Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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name		 GPCRdb
ID		 #Vendors

 Reference
ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 AssayType

 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
1392 73 48 None -323 4 Rat 4.0 pEC50 = 4 Functional
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 48 None -323 4 Rat 4.0 pEC50 = 4 Functional
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 48 None -323 4 Rat 4.0 pEC50 = 4 Functional
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 192829 0 None - 1 Rat 7.0 pEC50 = 7.0 Functional
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 192829 0 None - 1 Rat 7.0 pEC50 = 7.0 Functional
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 110 None -741 17 Human 6.0 pEC50 = 6.0 Functional
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 110 None -741 17 Human 6.0 pEC50 = 6.0 Functional
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 110 None -741 17 Human 6.0 pEC50 = 6.0 Functional
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 110 None -741 17 Human 6.0 pEC50 = 6.0 Functional
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 110 None -741 17 Human 6.0 pEC50 = 6.0 Functional
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 110 None -741 17 Human 6.0 pEC50 = 6.0 Functional
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 110 None -741 17 Human 6.0 pEC50 = 6.0 Functional
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 124240 0 None 22 2 Human 7.0 pEC50 = 7.0 Functional
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 124240 0 None 22 2 Human 7.0 pEC50 = 7.0 Functional
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 139024 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 139024 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 139024 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 139024 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 137695 2 None - 1 Human 7.9 pEC50 = 7.9 Functional
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 137695 2 None - 1 Human 7.9 pEC50 = 7.9 Functional
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 71889 38 None 4 2 Rat 5.0 pEC50 = 5.0 Functional
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 71889 38 None 4 2 Rat 5.0 pEC50 = 5.0 Functional
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 71889 38 None 4 2 Rat 5.0 pEC50 = 5.0 Functional
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 123931 0 None -1 3 Rat 7.0 pEC50 = 7.0 Functional
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 123931 0 None -1 3 Rat 7.0 pEC50 = 7.0 Functional
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 123934 0 None -1 2 Rat 7.0 pEC50 = 7.0 Functional
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 123934 0 None -1 2 Rat 7.0 pEC50 = 7.0 Functional
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 123931 0 None -1 3 Rat 7.0 pEC50 = 7.0 Functional
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 123931 0 None -1 3 Rat 7.0 pEC50 = 7.0 Functional
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 123934 0 None -1 2 Rat 7.0 pEC50 = 7.0 Functional
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 123934 0 None -1 2 Rat 7.0 pEC50 = 7.0 Functional
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 139039 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 139039 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 137695 2 None - 1 Human 4.9 pEC50 = 4.9 Functional
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 137695 2 None - 1 Human 4.9 pEC50 = 4.9 Functional
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 139039 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 139039 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 124257 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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 124257 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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 124238 0 None 53 2 Human 6.9 pEC50 = 6.9 Functional
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 124238 0 None 53 2 Human 6.9 pEC50 = 6.9 Functional
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 137792 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 137792 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 187637 0 None - 1 Rat 6.9 pEC50 = 6.9 Functional
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 187637 0 None - 1 Rat 6.9 pEC50 = 6.9 Functional
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 137792 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 137792 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 139090 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 139090 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 139090 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 139090 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 138954 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 138954 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 138954 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 138954 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 137829 0 None -1 2 Human 5.9 pEC50 = 5.9 Functional
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 137829 0 None -1 2 Human 5.9 pEC50 = 5.9 Functional
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 138969 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 138969 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 124257 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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 124257 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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 187636 0 None - 1 Rat 6.9 pEC50 = 6.9 Functional
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 187636 0 None - 1 Rat 6.9 pEC50 = 6.9 Functional
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 137829 0 None -1 2 Human 5.9 pEC50 = 5.9 Functional
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 137829 0 None -1 2 Human 5.9 pEC50 = 5.9 Functional
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 138969 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 138969 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 139042 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 139042 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 181755 0 None -1 3 Human 6.9 pEC50 = 6.9 Functional
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 181755 0 None -1 3 Human 6.9 pEC50 = 6.9 Functional
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 138983 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 138983 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 137697 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 137697 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 137697 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 137697 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 110 None -794 17 Rat 4.9 pEC50 = 4.9 Functional
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 110 None -794 17 Rat 4.9 pEC50 = 4.9 Functional
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 110 None -794 17 Rat 4.9 pEC50 = 4.9 Functional
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 110 None -794 17 Rat 4.9 pEC50 = 4.9 Functional
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 110 None -794 17 Rat 4.9 pEC50 = 4.9 Functional
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 110 None -794 17 Rat 4.9 pEC50 = 4.9 Functional
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 110 None -794 17 Rat 4.9 pEC50 = 4.9 Functional
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 187637 0 None - 1 Rat 6.9 pEC50 = 6.9 Functional
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 187637 0 None - 1 Rat 6.9 pEC50 = 6.9 Functional
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 140092 10 None 2 2 Human 5.9 pEC50 = 5.9 Functional
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 140092 10 None 2 2 Human 5.9 pEC50 = 5.9 Functional
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 137769 0 None 4 2 Human 6.9 pEC50 = 6.9 Functional
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 137769 0 None 4 2 Human 6.9 pEC50 = 6.9 Functional
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 137769 0 None 4 2 Human 6.9 pEC50 = 6.9 Functional
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 137769 0 None 4 2 Human 6.9 pEC50 = 6.9 Functional
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 140092 10 None 2 2 Human 5.9 pEC50 = 5.9 Functional
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 140092 10 None 2 2 Human 5.9 pEC50 = 5.9 Functional
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 124244 0 None 13 2 Human 6.8 pEC50 = 6.8 Functional
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 124244 0 None 13 2 Human 6.8 pEC50 = 6.8 Functional
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 138983 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 138983 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 137762 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 137762 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 137762 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 137762 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 124259 0 None 40 2 Human 7.8 pEC50 = 7.8 Functional
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 124259 0 None 40 2 Human 7.8 pEC50 = 7.8 Functional
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 42 None -8 14 Rat 4.8 pEC50 = 4.8 Functional
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 42 None -8 14 Rat 4.8 pEC50 = 4.8 Functional
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 42 None -8 14 Rat 4.8 pEC50 = 4.8 Functional
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 137765 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 137765 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 137765 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 137765 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 139083 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 139083 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 124241 0 None 18 2 Human 6.8 pEC50 = 6.8 Functional
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 124241 0 None 18 2 Human 6.8 pEC50 = 6.8 Functional
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 139083 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 139083 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 110 None -794 17 Rat 5.8 pEC50 = 5.8 Functional
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 110 None -794 17 Rat 5.8 pEC50 = 5.8 Functional
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 110 None -794 17 Rat 5.8 pEC50 = 5.8 Functional
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 110 None -794 17 Rat 5.8 pEC50 = 5.8 Functional
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 110 None -794 17 Rat 5.8 pEC50 = 5.8 Functional
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 110 None -794 17 Rat 5.8 pEC50 = 5.8 Functional
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 110 None -794 17 Rat 5.8 pEC50 = 5.8 Functional
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 124227 0 None 21 2 Human 7.8 pEC50 = 7.8 Functional
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 124227 0 None 21 2 Human 7.8 pEC50 = 7.8 Functional
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 124254 0 None 26 2 Human 7.8 pEC50 = 7.8 Functional
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 124254 0 None 26 2 Human 7.8 pEC50 = 7.8 Functional
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 110 None -794 17 Rat 5.8 pEC50 = 5.8 Functional
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 110 None -794 17 Rat 5.8 pEC50 = 5.8 Functional
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 110 None -794 17 Rat 5.8 pEC50 = 5.8 Functional
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 110 None -794 17 Rat 5.8 pEC50 = 5.8 Functional
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 110 None -794 17 Rat 5.8 pEC50 = 5.8 Functional
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 110 None -794 17 Rat 5.8 pEC50 = 5.8 Functional
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 110 None -794 17 Rat 5.8 pEC50 = 5.8 Functional
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 187640 0 None - 1 Rat 6.8 pEC50 = 6.8 Functional
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 187640 0 None - 1 Rat 6.8 pEC50 = 6.8 Functional
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 187604 0 None - 1 Rat 6.8 pEC50 = 6.8 Functional
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 187604 0 None - 1 Rat 6.8 pEC50 = 6.8 Functional
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 180086 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 180086 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 139931 14 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 139931 14 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 137810 0 None 1 2 Human 5.8 pEC50 = 5.8 Functional
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 137810 0 None 1 2 Human 5.8 pEC50 = 5.8 Functional
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 137831 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 137831 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 139931 14 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 139931 14 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 137810 0 None 1 2 Human 5.8 pEC50 = 5.8 Functional
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 137810 0 None 1 2 Human 5.8 pEC50 = 5.8 Functional
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 139044 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 139044 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 138973 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 138973 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 139044 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 139044 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 124075 0 None 36 2 Human 7.8 pEC50 = 7.8 Functional
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 124075 0 None 36 2 Human 7.8 pEC50 = 7.8 Functional
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 139651 1 None -3 2 Rat 5.8 pEC50 = 5.8 Functional
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 139651 1 None -3 2 Rat 5.8 pEC50 = 5.8 Functional
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 137741 0 None 2 2 Human 6.7 pEC50 = 6.7 Functional
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 137741 0 None 2 2 Human 6.7 pEC50 = 6.7 Functional
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 139651 1 None -3 2 Rat 5.7 pEC50 = 5.7 Functional
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 139651 1 None -3 2 Rat 5.7 pEC50 = 5.7 Functional
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 137741 0 None 2 2 Human 6.7 pEC50 = 6.7 Functional
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 137741 0 None 2 2 Human 6.7 pEC50 = 6.7 Functional
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 137737 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 137737 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 192829 0 None - 1 Rat 7.7 pEC50 = 7.7 Functional
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 192829 0 None - 1 Rat 7.7 pEC50 = 7.7 Functional
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 137660 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 137660 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 137794 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 137794 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 110 None -741 17 Human 4.7 pEC50 = 4.7 Functional
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 110 None -741 17 Human 4.7 pEC50 = 4.7 Functional
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 110 None -741 17 Human 4.7 pEC50 = 4.7 Functional
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 110 None -741 17 Human 4.7 pEC50 = 4.7 Functional
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 110 None -741 17 Human 4.7 pEC50 = 4.7 Functional
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 110 None -741 17 Human 4.7 pEC50 = 4.7 Functional
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 110 None -741 17 Human 4.7 pEC50 = 4.7 Functional
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 137737 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 137737 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 137794 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 137794 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 137660 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
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 137660 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
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 124248 0 None 17 2 Human 6.7 pEC50 = 6.7 Functional
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 124248 0 None 17 2 Human 6.7 pEC50 = 6.7 Functional
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 180455 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 180455 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 193134 0 None - 1 Rat 7.7 pEC50 = 7.7 Functional
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 193134 0 None - 1 Rat 7.7 pEC50 = 7.7 Functional
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 124253 0 None 17 2 Human 7.7 pEC50 = 7.7 Functional
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 124253 0 None 17 2 Human 7.7 pEC50 = 7.7 Functional
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 124256 0 None 41 2 Human 7.7 pEC50 = 7.7 Functional
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 124256 0 None 41 2 Human 7.7 pEC50 = 7.7 Functional
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 26 None 1 2 Rat 6.7 pEC50 = 6.7 Functional
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 26 None 1 2 Rat 6.7 pEC50 = 6.7 Functional
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 26 None 1 2 Rat 6.7 pEC50 = 6.7 Functional
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 124251 0 None 12 2 Human 6.7 pEC50 = 6.7 Functional
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 124251 0 None 12 2 Human 6.7 pEC50 = 6.7 Functional
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 138984 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 138984 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 187636 0 None - 1 Rat 7.7 pEC50 = 7.7 Functional
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 187636 0 None - 1 Rat 7.7 pEC50 = 7.7 Functional
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 124235 0 None 19 2 Human 7.7 pEC50 = 7.7 Functional
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 124235 0 None 19 2 Human 7.7 pEC50 = 7.7 Functional
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 137730 0 None 51 2 Human 7.7 pEC50 = 7.7 Functional
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 137730 0 None 51 2 Human 7.7 pEC50 = 7.7 Functional
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 138973 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 138973 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 138984 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 138984 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 182630 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 182630 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 137730 0 None 51 2 Human 7.7 pEC50 = 7.7 Functional
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 137730 0 None 51 2 Human 7.7 pEC50 = 7.7 Functional
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 124230 0 None 12 2 Human 7.7 pEC50 = 7.7 Functional
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 124230 0 None 12 2 Human 7.7 pEC50 = 7.7 Functional
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 137695 2 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 137695 2 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 137662 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 137662 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 137728 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 137728 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 0 None - 1 Rat 6.7 pEC50 = 6.7 Functional
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 0 None - 1 Rat 6.7 pEC50 = 6.7 Functional
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 0 None - 1 Rat 6.7 pEC50 = 6.7 Functional
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 182521 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 182521 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 137662 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
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 137662 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
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 138963 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 138963 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 137848 0 None 6 2 Human 6.6 pEC50 = 6.6 Functional
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 137848 0 None 6 2 Human 6.6 pEC50 = 6.6 Functional
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 124255 0 None 22 2 Human 7.6 pEC50 = 7.6 Functional
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 124255 0 None 22 2 Human 7.6 pEC50 = 7.6 Functional
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 123933 0 None 30 2 Human 7.6 pEC50 = 7.6 Functional
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 123933 0 None 30 2 Human 7.6 pEC50 = 7.6 Functional
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 37 None -60 11 Rat 4.6 pEC50 = 4.6 Functional
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 37 None -60 11 Rat 4.6 pEC50 = 4.6 Functional
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 37 None -60 11 Rat 4.6 pEC50 = 4.6 Functional
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 110 None -794 17 Rat 4.6 pEC50 = 4.6 Functional
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 110 None -794 17 Rat 4.6 pEC50 = 4.6 Functional
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 110 None -794 17 Rat 4.6 pEC50 = 4.6 Functional
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 110 None -794 17 Rat 4.6 pEC50 = 4.6 Functional
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 110 None -794 17 Rat 4.6 pEC50 = 4.6 Functional
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 110 None -794 17 Rat 4.6 pEC50 = 4.6 Functional
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 110 None -794 17 Rat 4.6 pEC50 = 4.6 Functional
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 137848 0 None 6 2 Human 6.6 pEC50 = 6.6 Functional
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 137848 0 None 6 2 Human 6.6 pEC50 = 6.6 Functional
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 139941 0 None -4 2 Rat 5.6 pEC50 = 5.6 Functional
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 139941 0 None -4 2 Rat 5.6 pEC50 = 5.6 Functional
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 123933 0 None 30 2 Human 7.6 pEC50 = 7.6 Functional
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 123933 0 None 30 2 Human 7.6 pEC50 = 7.6 Functional
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 123928 0 None 25 2 Human 7.6 pEC50 = 7.6 Functional
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 123928 0 None 25 2 Human 7.6 pEC50 = 7.6 Functional
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 123928 0 None 25 2 Human 7.6 pEC50 = 7.6 Functional
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 123928 0 None 25 2 Human 7.6 pEC50 = 7.6 Functional
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 139941 0 None -4 2 Rat 5.6 pEC50 = 5.6 Functional
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 139941 0 None -4 2 Rat 5.6 pEC50 = 5.6 Functional
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 137831 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
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 137831 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
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 138963 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
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 138963 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
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 139114 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
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 139114 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
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 26 None -1 2 Human 6.6 pEC50 = 6.6 Functional
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 26 None -1 2 Human 6.6 pEC50 = 6.6 Functional
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 26 None -1 2 Human 6.6 pEC50 = 6.6 Functional
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 139114 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
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 139114 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
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 26 None -1 2 Human 6.6 pEC50 = 6.6 Functional
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 26 None -1 2 Human 6.6 pEC50 = 6.6 Functional
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 26 None -1 2 Human 6.6 pEC50 = 6.6 Functional
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 139042 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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 139042 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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 187604 0 None - 1 Rat 7.6 pEC50 = 7.6 Functional
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 187604 0 None - 1 Rat 7.6 pEC50 = 7.6 Functional
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 137642 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
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 137642 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
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 137695 2 None - 1 Human 7.6 pEC50 = 7.6 Functional
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 137695 2 None - 1 Human 7.6 pEC50 = 7.6 Functional
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 137790 0 None 2 2 Human 6.6 pEC50 = 6.6 Functional
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 137790 0 None 2 2 Human 6.6 pEC50 = 6.6 Functional
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 137790 0 None 2 2 Human 6.6 pEC50 = 6.6 Functional
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 137790 0 None 2 2 Human 6.6 pEC50 = 6.6 Functional
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 137642 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
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 137642 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
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 124231 0 None 10 2 Human 7.6 pEC50 = 7.6 Functional
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 124231 0 None 10 2 Human 7.6 pEC50 = 7.6 Functional
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 187304 0 None - 1 Rat 6.6 pEC50 = 6.6 Functional
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 187304 0 None - 1 Rat 6.6 pEC50 = 6.6 Functional
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 139113 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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 139113 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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 137804 0 None 6 2 Human 6.6 pEC50 = 6.6 Functional
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 137804 0 None 6 2 Human 6.6 pEC50 = 6.6 Functional
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 139113 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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 139113 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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 137804 0 None 6 2 Human 6.6 pEC50 = 6.6 Functional
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 137804 0 None 6 2 Human 6.6 pEC50 = 6.6 Functional
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 139754 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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 139754 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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 139754 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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 139754 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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 26 None 1 2 Rat 6.6 pEC50 = 6.6 Functional
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 26 None 1 2 Rat 6.6 pEC50 = 6.6 Functional
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 26 None 1 2 Rat 6.6 pEC50 = 6.6 Functional
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 26 None 1 2 Rat 6.6 pEC50 = 6.6 Functional
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 26 None 1 2 Rat 6.6 pEC50 = 6.6 Functional
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 26 None 1 2 Rat 6.6 pEC50 = 6.6 Functional
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 124232 0 None 9 2 Human 7.6 pEC50 = 7.6 Functional
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 124232 0 None 9 2 Human 7.6 pEC50 = 7.6 Functional
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 124228 0 None 16 2 Human 7.5 pEC50 = 7.5 Functional
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 124228 0 None 16 2 Human 7.5 pEC50 = 7.5 Functional
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 124258 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
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 124258 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
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 123938 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 123938 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 110 None -794 17 Rat 5.5 pEC50 = 5.5 Functional
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 110 None -794 17 Rat 5.5 pEC50 = 5.5 Functional
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 110 None -794 17 Rat 5.5 pEC50 = 5.5 Functional
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 110 None -794 17 Rat 5.5 pEC50 = 5.5 Functional
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 110 None -794 17 Rat 5.5 pEC50 = 5.5 Functional
