/j.bmcl.2007.01.055
CHEMBL233851 87869 None 0 Rat Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay
ChEMBL 292 3 2 2 3.0 O=C1NCCc2c1[nH]c1cccc(OCc3ccccc3)c21 10.1016/j.bmcl.2007.01.055
57559545 83858 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 341 2 0 7 2.6 CN(C)c1ncnc2sc3c(=O)n(-c4ccc(F)cc4)cnc3c12 10.1016/j.bmcl.2012.09.048
CHEMBL2205924 83858 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 341 2 0 7 2.6 CN(C)c1ncnc2sc3c(=O)n(-c4ccc(F)cc4)cnc3c12 10.1016/j.bmcl.2012.09.048
11574901 85258 None 0 Human Functional pIC50 = 8.4 8.4 1 3
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 400 2 0 6 3.8 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12 10.1021/jm0504407
CHEMBL225590 85258 None 0 Human Functional pIC50 = 8.4 8.4 1 3
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 400 2 0 6 3.8 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12 10.1021/jm0504407
54585403 62679 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 352 4 1 6 3.7 C=CCNc1ccnc2sc3c(=O)n(-c4ccc(F)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1783863 62679 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 352 4 1 6 3.7 C=CCNc1ccnc2sc3c(=O)n(-c4ccc(F)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
16118397 71056 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 367 3 1 5 4.8 O=c1c2sc3nccc(NC4CC4)c3c2ccn1-c1ccc(Cl)cc1 10.1016/j.bmcl.2011.12.131
CHEMBL1951880 71056 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 367 3 1 5 4.8 O=c1c2sc3nccc(NC4CC4)c3c2ccn1-c1ccc(Cl)cc1 10.1016/j.bmcl.2011.12.131
54582003 62774 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 349 4 1 7 3.4 C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccccc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784059 62774 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 349 4 1 7 3.4 C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccccc4)cnc3c12 10.1016/j.bmcl.2009.04.104
16118120 70994 None 0 Human Functional pIC50 = 8.3 8.3 257 2
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 335 2 0 5 4.0 Cc1ccc(-n2ccc3c(sc4nccc(N(C)C)c43)c2=O)cc1 10.1016/j.bmcl.2011.12.131
CHEMBL1951659 70994 None 0 Human Functional pIC50 = 8.3 8.3 257 2
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 335 2 0 5 4.0 Cc1ccc(-n2ccc3c(sc4nccc(N(C)C)c43)c2=O)cc1 10.1016/j.bmcl.2011.12.131
45484965 201279 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL 287 2 0 5 3.2 Cc1c(-c2ccc3ncccc3c2)nnn1-c1cccnc1 10.1016/j.bmcl.2009.07.145
CHEMBL583590 201279 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL 287 2 0 5 3.2 Cc1c(-c2ccc3ncccc3c2)nnn1-c1cccnc1 10.1016/j.bmcl.2009.07.145
16659646 89991 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay
ChEMBL 348 2 1 6 3.5 COc1ccc(-n2cnc3c(sc4ncc5cc[nH]c5c43)c2=O)cc1 10.1021/jm070590c
CHEMBL238079 89991 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay
ChEMBL 348 2 1 6 3.5 COc1ccc(-n2cnc3c(sc4ncc5cc[nH]c5c43)c2=O)cc1 10.1021/jm070590c
24777581 94768 None 0 Rat Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 297 2 1 4 3.9 CC1(C)CC(=O)c2cc(C#N)c(NC3CCCCC3)nc2C1 10.1021/jm0611298
CHEMBL252940 94768 None 0 Rat Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 297 2 1 4 3.9 CC1(C)CC(=O)c2cc(C#N)c(NC3CCCCC3)nc2C1 10.1021/jm0611298
1297 170355 None 23 Human Functional pIC50 = 4.4 4.4 1 2
Ability to inhibit mGluR1-alpha-mediated PI (phospho inositol) hydrolysis was determined at BHK cells at 100 Micro M ConcentrationAbility to inhibit mGluR1-alpha-mediated PI (phospho inositol) hydrolysis was determined at BHK cells at 100 Micro M Concentration
ChEMBL 211 3 4 4 0.2 NC(C(=O)O)c1ccc(C(=O)O)c(O)c1 10.1021/jm00019a002
CHEMBL444589 170355 None 23 Human Functional pIC50 = 4.4 4.4 1 2
Ability to inhibit mGluR1-alpha-mediated PI (phospho inositol) hydrolysis was determined at BHK cells at 100 Micro M ConcentrationAbility to inhibit mGluR1-alpha-mediated PI (phospho inositol) hydrolysis was determined at BHK cells at 100 Micro M Concentration
ChEMBL 211 3 4 4 0.2 NC(C(=O)O)c1ccc(C(=O)O)c(O)c1 10.1021/jm00019a002
1374 2081 None 25 Human Functional pIC50 = 4.4 4.4 -15 4
Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor
ChEMBL 211 3 4 4 0.2 N[C@@H](c1ccc(c(c1)O)C(=O)O)C(=O)O 10.1021/jm060950g
5311455 2081 None 25 Human Functional pIC50 = 4.4 4.4 -15 4
Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor
ChEMBL 211 3 4 4 0.2 N[C@@H](c1ccc(c(c1)O)C(=O)O)C(=O)O 10.1021/jm060950g
CHEMBL39372 2081 None 25 Human Functional pIC50 = 4.4 4.4 -15 4
Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor
ChEMBL 211 3 4 4 0.2 N[C@@H](c1ccc(c(c1)O)C(=O)O)C(=O)O 10.1021/jm060950g
5311460 18982 None 18 Human Functional pIC50 = 4.4 4.4 - 1
Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor
ChEMBL 211 3 4 4 0.2 N[C@H](C(=O)O)c1ccc(O)c(C(=O)O)c1 10.1021/jm060950g
CHEMBL128772 18982 None 18 Human Functional pIC50 = 4.4 4.4 - 1
Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor
ChEMBL 211 3 4 4 0.2 N[C@H](C(=O)O)c1ccc(O)c(C(=O)O)c1 10.1021/jm060950g
89979971 125186 None 0 Human Functional pIC50 = 6.4 6.4 -15 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 414 2 0 6 3.0 O=C1CN=C(n2cnc(C3CC3)c2)C=C2c3cccc(-c4cncc(F)n4)c3CCN12 nan
CHEMBL3644415 125186 None 0 Human Functional pIC50 = 6.4 6.4 -15 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 414 2 0 6 3.0 O=C1CN=C(n2cnc(C3CC3)c2)C=C2c3cccc(-c4cncc(F)n4)c3CCN12 nan
11552320 136914 None 0 Human Functional pIC50 = 6.4 6.4 1 3
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 364 3 0 6 4.2 CC(C)c1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1 10.1021/jm0504407
CHEMBL374167 136914 None 0 Human Functional pIC50 = 6.4 6.4 1 3
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 364 3 0 6 4.2 CC(C)c1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1 10.1021/jm0504407
78324869 114398 None 4 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay
ChEMBL 338 2 0 4 4.8 O=c1c2scc(-c3ccccc3)c2ncn1-c1ccccc1Cl 10.1016/j.ejmech.2014.08.027
CHEMBL3330803 114398 None 4 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay
ChEMBL 338 2 0 4 4.8 O=c1c2scc(-c3ccccc3)c2ncn1-c1ccccc1Cl 10.1016/j.ejmech.2014.08.027
78324866 114208 None 4 Human Functional pIC50 = 6.4 6.4 - 1
FLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and diluteFLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and dilute
ChEMBL 322 2 0 4 4.3 O=c1c2scc(-c3ccccc3)c2ncn1-c1ccccc1F nan
CHEMBL3329236 114208 None 4 Human Functional pIC50 = 6.4 6.4 - 1
FLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and diluteFLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and dilute
ChEMBL 322 2 0 4 4.3 O=c1c2scc(-c3ccccc3)c2ncn1-c1ccccc1F nan
44431053 149833 None 0 Rat Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay
ChEMBL 278 2 2 2 3.2 O=C1NCCc2c1[nH]c1ccc(Oc3ccccc3)cc21 10.1016/j.bmcl.2007.01.055
CHEMBL394810 149833 None 0 Rat Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay
ChEMBL 278 2 2 2 3.2 O=C1NCCc2c1[nH]c1ccc(Oc3ccccc3)cc21 10.1016/j.bmcl.2007.01.055
6419 1045 None 0 Human Functional pIC50 = 6.4 6.4 -20 2
Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay
ChEMBL 431 6 1 6 5.3 CCCc1cccc(n1)c1c(snc1c1ccc2c(c1)cn(n2)C)NC(=O)[C@@H]1C[C@H]1C 10.1016/j.bmcl.2013.01.009
71559428 1045 None 0 Human Functional pIC50 = 6.4 6.4 -20 2
Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay
ChEMBL 431 6 1 6 5.3 CCCc1cccc(n1)c1c(snc1c1ccc2c(c1)cn(n2)C)NC(=O)[C@@H]1C[C@H]1C 10.1016/j.bmcl.2013.01.009
CHEMBL2334980 1045 None 0 Human Functional pIC50 = 6.4 6.4 -20 2
Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay
ChEMBL 431 6 1 6 5.3 CCCc1cccc(n1)c1c(snc1c1ccc2c(c1)cn(n2)C)NC(=O)[C@@H]1C[C@H]1C 10.1016/j.bmcl.2013.01.009
49788731 18127 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiologyAntagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiology
ChEMBL 523 18 5 5 3.7 NCCCNCCCCNCCCNC(=O)[C@H](CC1CCCCC1)NC(=O)Cc1cccc2ccccc12 10.1021/jm100886h
CHEMBL1269126 18127 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiologyAntagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiology
ChEMBL 523 18 5 5 3.7 NCCCNCCCCNCCCNC(=O)[C@H](CC1CCCCC1)NC(=O)Cc1cccc2ccccc12 10.1021/jm100886h
11660540 85073 None 0 Human Functional pIC50 = 7.4 7.4 1 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 362 4 1 6 4.1 CCc1ccc(-n2cnc3c(sc4nccc(NC5CC5)c43)c2=O)cc1 10.1021/jm0504407
CHEMBL224088 85073 None 0 Human Functional pIC50 = 7.4 7.4 1 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 362 4 1 6 4.1 CCc1ccc(-n2cnc3c(sc4nccc(NC5CC5)c43)c2=O)cc1 10.1021/jm0504407
73058380 125177 None 0 Human Functional pIC50 = 7.4 7.4 -40 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 362 3 1 5 2.0 O=C1CN=C(n2cnc(CCO)c2)C=C2c3cccc(C4CC4)c3CCN12 nan
CHEMBL3644406 125177 None 0 Human Functional pIC50 = 7.4 7.4 -40 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 362 3 1 5 2.0 O=C1CN=C(n2cnc(CCO)c2)C=C2c3cccc(C4CC4)c3CCN12 nan
24777695 155085 None 0 Rat Functional pIC50 = 4.4 4.4 - 1
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 349 2 1 4 4.5 CC1(C)CC(=O)c2cc(C#N)c(NC34CC5CC(CC(C5)C3)C4)nc2C1 10.1021/jm0611298
CHEMBL401331 155085 None 0 Rat Functional pIC50 = 4.4 4.4 - 1
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 349 2 1 4 4.5 CC1(C)CC(=O)c2cc(C#N)c(NC34CC5CC(CC(C5)C3)C4)nc2C1 10.1021/jm0611298
71683125 91067 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 357 2 0 3 3.5 C[C@@H]1CN(c2ccc(F)cn2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
CHEMBL2397342 91067 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 357 2 0 3 3.5 C[C@@H]1CN(c2ccc(F)cn2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
71683125 91067 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 357 2 0 3 3.5 C[C@@H]1CN(c2ccc(F)cn2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
CHEMBL2397342 91067 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 357 2 0 3 3.5 C[C@@H]1CN(c2ccc(F)cn2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
73335642 133151 None 0 Human Functional pIC50 = 5.4 5.4 -123 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 419 4 0 7 2.9 COCCc1cn(C2=NCC(=O)N3CCc4c(cccc4-c4cscn4)C3=C2)cn1 nan
CHEMBL3702424 133151 None 0 Human Functional pIC50 = 5.4 5.4 -123 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 419 4 0 7 2.9 COCCc1cn(C2=NCC(=O)N3CCc4c(cccc4-c4cscn4)C3=C2)cn1 nan
54583474 62686 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 426 4 1 6 4.7 C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1783870 62686 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 426 4 1 6 4.7 C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
11515548 212 None 10 Human Functional pIC50 = 7.4 7.4 -1 3
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 336 2 0 6 3.4 Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(cnc1)N(C)C 10.1021/jm0504407
6355 212 None 10 Human Functional pIC50 = 7.4 7.4 -1 3
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 336 2 0 6 3.4 Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(cnc1)N(C)C 10.1021/jm0504407
CHEMBL223869 212 None 10 Human Functional pIC50 = 7.4 7.4 -1 3
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 336 2 0 6 3.4 Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(cnc1)N(C)C 10.1021/jm0504407
122196094 124296 None 0 Human Functional pIC50 = 7.4 7.4 8 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 364 3 1 4 3.8 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)cc1 10.1016/j.bmcl.2015.10.013
CHEMBL3634417 124296 None 0 Human Functional pIC50 = 7.4 7.4 8 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 364 3 1 4 3.8 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)cc1 10.1016/j.bmcl.2015.10.013
10317627 78553 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Inhibition of Quisqualate-Induced PI Hydrolysis measured in CHO Metabotropic glutamate receptor 1 Expressing CellsInhibition of Quisqualate-Induced PI Hydrolysis measured in CHO Metabotropic glutamate receptor 1 Expressing Cells
ChEMBL 380 5 2 6 1.9 COC(=O)[C@H](Cc1ccccc1)NC(=O)[C@]12C[C@H]1/C(=N\O)c1ccccc1O2 10.1021/jm0009944
CHEMBL2111944 78553 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Inhibition of Quisqualate-Induced PI Hydrolysis measured in CHO Metabotropic glutamate receptor 1 Expressing CellsInhibition of Quisqualate-Induced PI Hydrolysis measured in CHO Metabotropic glutamate receptor 1 Expressing Cells
ChEMBL 380 5 2 6 1.9 COC(=O)[C@H](Cc1ccccc1)NC(=O)[C@]12C[C@H]1/C(=N\O)c1ccccc1O2 10.1021/jm0009944
1373 2475 None 35 Human Functional pIC50 = 5.4 5.4 -1 4
Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor
ChEMBL 209 3 3 3 0.6 OC(=O)c1ccc(cc1)[C@@](C(=O)O)(N)C 10.1021/jm060950g
139055582 2475 None 35 Human Functional pIC50 = 5.4 5.4 -1 4
Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor
ChEMBL 209 3 3 3 0.6 OC(=O)c1ccc(cc1)[C@@](C(=O)O)(N)C 10.1021/jm060950g
446355 2475 None 35 Human Functional pIC50 = 5.4 5.4 -1 4
Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor
ChEMBL 209 3 3 3 0.6 OC(=O)c1ccc(cc1)[C@@](C(=O)O)(N)C 10.1021/jm060950g
CHEMBL257626 2475 None 35 Human Functional pIC50 = 5.4 5.4 -1 4
Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor
ChEMBL 209 3 3 3 0.6 OC(=O)c1ccc(cc1)[C@@](C(=O)O)(N)C 10.1021/jm060950g
DB04256 2475 None 35 Human Functional pIC50 = 5.4 5.4 -1 4
Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor
ChEMBL 209 3 3 3 0.6 OC(=O)c1ccc(cc1)[C@@](C(=O)O)(N)C 10.1021/jm060950g
118735957 118972 None 0 Human Functional pIC50 = 4.4 4.4 - 1
Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay
ChEMBL 405 5 2 5 4.3 CC(C)c1cc(C(=O)N2CCc3c(sc(NCc4ccccc4)c3C#N)C2)[nH]n1 10.1016/j.ejmech.2015.04.060
CHEMBL3422873 118972 None 0 Human Functional pIC50 = 4.4 4.4 - 1
Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay
ChEMBL 405 5 2 5 4.3 CC(C)c1cc(C(=O)N2CCc3c(sc(NCc4ccccc4)c3C#N)C2)[nH]n1 10.1016/j.ejmech.2015.04.060
11501465 85137 None 0 Human Functional pIC50 = 7.4 7.4 1 3
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 364 3 0 6 3.9 CCc1ccc(-n2c(C)nc3c(sc4nccc(N(C)C)c43)c2=O)cc1 10.1021/jm0504407
CHEMBL224673 85137 None 0 Human Functional pIC50 = 7.4 7.4 1 3
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 364 3 0 6 3.9 CCc1ccc(-n2c(C)nc3c(sc4nccc(N(C)C)c43)c2=O)cc1 10.1021/jm0504407
2851338 154689 None 9 Rat Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 306 2 1 2 3.9 O=C(NC12CC3CC(CC(C3)C1)C2)c1ccc2ccccc2n1 10.1021/jm0611298
CHEMBL399161 154689 None 9 Rat Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 306 2 1 2 3.9 O=C(NC12CC3CC(CC(C3)C1)C2)c1ccc2ccccc2n1 10.1021/jm0611298
16659799 146477 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay
ChEMBL 366 1 1 7 3.2 Cc1ccc(-n2cnc3c(sc4ncc5sc(=O)[nH]c5c43)c2=O)cc1 10.1021/jm070590c
CHEMBL392164 146477 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay
ChEMBL 366 1 1 7 3.2 Cc1ccc(-n2cnc3c(sc4ncc5sc(=O)[nH]c5c43)c2=O)cc1 10.1021/jm070590c
78322374 149043 None 0 Human Functional pIC50 = 6.4 6.4 - 1
FLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and diluteFLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and dilute
ChEMBL 382 2 0 6 4.5 O=c1c2scc(-c3ccc4c(c3)OCO4)c2ncn1-c1ccc(Cl)cc1 nan
CHEMBL3942033 149043 None 0 Human Functional pIC50 = 6.4 6.4 - 1
FLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and diluteFLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and dilute
ChEMBL 382 2 0 6 4.5 O=c1c2scc(-c3ccc4c(c3)OCO4)c2ncn1-c1ccc(Cl)cc1 nan
25183668 122268 None 0 Rat Functional pIC50 = 6.4 6.4 -562 2
Negative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysisNegative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysis
ChEMBL 334 2 0 5 3.3 Cc1cccc(C#CC=C2CCN(c3ncccc3[N+](=O)[O-])CC2)n1 10.1016/j.bmc.2015.05.008
CHEMBL3597594 122268 None 0 Rat Functional pIC50 = 6.4 6.4 -562 2
Negative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysisNegative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysis
ChEMBL 334 2 0 5 3.3 Cc1cccc(C#CC=C2CCN(c3ncccc3[N+](=O)[O-])CC2)n1 10.1016/j.bmc.2015.05.008
54584892 62790 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 390 3 1 9 3.0 C#CCNc1ncnc2sc3c(=O)n(-c4ccc5scnc5c4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784075 62790 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 390 3 1 9 3.0 C#CCNc1ncnc2sc3c(=O)n(-c4ccc5scnc5c4)cnc3c12 10.1016/j.bmcl.2009.04.104
11661106 85167 None 0 Human Functional pIC50 = 7.4 7.4 1 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 390 2 0 6 4.4 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4Cl)cnc3c12 10.1021/jm0504407
CHEMBL224898 85167 None 0 Human Functional pIC50 = 7.4 7.4 1 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 390 2 0 6 4.4 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4Cl)cnc3c12 10.1021/jm0504407
78322060 114409 None 4 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay
ChEMBL 348 3 0 5 4.4 COc1ccc(-n2cnc3c(-c4ccccc4C)csc3c2=O)cc1 10.1016/j.ejmech.2014.08.027
CHEMBL3330823 114409 None 4 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay
ChEMBL 348 3 0 5 4.4 COc1ccc(-n2cnc3c(-c4ccccc4C)csc3c2=O)cc1 10.1016/j.ejmech.2014.08.027
89979519 133133 None 0 Human Functional pIC50 = 5.4 5.4 -316 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 388 3 0 4 3.8 COc1cccc(C2=NCC(=O)N3CCc4c(cccc4C4CCCO4)C3=C2)c1 nan
CHEMBL3702406 133133 None 0 Human Functional pIC50 = 5.4 5.4 -316 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 388 3 0 4 3.8 COc1cccc(C2=NCC(=O)N3CCc4c(cccc4C4CCCO4)C3=C2)c1 nan
24777444 94739 None 0 Rat Functional pIC50 = 4.4 4.4 -5 2
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 280 3 1 3 3.8 CC1(C)CC(=O)c2ccc(NCc3ccccc3)nc2C1 10.1021/jm0611298
CHEMBL252735 94739 None 0 Rat Functional pIC50 = 4.4 4.4 -5 2
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 280 3 1 3 3.8 CC1(C)CC(=O)c2ccc(NCc3ccccc3)nc2C1 10.1021/jm0611298
57908404 89135 None 0 Human Functional pIC50 = 5.3 5.3 -102 2
Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay
ChEMBL 417 5 2 5 5.5 CC(C)c1cccc(-c2c(-c3ccc4n[nH]cc4c3)nsc2NC(=O)[C@@H]2C[C@H]2C)n1 10.1016/j.bmcl.2013.01.009
CHEMBL2334987 89135 None 0 Human Functional pIC50 = 5.3 5.3 -102 2
Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay
ChEMBL 417 5 2 5 5.5 CC(C)c1cccc(-c2c(-c3ccc4n[nH]cc4c3)nsc2NC(=O)[C@@H]2C[C@H]2C)n1 10.1016/j.bmcl.2013.01.009
CHEMBL2365401 89135 None 0 Human Functional pIC50 = 5.3 5.3 -102 2
Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay
ChEMBL 417 5 2 5 5.5 CC(C)c1cccc(-c2c(-c3ccc4n[nH]cc4c3)nsc2NC(=O)[C@@H]2C[C@H]2C)n1 10.1016/j.bmcl.2013.01.009
122196107 124309 None 0 Human Functional pIC50 = 7.3 7.3 25 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 376 4 1 5 3.7 COc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2ccccc2C1=O 10.1016/j.bmcl.2015.10.013
CHEMBL3634430 124309 None 0 Human Functional pIC50 = 7.3 7.3 25 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 376 4 1 5 3.7 COc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2ccccc2C1=O 10.1016/j.bmcl.2015.10.013
127033446 139069 None 0 Rat Functional pIC50 = 6.3 6.3 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 295 3 1 5 3.7 C[C@@H](Nc1ncnc2c1nn1ccccc21)C1CCCCC1 10.1016/j.bmcl.2016.03.026
CHEMBL3785386 139069 None 0 Rat Functional pIC50 = 6.3 6.3 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 295 3 1 5 3.7 C[C@@H](Nc1ncnc2c1nn1ccccc21)C1CCCCC1 10.1016/j.bmcl.2016.03.026
44431051 93360 None 0 Rat Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay
ChEMBL 378 2 4 2 3.5 O=C(Nc1ccc2[nH]c3c(c2c1)CCNC3=O)NC12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2007.01.055
CHEMBL245187 93360 None 0 Rat Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay
ChEMBL 378 2 4 2 3.5 O=C(Nc1ccc2[nH]c3c(c2c1)CCNC3=O)NC12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2007.01.055
127033446 139069 None 0 Rat Functional pIC50 = 6.3 6.3 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 295 3 1 5 3.7 C[C@@H](Nc1ncnc2c1nn1ccccc21)C1CCCCC1 10.1016/j.bmcl.2016.03.026
CHEMBL3785386 139069 None 0 Rat Functional pIC50 = 6.3 6.3 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 295 3 1 5 3.7 C[C@@H](Nc1ncnc2c1nn1ccccc21)C1CCCCC1 10.1016/j.bmcl.2016.03.026
122196115 124316 None 0 Human Functional pIC50 = 5.3 5.3 1 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 348 3 1 6 2.4 Cc1ccoc1C(=O)Nc1cnc(N2C(=O)c3ccccc3C2=O)nc1 10.1016/j.bmcl.2015.10.013
CHEMBL3634437 124316 None 0 Human Functional pIC50 = 5.3 5.3 1 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 348 3 1 6 2.4 Cc1ccoc1C(=O)Nc1cnc(N2C(=O)c3ccccc3C2=O)nc1 10.1016/j.bmcl.2015.10.013
16117172 71052 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 364 2 1 7 4.3 CNc1ccnc2sc3c(=O)n(-c4ccc5scnc5c4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951876 71052 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 364 2 1 7 4.3 CNc1ccnc2sc3c(=O)n(-c4ccc5scnc5c4)ccc3c12 10.1016/j.bmcl.2011.12.131
122196091 124293 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 346 3 1 4 3.6 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)cc1 10.1016/j.bmcl.2015.10.013
CHEMBL3634414 124293 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 346 3 1 4 3.6 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)cc1 10.1016/j.bmcl.2015.10.013
45484889 199320 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL 278 3 0 5 2.8 CC(=O)c1ccc(-c2nnn(-c3cccnc3)c2C)cc1 10.1016/j.bmcl.2009.07.145
CHEMBL565972 199320 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL 278 3 0 5 2.8 CC(=O)c1ccc(-c2nnn(-c3cccnc3)c2C)cc1 10.1016/j.bmcl.2009.07.145
118735969 118981 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay
ChEMBL 387 4 1 4 4.7 Cc1ccc(C(=O)N2CCc3c(sc(NCc4ccccc4)c3C#N)C2)cc1 10.1016/j.ejmech.2015.04.060
CHEMBL3422885 118981 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay
ChEMBL 387 4 1 4 4.7 Cc1ccc(C(=O)N2CCc3c(sc(NCc4ccccc4)c3C#N)C2)cc1 10.1016/j.ejmech.2015.04.060
72163584 92066 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 369 2 0 3 3.3 O=C(N1C[C@@H]2CN(c3ccc(F)cn3)C[C@@H]2C1)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.07.029
CHEMBL2418381 92066 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 369 2 0 3 3.3 O=C(N1C[C@@H]2CN(c3ccc(F)cn3)C[C@@H]2C1)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.07.029
72163584 92066 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 369 2 0 3 3.3 O=C(N1C[C@@H]2CN(c3ccc(F)cn3)C[C@@H]2C1)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.07.029
CHEMBL2418381 92066 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 369 2 0 3 3.3 O=C(N1C[C@@H]2CN(c3ccc(F)cn3)C[C@@H]2C1)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.07.029
127031274 139203 None 0 Rat Functional pIC50 = 6.3 6.3 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 335 2 2 6 2.8 OC12CC3CC(C1)CC(Nc1ncnc4c1nn1ccccc41)(C3)C2 10.1016/j.bmcl.2016.03.026
CHEMBL3786767 139203 None 0 Rat Functional pIC50 = 6.3 6.3 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 335 2 2 6 2.8 OC12CC3CC(C1)CC(Nc1ncnc4c1nn1ccccc41)(C3)C2 10.1016/j.bmcl.2016.03.026
122196101 124303 None 0 Human Functional pIC50 = 7.3 7.3 20 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 394 3 1 4 4.6 Cc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(Cl)c2C1=O 10.1016/j.bmcl.2015.10.013
CHEMBL3634424 124303 None 0 Human Functional pIC50 = 7.3 7.3 20 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 394 3 1 4 4.6 Cc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(Cl)c2C1=O 10.1016/j.bmcl.2015.10.013
122196102 124304 None 0 Human Functional pIC50 = 7.3 7.3 22 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 378 3 1 4 4.1 Cc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(F)c2C1=O 10.1016/j.bmcl.2015.10.013
CHEMBL3634425 124304 None 0 Human Functional pIC50 = 7.3 7.3 22 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 378 3 1 4 4.1 Cc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(F)c2C1=O 10.1016/j.bmcl.2015.10.013
122196108 124310 None 0 Human Functional pIC50 = 7.3 7.3 18 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 390 4 1 5 4.0 COc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(C)c2C1=O 10.1016/j.bmcl.2015.10.013
CHEMBL3634431 124310 None 0 Human Functional pIC50 = 7.3 7.3 18 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 390 4 1 5 4.0 COc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(C)c2C1=O 10.1016/j.bmcl.2015.10.013
720466 94843 None 8 Rat Functional pIC50 = 5.3 5.3 12 2
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 322 3 0 4 4.4 CC1(C)CC(=O)c2cc(C#N)c(SCc3ccccc3)nc2C1 10.1021/jm0611298
CHEMBL253349 94843 None 8 Rat Functional pIC50 = 5.3 5.3 12 2
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 322 3 0 4 4.4 CC1(C)CC(=O)c2cc(C#N)c(SCc3ccccc3)nc2C1 10.1021/jm0611298
73335235 133107 None 0 Human Functional pIC50 = 5.3 5.3 -60 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 355 2 0 4 3.6 O=C1CN=C(c2ccco2)C=C2c3cccc(-c4ccncc4)c3CCN12 nan
CHEMBL3702380 133107 None 0 Human Functional pIC50 = 5.3 5.3 -60 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 355 2 0 4 3.6 O=C1CN=C(c2ccco2)C=C2c3cccc(-c4ccncc4)c3CCN12 nan
11681680 142443 None 0 Human Functional pIC50 = 6.3 6.3 1 3
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 342 2 0 6 3.8 CC1CCCC(n2cnc3c(sc4nccc(N(C)C)c43)c2=O)C1 10.1021/jm0504407
CHEMBL388827 142443 None 0 Human Functional pIC50 = 6.3 6.3 1 3
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 342 2 0 6 3.8 CC1CCCC(n2cnc3c(sc4nccc(N(C)C)c43)c2=O)C1 10.1021/jm0504407
127031274 139203 None 0 Rat Functional pIC50 = 6.3 6.3 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 335 2 2 6 2.8 OC12CC3CC(C1)CC(Nc1ncnc4c1nn1ccccc41)(C3)C2 10.1016/j.bmcl.2016.03.026
CHEMBL3786767 139203 None 0 Rat Functional pIC50 = 6.3 6.3 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 335 2 2 6 2.8 OC12CC3CC(C1)CC(Nc1ncnc4c1nn1ccccc41)(C3)C2 10.1016/j.bmcl.2016.03.026
11660511 166238 None 0 Human Functional pIC50 = 7.3 7.3 -1 3
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 361 4 1 7 3.5 CCc1ccc(-n2cnc3c(sc4nccc(NCC#N)c43)c2=O)cc1 10.1021/jm0504407
CHEMBL426190 166238 None 0 Human Functional pIC50 = 7.3 7.3 -1 3
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 361 4 1 7 3.5 CCc1ccc(-n2cnc3c(sc4nccc(NCC#N)c43)c2=O)cc1 10.1021/jm0504407
44588460 175653 None 0 Human Functional pIC50 = 7.3 7.3 3 3
Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 327 2 0 6 2.7 CC(C)(C)OC(=O)N1CC=C(c2cn(-c3ccccn3)nn2)CC1 10.1016/j.bmc.2008.09.060
CHEMBL457872 175653 None 0 Human Functional pIC50 = 7.3 7.3 3 3
Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 327 2 0 6 2.7 CC(C)(C)OC(=O)N1CC=C(c2cn(-c3ccccn3)nn2)CC1 10.1016/j.bmc.2008.09.060
16661409 199691 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 314 3 0 5 3.0 CN(C(=O)c1ccc(F)cc1)c1nc(-c2cnccn2)cs1 10.1016/j.bmcl.2009.07.097
CHEMBL568317 199691 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 314 3 0 5 3.0 CN(C(=O)c1ccc(F)cc1)c1nc(-c2cnccn2)cs1 10.1016/j.bmcl.2009.07.097
16661726 201052 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 313 3 0 4 3.6 CN(C(=O)c1ccc(F)cc1)c1nc(-c2ccncc2)cs1 10.1016/j.bmcl.2009.07.097
CHEMBL578580 201052 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 313 3 0 4 3.6 CN(C(=O)c1ccc(F)cc1)c1nc(-c2ccncc2)cs1 10.1016/j.bmcl.2009.07.097
89980648 125166 None 0 Human Functional pIC50 = 6.3 6.3 -34 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 362 3 0 5 2.7 C=C(C)c1cccc2c1CCN1C(=O)CN=C(n3cnc(COC)c3)C=C21 nan
CHEMBL3644395 125166 None 0 Human Functional pIC50 = 6.3 6.3 -34 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 362 3 0 5 2.7 C=C(C)c1cccc2c1CCN1C(=O)CN=C(n3cnc(COC)c3)C=C21 nan
73334945 133085 None 0 Human Functional pIC50 = 5.3 5.3 -24 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 349 3 0 5 2.3 COc1cc(C2=NCC(=O)N3CCc4c(OC)cccc4C3=C2)ccn1 nan
CHEMBL3702358 133085 None 0 Human Functional pIC50 = 5.3 5.3 -24 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 349 3 0 5 2.3 COc1cc(C2=NCC(=O)N3CCc4c(OC)cccc4C3=C2)ccn1 nan
78320479 114401 None 4 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay
ChEMBL 318 2 0 4 4.4 Cc1ccccc1-n1cnc2c(-c3ccccc3)csc2c1=O 10.1016/j.ejmech.2014.08.027
CHEMBL3330806 114401 None 4 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay
ChEMBL 318 2 0 4 4.4 Cc1ccccc1-n1cnc2c(-c3ccccc3)csc2c1=O 10.1016/j.ejmech.2014.08.027
57881754 83536 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 371 3 0 8 2.6 COc1ccc(-n2cnc3c(sc4ncnc(N(C)C)c43)c2=O)cc1F 10.1016/j.bmcl.2012.09.048
CHEMBL2203308 83536 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 371 3 0 8 2.6 COc1ccc(-n2cnc3c(sc4ncnc(N(C)C)c43)c2=O)cc1F 10.1016/j.bmcl.2012.09.048
57559597 83740 None 0 Human Functional pIC50 = 8.3 8.3 1995 2
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 339 3 1 8 2.4 CNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12 10.1016/j.bmcl.2012.09.048
CHEMBL2205378 83740 None 0 Human Functional pIC50 = 8.3 8.3 1995 2
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 339 3 1 8 2.4 CNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12 10.1016/j.bmcl.2012.09.048
16730193 83851 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 379 4 0 8 3.0 COc1ccc(-n2cnc3c(sc4ncnc(N(C)C5CC5)c43)c2=O)cc1 10.1016/j.bmcl.2012.09.048
CHEMBL2205917 83851 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 379 4 0 8 3.0 COc1ccc(-n2cnc3c(sc4ncnc(N(C)C5CC5)c43)c2=O)cc1 10.1016/j.bmcl.2012.09.048
744275 84878 None 12 Human Functional pIC50 = 8.3 8.3 1 3
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 336 2 0 6 3.4 Cc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1 10.1021/jm0504407
CHEMBL223496 84878 None 12 Human Functional pIC50 = 8.3 8.3 1 3
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 336 2 0 6 3.4 Cc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1 10.1021/jm0504407
11609353 85127 None 0 Human Functional pIC50 = 8.3 8.3 1 3
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 314 2 0 6 3.2 CN(C)c1ccnc2sc3c(=O)n(C4CCCC4)cnc3c12 10.1021/jm0504407
CHEMBL224617 85127 None 0 Human Functional pIC50 = 8.3 8.3 1 3
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 314 2 0 6 3.2 CN(C)c1ccnc2sc3c(=O)n(C4CCCC4)cnc3c12 10.1021/jm0504407
16118121 71003 None 0 Human Functional pIC50 = 8.3 8.3 263 2
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 378 2 0 7 4.3 CN(C)c1ccnc2sc3c(=O)n(-c4ccc5scnc5c4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951668 71003 None 0 Human Functional pIC50 = 8.3 8.3 263 2
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 378 2 0 7 4.3 CN(C)c1ccnc2sc3c(=O)n(-c4ccc5scnc5c4)ccc3c12 10.1016/j.bmcl.2011.12.131
11530404 210 None 14 Rat Functional pIC50 = 8.3 8.3 -1 4
Antagonist activity at rat mGluR1 expressed in 1321N1 cellsAntagonist activity at rat mGluR1 expressed in 1321N1 cells
ChEMBL 350 3 0 6 3.6 CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C 10.1016/j.bmcl.2006.06.053
6211 210 None 14 Rat Functional pIC50 = 8.3 8.3 -1 4
Antagonist activity at rat mGluR1 expressed in 1321N1 cellsAntagonist activity at rat mGluR1 expressed in 1321N1 cells
ChEMBL 350 3 0 6 3.6 CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C 10.1016/j.bmcl.2006.06.053
CHEMBL385336 210 None 14 Rat Functional pIC50 = 8.3 8.3 -1 4
Antagonist activity at rat mGluR1 expressed in 1321N1 cellsAntagonist activity at rat mGluR1 expressed in 1321N1 cells
ChEMBL 350 3 0 6 3.6 CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C 10.1016/j.bmcl.2006.06.053
1384 2880 None 48 Rat Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 307 2 1 3 3.3 O=C(c1cnc2c(n1)cccc2)NC12CC3CC(C2)CC(C1)C3 10.1021/jm0611298
7067728 2880 None 48 Rat Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 307 2 1 3 3.3 O=C(c1cnc2c(n1)cccc2)NC12CC3CC(C2)CC(C1)C3 10.1021/jm0611298
CHEMBL399160 2880 None 48 Rat Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 307 2 1 3 3.3 O=C(c1cnc2c(n1)cccc2)NC12CC3CC(C2)CC(C1)C3 10.1021/jm0611298
16660135 1642 None 33 Human Functional pIC50 = 8.3 8.3 2 3
Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 371 5 1 6 3.8 CC(Nc1ncnc(c1)c1csc(n1)N(C(=O)c1ccc(cc1)F)C)C 10.1016/j.bmcl.2009.07.097
8767 1642 None 33 Human Functional pIC50 = 8.3 8.3 2 3
Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 371 5 1 6 3.8 CC(Nc1ncnc(c1)c1csc(n1)N(C(=O)c1ccc(cc1)F)C)C 10.1016/j.bmcl.2009.07.097
CHEMBL566581 1642 None 33 Human Functional pIC50 = 8.3 8.3 2 3
Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 371 5 1 6 3.8 CC(Nc1ncnc(c1)c1csc(n1)N(C(=O)c1ccc(cc1)F)C)C 10.1016/j.bmcl.2009.07.097
16118681 70995 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 339 2 0 5 3.8 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(F)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951660 70995 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 339 2 0 5 3.8 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(F)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
16659968 88721 None 0 Human Functional pIC50 = 8.3 8.3 117 2
Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay
ChEMBL 364 1 1 7 3.5 Cc1ccc(-n2cnc3c(sc4ncc5c(c43)NC[C@@H](C)O5)c2=O)cc1 10.1021/jm070590c
CHEMBL235977 88721 None 0 Human Functional pIC50 = 8.3 8.3 117 2
Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay
ChEMBL 364 1 1 7 3.5 Cc1ccc(-n2cnc3c(sc4ncc5c(c43)NC[C@@H](C)O5)c2=O)cc1 10.1021/jm070590c
16118256 71011 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 314 2 0 5 4.1 COc1ccnc2sc3c(=O)n(C4CCCCC4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951677 71011 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 314 2 0 5 4.1 COc1ccnc2sc3c(=O)n(C4CCCCC4)ccc3c12 10.1016/j.bmcl.2011.12.131
11325594 201360 None 1 Human Functional pIC50 = 8.3 8.3 416 2
Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL 351 3 0 5 3.1 Cc1c(-c2ccc3c(c2)CN(C(C)C)C3=O)nnn1-c1cccnc1F 10.1016/j.bmcl.2009.07.145
CHEMBL584478 201360 None 1 Human Functional pIC50 = 8.3 8.3 416 2
Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL 351 3 0 5 3.1 Cc1c(-c2ccc3c(c2)CN(C(C)C)C3=O)nnn1-c1cccnc1F 10.1016/j.bmcl.2009.07.145
11245287 1697 None 29 Human Functional pIC50 = 8.3 8.3 -1 4
Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL 358 3 0 5 2.7 CC(N(C(=O)N1CCC(=CC1)c1nnn(c1C)c1cccnc1F)C)C 10.1016/j.bmcl.2009.07.145
6363 1697 None 29 Human Functional pIC50 = 8.3 8.3 -1 4
Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL 358 3 0 5 2.7 CC(N(C(=O)N1CCC(=CC1)c1nnn(c1C)c1cccnc1F)C)C 10.1016/j.bmcl.2009.07.145
CHEMBL502882 1697 None 29 Human Functional pIC50 = 8.3 8.3 -1 4
Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL 358 3 0 5 2.7 CC(N(C(=O)N1CCC(=CC1)c1nnn(c1C)c1cccnc1F)C)C 10.1016/j.bmcl.2009.07.145
16118123 70997 None 0 Human Functional pIC50 = 8.2 8.2 1348 2
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 399 2 0 5 4.4 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951662 70997 None 0 Human Functional pIC50 = 8.2 8.2 1348 2
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 399 2 0 5 4.4 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
11245287 1697 None 29 Human Functional pIC50 = 8.2 8.2 -1 4
Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 358 3 0 5 2.7 CC(N(C(=O)N1CCC(=CC1)c1nnn(c1C)c1cccnc1F)C)C 10.1016/j.bmc.2008.09.060
6363 1697 None 29 Human Functional pIC50 = 8.2 8.2 -1 4
Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 358 3 0 5 2.7 CC(N(C(=O)N1CCC(=CC1)c1nnn(c1C)c1cccnc1F)C)C 10.1016/j.bmc.2008.09.060
CHEMBL502882 1697 None 29 Human Functional pIC50 = 8.2 8.2 -1 4
Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 358 3 0 5 2.7 CC(N(C(=O)N1CCC(=CC1)c1nnn(c1C)c1cccnc1F)C)C 10.1016/j.bmc.2008.09.060
44435349 92022 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay
ChEMBL 420 2 1 6 4.5 CNc1c(Br)cnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12 10.1021/jm070590c
CHEMBL241547 92022 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay
ChEMBL 420 2 1 6 4.5 CNc1c(Br)cnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12 10.1021/jm070590c
11695588 143326 None 0 Human Functional pIC50 = 7.3 7.3 1 3
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 328 2 0 6 3.6 CN(C)c1ccnc2sc3c(=O)n(C4CCCCC4)cnc3c12 10.1021/jm0504407
CHEMBL389655 143326 None 0 Human Functional pIC50 = 7.3 7.3 1 3
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 328 2 0 6 3.6 CN(C)c1ccnc2sc3c(=O)n(C4CCCCC4)cnc3c12 10.1021/jm0504407
11695769 143625 None 0 Human Functional pIC50 = 7.3 7.3 1 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 338 2 1 7 2.8 CN(C)c1ccnc2sc3c(=O)n(-c4ccccc4O)cnc3c12 10.1021/jm0504407
CHEMBL389897 143625 None 0 Human Functional pIC50 = 7.3 7.3 1 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 338 2 1 7 2.8 CN(C)c1ccnc2sc3c(=O)n(-c4ccccc4O)cnc3c12 10.1021/jm0504407
78320170 114404 None 4 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay
ChEMBL 334 3 0 5 4.1 COc1ccc(-n2cnc3c(-c4ccccc4)csc3c2=O)cc1 10.1016/j.ejmech.2014.08.027
CHEMBL3330811 114404 None 4 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay
ChEMBL 334 3 0 5 4.1 COc1ccc(-n2cnc3c(-c4ccccc4)csc3c2=O)cc1 10.1016/j.ejmech.2014.08.027
44408564 75884 None 0 Rat Functional pIC50 = 6.3 6.3 - 1
Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method
ChEMBL 377 6 1 5 2.4 CC(=O)NCCCN1CCn2cc(C(=O)OC(C)C(C)(C)C)c(C)c2C1=O 10.1016/j.bmcl.2005.11.049
CHEMBL204878 75884 None 0 Rat Functional pIC50 = 6.3 6.3 - 1
Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method
ChEMBL 377 6 1 5 2.4 CC(=O)NCCCN1CCn2cc(C(=O)OC(C)C(C)(C)C)c(C)c2C1=O 10.1016/j.bmcl.2005.11.049
89981484 125172 None 0 Human Functional pIC50 = 6.3 6.3 -46 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 349 2 0 6 1.9 COc1ncn(C2=NCC(=O)N3CCc4c(cccc4C4CC4)C3=C2)n1 nan
CHEMBL3644401 125172 None 0 Human Functional pIC50 = 6.3 6.3 -46 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 349 2 0 6 1.9 COc1ncn(C2=NCC(=O)N3CCc4c(cccc4C4CC4)C3=C2)n1 nan
73350718 92059 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 326 1 0 3 2.3 O=C(N1CC2CCC(C2)C1)N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1 10.1016/j.bmcl.2013.07.029
CHEMBL2418362 92059 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 326 1 0 3 2.3 O=C(N1CC2CCC(C2)C1)N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1 10.1016/j.bmcl.2013.07.029
72163298 92062 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 313 2 0 3 2.9 CC1(C(=O)N2C[C@@H]3CN(c4ccccn4)C[C@@H]3C2)CCCCC1 10.1016/j.bmcl.2013.07.029
CHEMBL2418370 92062 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 313 2 0 3 2.9 CC1(C(=O)N2C[C@@H]3CN(c4ccccn4)C[C@@H]3C2)CCCCC1 10.1016/j.bmcl.2013.07.029
72163298 92062 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 313 2 0 3 2.9 CC1(C(=O)N2C[C@@H]3CN(c4ccccn4)C[C@@H]3C2)CCCCC1 10.1016/j.bmcl.2013.07.029
CHEMBL2418370 92062 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 313 2 0 3 2.9 CC1(C(=O)N2C[C@@H]3CN(c4ccccn4)C[C@@H]3C2)CCCCC1 10.1016/j.bmcl.2013.07.029
73350718 92059 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 326 1 0 3 2.3 O=C(N1CC2CCC(C2)C1)N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1 10.1016/j.bmcl.2013.07.029
CHEMBL2418362 92059 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 326 1 0 3 2.3 O=C(N1CC2CCC(C2)C1)N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1 10.1016/j.bmcl.2013.07.029
44416780 80262 None 0 Rat Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at rat mGluR1 expressed in 1321N1 cellsAntagonist activity at rat mGluR1 expressed in 1321N1 cells
ChEMBL 441 6 0 7 4.6 CCc1ccc(-n2cnc3c(sc4nccc(N(C)CCc5ccccn5)c43)c2=O)cc1 10.1016/j.bmcl.2006.06.053
CHEMBL213760 80262 None 0 Rat Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at rat mGluR1 expressed in 1321N1 cellsAntagonist activity at rat mGluR1 expressed in 1321N1 cells
ChEMBL 441 6 0 7 4.6 CCc1ccc(-n2cnc3c(sc4nccc(N(C)CCc5ccccn5)c43)c2=O)cc1 10.1016/j.bmcl.2006.06.053
12042753 94841 None 0 Rat Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 306 2 1 2 3.9 O=C(NC12CC3CC(CC(C3)C1)C2)c1cnc2ccccc2c1 10.1021/jm0611298
CHEMBL253347 94841 None 0 Rat Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 306 2 1 2 3.9 O=C(NC12CC3CC(CC(C3)C1)C2)c1cnc2ccccc2c1 10.1021/jm0611298
44442426 154855 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay
ChEMBL 356 2 0 5 4.4 Cc1nc2c(cnn2C2CCCCCC2)c(=O)n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2007.05.028
CHEMBL400110 154855 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay
ChEMBL 356 2 0 5 4.4 Cc1nc2c(cnn2C2CCCCCC2)c(=O)n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2007.05.028
73335134 133101 None 0 Human Functional pIC50 = 5.3 5.3 -1 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 362 3 0 5 2.4 COc1cccc2c1CCN1C(=O)CN=C(c3ccnc(N(C)C)c3)C=C21 nan
CHEMBL3702374 133101 None 0 Human Functional pIC50 = 5.3 5.3 -1 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 362 3 0 5 2.4 COc1cccc2c1CCN1C(=O)CN=C(c3ccnc(N(C)C)c3)C=C21 nan
54580946 62777 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 383 4 1 7 4.0 C=C(C)CNc1ncnc2sc3c(=O)n(-c4cccc(Cl)c4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784062 62777 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 383 4 1 7 4.0 C=C(C)CNc1ncnc2sc3c(=O)n(-c4cccc(Cl)c4)cnc3c12 10.1016/j.bmcl.2009.04.104
73335036 133094 None 0 Human Functional pIC50 = 6.3 6.3 -6 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 382 3 0 4 3.6 COc1cccc(C2=NCC(=O)N3CCc4c(ccc(Cl)c4OC)C3=C2)c1 nan
CHEMBL3702367 133094 None 0 Human Functional pIC50 = 6.3 6.3 -6 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 382 3 0 4 3.6 COc1cccc(C2=NCC(=O)N3CCc4c(ccc(Cl)c4OC)C3=C2)c1 nan
24777313 94691 None 0 Rat Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 319 3 0 4 3.7 CN(Cc1ccccc1)c1nc2c(cc1C#N)C(=O)CC(C)(C)C2 10.1021/jm0611298
CHEMBL252334 94691 None 0 Rat Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 319 3 0 4 3.7 CN(Cc1ccccc1)c1nc2c(cc1C#N)C(=O)CC(C)(C)C2 10.1021/jm0611298
118735975 118985 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay
ChEMBL 391 4 1 4 4.6 N#Cc1c(NCc2cccc(F)c2)sc2c1CCN(C(=O)c1ccccc1)C2 10.1016/j.ejmech.2015.04.060
CHEMBL3422891 118985 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay
ChEMBL 391 4 1 4 4.6 N#Cc1c(NCc2cccc(F)c2)sc2c1CCN(C(=O)c1ccccc1)C2 10.1016/j.ejmech.2015.04.060
122196104 124306 None 0 Human Functional pIC50 = 6.3 6.3 10 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 428 3 1 4 5.0 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c(C(F)(F)F)c1 10.1016/j.bmcl.2015.10.013
CHEMBL3634427 124306 None 0 Human Functional pIC50 = 6.3 6.3 10 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 428 3 1 4 5.0 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c(C(F)(F)F)c1 10.1016/j.bmcl.2015.10.013
122196118 124319 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 366 3 1 6 2.6 Cc1ccoc1C(=O)Nc1cnc(N2C(=O)c3cccc(F)c3C2=O)nc1 10.1016/j.bmcl.2015.10.013
CHEMBL3634440 124319 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 366 3 1 6 2.6 Cc1ccoc1C(=O)Nc1cnc(N2C(=O)c3cccc(F)c3C2=O)nc1 10.1016/j.bmcl.2015.10.013
16118945 71008 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 352 3 0 6 3.9 COc1ccc(-n2ccc3c(sc4nccc(OC)c43)c2=O)c(C)c1 10.1016/j.bmcl.2011.12.131
CHEMBL1951674 71008 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 352 3 0 6 3.9 COc1ccc(-n2ccc3c(sc4nccc(OC)c43)c2=O)c(C)c1 10.1016/j.bmcl.2011.12.131
89980399 125191 None 0 Human Functional pIC50 = 6.3 6.3 -12 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 362 3 0 5 2.6 COCc1cn(C2=NCC(=O)N3CCc4c(cccc4C4CC4)C3=C2)cn1 nan
CHEMBL3644420 125191 None 0 Human Functional pIC50 = 6.3 6.3 -12 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 362 3 0 5 2.6 COCc1cn(C2=NCC(=O)N3CCc4c(cccc4C4CC4)C3=C2)cn1 nan
16659647 167509 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay
ChEMBL 382 1 1 7 4.6 Cc1ccc(-n2cnc3c(sc4ncc5sc(=S)[nH]c5c43)c2=O)cc1 10.1021/jm070590c
CHEMBL429635 167509 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay
ChEMBL 382 1 1 7 4.6 Cc1ccc(-n2cnc3c(sc4ncc5sc(=S)[nH]c5c43)c2=O)cc1 10.1021/jm070590c
87549991 122271 None 0 Rat Functional pIC50 = 6.3 6.3 -301 2
Negative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysisNegative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysis
ChEMBL 333 2 0 4 3.9 Cc1cccc(C#CC=C2CCN(c3ncccc3[N+](=O)[O-])CC2)c1 10.1016/j.bmc.2015.05.008
CHEMBL3597597 122271 None 0 Rat Functional pIC50 = 6.3 6.3 -301 2
Negative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysisNegative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysis
ChEMBL 333 2 0 4 3.9 Cc1cccc(C#CC=C2CCN(c3ncccc3[N+](=O)[O-])CC2)c1 10.1016/j.bmc.2015.05.008
72163723 92054 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 376 2 0 4 3.1 N#Cc1ncccc1N1C[C@H]2CN(C(=O)C34CC5CC(CC(C5)C3)C4)C[C@H]2C1 10.1016/j.bmcl.2013.07.029
CHEMBL2418356 92054 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 376 2 0 4 3.1 N#Cc1ncccc1N1C[C@H]2CN(C(=O)C34CC5CC(CC(C5)C3)C4)C[C@H]2C1 10.1016/j.bmcl.2013.07.029
44329031 108330 None 0 Human Functional pIC50 = 4.3 4.3 -446 7
Antagonistic activity against metabotropic glutamate receptor 1 (mGluR1) was evaluatedAntagonistic activity against metabotropic glutamate receptor 1 (mGluR1) 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 108330 None 0 Human Functional pIC50 = 4.3 4.3 -446 7
Antagonistic activity against metabotropic glutamate receptor 1 (mGluR1) was evaluatedAntagonistic activity against metabotropic glutamate receptor 1 (mGluR1) 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
44588461 173670 None 0 Human Functional pIC50 = 7.3 7.3 3 3
Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 327 2 0 6 2.7 CC(C)(C)OC(=O)N1CC=C(c2cn(-c3cccnc3)nn2)CC1 10.1016/j.bmc.2008.09.060
CHEMBL453249 173670 None 0 Human Functional pIC50 = 7.3 7.3 3 3
Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 327 2 0 6 2.7 CC(C)(C)OC(=O)N1CC=C(c2cn(-c3cccnc3)nn2)CC1 10.1016/j.bmc.2008.09.060
16117042 71015 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 365 5 1 6 4.4 CCCNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951682 71015 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 365 5 1 6 4.4 CCCNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
25183670 122270 None 0 Rat Functional pIC50 = 6.3 6.3 -52 2
Negative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysisNegative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysis
ChEMBL 333 2 0 4 3.9 Cc1cccc(C#CC=C2CCN(c3ccccc3[N+](=O)[O-])CC2)n1 10.1016/j.bmc.2015.05.008
CHEMBL3597596 122270 None 0 Rat Functional pIC50 = 6.3 6.3 -52 2
Negative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysisNegative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysis
ChEMBL 333 2 0 4 3.9 Cc1cccc(C#CC=C2CCN(c3ccccc3[N+](=O)[O-])CC2)n1 10.1016/j.bmc.2015.05.008
72163723 92054 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 376 2 0 4 3.1 N#Cc1ncccc1N1C[C@H]2CN(C(=O)C34CC5CC(CC(C5)C3)C4)C[C@H]2C1 10.1016/j.bmcl.2013.07.029
CHEMBL2418356 92054 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 376 2 0 4 3.1 N#Cc1ncccc1N1C[C@H]2CN(C(=O)C34CC5CC(CC(C5)C3)C4)C[C@H]2C1 10.1016/j.bmcl.2013.07.029
44431054 93361 None 0 Rat Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay
ChEMBL 298 3 2 2 3.4 O=C1NCCc2c1[nH]c1ccc(OCC3CCCCC3)cc21 10.1016/j.bmcl.2007.01.055
CHEMBL245188 93361 None 0 Rat Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay
ChEMBL 298 3 2 2 3.4 O=C1NCCc2c1[nH]c1ccc(OCC3CCCCC3)cc21 10.1016/j.bmcl.2007.01.055
72163720 92069 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 376 2 0 4 3.1 N#Cc1cccnc1N1C[C@H]2CN(C(=O)C34CC5CC(CC(C5)C3)C4)C[C@H]2C1 10.1016/j.bmcl.2013.07.029
CHEMBL2418384 92069 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 376 2 0 4 3.1 N#Cc1cccnc1N1C[C@H]2CN(C(=O)C34CC5CC(CC(C5)C3)C4)C[C@H]2C1 10.1016/j.bmcl.2013.07.029
73335829 125193 None 0 Human Functional pIC50 = 6.3 6.3 -29 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 385 2 0 6 3.1 O=C1CN=C(n2cnc(C3CC3)c2)C=C2c3cccc(-c4ccno4)c3CCN12 nan
CHEMBL3644422 125193 None 0 Human Functional pIC50 = 6.3 6.3 -29 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 385 2 0 6 3.1 O=C1CN=C(n2cnc(C3CC3)c2)C=C2c3cccc(-c4ccno4)c3CCN12 nan
127034265 139160 None 0 Rat Functional pIC50 = 5.3 5.3 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 296 2 2 6 2.9 C[C@H]1CC[C@H](Nc2nc(N)nc3c2nn2ccccc32)CC1 10.1016/j.bmcl.2016.03.026
CHEMBL3786386 139160 None 0 Rat Functional pIC50 = 5.3 5.3 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 296 2 2 6 2.9 C[C@H]1CC[C@H](Nc2nc(N)nc3c2nn2ccccc32)CC1 10.1016/j.bmcl.2016.03.026
89979991 133193 None 0 Human Functional pIC50 = 6.3 6.3 -186 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 380 3 0 5 2.7 COCc1cn(C2=NCC(=O)N3CCc4c(cc(F)cc4C4CC4)C3=C2)cn1 nan
CHEMBL3702467 133193 None 0 Human Functional pIC50 = 6.3 6.3 -186 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 380 3 0 5 2.7 COCc1cn(C2=NCC(=O)N3CCc4c(cc(F)cc4C4CC4)C3=C2)cn1 nan
72163720 92069 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 376 2 0 4 3.1 N#Cc1cccnc1N1C[C@H]2CN(C(=O)C34CC5CC(CC(C5)C3)C4)C[C@H]2C1 10.1016/j.bmcl.2013.07.029
CHEMBL2418384 92069 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 376 2 0 4 3.1 N#Cc1cccnc1N1C[C@H]2CN(C(=O)C34CC5CC(CC(C5)C3)C4)C[C@H]2C1 10.1016/j.bmcl.2013.07.029
127034265 139160 None 0 Rat Functional pIC50 = 5.3 5.3 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 296 2 2 6 2.9 C[C@H]1CC[C@H](Nc2nc(N)nc3c2nn2ccccc32)CC1 10.1016/j.bmcl.2016.03.026
CHEMBL3786386 139160 None 0 Rat Functional pIC50 = 5.3 5.3 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 296 2 2 6 2.9 C[C@H]1CC[C@H](Nc2nc(N)nc3c2nn2ccccc32)CC1 10.1016/j.bmcl.2016.03.026
78322694 152246 None 0 Human Functional pIC50 = 6.3 6.3 - 1
FLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and diluteFLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and dilute
ChEMBL 348 3 0 5 4.4 COc1ccc(-n2c(C)nc3c(-c4ccccc4)csc3c2=O)cc1 nan
CHEMBL3968177 152246 None 0 Human Functional pIC50 = 6.3 6.3 - 1
FLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and diluteFLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and dilute
ChEMBL 348 3 0 5 4.4 COc1ccc(-n2c(C)nc3c(-c4ccccc4)csc3c2=O)cc1 nan
44588428 176937 None 0 Human Functional pIC50 = 7.2 7.2 5 3
Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 343 2 1 4 3.0 CC(C)(C)NC(=O)N1CC=C(c2cn(-c3ccccc3F)nn2)CC1 10.1016/j.bmc.2008.09.060
CHEMBL461034 176937 None 0 Human Functional pIC50 = 7.2 7.2 5 3
Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 343 2 1 4 3.0 CC(C)(C)NC(=O)N1CC=C(c2cn(-c3ccccc3F)nn2)CC1 10.1016/j.bmc.2008.09.060
78321115 114407 None 4 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay
ChEMBL 352 3 0 5 4.3 COc1ccc(-n2cnc3c(-c4ccccc4F)csc3c2=O)cc1 10.1016/j.ejmech.2014.08.027
CHEMBL3330817 114407 None 4 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay
ChEMBL 352 3 0 5 4.3 COc1ccc(-n2cnc3c(-c4ccccc4F)csc3c2=O)cc1 10.1016/j.ejmech.2014.08.027
45486817 200931 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 314 3 0 5 3.0 CN(C(=O)c1ccc(F)cc1)c1nc(-c2ncccn2)cs1 10.1016/j.bmcl.2009.07.097
CHEMBL577505 200931 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 314 3 0 5 3.0 CN(C(=O)c1ccc(F)cc1)c1nc(-c2ncccn2)cs1 10.1016/j.bmcl.2009.07.097
44329029 163616 None 0 Human Functional pIC50 = 5.2 5.2 -2 6
Antagonistic activity against metabotropic glutamate receptor 1 (mGluR1) was evaluatedAntagonistic activity against metabotropic glutamate receptor 1 (mGluR1) 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 163616 None 0 Human Functional pIC50 = 5.2 5.2 -2 6
Antagonistic activity against metabotropic glutamate receptor 1 (mGluR1) was evaluatedAntagonistic activity against metabotropic glutamate receptor 1 (mGluR1) 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
44328753 210213 None 0 Human Functional pIC50 = 4.2 4.2 -1995 6
Antagonistic activity against metabotropic glutamate receptor 1 (mGluR1) was evaluatedAntagonistic activity against metabotropic glutamate receptor 1 (mGluR1) 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 210213 None 0 Human Functional pIC50 = 4.2 4.2 -1995 6
Antagonistic activity against metabotropic glutamate receptor 1 (mGluR1) was evaluatedAntagonistic activity against metabotropic glutamate receptor 1 (mGluR1) 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
22884216 201173 None 5 Human Functional pIC50 = 4.2 4.2 - 1
In vitro antagonist activity at recombinant human Metabotropic glutamate receptor 1 expressed in RGT cells.In vitro antagonist activity at recombinant human Metabotropic glutamate receptor 1 expressed in RGT cells.