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 110 None -794 17 Rat 5.5 pEC50 = 5.5 Functional
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 110 None -794 17 Rat 5.5 pEC50 = 5.5 Functional
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 183582 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 183582 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 123932 6 None 1 3 Human 7.5 pEC50 = 7.5 Functional
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 123932 6 None 1 3 Human 7.5 pEC50 = 7.5 Functional
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 123932 6 None 1 3 Human 7.5 pEC50 = 7.5 Functional
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 123932 6 None 1 3 Human 7.5 pEC50 = 7.5 Functional
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 123932 6 None 1 3 Human 7.5 pEC50 = 7.5 Functional
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 123932 6 None 1 3 Human 7.5 pEC50 = 7.5 Functional
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 42 None -1023 7 Rat 4.5 pEC50 = 4.5 Functional
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 42 None -1023 7 Rat 4.5 pEC50 = 4.5 Functional
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 42 None -1023 7 Rat 4.5 pEC50 = 4.5 Functional
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 123930 0 None 34 2 Human 7.5 pEC50 = 7.5 Functional
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 123930 0 None 34 2 Human 7.5 pEC50 = 7.5 Functional
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 123930 0 None 34 2 Human 7.5 pEC50 = 7.5 Functional
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 123930 0 None 34 2 Human 7.5 pEC50 = 7.5 Functional
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 124260 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 124260 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 137852 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
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 137852 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
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 137852 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
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 137852 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
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 124233 0 None 19 2 Human 7.5 pEC50 = 7.5 Functional
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 124233 0 None 19 2 Human 7.5 pEC50 = 7.5 Functional
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 124247 0 None 32 2 Human 7.5 pEC50 = 7.5 Functional
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 124247 0 None 32 2 Human 7.5 pEC50 = 7.5 Functional
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 138964 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
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 138964 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
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 138986 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 138986 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 137649 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 137649 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 138986 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 138986 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 40 None -1 3 Rat 6.5 pEC50 = 6.5 Functional
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 40 None -1 3 Rat 6.5 pEC50 = 6.5 Functional
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 40 None -1 3 Rat 6.5 pEC50 = 6.5 Functional
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 140092 10 None -2 2 Rat 5.4 pEC50 = 5.4 Functional
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 140092 10 None -2 2 Rat 5.4 pEC50 = 5.4 Functional
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 139023 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
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 139023 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
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 138964 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
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 138964 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
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 139023 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
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 139023 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
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 140092 10 None -2 2 Rat 5.4 pEC50 = 5.4 Functional
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 140092 10 None -2 2 Rat 5.4 pEC50 = 5.4 Functional
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 139188 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
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 139188 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
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 139188 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
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 139188 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
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 137649 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
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 137649 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
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 187639 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
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 187639 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
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 124245 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
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 124245 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
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 138981 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
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 138981 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
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 40 None -1 3 Human 6.4 pEC50 = 6.4 Functional
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 40 None -1 3 Human 6.4 pEC50 = 6.4 Functional
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 40 None -1 3 Human 6.4 pEC50 = 6.4 Functional
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 40 None -1 3 Human 6.4 pEC50 = 6.4 Functional
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 40 None -1 3 Human 6.4 pEC50 = 6.4 Functional
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 40 None -1 3 Human 6.4 pEC50 = 6.4 Functional
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 138981 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
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 138981 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
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 187639 0 None - 1 Rat 6.4 pEC50 = 6.4 Functional
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 187639 0 None - 1 Rat 6.4 pEC50 = 6.4 Functional
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 187237 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
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 187237 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
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 187304 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
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 187304 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
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 123932 6 None -1 3 Rat 7.4 pEC50 = 7.4 Functional
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 123932 6 None -1 3 Rat 7.4 pEC50 = 7.4 Functional
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 123932 6 None -1 3 Rat 7.4 pEC50 = 7.4 Functional
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 123932 6 None -1 3 Rat 7.4 pEC50 = 7.4 Functional
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 137675 0 None 4 2 Human 7.4 pEC50 = 7.4 Functional
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 137675 0 None 4 2 Human 7.4 pEC50 = 7.4 Functional
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 137675 0 None 4 2 Human 7.4 pEC50 = 7.4 Functional
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 137675 0 None 4 2 Human 7.4 pEC50 = 7.4 Functional
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 183529 0 None 5 3 Human 7.4 pEC50 = 7.4 Functional
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 183529 0 None 5 3 Human 7.4 pEC50 = 7.4 Functional
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 42 None -8 14 Rat 4.4 pEC50 = 4.4 Functional
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 42 None -8 14 Rat 4.4 pEC50 = 4.4 Functional
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 42 None -8 14 Rat 4.4 pEC50 = 4.4 Functional
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 102201 23 None -4 5 Rat 4.4 pEC50 = 4.4 Functional
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 102201 23 None -4 5 Rat 4.4 pEC50 = 4.4 Functional
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 102201 23 None -4 5 Rat 4.4 pEC50 = 4.4 Functional
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 64 None -21 2 Rat 4.4 pEC50 = 4.4 Functional
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 64 None -21 2 Rat 4.4 pEC50 = 4.4 Functional
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 64 None -21 2 Rat 4.4 pEC50 = 4.4 Functional
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 64 None -21 2 Rat 4.4 pEC50 = 4.4 Functional
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 137783 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
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 137783 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
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 187673 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
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 187673 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
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 124229 0 None 8 2 Human 7.4 pEC50 = 7.4 Functional
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 124229 0 None 8 2 Human 7.4 pEC50 = 7.4 Functional
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 123926 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
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 123926 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
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 123926 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
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 123926 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
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 124242 0 None 25 2 Human 7.3 pEC50 = 7.3 Functional
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 124242 0 None 25 2 Human 7.3 pEC50 = 7.3 Functional
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 124249 0 None 1 2 Human 5.3 pEC50 = 5.3 Functional
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 124249 0 None 1 2 Human 5.3 pEC50 = 5.3 Functional
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 137773 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
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 137773 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
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 139164 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
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 139164 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
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 187640 0 None - 1 Rat 7.3 pEC50 = 7.3 Functional
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 187640 0 None - 1 Rat 7.3 pEC50 = 7.3 Functional
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 137773 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
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 137773 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
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 40701 11 None 2 2 Human 5.3 pEC50 = 5.3 Functional
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 40701 11 None 2 2 Human 5.3 pEC50 = 5.3 Functional
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 139164 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
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 139164 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
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 124226 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
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 124226 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
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 40701 11 None 2 2 Human 5.3 pEC50 = 5.3 Functional
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 40701 11 None 2 2 Human 5.3 pEC50 = 5.3 Functional
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 139074 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
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 139074 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
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 139074 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
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 139074 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
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 124236 0 None 20 2 Human 7.3 pEC50 = 7.3 Functional
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 124236 0 None 20 2 Human 7.3 pEC50 = 7.3 Functional
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 124237 0 None 22 2 Human 7.3 pEC50 = 7.3 Functional
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 124237 0 None 22 2 Human 7.3 pEC50 = 7.3 Functional
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 124243 0 None 18 2 Human 7.3 pEC50 = 7.3 Functional
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 124243 0 None 18 2 Human 7.3 pEC50 = 7.3 Functional
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 137783 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
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 137783 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
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 137834 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
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 137834 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
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 137633 0 None 38 2 Human 7.3 pEC50 = 7.3 Functional
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 137633 0 None 38 2 Human 7.3 pEC50 = 7.3 Functional
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 181978 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
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 181978 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
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 137633 0 None 38 2 Human 7.3 pEC50 = 7.3 Functional
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 137633 0 None 38 2 Human 7.3 pEC50 = 7.3 Functional
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 0 None - 1 Rat 7.3 pEC50 = 7.3 Functional
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 0 None - 1 Rat 7.3 pEC50 = 7.3 Functional
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 0 None - 1 Rat 7.3 pEC50 = 7.3 Functional
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 137719 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
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 137719 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
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 137719 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
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 137719 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
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 124239 0 None 10 2 Human 6.3 pEC50 = 6.3 Functional
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 124239 0 None 10 2 Human 6.3 pEC50 = 6.3 Functional
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 137834 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
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 137834 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
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 124252 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
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 124252 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
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 137758 0 None 7 2 Human 7.3 pEC50 = 7.3 Functional
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 137758 0 None 7 2 Human 7.3 pEC50 = 7.3 Functional
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 123929 0 None 5 2 Human 7.3 pEC50 = 7.3 Functional
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 123929 0 None 5 2 Human 7.3 pEC50 = 7.3 Functional
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 137758 0 None 7 2 Human 7.3 pEC50 = 7.3 Functional
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 137758 0 None 7 2 Human 7.3 pEC50 = 7.3 Functional
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 123929 0 None 5 2 Human 7.3 pEC50 = 7.3 Functional
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 123929 0 None 5 2 Human 7.3 pEC50 = 7.3 Functional
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 123925 4 None - 1 Human 6.3 pEC50 = 6.3 Functional
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 123925 4 None - 1 Human 6.3 pEC50 = 6.3 Functional
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 123925 4 None - 1 Human 6.3 pEC50 = 6.3 Functional
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 123925 4 None - 1 Human 6.3 pEC50 = 6.3 Functional
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 137807 0 None 4 2 Human 6.3 pEC50 = 6.3 Functional
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 137807 0 None 4 2 Human 6.3 pEC50 = 6.3 Functional
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 26 None 1 2 Rat 7.3 pEC50 = 7.3 Functional
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 26 None 1 2 Rat 7.3 pEC50 = 7.3 Functional
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 26 None 1 2 Rat 7.3 pEC50 = 7.3 Functional
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 137685 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
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 137685 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
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 182513 0 None 3 3 Human 7.3 pEC50 = 7.3 Functional
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 182513 0 None 3 3 Human 7.3 pEC50 = 7.3 Functional
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 137807 0 None 4 2 Human 6.3 pEC50 = 6.3 Functional
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 137807 0 None 4 2 Human 6.3 pEC50 = 6.3 Functional
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 138960 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
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 138960 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
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 138960 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
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 138960 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
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 182895 0 None 4 3 Human 7.2 pEC50 = 7.2 Functional
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 182895 0 None 4 3 Human 7.2 pEC50 = 7.2 Functional
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 183390 0 None 1 3 Human 7.2 pEC50 = 7.2 Functional
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 183390 0 None 1 3 Human 7.2 pEC50 = 7.2 Functional
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 137685 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
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 137685 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
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 179580 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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 179580 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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 137728 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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 137728 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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 137721 0 None 4 2 Human 7.2 pEC50 = 7.2 Functional
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 137721 0 None 4 2 Human 7.2 pEC50 = 7.2 Functional
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 179952 0 None 4 3 Human 7.2 pEC50 = 7.2 Functional
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 179952 0 None 4 3 Human 7.2 pEC50 = 7.2 Functional
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 137721 0 None 4 2 Human 7.2 pEC50 = 7.2 Functional
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 137721 0 None 4 2 Human 7.2 pEC50 = 7.2 Functional
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 137768 0 None 9 2 Human 6.2 pEC50 = 6.2 Functional
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 137768 0 None 9 2 Human 6.2 pEC50 = 6.2 Functional
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 137768 0 None 9 2 Human 6.2 pEC50 = 6.2 Functional
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 137768 0 None 9 2 Human 6.2 pEC50 = 6.2 Functional
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 139192 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
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 139192 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
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 146452 53 None -16 3 Human 5.2 pEC50 = 5.2 Functional
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 146452 53 None -16 3 Human 5.2 pEC50 = 5.2 Functional
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 146452 53 None -16 3 Human 5.2 pEC50 = 5.2 Functional
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 139192 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
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 139192 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
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 193134 0 None - 1 Rat 7.2 pEC50 = 7.2 Functional
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 193134 0 None - 1 Rat 7.2 pEC50 = 7.2 Functional
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 137726 0 None 1 2 Human 6.2 pEC50 = 6.2 Functional
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 137726 0 None 1 2 Human 6.2 pEC50 = 6.2 Functional
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 137726 0 None 1 2 Human 6.2 pEC50 = 6.2 Functional
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 137726 0 None 1 2 Human 6.2 pEC50 = 6.2 Functional
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 139135 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
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 139135 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
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 139135 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
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 139135 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
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 139651 1 None 3 2 Human 6.2 pEC50 = 6.2 Functional
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 139651 1 None 3 2 Human 6.2 pEC50 = 6.2 Functional
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 139651 1 None 3 2 Human 6.1 pEC50 = 6.1 Functional
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 139651 1 None 3 2 Human 6.1 pEC50 = 6.1 Functional
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 110 None -794 17 Rat 5.1 pEC50 = 5.1 Functional
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 110 None -794 17 Rat 5.1 pEC50 = 5.1 Functional
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 110 None -794 17 Rat 5.1 pEC50 = 5.1 Functional
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 110 None -794 17 Rat 5.1 pEC50 = 5.1 Functional
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 110 None -794 17 Rat 5.1 pEC50 = 5.1 Functional
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 110 None -794 17 Rat 5.1 pEC50 = 5.1 Functional
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 110 None -794 17 Rat 5.1 pEC50 = 5.1 Functional
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 110 None -794 17 Rat 5.1 pEC50 = 5.1 Functional
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 110 None -794 17 Rat 5.1 pEC50 = 5.1 Functional
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 110 None -794 17 Rat 5.1 pEC50 = 5.1 Functional
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 110 None -794 17 Rat 5.1 pEC50 = 5.1 Functional
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 110 None -794 17 Rat 5.1 pEC50 = 5.1 Functional
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 110 None -794 17 Rat 5.1 pEC50 = 5.1 Functional
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 110 None -794 17 Rat 5.1 pEC50 = 5.1 Functional
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 179904 0 None 1 5 Human 7.1 pEC50 = 7.1 Functional
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 179904 0 None 1 5 Human 7.1 pEC50 = 7.1 Functional
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 124250 0 None 5 2 Human 6.1 pEC50 = 6.1 Functional
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 124250 0 None 5 2 Human 6.1 pEC50 = 6.1 Functional
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 181434 0 None 1 3 Human 7.1 pEC50 = 7.1 Functional
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 181434 0 None 1 3 Human 7.1 pEC50 = 7.1 Functional
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 138965 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 138965 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 183282 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
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 183282 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
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 138965 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 138965 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 123931 0 None 1 3 Human 7.1 pEC50 = 7.1 Functional
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 123931 0 None 1 3 Human 7.1 pEC50 = 7.1 Functional
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 123931 0 None 1 3 Human 7.1 pEC50 = 7.1 Functional
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 123931 0 None 1 3 Human 7.1 pEC50 = 7.1 Functional
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 96086 1 None 1 2 Rat 4.1 pEC50 = 4.1 Functional
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 96086 1 None 1 2 Rat 4.1 pEC50 = 4.1 Functional
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 137745 0 None 3 2 Human 6.1 pEC50 = 6.1 Functional
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 137745 0 None 3 2 Human 6.1 pEC50 = 6.1 Functional
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 137745 0 None 3 2 Human 6.1 pEC50 = 6.1 Functional
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 137745 0 None 3 2 Human 6.1 pEC50 = 6.1 Functional
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 139053 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 139053 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 124234 0 None 10 2 Human 7.1 pEC50 = 7.1 Functional
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 124234 0 None 10 2 Human 7.1 pEC50 = 7.1 Functional
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 139053 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 139053 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 187673 0 None - 1 Rat 7.1 pEC50 = 7.1 Functional
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 187673 0 None - 1 Rat 7.1 pEC50 = 7.1 Functional
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 139941 0 None 4 2 Human 6.1 pEC50 = 6.1 Functional
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 139941 0 None 4 2 Human 6.1 pEC50 = 6.1 Functional
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 139941 0 None 4 2 Human 6.0 pEC50 = 6.0 Functional
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 139941 0 None 4 2 Human 6.0 pEC50 = 6.0 Functional
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 139098 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 139098 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 42 None -4 14 Human 5.0 pEC50 = 5.0 Functional
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 42 None -4 14 Human 5.0 pEC50 = 5.0 Functional
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 42 None -4 14 Human 5.0 pEC50 = 5.0 Functional
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 139098 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 139098 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 124246 0 None 52 2 Human 7.0 pEC50 = 7.0 Functional
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 124246 0 None 52 2 Human 7.0 pEC50 = 7.0 Functional
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 138993 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 138993 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 138993 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 138993 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 138952 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
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 138952 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
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 138952 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
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 138952 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
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 123927 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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 123927 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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 123927 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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 123927 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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 123934 0 None 1 2 Human 7.0 pEC50 = 7.0 Functional