ChEMBL 209 4 3 3 1.3 C[C@H](Nc1ccc(C(=O)O)cc1)C(=O)O 10.1016/s0960-894x(98)00352-7
CHEMBL58247 201173 None 5 Human Functional pIC50 = 4.2 4.2 - 1
In vitro antagonist activity at recombinant human Metabotropic glutamate receptor 1 expressed in RGT cells.In vitro antagonist activity at recombinant human Metabotropic glutamate receptor 1 expressed in RGT cells.
ChEMBL 209 4 3 3 1.3 C[C@H](Nc1ccc(C(=O)O)cc1)C(=O)O 10.1016/s0960-894x(98)00352-7
78324867 114396 None 4 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay
ChEMBL 322 2 0 4 4.3 O=c1c2scc(-c3ccccc3)c2ncn1-c1cccc(F)c1 10.1016/j.ejmech.2014.08.027
CHEMBL3330801 114396 None 4 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay
ChEMBL 322 2 0 4 4.3 O=c1c2scc(-c3ccccc3)c2ncn1-c1cccc(F)c1 10.1016/j.ejmech.2014.08.027
44588426 189311 None 0 Mouse Functional pIC50 = 7.2 7.2 -5 3
Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 340 2 0 5 3.6 Cc1ccccc1-n1cc(C2=CCN(C(=O)OC(C)(C)C)CC2)nn1 10.1016/j.bmc.2008.09.060
CHEMBL511352 189311 None 0 Mouse Functional pIC50 = 7.2 7.2 -5 3
Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 340 2 0 5 3.6 Cc1ccccc1-n1cc(C2=CCN(C(=O)OC(C)(C)C)CC2)nn1 10.1016/j.bmc.2008.09.060
78324870 114399 None 4 Human Functional pIC50 = 7.2 7.2 - 1
FLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and diluteFLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and dilute
ChEMBL 338 2 0 4 4.8 O=c1c2scc(-c3ccccc3)c2ncn1-c1cccc(Cl)c1 nan
CHEMBL3330804 114399 None 4 Human Functional pIC50 = 7.2 7.2 - 1
FLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and diluteFLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and dilute
ChEMBL 338 2 0 4 4.8 O=c1c2scc(-c3ccccc3)c2ncn1-c1cccc(Cl)c1 nan
1418 3449 None 40 Human Functional pIC50 = 4.2 4.2 -1 2
Compound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysisCompound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysis
ChEMBL 195 3 3 3 0.5 N[C@@H](c1ccc(cc1)C(=O)O)C(=O)O 10.1016/S0960-894X(97)10071-3
5311459 3449 None 40 Human Functional pIC50 = 4.2 4.2 -1 2
Compound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysisCompound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysis
ChEMBL 195 3 3 3 0.5 N[C@@H](c1ccc(cc1)C(=O)O)C(=O)O 10.1016/S0960-894X(97)10071-3
CHEMBL94990 3449 None 40 Human Functional pIC50 = 4.2 4.2 -1 2
Compound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysisCompound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysis
ChEMBL 195 3 3 3 0.5 N[C@@H](c1ccc(cc1)C(=O)O)C(=O)O 10.1016/S0960-894X(97)10071-3
73334945 133085 None 0 Human Functional pIC50 = 6.2 6.2 -24 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 349 3 0 5 2.3 COc1cc(C2=NCC(=O)N3CCc4c(OC)cccc4C3=C2)ccn1 nan
CHEMBL3702358 133085 None 0 Human Functional pIC50 = 6.2 6.2 -24 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 349 3 0 5 2.3 COc1cc(C2=NCC(=O)N3CCc4c(OC)cccc4C3=C2)ccn1 nan
89980086 133175 None 0 Human Functional pIC50 = 5.2 5.2 -85 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 413 2 0 5 3.6 O=C1CN=C(n2cnc(C3CC3)c2)C=C2c3cccc(-c4cnccc4F)c3CCN12 nan
CHEMBL3702447 133175 None 0 Human Functional pIC50 = 5.2 5.2 -85 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 413 2 0 5 3.6 O=C1CN=C(n2cnc(C3CC3)c2)C=C2c3cccc(-c4cnccc4F)c3CCN12 nan
76328955 105660 None 0 Human Functional pIC50 = 5.2 5.2 -1047 2
Negative allosteric modulation of human mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium flux after 16 to 24 hrs by FLIPR assayNegative allosteric modulation of human mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium flux after 16 to 24 hrs by FLIPR assay
ChEMBL 339 6 0 6 2.4 CCN(CC)C(=O)c1nn(C)c2nc(OCc3ccccn3)ccc12 10.1021/jm401622k
CHEMBL3122224 105660 None 0 Human Functional pIC50 = 5.2 5.2 -1047 2
Negative allosteric modulation of human mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium flux after 16 to 24 hrs by FLIPR assayNegative allosteric modulation of human mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium flux after 16 to 24 hrs by FLIPR assay
ChEMBL 339 6 0 6 2.4 CCN(CC)C(=O)c1nn(C)c2nc(OCc3ccccn3)ccc12 10.1021/jm401622k
44588427 176936 None 0 Human Functional pIC50 = 6.2 6.2 2 3
Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 356 3 0 6 3.3 COc1ccccc1-n1cc(C2=CCN(C(=O)OC(C)(C)C)CC2)nn1 10.1016/j.bmc.2008.09.060
CHEMBL461033 176936 None 0 Human Functional pIC50 = 6.2 6.2 2 3
Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 356 3 0 6 3.3 COc1ccccc1-n1cc(C2=CCN(C(=O)OC(C)(C)C)CC2)nn1 10.1016/j.bmc.2008.09.060
73335735 133161 None 0 Human Functional pIC50 = 5.2 5.2 -489 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 400 2 0 4 3.9 CCc1cn(C2=NCC(=O)N3CCc4c(cccc4-c4ccc(F)cc4)C3=C2)cn1 nan
CHEMBL3702434 133161 None 0 Human Functional pIC50 = 5.2 5.2 -489 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 400 2 0 4 3.9 CCc1cn(C2=NCC(=O)N3CCc4c(cccc4-c4ccc(F)cc4)C3=C2)cn1 nan
89979678 133182 None 0 Human Functional pIC50 = 5.2 5.2 -158 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 413 2 0 5 3.6 O=C1CN=C(n2cnc(C3CC3)c2)C=C2c3cccc(-c4cccnc4F)c3CCN12 nan
CHEMBL3702454 133182 None 0 Human Functional pIC50 = 5.2 5.2 -158 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 413 2 0 5 3.6 O=C1CN=C(n2cnc(C3CC3)c2)C=C2c3cccc(-c4cccnc4F)c3CCN12 nan
71682802 91080 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 339 2 0 3 3.3 C[C@@H]1CN(c2cccnc2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
CHEMBL2397368 91080 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 339 2 0 3 3.3 C[C@@H]1CN(c2cccnc2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
57559562 966 None 0 Human Functional pIC50 = 8.2 8.2 1659 2
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 365 4 1 8 3.0 COc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ncn1)NC1CC1 10.1016/j.bmcl.2012.09.048
6365 966 None 0 Human Functional pIC50 = 8.2 8.2 1659 2
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 365 4 1 8 3.0 COc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ncn1)NC1CC1 10.1016/j.bmcl.2012.09.048
CHEMBL2205915 966 None 0 Human Functional pIC50 = 8.2 8.2 1659 2
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 365 4 1 8 3.0 COc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ncn1)NC1CC1 10.1016/j.bmcl.2012.09.048
16661408 200267 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 313 3 0 4 3.6 CN(C(=O)c1ccc(F)cc1)c1nc(-c2ccccn2)cs1 10.1016/j.bmcl.2009.07.097
CHEMBL572135 200267 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 313 3 0 4 3.6 CN(C(=O)c1ccc(F)cc1)c1nc(-c2ccccn2)cs1 10.1016/j.bmcl.2009.07.097
16659963 149963 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay
ChEMBL 353 1 1 6 3.5 O=c1c2sc3ncc4nc[nH]c4c3c2ncn1-c1ccc(Cl)cc1 10.1021/jm070590c
CHEMBL394914 149963 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay
ChEMBL 353 1 1 6 3.5 O=c1c2sc3ncc4nc[nH]c4c3c2ncn1-c1ccc(Cl)cc1 10.1021/jm070590c
44447971 95025 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor
ChEMBL 357 4 0 5 3.2 Cc1c(C2=CCC(C(=O)N(C)C(C)C)CC2)nnn1-c1cccnc1F 10.1021/jm060950g
CHEMBL254573 95025 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor
ChEMBL 357 4 0 5 3.2 Cc1c(C2=CCC(C(=O)N(C)C(C)C)CC2)nnn1-c1cccnc1F 10.1021/jm060950g
9926083 94803 None 6 Rat Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 292 2 0 4 2.8 CCc1nc(C#N)c(N2CCc3ccccc3CC2)nc1C 10.1021/jm0611298
CHEMBL253142 94803 None 6 Rat Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 292 2 0 4 2.8 CCc1nc(C#N)c(N2CCc3ccccc3CC2)nc1C 10.1021/jm0611298
44588385 177000 None 0 Human Functional pIC50 = 8.2 8.2 2 3
Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 344 2 0 5 3.4 CC(C)(C)OC(=O)N1CC=C(c2cn(-c3ccccc3F)nn2)CC1 10.1016/j.bmc.2008.09.060
CHEMBL461673 177000 None 0 Human Functional pIC50 = 8.2 8.2 2 3
Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 344 2 0 5 3.4 CC(C)(C)OC(=O)N1CC=C(c2cn(-c3ccccc3F)nn2)CC1 10.1016/j.bmc.2008.09.060
16118119 1149 None 0 Human Functional pIC50 = 8.2 8.2 741 2
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 351 3 0 6 3.7 COc1ccc(cc1)n1ccc2c(c1=O)sc1c2c(ccn1)N(C)C 10.1016/j.bmcl.2011.12.131
6356 1149 None 0 Human Functional pIC50 = 8.2 8.2 741 2
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 351 3 0 6 3.7 COc1ccc(cc1)n1ccc2c(c1=O)sc1c2c(ccn1)N(C)C 10.1016/j.bmcl.2011.12.131
CHEMBL1951658 1149 None 0 Human Functional pIC50 = 8.2 8.2 741 2
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 351 3 0 6 3.7 COc1ccc(cc1)n1ccc2c(c1=O)sc1c2c(ccn1)N(C)C 10.1016/j.bmcl.2011.12.131
16118126 71005 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 338 3 0 6 3.6 COc1ccc(-n2ccc3c(sc4nccc(OC)c43)c2=O)cc1 10.1016/j.bmcl.2011.12.131
CHEMBL1951670 71005 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 338 3 0 6 3.6 COc1ccc(-n2ccc3c(sc4nccc(OC)c43)c2=O)cc1 10.1016/j.bmcl.2011.12.131
16118815 71059 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 352 3 0 7 3.1 COc1ccc(-n2ccc3c(sc4ncnc(N(C)C)c43)c2=O)cc1 10.1016/j.bmcl.2011.12.131
CHEMBL1951883 71059 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 352 3 0 7 3.1 COc1ccc(-n2ccc3c(sc4ncnc(N(C)C)c43)c2=O)cc1 10.1016/j.bmcl.2011.12.131
16118818 71063 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 336 2 0 6 3.4 Cc1ccc(-n2ccc3c(sc4ncnc(N(C)C)c43)c2=O)cc1 10.1016/j.bmcl.2011.12.131
CHEMBL1951887 71063 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 336 2 0 6 3.4 Cc1ccc(-n2ccc3c(sc4ncnc(N(C)C)c43)c2=O)cc1 10.1016/j.bmcl.2011.12.131
23634102 977 None 2 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay
ChEMBL 362 4 1 7 3.0 C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)OC 10.1016/j.ejmech.2014.08.027
6215 977 None 2 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay
ChEMBL 362 4 1 7 3.0 C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)OC 10.1016/j.ejmech.2014.08.027
CHEMBL1783876 977 None 2 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay
ChEMBL 362 4 1 7 3.0 C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)OC 10.1016/j.ejmech.2014.08.027
54584443 62678 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 382 5 1 7 3.7 C=CCNc1ccnc2sc3c(=O)n(-c4ccc(F)c(OC)c4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1783862 62678 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 382 5 1 7 3.7 C=CCNc1ccnc2sc3c(=O)n(-c4ccc(F)c(OC)c4)cnc3c12 10.1016/j.bmcl.2009.04.104
54585851 62785 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 411 3 1 7 3.2 C#CCNc1ncnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784070 62785 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 411 3 1 7 3.2 C#CCNc1ncnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
54581505 62681 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 378 5 0 7 3.6 C=CCN(C)c1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1783865 62681 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 378 5 0 7 3.6 C=CCN(C)c1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
54586361 62676 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 368 4 1 6 4.2 C=CCNc1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1783860 62676 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 368 4 1 6 4.2 C=CCNc1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
57881958 83852 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 379 4 1 8 3.4 COc1ccc(-n2cnc3c(sc4ncnc(NC5CCC5)c43)c2=O)cc1 10.1016/j.bmcl.2012.09.048
CHEMBL2205918 83852 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 379 4 1 8 3.4 COc1ccc(-n2cnc3c(sc4ncnc(NC5CCC5)c43)c2=O)cc1 10.1016/j.bmcl.2012.09.048
118735966 118978 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay
ChEMBL 391 4 1 4 4.6 N#Cc1c(NCc2ccccc2)sc2c1CCN(C(=O)c1ccc(F)cc1)C2 10.1016/j.ejmech.2015.04.060
CHEMBL3422882 118978 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay
ChEMBL 391 4 1 4 4.6 N#Cc1c(NCc2ccccc2)sc2c1CCN(C(=O)c1ccc(F)cc1)C2 10.1016/j.ejmech.2015.04.060
9815955 106041 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Compound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysisCompound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysis
ChEMBL 225 3 4 4 0.5 Cc1c(C(N)C(=O)O)ccc(C(=O)O)c1O 10.1016/S0960-894X(97)10071-3
CHEMBL313124 106041 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Compound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysisCompound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysis
ChEMBL 225 3 4 4 0.5 Cc1c(C(N)C(=O)O)ccc(C(=O)O)c1O 10.1016/S0960-894X(97)10071-3
71682802 91080 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 339 2 0 3 3.3 C[C@@H]1CN(c2cccnc2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
CHEMBL2397368 91080 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 339 2 0 3 3.3 C[C@@H]1CN(c2cccnc2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
16661404 200871 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 329 3 0 4 4.1 CN(C(=O)c1ccc(Cl)cc1)c1nc(-c2ccncc2)cs1 10.1016/j.bmcl.2009.07.097
CHEMBL577035 200871 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 329 3 0 4 4.1 CN(C(=O)c1ccc(Cl)cc1)c1nc(-c2ccncc2)cs1 10.1016/j.bmcl.2009.07.097
18138918 58836 None 1 Human Functional pIC50 = 6.2 6.2 -1 3
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 331 2 0 4 3.0 O=C(N1CCN(c2nccs2)CC1)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
CHEMBL1688377 58836 None 1 Human Functional pIC50 = 6.2 6.2 -1 3
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 331 2 0 4 3.0 O=C(N1CCN(c2nccs2)CC1)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
18138918 58836 None 1 Human Functional pIC50 = 6.2 6.2 -1 3
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 331 2 0 4 3.0 O=C(N1CCN(c2nccs2)CC1)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
CHEMBL1688377 58836 None 1 Human Functional pIC50 = 6.2 6.2 -1 3
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 331 2 0 4 3.0 O=C(N1CCN(c2nccs2)CC1)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
11565466 85080 None 0 Human Functional pIC50 = 6.2 6.2 1 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 286 2 0 6 2.4 CN(C)c1ccnc2sc3c(=O)n(C4CC4)cnc3c12 10.1021/jm0504407
CHEMBL224135 85080 None 0 Human Functional pIC50 = 6.2 6.2 1 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 286 2 0 6 2.4 CN(C)c1ccnc2sc3c(=O)n(C4CC4)cnc3c12 10.1021/jm0504407
16659798 88679 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay
ChEMBL 396 2 0 8 4.6 CSc1nc2c(cnc3sc4c(=O)n(-c5ccc(C)cc5)cnc4c32)s1 10.1021/jm070590c
CHEMBL235767 88679 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay
ChEMBL 396 2 0 8 4.6 CSc1nc2c(cnc3sc4c(=O)n(-c5ccc(C)cc5)cnc4c32)s1 10.1021/jm070590c
73335827 133179 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 347 1 0 5 2.5 Cc1ncn(C2=NCC(=O)N3CCc4c(cccc4C4CCC4)C3=C2)n1 nan
CHEMBL3702451 133179 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 347 1 0 5 2.5 Cc1ncn(C2=NCC(=O)N3CCc4c(cccc4C4CCC4)C3=C2)n1 nan
73334852 125187 None 0 Human Functional pIC50 = 5.2 5.2 -23 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 348 3 0 4 2.9 COc1cccc(C2=NCC(=O)N3CCc4c(OC)cccc4C3=C2)c1 nan
CHEMBL3644416 125187 None 0 Human Functional pIC50 = 5.2 5.2 -23 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 348 3 0 4 2.9 COc1cccc(C2=NCC(=O)N3CCc4c(OC)cccc4C3=C2)c1 nan
91618208 133146 None 0 Human Functional pIC50 = 5.2 5.2 -239 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 388 3 1 6 2.1 COCc1cn(C2=NCC(=O)N3CCc4c(cccc4-c4ncc[nH]4)C3=C2)cn1 nan
CHEMBL3702419 133146 None 0 Human Functional pIC50 = 5.2 5.2 -239 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 388 3 1 6 2.1 COCc1cn(C2=NCC(=O)N3CCc4c(cccc4-c4ncc[nH]4)C3=C2)cn1 nan
685051 91732 None 6 Human Functional pIC50 = 4.2 4.2 -25 2
Negative allosteric modulation of human mGluR1 expressed in CHO cells assessed as inhibition of L-glutamate-induced intracellular cAMP accumulation treated 5 mins before L-quisqualate addition by FLIPR assayNegative allosteric modulation of human mGluR1 expressed in CHO cells assessed as inhibition of L-glutamate-induced intracellular cAMP accumulation treated 5 mins before L-quisqualate addition by FLIPR assay
ChEMBL 248 2 1 3 3.9 Fc1ccc(Nc2nc3c(s2)CCCC3)cc1 10.1016/j.bmcl.2013.06.049
CHEMBL2408581 91732 None 6 Human Functional pIC50 = 4.2 4.2 -25 2
Negative allosteric modulation of human mGluR1 expressed in CHO cells assessed as inhibition of L-glutamate-induced intracellular cAMP accumulation treated 5 mins before L-quisqualate addition by FLIPR assayNegative allosteric modulation of human mGluR1 expressed in CHO cells assessed as inhibition of L-glutamate-induced intracellular cAMP accumulation treated 5 mins before L-quisqualate addition by FLIPR assay
ChEMBL 248 2 1 3 3.9 Fc1ccc(Nc2nc3c(s2)CCCC3)cc1 10.1016/j.bmcl.2013.06.049
44243470 89132 None 0 Human Functional pIC50 = 6.2 6.2 -33 3
Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay
ChEMBL 431 5 1 6 5.5 CC(C)c1cccc(-c2c(-c3ccc4nn(C)cc4c3)nsc2NC(=O)[C@@H]2C[C@H]2C)n1 10.1016/j.bmcl.2013.01.009
CHEMBL2334981 89132 None 0 Human Functional pIC50 = 6.2 6.2 -33 3
Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay
ChEMBL 431 5 1 6 5.5 CC(C)c1cccc(-c2c(-c3ccc4nn(C)cc4c3)nsc2NC(=O)[C@@H]2C[C@H]2C)n1 10.1016/j.bmcl.2013.01.009
CHEMBL2365395 89132 None 0 Human Functional pIC50 = 6.2 6.2 -33 3
Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay
ChEMBL 431 5 1 6 5.5 CC(C)c1cccc(-c2c(-c3ccc4nn(C)cc4c3)nsc2NC(=O)[C@@H]2C[C@H]2C)n1 10.1016/j.bmcl.2013.01.009
67179855 73239 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Allosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assayAllosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assay
ChEMBL 272 3 1 3 3.7 Cc1c(-c2ccccc2)nsc1NC(=O)[C@@H]1C[C@H]1C 10.1016/j.bmcl.2012.02.003
CHEMBL2011872 73239 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Allosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assayAllosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assay
ChEMBL 272 3 1 3 3.7 Cc1c(-c2ccccc2)nsc1NC(=O)[C@@H]1C[C@H]1C 10.1016/j.bmcl.2012.02.003
73335824 133176 None 0 Human Functional pIC50 = 6.2 6.2 -22 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 348 2 0 4 3.3 CCc1cccc2c1CCN1C(=O)CN=C(n3cnc(C(C)C)c3)C=C21 nan
CHEMBL3702448 133176 None 0 Human Functional pIC50 = 6.2 6.2 -22 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 348 2 0 4 3.3 CCc1cccc2c1CCN1C(=O)CN=C(n3cnc(C(C)C)c3)C=C21 nan
73335445 133135 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 378 4 0 5 2.9 COc1cccc(C2=NCC(=O)N3CCc4c(ccc(OC)c4OC)C3=C2)c1 nan
CHEMBL3702408 133135 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 378 4 0 5 2.9 COc1cccc(C2=NCC(=O)N3CCc4c(ccc(OC)c4OC)C3=C2)c1 nan
5115 112110 None 33 Human Functional pIC50 = 4.2 4.2 - 1
Ability to inhibit mGluR1-alpha-mediated PI (phospho inositol) hydrolysis was determined at BHK cells at 100 Micro M ConcentrationAbility to inhibit mGluR1-alpha-mediated PI (phospho inositol) hydrolysis was determined at BHK cells at 100 Micro M Concentration
ChEMBL 195 3 3 3 0.5 NC(C(=O)O)c1ccc(C(=O)O)cc1 10.1021/jm00019a002
CHEMBL328984 112110 None 33 Human Functional pIC50 = 4.2 4.2 - 1
Ability to inhibit mGluR1-alpha-mediated PI (phospho inositol) hydrolysis was determined at BHK cells at 100 Micro M ConcentrationAbility to inhibit mGluR1-alpha-mediated PI (phospho inositol) hydrolysis was determined at BHK cells at 100 Micro M Concentration
ChEMBL 195 3 3 3 0.5 NC(C(=O)O)c1ccc(C(=O)O)cc1 10.1021/jm00019a002
127033444 139120 None 0 Rat Functional pIC50 = 5.2 5.2 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 269 2 1 5 3.1 C[C@H](Nc1ncnc2c1nn1ccccc21)C(C)(C)C 10.1016/j.bmcl.2016.03.026
CHEMBL3785899 139120 None 0 Rat Functional pIC50 = 5.2 5.2 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 269 2 1 5 3.1 C[C@H](Nc1ncnc2c1nn1ccccc21)C(C)(C)C 10.1016/j.bmcl.2016.03.026
54586362 62682 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 426 4 0 6 4.4 C=CCN(C)c1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1783866 62682 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 426 4 0 6 4.4 C=CCN(C)c1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
78324868 114397 None 4 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay
ChEMBL 322 2 0 4 4.3 O=c1c2scc(-c3ccccc3)c2ncn1-c1ccc(F)cc1 10.1016/j.ejmech.2014.08.027
CHEMBL3330802 114397 None 4 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay
ChEMBL 322 2 0 4 4.3 O=c1c2scc(-c3ccccc3)c2ncn1-c1ccc(F)cc1 10.1016/j.ejmech.2014.08.027
78324871 114400 None 4 Human Functional pIC50 = 7.2 7.2 - 1
FLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and diluteFLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and dilute
ChEMBL 338 2 0 4 4.8 O=c1c2scc(-c3ccccc3)c2ncn1-c1ccc(Cl)cc1 nan
CHEMBL3330805 114400 None 4 Human Functional pIC50 = 7.2 7.2 - 1
FLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and diluteFLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and dilute
ChEMBL 338 2 0 4 4.8 O=c1c2scc(-c3ccccc3)c2ncn1-c1ccc(Cl)cc1 nan
89980452 125163 None 0 Human Functional pIC50 = 6.2 6.2 -19 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 374 2 0 5 3.0 CC(=O)c1cccc2c1CCN1C(=O)CN=C(n3cnc(C4CCC4)c3)C=C21 nan
CHEMBL3644392 125163 None 0 Human Functional pIC50 = 6.2 6.2 -19 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 374 2 0 5 3.0 CC(=O)c1cccc2c1CCN1C(=O)CN=C(n3cnc(C4CCC4)c3)C=C21 nan
1382 1190 None 28 Human Functional pIC50 = 5.2 5.2 -1 3
Antagonist activity at human mGlu1b receptorAntagonist activity at human mGlu1b receptor
ChEMBL 247 2 1 5 1.6 CCOC(=O)C12CC2/C(=N\O)/c2c(O1)cccc2 10.1021/jm060950g
6278000 1190 None 28 Human Functional pIC50 = 5.2 5.2 -1 3
Antagonist activity at human mGlu1b receptorAntagonist activity at human mGlu1b receptor
ChEMBL 247 2 1 5 1.6 CCOC(=O)C12CC2/C(=N\O)/c2c(O1)cccc2 10.1021/jm060950g
CHEMBL327783 1190 None 28 Human Functional pIC50 = 5.2 5.2 -1 3
Antagonist activity at human mGlu1b receptorAntagonist activity at human mGlu1b receptor
ChEMBL 247 2 1 5 1.6 CCOC(=O)C12CC2/C(=N\O)/c2c(O1)cccc2 10.1021/jm060950g
71682497 91077 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 315 2 0 3 3.5 C[C@@H]1CN(c2ccccn2)CCN1C(=O)C1CCCCCCC1 10.1016/j.bmcl.2013.05.020
CHEMBL2397360 91077 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 315 2 0 3 3.5 C[C@@H]1CN(c2ccccn2)CCN1C(=O)C1CCCCCCC1 10.1016/j.bmcl.2013.05.020
127033444 139120 None 0 Rat Functional pIC50 = 5.2 5.2 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 269 2 1 5 3.1 C[C@H](Nc1ncnc2c1nn1ccccc21)C(C)(C)C 10.1016/j.bmcl.2016.03.026
CHEMBL3785899 139120 None 0 Rat Functional pIC50 = 5.2 5.2 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 269 2 1 5 3.1 C[C@H](Nc1ncnc2c1nn1ccccc21)C(C)(C)C 10.1016/j.bmcl.2016.03.026
86729808 114411 None 4 Human Functional pIC50 = 6.2 6.2 - 1
FLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and diluteFLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and dilute
ChEMBL 348 3 0 5 4.4 COc1ccc(-n2cnc3c(-c4ccc(C)cc4)csc3c2=O)cc1 nan
CHEMBL3330825 114411 None 4 Human Functional pIC50 = 6.2 6.2 - 1
FLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and diluteFLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and dilute
ChEMBL 348 3 0 5 4.4 COc1ccc(-n2cnc3c(-c4ccc(C)cc4)csc3c2=O)cc1 nan
71682497 91077 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 315 2 0 3 3.5 C[C@@H]1CN(c2ccccn2)CCN1C(=O)C1CCCCCCC1 10.1016/j.bmcl.2013.05.020
CHEMBL2397360 91077 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 315 2 0 3 3.5 C[C@@H]1CN(c2ccccn2)CCN1C(=O)C1CCCCCCC1 10.1016/j.bmcl.2013.05.020
72163582 92064 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 352 2 0 4 2.6 O=C(N1C[C@@H]2CN(c3cnccn3)C[C@@H]2C1)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.07.029
CHEMBL2418379 92064 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 352 2 0 4 2.6 O=C(N1C[C@@H]2CN(c3cnccn3)C[C@@H]2C1)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.07.029
67181693 73246 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Allosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assayAllosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assay
ChEMBL 336 4 1 3 4.8 Cc1c(-c2ccc(C(C)(F)F)cc2)nsc1NC(=O)[C@@H]1C[C@H]1C 10.1016/j.bmcl.2012.02.003
CHEMBL2011879 73246 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Allosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assayAllosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assay
ChEMBL 336 4 1 3 4.8 Cc1c(-c2ccc(C(C)(F)F)cc2)nsc1NC(=O)[C@@H]1C[C@H]1C 10.1016/j.bmcl.2012.02.003
89980670 124465 None 0 Human Functional pIC50 = 6.2 6.2 -338 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 350 2 0 4 2.9 O=C1CN=C(n2cnc(CF)c2)C=C2c3cccc(C4CC4)c3CCN12 nan
CHEMBL3639432 124465 None 0 Human Functional pIC50 = 6.2 6.2 -338 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 350 2 0 4 2.9 O=C1CN=C(n2cnc(CF)c2)C=C2c3cccc(C4CC4)c3CCN12 nan
72163582 92064 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 352 2 0 4 2.6 O=C(N1C[C@@H]2CN(c3cnccn3)C[C@@H]2C1)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.07.029
CHEMBL2418379 92064 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 352 2 0 4 2.6 O=C(N1C[C@@H]2CN(c3cnccn3)C[C@@H]2C1)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.07.029
78324866 114208 None 4 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay
ChEMBL 322 2 0 4 4.3 O=c1c2scc(-c3ccccc3)c2ncn1-c1ccccc1F 10.1016/j.ejmech.2014.08.027
CHEMBL3329236 114208 None 4 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay
ChEMBL 322 2 0 4 4.3 O=c1c2scc(-c3ccccc3)c2ncn1-c1ccccc1F 10.1016/j.ejmech.2014.08.027
46886137 8233 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 327 1 1 7 2.4 Cc1nc(N)c2c(n1)sc1c(=O)n(-c3ccc(F)cc3)cnc12 10.1016/j.bmcl.2010.03.004
CHEMBL1092276 8233 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 327 1 1 7 2.4 Cc1nc(N)c2c(n1)sc1c(=O)n(-c3ccc(F)cc3)cnc12 10.1016/j.bmcl.2010.03.004