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 123934 0 None 1 2 Human 7.0 pEC50 = 7.0 Functional
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 123934 0 None 1 2 Human 7.0 pEC50 = 7 Functional
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 123934 0 None 1 2 Human 7.0 pEC50 = 7 Functional
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 182175 0 None - 1 Human 7.0 pEC50 = 7 Functional
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 182175 0 None - 1 Human 7.0 pEC50 = 7 Functional
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 89956 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
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 89956 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
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 70972 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
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 70972 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
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 148333 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
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 148333 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
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 71024 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
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 71024 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
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 1 None - 1 Human 9.1 pIC50 = 9.1 Functional
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 1 None - 1 Human 9.1 pIC50 = 9.1 Functional
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 1 None - 1 Human 9.1 pIC50 = 9.1 Functional
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 73212 1 None 18 3 Rat 9.1 pIC50 = 9.1 Functional
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 73212 1 None 18 3 Rat 9.1 pIC50 = 9.1 Functional
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 83822 0 None 10000 2 Human 9.0 pIC50 = 9 Functional
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 83822 0 None 10000 2 Human 9.0 pIC50 = 9 Functional
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 83823 0 None - 1 Human 9.0 pIC50 = 9 Functional
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 83823 0 None - 1 Human 9.0 pIC50 = 9 Functional
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 83824 0 None - 1 Human 9.0 pIC50 = 9 Functional
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 83824 0 None - 1 Human 9.0 pIC50 = 9 Functional
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 12 None -3 3 Human 9.0 pIC50 = 9 Functional
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 12 None -3 3 Human 9.0 pIC50 = 9 Functional
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 12 None -3 3 Human 9.0 pIC50 = 9 Functional
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 42 None 4 3 Rat 9.0 pIC50 = 9 Functional
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 42 None 4 3 Rat 9.0 pIC50 = 9 Functional
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 42 None 4 3 Rat 9.0 pIC50 = 9 Functional
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 62660 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
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 62660 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
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 62 None 3 2 Human 8.9 pIC50 = 8.9 Functional
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 62 None 3 2 Human 8.9 pIC50 = 8.9 Functional
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 62 None 3 2 Human 8.9 pIC50 = 8.9 Functional
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 62 None 3 2 Human 8.9 pIC50 = 8.9 Functional
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 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
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 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
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 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
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 62670 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
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 62670 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
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 175070 0 None 4 3 Mouse 8.8 pIC50 = 8.8 Functional
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 175070 0 None 4 3 Mouse 8.8 pIC50 = 8.8 Functional
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 62744 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 62744 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 197378 2 None 4365 2 Human 8.7 pIC50 = 8.7 Functional
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 197378 2 None 4365 2 Human 8.7 pIC50 = 8.7 Functional
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 62748 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 62748 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 42 None -4 3 Human 8.0 pIC50 = 8 Functional
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 42 None -4 3 Human 8.0 pIC50 = 8 Functional
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 42 None -4 3 Human 8.0 pIC50 = 8 Functional
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 197347 0 None - 1 Human 8.0 pIC50 = 8 Functional
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 197347 0 None - 1 Human 8.0 pIC50 = 8 Functional
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 70974 0 None - 1 Human 8.0 pIC50 = 8 Functional
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 70974 0 None - 1 Human 8.0 pIC50 = 8 Functional
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 62665 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
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 62665 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
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 62663 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
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 62663 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
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 62756 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
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 62756 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
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 62747 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
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 62747 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
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 73217 0 None - 1 Human 7.0 pIC50 = 7 Functional
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 73217 0 None - 1 Human 7.0 pIC50 = 7 Functional
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 198648 0 None - 1 Human 7.0 pIC50 = 7 Functional
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 198648 0 None - 1 Human 7.0 pIC50 = 7 Functional
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 155059 0 None - 1 Human 6.0 pIC50 = 6 Functional
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 155059 0 None - 1 Human 6.0 pIC50 = 6 Functional
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 175551 0 None -4 2 Mouse 6.0 pIC50 = 6 Functional
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 175551 0 None -4 2 Mouse 6.0 pIC50 = 6 Functional
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 92033 0 None - 1 Human 6.0 pIC50 = 6 Functional
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 92033 0 None - 1 Human 6.0 pIC50 = 6 Functional
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 53 None -1 2 Human 5.0 pIC50 = 5 Functional
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 53 None -1 2 Human 5.0 pIC50 = 5 Functional
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 53 None -1 2 Human 5.0 pIC50 = 5 Functional
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 125122 0 None -501 2 Human 5.0 pIC50 = 5 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 125122 0 None -501 2 Human 5.0 pIC50 = 5 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 142071 0 None 1 3 Human 7.0 pIC50 = 7 Functional
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 142071 0 None 1 3 Human 7.0 pIC50 = 7 Functional
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 86752 0 None - 1 Rat 6.0 pIC50 = 6.0 Functional
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 86752 0 None - 1 Rat 6.0 pIC50 = 6.0 Functional
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 87517 0 None -12 2 Human 6.0 pIC50 = 6.0 Functional
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 87517 0 None -12 2 Human 6.0 pIC50 = 6.0 Functional
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 62667 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
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 62667 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
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 92353 20 None - 1 Rat 7.0 pIC50 = 7.0 Functional
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 92353 20 None - 1 Rat 7.0 pIC50 = 7.0 Functional
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 124240 0 None 22 2 Human 7.0 pIC50 = 7.0 Functional
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 124240 0 None 22 2 Human 7.0 pIC50 = 7.0 Functional
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 142343 0 None - 1 Rat 6.0 pIC50 = 6.0 Functional
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 142343 0 None - 1 Rat 6.0 pIC50 = 6.0 Functional
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 94753 1 None - 1 Rat 5.0 pIC50 = 5.0 Functional
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 94753 1 None - 1 Rat 5.0 pIC50 = 5.0 Functional
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 18121 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
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 18121 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
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 133104 0 None -22 2 Human 6.0 pIC50 = 6.0 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133104 0 None -22 2 Human 6.0 pIC50 = 6.0 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 62743 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
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 62743 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
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 195185 7 None - 1 Rat 5.0 pIC50 = 5.0 Functional
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 195185 7 None - 1 Rat 5.0 pIC50 = 5.0 Functional
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 118910 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
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 118910 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
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 18315 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
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 18315 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
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 8232 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
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 8232 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
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 62655 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
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 62655 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
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 189202 0 None 5 3 Human 8.0 pIC50 = 8.0 Functional
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 189202 0 None 5 3 Human 8.0 pIC50 = 8.0 Functional
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 197258 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
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 197258 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
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 73213 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
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 73213 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
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 154944 0 None - 1 Rat 7.0 pIC50 = 7.0 Functional
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 154944 0 None - 1 Rat 7.0 pIC50 = 7.0 Functional
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 154573 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
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 154573 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
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 125100 0 None -218 2 Human 6.0 pIC50 = 6.0 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 125100 0 None -218 2 Human 6.0 pIC50 = 6.0 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 125136 0 None -64 2 Human 6.0 pIC50 = 6.0 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 125136 0 None -64 2 Human 6.0 pIC50 = 6.0 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 114339 3 None - 1 Human 7.0 pIC50 = 7.0 Functional
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 114339 3 None - 1 Human 7.0 pIC50 = 7.0 Functional
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 114339 3 None - 1 Human 7.0 pIC50 = 7.0 Functional
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 114339 3 None - 1 Human 7.0 pIC50 = 7.0 Functional
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 85154 0 None 1 2 Human 7.0 pIC50 = 7.0 Functional
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 85154 0 None 1 2 Human 7.0 pIC50 = 7.0 Functional
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 91048 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 91048 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 92021 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
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 92021 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
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 70982 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
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 70982 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
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 91048 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 91048 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 92021 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
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 92021 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
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 125109 0 None -169 2 Human 5.9 pIC50 = 5.9 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 125109 0 None -169 2 Human 5.9 pIC50 = 5.9 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133120 0 None -117 2 Human 4.9 pIC50 = 4.9 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133120 0 None -117 2 Human 4.9 pIC50 = 4.9 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 83815 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 83815 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 148612 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 148612 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 71042 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 71042 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 173309 0 None -4 3 Mouse 7.9 pIC50 = 7.9 Functional
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 173309 0 None -4 3 Mouse 7.9 pIC50 = 7.9 Functional
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 62750 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 62750 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 62745 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 62745 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 124257 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 124257 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 62657 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 62657 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 176833 0 None 1 2 Human 6.9 pIC50 = 6.9 Functional
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 176833 0 None 1 2 Human 6.9 pIC50 = 6.9 Functional
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 88473 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
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 88473 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
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 133081 0 None -54 2 Human 5.9 pIC50 = 5.9 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133081 0 None -54 2 Human 5.9 pIC50 = 5.9 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 29048 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 29048 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 94665 0 None - 1 Rat 4.9 pIC50 = 4.9 Functional
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 94665 0 None - 1 Rat 4.9 pIC50 = 4.9 Functional
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 85194 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
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 85194 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
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 118906 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
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 118906 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
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 124238 0 None 53 2 Human 6.9 pIC50 = 6.9 Functional
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 124238 0 None 53 2 Human 6.9 pIC50 = 6.9 Functional
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 70992 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
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 70992 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
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 118915 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 118915 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 93930 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
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 93930 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
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 114342 3 None - 1 Human 6.9 pIC50 = 6.9 Functional
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 114342 3 None - 1 Human 6.9 pIC50 = 6.9 Functional
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 62764 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 62764 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 84809 1 None 1 3 Human 7.9 pIC50 = 7.9 Functional
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 84809 1 None 1 3 Human 7.9 pIC50 = 7.9 Functional
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 85102 0 None 1 2 Human 6.9 pIC50 = 6.9 Functional
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 85102 0 None 1 2 Human 6.9 pIC50 = 6.9 Functional
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 197105 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
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 197105 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
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 94754 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
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 94754 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
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 125078 0 None -181 2 Human 5.9 pIC50 = 5.9 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 125078 0 None -181 2 Human 5.9 pIC50 = 5.9 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133025 0 None -28 2 Human 5.9 pIC50 = 5.9 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133025 0 None -28 2 Human 5.9 pIC50 = 5.9 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133042 0 None -5 2 Human 5.9 pIC50 = 5.9 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133042 0 None -5 2 Human 5.9 pIC50 = 5.9 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 87516 0 None -25 2 Human 5.9 pIC50 = 5.9 Functional
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 87516 0 None -25 2 Human 5.9 pIC50 = 5.9 Functional
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 154844 0 None - 1 Rat 4.9 pIC50 = 4.9 Functional
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 154844 0 None - 1 Rat 4.9 pIC50 = 4.9 Functional
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 91049 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 91049 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 70994 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
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 70994 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
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 91049 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 91049 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 122206 0 None -354 2 Rat 5.9 pIC50 = 5.9 Functional
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 122206 0 None -354 2 Rat 5.9 pIC50 = 5.9 Functional
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 114331 3 None - 1 Human 6.9 pIC50 = 6.9 Functional
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 114331 3 None - 1 Human 6.9 pIC50 = 6.9 Functional
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 62769 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
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 62769 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
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 73222 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
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 73222 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
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 91036 1 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 91036 1 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 85008 0 None 1 2 Human 6.9 pIC50 = 6.9 Functional
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 85008 0 None 1 2 Human 6.9 pIC50 = 6.9 Functional
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 83826 0 None 707 2 Human 7.9 pIC50 = 7.9 Functional
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 83826 0 None 707 2 Human 7.9 pIC50 = 7.9 Functional
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 70978 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 70978 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
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 62752 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
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 62752 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
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 85063 0 None 1 3 Human 6.9 pIC50 = 6.9 Functional
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 85063 0 None 1 3 Human 6.9 pIC50 = 6.9 Functional
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 123939 6 None - 1 Human 6.9 pIC50 = 6.9 Functional
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 123939 6 None - 1 Human 6.9 pIC50 = 6.9 Functional
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 133041 0 None -9 2 Human 5.9 pIC50 = 5.9 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133041 0 None -9 2 Human 5.9 pIC50 = 5.9 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133043 0 None -109 2 Human 5.9 pIC50 = 5.9 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133043 0 None -109 2 Human 5.9 pIC50 = 5.9 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133074 0 None -1 2 Human 5.9 pIC50 = 5.9 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133074 0 None -1 2 Human 5.9 pIC50 = 5.9 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 168297 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 168297 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 91036 1 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 91036 1 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 105603 0 None -3715 2 Human 4.9 pIC50 = 4.9 Functional
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 105603 0 None -3715 2 Human 4.9 pIC50 = 4.9 Functional
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 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 118909 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 118909 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 92029 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
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 92029 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
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 124244 0 None 13 2 Human 6.8 pIC50 = 6.8 Functional
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 124244 0 None 13 2 Human 6.8 pIC50 = 6.8 Functional
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 92029 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
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 92029 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
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 85068 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
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 85068 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
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 139148 0 None 15 2 Rat 6.8 pIC50 = 6.8 Functional
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 139148 0 None 15 2 Rat 6.8 pIC50 = 6.8 Functional
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 139148 0 None 15 2 Rat 6.8 pIC50 = 6.8 Functional
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 139148 0 None 15 2 Rat 6.8 pIC50 = 6.8 Functional
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 125117 0 None -18 2 Human 5.8 pIC50 = 5.8 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 125117 0 None -18 2 Human 5.8 pIC50 = 5.8 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 83706 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
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 83706 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
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 70990 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
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 70990 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
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 71038 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
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 71038 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
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 71041 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
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 71041 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
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 133019 0 None 2 2 Human 7.8 pIC50 = 7.8 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133019 0 None 2 2 Human 7.8 pIC50 = 7.8 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133045 0 None -1 2 Human 7.8 pIC50 = 7.8 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133045 0 None -1 2 Human 7.8 pIC50 = 7.8 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 124259 0 None 40 2 Human 7.8 pIC50 = 7.8 Functional
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 124259 0 None 40 2 Human 7.8 pIC50 = 7.8 Functional
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 141263 0 None - 1 Rat 7.8 pIC50 = 7.8 Functional
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 141263 0 None - 1 Rat 7.8 pIC50 = 7.8 Functional
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 124254 0 None 26 2 Human 7.8 pIC50 = 7.8 Functional
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 124254 0 None 26 2 Human 7.8 pIC50 = 7.8 Functional
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 175549 0 None -3 3 Mouse 6.8 pIC50 = 6.8 Functional
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 175549 0 None -3 3 Mouse 6.8 pIC50 = 6.8 Functional
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 133018 0 None 1 2 Human 6.8 pIC50 = 6.8 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133018 0 None 1 2 Human 6.8 pIC50 = 6.8 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 198330 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
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 198330 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
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 197236 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
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 197236 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
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 198634 0 None 4 2 Human 5.8 pIC50 = 5.8 Functional
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 198634 0 None 4 2 Human 5.8 pIC50 = 5.8 Functional
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 94717 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
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 94717 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
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 125133 0 None -758 2 Human 5.8 pIC50 = 5.8 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 125133 0 None -758 2 Human 5.8 pIC50 = 5.8 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133072 0 None -7 2 Human 5.8 pIC50 = 5.8 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133072 0 None -7 2 Human 5.8 pIC50 = 5.8 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133109 0 None -151 2 Human 5.8 pIC50 = 5.8 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133109 0 None -151 2 Human 5.8 pIC50 = 5.8 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133112 0 None -501 2 Human 5.8 pIC50 = 5.8 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133112 0 None -501 2 Human 5.8 pIC50 = 5.8 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 78523 2 None - 1 Human 5.8 pIC50 = 5.8 Functional
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 78523 2 None - 1 Human 5.8 pIC50 = 5.8 Functional
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 167178 0 None - 1 Rat 4.8 pIC50 = 4.8 Functional
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 167178 0 None - 1 Rat 4.8 pIC50 = 4.8 Functional
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 138956 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
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 138956 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
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 138956 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
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 138956 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
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 195776 13 None - 1 Rat 4.8 pIC50 = 4.8 Functional
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 195776 13 None - 1 Rat 4.8 pIC50 = 4.8 Functional
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 83817 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 83817 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 124241 0 None 18 2 Human 6.8 pIC50 = 6.8 Functional
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 124241 0 None 18 2 Human 6.8 pIC50 = 6.8 Functional
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 89075 0 None -25 2 Human 5.8 pIC50 = 5.8 Functional
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 89075 0 None -25 2 Human 5.8 pIC50 = 5.8 Functional
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 89075 0 None -25 2 Human 5.8 pIC50 = 5.8 Functional
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 7921 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
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 7921 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
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 62758 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
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 62758 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
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 83827 0 None 630 2 Human 7.8 pIC50 = 7.8 Functional
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 83827 0 None 630 2 Human 7.8 pIC50 = 7.8 Functional
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 85222 11 None 1 3 Human 7.8 pIC50 = 7.8 Functional
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 85222 11 None 1 3 Human 7.8 pIC50 = 7.8 Functional
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 176808 0 None 1 3 Human 7.8 pIC50 = 7.8 Functional
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 176808 0 None 1 3 Human 7.8 pIC50 = 7.8 Functional
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 94998 17 None - 1 Human 7.8 pIC50 = 7.8 Functional
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 94998 17 None - 1 Human 7.8 pIC50 = 7.8 Functional
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 176895 0 None -2 3 Mouse 7.8 pIC50 = 7.8 Functional
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 176895 0 None -2 3 Mouse 7.8 pIC50 = 7.8 Functional
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 1 None - 1 Rat 7.8 pIC50 = 7.8 Functional
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 1 None - 1 Rat 7.8 pIC50 = 7.8 Functional
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 1 None - 1 Rat 7.8 pIC50 = 7.8 Functional
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 124227 0 None 21 2 Human 7.8 pIC50 = 7.8 Functional
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 124227 0 None 21 2 Human 7.8 pIC50 = 7.8 Functional
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 62664 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
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 62664 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
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 90219 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
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 90219 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
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 30 None -3 2 Human 6.8 pIC50 = 6.8 Functional
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 30 None -3 2 Human 6.8 pIC50 = 6.8 Functional
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 30 None -3 2 Human 6.8 pIC50 = 6.8 Functional
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 176833 0 None -1 2 Mouse 6.8 pIC50 = 6.8 Functional
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 176833 0 None -1 2 Mouse 6.8 pIC50 = 6.8 Functional
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 94823 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
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 94823 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
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 176831 0 None -2 3 Mouse 5.8 pIC50 = 5.8 Functional
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 176831 0 None -2 3 Mouse 5.8 pIC50 = 5.8 Functional
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 133049 0 None -2 2 Human 5.8 pIC50 = 5.8 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133049 0 None -2 2 Human 5.8 pIC50 = 5.8 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133069 0 None -2 2 Human 5.8 pIC50 = 5.8 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133069 0 None -2 2 Human 5.8 pIC50 = 5.8 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133092 0 None -40 2 Human 5.8 pIC50 = 5.8 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133092 0 None -40 2 Human 5.8 pIC50 = 5.8 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 91040 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 91040 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 139027 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
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 139027 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
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 139036 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
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 139036 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
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 114336 3 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 114336 3 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 91040 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 91040 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 139027 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
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 139027 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
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 139036 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
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 139036 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
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 125106 0 None -29 2 Human 5.8 pIC50 = 5.8 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 125106 0 None -29 2 Human 5.8 pIC50 = 5.8 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 91042 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 91042 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 91045 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 91045 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 91042 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 91042 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 141728 0 None 1 2 Human 6.8 pIC50 = 6.8 Functional
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 141728 0 None 1 2 Human 6.8 pIC50 = 6.8 Functional
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 141831 0 None -5 2 Human 6.8 pIC50 = 6.8 Functional
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 141831 0 None -5 2 Human 6.8 pIC50 = 6.8 Functional
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 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
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 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
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 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
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 91045 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 91045 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 150270 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
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 150270 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
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 62759 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
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 62759 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
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 85065 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
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 85065 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
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 70995 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
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 70995 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
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 198593 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 198593 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 133082 0 None -19 2 Human 6.8 pIC50 = 6.8 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133082 0 None -19 2 Human 6.8 pIC50 = 6.8 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 195912 17 None - 1 Rat 5.8 pIC50 = 5.8 Functional
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 195912 17 None - 1 Rat 5.8 pIC50 = 5.8 Functional
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 94751 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
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 94751 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
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 62775 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 62775 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 139092 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
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 139092 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
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 176761 0 None 2 3 Human 7.8 pIC50 = 7.8 Functional
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 176761 0 None 2 3 Human 7.8 pIC50 = 7.8 Functional
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 197106 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
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 197106 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
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 124075 0 None 36 2 Human 7.7 pIC50 = 7.7 Functional
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 124075 0 None 36 2 Human 7.7 pIC50 = 7.7 Functional
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 166113 0 None 1 3 Human 6.8 pIC50 = 6.8 Functional
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 166113 0 None 1 3 Human 6.8 pIC50 = 6.8 Functional
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 154809 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 154809 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
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 173566 0 None -3 3 Mouse 6.8 pIC50 = 6.8 Functional
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 173566 0 None -3 3 Mouse 6.8 pIC50 = 6.8 Functional
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 175165 0 None -4 3 Mouse 6.8 pIC50 = 6.8 Functional
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 175165 0 None -4 3 Mouse 6.8 pIC50 = 6.8 Functional
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 198928 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
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 198928 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
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 125128 0 None -177 2 Human 5.8 pIC50 = 5.8 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 125128 0 None -177 2 Human 5.8 pIC50 = 5.8 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 139092 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
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 139092 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
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 112544 0 None -177 5 Human 4.8 pIC50 = 4.8 Functional
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 112544 0 None -177 5 Human 4.8 pIC50 = 4.8 Functional
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 118919 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
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 118919 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
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 133121 0 None -83 2 Human 4.7 pIC50 = 4.7 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133121 0 None -83 2 Human 4.7 pIC50 = 4.7 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 85119 0 None 11 2 Human 6.7 pIC50 = 6.7 Functional
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 85119 0 None 11 2 Human 6.7 pIC50 = 6.7 Functional
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 114338 3 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 114338 3 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 92034 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 92034 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 133106 0 None -33 2 Human 5.7 pIC50 = 5.7 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133106 0 None -33 2 Human 5.7 pIC50 = 5.7 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 92034 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 92034 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 8230 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 8230 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 83704 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
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 83704 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
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 83812 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
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 83812 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
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 136842 0 None 42 2 Human 7.7 pIC50 = 7.7 Functional
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 136842 0 None 42 2 Human 7.7 pIC50 = 7.7 Functional
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 124256 0 None 41 2 Human 7.7 pIC50 = 7.7 Functional
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 124256 0 None 41 2 Human 7.7 pIC50 = 7.7 Functional
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 75706 0 None - 1 Rat 7.7 pIC50 = 7.7 Functional
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 75706 0 None - 1 Rat 7.7 pIC50 = 7.7 Functional
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 138516 0 None - 1 Rat 7.7 pIC50 = 7.7 Functional
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 138516 0 None - 1 Rat 7.7 pIC50 = 7.7 Functional
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 170106 0 None - 1 Rat 7.7 pIC50 = 7.7 Functional
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 170106 0 None - 1 Rat 7.7 pIC50 = 7.7 Functional
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 87518 0 None -5 2 Human 6.7 pIC50 = 6.7 Functional
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 87518 0 None -5 2 Human 6.7 pIC50 = 6.7 Functional
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 94716 0 None - 1 Rat 5.7 pIC50 = 5.7 Functional
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 94716 0 None - 1 Rat 5.7 pIC50 = 5.7 Functional
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 44 None - 1 Human 4.7 pIC50 = 4.7 Functional
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 44 None - 1 Human 4.7 pIC50 = 4.7 Functional
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 44 None - 1 Human 4.7 pIC50 = 4.7 Functional
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 92026 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
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 92026 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
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 92026 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
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 92026 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
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 125086 0 None -83 2 Human 5.7 pIC50 = 5.7 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 125086 0 None -83 2 Human 5.7 pIC50 = 5.7 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 83699 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 83699 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 70993 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 70993 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 133102 0 None -19 2 Human 5.7 pIC50 = 5.7 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133102 0 None -19 2 Human 5.7 pIC50 = 5.7 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 62668 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 62668 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 152542 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
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 152542 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
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 124248 0 None 17 2 Human 6.7 pIC50 = 6.7 Functional
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 124248 0 None 17 2 Human 6.7 pIC50 = 6.7 Functional
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 62654 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 62654 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 83821 0 None 501 2 Human 8.7 pIC50 = 8.7 Functional
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 83821 0 None 501 2 Human 8.7 pIC50 = 8.7 Functional
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 70999 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 70999 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 71033 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 71033 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 2 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 2 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 2 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 88686 0 None 323 2 Human 8.7 pIC50 = 8.7 Functional
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 88686 0 None 323 2 Human 8.7 pIC50 = 8.7 Functional
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 71034 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
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 71034 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
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 198495 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
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 198495 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
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 88742 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
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 88742 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
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 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
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 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
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 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
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 173309 0 None 4 3 Human 8.6 pIC50 = 8.6 Functional
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 173309 0 None 4 3 Human 8.6 pIC50 = 8.6 Functional
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 196859 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
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 196859 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
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 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
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 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
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 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
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 83831 0 None 501 2 Human 7.7 pIC50 = 7.7 Functional
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 83831 0 None 501 2 Human 7.7 pIC50 = 7.7 Functional
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 85092 11 None 1 2 Human 7.7 pIC50 = 7.7 Functional
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 85092 11 None 1 2 Human 7.7 pIC50 = 7.7 Functional
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 124253 0 None 17 2 Human 7.7 pIC50 = 7.7 Functional
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 124253 0 None 17 2 Human 7.7 pIC50 = 7.7 Functional
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 197814 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
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 197814 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
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 71025 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 71025 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 118912 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
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 118912 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
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 83830 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 83830 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 195650 24 None - 1 Rat 4.7 pIC50 = 4.7 Functional
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 195650 24 None - 1 Rat 4.7 pIC50 = 4.7 Functional
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 122201 2 None -524 2 Rat 6.7 pIC50 = 6.7 Functional
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 122201 2 None -524 2 Rat 6.7 pIC50 = 6.7 Functional
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 125112 0 None -33 2 Human 5.7 pIC50 = 5.7 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 125112 0 None -33 2 Human 5.7 pIC50 = 5.7 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 125069 0 None -346 2 Human 5.7 pIC50 = 5.7 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 125069 0 None -346 2 Human 5.7 pIC50 = 5.7 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 124251 0 None 12 2 Human 6.7 pIC50 = 6.7 Functional
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 124251 0 None 12 2 Human 6.7 pIC50 = 6.7 Functional
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 62771 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 62771 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 18316 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
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 18316 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
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 62772 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
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 62772 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
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 80839 0 None - 1 Rat 7.7 pIC50 = 7.7 Functional
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 80839 0 None - 1 Rat 7.7 pIC50 = 7.7 Functional
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 124235 0 None 19 2 Human 7.7 pIC50 = 7.7 Functional
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 124235 0 None 19 2 Human 7.7 pIC50 = 7.7 Functional
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 196860 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 196860 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 196855 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 196855 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 133021 0 None -8 2 Human 6.7 pIC50 = 6.7 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133021 0 None -8 2 Human 6.7 pIC50 = 6.7 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 87842 0 None -35 2 Rat 5.7 pIC50 = 5.7 Functional
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 87842 0 None -35 2 Rat 5.7 pIC50 = 5.7 Functional
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 94943 0 None 2 2 Rat 4.7 pIC50 = 4.7 Functional
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 94943 0 None 2 2 Rat 4.7 pIC50 = 4.7 Functional
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 94685 1 None -1 2 Rat 4.7 pIC50 = 4.7 Functional
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 94685 1 None -1 2 Rat 4.7 pIC50 = 4.7 Functional
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 94685 1 None -1 2 Rat 4.7 pIC50 = 4.7 Functional
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 62766 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 62766 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 139052 0 None - 1 Rat 5.7 pIC50 = 5.7 Functional
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 139052 0 None - 1 Rat 5.7 pIC50 = 5.7 Functional
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 139052 0 None - 1 Rat 5.7 pIC50 = 5.7 Functional
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 139052 0 None - 1 Rat 5.7 pIC50 = 5.7 Functional
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 62773 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 62773 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 197288 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
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 197288 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
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 133048 0 None 2 2 Human 7.7 pIC50 = 7.7 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133048 0 None 2 2 Human 7.7 pIC50 = 7.7 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 124230 0 None 12 2 Human 7.7 pIC50 = 7.7 Functional
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 124230 0 None 12 2 Human 7.7 pIC50 = 7.7 Functional
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 124255 0 None 22 2 Human 7.7 pIC50 = 7.7 Functional
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 124255 0 None 22 2 Human 7.7 pIC50 = 7.7 Functional
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 175551 0 None 4 2 Human 6.7 pIC50 = 6.7 Functional
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 175551 0 None 4 2 Human 6.7 pIC50 = 6.7 Functional
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 154624 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 154624 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 133110 0 None -24 2 Human 6.7 pIC50 = 6.7 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133110 0 None -24 2 Human 6.7 pIC50 = 6.7 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 125120 0 None -23 2 Human 5.7 pIC50 = 5.7 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 125120 0 None -23 2 Human 5.7 pIC50 = 5.7 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133056 0 None -8 2 Human 5.7 pIC50 = 5.7 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133056 0 None -8 2 Human 5.7 pIC50 = 5.7 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 114344 3 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 114344 3 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 114346 3 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 114346 3 None - 1 Human 6.7 pIC50 = 6.7 Functional
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 89087 0 None -48 2 Human 5.7 pIC50 = 5.7 Functional
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 89087 0 None -48 2 Human 5.7 pIC50 = 5.7 Functional
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 89087 0 None -48 2 Human 5.7 pIC50 = 5.7 Functional
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 139189 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
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 139189 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
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 139012 0 None - 1 Rat 5.7 pIC50 = 5.7 Functional
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 139012 0 None - 1 Rat 5.7 pIC50 = 5.7 Functional
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 139012 0 None - 1 Rat 5.7 pIC50 = 5.7 Functional
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 139012 0 None - 1 Rat 5.7 pIC50 = 5.7 Functional
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 139189 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
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 139189 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
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 196590 2 None - 1 Rat 4.7 pIC50 = 4.7 Functional
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 196590 2 None - 1 Rat 4.7 pIC50 = 4.7 Functional
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 92352 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
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 92352 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
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 125104 0 None -28 2 Human 6.7 pIC50 = 6.7 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 125104 0 None -28 2 Human 6.7 pIC50 = 6.7 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 54709 16 None - 1 Human 7.6 pIC50 = 7.6 Functional
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 54709 16 None - 1 Human 7.6 pIC50 = 7.6 Functional
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 85152 0 None 1 3 Human 7.6 pIC50 = 7.6 Functional
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 85152 0 None 1 3 Human 7.6 pIC50 = 7.6 Functional
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 154574 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
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 154574 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
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 197758 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
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 197758 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
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 94718 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
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 94718 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
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 125129 0 None -19 2 Human 5.6 pIC50 = 5.6 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 125129 0 None -19 2 Human 5.6 pIC50 = 5.6 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133057 0 None -66 2 Human 5.6 pIC50 = 5.6 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133057 0 None -66 2 Human 5.6 pIC50 = 5.6 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 94942 0 None - 1 Rat 4.6 pIC50 = 4.6 Functional
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 94942 0 None - 1 Rat 4.6 pIC50 = 4.6 Functional