16117168 71021 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 325 2 1 5 3.8 CNc1ccnc2sc3c(=O)n(-c4ccc(F)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951689 71021 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 325 2 1 5 3.8 CNc1ccnc2sc3c(=O)n(-c4ccc(F)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
44431060 86785 None 0 Rat Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay
ChEMBL 278 3 2 2 3.0 O=C1NCc2c1[nH]c1ccc(OCc3ccccc3)cc21 10.1016/j.bmcl.2007.01.055
CHEMBL232012 86785 None 0 Rat Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay
ChEMBL 278 3 2 2 3.0 O=C1NCc2c1[nH]c1ccc(OCc3ccccc3)cc21 10.1016/j.bmcl.2007.01.055
73336217 133191 None 0 Human Functional pIC50 = 6.2 6.2 -43 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 380 3 0 5 2.7 COCc1cn(C2=NCC(=O)N3CCc4c(C5CC5)ccc(F)c4C3=C2)cn1 nan
CHEMBL3702465 133191 None 0 Human Functional pIC50 = 6.2 6.2 -43 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 380 3 0 5 2.7 COCc1cn(C2=NCC(=O)N3CCc4c(C5CC5)ccc(F)c4C3=C2)cn1 nan
57908400 89136 None 0 Human Functional pIC50 = 6.2 6.2 -12 2
Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay
ChEMBL 443 5 1 6 5.6 C[C@@H]1C[C@H]1C(=O)Nc1snc(-c2ccc3nn(C)cc3c2)c1-c1cccc(C2CCC2)n1 10.1016/j.bmcl.2013.01.009
CHEMBL2334983 89136 None 0 Human Functional pIC50 = 6.2 6.2 -12 2
Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay
ChEMBL 443 5 1 6 5.6 C[C@@H]1C[C@H]1C(=O)Nc1snc(-c2ccc3nn(C)cc3c2)c1-c1cccc(C2CCC2)n1 10.1016/j.bmcl.2013.01.009
CHEMBL2365403 89136 None 0 Human Functional pIC50 = 6.2 6.2 -12 2
Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay
ChEMBL 443 5 1 6 5.6 C[C@@H]1C[C@H]1C(=O)Nc1snc(-c2ccc3nn(C)cc3c2)c1-c1cccc(C2CCC2)n1 10.1016/j.bmcl.2013.01.009
45484921 200980 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL 290 2 0 5 2.8 Cc1c(-c2ccc3c(c2)CCC3=O)nnn1-c1cccnc1 10.1016/j.bmcl.2009.07.145
CHEMBL577943 200980 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL 290 2 0 5 2.8 Cc1c(-c2ccc3c(c2)CCC3=O)nnn1-c1cccnc1 10.1016/j.bmcl.2009.07.145
127034286 139247 None 0 Rat Functional pIC50 = 7.2 7.2 1 2
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 295 2 1 5 3.7 CC1(C)CCC(Nc2ncnc3c2nn2ccccc32)CC1 10.1016/j.bmcl.2016.03.026
CHEMBL3787247 139247 None 0 Rat Functional pIC50 = 7.2 7.2 1 2
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 295 2 1 5 3.7 CC1(C)CCC(Nc2ncnc3c2nn2ccccc32)CC1 10.1016/j.bmcl.2016.03.026
127034286 139247 None 0 Rat Functional pIC50 = 7.2 7.2 1 2
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 295 2 1 5 3.7 CC1(C)CCC(Nc2ncnc3c2nn2ccccc32)CC1 10.1016/j.bmcl.2016.03.026
CHEMBL3787247 139247 None 0 Rat Functional pIC50 = 7.2 7.2 1 2
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 295 2 1 5 3.7 CC1(C)CCC(Nc2ncnc3c2nn2ccccc32)CC1 10.1016/j.bmcl.2016.03.026
73335034 133092 None 0 Human Functional pIC50 = 6.2 6.2 -4 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 322 2 0 5 1.7 COc1cccc2c1CCN1C(=O)CN=C(c3ccn(C)n3)C=C21 nan
CHEMBL3702365 133092 None 0 Human Functional pIC50 = 6.2 6.2 -4 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 322 2 0 5 1.7 COc1cccc2c1CCN1C(=O)CN=C(c3ccn(C)n3)C=C21 nan
73335338 133114 None 0 Human Functional pIC50 = 5.2 5.2 -1 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 418 1 0 4 2.3 Cn1cnc(C2=NCC(=O)N3CCc4c(I)cccc4C3=C2)c1 nan
CHEMBL3702387 133114 None 0 Human Functional pIC50 = 5.2 5.2 -1 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 418 1 0 4 2.3 Cn1cnc(C2=NCC(=O)N3CCc4c(I)cccc4C3=C2)c1 nan
67182345 73241 None 0 Human Functional pIC50 = 8.2 8.2 22 2
Allosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assayAllosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assay
ChEMBL 320 4 1 4 3.9 COc1ccc(-c2nsc(NC(=O)[C@@H]3C[C@H]3C)c2C)cc1F 10.1016/j.bmcl.2012.02.003
CHEMBL2011874 73241 None 0 Human Functional pIC50 = 8.2 8.2 22 2
Allosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assayAllosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assay
ChEMBL 320 4 1 4 3.9 COc1ccc(-c2nsc(NC(=O)[C@@H]3C[C@H]3C)c2C)cc1F 10.1016/j.bmcl.2012.02.003
67182239 73244 None 0 Human Functional pIC50 = 8.2 8.2 102 2
Allosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assayAllosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assay
ChEMBL 350 3 1 3 4.5 Cc1c(-c2ccc(Br)cc2)nsc1NC(=O)[C@@H]1C[C@H]1C 10.1016/j.bmcl.2012.02.003
CHEMBL2011877 73244 None 0 Human Functional pIC50 = 8.2 8.2 102 2
Allosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assayAllosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assay
ChEMBL 350 3 1 3 4.5 Cc1c(-c2ccc(Br)cc2)nsc1NC(=O)[C@@H]1C[C@H]1C 10.1016/j.bmcl.2012.02.003
16725048 1153 None 0 Human Functional pIC50 = 8.2 8.2 1412 2
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 371 3 0 8 2.6 COc1ccc(c(c1)F)n1cnc2c(c1=O)sc1c2c(ncn1)N(C)C 10.1016/j.bmcl.2012.09.048
6362 1153 None 0 Human Functional pIC50 = 8.2 8.2 1412 2
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 371 3 0 8 2.6 COc1ccc(c(c1)F)n1cnc2c(c1=O)sc1c2c(ncn1)N(C)C 10.1016/j.bmcl.2012.09.048
CHEMBL2205377 1153 None 0 Human Functional pIC50 = 8.2 8.2 1412 2
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 371 3 0 8 2.6 COc1ccc(c(c1)F)n1cnc2c(c1=O)sc1c2c(ncn1)N(C)C 10.1016/j.bmcl.2012.09.048
57559437 83842 None 0 Human Functional pIC50 = 8.2 8.2 1412 2
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 353 4 1 8 2.8 CCNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12 10.1016/j.bmcl.2012.09.048
CHEMBL2205908 83842 None 0 Human Functional pIC50 = 8.2 8.2 1412 2
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 353 4 1 8 2.8 CCNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12 10.1016/j.bmcl.2012.09.048
57881665 83862 None 0 Human Functional pIC50 = 8.2 8.2 28 2
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 329 2 0 7 3.0 CN(C)c1ncnc2sc3c(=O)n(C4CCCCC4)cnc3c12 10.1016/j.bmcl.2012.09.048
CHEMBL2205928 83862 None 0 Human Functional pIC50 = 8.2 8.2 28 2
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 329 2 0 7 3.0 CN(C)c1ncnc2sc3c(=O)n(C4CCCCC4)cnc3c12 10.1016/j.bmcl.2012.09.048
44588464 175174 None 0 Human Functional pIC50 = 8.2 8.2 -4 3
Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 359 2 0 6 3.1 Cc1c(C2=CCN(C(=O)OC(C)(C)C)CC2)nnn1-c1ncccc1F 10.1016/j.bmc.2008.09.060
CHEMBL456823 175174 None 0 Human Functional pIC50 = 8.2 8.2 -4 3
Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 359 2 0 6 3.1 Cc1c(C2=CCN(C(=O)OC(C)(C)C)CC2)nnn1-c1ncccc1F 10.1016/j.bmc.2008.09.060
11695894 174896 None 0 Human Functional pIC50 = 8.1 8.1 -2 3
Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 345 3 0 6 2.7 Cc1c(C2=CCN(C(=O)OC(C)C)CC2)nnn1-c1cccnc1F 10.1016/j.bmc.2008.09.060
CHEMBL456196 174896 None 0 Human Functional pIC50 = 8.1 8.1 -2 3
Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 345 3 0 6 2.7 Cc1c(C2=CCN(C(=O)OC(C)C)CC2)nnn1-c1cccnc1F 10.1016/j.bmc.2008.09.060
54579958 62769 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 383 4 1 7 4.0 C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784054 62769 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 383 4 1 7 4.0 C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
16118535 71053 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 335 3 1 5 4.3 CCNc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951877 71053 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 335 3 1 5 4.3 CCNc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
57881832 83736 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 341 3 1 7 3.5 O=c1c2sc3ncnc(NC4CC4)c3c2ncn1C1CCCCC1 10.1016/j.bmcl.2012.09.048
CHEMBL2205373 83736 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 341 3 1 7 3.5 O=c1c2sc3ncnc(NC4CC4)c3c2ncn1C1CCCCC1 10.1016/j.bmcl.2012.09.048
1376 321 None 33 Human Functional pIC50 = 5.2 5.2 - 1
Ability to inhibit mGluR1-alpha-mediated PI (phospho inositol) hydrolysis was determined at BHK cells at 100 Micro M ConcentrationAbility to inhibit mGluR1-alpha-mediated PI (phospho inositol) hydrolysis was determined at BHK cells at 100 Micro M Concentration
ChEMBL 221 2 3 3 0.6 OC(=O)c1ccc2c(c1)CCC2(N)C(=O)O 10.1021/jm00019a002
2071 321 None 33 Human Functional pIC50 = 5.2 5.2 - 1
Ability to inhibit mGluR1-alpha-mediated PI (phospho inositol) hydrolysis was determined at BHK cells at 100 Micro M ConcentrationAbility to inhibit mGluR1-alpha-mediated PI (phospho inositol) hydrolysis was determined at BHK cells at 100 Micro M Concentration
ChEMBL 221 2 3 3 0.6 OC(=O)c1ccc2c(c1)CCC2(N)C(=O)O 10.1021/jm00019a002
CHEMBL313938 321 None 33 Human Functional pIC50 = 5.2 5.2 - 1
Ability to inhibit mGluR1-alpha-mediated PI (phospho inositol) hydrolysis was determined at BHK cells at 100 Micro M ConcentrationAbility to inhibit mGluR1-alpha-mediated PI (phospho inositol) hydrolysis was determined at BHK cells at 100 Micro M Concentration
ChEMBL 221 2 3 3 0.6 OC(=O)c1ccc2c(c1)CCC2(N)C(=O)O 10.1021/jm00019a002
2931812 94842 None 8 Rat Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 257 2 1 3 2.2 O=C(NC12CC3CC(CC(C3)C1)C2)c1cnccn1 10.1021/jm0611298
CHEMBL253348 94842 None 8 Rat Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 257 2 1 3 2.2 O=C(NC12CC3CC(CC(C3)C1)C2)c1cnccn1 10.1021/jm0611298
89980255 125168 None 0 Human Functional pIC50 = 5.2 5.2 -2290 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 376 3 0 5 3.2 CO[C@H](C)c1cn(C2=NCC(=O)N3CCc4c(cccc4C4CC4)C3=C2)cn1 nan
CHEMBL3644397 125168 None 0 Human Functional pIC50 = 5.2 5.2 -2290 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 376 3 0 5 3.2 CO[C@H](C)c1cn(C2=NCC(=O)N3CCc4c(cccc4C4CC4)C3=C2)cn1 nan
89980164 125135 None 0 Human Functional pIC50 = 6.2 6.2 -354 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 368 2 0 4 3.4 O=C1CN=C(n2cnc(C(F)F)c2)C=C2c3cccc(C4CC4)c3CCN12 nan
CHEMBL3644362 125135 None 0 Human Functional pIC50 = 6.2 6.2 -354 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 368 2 0 4 3.4 O=C1CN=C(n2cnc(C(F)F)c2)C=C2c3cccc(C4CC4)c3CCN12 nan
71683126 91068 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 357 2 0 3 3.5 C[C@@H]1CN(c2ncccc2F)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
CHEMBL2397343 91068 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 357 2 0 3 3.5 C[C@@H]1CN(c2ncccc2F)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
71682806 91081 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 340 2 0 4 2.7 C[C@@H]1CN(c2ncccn2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
CHEMBL2397372 91081 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 340 2 0 4 2.7 C[C@@H]1CN(c2ncccn2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
11581985 85187 None 0 Human Functional pIC50 = 7.2 7.2 1 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 394 6 0 7 3.6 CCc1ccc(-n2cnc3c(sc4nccc(N(C)CCOC)c43)c2=O)cc1 10.1021/jm0504407
CHEMBL225125 85187 None 0 Human Functional pIC50 = 7.2 7.2 1 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 394 6 0 7 3.6 CCc1ccc(-n2cnc3c(sc4nccc(N(C)CCOC)c43)c2=O)cc1 10.1021/jm0504407
44431045 86757 None 0 Rat Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay
ChEMBL 363 2 3 2 3.2 O=C(NC12CC3CC(CC(C3)C1)C2)c1ccc2[nH]c3c(c2c1)CCNC3=O 10.1016/j.bmcl.2007.01.055
CHEMBL231842 86757 None 0 Rat Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay
ChEMBL 363 2 3 2 3.2 O=C(NC12CC3CC(CC(C3)C1)C2)c1ccc2[nH]c3c(c2c1)CCNC3=O 10.1016/j.bmcl.2007.01.055
44431050 142431 None 0 Rat Functional pIC50 = 7.2 7.2 -1 2
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay
ChEMBL 363 2 3 2 3.6 O=C1NCCc2c1[nH]c1ccc(NC(=O)C34CC5CC(CC(C5)C3)C4)cc21 10.1016/j.bmcl.2007.01.055
CHEMBL388669 142431 None 0 Rat Functional pIC50 = 7.2 7.2 -1 2
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay
ChEMBL 363 2 3 2 3.6 O=C1NCCc2c1[nH]c1ccc(NC(=O)C34CC5CC(CC(C5)C3)C4)cc21 10.1016/j.bmcl.2007.01.055
86711407 125199 None 0 Human Functional pIC50 = 6.2 6.2 -117 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 348 2 1 5 1.9 O=C1CN=C(n2cnc(CO)c2)C=C2c3cccc(C4CC4)c3CCN12 nan
CHEMBL3644428 125199 None 0 Human Functional pIC50 = 6.2 6.2 -117 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 348 2 1 5 1.9 O=C1CN=C(n2cnc(CO)c2)C=C2c3cccc(C4CC4)c3CCN12 nan
71683126 91068 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 357 2 0 3 3.5 C[C@@H]1CN(c2ncccc2F)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
CHEMBL2397343 91068 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 357 2 0 3 3.5 C[C@@H]1CN(c2ncccc2F)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
45375910 5505 None 1 Rat Functional pIC50 = 6.2 6.2 -7 2
Antagonist activity at rat mGluR1 expressed in BHK cells by calcium mobilization assayAntagonist activity at rat mGluR1 expressed in BHK cells by calcium mobilization assay
ChEMBL 317 2 1 3 4.3 Fc1ccc2ncnc(Nc3cccc(Br)c3)c2c1 10.1016/j.bmcl.2009.10.024
CHEMBL1076333 5505 None 1 Rat Functional pIC50 = 6.2 6.2 -7 2
Antagonist activity at rat mGluR1 expressed in BHK cells by calcium mobilization assayAntagonist activity at rat mGluR1 expressed in BHK cells by calcium mobilization assay
ChEMBL 317 2 1 3 4.3 Fc1ccc2ncnc(Nc3cccc(Br)c3)c2c1 10.1016/j.bmcl.2009.10.024
71682806 91081 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 340 2 0 4 2.7 C[C@@H]1CN(c2ncccn2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
CHEMBL2397372 91081 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 340 2 0 4 2.7 C[C@@H]1CN(c2ncccn2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
54584889 62773 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 397 5 1 8 3.5 C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc(OC)c(F)c4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784058 62773 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 397 5 1 8 3.5 C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc(OC)c(F)c4)cnc3c12 10.1016/j.bmcl.2009.04.104
10036599 112585 None 0 Human Functional pIC50 = 4.1 4.1 - 1
Compound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysisCompound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysis
ChEMBL 225 3 4 4 0.5 Cc1cc(C(=O)O)c(O)cc1C(N)C(=O)O 10.1016/S0960-894X(97)10071-3
CHEMBL329905 112585 None 0 Human Functional pIC50 = 4.1 4.1 - 1
Compound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysisCompound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysis
ChEMBL 225 3 4 4 0.5 Cc1cc(C(=O)O)c(O)cc1C(N)C(=O)O 10.1016/S0960-894X(97)10071-3
89980507 125149 None 0 Human Functional pIC50 = 5.1 5.1 -44 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 370 1 0 6 2.3 Cc1cn(C2=NCC(=O)N3CCc4c(cccc4-c4cnccn4)C3=C2)cn1 nan
CHEMBL3644376 125149 None 0 Human Functional pIC50 = 5.1 5.1 -44 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 370 1 0 6 2.3 Cc1cn(C2=NCC(=O)N3CCc4c(cccc4-c4cnccn4)C3=C2)cn1 nan
67425269 89092 None 0 Human Functional pIC50 = 6.1 6.1 -24 2
Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay
ChEMBL 429 5 1 6 5.2 C[C@@H]1C[C@H]1C(=O)Nc1snc(-c2ccc3nn(C)cc3c2)c1-c1cccc(C2CC2)n1 10.1016/j.bmcl.2013.01.009
CHEMBL2334982 89092 None 0 Human Functional pIC50 = 6.1 6.1 -24 2
Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay
ChEMBL 429 5 1 6 5.2 C[C@@H]1C[C@H]1C(=O)Nc1snc(-c2ccc3nn(C)cc3c2)c1-c1cccc(C2CC2)n1 10.1016/j.bmcl.2013.01.009
CHEMBL2364958 89092 None 0 Human Functional pIC50 = 6.1 6.1 -24 2
Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay
ChEMBL 429 5 1 6 5.2 C[C@@H]1C[C@H]1C(=O)Nc1snc(-c2ccc3nn(C)cc3c2)c1-c1cccc(C2CC2)n1 10.1016/j.bmcl.2013.01.009
78320802 114405 None 4 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay
ChEMBL 330 3 0 4 4.8 C=Cc1cccc(-n2cnc3c(-c4ccccc4)csc3c2=O)c1 10.1016/j.ejmech.2014.08.027
CHEMBL3330812 114405 None 4 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay
ChEMBL 330 3 0 4 4.8 C=Cc1cccc(-n2cnc3c(-c4ccccc4)csc3c2=O)c1 10.1016/j.ejmech.2014.08.027
78320802 114405 None 4 Human Functional pIC50 = 7.1 7.1 - 1
FLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and diluteFLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and dilute
ChEMBL 330 3 0 4 4.8 C=Cc1cccc(-n2cnc3c(-c4ccccc4)csc3c2=O)c1 nan
CHEMBL3330812 114405 None 4 Human Functional pIC50 = 7.1 7.1 - 1
FLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and diluteFLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and dilute
ChEMBL 330 3 0 4 4.8 C=Cc1cccc(-n2cnc3c(-c4ccccc4)csc3c2=O)c1 nan
5766229 198373 None 2 Rat Functional pIC50 = 6.1 6.1 - 1
Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting
ChEMBL 313 3 0 3 5.2 Cc1ccc2nc(Cl)c(/C=C/C(=O)c3cccs3)cc2c1 10.1016/j.bmc.2009.05.072
CHEMBL559310 198373 None 2 Rat Functional pIC50 = 6.1 6.1 - 1
Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting
ChEMBL 313 3 0 3 5.2 Cc1ccc2nc(Cl)c(/C=C/C(=O)c3cccs3)cc2c1 10.1016/j.bmc.2009.05.072
44445036 155084 None 0 Rat Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 283 2 1 4 3.6 N#Cc1cc2c(nc1NC1CCCCCC1)CCCC2=O 10.1021/jm0611298
CHEMBL401330 155084 None 0 Rat Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 283 2 1 4 3.6 N#Cc1cc2c(nc1NC1CCCCCC1)CCCC2=O 10.1021/jm0611298
78322063 114412 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay
ChEMBL 364 4 0 6 4.1 COc1ccc(-n2cnc3c(-c4ccccc4OC)csc3c2=O)cc1 10.1016/j.ejmech.2014.08.027
CHEMBL3330826 114412 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay
ChEMBL 364 4 0 6 4.1 COc1ccc(-n2cnc3c(-c4ccccc4OC)csc3c2=O)cc1 10.1016/j.ejmech.2014.08.027
16117300 71050 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 355 3 1 6 3.8 CNc1ccnc2sc3c(=O)n(-c4ccc(OC)c(F)c4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951874 71050 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 355 3 1 6 3.8 CNc1ccnc2sc3c(=O)n(-c4ccc(OC)c(F)c4)ccc3c12 10.1016/j.bmcl.2011.12.131
127034014 139095 None 0 Rat Functional pIC50 = 6.1 6.1 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 335 2 1 5 4.1 Cc1nc(N[C@@H]2C[C@@H]3C[C@H]([C@H]2C)C3(C)C)c2nn3ccccc3c2n1 10.1016/j.bmcl.2016.03.026
CHEMBL3785636 139095 None 0 Rat Functional pIC50 = 6.1 6.1 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 335 2 1 5 4.1 Cc1nc(N[C@@H]2C[C@@H]3C[C@H]([C@H]2C)C3(C)C)c2nn3ccccc3c2n1 10.1016/j.bmcl.2016.03.026
122196116 124317 None 0 Human Functional pIC50 = 6.1 6.1 5 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 362 3 1 6 2.7 Cc1ccoc1C(=O)Nc1cnc(N2C(=O)c3cccc(C)c3C2=O)nc1 10.1016/j.bmcl.2015.10.013
CHEMBL3634438 124317 None 0 Human Functional pIC50 = 6.1 6.1 5 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 362 3 1 6 2.7 Cc1ccoc1C(=O)Nc1cnc(N2C(=O)c3cccc(C)c3C2=O)nc1 10.1016/j.bmcl.2015.10.013
127034014 139095 None 0 Rat Functional pIC50 = 6.1 6.1 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 335 2 1 5 4.1 Cc1nc(N[C@@H]2C[C@@H]3C[C@H]([C@H]2C)C3(C)C)c2nn3ccccc3c2n1 10.1016/j.bmcl.2016.03.026
CHEMBL3785636 139095 None 0 Rat Functional pIC50 = 6.1 6.1 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 335 2 1 5 4.1 Cc1nc(N[C@@H]2C[C@@H]3C[C@H]([C@H]2C)C3(C)C)c2nn3ccccc3c2n1 10.1016/j.bmcl.2016.03.026
11696595 85098 None 0 Human Functional pIC50 = 7.1 7.1 1 3
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 380 2 0 6 4.0 CN(C)c1ccnc2sc3c(=O)n(C45CC6CC(CC(C6)C4)C5)cnc3c12 10.1021/jm0504407
CHEMBL224322 85098 None 0 Human Functional pIC50 = 7.1 7.1 1 3
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 380 2 0 6 4.0 CN(C)c1ccnc2sc3c(=O)n(C45CC6CC(CC(C6)C4)C5)cnc3c12 10.1021/jm0504407
44442423 93707 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay
ChEMBL 322 2 0 5 3.8 Cc1nc2c(cnn2-c2ccccc2)c(=O)n1C1CCCCCC1 10.1016/j.bmcl.2007.05.028
CHEMBL246840 93707 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay
ChEMBL 322 2 0 5 3.8 Cc1nc2c(cnn2-c2ccccc2)c(=O)n1C1CCCCCC1 10.1016/j.bmcl.2007.05.028
24777319 154764 None 0 Rat Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 390 3 0 6 3.4 COc1ccc(N2CCN(c3nc4c(cc3C#N)C(=O)CC(C)(C)C4)CC2)cc1 10.1021/jm0611298
CHEMBL399640 154764 None 0 Rat Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 390 3 0 6 3.4 COc1ccc(N2CCN(c3nc4c(cc3C#N)C(=O)CC(C)(C)C4)CC2)cc1 10.1021/jm0611298
89979742 133171 None 0 Human Functional pIC50 = 6.1 6.1 -44 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 402 2 0 7 3.0 O=C1CN=C(n2cnc(C3CC3)n2)C=C2c3cccc(-c4nccs4)c3CCN12 nan
CHEMBL3702443 133171 None 0 Human Functional pIC50 = 6.1 6.1 -44 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 402 2 0 7 3.0 O=C1CN=C(n2cnc(C3CC3)n2)C=C2c3cccc(-c4nccs4)c3CCN12 nan
72163838 92057 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 354 1 0 3 3.2 O=C(N1CCC2(CCCC2)CC1)N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1 10.1016/j.bmcl.2013.07.029
CHEMBL2418360 92057 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 354 1 0 3 3.2 O=C(N1CCC2(CCCC2)CC1)N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1 10.1016/j.bmcl.2013.07.029
45486778 201325 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 385 5 0 6 3.9 CC(C)N(C)c1cc(-c2csc(N(C)C(=O)c3ccc(F)cc3)n2)ncn1 10.1016/j.bmcl.2009.07.097
CHEMBL584066 201325 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 385 5 0 6 3.9 CC(C)N(C)c1cc(-c2csc(N(C)C(=O)c3ccc(F)cc3)n2)ncn1 10.1016/j.bmcl.2009.07.097
72163838 92057 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 354 1 0 3 3.2 O=C(N1CCC2(CCCC2)CC1)N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1 10.1016/j.bmcl.2013.07.029
CHEMBL2418360 92057 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 354 1 0 3 3.2 O=C(N1CCC2(CCCC2)CC1)N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1 10.1016/j.bmcl.2013.07.029
1284324 93977 None 5 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay
ChEMBL 380 2 0 5 3.6 Cc1nc2c(cnn2-c2ccccc2)c(=O)n1-c1ccc(Br)cc1 10.1016/j.bmcl.2007.05.028
CHEMBL248208 93977 None 5 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay
ChEMBL 380 2 0 5 3.6 Cc1nc2c(cnn2-c2ccccc2)c(=O)n1-c1ccc(Br)cc1 10.1016/j.bmcl.2007.05.028
24777314 154854 None 0 Rat Functional pIC50 = 7.1 7.1 630 2
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 283 2 1 4 3.5 CC1(C)CC(=O)c2cc(C#N)c(NC3CCCC3)nc2C1 10.1021/jm0611298
CHEMBL400105 154854 None 0 Rat Functional pIC50 = 7.1 7.1 630 2
Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate
ChEMBL 283 2 1 4 3.5 CC1(C)CC(=O)c2cc(C#N)c(NC3CCCC3)nc2C1 10.1021/jm0611298
1378 2417 None 39 Human Functional pIC50 = 5.1 5.1 -1047 14
Antagonistic activity against metabotropic glutamate receptor 1 (mGluR1) was evaluatedAntagonistic activity against metabotropic glutamate receptor 1 (mGluR1) was evaluated
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1016/s0960-894x(98)00510-1
1399 2417 None 39 Human Functional pIC50 = 5.1 5.1 -1047 14
Antagonistic activity against metabotropic glutamate receptor 1 (mGluR1) was evaluatedAntagonistic activity against metabotropic glutamate receptor 1 (mGluR1) was evaluated
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1016/s0960-894x(98)00510-1
9819927 2417 None 39 Human Functional pIC50 = 5.1 5.1 -1047 14
Antagonistic activity against metabotropic glutamate receptor 1 (mGluR1) was evaluatedAntagonistic activity against metabotropic glutamate receptor 1 (mGluR1) was evaluated
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1016/s0960-894x(98)00510-1
CHEMBL432038 2417 None 39 Human Functional pIC50 = 5.1 5.1 -1047 14
Antagonistic activity against metabotropic glutamate receptor 1 (mGluR1) was evaluatedAntagonistic activity against metabotropic glutamate receptor 1 (mGluR1) 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
16118946 71010 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 348 3 0 5 4.5 COc1ccnc2sc3c(=O)n(-c4ccc(C5CC5)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951676 71010 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 348 3 0 5 4.5 COc1ccnc2sc3c(=O)n(-c4ccc(C5CC5)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
24777812 94967 None 0 Rat Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at rat mGluR1 by FLIPR assayAntagonist activity at rat mGluR1 by FLIPR assay
ChEMBL 292 2 1 3 4.2 CC1(C)CC(=O)c2cc(Cl)c(NC3CCCC3)nc2C1 10.1021/jm0611298
CHEMBL254221 94967 None 0 Rat Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at rat mGluR1 by FLIPR assayAntagonist activity at rat mGluR1 by FLIPR assay
ChEMBL 292 2 1 3 4.2 CC1(C)CC(=O)c2cc(Cl)c(NC3CCCC3)nc2C1 10.1021/jm0611298
57559301 83861 None 0 Human Functional pIC50 = 8.1 8.1 1258 2
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 369 3 0 8 3.2 CSc1ccc(-n2cnc3c(sc4ncnc(N(C)C)c43)c2=O)cc1 10.1016/j.bmcl.2012.09.048
CHEMBL2205927 83861 None 0 Human Functional pIC50 = 8.1 8.1 1258 2
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 369 3 0 8 3.2 CSc1ccc(-n2cnc3c(sc4ncnc(N(C)C)c43)c2=O)cc1 10.1016/j.bmcl.2012.09.048
73335237 133108 None 0 Human Functional pIC50 = 8.1 8.1 11 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 372 1 0 3 3.7 O=C1CN=C(c2cccs2)C=C2c3cccc(Br)c3CCN12 nan
CHEMBL3702381 133108 None 0 Human Functional pIC50 = 8.1 8.1 11 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 372 1 0 3 3.7 O=C1CN=C(c2cccs2)C=C2c3cccc(Br)c3CCN12 nan
16117979 71000 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 327 2 0 5 4.2 CN(C)c1ccnc2sc3c(=O)n(C4CCCCC4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951665 71000 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 327 2 0 5 4.2 CN(C)c1ccnc2sc3c(=O)n(C4CCCCC4)ccc3c12 10.1016/j.bmcl.2011.12.131
54582945 62787 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 351 3 1 7 2.6 C#CCNc1ncnc2sc3c(=O)n(-c4ccc(F)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784072 62787 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 351 3 1 7 2.6 C#CCNc1ncnc2sc3c(=O)n(-c4ccc(F)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
16118122 70999 None 0 Human Functional pIC50 = 8.1 8.1 63 2
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 349 3 0 5 4.2 CCc1ccc(-n2ccc3c(sc4nccc(N(C)C)c43)c2=O)cc1 10.1016/j.bmcl.2011.12.131
CHEMBL1951664 70999 None 0 Human Functional pIC50 = 8.1 8.1 63 2
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 349 3 0 5 4.2 CCc1ccc(-n2ccc3c(sc4nccc(N(C)C)c43)c2=O)cc1 10.1016/j.bmcl.2011.12.131
54584890 62780 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 405 4 1 8 4.6 C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc5sccc5c4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784065 62780 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 405 4 1 8 4.6 C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc5sccc5c4)cnc3c12 10.1016/j.bmcl.2009.04.104
16661406 200773 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 295 3 0 4 3.5 CN(C(=O)c1ccccc1)c1nc(-c2ccncc2)cs1 10.1016/j.bmcl.2009.07.097
CHEMBL576121 200773 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 295 3 0 4 3.5 CN(C(=O)c1ccccc1)c1nc(-c2ccncc2)cs1 10.1016/j.bmcl.2009.07.097
86729807 150548 None 4 Human Functional pIC50 = 7.1 7.1 - 1
FLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and diluteFLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and dilute
ChEMBL 352 2 0 4 5.1 Cc1ccc(-c2csc3c(=O)n(-c4ccc(Cl)cc4)cnc23)cc1 nan
CHEMBL3954190 150548 None 4 Human Functional pIC50 = 7.1 7.1 - 1
FLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and diluteFLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and dilute
ChEMBL 352 2 0 4 5.1 Cc1ccc(-c2csc3c(=O)n(-c4ccc(Cl)cc4)cnc23)cc1 nan
44442422 93706 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay
ChEMBL 354 2 0 5 3.7 Cc1nc2c(cnn2-c2ccccc2)c(=O)n1-c1ccc(Cl)c(F)c1 10.1016/j.bmcl.2007.05.028
CHEMBL246839 93706 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay
ChEMBL 354 2 0 5 3.7 Cc1nc2c(cnn2-c2ccccc2)c(=O)n1-c1ccc(Cl)c(F)c1 10.1016/j.bmcl.2007.05.028
89980420 133099 None 0 Human Functional pIC50 = 6.1 6.1 5 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 312 1 0 3 3.1 O=C1CN=C(c2cccs2)C=C2c3cccc(F)c3CCN12 nan
CHEMBL3702372 133099 None 0 Human Functional pIC50 = 6.1 6.1 5 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 312 1 0 3 3.1 O=C1CN=C(c2cccs2)C=C2c3cccc(F)c3CCN12 nan
16661729 199565 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 341 5 0 4 4.4 CCCN(C(=O)c1ccc(F)cc1)c1nc(-c2ccccn2)cs1 10.1016/j.bmcl.2009.07.097
CHEMBL567673 199565 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 341 5 0 4 4.4 CCCN(C(=O)c1ccc(F)cc1)c1nc(-c2ccccn2)cs1 10.1016/j.bmcl.2009.07.097
89980559 125138 None 0 Human Functional pIC50 = 6.1 6.1 -407 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 381 3 0 6 2.1 COCc1ncn(C2=NCC(=O)N3CCc4c(ccc(F)c4C4CC4)C3=C2)n1 nan
CHEMBL3644365 125138 None 0 Human Functional pIC50 = 6.1 6.1 -407 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 381 3 0 6 2.1 COCc1ncn(C2=NCC(=O)N3CCc4c(ccc(F)c4C4CC4)C3=C2)n1 nan
57881906 83735 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 353 3 1 7 3.1 O=c1c2sc3ncnc(NC4CC4)c3c2ncn1-c1ccc(F)cc1 10.1016/j.bmcl.2012.09.048
CHEMBL2205372 83735 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 353 3 1 7 3.1 O=c1c2sc3ncnc(NC4CC4)c3c2ncn1-c1ccc(F)cc1 10.1016/j.bmcl.2012.09.048
11493585 85087 None 0 Human Functional pIC50 = 7.1 7.1 11 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 326 2 0 6 3.4 CC1CCC(n2cnc3c(oc4nccc(N(C)C)c43)c2=O)CC1 10.1021/jm0504407
CHEMBL224200 85087 None 0 Human Functional pIC50 = 7.1 7.1 11 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 326 2 0 6 3.4 CC1CCC(n2cnc3c(oc4nccc(N(C)C)c43)c2=O)CC1 10.1021/jm0504407
89979749 133187 None 0 Human Functional pIC50 = 5.1 5.1 -66 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 384 2 1 5 2.8 O=C1CN=C(n2cnc(C3CC3)c2)C=C2c3cccc(-c4cc[nH]n4)c3CCN12 nan
CHEMBL3702461 133187 None 0 Human Functional pIC50 = 5.1 5.1 -66 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 384 2 1 5 2.8 O=C1CN=C(n2cnc(C3CC3)c2)C=C2c3cccc(-c4cc[nH]n4)c3CCN12 nan
16661405 201107 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 309 3 0 4 3.8 Cc1ccc(C(=O)N(C)c2nc(-c3ccncc3)cs2)cc1 10.1016/j.bmcl.2009.07.097
CHEMBL579225 201107 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 309 3 0 4 3.8 Cc1ccc(C(=O)N(C)c2nc(-c3ccncc3)cs2)cc1 10.1016/j.bmcl.2009.07.097
127034283 139149 None 0 Rat Functional pIC50 = 7.1 7.1 20 2
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 319 2 1 5 3.5 c1ccn2nc3c(NC4C5CC6CC(C5)CC4C6)ncnc3c2c1 10.1016/j.bmcl.2016.03.026
CHEMBL3786284 139149 None 0 Rat Functional pIC50 = 7.1 7.1 20 2
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 319 2 1 5 3.5 c1ccn2nc3c(NC4C5CC6CC(C5)CC4C6)ncnc3c2c1 10.1016/j.bmcl.2016.03.026
72163721 92070 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 376 2 0 4 3.1 N#Cc1ccncc1N1C[C@H]2CN(C(=O)C34CC5CC(CC(C5)C3)C4)C[C@H]2C1 10.1016/j.bmcl.2013.07.029
CHEMBL2418385 92070 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 376 2 0 4 3.1 N#Cc1ccncc1N1C[C@H]2CN(C(=O)C34CC5CC(CC(C5)C3)C4)C[C@H]2C1 10.1016/j.bmcl.2013.07.029
72163721 92070 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 376 2 0 4 3.1 N#Cc1ccncc1N1C[C@H]2CN(C(=O)C34CC5CC(CC(C5)C3)C4)C[C@H]2C1 10.1016/j.bmcl.2013.07.029
CHEMBL2418385 92070 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 376 2 0 4 3.1 N#Cc1ccncc1N1C[C@H]2CN(C(=O)C34CC5CC(CC(C5)C3)C4)C[C@H]2C1 10.1016/j.bmcl.2013.07.029
11530971 85194 None 0 Human Functional pIC50 = 7.1 7.1 1 3
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 378 4 0 6 4.2 CCc1ccc(-n2c(CC)nc3c(sc4nccc(N(C)C)c43)c2=O)cc1 10.1021/jm0504407
CHEMBL225201 85194 None 0 Human Functional pIC50 = 7.1 7.1 1 3
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 378 4 0 6 4.2 CCc1ccc(-n2c(CC)nc3c(sc4nccc(N(C)C)c43)c2=O)cc1 10.1021/jm0504407
127034283 139149 None 0 Rat Functional pIC50 = 7.1 7.1 20 2
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 319 2 1 5 3.5 c1ccn2nc3c(NC4C5CC6CC(C5)CC4C6)ncnc3c2c1 10.1016/j.bmcl.2016.03.026
CHEMBL3786284 139149 None 0 Rat Functional pIC50 = 7.1 7.1 20 2
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 319 2 1 5 3.5 c1ccn2nc3c(NC4C5CC6CC(C5)CC4C6)ncnc3c2c1 10.1016/j.bmcl.2016.03.026
54582005 62788 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 381 4 1 8 2.6 C#CCNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4F)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784073 62788 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 381 4 1 8 2.6 C#CCNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4F)cnc3c12 10.1016/j.bmcl.2009.04.104
16118949 71007 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 322 2 0 5 3.9 COc1ccnc2sc3c(=O)n(-c4ccccc4C)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951673 71007 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 322 2 0 5 3.9 COc1ccnc2sc3c(=O)n(-c4ccccc4C)ccc3c12 10.1016/j.bmcl.2011.12.131
72163432 92061 None 0 Human Functional pIC50 = 7.1 7.1 39 3
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 351 2 0 3 3.2 O=C(N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.07.029
CHEMBL2418364 92061 None 0 Human Functional pIC50 = 7.1 7.1 39 3
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 351 2 0 3 3.2 O=C(N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.07.029
72163432 92061 None 0 Human Functional pIC50 = 7.1 7.1 39 3
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 351 2 0 3 3.2 O=C(N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.07.029
CHEMBL2418364 92061 None 0 Human Functional pIC50 = 7.1 7.1 39 3
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 351 2 0 3 3.2 O=C(N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.07.029
5766225 198605 None 6 Rat Functional pIC50 = 5.1 5.1 - 1
Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting
ChEMBL 307 3 0 2 5.1 Cc1cccc2cc(/C=C/C(=O)c3ccccc3)c(Cl)nc12 10.1016/j.bmc.2009.05.072
CHEMBL561189 198605 None 6 Rat Functional pIC50 = 5.1 5.1 - 1
Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting
ChEMBL 307 3 0 2 5.1 Cc1cccc2cc(/C=C/C(=O)c3ccccc3)c(Cl)nc12 10.1016/j.bmc.2009.05.072
44421618 85229 None 0 Human Functional pIC50 = 5.1 5.1 1 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 378 2 0 6 4.4 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(C(C)(C)C)cc4)cnc3c12 10.1021/jm0504407
CHEMBL225439 85229 None 0 Human Functional pIC50 = 5.1 5.1 1 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 378 2 0 6 4.4 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(C(C)(C)C)cc4)cnc3c12 10.1021/jm0504407
57559370 83847 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 369 5 2 9 1.8 COc1ccc(-n2cnc3c(sc4ncnc(NCCO)c43)c2=O)cc1 10.1016/j.bmcl.2012.09.048
CHEMBL2205912 83847 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 369 5 2 9 1.8 COc1ccc(-n2cnc3c(sc4ncnc(NCCO)c43)c2=O)cc1 10.1016/j.bmcl.2012.09.048
49788729 18126 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiologyAntagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiology
ChEMBL 535 18 5 5 4.2 NCCCNCCCCNCCCNC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm100886h
CHEMBL1269125 18126 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiologyAntagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiology
ChEMBL 535 18 5 5 4.2 NCCCNCCCCNCCCNC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm100886h
11588590 142122 None 0 Human Functional pIC50 = 7.1 7.1 1 3
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 362 3 0 6 3.9 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(C5CC5)cc4)cnc3c12 10.1021/jm0504407
CHEMBL387687 142122 None 0 Human Functional pIC50 = 7.1 7.1 1 3
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 362 3 0 6 3.9 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(C5CC5)cc4)cnc3c12 10.1021/jm0504407
16117303 71051 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 355 3 1 6 3.8 CNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4F)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951875 71051 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 355 3 1 6 3.8 CNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4F)ccc3c12 10.1016/j.bmcl.2011.12.131
16117433 71060 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 338 3 1 7 3.0 CNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951884 71060 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 338 3 1 7 3.0 CNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
45484905 200808 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL 335 4 0 5 3.1 Cc1c(-c2ccc(C(=O)N(C)C(C)C)cc2)nnn1-c1cccnc1 10.1016/j.bmcl.2009.07.145
CHEMBL576434 200808 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR
ChEMBL 335 4 0 5 3.1 Cc1c(-c2ccc(C(=O)N(C)C(C)C)cc2)nnn1-c1cccnc1 10.1016/j.bmcl.2009.07.145
1379 2420 None 35 Human Functional pIC50 = 5.1 5.1 - 1
Compound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysisCompound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysis
ChEMBL 209 3 3 3 0.8 OC(=O)c1ccc(c(c1)C)[C@@H](C(=O)O)N 10.1016/S0960-894X(97)10071-3
5311261 2420 None 35 Human Functional pIC50 = 5.1 5.1 - 1
Compound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysisCompound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysis
ChEMBL 209 3 3 3 0.8 OC(=O)c1ccc(c(c1)C)[C@@H](C(=O)O)N 10.1016/S0960-894X(97)10071-3
CHEMBL94631 2420 None 35 Human Functional pIC50 = 5.1 5.1 - 1
Compound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysisCompound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysis
ChEMBL 209 3 3 3 0.8 OC(=O)c1ccc(c(c1)C)[C@@H](C(=O)O)N 10.1016/S0960-894X(97)10071-3
1379 2420 None 35 Human Functional pIC50 = 5.1 5.1 - 1
Compound was tested for its agonist activity against Ser165 and Thr188 (Metabotropic glutamate receptor 1) receptor.Compound was tested for its agonist activity against Ser165 and Thr188 (Metabotropic glutamate receptor 1) receptor.
ChEMBL 209 3 3 3 0.8 OC(=O)c1ccc(c(c1)C)[C@@H](C(=O)O)N 10.1021/jm990353c
5311261 2420 None 35 Human Functional pIC50 = 5.1 5.1 - 1
Compound was tested for its agonist activity against Ser165 and Thr188 (Metabotropic glutamate receptor 1) receptor.Compound was tested for its agonist activity against Ser165 and Thr188 (Metabotropic glutamate receptor 1) receptor.
ChEMBL 209 3 3 3 0.8 OC(=O)c1ccc(c(c1)C)[C@@H](C(=O)O)N 10.1021/jm990353c
CHEMBL94631 2420 None 35 Human Functional pIC50 = 5.1 5.1 - 1
Compound was tested for its agonist activity against Ser165 and Thr188 (Metabotropic glutamate receptor 1) receptor.Compound was tested for its agonist activity against Ser165 and Thr188 (Metabotropic glutamate receptor 1) receptor.
ChEMBL 209 3 3 3 0.8 OC(=O)c1ccc(c(c1)C)[C@@H](C(=O)O)N 10.1021/jm990353c
127033445 139074 None 0 Rat Functional pIC50 = 6.1 6.1 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 269 2 1 5 3.1 C[C@@H](Nc1ncnc2c1nn1ccccc21)C(C)(C)C 10.1016/j.bmcl.2016.03.026
CHEMBL3785407 139074 None 0 Rat Functional pIC50 = 6.1 6.1 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 269 2 1 5 3.1 C[C@@H](Nc1ncnc2c1nn1ccccc21)C(C)(C)C 10.1016/j.bmcl.2016.03.026
122196099 124301 None 0 Human Functional pIC50 = 7.1 7.1 10 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 360 3 1 4 3.9 Cc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2ccccc2C1=O 10.1016/j.bmcl.2015.10.013
CHEMBL3634422 124301 None 0 Human Functional pIC50 = 7.1 7.1 10 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 360 3 1 4 3.9 Cc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2ccccc2C1=O 10.1016/j.bmcl.2015.10.013
89980785 125165 None 0 Human Functional pIC50 = 6.1 6.1 -125 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 388 3 0 5 3.3 COCc1cn(C2=NCC(=O)N3CCc4c(C5=CCCC5)cccc4C3=C2)cn1 nan
CHEMBL3644394 125165 None 0 Human Functional pIC50 = 6.1 6.1 -125 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 388 3 0 5 3.3 COCc1cn(C2=NCC(=O)N3CCc4c(C5=CCCC5)cccc4C3=C2)cn1 nan
89979907 133134 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 335 2 1 5 2.0 COc1cccc2c1CCN1C(=O)CN=C(c3cccc(O)n3)C=C21 nan
CHEMBL3702407 133134 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 335 2 1 5 2.0 COc1cccc2c1CCN1C(=O)CN=C(c3cccc(O)n3)C=C21 nan
71559536 87554 None 0 Human Functional pIC50 = 6.1 6.1 -33 2
Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay
ChEMBL 457 5 1 6 6.0 C[C@@H]1C[C@H]1C(=O)Nc1snc(-c2ccc3nn(C)cc3c2)c1-c1cccc(C2CCCC2)n1 10.1016/j.bmcl.2013.01.009
CHEMBL2334984 87554 None 0 Human Functional pIC50 = 6.1 6.1 -33 2
Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay
ChEMBL 457 5 1 6 6.0 C[C@@H]1C[C@H]1C(=O)Nc1snc(-c2ccc3nn(C)cc3c2)c1-c1cccc(C2CCCC2)n1 10.1016/j.bmcl.2013.01.009
127033445 139074 None 0 Rat Functional pIC50 = 6.1 6.1 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 269 2 1 5 3.1 C[C@@H](Nc1ncnc2c1nn1ccccc21)C(C)(C)C 10.1016/j.bmcl.2016.03.026
CHEMBL3785407 139074 None 0 Rat Functional pIC50 = 6.1 6.1 - 1
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 269 2 1 5 3.1 C[C@@H](Nc1ncnc2c1nn1ccccc21)C(C)(C)C 10.1016/j.bmcl.2016.03.026
57404255 73237 None 1 Human Functional pIC50 = 8.1 8.1 -18 3
Allosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assayAllosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assay
ChEMBL 302 4 1 4 3.7 COc1ccc(-c2nsc(NC(=O)[C@@H]3C[C@H]3C)c2C)cc1 10.1016/j.bmcl.2012.02.003
CHEMBL2011870 73237 None 1 Human Functional pIC50 = 8.1 8.1 -18 3
Allosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assayAllosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assay
ChEMBL 302 4 1 4 3.7 COc1ccc(-c2nsc(NC(=O)[C@@H]3C[C@H]3C)c2C)cc1 10.1016/j.bmcl.2012.02.003
24884476 73243 None 0 Human Functional pIC50 = 8.1 8.1 138 2
Allosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assayAllosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assay
ChEMBL 306 3 1 3 4.4 Cc1c(-c2ccc(Cl)cc2)nsc1NC(=O)[C@@H]1C[C@H]1C 10.1016/j.bmcl.2012.02.003
CHEMBL2011876 73243 None 0 Human Functional pIC50 = 8.1 8.1 138 2
Allosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assayAllosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assay
ChEMBL 306 3 1 3 4.4 Cc1c(-c2ccc(Cl)cc2)nsc1NC(=O)[C@@H]1C[C@H]1C 10.1016/j.bmcl.2012.02.003
57559572 83733 None 0 Human Functional pIC50 = 8.1 8.1 1122 2
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 349 3 1 7 3.3 Cc1ccc(-n2cnc3c(sc4ncnc(NC5CC5)c43)c2=O)cc1 10.1016/j.bmcl.2012.09.048
CHEMBL2205370 83733 None 0 Human Functional pIC50 = 8.1 8.1 1122 2
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 349 3 1 7 3.3 Cc1ccc(-n2cnc3c(sc4ncnc(NC5CC5)c43)c2=O)cc1 10.1016/j.bmcl.2012.09.048
57881727 83849 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 397 7 2 9 2.6 COc1ccc(-n2cnc3c(sc4ncnc(NCCCCO)c43)c2=O)cc1 10.1016/j.bmcl.2012.09.048
CHEMBL2205914 83849 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 397 7 2 9 2.6 COc1ccc(-n2cnc3c(sc4ncnc(NCCCCO)c43)c2=O)cc1 10.1016/j.bmcl.2012.09.048
11717278 85072 None 0 Human Functional pIC50 = 8.1 8.1 1 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 350 3 0 6 3.6 CCc1cccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)c1 10.1021/jm0504407
CHEMBL224084 85072 None 0 Human Functional pIC50 = 8.1 8.1 1 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 350 3 0 6 3.6 CCc1cccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)c1 10.1021/jm0504407
57404255 73237 None 1 Human Functional pIC50 = 8.1 8.1 -18 3
Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay
ChEMBL 302 4 1 4 3.7 COc1ccc(-c2nsc(NC(=O)[C@@H]3C[C@H]3C)c2C)cc1 10.1016/j.bmcl.2013.01.009
CHEMBL2011870 73237 None 1 Human Functional pIC50 = 8.1 8.1 -18 3
Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay
ChEMBL 302 4 1 4 3.7 COc1ccc(-c2nsc(NC(=O)[C@@H]3C[C@H]3C)c2C)cc1 10.1016/j.bmcl.2013.01.009
1208332 167151 None 13 Human Functional pIC50 = 8.0 8.0 1047 2
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 352 3 0 7 3.1 COc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1 10.1016/j.bmcl.2009.04.104
1208332 167151 None 13 Human Functional pIC50 = 8.0 8.0 1047 2
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 352 3 0 7 3.1 COc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1 10.1016/j.bmcl.2010.03.004
CHEMBL428909 167151 None 13 Human Functional pIC50 = 8.0 8.0 1047 2
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 352 3 0 7 3.1 COc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1 10.1016/j.bmcl.2009.04.104
CHEMBL428909 167151 None 13 Human Functional pIC50 = 8.0 8.0 1047 2
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 352 3 0 7 3.1 COc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1 10.1016/j.bmcl.2010.03.004
1208332 167151 None 13 Human Functional pIC50 = 8.0 8.0 1047 2
Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay
ChEMBL 352 3 0 7 3.1 COc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1 10.1021/jm070590c
CHEMBL428909 167151 None 13 Human Functional pIC50 = 8.0 8.0 1047 2
Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay
ChEMBL 352 3 0 7 3.1 COc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1 10.1021/jm070590c
54582942 62771 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 379 5 1 8 3.4 C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784056 62771 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 379 5 1 8 3.4 C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
19705292 189312 None 0 Human Functional pIC50 = 8.0 8.0 2 3
Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 326 2 0 5 3.3 CC(C)(C)OC(=O)N1CC=C(c2cn(-c3ccccc3)nn2)CC1 10.1016/j.bmc.2008.09.060
CHEMBL511355 189312 None 0 Human Functional pIC50 = 8.0 8.0 2 3
Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay
ChEMBL 326 2 0 5 3.3 CC(C)(C)OC(=O)N1CC=C(c2cn(-c3ccccc3)nn2)CC1 10.1016/j.bmc.2008.09.060
16659964 89994 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay
ChEMBL 367 1 0 7 3.5 Cn1cnc2cnc3sc4c(=O)n(-c5ccc(Cl)cc5)cnc4c3c21 10.1021/jm070590c
CHEMBL238090 89994 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay
ChEMBL 367 1 0 7 3.5 Cn1cnc2cnc3sc4c(=O)n(-c5ccc(Cl)cc5)cnc4c3c21 10.1021/jm070590c
16118400 71054 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 347 3 1 5 4.5 Cc1ccc(-n2ccc3c(sc4nccc(NC5CC5)c43)c2=O)cc1 10.1016/j.bmcl.2011.12.131
CHEMBL1951878 71054 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1
ChEMBL 347 3 1 5 4.5 Cc1ccc(-n2ccc3c(sc4nccc(NC5CC5)c43)c2=O)cc1 10.1016/j.bmcl.2011.12.131
44442424 93941 None 0 Human Functional pIC50 = 7.0 7.0 30 2
Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay
ChEMBL 309 2 0 6 2.0 Cc1nc2c(cnn2-c2ccccc2)c(=O)n1N1CCCCC1 10.1016/j.bmcl.2007.05.028
CHEMBL248052 93941 None 0 Human Functional pIC50 = 7.0 7.0 30 2
Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay
ChEMBL 309 2 0 6 2.0 Cc1nc2c(cnn2-c2ccccc2)c(=O)n1N1CCCCC1 10.1016/j.bmcl.2007.05.028
67181122 73240 None 0 Human Functional pIC50 = 7.0 7.0 -4 2
Allosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assayAllosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assay
ChEMBL 316 5 1 4 4.1 CCOc1ccc(-c2nsc(NC(=O)[C@@H]3C[C@H]3C)c2C)cc1 10.1016/j.bmcl.2012.02.003
CHEMBL2011873 73240 None 0 Human Functional pIC50 = 7.0 7.0 -4 2
Allosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assayAllosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assay
ChEMBL 316 5 1 4 4.1 CCOc1ccc(-c2nsc(NC(=O)[C@@H]3C[C@H]3C)c2C)cc1 10.1016/j.bmcl.2012.02.003
44431046 86758 None 0 Rat Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay
ChEMBL 363 2 3 2 3.0 O=C(NC1C2CC3CC(C2)CC1C3)c1ccc2[nH]c3c(c2c1)CCNC3=O 10.1016/j.bmcl.2007.01.055
CHEMBL231843 86758 None 0 Rat Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay
ChEMBL 363 2 3 2 3.0 O=C(NC1C2CC3CC(C2)CC1C3)c1ccc2[nH]c3c(c2c1)CCNC3=O 10.1016/j.bmcl.2007.01.055
73335239 133112 None 0 Human Functional pIC50 = 7.0 7.0 -2 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 404 1 0 3 3.1 O=C1CN=C(c2ccoc2)C=C2c3cccc(I)c3CCN12 nan
CHEMBL3702385 133112 None 0 Human Functional pIC50 = 7.0 7.0 -2 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 404 1 0 3 3.1 O=C1CN=C(c2ccoc2)C=C2c3cccc(I)c3CCN12 nan
72163583 92065 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 369 2 0 3 3.3 O=C(N1C[C@@H]2CN(c3cccc(F)n3)C[C@@H]2C1)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.07.029
CHEMBL2418380 92065 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 369 2 0 3 3.3 O=C(N1C[C@@H]2CN(c3cccc(F)n3)C[C@@H]2C1)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.07.029
127030962 139132 None 0 Rat Functional pIC50 = 7.0 7.0 24 2
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 281 2 1 5 3.3 C[C@H]1CC[C@H](Nc2ncnc3c2nn2ccccc32)CC1 10.1016/j.bmcl.2016.03.026
CHEMBL3786063 139132 None 0 Rat Functional pIC50 = 7.0 7.0 24 2
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 281 2 1 5 3.3 C[C@H]1CC[C@H](Nc2ncnc3c2nn2ccccc32)CC1 10.1016/j.bmcl.2016.03.026
72163583 92065 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 369 2 0 3 3.3 O=C(N1C[C@@H]2CN(c3cccc(F)n3)C[C@@H]2C1)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.07.029
CHEMBL2418380 92065 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 369 2 0 3 3.3 O=C(N1C[C@@H]2CN(c3cccc(F)n3)C[C@@H]2C1)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.07.029
127030962 139132 None 0 Rat Functional pIC50 = 7.0 7.0 24 2
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 281 2 1 5 3.3 C[C@H]1CC[C@H](Nc2ncnc3c2nn2ccccc32)CC1 10.1016/j.bmcl.2016.03.026
CHEMBL3786063 139132 None 0 Rat Functional pIC50 = 7.0 7.0 24 2
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 281 2 1 5 3.3 C[C@H]1CC[C@H](Nc2ncnc3c2nn2ccccc32)CC1 10.1016/j.bmcl.2016.03.026
127033451 139254 None 0 Rat Functional pIC50 = 7.0 7.0 35 2
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 295 2 1 5 3.8 c1ccn2nc3c(NC4CCCCCCC4)ncnc3c2c1 10.1016/j.bmcl.2016.03.026
CHEMBL3787343 139254 None 0 Rat Functional pIC50 = 7.0 7.0 35 2
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 295 2 1 5 3.8 c1ccn2nc3c(NC4CCCCCCC4)ncnc3c2c1 10.1016/j.bmcl.2016.03.026
10809781 78552 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Inhibition of Quisqualate-Induced PI Hydrolysis Measured in CHO Metabotropic glutamate receptor 1 Expressing CellsInhibition of Quisqualate-Induced PI Hydrolysis Measured in CHO Metabotropic glutamate receptor 1 Expressing Cells
ChEMBL 380 5 2 6 1.9 COC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@]12C[C@@H]1/C(=N\O)c1ccccc1O2 10.1021/jm0009944
CHEMBL2111943 78552 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Inhibition of Quisqualate-Induced PI Hydrolysis Measured in CHO Metabotropic glutamate receptor 1 Expressing CellsInhibition of Quisqualate-Induced PI Hydrolysis Measured in CHO Metabotropic glutamate receptor 1 Expressing Cells
ChEMBL 380 5 2 6 1.9 COC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@]12C[C@@H]1/C(=N\O)c1ccccc1O2 10.1021/jm0009944
73336019 125158 None 0 Human Functional pIC50 = 5.0 5.0 -177 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 376 2 0 5 3.0 CCc1cn(C2=NCC(=O)N3CCc4c(cccc4C4CCCO4)C3=C2)cn1 nan
CHEMBL3644387 125158 None 0 Human Functional pIC50 = 5.0 5.0 -177 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 376 2 0 5 3.0 CCc1cn(C2=NCC(=O)N3CCc4c(cccc4C4CCCO4)C3=C2)cn1 nan
11777615 98915 None 0 Rat Functional pIC50 = 4.0 4.0 -2 2
Antagonistic activity against Metabotropic glutamate receptor 1 was determinedAntagonistic activity against Metabotropic glutamate receptor 1 was determined
ChEMBL 265 2 3 4 1.2 CC1(C)CC(N)(C(=O)O)c2ccc(C(=O)O)cc2O1 10.1016/S0960-894X(97)00177-7
CHEMBL278949 98915 None 0 Rat Functional pIC50 = 4.0 4.0 -2 2
Antagonistic activity against Metabotropic glutamate receptor 1 was determinedAntagonistic activity against Metabotropic glutamate receptor 1 was determined
ChEMBL 265 2 3 4 1.2 CC1(C)CC(N)(C(=O)O)c2ccc(C(=O)O)cc2O1 10.1016/S0960-894X(97)00177-7
127033451 139254 None 0 Rat Functional pIC50 = 7.0 7.0 35 2
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 295 2 1 5 3.8 c1ccn2nc3c(NC4CCCCCCC4)ncnc3c2c1 10.1016/j.bmcl.2016.03.026
CHEMBL3787343 139254 None 0 Rat Functional pIC50 = 7.0 7.0 35 2
Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay
ChEMBL 295 2 1 5 3.8 c1ccn2nc3c(NC4CCCCCCC4)ncnc3c2c1 10.1016/j.bmcl.2016.03.026
73335033 133091 None 0 Human Functional pIC50 = 6.0 6.0 -2 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 347 3 0 4 2.9 CCc1cc(C2=NCC(=O)N3CCc4c(OC)cccc4C3=C2)ccn1 nan
CHEMBL3702364 133091 None 0 Human Functional pIC50 = 6.0 6.0 -2 2
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).