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 139055 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
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 139055 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
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 139123 0 None 8 2 Rat 6.6 pIC50 = 6.6 Functional
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 139123 0 None 8 2 Rat 6.6 pIC50 = 6.6 Functional
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 139055 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
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 139055 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
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 139123 0 None 8 2 Rat 6.6 pIC50 = 6.6 Functional
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 139123 0 None 8 2 Rat 6.6 pIC50 = 6.6 Functional
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 125103 0 None -2344 2 Human 5.6 pIC50 = 5.6 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 125103 0 None -2344 2 Human 5.6 pIC50 = 5.6 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 89094 0 None -8 2 Human 6.6 pIC50 = 6.6 Functional
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 89094 0 None -8 2 Human 6.6 pIC50 = 6.6 Functional
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 89094 0 None -8 2 Human 6.6 pIC50 = 6.6 Functional
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 118922 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
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 118922 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
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 166507 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
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 166507 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
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 195782 14 None - 1 Rat 4.6 pIC50 = 4.6 Functional
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 195782 14 None - 1 Rat 4.6 pIC50 = 4.6 Functional
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 196033 20 None - 1 Rat 4.6 pIC50 = 4.6 Functional
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 196033 20 None - 1 Rat 4.6 pIC50 = 4.6 Functional
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 91039 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
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 91039 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
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 83813 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
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 83813 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
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 189203 0 None -2 3 Mouse 7.6 pIC50 = 7.6 Functional
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 189203 0 None -2 3 Mouse 7.6 pIC50 = 7.6 Functional
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 88744 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
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 88744 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
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 93601 0 None 15 2 Human 6.6 pIC50 = 6.6 Functional
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 93601 0 None 15 2 Human 6.6 pIC50 = 6.6 Functional
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 93925 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
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 93925 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
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 197216 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
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 197216 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
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 133115 0 None -169 2 Human 5.6 pIC50 = 5.6 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133115 0 None -169 2 Human 5.6 pIC50 = 5.6 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 62669 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
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 62669 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
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 93770 13 None 39 2 Human 6.6 pIC50 = 6.6 Functional
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 93770 13 None 39 2 Human 6.6 pIC50 = 6.6 Functional
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 91039 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
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 91039 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
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 139031 0 None 10 2 Rat 6.6 pIC50 = 6.6 Functional
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 139031 0 None 10 2 Rat 6.6 pIC50 = 6.6 Functional
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 118911 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
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 118911 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
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 91051 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
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 91051 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
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 91051 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
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 91051 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
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 139031 0 None 10 2 Rat 6.6 pIC50 = 6.6 Functional
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 139031 0 None 10 2 Rat 6.6 pIC50 = 6.6 Functional
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 140338 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
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 140338 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
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 198369 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
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 198369 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
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 94637 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
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 94637 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
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 41 None 1 3 Human 4.6 pIC50 = 4.6 Functional
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 41 None 1 3 Human 4.6 pIC50 = 4.6 Functional
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 41 None 1 3 Human 4.6 pIC50 = 4.6 Functional
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 94661 0 None 3 2 Rat 4.6 pIC50 = 4.6 Functional
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 94661 0 None 3 2 Rat 4.6 pIC50 = 4.6 Functional
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 154763 7 None -13 2 Rat 4.6 pIC50 = 4.6 Functional
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 154763 7 None -13 2 Rat 4.6 pIC50 = 4.6 Functional
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 46313 10 None - 1 Human 4.6 pIC50 = 4.6 Functional
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 46313 10 None - 1 Human 4.6 pIC50 = 4.6 Functional
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 41 None 1 3 Human 4.6 pIC50 = 4.6 Functional
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 41 None 1 3 Human 4.6 pIC50 = 4.6 Functional
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 41 None 1 3 Human 4.6 pIC50 = 4.6 Functional
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 137543 0 None 1 2 Human 6.6 pIC50 = 6.6 Functional
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 137543 0 None 1 2 Human 6.6 pIC50 = 6.6 Functional
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 75427 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
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 75427 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
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 75562 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
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 75562 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
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 91032 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
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 91032 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
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 114349 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
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 114349 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
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 91032 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
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 91032 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
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 141911 0 None 1 2 Human 7.6 pIC50 = 7.6 Functional
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 141911 0 None 1 2 Human 7.6 pIC50 = 7.6 Functional
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 124231 0 None 10 2 Human 7.6 pIC50 = 7.6 Functional
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 124231 0 None 10 2 Human 7.6 pIC50 = 7.6 Functional
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 24 None 1 4 Rat 5.6 pIC50 = 5.6 Functional
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 24 None 1 4 Rat 5.6 pIC50 = 5.6 Functional
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 24 None 1 4 Rat 5.6 pIC50 = 5.6 Functional
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 154363 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
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 154363 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
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 125097 0 None -109 2 Human 5.6 pIC50 = 5.6 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 125097 0 None -109 2 Human 5.6 pIC50 = 5.6 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 91050 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
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 91050 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
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 91050 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
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 91050 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
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 139130 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
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 139130 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
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 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
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 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
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 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
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 70989 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
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 70989 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
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 133016 0 None 3 2 Human 7.6 pIC50 = 7.6 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133016 0 None 3 2 Human 7.6 pIC50 = 7.6 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 124232 0 None 9 2 Human 7.6 pIC50 = 7.6 Functional
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 124232 0 None 9 2 Human 7.6 pIC50 = 7.6 Functional
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 122196 0 None -301 2 Rat 6.6 pIC50 = 6.6 Functional
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 122196 0 None -301 2 Rat 6.6 pIC50 = 6.6 Functional
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 139130 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
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 139130 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
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 83820 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
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 83820 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
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 89076 0 None -28 2 Human 6.6 pIC50 = 6.6 Functional
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 89076 0 None -28 2 Human 6.6 pIC50 = 6.6 Functional
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 89076 0 None -28 2 Human 6.6 pIC50 = 6.6 Functional
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 9 None - 1 Human 7.6 pIC50 = 7.6 Functional
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 9 None - 1 Human 7.6 pIC50 = 7.6 Functional
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 9 None - 1 Human 7.6 pIC50 = 7.6 Functional
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 124228 0 None 16 2 Human 7.5 pIC50 = 7.5 Functional
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 124228 0 None 16 2 Human 7.5 pIC50 = 7.5 Functional
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 124258 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
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 124258 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
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 133032 0 None -2 2 Human 5.6 pIC50 = 5.6 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133032 0 None -2 2 Human 5.6 pIC50 = 5.6 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 142082 10 None 1 2 Human 6.6 pIC50 = 6.6 Functional
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 142082 10 None 1 2 Human 6.6 pIC50 = 6.6 Functional
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 118913 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
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 118913 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
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 195849 2 None - 1 Rat 4.6 pIC50 = 4.6 Functional
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 195849 2 None - 1 Rat 4.6 pIC50 = 4.6 Functional
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 152305 0 None - 1 Rat 5.5 pIC50 = 5.5 Functional
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 152305 0 None - 1 Rat 5.5 pIC50 = 5.5 Functional
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 125125 0 None -144 2 Human 6.5 pIC50 = 6.5 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 125125 0 None -144 2 Human 6.5 pIC50 = 6.5 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 176832 0 None -5 3 Mouse 6.5 pIC50 = 6.5 Functional
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 176832 0 None -5 3 Mouse 6.5 pIC50 = 6.5 Functional
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 118916 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
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 118916 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
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 92022 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
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 92022 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
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 92022 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
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 92022 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
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 195633 20 None - 1 Rat 5.5 pIC50 = 5.5 Functional
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 195633 20 None - 1 Rat 5.5 pIC50 = 5.5 Functional
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 105605 0 None -2041 2 Human 4.5 pIC50 = 4.5 Functional
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 105605 0 None -2041 2 Human 4.5 pIC50 = 4.5 Functional
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 62762 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
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 62762 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
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 83701 0 None 3311 2 Human 8.5 pIC50 = 8.5 Functional
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 83701 0 None 3311 2 Human 8.5 pIC50 = 8.5 Functional
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 83810 0 None 3311 2 Human 8.5 pIC50 = 8.5 Functional
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 83810 0 None 3311 2 Human 8.5 pIC50 = 8.5 Functional
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 14 None 1 4 Human 8.5 pIC50 = 8.5 Functional
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 14 None 1 4 Human 8.5 pIC50 = 8.5 Functional
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 14 None 1 4 Human 8.5 pIC50 = 8.5 Functional
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 14 None 1 4 Human 8.5 pIC50 = 8.5 Functional
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 14 None 1 4 Human 8.5 pIC50 = 8.5 Functional
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 14 None 1 4 Human 8.5 pIC50 = 8.5 Functional
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 71031 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
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 71031 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
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 14 None 1 4 Human 8.5 pIC50 = 8.5 Functional
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 14 None 1 4 Human 8.5 pIC50 = 8.5 Functional
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 14 None 1 4 Human 8.5 pIC50 = 8.5 Functional
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 0 None 1 2 Human 8.5 pIC50 = 8.5 Functional
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 0 None 1 2 Human 8.5 pIC50 = 8.5 Functional
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 0 None 1 2 Human 8.5 pIC50 = 8.5 Functional
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 6 None - 1 Rat 8.5 pIC50 = 8.5 Functional
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 6 None - 1 Rat 8.5 pIC50 = 8.5 Functional
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 6 None - 1 Rat 8.5 pIC50 = 8.5 Functional
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 6 None - 1 Rat 8.5 pIC50 = 8.5 Functional
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 8474 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
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 8474 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
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 70980 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
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 70980 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
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 34 None 1 4 Mouse 8.5 pIC50 = 8.5 Functional
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 34 None 1 4 Mouse 8.5 pIC50 = 8.5 Functional
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 34 None 1 4 Mouse 8.5 pIC50 = 8.5 Functional
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 198514 1 None 331 2 Human 8.5 pIC50 = 8.5 Functional
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 198514 1 None 331 2 Human 8.5 pIC50 = 8.5 Functional
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 174792 0 None 2 3 Mouse 8.5 pIC50 = 8.5 Functional
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 174792 0 None 2 3 Mouse 8.5 pIC50 = 8.5 Functional
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 70996 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
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 70996 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
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 40 None 1819 2 Human 8.5 pIC50 = 8.5 Functional
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 40 None 1819 2 Human 8.5 pIC50 = 8.5 Functional
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 40 None 1819 2 Human 8.5 pIC50 = 8.5 Functional
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 197255 0 None 776 2 Human 8.4 pIC50 = 8.4 Functional
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 197255 0 None 776 2 Human 8.4 pIC50 = 8.4 Functional
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 197255 0 None 776 2 Human 8.4 pIC50 = 8.4 Functional
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 33 None 1 2 Rat 8.4 pIC50 = 8.4 Functional
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 33 None 1 2 Rat 8.4 pIC50 = 8.4 Functional
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 33 None 1 2 Rat 8.4 pIC50 = 8.4 Functional
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 196939 1 None 2454 2 Human 8.4 pIC50 = 8.4 Functional
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 196939 1 None 2454 2 Human 8.4 pIC50 = 8.4 Functional
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 62746 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
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 62746 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
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 62763 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
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 62763 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
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 70977 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
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 70977 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
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 83705 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
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 83705 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
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 150604 3 None - 1 Human 7.5 pIC50 = 7.5 Functional
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 150604 3 None - 1 Human 7.5 pIC50 = 7.5 Functional
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 197094 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
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 197094 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
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 188078 1 None - 1 Human 6.5 pIC50 = 6.5 Functional
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 188078 1 None - 1 Human 6.5 pIC50 = 6.5 Functional
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 94687 0 None - 1 Rat 5.5 pIC50 = 5.5 Functional
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 94687 0 None - 1 Rat 5.5 pIC50 = 5.5 Functional
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 195831 8 None - 1 Rat 4.5 pIC50 = 4.5 Functional
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 195831 8 None - 1 Rat 4.5 pIC50 = 4.5 Functional
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 94636 16 None -6 3 Rat 4.5 pIC50 = 4.5 Functional
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 94636 16 None -6 3 Rat 4.5 pIC50 = 4.5 Functional
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 133020 0 None -39 2 Human 5.5 pIC50 = 5.5 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133020 0 None -39 2 Human 5.5 pIC50 = 5.5 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 105592 13 None -12022 2 Human 4.5 pIC50 = 4.5 Functional
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 105592 13 None -12022 2 Human 4.5 pIC50 = 4.5 Functional
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 144149 0 None 1 2 Human 6.5 pIC50 = 6.5 Functional
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 144149 0 None 1 2 Human 6.5 pIC50 = 6.5 Functional
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 118924 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
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 118924 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
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 71040 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
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 71040 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
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 176808 0 None -1 3 Mouse 7.5 pIC50 = 7.5 Functional
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 176808 0 None -1 3 Mouse 7.5 pIC50 = 7.5 Functional
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 133068 0 None -8 2 Human 5.5 pIC50 = 5.5 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133068 0 None -8 2 Human 5.5 pIC50 = 5.5 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 89093 0 None -85 2 Human 5.5 pIC50 = 5.5 Functional
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 89093 0 None -85 2 Human 5.5 pIC50 = 5.5 Functional
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 89093 0 None -85 2 Human 5.5 pIC50 = 5.5 Functional
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 93304 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
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 93304 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
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 62774 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
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 62774 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
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 118918 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
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 118918 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
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 75033 0 None - 1 Rat 5.5 pIC50 = 5.5 Functional
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 75033 0 None - 1 Rat 5.5 pIC50 = 5.5 Functional
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 75924 0 None - 1 Rat 5.5 pIC50 = 5.5 Functional
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 75924 0 None - 1 Rat 5.5 pIC50 = 5.5 Functional
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 73212 1 None -18 3 Human 7.5 pIC50 = 7.5 Functional
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 73212 1 None -18 3 Human 7.5 pIC50 = 7.5 Functional
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 18301 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
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 18301 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
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 85067 0 None 1 2 Human 7.5 pIC50 = 7.5 Functional
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 85067 0 None 1 2 Human 7.5 pIC50 = 7.5 Functional
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 133070 0 None -5 2 Human 5.5 pIC50 = 5.5 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133070 0 None -5 2 Human 5.5 pIC50 = 5.5 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133124 0 None -457 2 Human 5.5 pIC50 = 5.5 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133124 0 None -457 2 Human 5.5 pIC50 = 5.5 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 8485 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
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 8485 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
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 62761 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
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 62761 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
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 197256 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
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 197256 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
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 141831 0 None 5 2 Rat 7.5 pIC50 = 7.5 Functional
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 141831 0 None 5 2 Rat 7.5 pIC50 = 7.5 Functional
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 125108 0 None -660 2 Human 5.5 pIC50 = 5.5 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 125108 0 None -660 2 Human 5.5 pIC50 = 5.5 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 125127 0 None -186 2 Human 5.5 pIC50 = 5.5 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 125127 0 None -186 2 Human 5.5 pIC50 = 5.5 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 124260 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
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 124260 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
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 125111 0 None -123 2 Human 5.5 pIC50 = 5.5 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 125111 0 None -123 2 Human 5.5 pIC50 = 5.5 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 84998 0 None 1 2 Human 6.5 pIC50 = 6.5 Functional
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 84998 0 None 1 2 Human 6.5 pIC50 = 6.5 Functional
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 139040 0 None 10 2 Rat 6.5 pIC50 = 6.5 Functional
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 139040 0 None 10 2 Rat 6.5 pIC50 = 6.5 Functional
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 71037 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
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 71037 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
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 124233 0 None 19 2 Human 7.5 pIC50 = 7.5 Functional
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 124233 0 None 19 2 Human 7.5 pIC50 = 7.5 Functional
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 124247 0 None 32 2 Human 7.5 pIC50 = 7.5 Functional
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 124247 0 None 32 2 Human 7.5 pIC50 = 7.5 Functional
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 125121 0 None -47 2 Human 5.5 pIC50 = 5.5 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 125121 0 None -47 2 Human 5.5 pIC50 = 5.5 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133052 0 None -107 2 Human 5.5 pIC50 = 5.5 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133052 0 None -107 2 Human 5.5 pIC50 = 5.5 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 33 None -1 3 Human 5.5 pIC50 = 5.5 Functional
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 33 None -1 3 Human 5.5 pIC50 = 5.5 Functional