ChEMBL 347 3 0 4 2.9 CCc1cc(C2=NCC(=O)N3CCc4c(OC)cccc4C3=C2)ccn1 nan
11703031 143652 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 349 3 0 5 4.2 CCc1ccc(-n2cnc3c(sc4cccc(N(C)C)c43)c2=O)cc1 10.1021/jm0504407
CHEMBL389918 143652 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 349 3 0 5 4.2 CCc1ccc(-n2cnc3c(sc4cccc(N(C)C)c43)c2=O)cc1 10.1021/jm0504407
122196112 124313 None 0 Human Functional pIC50 = 7.0 7.0 52 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 361 3 1 5 3.3 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)nc1 10.1016/j.bmcl.2015.10.013
CHEMBL3634434 124313 None 0 Human Functional pIC50 = 7.0 7.0 52 2
Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay
ChEMBL 361 3 1 5 3.3 Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)nc1 10.1016/j.bmcl.2015.10.013
67425323 87553 None 0 Human Functional pIC50 = 5.0 5.0 -478 2
Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay
ChEMBL 432 5 1 7 4.4 C[C@@H]1C[C@H]1C(=O)Nc1snc(-c2ccc3nn(C)cc3c2)c1-c1cccc(N(C)C)n1 10.1016/j.bmcl.2013.01.009
CHEMBL2334979 87553 None 0 Human Functional pIC50 = 5.0 5.0 -478 2
Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay
ChEMBL 432 5 1 7 4.4 C[C@@H]1C[C@H]1C(=O)Nc1snc(-c2ccc3nn(C)cc3c2)c1-c1cccc(N(C)C)n1 10.1016/j.bmcl.2013.01.009
54580945 62775 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 350 4 1 8 2.8 C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccncc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784060 62775 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human mGluR1Antagonist activity at human mGluR1
ChEMBL 350 4 1 8 2.8 C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccncc4)cnc3c12 10.1016/j.bmcl.2009.04.104
11056756 5478 None 0 Rat Functional pIC50 = 6.0 6.0 -7 2
Antagonist activity at rat mGluR1 expressed in BHK cells by calcium mobilization assayAntagonist activity at rat mGluR1 expressed in BHK cells by calcium mobilization assay
ChEMBL 333 2 1 3 4.8 Clc1ccc2ncnc(Nc3cccc(Br)c3)c2c1 10.1016/j.bmcl.2009.10.024
CHEMBL1075626 5478 None 0 Rat Functional pIC50 = 6.0 6.0 -7 2
Antagonist activity at rat mGluR1 expressed in BHK cells by calcium mobilization assayAntagonist activity at rat mGluR1 expressed in BHK cells by calcium mobilization assay
ChEMBL 333 2 1 3 4.8 Clc1ccc2ncnc(Nc3cccc(Br)c3)c2c1 10.1016/j.bmcl.2009.10.024
3346 2424 None 10 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor
ChEMBL 281 4 1 5 3.4 COc1ccc(cc1)Nc1ncnc2c1cc(OC)cc2 10.1021/jm060950g
9926999 2424 None 10 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor
ChEMBL 281 4 1 5 3.4 COc1ccc(cc1)Nc1ncnc2c1cc(OC)cc2 10.1021/jm060950g
CHEMBL254575 2424 None 10 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor
ChEMBL 281 4 1 5 3.4 COc1ccc(cc1)Nc1ncnc2c1cc(OC)cc2 10.1021/jm060950g
71680760 91072 None 14 Human Functional pIC50 = 7.0 7.0 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 364 2 0 4 3.2 C[C@@H]1CN(c2cccnc2C#N)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
CHEMBL2397347 91072 None 14 Human Functional pIC50 = 7.0 7.0 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 364 2 0 4 3.2 C[C@@H]1CN(c2cccnc2C#N)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
71682341 91075 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 339 2 0 3 3.3 C[C@H]1CN(C(=O)C23CC4CC(CC(C4)C2)C3)CCN1c1ccccn1 10.1016/j.bmcl.2013.05.020
CHEMBL2397350 91075 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 339 2 0 3 3.3 C[C@H]1CN(C(=O)C23CC4CC(CC(C4)C2)C3)CCN1c1ccccn1 10.1016/j.bmcl.2013.05.020
11681575 137264 None 0 Human Functional pIC50 = 7.0 7.0 1 3
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 336 3 1 6 3.6 CCc1ccc(-n2cnc3c(sc4nccc(NC)c43)c2=O)cc1 10.1021/jm0504407
CHEMBL374815 137264 None 0 Human Functional pIC50 = 7.0 7.0 1 3
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 336 3 1 6 3.6 CCc1ccc(-n2cnc3c(sc4nccc(NC)c43)c2=O)cc1 10.1021/jm0504407
2660431 200271 None 3 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 299 3 1 4 3.6 O=C(Nc1nc(-c2ccccn2)cs1)c1ccc(F)cc1 10.1016/j.bmcl.2009.07.097
CHEMBL572145 200271 None 3 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay
ChEMBL 299 3 1 4 3.6 O=C(Nc1nc(-c2ccccn2)cs1)c1ccc(F)cc1 10.1016/j.bmcl.2009.07.097
44442435 93790 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay
ChEMBL 338 2 0 7 2.3 Cc1nc2c(cnn2-c2cncnc2)c(=O)n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2007.05.028
CHEMBL247216 93790 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay
ChEMBL 338 2 0 7 2.3 Cc1nc2c(cnn2-c2cncnc2)c(=O)n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2007.05.028
71682341 91075 None 0 Human Functional pIC50 = 6 6.0 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 339 2 0 3 3.3 C[C@H]1CN(C(=O)C23CC4CC(CC(C4)C2)C3)CCN1c1ccccn1 10.1016/j.bmcl.2013.05.020
CHEMBL2397350 91075 None 0 Human Functional pIC50 = 6 6.0 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 339 2 0 3 3.3 C[C@H]1CN(C(=O)C23CC4CC(CC(C4)C2)C3)CCN1c1ccccn1 10.1016/j.bmcl.2013.05.020
11582178 138014 None 0 Human Functional pIC50 = 7 7.0 1 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 404 4 1 6 4.5 CCc1ccc(-n2cnc3c(sc4nccc(NCC(F)(F)F)c43)c2=O)cc1 10.1021/jm0504407
CHEMBL376372 138014 None 0 Human Functional pIC50 = 7 7.0 1 2
Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization
ChEMBL 404 4 1 6 4.5 CCc1ccc(-n2cnc3c(sc4nccc(NCC(F)(F)F)c43)c2=O)cc1 10.1021/jm0504407
71680760 91072 None 14 Human Functional pIC50 = 7 7.0 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 364 2 0 4 3.2 C[C@@H]1CN(c2cccnc2C#N)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.07.029
CHEMBL2397347 91072 None 14 Human Functional pIC50 = 7 7.0 - 1
Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins
ChEMBL 364 2 0 4 3.2 C[C@@H]1CN(c2cccnc2C#N)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.07.029
71680760 91072 None 14 Human Functional pIC50 = 7 7.0 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 364 2 0 4 3.2 C[C@@H]1CN(c2cccnc2C#N)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
CHEMBL2397347 91072 None 14 Human Functional pIC50 = 7 7.0 - 1
Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization
ChEMBL 364 2 0 4 3.2 C[C@@H]1CN(c2cccnc2C#N)CCN1C(=O)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2013.05.020
54585405 62684 None 0 Rat Functional pKi = 9.7 9.7 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 362 4 1 6 4.3 C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1783868 62684 None 0 Rat Functional pKi = 9.7 9.7 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 362 4 1 6 4.3 C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
54585406 62685 None 0 Rat Functional pKi = 9.4 9.4 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 378 5 1 7 4.0 C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1783869 62685 None 0 Rat Functional pKi = 9.4 9.4 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 378 5 1 7 4.0 C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
16118123 70997 None 0 Rat Functional pKi = 9.4 9.4 - 2
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 399 2 0 5 4.4 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951662 70997 None 0 Rat Functional pKi = 9.4 9.4 - 2
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 399 2 0 5 4.4 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
23634171 976 None 1 Rat Functional pKi = 9.2 9.2 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 366 3 1 6 3.7 C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)Cl 10.1016/j.bmcl.2009.04.104
6214 976 None 1 Rat Functional pKi = 9.2 9.2 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 366 3 1 6 3.7 C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)Cl 10.1016/j.bmcl.2009.04.104
CHEMBL1783874 976 None 1 Rat Functional pKi = 9.2 9.2 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 366 3 1 6 3.7 C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)Cl 10.1016/j.bmcl.2009.04.104
54580485 62677 None 0 Rat Functional pKi = 9.2 9.2 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 412 4 1 6 4.4 C=CCNc1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1783861 62677 None 0 Rat Functional pKi = 9.2 9.2 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 412 4 1 6 4.4 C=CCNc1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
23634249 62764 None 0 Rat Functional pKi = 9.2 9.2 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 410 3 1 6 3.8 C#CCNc1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784049 62764 None 0 Rat Functional pKi = 9.2 9.2 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 410 3 1 6 3.8 C#CCNc1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
23634326 62674 None 0 Rat Functional pKi = 9.0 9.0 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 364 5 1 7 3.6 C=CCNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1783858 62674 None 0 Rat Functional pKi = 9.0 9.0 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 364 5 1 7 3.6 C=CCNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
54586361 62676 None 0 Rat Functional pKi = 9.0 9.0 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 368 4 1 6 4.2 C=CCNc1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1783860 62676 None 0 Rat Functional pKi = 9.0 9.0 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 368 4 1 6 4.2 C=CCNc1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
54585404 62683 None 0 Rat Functional pKi = 8.9 8.9 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 382 4 1 6 4.6 C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1783867 62683 None 0 Rat Functional pKi = 8.9 8.9 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 382 4 1 6 4.6 C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
54583474 62686 None 0 Rat Functional pKi = 8.8 8.8 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 426 4 1 6 4.7 C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1783870 62686 None 0 Rat Functional pKi = 8.8 8.8 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 426 4 1 6 4.7 C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
23634169 62690 None 0 Rat Functional pKi = 8.8 8.8 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 346 3 1 6 3.3 C#CCNc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1783875 62690 None 0 Rat Functional pKi = 8.8 8.8 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 346 3 1 6 3.3 C#CCNc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
16118120 70994 None 0 Rat Functional pKi = 8.7 8.7 - 2
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 335 2 0 5 4.0 Cc1ccc(-n2ccc3c(sc4nccc(N(C)C)c43)c2=O)cc1 10.1016/j.bmcl.2011.12.131
CHEMBL1951659 70994 None 0 Rat Functional pKi = 8.7 8.7 - 2
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 335 2 0 5 4.0 Cc1ccc(-n2ccc3c(sc4nccc(N(C)C)c43)c2=O)cc1 10.1016/j.bmcl.2011.12.131
16118680 70996 None 0 Rat Functional pKi = 8.7 8.7 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 355 2 0 5 4.3 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951661 70996 None 0 Rat Functional pKi = 8.7 8.7 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 355 2 0 5 4.3 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
44592072 179162 None 0 Rat Functional pKi = 8 8.0 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 356 6 2 7 2.5 c1nc(NC2CCCCC2)c2cc(NCCN3CCOCC3)ncc2n1 10.1016/j.bmcl.2009.02.106
CHEMBL471435 179162 None 0 Rat Functional pKi = 8 8.0 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 356 6 2 7 2.5 c1nc(NC2CCCCC2)c2cc(NCCN3CCOCC3)ncc2n1 10.1016/j.bmcl.2009.02.106
54580945 62775 None 0 Rat Functional pKi = 6 6.0 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 350 4 1 8 2.8 C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccncc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784060 62775 None 0 Rat Functional pKi = 6 6.0 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 350 4 1 8 2.8 C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccncc4)cnc3c12 10.1016/j.bmcl.2009.04.104
1310 2315 None 61 Human Functional pKi = 5 5.0 -741 17
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm000007r
1369 2315 None 61 Human Functional pKi = 5 5.0 -741 17
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm000007r
33032 2315 None 61 Human Functional pKi = 5 5.0 -741 17
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm000007r
44272391 2315 None 61 Human Functional pKi = 5 5.0 -741 17
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm000007r
88747398 2315 None 61 Human Functional pKi = 5 5.0 -741 17
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm000007r
CHEMBL575060 2315 None 61 Human Functional pKi = 5 5.0 -741 17
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm000007r
DB00142 2315 None 61 Human Functional pKi = 5 5.0 -741 17
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm000007r
3246152 161386 None 27 Human Functional pKi = 5 5.0 - 0
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 161 4 3 3 -0.5 C[C@@H](C[C@H](N)C(=O)O)C(=O)O 10.1021/jm000007r
CHEMBL41221 161386 None 27 Human Functional pKi = 5 5.0 - 0
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 161 4 3 3 -0.5 C[C@@H](C[C@H](N)C(=O)O)C(=O)O 10.1021/jm000007r
44592033 179194 None 0 Rat Functional pKi = 7 7.0 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 302 6 1 6 2.8 COCCOc1cc2c(NC3CCCCC3)ncnc2cn1 10.1016/j.bmcl.2009.02.106
CHEMBL471666 179194 None 0 Rat Functional pKi = 7 7.0 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 302 6 1 6 2.8 COCCOc1cc2c(NC3CCCCC3)ncnc2cn1 10.1016/j.bmcl.2009.02.106
44592030 178945 None 0 Rat Functional pKi = 7.0 7.0 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 348 6 2 6 2.6 CN(C)CCNc1cc2c(NC3Cc4ccccc4C3)ncnc2cn1 10.1016/j.bmcl.2009.02.106
CHEMBL469381 178945 None 0 Rat Functional pKi = 7.0 7.0 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 348 6 2 6 2.6 CN(C)CCNc1cc2c(NC3Cc4ccccc4C3)ncnc2cn1 10.1016/j.bmcl.2009.02.106
54582946 62791 None 0 Rat Functional pKi = 7.0 7.0 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 390 3 1 9 3.0 C#CCNc1ncnc2sc3c(=O)n(-c4ccc5ncsc5c4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784076 62791 None 0 Rat Functional pKi = 7.0 7.0 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 390 3 1 9 3.0 C#CCNc1ncnc2sc3c(=O)n(-c4ccc5ncsc5c4)cnc3c12 10.1016/j.bmcl.2009.04.104
57403925 71017 None 0 Rat Functional pKi = 7.0 7.0 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 381 6 1 7 3.7 COCCNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951685 71017 None 0 Rat Functional pKi = 7.0 7.0 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 381 6 1 7 3.7 COCCNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
44438573 93760 None 0 Rat Functional pKi = 6.0 6.0 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 404 3 0 6 2.5 CN1CCN(c2nccn3cc(C(=O)N4CCCC(c5ccccc5)C4)nc23)CC1 10.1016/j.bmcl.2006.10.015
CHEMBL247092 93760 None 0 Rat Functional pKi = 6.0 6.0 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 404 3 0 6 2.5 CN1CCN(c2nccn3cc(C(=O)N4CCCC(c5ccccc5)C4)nc23)CC1 10.1016/j.bmcl.2006.10.015
44438588 93549 None 1 Rat Functional pKi = 8.0 8.0 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 338 5 1 4 3.2 CC(C)(CNC(=O)c1cncc(N2CCCCC2)n1)c1ccccc1 10.1016/j.bmcl.2006.10.015
CHEMBL246245 93549 None 1 Rat Functional pKi = 8.0 8.0 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 338 5 1 4 3.2 CC(C)(CNC(=O)c1cncc(N2CCCCC2)n1)c1ccccc1 10.1016/j.bmcl.2006.10.015
44592031 178946 None 0 Rat Functional pKi = 8.0 8.0 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 301 6 2 6 2.8 COCCNc1cc2c(NC3CCCCC3)ncnc2cn1 10.1016/j.bmcl.2009.02.106
CHEMBL469383 178946 None 0 Rat Functional pKi = 8.0 8.0 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 301 6 2 6 2.8 COCCNc1cc2c(NC3CCCCC3)ncnc2cn1 10.1016/j.bmcl.2009.02.106
16117979 71000 None 0 Rat Functional pKi = 8.0 8.0 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 327 2 0 5 4.2 CN(C)c1ccnc2sc3c(=O)n(C4CCCCC4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951665 71000 None 0 Rat Functional pKi = 8.0 8.0 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 327 2 0 5 4.2 CN(C)c1ccnc2sc3c(=O)n(C4CCCCC4)ccc3c12 10.1016/j.bmcl.2011.12.131
16118121 71003 None 0 Rat Functional pKi = 8.0 8.0 - 2
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 378 2 0 7 4.3 CN(C)c1ccnc2sc3c(=O)n(-c4ccc5scnc5c4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951668 71003 None 0 Rat Functional pKi = 8.0 8.0 - 2
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 378 2 0 7 4.3 CN(C)c1ccnc2sc3c(=O)n(-c4ccc5scnc5c4)ccc3c12 10.1016/j.bmcl.2011.12.131
1370 3263 None 42 Human Functional pKi = 6.0 6.0 -11 6
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm000007r
1372 3263 None 42 Human Functional pKi = 6.0 6.0 -11 6
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm000007r
40539 3263 None 42 Human Functional pKi = 6.0 6.0 -11 6
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm000007r
6971145 3263 None 42 Human Functional pKi = 6.0 6.0 -11 6
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm000007r
CHEMBL279956 3263 None 42 Human Functional pKi = 6.0 6.0 -11 6
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm000007r
DB02999 3263 None 42 Human Functional pKi = 6.0 6.0 -11 6
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm000007r
44591866 189587 None 0 Rat Functional pKi = 6.9 6.9 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 292 3 1 5 2.6 COc1cc2c(NC3Cc4ccccc4C3)ncnc2cn1 10.1016/j.bmcl.2009.02.106
CHEMBL513761 189587 None 0 Rat Functional pKi = 6.9 6.9 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 292 3 1 5 2.6 COc1cc2c(NC3Cc4ccccc4C3)ncnc2cn1 10.1016/j.bmcl.2009.02.106
16118946 71010 None 0 Rat Functional pKi = 6.9 6.9 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 348 3 0 5 4.5 COc1ccnc2sc3c(=O)n(-c4ccc(C5CC5)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951676 71010 None 0 Rat Functional pKi = 6.9 6.9 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 348 3 0 5 4.5 COc1ccnc2sc3c(=O)n(-c4ccc(C5CC5)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
16118124 71004 None 0 Rat Functional pKi = 7.9 7.9 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 378 2 0 7 4.3 CN(C)c1ccnc2sc3c(=O)n(-c4ccc5ncsc5c4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951669 71004 None 0 Rat Functional pKi = 7.9 7.9 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 378 2 0 7 4.3 CN(C)c1ccnc2sc3c(=O)n(-c4ccc5ncsc5c4)ccc3c12 10.1016/j.bmcl.2011.12.131
16118400 71054 None 0 Rat Functional pKi = 7.9 7.9 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 347 3 1 5 4.5 Cc1ccc(-n2ccc3c(sc4nccc(NC5CC5)c43)c2=O)cc1 10.1016/j.bmcl.2011.12.131
CHEMBL1951878 71054 None 0 Rat Functional pKi = 7.9 7.9 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 347 3 1 5 4.5 Cc1ccc(-n2ccc3c(sc4nccc(NC5CC5)c43)c2=O)cc1 10.1016/j.bmcl.2011.12.131
44438576 93904 None 0 Rat Functional pKi = 5.9 5.9 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 378 5 1 6 2.0 CC(CNC(=O)c1cn2ccnc(N3CCN(C)CC3)c2n1)c1ccccc1 10.1016/j.bmcl.2006.10.015
CHEMBL247862 93904 None 0 Rat Functional pKi = 5.9 5.9 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 378 5 1 6 2.0 CC(CNC(=O)c1cn2ccnc(N3CCN(C)CC3)c2n1)c1ccccc1 10.1016/j.bmcl.2006.10.015
44438586 153205 None 2 Rat Functional pKi = 5.9 5.9 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 291 5 1 3 3.7 CC(C)(CNCc1cnc2ccccc2n1)c1ccccc1 10.1016/j.bmcl.2006.10.015
CHEMBL397639 153205 None 2 Rat Functional pKi = 5.9 5.9 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 291 5 1 3 3.7 CC(C)(CNCc1cnc2ccccc2n1)c1ccccc1 10.1016/j.bmcl.2006.10.015
44438577 170385 None 1 Rat Functional pKi = 6.9 6.9 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 317 2 0 3 3.7 O=C(c1cnc2ccccc2n1)N1CCCC(c2ccccc2)C1 10.1016/j.bmcl.2006.10.015
CHEMBL444629 170385 None 1 Rat Functional pKi = 6.9 6.9 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 317 2 0 3 3.7 O=C(c1cnc2ccccc2n1)N1CCCC(c2ccccc2)C1 10.1016/j.bmcl.2006.10.015
44591992 189507 None 0 Rat Functional pKi = 6.9 6.9 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 321 5 3 6 2.0 OCCNc1ncnc2cnc(NC3Cc4ccccc4C3)cc12 10.1016/j.bmcl.2009.02.106
CHEMBL513032 189507 None 0 Rat Functional pKi = 6.9 6.9 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 321 5 3 6 2.0 OCCNc1ncnc2cnc(NC3Cc4ccccc4C3)cc12 10.1016/j.bmcl.2009.02.106
54582494 62687 None 0 Rat Functional pKi = 7.9 7.9 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 396 5 1 7 4.1 C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc(OC)c(F)c4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1783871 62687 None 0 Rat Functional pKi = 7.9 7.9 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 396 5 1 7 4.1 C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc(OC)c(F)c4)cnc3c12 10.1016/j.bmcl.2009.04.104
54587386 62688 None 0 Rat Functional pKi = 7.9 7.9 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 406 4 1 8 3.8 C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc5c(c4)OCCO5)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1783872 62688 None 0 Rat Functional pKi = 7.9 7.9 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 406 4 1 8 3.8 C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc5c(c4)OCCO5)cnc3c12 10.1016/j.bmcl.2009.04.104
16118682 71001 None 0 Rat Functional pKi = 7.9 7.9 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 369 3 0 6 3.8 COc1ccc(-n2ccc3c(sc4nccc(N(C)C)c43)c2=O)cc1F 10.1016/j.bmcl.2011.12.131
CHEMBL1951666 71001 None 0 Rat Functional pKi = 7.9 7.9 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 369 3 0 6 3.8 COc1ccc(-n2ccc3c(sc4nccc(N(C)C)c43)c2=O)cc1F 10.1016/j.bmcl.2011.12.131
16118540 71023 None 0 Rat Functional pKi = 7.9 7.9 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 341 2 1 5 4.3 CNc1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951690 71023 None 0 Rat Functional pKi = 7.9 7.9 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 341 2 1 5 4.3 CNc1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
16118816 71062 None 0 Rat Functional pKi = 7.9 7.9 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 364 4 1 7 3.6 COc1ccc(-n2ccc3c(sc4ncnc(NC5CC5)c43)c2=O)cc1 10.1016/j.bmcl.2011.12.131
CHEMBL1951886 71062 None 0 Rat Functional pKi = 7.9 7.9 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 364 4 1 7 3.6 COc1ccc(-n2ccc3c(sc4ncnc(NC5CC5)c43)c2=O)cc1 10.1016/j.bmcl.2011.12.131
16725048 1153 None 0 Rat Functional pKi = 7.9 7.9 - 2
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 371 3 0 8 2.6 COc1ccc(c(c1)F)n1cnc2c(c1=O)sc1c2c(ncn1)N(C)C 10.1016/j.bmcl.2012.09.048
6362 1153 None 0 Rat Functional pKi = 7.9 7.9 - 2
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 371 3 0 8 2.6 COc1ccc(c(c1)F)n1cnc2c(c1=O)sc1c2c(ncn1)N(C)C 10.1016/j.bmcl.2012.09.048
CHEMBL2205377 1153 None 0 Rat Functional pKi = 7.9 7.9 - 2
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 371 3 0 8 2.6 COc1ccc(c(c1)F)n1cnc2c(c1=O)sc1c2c(ncn1)N(C)C 10.1016/j.bmcl.2012.09.048
57403924 71016 None 0 Rat Functional pKi = 6.9 6.9 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 367 5 2 7 3.0 COc1ccc(-n2ccc3c(sc4nccc(NCCO)c43)c2=O)cc1 10.1016/j.bmcl.2011.12.131
CHEMBL1951684 71016 None 0 Rat Functional pKi = 6.9 6.9 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 367 5 2 7 3.0 COc1ccc(-n2ccc3c(sc4nccc(NCCO)c43)c2=O)cc1 10.1016/j.bmcl.2011.12.131
54584443 62678 None 0 Rat Functional pKi = 7.9 7.9 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 382 5 1 7 3.7 C=CCNc1ccnc2sc3c(=O)n(-c4ccc(F)c(OC)c4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1783862 62678 None 0 Rat Functional pKi = 7.9 7.9 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 382 5 1 7 3.7 C=CCNc1ccnc2sc3c(=O)n(-c4ccc(F)c(OC)c4)cnc3c12 10.1016/j.bmcl.2009.04.104
54586363 62689 None 0 Rat Functional pKi = 7.9 7.9 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 392 4 1 8 3.7 C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc5c(c4)OCO5)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1783873 62689 None 0 Rat Functional pKi = 7.9 7.9 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 392 4 1 8 3.7 C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc5c(c4)OCO5)cnc3c12 10.1016/j.bmcl.2009.04.104
44438598 147835 None 0 Rat Functional pKi = 7.9 7.9 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 337 7 1 5 2.5 CN(CCC#N)c1cnc(C(=O)NCC(C)(C)c2ccccc2)cn1 10.1016/j.bmcl.2006.10.015
CHEMBL393237 147835 None 0 Rat Functional pKi = 7.9 7.9 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 337 7 1 5 2.5 CN(CCC#N)c1cnc(C(=O)NCC(C)(C)c2ccccc2)cn1 10.1016/j.bmcl.2006.10.015
44591865 179316 None 0 Rat Functional pKi = 7.9 7.9 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 291 3 2 5 2.6 CNc1cc2c(NC3Cc4ccccc4C3)ncnc2cn1 10.1016/j.bmcl.2009.02.106
CHEMBL472490 179316 None 0 Rat Functional pKi = 7.9 7.9 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 291 3 2 5 2.6 CNc1cc2c(NC3Cc4ccccc4C3)ncnc2cn1 10.1016/j.bmcl.2009.02.106
16118256 71011 None 0 Rat Functional pKi = 7.9 7.9 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 314 2 0 5 4.1 COc1ccnc2sc3c(=O)n(C4CCCCC4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951677 71011 None 0 Rat Functional pKi = 7.9 7.9 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 314 2 0 5 4.1 COc1ccnc2sc3c(=O)n(C4CCCCC4)ccc3c12 10.1016/j.bmcl.2011.12.131
57559562 966 None 0 Rat Functional pKi = 7.8 7.8 - 2
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 365 4 1 8 3.0 COc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ncn1)NC1CC1 10.1016/j.bmcl.2012.09.048
6365 966 None 0 Rat Functional pKi = 7.8 7.8 - 2
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 365 4 1 8 3.0 COc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ncn1)NC1CC1 10.1016/j.bmcl.2012.09.048
CHEMBL2205915 966 None 0 Rat Functional pKi = 7.8 7.8 - 2
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 365 4 1 8 3.0 COc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ncn1)NC1CC1 10.1016/j.bmcl.2012.09.048
44592518 188186 None 0 Rat Functional pKi = 5.9 5.9 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 293 4 1 5 3.3 C[C@H](Nc1ncnc2cnc(N(C)C)cc12)c1ccccc1 10.1016/j.bmcl.2009.02.106