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 33 None -1 3 Human 5.5 pIC50 = 5.5 Functional
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 139040 0 None 10 2 Rat 6.5 pIC50 = 6.5 Functional
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 139040 0 None 10 2 Rat 6.5 pIC50 = 6.5 Functional
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 91035 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
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 91035 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
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 91035 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
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 91035 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
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 70985 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
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 70985 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
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 133042 0 None -5 2 Human 7.5 pIC50 = 7.5 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133042 0 None -5 2 Human 7.5 pIC50 = 7.5 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 93603 0 None 27 2 Human 6.5 pIC50 = 6.5 Functional
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 93603 0 None 27 2 Human 6.5 pIC50 = 6.5 Functional
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 133028 0 None -1 2 Human 5.5 pIC50 = 5.5 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133028 0 None -1 2 Human 5.5 pIC50 = 5.5 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 105601 0 None -1548 2 Human 4.5 pIC50 = 4.5 Functional
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 105601 0 None -1548 2 Human 4.5 pIC50 = 4.5 Functional
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 62776 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
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 62776 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
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 91044 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
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 91044 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
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 92024 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
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 92024 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
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 91044 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
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 91044 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
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 92024 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
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 92024 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
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 84847 0 None 1 3 Human 7.4 pIC50 = 7.4 Functional
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 84847 0 None 1 3 Human 7.4 pIC50 = 7.4 Functional
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 90220 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
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 90220 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
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 114335 3 None - 1 Human 6.4 pIC50 = 6.4 Functional
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 114335 3 None - 1 Human 6.4 pIC50 = 6.4 Functional
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 166600 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
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 166600 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
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 133101 0 None -114 2 Human 5.4 pIC50 = 5.4 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133101 0 None -114 2 Human 5.4 pIC50 = 5.4 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 124245 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
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 124245 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
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 73220 0 None 169 2 Human 7.4 pIC50 = 7.4 Functional
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 73220 0 None 169 2 Human 7.4 pIC50 = 7.4 Functional
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 143494 0 None 1 2 Human 7.4 pIC50 = 7.4 Functional
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 143494 0 None 1 2 Human 7.4 pIC50 = 7.4 Functional
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 175165 0 None 4 3 Human 7.4 pIC50 = 7.4 Functional
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 175165 0 None 4 3 Human 7.4 pIC50 = 7.4 Functional
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 176761 0 None -2 3 Mouse 7.4 pIC50 = 7.4 Functional
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 176761 0 None -2 3 Mouse 7.4 pIC50 = 7.4 Functional
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 122200 0 None -13 2 Rat 7.4 pIC50 = 7.4 Functional
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 122200 0 None -13 2 Rat 7.4 pIC50 = 7.4 Functional
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 166000 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
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 166000 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
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 197257 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
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 197257 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
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 196188 13 None - 1 Rat 4.4 pIC50 = 4.4 Functional
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 196188 13 None - 1 Rat 4.4 pIC50 = 4.4 Functional
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 89065 0 None -10 2 Human 6.4 pIC50 = 6.4 Functional
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 89065 0 None -10 2 Human 6.4 pIC50 = 6.4 Functional
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 89065 0 None -10 2 Human 6.4 pIC50 = 6.4 Functional
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 5863 13 None -1 2 Rat 6.4 pIC50 = 6.4 Functional
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 5863 13 None -1 2 Rat 6.4 pIC50 = 6.4 Functional
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 91037 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
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 91037 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
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 74432 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
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 74432 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
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 75251 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
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 75251 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
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 139808 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
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 139808 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
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 91037 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
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 91037 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
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 87835 0 None - 1 Rat 5.4 pIC50 = 5.4 Functional
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 87835 0 None - 1 Rat 5.4 pIC50 = 5.4 Functional
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 83825 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
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 83825 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
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 85224 0 None 1 3 Human 8.4 pIC50 = 8.4 Functional
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 85224 0 None 1 3 Human 8.4 pIC50 = 8.4 Functional
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 62659 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
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 62659 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
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 71032 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
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 71032 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
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 62754 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
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 62754 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
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 70970 0 None 257 2 Human 8.3 pIC50 = 8.3 Functional
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 70970 0 None 257 2 Human 8.3 pIC50 = 8.3 Functional
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 198823 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
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 198823 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
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 89957 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
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 89957 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
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 94715 0 None - 1 Rat 5.4 pIC50 = 5.4 Functional
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 94715 0 None - 1 Rat 5.4 pIC50 = 5.4 Functional
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 170252 36 None 1 2 Human 4.4 pIC50 = 4.4 Functional
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 170252 36 None 1 2 Human 4.4 pIC50 = 4.4 Functional
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 35 None -15 4 Human 4.4 pIC50 = 4.4 Functional
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 35 None -15 4 Human 4.4 pIC50 = 4.4 Functional
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 35 None -15 4 Human 4.4 pIC50 = 4.4 Functional
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 18975 26 None - 1 Human 4.4 pIC50 = 4.4 Functional
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 18975 26 None - 1 Human 4.4 pIC50 = 4.4 Functional
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 125119 0 None -15 2 Human 6.4 pIC50 = 6.4 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 125119 0 None -15 2 Human 6.4 pIC50 = 6.4 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 136827 0 None 1 3 Human 6.4 pIC50 = 6.4 Functional
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 136827 0 None 1 3 Human 6.4 pIC50 = 6.4 Functional
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 114334 3 None - 1 Human 6.4 pIC50 = 6.4 Functional
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 114334 3 None - 1 Human 6.4 pIC50 = 6.4 Functional
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 114144 3 None - 1 Human 6.4 pIC50 = 6.4 Functional
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 114144 3 None - 1 Human 6.4 pIC50 = 6.4 Functional
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 149745 0 None - 1 Rat 5.4 pIC50 = 5.4 Functional
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 149745 0 None - 1 Rat 5.4 pIC50 = 5.4 Functional
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 0 None -20 2 Human 6.4 pIC50 = 6.4 Functional
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 0 None -20 2 Human 6.4 pIC50 = 6.4 Functional
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 0 None -20 2 Human 6.4 pIC50 = 6.4 Functional
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 18120 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
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 18120 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
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 85039 0 None 1 2 Human 7.4 pIC50 = 7.4 Functional
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 85039 0 None 1 2 Human 7.4 pIC50 = 7.4 Functional
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 125110 0 None -40 2 Human 7.4 pIC50 = 7.4 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 125110 0 None -40 2 Human 7.4 pIC50 = 7.4 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 154995 0 None - 1 Rat 4.4 pIC50 = 4.4 Functional
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 154995 0 None - 1 Rat 4.4 pIC50 = 4.4 Functional
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 91033 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
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 91033 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
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 91033 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
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 91033 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
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 133083 0 None -123 2 Human 5.4 pIC50 = 5.4 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133083 0 None -123 2 Human 5.4 pIC50 = 5.4 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 62666 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
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 62666 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
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 9 None -1 3 Human 7.4 pIC50 = 7.4 Functional
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 9 None -1 3 Human 7.4 pIC50 = 7.4 Functional
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 9 None -1 3 Human 7.4 pIC50 = 7.4 Functional
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 124229 0 None 8 2 Human 7.4 pIC50 = 7.4 Functional
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 124229 0 None 8 2 Human 7.4 pIC50 = 7.4 Functional
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 78522 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
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 78522 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
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 51 None -1 4 Human 5.4 pIC50 = 5.4 Functional
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 51 None -1 4 Human 5.4 pIC50 = 5.4 Functional
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 51 None -1 4 Human 5.4 pIC50 = 5.4 Functional
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 51 None -1 4 Human 5.4 pIC50 = 5.4 Functional
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 51 None -1 4 Human 5.4 pIC50 = 5.4 Functional
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 118908 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
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 118908 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
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 85103 0 None 1 3 Human 7.4 pIC50 = 7.4 Functional
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 85103 0 None 1 3 Human 7.4 pIC50 = 7.4 Functional
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 154599 12 None - 1 Rat 6.4 pIC50 = 6.4 Functional
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 154599 12 None - 1 Rat 6.4 pIC50 = 6.4 Functional
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 146389 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
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 146389 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
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 148955 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
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 148955 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
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 122202 0 None -562 2 Rat 6.4 pIC50 = 6.4 Functional
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 122202 0 None -562 2 Rat 6.4 pIC50 = 6.4 Functional
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 62770 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
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 62770 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
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 85133 0 None 1 2 Human 7.4 pIC50 = 7.4 Functional
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 85133 0 None 1 2 Human 7.4 pIC50 = 7.4 Functional
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 114345 3 None - 1 Human 7.4 pIC50 = 7.4 Functional
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 114345 3 None - 1 Human 7.4 pIC50 = 7.4 Functional
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 133065 0 None -316 2 Human 5.4 pIC50 = 5.4 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133065 0 None -316 2 Human 5.4 pIC50 = 5.4 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 94686 1 None -5 2 Rat 4.4 pIC50 = 4.4 Functional
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 94686 1 None -5 2 Rat 4.4 pIC50 = 4.4 Functional
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 89101 0 None -102 2 Human 5.3 pIC50 = 5.3 Functional
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 89101 0 None -102 2 Human 5.3 pIC50 = 5.3 Functional
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 89101 0 None -102 2 Human 5.3 pIC50 = 5.3 Functional
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 124242 0 None 25 2 Human 7.3 pIC50 = 7.3 Functional
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 124242 0 None 25 2 Human 7.3 pIC50 = 7.3 Functional
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 138982 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
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 138982 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
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 93307 0 None - 1 Rat 5.3 pIC50 = 5.3 Functional
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 93307 0 None - 1 Rat 5.3 pIC50 = 5.3 Functional
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 138982 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
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 138982 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
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 124249 0 None 1 2 Human 5.3 pIC50 = 5.3 Functional
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 124249 0 None 1 2 Human 5.3 pIC50 = 5.3 Functional
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 71028 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
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 71028 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
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 124226 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
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 124226 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
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 196864 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
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 196864 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
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 118917 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
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 118917 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
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 92032 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
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 92032 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
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 92032 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
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 92032 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
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 139116 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
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 139116 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
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 124236 0 None 20 2 Human 7.3 pIC50 = 7.3 Functional
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 124236 0 None 20 2 Human 7.3 pIC50 = 7.3 Functional
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 124237 0 None 22 2 Human 7.3 pIC50 = 7.3 Functional
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 124237 0 None 22 2 Human 7.3 pIC50 = 7.3 Functional
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 124243 0 None 18 2 Human 7.3 pIC50 = 7.3 Functional
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 124243 0 None 18 2 Human 7.3 pIC50 = 7.3 Functional
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 94790 14 None 12 2 Rat 5.3 pIC50 = 5.3 Functional
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 94790 14 None 12 2 Rat 5.3 pIC50 = 5.3 Functional
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 133039 0 None -60 2 Human 5.3 pIC50 = 5.3 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133039 0 None -60 2 Human 5.3 pIC50 = 5.3 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 142356 0 None 1 3 Human 6.3 pIC50 = 6.3 Functional
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 142356 0 None 1 3 Human 6.3 pIC50 = 6.3 Functional
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 139116 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
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 139116 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
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 166143 0 None -1 3 Human 7.3 pIC50 = 7.3 Functional
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 166143 0 None -1 3 Human 7.3 pIC50 = 7.3 Functional
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 175549 0 None 3 3 Human 7.3 pIC50 = 7.3 Functional
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 175549 0 None 3 3 Human 7.3 pIC50 = 7.3 Functional
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 197235 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
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 197235 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
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 198596 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
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 198596 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
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 125099 0 None -34 2 Human 6.3 pIC50 = 6.3 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 125099 0 None -34 2 Human 6.3 pIC50 = 6.3 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133017 0 None -24 2 Human 5.3 pIC50 = 5.3 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133017 0 None -24 2 Human 5.3 pIC50 = 5.3 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 114337 3 None - 1 Human 6.3 pIC50 = 6.3 Functional
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 114337 3 None - 1 Human 6.3 pIC50 = 6.3 Functional
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 83503 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
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 83503 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
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 83707 0 None 1995 2 Human 8.3 pIC50 = 8.3 Functional
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 83707 0 None 1995 2 Human 8.3 pIC50 = 8.3 Functional
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 83818 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
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 83818 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
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 84844 14 None 1 3 Human 8.3 pIC50 = 8.3 Functional
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 84844 14 None 1 3 Human 8.3 pIC50 = 8.3 Functional
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 85093 0 None 1 3 Human 8.3 pIC50 = 8.3 Functional
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 85093 0 None 1 3 Human 8.3 pIC50 = 8.3 Functional
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 70979 0 None 263 2 Human 8.3 pIC50 = 8.3 Functional
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 70979 0 None 263 2 Human 8.3 pIC50 = 8.3 Functional
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 14 None -1 4 Rat 8.3 pIC50 = 8.3 Functional
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 14 None -1 4 Rat 8.3 pIC50 = 8.3 Functional
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 14 None -1 4 Rat 8.3 pIC50 = 8.3 Functional
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 59 None - 1 Rat 8.3 pIC50 = 8.3 Functional
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 59 None - 1 Rat 8.3 pIC50 = 8.3 Functional
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 59 None - 1 Rat 8.3 pIC50 = 8.3 Functional
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 36 None 2 3 Human 8.3 pIC50 = 8.3 Functional
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 36 None 2 3 Human 8.3 pIC50 = 8.3 Functional
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 36 None 2 3 Human 8.3 pIC50 = 8.3 Functional
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 70971 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
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 70971 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
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 88687 0 None 117 2 Human 8.3 pIC50 = 8.3 Functional
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 88687 0 None 117 2 Human 8.3 pIC50 = 8.3 Functional
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 70987 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
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 70987 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
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 198904 1 None 416 2 Human 8.3 pIC50 = 8.3 Functional
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 198904 1 None 416 2 Human 8.3 pIC50 = 8.3 Functional
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 34 None -1 4 Human 8.3 pIC50 = 8.3 Functional
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 34 None -1 4 Human 8.3 pIC50 = 8.3 Functional
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 34 None -1 4 Human 8.3 pIC50 = 8.3 Functional
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 70973 0 None 1348 2 Human 8.2 pIC50 = 8.2 Functional
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 70973 0 None 1348 2 Human 8.2 pIC50 = 8.2 Functional
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 34 None -1 4 Human 8.2 pIC50 = 8.2 Functional
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 34 None -1 4 Human 8.2 pIC50 = 8.2 Functional
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 34 None -1 4 Human 8.2 pIC50 = 8.2 Functional
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 91988 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
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 91988 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
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 143239 0 None 1 3 Human 7.3 pIC50 = 7.3 Functional
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 143239 0 None 1 3 Human 7.3 pIC50 = 7.3 Functional
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 143538 0 None 1 2 Human 7.3 pIC50 = 7.3 Functional
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 143538 0 None 1 2 Human 7.3 pIC50 = 7.3 Functional
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 114340 3 None - 1 Human 7.3 pIC50 = 7.3 Functional
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 114340 3 None - 1 Human 7.3 pIC50 = 7.3 Functional
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 75857 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
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 75857 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
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 125105 0 None -46 2 Human 6.3 pIC50 = 6.3 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 125105 0 None -46 2 Human 6.3 pIC50 = 6.3 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 92025 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
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 92025 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
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 92028 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
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 92028 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
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 92028 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
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 92028 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
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 92025 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
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 92025 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
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 80231 0 None - 1 Rat 7.3 pIC50 = 7.3 Functional
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 80231 0 None - 1 Rat 7.3 pIC50 = 7.3 Functional
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 94788 0 None - 1 Rat 7.3 pIC50 = 7.3 Functional
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 94788 0 None - 1 Rat 7.3 pIC50 = 7.3 Functional
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 154765 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
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 154765 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
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 133033 0 None -1 2 Human 5.3 pIC50 = 5.3 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133033 0 None -1 2 Human 5.3 pIC50 = 5.3 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 62757 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
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 62757 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
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 133026 0 None -6 2 Human 6.3 pIC50 = 6.3 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133026 0 None -6 2 Human 6.3 pIC50 = 6.3 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 94638 0 None - 1 Rat 5.3 pIC50 = 5.3 Functional
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 94638 0 None - 1 Rat 5.3 pIC50 = 5.3 Functional
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 118921 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
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 118921 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
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 124239 0 None 10 2 Human 6.3 pIC50 = 6.3 Functional
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 124239 0 None 10 2 Human 6.3 pIC50 = 6.3 Functional
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 124252 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
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 124252 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
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 70984 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
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 70984 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
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 125124 0 None -12 2 Human 6.3 pIC50 = 6.3 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 125124 0 None -12 2 Human 6.3 pIC50 = 6.3 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 167413 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
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 167413 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
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 122205 0 None -301 2 Rat 6.3 pIC50 = 6.3 Functional
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 122205 0 None -301 2 Rat 6.3 pIC50 = 6.3 Functional
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 92020 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
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 92020 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
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 108274 0 None -446 7 Human 4.3 pIC50 = 4.3 Functional
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 108274 0 None -446 7 Human 4.3 pIC50 = 4.3 Functional
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 173566 0 None 3 3 Human 7.3 pIC50 = 7.3 Functional
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 173566 0 None 3 3 Human 7.3 pIC50 = 7.3 Functional
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 70991 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
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 70991 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
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 122204 0 None -52 2 Rat 6.3 pIC50 = 6.3 Functional
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 122204 0 None -52 2 Rat 6.3 pIC50 = 6.3 Functional
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 92020 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
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 92020 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
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 93308 0 None - 1 Rat 5.3 pIC50 = 5.3 Functional
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 93308 0 None - 1 Rat 5.3 pIC50 = 5.3 Functional
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 92035 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
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 92035 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
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 125126 0 None -29 2 Human 6.3 pIC50 = 6.3 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 125126 0 None -29 2 Human 6.3 pIC50 = 6.3 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 139073 0 None - 1 Rat 5.3 pIC50 = 5.3 Functional
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 139073 0 None - 1 Rat 5.3 pIC50 = 5.3 Functional
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 133125 0 None -186 2 Human 6.3 pIC50 = 6.3 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133125 0 None -186 2 Human 6.3 pIC50 = 6.3 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 92035 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
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 92035 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
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 139073 0 None - 1 Rat 5.3 pIC50 = 5.3 Functional
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 139073 0 None - 1 Rat 5.3 pIC50 = 5.3 Functional
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 152157 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
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 152157 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
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 176832 0 None 5 3 Human 7.2 pIC50 = 7.2 Functional
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 176832 0 None 5 3 Human 7.2 pIC50 = 7.2 Functional
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 114343 3 None - 1 Human 7.2 pIC50 = 7.2 Functional
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 114343 3 None - 1 Human 7.2 pIC50 = 7.2 Functional
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 198475 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
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 198475 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
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 163521 0 None -2 6 Human 5.2 pIC50 = 5.2 Functional
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 163521 0 None -2 6 Human 5.2 pIC50 = 5.2 Functional
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 207754 0 None -1995 6 Human 4.2 pIC50 = 4.2 Functional
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 207754 0 None -1995 6 Human 4.2 pIC50 = 4.2 Functional
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 198717 11 None - 1 Human 4.2 pIC50 = 4.2 Functional
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 198717 11 None - 1 Human 4.2 pIC50 = 4.2 Functional
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 114332 3 None - 1 Human 7.2 pIC50 = 7.2 Functional
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 114332 3 None - 1 Human 7.2 pIC50 = 7.2 Functional
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 189202 0 None -5 3 Mouse 7.2 pIC50 = 7.2 Functional
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 189202 0 None -5 3 Mouse 7.2 pIC50 = 7.2 Functional
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 114335 3 None - 1 Human 7.2 pIC50 = 7.2 Functional
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 114335 3 None - 1 Human 7.2 pIC50 = 7.2 Functional
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 53 None -1 2 Human 4.2 pIC50 = 4.2 Functional
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 53 None -1 2 Human 4.2 pIC50 = 4.2 Functional
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 53 None -1 2 Human 4.2 pIC50 = 4.2 Functional
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 133017 0 None -24 2 Human 6.2 pIC50 = 6.2 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133017 0 None -24 2 Human 6.2 pIC50 = 6.2 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133107 0 None -85 2 Human 5.2 pIC50 = 5.2 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133107 0 None -85 2 Human 5.2 pIC50 = 5.2 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 105604 0 None -1047 2 Human 5.2 pIC50 = 5.2 Functional
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 105604 0 None -1047 2 Human 5.2 pIC50 = 5.2 Functional
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 176831 0 None 2 3 Human 6.2 pIC50 = 6.2 Functional
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 176831 0 None 2 3 Human 6.2 pIC50 = 6.2 Functional
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 133093 0 None -489 2 Human 5.2 pIC50 = 5.2 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133093 0 None -489 2 Human 5.2 pIC50 = 5.2 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133114 0 None -158 2 Human 5.2 pIC50 = 5.2 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133114 0 None -158 2 Human 5.2 pIC50 = 5.2 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 91046 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
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 91046 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
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 0 None 1659 2 Human 8.2 pIC50 = 8.2 Functional
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 0 None 1659 2 Human 8.2 pIC50 = 8.2 Functional
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 0 None 1659 2 Human 8.2 pIC50 = 8.2 Functional
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 197811 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
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 197811 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
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 149875 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
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 149875 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
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 94972 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
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 94972 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
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 94750 7 None - 1 Rat 8.2 pIC50 = 8.2 Functional
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 94750 7 None - 1 Rat 8.2 pIC50 = 8.2 Functional
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 176895 0 None 2 3 Human 8.2 pIC50 = 8.2 Functional
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 176895 0 None 2 3 Human 8.2 pIC50 = 8.2 Functional
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 0 None 741 2 Human 8.2 pIC50 = 8.2 Functional
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 0 None 741 2 Human 8.2 pIC50 = 8.2 Functional
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 0 None 741 2 Human 8.2 pIC50 = 8.2 Functional
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 70981 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
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 70981 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
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 71035 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
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 71035 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
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 71039 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
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 71039 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
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 2 None - 1 Human 8.2 pIC50 = 8.2 Functional
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 2 None - 1 Human 8.2 pIC50 = 8.2 Functional
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 2 None - 1 Human 8.2 pIC50 = 8.2 Functional
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 62658 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
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 62658 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
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 62765 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
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 62765 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
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 62661 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
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 62661 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
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 62656 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
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 62656 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
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 83819 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
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 83819 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
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 118914 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
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 118914 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
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 105985 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
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 105985 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
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 91046 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
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 91046 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
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 198415 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
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 198415 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
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 58819 2 None -1 3 Human 6.2 pIC50 = 6.2 Functional
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 58819 2 None -1 3 Human 6.2 pIC50 = 6.2 Functional
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 58819 2 None -1 3 Human 6.2 pIC50 = 6.2 Functional
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 58819 2 None -1 3 Human 6.2 pIC50 = 6.2 Functional
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 85046 0 None 1 2 Human 6.2 pIC50 = 6.2 Functional
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 85046 0 None 1 2 Human 6.2 pIC50 = 6.2 Functional
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 88645 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
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 88645 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
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 133111 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133111 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 125120 0 None -23 2 Human 5.2 pIC50 = 5.2 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 125120 0 None -23 2 Human 5.2 pIC50 = 5.2 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133078 0 None -239 2 Human 5.2 pIC50 = 5.2 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133078 0 None -239 2 Human 5.2 pIC50 = 5.2 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 91698 10 None -25 2 Human 4.2 pIC50 = 4.2 Functional
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 91698 10 None -25 2 Human 4.2 pIC50 = 4.2 Functional
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 89098 0 None -33 3 Human 6.2 pIC50 = 6.2 Functional
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 89098 0 None -33 3 Human 6.2 pIC50 = 6.2 Functional
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 89098 0 None -33 3 Human 6.2 pIC50 = 6.2 Functional
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 73214 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
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 73214 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
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 133108 0 None -22 2 Human 6.2 pIC50 = 6.2 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133108 0 None -22 2 Human 6.2 pIC50 = 6.2 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133067 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133067 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 112047 47 None - 1 Human 4.2 pIC50 = 4.2 Functional
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 112047 47 None - 1 Human 4.2 pIC50 = 4.2 Functional
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 139033 0 None - 1 Rat 5.2 pIC50 = 5.2 Functional
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 139033 0 None - 1 Rat 5.2 pIC50 = 5.2 Functional
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 62662 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
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 62662 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
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 114333 3 None - 1 Human 7.2 pIC50 = 7.2 Functional
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 114333 3 None - 1 Human 7.2 pIC50 = 7.2 Functional
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 114336 3 None - 1 Human 7.2 pIC50 = 7.2 Functional
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 114336 3 None - 1 Human 7.2 pIC50 = 7.2 Functional
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 125096 0 None -19 2 Human 6.2 pIC50 = 6.2 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 125096 0 None -19 2 Human 6.2 pIC50 = 6.2 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 33 None -1 3 Human 5.2 pIC50 = 5.2 Functional
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 33 None -1 3 Human 5.2 pIC50 = 5.2 Functional
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 33 None -1 3 Human 5.2 pIC50 = 5.2 Functional
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 91043 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
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 91043 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
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 139033 0 None - 1 Rat 5.2 pIC50 = 5.2 Functional
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 139033 0 None - 1 Rat 5.2 pIC50 = 5.2 Functional
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 114347 3 None - 1 Human 6.2 pIC50 = 6.2 Functional
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 114347 3 None - 1 Human 6.2 pIC50 = 6.2 Functional
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 91043 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
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 91043 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
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 92030 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
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 92030 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
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 73221 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
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 73221 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
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 124398 0 None -338 2 Human 6.2 pIC50 = 6.2 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 124398 0 None -338 2 Human 6.2 pIC50 = 6.2 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 92030 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
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 92030 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
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 114144 3 None - 1 Human 6.2 pIC50 = 6.2 Functional
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 114144 3 None - 1 Human 6.2 pIC50 = 6.2 Functional
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 8231 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
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 8231 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
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 70997 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
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 70997 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
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 86751 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
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 86751 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
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 133123 0 None -43 2 Human 6.2 pIC50 = 6.2 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133123 0 None -43 2 Human 6.2 pIC50 = 6.2 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 89102 0 None -12 2 Human 6.2 pIC50 = 6.2 Functional
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 89102 0 None -12 2 Human 6.2 pIC50 = 6.2 Functional
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 89102 0 None -12 2 Human 6.2 pIC50 = 6.2 Functional
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 198524 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
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 198524 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
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 139160 0 None 1 2 Rat 7.2 pIC50 = 7.2 Functional
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 139160 0 None 1 2 Rat 7.2 pIC50 = 7.2 Functional
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 139160 0 None 1 2 Rat 7.2 pIC50 = 7.2 Functional
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 139160 0 None 1 2 Rat 7.2 pIC50 = 7.2 Functional
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 133024 0 None -4 2 Human 6.2 pIC50 = 6.2 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133024 0 None -4 2 Human 6.2 pIC50 = 6.2 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133046 0 None -1 2 Human 5.2 pIC50 = 5.2 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133046 0 None -1 2 Human 5.2 pIC50 = 5.2 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 73216 0 None 22 2 Human 8.2 pIC50 = 8.2 Functional
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 73216 0 None 22 2 Human 8.2 pIC50 = 8.2 Functional
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 73219 0 None 102 2 Human 8.2 pIC50 = 8.2 Functional
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 73219 0 None 102 2 Human 8.2 pIC50 = 8.2 Functional
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 0 None 1412 2 Human 8.2 pIC50 = 8.2 Functional
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 0 None 1412 2 Human 8.2 pIC50 = 8.2 Functional
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 0 None 1412 2 Human 8.2 pIC50 = 8.2 Functional
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 83809 0 None 1412 2 Human 8.2 pIC50 = 8.2 Functional
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 83809 0 None 1412 2 Human 8.2 pIC50 = 8.2 Functional
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 83829 0 None 28 2 Human 8.2 pIC50 = 8.2 Functional
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 83829 0 None 28 2 Human 8.2 pIC50 = 8.2 Functional
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 175070 0 None -4 3 Human 8.2 pIC50 = 8.2 Functional
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 175070 0 None -4 3 Human 8.2 pIC50 = 8.2 Functional
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 174792 0 None -2 3 Human 8.1 pIC50 = 8.1 Functional
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 174792 0 None -2 3 Human 8.1 pIC50 = 8.1 Functional
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 62749 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
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 62749 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
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 71029 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
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 71029 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
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 83703 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
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 83703 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
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 55 None - 1 Human 5.2 pIC50 = 5.2 Functional
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 55 None - 1 Human 5.2 pIC50 = 5.2 Functional
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 55 None - 1 Human 5.2 pIC50 = 5.2 Functional
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 94789 13 None - 1 Rat 5.2 pIC50 = 5.2 Functional
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 94789 13 None - 1 Rat 5.2 pIC50 = 5.2 Functional
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 125101 0 None -2290 2 Human 5.2 pIC50 = 5.2 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 125101 0 None -2290 2 Human 5.2 pIC50 = 5.2 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 125068 0 None -354 2 Human 6.2 pIC50 = 6.2 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 125068 0 None -354 2 Human 6.2 pIC50 = 6.2 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 91034 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
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 91034 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
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 91047 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
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 91047 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
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 85153 0 None 1 2 Human 7.2 pIC50 = 7.2 Functional
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 85153 0 None 1 2 Human 7.2 pIC50 = 7.2 Functional
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 86723 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
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 86723 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
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 142344 0 None -1 2 Rat 7.2 pIC50 = 7.2 Functional
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 142344 0 None -1 2 Rat 7.2 pIC50 = 7.2 Functional
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 125132 0 None -117 2 Human 6.2 pIC50 = 6.2 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 125132 0 None -117 2 Human 6.2 pIC50 = 6.2 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 91034 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
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 91034 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
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 5503 2 None -7 2 Rat 6.2 pIC50 = 6.2 Functional
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 5503 2 None -7 2 Rat 6.2 pIC50 = 6.2 Functional
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 91047 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
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 91047 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
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 62753 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
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 62753 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
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 112522 0 None - 1 Human 4.1 pIC50 = 4.1 Functional
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 112522 0 None - 1 Human 4.1 pIC50 = 4.1 Functional
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 125082 0 None -44 2 Human 5.1 pIC50 = 5.1 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 125082 0 None -44 2 Human 5.1 pIC50 = 5.1 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 89058 0 None -24 2 Human 6.1 pIC50 = 6.1 Functional
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 89058 0 None -24 2 Human 6.1 pIC50 = 6.1 Functional
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 89058 0 None -24 2 Human 6.1 pIC50 = 6.1 Functional
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 114341 3 None - 1 Human 7.1 pIC50 = 7.1 Functional
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 114341 3 None - 1 Human 7.1 pIC50 = 7.1 Functional
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 114341 3 None - 1 Human 7.1 pIC50 = 7.1 Functional
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 114341 3 None - 1 Human 7.1 pIC50 = 7.1 Functional
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 195917 6 None - 1 Rat 6.1 pIC50 = 6.1 Functional
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 195917 6 None - 1 Rat 6.1 pIC50 = 6.1 Functional
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 154994 0 None - 1 Rat 5.1 pIC50 = 5.1 Functional
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 154994 0 None - 1 Rat 5.1 pIC50 = 5.1 Functional
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 114348 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
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 114348 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
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 71026 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
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 71026 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
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 139008 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
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 139008 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
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 124250 0 None 5 2 Human 6.1 pIC50 = 6.1 Functional
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 124250 0 None 5 2 Human 6.1 pIC50 = 6.1 Functional
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 139008 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
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 139008 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
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 85064 0 None 1 3 Human 7.1 pIC50 = 7.1 Functional
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 85064 0 None 1 3 Human 7.1 pIC50 = 7.1 Functional
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 93654 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
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 93654 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
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 154674 0 None - 1 Rat 5.1 pIC50 = 5.1 Functional
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 154674 0 None - 1 Rat 5.1 pIC50 = 5.1 Functional
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 133103 0 None -44 2 Human 6.1 pIC50 = 6.1 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133103 0 None -44 2 Human 6.1 pIC50 = 6.1 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 92023 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
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 92023 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
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 198869 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
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 198869 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