CHEMBL497919 188186 None 0 Rat Functional pKi = 5.9 5.9 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 293 4 1 5 3.3 C[C@H](Nc1ncnc2cnc(N(C)C)cc12)c1ccccc1 10.1016/j.bmcl.2009.02.106
44438580 93505 None 2 Rat Functional pKi = 7.8 7.8 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 321 5 1 4 2.9 COC(C)(CNC(=O)c1cnc2ccccc2n1)c1ccccc1 10.1016/j.bmcl.2006.10.015
CHEMBL246024 93505 None 2 Rat Functional pKi = 7.8 7.8 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 321 5 1 4 2.9 COC(C)(CNC(=O)c1cnc2ccccc2n1)c1ccccc1 10.1016/j.bmcl.2006.10.015
439282 141671 None 3 Human Functional pKi = 6.8 6.8 - 0
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 159 4 3 3 -0.6 C=C(C[C@H](N)C(=O)O)C(=O)O 10.1021/jm000007r
CHEMBL38499 141671 None 3 Human Functional pKi = 6.8 6.8 - 0
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 159 4 3 3 -0.6 C=C(C[C@H](N)C(=O)O)C(=O)O 10.1021/jm000007r
16118542 71020 None 0 Rat Functional pKi = 7.8 7.8 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 321 2 1 5 4.0 CNc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951688 71020 None 0 Rat Functional pKi = 7.8 7.8 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 321 2 1 5 4.0 CNc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
54583942 62763 None 0 Rat Functional pKi = 6.8 6.8 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 391 3 1 9 2.2 C#CCNc1ncnc2sc3c(=O)n(-c4ccc5c(c4)OCCO5)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784048 62763 None 0 Rat Functional pKi = 6.8 6.8 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 391 3 1 9 2.2 C#CCNc1ncnc2sc3c(=O)n(-c4ccc5c(c4)OCCO5)cnc3c12 10.1016/j.bmcl.2009.04.104
44591991 172094 None 0 Rat Functional pKi = 6.8 6.8 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 291 3 2 5 2.6 CNc1ncnc2cnc(NC3Cc4ccccc4C3)cc12 10.1016/j.bmcl.2009.02.106
CHEMBL447113 172094 None 0 Rat Functional pKi = 6.8 6.8 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 291 3 2 5 2.6 CNc1ncnc2cnc(NC3Cc4ccccc4C3)cc12 10.1016/j.bmcl.2009.02.106
44322921 209295 None 1 Human Functional pKi = 5.8 5.8 - 0
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 185 2 3 3 -0.5 N[C@@]1(C(=O)O)CC2CC1[C@H]2C(=O)O 10.1021/jm000007r
CHEMBL90501 209295 None 1 Human Functional pKi = 5.8 5.8 - 0
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 185 2 3 3 -0.5 N[C@@]1(C(=O)O)CC2CC1[C@H]2C(=O)O 10.1021/jm000007r
44591990 179028 None 0 Rat Functional pKi = 5.8 5.8 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 260 2 1 2 3.8 c1ccc2c(c1)CC(Nc1nccc3ccccc13)C2 10.1016/j.bmcl.2009.02.106
CHEMBL470205 179028 None 0 Rat Functional pKi = 5.8 5.8 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 260 2 1 2 3.8 c1ccc2c(c1)CC(Nc1nccc3ccccc13)C2 10.1016/j.bmcl.2009.02.106
44438589 169625 None 1 Rat Functional pKi = 7.8 7.8 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 338 5 1 4 3.2 CC(C)(CNC(=O)c1cnc(N2CCCCC2)cn1)c1ccccc1 10.1016/j.bmcl.2006.10.015
CHEMBL443489 169625 None 1 Rat Functional pKi = 7.8 7.8 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 338 5 1 4 3.2 CC(C)(CNC(=O)c1cnc(N2CCCCC2)cn1)c1ccccc1 10.1016/j.bmcl.2006.10.015
16118119 1149 None 0 Rat Functional pKi = 7.8 7.8 - 2
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 351 3 0 6 3.7 COc1ccc(cc1)n1ccc2c(c1=O)sc1c2c(ccn1)N(C)C 10.1016/j.bmcl.2011.12.131
6356 1149 None 0 Rat Functional pKi = 7.8 7.8 - 2
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 351 3 0 6 3.7 COc1ccc(cc1)n1ccc2c(c1=O)sc1c2c(ccn1)N(C)C 10.1016/j.bmcl.2011.12.131
CHEMBL1951658 1149 None 0 Rat Functional pKi = 7.8 7.8 - 2
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 351 3 0 6 3.7 COc1ccc(cc1)n1ccc2c(c1=O)sc1c2c(ccn1)N(C)C 10.1016/j.bmcl.2011.12.131
44592032 178947 None 0 Rat Functional pKi = 6.8 6.8 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 288 5 2 6 2.1 OCCOc1cc2c(NC3CCCCC3)ncnc2cn1 10.1016/j.bmcl.2009.02.106
CHEMBL469386 178947 None 0 Rat Functional pKi = 6.8 6.8 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 288 5 2 6 2.1 OCCOc1cc2c(NC3CCCCC3)ncnc2cn1 10.1016/j.bmcl.2009.02.106
44438585 93830 None 2 Rat Functional pKi = 6.8 6.8 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 331 5 1 3 3.9 CC(C)(CNC(=O)c1cnc(-c2ccccc2)cn1)c1ccccc1 10.1016/j.bmcl.2006.10.015
CHEMBL247476 93830 None 2 Rat Functional pKi = 6.8 6.8 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 331 5 1 3 3.9 CC(C)(CNC(=O)c1cnc(-c2ccccc2)cn1)c1ccccc1 10.1016/j.bmcl.2006.10.015
54586817 62766 None 0 Rat Functional pKi = 7.8 7.8 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 380 3 0 6 3.7 C#CCN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784051 62766 None 0 Rat Functional pKi = 7.8 7.8 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 380 3 0 6 3.7 C#CCN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
16118122 70999 None 0 Rat Functional pKi = 7.8 7.8 - 2
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 349 3 0 5 4.2 CCc1ccc(-n2ccc3c(sc4nccc(N(C)C)c43)c2=O)cc1 10.1016/j.bmcl.2011.12.131
CHEMBL1951664 70999 None 0 Rat Functional pKi = 7.8 7.8 - 2
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 349 3 0 5 4.2 CCc1ccc(-n2ccc3c(sc4nccc(N(C)C)c43)c2=O)cc1 10.1016/j.bmcl.2011.12.131
16117046 71013 None 0 Rat Functional pKi = 7.8 7.8 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 337 3 1 6 3.7 CNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951680 71013 None 0 Rat Functional pKi = 7.8 7.8 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 337 3 1 6 3.7 CNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
44592520 188040 None 0 Rat Functional pKi = 6.7 6.7 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 305 3 1 5 2.7 CN(C)c1cc2c(NC3Cc4ccccc4C3)ncnc2cn1 10.1016/j.bmcl.2009.02.106
CHEMBL496897 188040 None 0 Rat Functional pKi = 6.7 6.7 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 305 3 1 5 2.7 CN(C)c1cc2c(NC3Cc4ccccc4C3)ncnc2cn1 10.1016/j.bmcl.2009.02.106
16118813 71002 None 0 Rat Functional pKi = 7.7 7.7 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 369 3 0 6 3.8 COc1ccc(-n2ccc3c(sc4nccc(N(C)C)c43)c2=O)c(F)c1 10.1016/j.bmcl.2011.12.131
CHEMBL1951667 71002 None 0 Rat Functional pKi = 7.7 7.7 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 369 3 0 6 3.8 COc1ccc(-n2ccc3c(sc4nccc(N(C)C)c43)c2=O)c(F)c1 10.1016/j.bmcl.2011.12.131
16118815 71059 None 0 Rat Functional pKi = 7.7 7.7 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 352 3 0 7 3.1 COc1ccc(-n2ccc3c(sc4ncnc(N(C)C)c43)c2=O)cc1 10.1016/j.bmcl.2011.12.131
CHEMBL1951883 71059 None 0 Rat Functional pKi = 7.7 7.7 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 352 3 0 7 3.1 COc1ccc(-n2ccc3c(sc4ncnc(N(C)C)c43)c2=O)cc1 10.1016/j.bmcl.2011.12.131
44592517 188185 None 0 Rat Functional pKi = 6.7 6.7 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 271 3 1 5 2.8 CN(C)c1cc2c(NC3CCCCC3)ncnc2cn1 10.1016/j.bmcl.2009.02.106
CHEMBL497918 188185 None 0 Rat Functional pKi = 6.7 6.7 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 271 3 1 5 2.8 CN(C)c1cc2c(NC3CCCCC3)ncnc2cn1 10.1016/j.bmcl.2009.02.106
44438579 93504 None 2 Rat Functional pKi = 8.7 8.7 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 323 4 1 3 3.5 CC(C)(CNC(=O)c1cnc2ccccc2n1)c1ccc(F)cc1 10.1016/j.bmcl.2006.10.015
CHEMBL246023 93504 None 2 Rat Functional pKi = 8.7 8.7 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 323 4 1 3 3.5 CC(C)(CNC(=O)c1cnc2ccccc2n1)c1ccc(F)cc1 10.1016/j.bmcl.2006.10.015
44438587 93548 None 0 Rat Functional pKi = 8.7 8.7 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 309 4 1 3 3.1 CC(C)(CNC(=O)c1cnc2c(n1)CCCC2)c1ccccc1 10.1016/j.bmcl.2006.10.015
CHEMBL246244 93548 None 0 Rat Functional pKi = 8.7 8.7 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 309 4 1 3 3.1 CC(C)(CNC(=O)c1cnc2c(n1)CCCC2)c1ccccc1 10.1016/j.bmcl.2006.10.015
54579958 62769 None 0 Rat Functional pKi = 8.7 8.7 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 383 4 1 7 4.0 C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784054 62769 None 0 Rat Functional pKi = 8.7 8.7 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 383 4 1 7 4.0 C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
54584890 62780 None 0 Rat Functional pKi = 8.6 8.6 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 405 4 1 8 4.6 C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc5sccc5c4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784065 62780 None 0 Rat Functional pKi = 8.6 8.6 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 405 4 1 8 4.6 C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc5sccc5c4)cnc3c12 10.1016/j.bmcl.2009.04.104
54584442 62675 None 0 Rat Functional pKi = 8.6 8.6 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 348 4 1 6 3.9 C=CCNc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1783859 62675 None 0 Rat Functional pKi = 8.6 8.6 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 348 4 1 6 3.9 C=CCNc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
54582002 62770 None 0 Rat Functional pKi = 8.5 8.5 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 363 4 1 7 3.7 C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784055 62770 None 0 Rat Functional pKi = 8.5 8.5 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 363 4 1 7 3.7 C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
11451117 179220 None 0 Rat Functional pKi = 7.7 7.7 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 355 6 1 6 2.8 O=C1CCCN1CCOc1cc2c(NC3CCCCC3)ncnc2cn1 10.1016/j.bmcl.2009.02.106
CHEMBL471875 179220 None 0 Rat Functional pKi = 7.7 7.7 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 355 6 1 6 2.8 O=C1CCCN1CCOc1cc2c(NC3CCCCC3)ncnc2cn1 10.1016/j.bmcl.2009.02.106
44592071 179161 None 0 Rat Functional pKi = 6.7 6.7 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 300 6 3 6 2.5 NCCCNc1cc2c(NC3CCCCC3)ncnc2cn1 10.1016/j.bmcl.2009.02.106
CHEMBL471434 179161 None 0 Rat Functional pKi = 6.7 6.7 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 300 6 3 6 2.5 NCCCNc1cc2c(NC3CCCCC3)ncnc2cn1 10.1016/j.bmcl.2009.02.106
16118949 71007 None 0 Rat Functional pKi = 6.7 6.7 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 322 2 0 5 3.9 COc1ccnc2sc3c(=O)n(-c4ccccc4C)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951673 71007 None 0 Rat Functional pKi = 6.7 6.7 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 322 2 0 5 3.9 COc1ccnc2sc3c(=O)n(-c4ccccc4C)ccc3c12 10.1016/j.bmcl.2011.12.131
44591995 178962 None 0 Rat Functional pKi = 7.7 7.7 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 321 5 3 6 2.0 OCCNc1cc2c(NC3Cc4ccccc4C3)ncnc2cn1 10.1016/j.bmcl.2009.02.106
CHEMBL469588 178962 None 0 Rat Functional pKi = 7.7 7.7 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 321 5 3 6 2.0 OCCNc1cc2c(NC3Cc4ccccc4C3)ncnc2cn1 10.1016/j.bmcl.2009.02.106
22136331 92040 None 1 Rat Functional pKi = 7.7 7.7 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 291 4 1 3 3.2 CC(CNC(=O)c1cnc2ccccc2n1)c1ccccc1 10.1016/j.bmcl.2006.10.015
CHEMBL241699 92040 None 1 Rat Functional pKi = 7.7 7.7 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 291 4 1 3 3.2 CC(CNC(=O)c1cnc2ccccc2n1)c1ccccc1 10.1016/j.bmcl.2006.10.015
16118817 71066 None 0 Rat Functional pKi = 7.7 7.7 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 348 3 1 6 3.9 Cc1ccc(-n2ccc3c(sc4ncnc(NC5CC5)c43)c2=O)cc1 10.1016/j.bmcl.2011.12.131
CHEMBL1951890 71066 None 0 Rat Functional pKi = 7.7 7.7 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 348 3 1 6 3.9 Cc1ccc(-n2ccc3c(sc4ncnc(NC5CC5)c43)c2=O)cc1 10.1016/j.bmcl.2011.12.131
44592070 189129 None 0 Rat Functional pKi = 5.7 5.7 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 286 5 3 6 2.1 NCCNc1cc2c(NC3CCCCC3)ncnc2cn1 10.1016/j.bmcl.2009.02.106
CHEMBL509066 189129 None 0 Rat Functional pKi = 5.7 5.7 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 286 5 3 6 2.1 NCCNc1cc2c(NC3CCCCC3)ncnc2cn1 10.1016/j.bmcl.2009.02.106
16117042 71015 None 0 Rat Functional pKi = 7.6 7.6 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 365 5 1 6 4.4 CCCNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951682 71015 None 0 Rat Functional pKi = 7.6 7.6 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 365 5 1 6 4.4 CCCNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
54582003 62774 None 0 Rat Functional pKi = 7.6 7.6 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 349 4 1 7 3.4 C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccccc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784059 62774 None 0 Rat Functional pKi = 7.6 7.6 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 349 4 1 7 3.4 C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccccc4)cnc3c12 10.1016/j.bmcl.2009.04.104
54580948 62784 None 0 Rat Functional pKi = 7.6 7.6 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 363 4 1 8 2.4 C#CCNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784069 62784 None 0 Rat Functional pKi = 7.6 7.6 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 363 4 1 8 2.4 C#CCNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
3421 3544 None 30 Human Functional pKi = 4.6 4.6 1 3
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 185 3 3 3 -0.3 OC(=O)[C@H](C12CC(C1)(C2)C(=O)O)N 10.1021/jm000007r
5311040 3544 None 30 Human Functional pKi = 4.6 4.6 1 3
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 185 3 3 3 -0.3 OC(=O)[C@H](C12CC(C1)(C2)C(=O)O)N 10.1021/jm000007r
CHEMBL43412 3544 None 30 Human Functional pKi = 4.6 4.6 1 3
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 185 3 3 3 -0.3 OC(=O)[C@H](C12CC(C1)(C2)C(=O)O)N 10.1021/jm000007r
54584887 62767 None 0 Rat Functional pKi = 7.6 7.6 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 376 4 0 7 3.1 C#CCN(C)c1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784052 62767 None 0 Rat Functional pKi = 7.6 7.6 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 376 4 0 7 3.1 C#CCN(C)c1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
44438590 93612 None 0 Rat Functional pKi = 7.6 7.6 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 390 8 3 5 3.3 CC(C)(CNC(=O)c1cncc(N[C@@H](CO)c2ccccc2)n1)c1ccccc1 10.1016/j.bmcl.2006.10.015
CHEMBL246449 93612 None 0 Rat Functional pKi = 7.6 7.6 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 390 8 3 5 3.3 CC(C)(CNC(=O)c1cncc(N[C@@H](CO)c2ccccc2)n1)c1ccccc1 10.1016/j.bmcl.2006.10.015
44438599 93613 None 0 Rat Functional pKi = 7.6 7.6 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 369 8 1 5 2.6 CC(CN(C)C)N(C)c1cnc(C(=O)NCC(C)(C)c2ccccc2)cn1 10.1016/j.bmcl.2006.10.015
CHEMBL246455 93613 None 0 Rat Functional pKi = 7.6 7.6 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 369 8 1 5 2.6 CC(CN(C)C)N(C)c1cnc(C(=O)NCC(C)(C)c2ccccc2)cn1 10.1016/j.bmcl.2006.10.015
13231190 189503 None 14 Rat Functional pKi = 7.6 7.6 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 227 2 1 3 3.4 c1ccc2c(NC3CCCCC3)ncnc2c1 10.1016/j.bmcl.2009.02.106
CHEMBL513012 189503 None 14 Rat Functional pKi = 7.6 7.6 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 227 2 1 3 3.4 c1ccc2c(NC3CCCCC3)ncnc2c1 10.1016/j.bmcl.2009.02.106
16117168 71021 None 0 Rat Functional pKi = 6.6 6.6 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 325 2 1 5 3.8 CNc1ccnc2sc3c(=O)n(-c4ccc(F)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951689 71021 None 0 Rat Functional pKi = 6.6 6.6 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 325 2 1 5 3.8 CNc1ccnc2sc3c(=O)n(-c4ccc(F)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
54585850 62765 None 0 Rat Functional pKi = 7.6 7.6 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 380 4 1 7 3.2 C#CCNc1ccnc2sc3c(=O)n(-c4ccc(OC)c(F)c4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784050 62765 None 0 Rat Functional pKi = 7.6 7.6 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 380 4 1 7 3.2 C#CCNc1ccnc2sc3c(=O)n(-c4ccc(OC)c(F)c4)cnc3c12 10.1016/j.bmcl.2009.04.104
16118818 71063 None 0 Rat Functional pKi = 7.6 7.6 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 336 2 0 6 3.4 Cc1ccc(-n2ccc3c(sc4ncnc(N(C)C)c43)c2=O)cc1 10.1016/j.bmcl.2011.12.131
CHEMBL1951887 71063 None 0 Rat Functional pKi = 7.6 7.6 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 336 2 0 6 3.4 Cc1ccc(-n2ccc3c(sc4ncnc(N(C)C)c43)c2=O)cc1 10.1016/j.bmcl.2011.12.131
54585851 62785 None 0 Rat Functional pKi = 7.5 7.5 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 411 3 1 7 3.2 C#CCNc1ncnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784070 62785 None 0 Rat Functional pKi = 7.5 7.5 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 411 3 1 7 3.2 C#CCNc1ncnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
16118681 70995 None 0 Rat Functional pKi = 7.5 7.5 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 339 2 0 5 3.8 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(F)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951660 70995 None 0 Rat Functional pKi = 7.5 7.5 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 339 2 0 5 3.8 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(F)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
44438578 93464 None 2 Rat Functional pKi = 8.5 8.5 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 305 4 1 3 3.3 CC(C)(CNC(=O)c1cnc2ccccc2n1)c1ccccc1 10.1016/j.bmcl.2006.10.015
CHEMBL245819 93464 None 2 Rat Functional pKi = 8.5 8.5 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 305 4 1 3 3.3 CC(C)(CNC(=O)c1cnc2ccccc2n1)c1ccccc1 10.1016/j.bmcl.2006.10.015
44438596 93551 None 1 Rat Functional pKi = 8.5 8.5 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 302 3 1 4 2.8 C[C@H]1CC[C@H](NC(=O)c2cnc(N3CCCCC3)cn2)CC1 10.1016/j.bmcl.2006.10.015
CHEMBL246250 93551 None 1 Rat Functional pKi = 8.5 8.5 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 302 3 1 4 2.8 C[C@H]1CC[C@H](NC(=O)c2cnc(N3CCCCC3)cn2)CC1 10.1016/j.bmcl.2006.10.015
11772954 1034 None 0 Rat Functional pKi = 8.5 8.5 -1 2
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 365 8 3 7 2.0 OCCOCCNc1ncc2c(c1)c(ncn2)NC1Cc2c(C1)cccc2 10.1016/j.bmcl.2009.02.106
6349 1034 None 0 Rat Functional pKi = 8.5 8.5 -1 2
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 365 8 3 7 2.0 OCCOCCNc1ncc2c(c1)c(ncn2)NC1Cc2c(C1)cccc2 10.1016/j.bmcl.2009.02.106
CHEMBL469382 1034 None 0 Rat Functional pKi = 8.5 8.5 -1 2
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 365 8 3 7 2.0 OCCOCCNc1ncc2c(c1)c(ncn2)NC1Cc2c(C1)cccc2 10.1016/j.bmcl.2009.02.106
54586362 62682 None 0 Rat Functional pKi = 8.5 8.5 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 426 4 0 6 4.4 C=CCN(C)c1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1783866 62682 None 0 Rat Functional pKi = 8.5 8.5 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 426 4 0 6 4.4 C=CCN(C)c1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
16118686 71058 None 0 Rat Functional pKi = 8.5 8.5 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 411 3 1 5 4.9 O=c1c2sc3nccc(NC4CC4)c3c2ccn1-c1ccc(Br)cc1 10.1016/j.bmcl.2011.12.131
CHEMBL1951882 71058 None 0 Rat Functional pKi = 8.5 8.5 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 411 3 1 5 4.9 O=c1c2sc3nccc(NC4CC4)c3c2ccn1-c1ccc(Br)cc1 10.1016/j.bmcl.2011.12.131
23634102 977 None 2 Rat Functional pKi = 8.5 8.5 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 362 4 1 7 3.0 C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)OC 10.1016/j.bmcl.2009.04.104
6215 977 None 2 Rat Functional pKi = 8.5 8.5 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 362 4 1 7 3.0 C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)OC 10.1016/j.bmcl.2009.04.104
CHEMBL1783876 977 None 2 Rat Functional pKi = 8.5 8.5 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 362 4 1 7 3.0 C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)OC 10.1016/j.bmcl.2009.04.104
54584888 62772 None 0 Rat Functional pKi = 8.4 8.4 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 427 4 1 7 4.1 C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784057 62772 None 0 Rat Functional pKi = 8.4 8.4 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 427 4 1 7 4.1 C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
44438591 153206 None 2 Rat Functional pKi = 7.5 7.5 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 304 6 1 4 3.2 CCCCN(C)c1cncc(C(=O)NC2CCCCCC2)n1 10.1016/j.bmcl.2006.10.015
CHEMBL397640 153206 None 2 Rat Functional pKi = 7.5 7.5 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 304 6 1 4 3.2 CCCCN(C)c1cncc(C(=O)NC2CCCCCC2)n1 10.1016/j.bmcl.2006.10.015
44591863 189377 None 0 Rat Functional pKi = 6.5 6.5 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 319 3 0 5 2.7 CN(C)c1cc2c(N(C)C3Cc4ccccc4C3)ncnc2cn1 10.1016/j.bmcl.2009.02.106
CHEMBL511838 189377 None 0 Rat Functional pKi = 6.5 6.5 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 319 3 0 5 2.7 CN(C)c1cc2c(N(C)C3Cc4ccccc4C3)ncnc2cn1 10.1016/j.bmcl.2009.02.106
1426 2613 None 49 Human Functional pKi = 4.5 4.5 - 4
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 193 0 0 1 2.8 Cc1cccc(n1)C#Cc1ccccc1 10.1021/jm000007r
3025961 2613 None 49 Human Functional pKi = 4.5 4.5 - 4
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 193 0 0 1 2.8 Cc1cccc(n1)C#Cc1ccccc1 10.1021/jm000007r
CHEMBL66654 2613 None 49 Human Functional pKi = 4.5 4.5 - 4
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 193 0 0 1 2.8 Cc1cccc(n1)C#Cc1ccccc1 10.1021/jm000007r
1297 170355 None 23 Human Functional pKi = 4.5 4.5 1 2
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 211 3 4 4 0.2 NC(C(=O)O)c1ccc(C(=O)O)c(O)c1 10.1021/jm000007r
CHEMBL444589 170355 None 23 Human Functional pKi = 4.5 4.5 1 2
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 211 3 4 4 0.2 NC(C(=O)O)c1ccc(C(=O)O)c(O)c1 10.1021/jm000007r
57391670 71049 None 0 Rat Functional pKi = 6.5 6.5 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 332 2 1 6 3.5 CNc1ccnc2sc3c(=O)n(-c4ccc(C#N)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951873 71049 None 0 Rat Functional pKi = 6.5 6.5 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 332 2 1 6 3.5 CNc1ccnc2sc3c(=O)n(-c4ccc(C#N)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
44591994 189504 None 0 Rat Functional pKi = 7.5 7.5 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 393 4 2 5 4.2 c1ccc2c(c1)CC(Nc1cc3c(NC4Cc5ccccc5C4)ncnc3cn1)C2 10.1016/j.bmcl.2009.02.106
CHEMBL513018 189504 None 0 Rat Functional pKi = 7.5 7.5 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 393 4 2 5 4.2 c1ccc2c(c1)CC(Nc1cc3c(NC4Cc5ccccc5C4)ncnc3cn1)C2 10.1016/j.bmcl.2009.02.106
44438584 93829 None 2 Rat Functional pKi = 6.5 6.5 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 331 5 1 3 3.9 CC(C)(CNC(=O)c1cncc(-c2ccccc2)n1)c1ccccc1 10.1016/j.bmcl.2006.10.015
CHEMBL247475 93829 None 2 Rat Functional pKi = 6.5 6.5 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 331 5 1 3 3.9 CC(C)(CNC(=O)c1cncc(-c2ccccc2)n1)c1ccccc1 10.1016/j.bmcl.2006.10.015
54582005 62788 None 0 Rat Functional pKi = 7.5 7.5 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 381 4 1 8 2.6 C#CCNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4F)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784073 62788 None 0 Rat Functional pKi = 7.5 7.5 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 381 4 1 8 2.6 C#CCNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4F)cnc3c12 10.1016/j.bmcl.2009.04.104
16118945 71008 None 0 Rat Functional pKi = 7.5 7.5 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 352 3 0 6 3.9 COc1ccc(-n2ccc3c(sc4nccc(OC)c43)c2=O)c(C)c1 10.1016/j.bmcl.2011.12.131
CHEMBL1951674 71008 None 0 Rat Functional pKi = 7.5 7.5 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 352 3 0 6 3.9 COc1ccc(-n2ccc3c(sc4nccc(OC)c43)c2=O)c(C)c1 10.1016/j.bmcl.2011.12.131
16117303 71051 None 0 Rat Functional pKi = 7.5 7.5 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 355 3 1 6 3.8 CNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4F)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951875 71051 None 0 Rat Functional pKi = 7.5 7.5 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 355 3 1 6 3.8 CNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4F)ccc3c12 10.1016/j.bmcl.2011.12.131
16117432 71061 None 0 Rat Functional pKi = 7.5 7.5 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 352 4 1 7 3.4 CCNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951885 71061 None 0 Rat Functional pKi = 7.5 7.5 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 352 4 1 7 3.4 CCNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
44592069 189407 None 0 Rat Functional pKi = 7.5 7.5 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 302 6 2 6 2.5 OCCCOc1cc2c(NC3CCCCC3)ncnc2cn1 10.1016/j.bmcl.2009.02.106
CHEMBL512178 189407 None 0 Rat Functional pKi = 7.5 7.5 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 302 6 2 6 2.5 OCCCOc1cc2c(NC3CCCCC3)ncnc2cn1 10.1016/j.bmcl.2009.02.106
23186964 179135 None 0 Rat Functional pKi = 7.5 7.5 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 261 2 1 3 3.2 c1ccc2c(c1)CC(Nc1ncnc3ccccc13)C2 10.1016/j.bmcl.2009.02.106
CHEMBL471242 179135 None 0 Rat Functional pKi = 7.5 7.5 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 261 2 1 3 3.2 c1ccc2c(c1)CC(Nc1ncnc3ccccc13)C2 10.1016/j.bmcl.2009.02.106
44438600 93614 None 0 Rat Functional pKi = 7.5 7.5 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 368 6 2 5 2.4 CC(C)(CNC(=O)c1cnc(N2CCC(CO)CC2)cn1)c1ccccc1 10.1016/j.bmcl.2006.10.015
CHEMBL246456 93614 None 0 Rat Functional pKi = 7.5 7.5 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 368 6 2 5 2.4 CC(C)(CNC(=O)c1cnc(N2CCC(CO)CC2)cn1)c1ccccc1 10.1016/j.bmcl.2006.10.015
5311262 209584 None 12 Human Functional pKi = 6.5 6.5 - 0
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 383 5 3 4 3.6 N[C@](CC1c2ccccc2Sc2ccccc21)(C(=O)O)[C@H]1C[C@@H](C(=O)O)C1 10.1021/jm000007r
CHEMBL92162 209584 None 12 Human Functional pKi = 6.5 6.5 - 0
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 383 5 3 4 3.6 N[C@](CC1c2ccccc2Sc2ccccc21)(C(=O)O)[C@H]1C[C@@H](C(=O)O)C1 10.1021/jm000007r
1426 2613 None 49 Human Functional pKi = 7.4 7.4 - 4
Antagonist activity at human mGLUR1Antagonist activity at human mGLUR1
ChEMBL 193 0 0 1 2.8 Cc1cccc(n1)C#Cc1ccccc1 10.1016/j.bmcl.2010.06.075
3025961 2613 None 49 Human Functional pKi = 7.4 7.4 - 4
Antagonist activity at human mGLUR1Antagonist activity at human mGLUR1
ChEMBL 193 0 0 1 2.8 Cc1cccc(n1)C#Cc1ccccc1 10.1016/j.bmcl.2010.06.075
CHEMBL66654 2613 None 49 Human Functional pKi = 7.4 7.4 - 4
Antagonist activity at human mGLUR1Antagonist activity at human mGLUR1
ChEMBL 193 0 0 1 2.8 Cc1cccc(n1)C#Cc1ccccc1 10.1016/j.bmcl.2010.06.075
54582943 62776 None 0 Rat Functional pKi = 7.4 7.4 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 367 4 1 7 3.5 C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc(F)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784061 62776 None 0 Rat Functional pKi = 7.4 7.4 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 367 4 1 7 3.5 C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc(F)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
54582945 62787 None 0 Rat Functional pKi = 7.4 7.4 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 351 3 1 7 2.6 C#CCNc1ncnc2sc3c(=O)n(-c4ccc(F)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784072 62787 None 0 Rat Functional pKi = 7.4 7.4 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 351 3 1 7 2.6 C#CCNc1ncnc2sc3c(=O)n(-c4ccc(F)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
54581505 62681 None 0 Rat Functional pKi = 8.4 8.4 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 378 5 0 7 3.6 C=CCN(C)c1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1783865 62681 None 0 Rat Functional pKi = 8.4 8.4 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 378 5 0 7 3.6 C=CCN(C)c1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
54584891 62782 None 0 Rat Functional pKi = 8.4 8.4 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 367 3 1 7 3.1 C#CCNc1ncnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784067 62782 None 0 Rat Functional pKi = 8.4 8.4 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 367 3 1 7 3.1 C#CCNc1ncnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
44438582 93506 None 1 Rat Functional pKi = 7.4 7.4 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 306 4 1 4 2.7 CC(C)(CNC(=O)c1cnc2ccccc2n1)c1ccccn1 10.1016/j.bmcl.2006.10.015
CHEMBL246025 93506 None 1 Rat Functional pKi = 7.4 7.4 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 306 4 1 4 2.7 CC(C)(CNC(=O)c1cnc2ccccc2n1)c1ccccn1 10.1016/j.bmcl.2006.10.015
44438592 93832 None 0 Rat Functional pKi = 7.4 7.4 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 296 4 1 4 1.8 CCN(C)c1cncc(C(=O)NC2Cc3ccccc3C2)n1 10.1016/j.bmcl.2006.10.015
CHEMBL247485 93832 None 0 Rat Functional pKi = 7.4 7.4 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 296 4 1 4 1.8 CCN(C)c1cncc(C(=O)NC2Cc3ccccc3C2)n1 10.1016/j.bmcl.2006.10.015
9948445 148388 None 0 Rat Functional pKi = 7.4 7.4 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 305 4 1 3 3.4 CC(C)(Cc1ccccc1)NC(=O)c1cnc2ccccc2n1 10.1016/j.bmcl.2006.10.015
CHEMBL393681 148388 None 0 Rat Functional pKi = 7.4 7.4 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 305 4 1 3 3.4 CC(C)(Cc1ccccc1)NC(=O)c1cnc2ccccc2n1 10.1016/j.bmcl.2006.10.015
16117300 71050 None 0 Rat Functional pKi = 7.4 7.4 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 355 3 1 6 3.8 CNc1ccnc2sc3c(=O)n(-c4ccc(OC)c(F)c4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951874 71050 None 0 Rat Functional pKi = 7.4 7.4 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 355 3 1 6 3.8 CNc1ccnc2sc3c(=O)n(-c4ccc(OC)c(F)c4)ccc3c12 10.1016/j.bmcl.2011.12.131
44438572 93716 None 0 Rat Functional pKi = 6.4 6.4 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 420 3 0 8 1.2 CN1CCN(c2nccn3cc(C(=O)N4CCCN(c5ccccn5)CC4)nc23)CC1 10.1016/j.bmcl.2006.10.015
CHEMBL246890 93716 None 0 Rat Functional pKi = 6.4 6.4 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 420 3 0 8 1.2 CN1CCN(c2nccn3cc(C(=O)N4CCCN(c5ccccn5)CC4)nc23)CC1 10.1016/j.bmcl.2006.10.015
44592073 189448 None 0 Rat Functional pKi = 7.4 7.4 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 357 6 1 7 2.5 c1nc(NC2CCCCC2)c2cc(OCCN3CCOCC3)ncc2n1 10.1016/j.bmcl.2009.02.106
CHEMBL512523 189448 None 0 Rat Functional pKi = 7.4 7.4 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 357 6 1 7 2.5 c1nc(NC2CCCCC2)c2cc(OCCN3CCOCC3)ncc2n1 10.1016/j.bmcl.2009.02.106
16118943 71009 None 0 Rat Functional pKi = 7.4 7.4 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 336 3 0 5 4.2 CCc1ccc(-n2ccc3c(sc4nccc(OC)c43)c2=O)cc1 10.1016/j.bmcl.2011.12.131
CHEMBL1951675 71009 None 0 Rat Functional pKi = 7.4 7.4 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 336 3 0 5 4.2 CCc1ccc(-n2ccc3c(sc4nccc(OC)c43)c2=O)cc1 10.1016/j.bmcl.2011.12.131
104766 33 None 30 Human Functional pKi = 4.4 4.4 -4 14
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1021/jm000007r
1365 33 None 30 Human Functional pKi = 4.4 4.4 -4 14
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1021/jm000007r
CHEMBL34453 33 None 30 Human Functional pKi = 4.4 4.4 -4 14
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1021/jm000007r
54586818 62778 None 0 Rat Functional pKi = 7.4 7.4 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 406 4 1 9 4.0 C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc5scnc5c4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784063 62778 None 0 Rat Functional pKi = 7.4 7.4 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 406 4 1 9 4.0 C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc5scnc5c4)cnc3c12 10.1016/j.bmcl.2009.04.104
44438593 93833 None 0 Rat Functional pKi = 7.4 7.4 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 328 7 2 5 1.6 CN(CCO)c1cncc(C(=O)NCC(C)(C)c2ccccc2)n1 10.1016/j.bmcl.2006.10.015
CHEMBL247487 93833 None 0 Rat Functional pKi = 7.4 7.4 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 328 7 2 5 1.6 CN(CCO)c1cncc(C(=O)NCC(C)(C)c2ccccc2)n1 10.1016/j.bmcl.2006.10.015
12310764 1970 None 46 Human Functional pKi = 4.4 4.4 - 2
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 158 2 3 4 -0.9 OC(=O)C(c1o[nH]c(=O)c1)N 10.1021/jm000007r
1233 1970 None 46 Human Functional pKi = 4.4 4.4 - 2
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 158 2 3 4 -0.9 OC(=O)C(c1o[nH]c(=O)c1)N 10.1021/jm000007r
1371 1970 None 46 Human Functional pKi = 4.4 4.4 - 2
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 158 2 3 4 -0.9 OC(=O)C(c1o[nH]c(=O)c1)N 10.1021/jm000007r
CHEMBL284895 1970 None 46 Human Functional pKi = 4.4 4.4 - 2
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 158 2 3 4 -0.9 OC(=O)C(c1o[nH]c(=O)c1)N 10.1021/jm000007r
44438594 147552 None 0 Rat Functional pKi = 7.4 7.4 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 312 7 3 5 2.0 O=C(NCC1CC1)c1cncc(NCCc2cccc(O)c2)n1 10.1016/j.bmcl.2006.10.015
CHEMBL393029 147552 None 0 Rat Functional pKi = 7.4 7.4 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 312 7 3 5 2.0 O=C(NCC1CC1)c1cncc(NCCc2cccc(O)c2)n1 10.1016/j.bmcl.2006.10.015
54582944 62779 None 0 Rat Functional pKi = 7.3 7.3 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 406 4 1 9 4.0 C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc5ncsc5c4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784064 62779 None 0 Rat Functional pKi = 7.3 7.3 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 406 4 1 9 4.0 C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc5ncsc5c4)cnc3c12 10.1016/j.bmcl.2009.04.104
11404904 189300 None 0 Rat Functional pKi = 8.3 8.3 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 335 6 2 6 2.7 COCCNc1cc2c(NC3Cc4ccccc4C3)ncnc2cn1 10.1016/j.bmcl.2009.02.106
CHEMBL511266 189300 None 0 Rat Functional pKi = 8.3 8.3 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 335 6 2 6 2.7 COCCNc1cc2c(NC3Cc4ccccc4C3)ncnc2cn1 10.1016/j.bmcl.2009.02.106
16118537 978 None 0 Rat Functional pKi = 8.3 8.3 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 363 4 1 6 4.2 COc1ccc(cc1)n1ccc2c(c1=O)sc1c2c(ccn1)NC1CC1 10.1016/j.bmcl.2011.12.131
6357 978 None 0 Rat Functional pKi = 8.3 8.3 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 363 4 1 6 4.2 COc1ccc(cc1)n1ccc2c(c1=O)sc1c2c(ccn1)NC1CC1 10.1016/j.bmcl.2011.12.131
CHEMBL1951683 978 None 0 Rat Functional pKi = 8.3 8.3 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 363 4 1 6 4.2 COc1ccc(cc1)n1ccc2c(c1=O)sc1c2c(ccn1)NC1CC1 10.1016/j.bmcl.2011.12.131
23634254 62680 None 0 Rat Functional pKi = 8.3 8.3 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 382 4 0 6 4.3 C=CCN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1783864 62680 None 0 Rat Functional pKi = 8.3 8.3 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 382 4 0 6 4.3 C=CCN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
1368 2290 None 30 Human Functional pKi = 4.3 4.3 - 11
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 10.1021/jm000007r
5310956 2290 None 30 Human Functional pKi = 4.3 4.3 - 11
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 10.1021/jm000007r
CHEMBL280563 2290 None 30 Human Functional pKi = 4.3 4.3 - 11
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 10.1021/jm000007r
44438581 148176 None 2 Rat Functional pKi = 6.3 6.3 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 320 5 2 4 2.5 CNC(C)(CNC(=O)c1cnc2ccccc2n1)c1ccccc1 10.1016/j.bmcl.2006.10.015
CHEMBL393507 148176 None 2 Rat Functional pKi = 6.3 6.3 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 320 5 2 4 2.5 CNC(C)(CNC(=O)c1cnc2ccccc2n1)c1ccccc1 10.1016/j.bmcl.2006.10.015
16118942 71065 None 0 Rat Functional pKi = 7.3 7.3 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 336 3 1 6 3.7 CCNc1ncnc2sc3c(=O)n(-c4ccc(C)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951889 71065 None 0 Rat Functional pKi = 7.3 7.3 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 336 3 1 6 3.7 CCNc1ncnc2sc3c(=O)n(-c4ccc(C)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
44591864 179315 None 0 Rat Functional pKi = 7.3 7.3 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 305 3 1 5 2.7 CNc1cc2c(N(C)C3Cc4ccccc4C3)ncnc2cn1 10.1016/j.bmcl.2009.02.106
CHEMBL472489 179315 None 0 Rat Functional pKi = 7.3 7.3 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 305 3 1 5 2.7 CNc1cc2c(N(C)C3Cc4ccccc4C3)ncnc2cn1 10.1016/j.bmcl.2009.02.106
44438595 93550 None 0 Rat Functional pKi = 7.3 7.3 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 365 6 1 5 2.3 O=C(NCC1CC1)c1cncc(N2CCCN(Cc3ccccc3)CC2)n1 10.1016/j.bmcl.2006.10.015
CHEMBL246249 93550 None 0 Rat Functional pKi = 7.3 7.3 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 365 6 1 5 2.3 O=C(NCC1CC1)c1cncc(N2CCCN(Cc3ccccc3)CC2)n1 10.1016/j.bmcl.2006.10.015
16118812 70998 None 0 Rat Functional pKi = 7.3 7.3 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 346 2 0 6 3.5 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(C#N)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951663 70998 None 0 Rat Functional pKi = 7.3 7.3 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 346 2 0 6 3.5 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(C#N)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
57397023 71006 None 0 Rat Functional pKi = 6.3 6.3 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 338 3 0 6 3.6 COc1cccc(-n2ccc3c(sc4nccc(OC)c43)c2=O)c1 10.1016/j.bmcl.2011.12.131
CHEMBL1951671 71006 None 0 Rat Functional pKi = 6.3 6.3 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 338 3 0 6 3.6 COc1cccc(-n2ccc3c(sc4nccc(OC)c43)c2=O)c1 10.1016/j.bmcl.2011.12.131
9844204 209574 None 2 Human Functional pKi = 5.2 5.2 - 0
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 405 5 3 4 4.3 NC(CC1c2ccccc2Sc2ccccc21)(C(=O)O)c1ccc(C(=O)O)cc1 10.1021/jm000007r
CHEMBL92118 209574 None 2 Human Functional pKi = 5.2 5.2 - 0
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 405 5 3 4 4.3 NC(CC1c2ccccc2Sc2ccccc21)(C(=O)O)c1ccc(C(=O)O)cc1 10.1021/jm000007r
11337722 1070 None 0 Rat Functional pKi = 8.2 8.2 - 1
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 371 6 1 7 2.9 C1CCCC(CC1)Nc1ncnc2c1cc(OCCN1CCOCC1)nc2 10.1016/j.bmcl.2009.02.106
6351 1070 None 0 Rat Functional pKi = 8.2 8.2 - 1
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 371 6 1 7 2.9 C1CCCC(CC1)Nc1ncnc2c1cc(OCCN1CCOCC1)nc2 10.1016/j.bmcl.2009.02.106
CHEMBL470396 1070 None 0 Rat Functional pKi = 8.2 8.2 - 1
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 371 6 1 7 2.9 C1CCCC(CC1)Nc1ncnc2c1cc(OCCN1CCOCC1)nc2 10.1016/j.bmcl.2009.02.106
15953801 71048 None 0 Rat Functional pKi = 8.2 8.2 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 385 2 1 5 4.4 CNc1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951872 71048 None 0 Rat Functional pKi = 8.2 8.2 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 385 2 1 5 4.4 CNc1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
16118126 71005 None 0 Rat Functional pKi = 8.2 8.2 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 338 3 0 6 3.6 COc1ccc(-n2ccc3c(sc4nccc(OC)c43)c2=O)cc1 10.1016/j.bmcl.2011.12.131
CHEMBL1951670 71005 None 0 Rat Functional pKi = 8.2 8.2 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 338 3 0 6 3.6 COc1ccc(-n2ccc3c(sc4nccc(OC)c43)c2=O)cc1 10.1016/j.bmcl.2011.12.131
135413554 1627 None 46 Human Functional pKi = 8.2 8.2 - 2
Antagonist activity at human mGLUR1Antagonist activity at human mGLUR1
ChEMBL 266 1 2 3 1.3 O=C(NC1=NC(=O)CN1C)Nc1cccc(c1)Cl 10.1016/j.bmcl.2010.06.075
135497698 1627 None 46 Human Functional pKi = 8.2 8.2 - 2
Antagonist activity at human mGLUR1Antagonist activity at human mGLUR1
ChEMBL 266 1 2 3 1.3 O=C(NC1=NC(=O)CN1C)Nc1cccc(c1)Cl 10.1016/j.bmcl.2010.06.075
135659063 1627 None 46 Human Functional pKi = 8.2 8.2 - 2
Antagonist activity at human mGLUR1Antagonist activity at human mGLUR1
ChEMBL 266 1 2 3 1.3 O=C(NC1=NC(=O)CN1C)Nc1cccc(c1)Cl 10.1016/j.bmcl.2010.06.075
1433 1627 None 46 Human Functional pKi = 8.2 8.2 - 2
Antagonist activity at human mGLUR1Antagonist activity at human mGLUR1
ChEMBL 266 1 2 3 1.3 O=C(NC1=NC(=O)CN1C)Nc1cccc(c1)Cl 10.1016/j.bmcl.2010.06.075
1434 1627 None 46 Human Functional pKi = 8.2 8.2 - 2
Antagonist activity at human mGLUR1Antagonist activity at human mGLUR1
ChEMBL 266 1 2 3 1.3 O=C(NC1=NC(=O)CN1C)Nc1cccc(c1)Cl 10.1016/j.bmcl.2010.06.075
162834 1627 None 46 Human Functional pKi = 8.2 8.2 - 2
Antagonist activity at human mGLUR1Antagonist activity at human mGLUR1
ChEMBL 266 1 2 3 1.3 O=C(NC1=NC(=O)CN1C)Nc1cccc(c1)Cl 10.1016/j.bmcl.2010.06.075
CHEMBL239800 1627 None 46 Human Functional pKi = 8.2 8.2 - 2
Antagonist activity at human mGLUR1Antagonist activity at human mGLUR1
ChEMBL 266 1 2 3 1.3 O=C(NC1=NC(=O)CN1C)Nc1cccc(c1)Cl 10.1016/j.bmcl.2010.06.075
DB12931 1627 None 46 Human Functional pKi = 8.2 8.2 - 2
Antagonist activity at human mGLUR1Antagonist activity at human mGLUR1
ChEMBL 266 1 2 3 1.3 O=C(NC1=NC(=O)CN1C)Nc1cccc(c1)Cl 10.1016/j.bmcl.2010.06.075
9815955 106041 None 0 Human Functional pKi = 5.2 5.2 - 1
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 225 3 4 4 0.5 Cc1c(C(N)C(=O)O)ccc(C(=O)O)c1O 10.1021/jm000007r
CHEMBL313124 106041 None 0 Human Functional pKi = 5.2 5.2 - 1
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 225 3 4 4 0.5 Cc1c(C(N)C(=O)O)ccc(C(=O)O)c1O 10.1021/jm000007r
44591993 189223 None 0 Rat Functional pKi = 5.2 5.2 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 249 6 4 7 -0.2 OCCNc1cc2c(NCCO)ncnc2cn1 10.1016/j.bmcl.2009.02.106
CHEMBL510310 189223 None 0 Rat Functional pKi = 5.2 5.2 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 249 6 4 7 -0.2 OCCNc1cc2c(NCCO)ncnc2cn1 10.1016/j.bmcl.2009.02.106
44591867 172745 None 1 Rat Functional pKi = 5.2 5.2 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 226 2 1 2 4.0 c1ccc2c(NC3CCCCC3)ccnc2c1 10.1016/j.bmcl.2009.02.106
CHEMBL449616 172745 None 1 Rat Functional pKi = 5.2 5.2 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 226 2 1 2 4.0 c1ccc2c(NC3CCCCC3)ccnc2c1 10.1016/j.bmcl.2009.02.106
54580946 62777 None 0 Rat Functional pKi = 7.2 7.2 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 383 4 1 7 4.0 C=C(C)CNc1ncnc2sc3c(=O)n(-c4cccc(Cl)c4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784062 62777 None 0 Rat Functional pKi = 7.2 7.2 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 383 4 1 7 4.0 C=C(C)CNc1ncnc2sc3c(=O)n(-c4cccc(Cl)c4)cnc3c12 10.1016/j.bmcl.2009.04.104
54583943 62792 None 0 Rat Functional pKi = 7.2 7.2 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 373 3 1 8 3.2 C#CCNc1ncnc2sc3c(=O)n(-c4ccc5occc5c4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784077 62792 None 0 Rat Functional pKi = 7.2 7.2 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 373 3 1 8 3.2 C#CCNc1ncnc2sc3c(=O)n(-c4ccc5occc5c4)cnc3c12 10.1016/j.bmcl.2009.04.104
16118539 71019 None 0 Rat Functional pKi = 7.2 7.2 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 381 5 1 7 3.0 COc1ccc(-n2ccc3c(sc4nccc(N(C)CCO)c43)c2=O)cc1 10.1016/j.bmcl.2011.12.131
CHEMBL1951687 71019 None 0 Rat Functional pKi = 7.2 7.2 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 381 5 1 7 3.0 COc1ccc(-n2ccc3c(sc4nccc(N(C)CCO)c43)c2=O)cc1 10.1016/j.bmcl.2011.12.131
54580947 62781 None 0 Rat Functional pKi = 7.2 7.2 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 407 4 1 9 3.2 C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc5c(c4)OCCO5)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784066 62781 None 0 Rat Functional pKi = 7.2 7.2 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 407 4 1 9 3.2 C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc5c(c4)OCCO5)cnc3c12 10.1016/j.bmcl.2009.04.104
54584892 62790 None 0 Rat Functional pKi = 7.2 7.2 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 390 3 1 9 3.0 C#CCNc1ncnc2sc3c(=O)n(-c4ccc5scnc5c4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784075 62790 None 0 Rat Functional pKi = 7.2 7.2 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 390 3 1 9 3.0 C#CCNc1ncnc2sc3c(=O)n(-c4ccc5scnc5c4)cnc3c12 10.1016/j.bmcl.2009.04.104
44438575 146126 None 0 Rat Functional pKi = 6.2 6.2 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 434 3 0 8 1.5 Cc1cccc(N2CCCN(C(=O)c3cn4ccnc(N5CCN(C)CC5)c4n3)CC2)n1 10.1016/j.bmcl.2006.10.015
CHEMBL391879 146126 None 0 Rat Functional pKi = 6.2 6.2 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 434 3 0 8 1.5 Cc1cccc(N2CCCN(C(=O)c3cn4ccnc(N5CCN(C)CC5)c4n3)CC2)n1 10.1016/j.bmcl.2006.10.015
36039661 93507 None 2 Rat Functional pKi = 5.2 5.2 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 255 4 1 3 2.2 CC(C)(CNC(=O)c1cnccn1)c1ccccc1 10.1016/j.bmcl.2006.10.015
CHEMBL246026 93507 None 2 Rat Functional pKi = 5.2 5.2 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 255 4 1 3 2.2 CC(C)(CNC(=O)c1cnccn1)c1ccccc1 10.1016/j.bmcl.2006.10.015
443586 146540 None 39 Human Functional pKi = 5.2 5.2 -16 3
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 183 2 4 4 0.2 N[C@H](C(=O)O)c1cc(O)cc(O)c1 10.1021/jm000007r
71668376 146540 None 39 Human Functional pKi = 5.2 5.2 -16 3
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 183 2 4 4 0.2 N[C@H](C(=O)O)c1cc(O)cc(O)c1 10.1021/jm000007r
CHEMBL39221 146540 None 39 Human Functional pKi = 5.2 5.2 -16 3
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 183 2 4 4 0.2 N[C@H](C(=O)O)c1cc(O)cc(O)c1 10.1021/jm000007r
54584889 62773 None 0 Rat Functional pKi = 7.2 7.2 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 397 5 1 8 3.5 C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc(OC)c(F)c4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784058 62773 None 0 Rat Functional pKi = 7.2 7.2 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 397 5 1 8 3.5 C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc(OC)c(F)c4)cnc3c12 10.1016/j.bmcl.2009.04.104
1378 2417 None 39 Human Functional pKi = 5.2 5.2 -1047 14
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/jm000007r
1399 2417 None 39 Human Functional pKi = 5.2 5.2 -1047 14
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/jm000007r
9819927 2417 None 39 Human Functional pKi = 5.2 5.2 -1047 14
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/jm000007r
CHEMBL432038 2417 None 39 Human Functional pKi = 5.2 5.2 -1047 14
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/jm000007r
54579959 62793 None 0 Rat Functional pKi = 7.2 7.2 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 389 3 1 8 3.7 C#CCNc1ncnc2sc3c(=O)n(-c4ccc5sccc5c4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784078 62793 None 0 Rat Functional pKi = 7.2 7.2 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 389 3 1 8 3.7 C#CCNc1ncnc2sc3c(=O)n(-c4ccc5sccc5c4)cnc3c12 10.1016/j.bmcl.2009.04.104
5300647 93465 None 8 Rat Functional pKi = 7.2 7.2 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 277 4 1 3 2.6 O=C(NCCc1ccccc1)c1cnc2ccccc2n1 10.1016/j.bmcl.2006.10.015
CHEMBL245820 93465 None 8 Rat Functional pKi = 7.2 7.2 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 277 4 1 3 2.6 O=C(NCCc1ccccc1)c1cnc2ccccc2n1 10.1016/j.bmcl.2006.10.015
44591868 179218 None 0 Rat Functional pKi = 6.2 6.2 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 228 2 0 3 3.3 c1ccc2c(OC3CCCCC3)ncnc2c1 10.1016/j.bmcl.2009.02.106
CHEMBL471866 179218 None 0 Rat Functional pKi = 6.2 6.2 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge
ChEMBL 228 2 0 3 3.3 c1ccc2c(OC3CCCCC3)ncnc2c1 10.1016/j.bmcl.2009.02.106
16118397 71056 None 0 Rat Functional pKi = 8.1 8.1 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 367 3 1 5 4.8 O=c1c2sc3nccc(NC4CC4)c3c2ccn1-c1ccc(Cl)cc1 10.1016/j.bmcl.2011.12.131
CHEMBL1951880 71056 None 0 Rat Functional pKi = 8.1 8.1 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 367 3 1 5 4.8 O=c1c2sc3nccc(NC4CC4)c3c2ccn1-c1ccc(Cl)cc1 10.1016/j.bmcl.2011.12.131
16118685 71057 None 0 Rat Functional pKi = 8.1 8.1 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 399 3 1 5 4.8 CCNc1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951881 71057 None 0 Rat Functional pKi = 8.1 8.1 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 399 3 1 5 4.8 CCNc1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
54582942 62771 None 0 Rat Functional pKi = 8.1 8.1 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 379 5 1 8 3.4 C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784056 62771 None 0 Rat Functional pKi = 8.1 8.1 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 379 5 1 8 3.4 C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
54585403 62679 None 0 Rat Functional pKi = 8.1 8.1 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 352 4 1 6 3.7 C=CCNc1ccnc2sc3c(=O)n(-c4ccc(F)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1783863 62679 None 0 Rat Functional pKi = 8.1 8.1 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 352 4 1 6 3.7 C=CCNc1ccnc2sc3c(=O)n(-c4ccc(F)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
1208332 167151 None 13 Rat Functional pKi = 8.1 8.1 - 2
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 352 3 0 7 3.1 COc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1 10.1016/j.bmcl.2009.04.104
CHEMBL428909 167151 None 13 Rat Functional pKi = 8.1 8.1 - 2
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 352 3 0 7 3.1 COc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1 10.1016/j.bmcl.2009.04.104
16117172 71052 None 0 Rat Functional pKi = 7.2 7.2 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 364 2 1 7 4.3 CNc1ccnc2sc3c(=O)n(-c4ccc5scnc5c4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951876 71052 None 0 Rat Functional pKi = 7.2 7.2 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 364 2 1 7 4.3 CNc1ccnc2sc3c(=O)n(-c4ccc5scnc5c4)ccc3c12 10.1016/j.bmcl.2011.12.131
54585852 62786 None 0 Rat Functional pKi = 7.1 7.1 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 381 4 1 8 2.6 C#CCNc1ncnc2sc3c(=O)n(-c4ccc(OC)c(F)c4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784071 62786 None 0 Rat Functional pKi = 7.1 7.1 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 381 4 1 8 2.6 C#CCNc1ncnc2sc3c(=O)n(-c4ccc(OC)c(F)c4)cnc3c12 10.1016/j.bmcl.2009.04.104
16117433 71060 None 0 Rat Functional pKi = 7.1 7.1 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 338 3 1 7 3.0 CNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951884 71060 None 0 Rat Functional pKi = 7.1 7.1 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 338 3 1 7 3.0 CNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
57402169 71012 None 0 Rat Functional pKi = 6.1 6.1 - 0
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 260 2 0 5 2.6 CCn1ccc2c(sc3nccc(OC)c32)c1=O 10.1016/j.bmcl.2011.12.131
CHEMBL1951678 71012 None 0 Rat Functional pKi = 6.1 6.1 - 0
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 260 2 0 5 2.6 CCn1ccc2c(sc3nccc(OC)c32)c1=O 10.1016/j.bmcl.2011.12.131
23634325 62768 None 0 Rat Functional pKi = 8.1 8.1 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 424 3 0 6 3.8 C#CCN(C)c1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784053 62768 None 0 Rat Functional pKi = 8.1 8.1 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 424 3 0 6 3.8 C#CCN(C)c1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
44438597 93552 None 1 Rat Functional pKi = 8.1 8.1 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 302 3 1 4 2.9 O=C(NC1CCCCCC1)c1cnc(N2CCCCC2)cn1 10.1016/j.bmcl.2006.10.015
CHEMBL246251 93552 None 1 Rat Functional pKi = 8.1 8.1 - 0
Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay
ChEMBL 302 3 1 4 2.9 O=C(NC1CCCCCC1)c1cnc(N2CCCCC2)cn1 10.1016/j.bmcl.2006.10.015
54582004 62783 None 0 Rat Functional pKi = 8.1 8.1 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 347 3 1 7 2.7 C#CCNc1ncnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784068 62783 None 0 Rat Functional pKi = 8.1 8.1 - 1
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 347 3 1 7 2.7 C#CCNc1ncnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12 10.1016/j.bmcl.2009.04.104
16118536 71014 None 0 Rat Functional pKi = 8.1 8.1 - 1
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1
ChEMBL 351 4 1 6 4.0 CCNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)ccc3c12 10.1016/j.bmcl.2011.12.131
CHEMBL1951681 71014 None 0 Rat Functional pKi = 8.1 8.1 - 1