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 92023 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
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 92023 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
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 93924 9 None - 1 Human 7.1 pIC50 = 7.1 Functional
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 93924 9 None - 1 Human 7.1 pIC50 = 7.1 Functional
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 154764 0 None 630 2 Rat 7.1 pIC50 = 7.1 Functional
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 154764 0 None 630 2 Rat 7.1 pIC50 = 7.1 Functional
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 54 None -1047 14 Human 5.1 pIC50 = 5.1 Functional
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 54 None -1047 14 Human 5.1 pIC50 = 5.1 Functional
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 54 None -1047 14 Human 5.1 pIC50 = 5.1 Functional
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 54 None -1047 14 Human 5.1 pIC50 = 5.1 Functional
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 70986 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
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 70986 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
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 94914 0 None - 1 Rat 5.1 pIC50 = 5.1 Functional
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 94914 0 None - 1 Rat 5.1 pIC50 = 5.1 Functional
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 83828 0 None 1258 2 Human 8.1 pIC50 = 8.1 Functional
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 83828 0 None 1258 2 Human 8.1 pIC50 = 8.1 Functional
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 133040 0 None 11 2 Human 8.1 pIC50 = 8.1 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133040 0 None 11 2 Human 8.1 pIC50 = 8.1 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 70976 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
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 70976 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
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 62767 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
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 62767 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
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 70975 0 None 63 2 Human 8.1 pIC50 = 8.1 Functional
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 70975 0 None 63 2 Human 8.1 pIC50 = 8.1 Functional
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 62760 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
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 62760 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
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 198317 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
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 198317 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
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 150460 3 None - 1 Human 7.1 pIC50 = 7.1 Functional
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 150460 3 None - 1 Human 7.1 pIC50 = 7.1 Functional
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 93653 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
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 93653 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
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 133031 0 None 5 2 Human 6.1 pIC50 = 6.1 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133031 0 None 5 2 Human 6.1 pIC50 = 6.1 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 197109 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
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 197109 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
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 125071 0 None -407 2 Human 6.1 pIC50 = 6.1 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 125071 0 None -407 2 Human 6.1 pIC50 = 6.1 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 83702 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
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 83702 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
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 85053 0 None 11 2 Human 7.1 pIC50 = 7.1 Functional
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 85053 0 None 11 2 Human 7.1 pIC50 = 7.1 Functional
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 133119 0 None -66 2 Human 5.1 pIC50 = 5.1 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133119 0 None -66 2 Human 5.1 pIC50 = 5.1 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 198651 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
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 198651 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
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 139062 0 None 20 2 Rat 7.1 pIC50 = 7.1 Functional
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 139062 0 None 20 2 Rat 7.1 pIC50 = 7.1 Functional
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 92036 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
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 92036 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
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 92036 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
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 92036 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
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 85160 0 None 1 3 Human 7.1 pIC50 = 7.1 Functional
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 85160 0 None 1 3 Human 7.1 pIC50 = 7.1 Functional
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 139062 0 None 20 2 Rat 7.1 pIC50 = 7.1 Functional
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 139062 0 None 20 2 Rat 7.1 pIC50 = 7.1 Functional
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 62768 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
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 62768 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
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 70983 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
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 70983 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
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 92027 0 None 39 3 Human 7.1 pIC50 = 7.1 Functional
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 92027 0 None 39 3 Human 7.1 pIC50 = 7.1 Functional
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 92027 0 None 39 3 Human 7.1 pIC50 = 7.1 Functional
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 92027 0 None 39 3 Human 7.1 pIC50 = 7.1 Functional
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 196149 10 None - 1 Rat 5.1 pIC50 = 5.1 Functional
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 196149 10 None - 1 Rat 5.1 pIC50 = 5.1 Functional
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 85195 0 None 1 2 Human 5.1 pIC50 = 5.1 Functional
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 85195 0 None 1 2 Human 5.1 pIC50 = 5.1 Functional
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 83814 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
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 83814 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
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 18119 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
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 18119 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
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 142035 0 None 1 3 Human 7.1 pIC50 = 7.1 Functional
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 142035 0 None 1 3 Human 7.1 pIC50 = 7.1 Functional
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 71027 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
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 71027 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
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 71036 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
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 71036 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
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 198352 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
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 198352 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
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 44 None - 1 Human 5.1 pIC50 = 5.1 Functional
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 44 None - 1 Human 5.1 pIC50 = 5.1 Functional
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 44 None - 1 Human 5.1 pIC50 = 5.1 Functional
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 44 None - 1 Human 5.1 pIC50 = 5.1 Functional
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 44 None - 1 Human 5.1 pIC50 = 5.1 Functional
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 44 None - 1 Human 5.1 pIC50 = 5.1 Functional
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 138987 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
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 138987 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
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 124234 0 None 10 2 Human 7.1 pIC50 = 7.1 Functional
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 124234 0 None 10 2 Human 7.1 pIC50 = 7.1 Functional
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 125098 0 None -125 2 Human 6.1 pIC50 = 6.1 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 125098 0 None -125 2 Human 6.1 pIC50 = 6.1 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133066 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133066 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 87520 0 None -33 2 Human 6.1 pIC50 = 6.1 Functional
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 87520 0 None -33 2 Human 6.1 pIC50 = 6.1 Functional
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 138987 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
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 138987 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
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 73212 1 None -18 3 Human 8.1 pIC50 = 8.1 Functional
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 73212 1 None -18 3 Human 8.1 pIC50 = 8.1 Functional
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 73218 0 None 138 2 Human 8.1 pIC50 = 8.1 Functional
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 73218 0 None 138 2 Human 8.1 pIC50 = 8.1 Functional
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 83700 0 None 1122 2 Human 8.1 pIC50 = 8.1 Functional
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 83700 0 None 1122 2 Human 8.1 pIC50 = 8.1 Functional
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 83816 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
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 83816 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
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 85038 0 None 1 2 Human 8.1 pIC50 = 8.1 Functional
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 85038 0 None 1 2 Human 8.1 pIC50 = 8.1 Functional
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 73212 1 None -18 3 Human 8.1 pIC50 = 8.1 Functional
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 73212 1 None -18 3 Human 8.1 pIC50 = 8.1 Functional
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 167055 13 None 1047 2 Human 8.0 pIC50 = 8.0 Functional
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 167055 13 None 1047 2 Human 8.0 pIC50 = 8.0 Functional
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 167055 13 None 1047 2 Human 8.0 pIC50 = 8.0 Functional
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 167055 13 None 1047 2 Human 8.0 pIC50 = 8.0 Functional
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 167055 13 None 1047 2 Human 8.0 pIC50 = 8.0 Functional
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 167055 13 None 1047 2 Human 8.0 pIC50 = 8.0 Functional
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 62751 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
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 62751 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
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 189203 0 None 2 3 Human 8.0 pIC50 = 8.0 Functional
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 189203 0 None 2 3 Human 8.0 pIC50 = 8.0 Functional
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 89960 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
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 89960 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
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 71030 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
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 71030 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
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 93888 0 None 30 2 Human 7.0 pIC50 = 7.0 Functional
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 93888 0 None 30 2 Human 7.0 pIC50 = 7.0 Functional
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 73215 0 None -4 2 Human 7.0 pIC50 = 7.0 Functional
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 73215 0 None -4 2 Human 7.0 pIC50 = 7.0 Functional
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 86724 0 None - 1 Rat 7.0 pIC50 = 7.0 Functional
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 86724 0 None - 1 Rat 7.0 pIC50 = 7.0 Functional
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 133044 0 None -2 2 Human 7.0 pIC50 = 7.0 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133044 0 None -2 2 Human 7.0 pIC50 = 7.0 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 92031 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
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 92031 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
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 139045 0 None 24 2 Rat 7.0 pIC50 = 7.0 Functional
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 139045 0 None 24 2 Rat 7.0 pIC50 = 7.0 Functional
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 92031 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
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 92031 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
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 139045 0 None 24 2 Rat 7.0 pIC50 = 7.0 Functional
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 139045 0 None 24 2 Rat 7.0 pIC50 = 7.0 Functional
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 139167 0 None 35 2 Rat 7.0 pIC50 = 7.0 Functional
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 139167 0 None 35 2 Rat 7.0 pIC50 = 7.0 Functional
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 78521 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
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 78521 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
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 125091 0 None -177 2 Human 5.0 pIC50 = 5.0 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 125091 0 None -177 2 Human 5.0 pIC50 = 5.0 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 98861 0 None -2 2 Rat 4.0 pIC50 = 4.0 Functional
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 98861 0 None -2 2 Rat 4.0 pIC50 = 4.0 Functional
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 139167 0 None 35 2 Rat 7.0 pIC50 = 7.0 Functional
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 139167 0 None 35 2 Rat 7.0 pIC50 = 7.0 Functional
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 133023 0 None -2 2 Human 6.0 pIC50 = 6.0 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 133023 0 None -2 2 Human 6.0 pIC50 = 6.0 Functional
Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined 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 143565 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
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 143565 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
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 124246 0 None 52 2 Human 7.0 pIC50 = 7.0 Functional
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 124246 0 None 52 2 Human 7.0 pIC50 = 7.0 Functional
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 87519 0 None -478 2 Human 5.0 pIC50 = 5.0 Functional
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 87519 0 None -478 2 Human 5.0 pIC50 = 5.0 Functional
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 62755 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
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 62755 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
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 5476 0 None -7 2 Rat 6.0 pIC50 = 6.0 Functional
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 5476 0 None -7 2 Rat 6.0 pIC50 = 6.0 Functional
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 14 None - 1 Human 7.0 pIC50 = 7.0 Functional
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 14 None - 1 Human 7.0 pIC50 = 7.0 Functional
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 14 None - 1 Human 7.0 pIC50 = 7.0 Functional
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 91038 12 None - 1 Human 7.0 pIC50 = 7.0 Functional
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 91038 12 None - 1 Human 7.0 pIC50 = 7.0 Functional
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 91041 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
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 91041 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
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 137177 0 None 1 3 Human 7.0 pIC50 = 7.0 Functional
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 137177 0 None 1 3 Human 7.0 pIC50 = 7.0 Functional
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 197815 6 None - 1 Human 6.0 pIC50 = 6.0 Functional
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 197815 6 None - 1 Human 6.0 pIC50 = 6.0 Functional
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 93737 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
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 93737 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
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 91041 0 None - 1 Human 6.0 pIC50 = 6 Functional
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 91041 0 None - 1 Human 6.0 pIC50 = 6 Functional
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 137927 0 None 1 2 Human 7.0 pIC50 = 7 Functional
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 137927 0 None 1 2 Human 7.0 pIC50 = 7 Functional
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 91038 12 None - 1 Human 7.0 pIC50 = 7 Functional
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 91038 12 None - 1 Human 7.0 pIC50 = 7 Functional
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 91038 12 None - 1 Human 7.0 pIC50 = 7 Functional
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 91038 12 None - 1 Human 7.0 pIC50 = 7 Functional
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 62664 0 None - 1 Rat 9.7 pKi = 9.7 Functional
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 62664 0 None - 1 Rat 9.7 pKi = 9.7 Functional
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 62665 0 None - 1 Rat 9.4 pKi = 9.4 Functional
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 62665 0 None - 1 Rat 9.4 pKi = 9.4 Functional
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 70973 0 None - 2 Rat 9.4 pKi = 9.4 Functional
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 70973 0 None - 2 Rat 9.4 pKi = 9.4 Functional
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 1 None - 1 Rat 9.2 pKi = 9.2 Functional
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 1 None - 1 Rat 9.2 pKi = 9.2 Functional
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 1 None - 1 Rat 9.2 pKi = 9.2 Functional
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 62657 0 None - 1 Rat 9.2 pKi = 9.2 Functional
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 62657 0 None - 1 Rat 9.2 pKi = 9.2 Functional
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 62744 0 None - 1 Rat 9.2 pKi = 9.2 Functional
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 62744 0 None - 1 Rat 9.2 pKi = 9.2 Functional
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 62654 0 None - 1 Rat 9.0 pKi = 9.0 Functional
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 62654 0 None - 1 Rat 9.0 pKi = 9.0 Functional
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 62656 0 None - 1 Rat 9.0 pKi = 9.0 Functional
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 62656 0 None - 1 Rat 9.0 pKi = 9.0 Functional
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 62663 0 None - 1 Rat 8.9 pKi = 8.9 Functional
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 62663 0 None - 1 Rat 8.9 pKi = 8.9 Functional
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 62666 0 None - 1 Rat 8.8 pKi = 8.8 Functional
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 62666 0 None - 1 Rat 8.8 pKi = 8.8 Functional
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 62670 0 None - 1 Rat 8.8 pKi = 8.8 Functional
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 62670 0 None - 1 Rat 8.8 pKi = 8.8 Functional
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 70970 0 None - 2 Rat 8.7 pKi = 8.7 Functional
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 70970 0 None - 2 Rat 8.7 pKi = 8.7 Functional
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 70972 0 None - 1 Rat 8.7 pKi = 8.7 Functional
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 70972 0 None - 1 Rat 8.7 pKi = 8.7 Functional
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 179056 0 None - 0 Rat 8.0 pKi = 8 Functional
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 179056 0 None - 0 Rat 8.0 pKi = 8 Functional
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 62755 0 None - 1 Rat 6.0 pKi = 6 Functional
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 62755 0 None - 1 Rat 6.0 pKi = 6 Functional
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 110 None -741 17 Human 5.0 pKi = 5 Functional
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 110 None -741 17 Human 5.0 pKi = 5 Functional
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 110 None -741 17 Human 5.0 pKi = 5 Functional
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 110 None -741 17 Human 5.0 pKi = 5 Functional
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 110 None -741 17 Human 5.0 pKi = 5 Functional
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 110 None -741 17 Human 5.0 pKi = 5 Functional
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 110 None -741 17 Human 5.0 pKi = 5 Functional
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 161292 31 None - 0 Human 5.0 pKi = 5 Functional
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 161292 31 None - 0 Human 5.0 pKi = 5 Functional
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 179088 0 None - 0 Rat 7.0 pKi = 7 Functional
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 179088 0 None - 0 Rat 7.0 pKi = 7 Functional
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 178840 0 None - 0 Rat 7.0 pKi = 7.0 Functional
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 178840 0 None - 0 Rat 7.0 pKi = 7.0 Functional
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 62771 0 None - 1 Rat 7.0 pKi = 7.0 Functional
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 62771 0 None - 1 Rat 7.0 pKi = 7.0 Functional
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 70993 0 None - 1 Rat 7.0 pKi = 7.0 Functional
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 70993 0 None - 1 Rat 7.0 pKi = 7.0 Functional
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 93707 0 None - 0 Rat 6.0 pKi = 6.0 Functional
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 93707 0 None - 0 Rat 6.0 pKi = 6.0 Functional
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 93496 2 None - 0 Rat 8.0 pKi = 8.0 Functional
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 93496 2 None - 0 Rat 8.0 pKi = 8.0 Functional
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 178841 0 None - 0 Rat 8.0 pKi = 8.0 Functional
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 178841 0 None - 0 Rat 8.0 pKi = 8.0 Functional
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 70976 0 None - 1 Rat 8.0 pKi = 8.0 Functional
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 70976 0 None - 1 Rat 8.0 pKi = 8.0 Functional
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 70979 0 None - 2 Rat 8.0 pKi = 8.0 Functional
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 70979 0 None - 2 Rat 8.0 pKi = 8.0 Functional
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 67 None -11 6 Human 6.0 pKi = 6.0 Functional
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 67 None -11 6 Human 6.0 pKi = 6.0 Functional
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 67 None -11 6 Human 6.0 pKi = 6.0 Functional
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 67 None -11 6 Human 6.0 pKi = 6.0 Functional
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 67 None -11 6 Human 6.0 pKi = 6.0 Functional
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 67 None -11 6 Human 6.0 pKi = 6.0 Functional
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 189478 0 None - 0 Rat 6.9 pKi = 6.9 Functional
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 189478 0 None - 0 Rat 6.9 pKi = 6.9 Functional
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 70986 0 None - 1 Rat 6.9 pKi = 6.9 Functional
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 70986 0 None - 1 Rat 6.9 pKi = 6.9 Functional
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 70980 0 None - 1 Rat 7.9 pKi = 7.9 Functional
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 70980 0 None - 1 Rat 7.9 pKi = 7.9 Functional
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 71030 0 None - 1 Rat 7.9 pKi = 7.9 Functional
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 71030 0 None - 1 Rat 7.9 pKi = 7.9 Functional
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 93851 0 None - 0 Rat 5.9 pKi = 5.9 Functional
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 93851 0 None - 0 Rat 5.9 pKi = 5.9 Functional
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 153116 4 None - 0 Rat 5.9 pKi = 5.9 Functional
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 153116 4 None - 0 Rat 5.9 pKi = 5.9 Functional
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 170282 3 None - 0 Rat 6.9 pKi = 6.9 Functional
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 170282 3 None - 0 Rat 6.9 pKi = 6.9 Functional
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 189398 0 None - 0 Rat 6.9 pKi = 6.9 Functional
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 189398 0 None - 0 Rat 6.9 pKi = 6.9 Functional
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 62667 0 None - 1 Rat 7.9 pKi = 7.9 Functional
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 62667 0 None - 1 Rat 7.9 pKi = 7.9 Functional
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 62668 0 None - 1 Rat 7.9 pKi = 7.9 Functional
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 62668 0 None - 1 Rat 7.9 pKi = 7.9 Functional
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 70977 0 None - 1 Rat 7.9 pKi = 7.9 Functional
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 70977 0 None - 1 Rat 7.9 pKi = 7.9 Functional
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 70999 0 None - 1 Rat 7.9 pKi = 7.9 Functional
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 70999 0 None - 1 Rat 7.9 pKi = 7.9 Functional
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 71038 0 None - 1 Rat 7.9 pKi = 7.9 Functional
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 71038 0 None - 1 Rat 7.9 pKi = 7.9 Functional
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 0 None - 2 Rat 7.9 pKi = 7.9 Functional
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 0 None - 2 Rat 7.9 pKi = 7.9 Functional
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 0 None - 2 Rat 7.9 pKi = 7.9 Functional
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 70992 0 None - 1 Rat 6.9 pKi = 6.9 Functional
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 70992 0 None - 1 Rat 6.9 pKi = 6.9 Functional
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 62658 0 None - 1 Rat 7.9 pKi = 7.9 Functional
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 62658 0 None - 1 Rat 7.9 pKi = 7.9 Functional
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 62669 0 None - 1 Rat 7.9 pKi = 7.9 Functional
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 62669 0 None - 1 Rat 7.9 pKi = 7.9 Functional
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 147747 0 None - 0 Rat 7.9 pKi = 7.9 Functional
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 147747 0 None - 0 Rat 7.9 pKi = 7.9 Functional
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 179210 0 None - 0 Rat 7.9 pKi = 7.9 Functional
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 179210 0 None - 0 Rat 7.9 pKi = 7.9 Functional
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 70987 0 None - 1 Rat 7.9 pKi = 7.9 Functional
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 70987 0 None - 1 Rat 7.9 pKi = 7.9 Functional
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 0 None - 2 Rat 7.8 pKi = 7.8 Functional
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 0 None - 2 Rat 7.8 pKi = 7.8 Functional
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 0 None - 2 Rat 7.8 pKi = 7.8 Functional
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 188080 0 None - 0 Rat 5.9 pKi = 5.9 Functional
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 188080 0 None - 0 Rat 5.9 pKi = 5.9 Functional
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 93452 3 None - 0 Rat 7.8 pKi = 7.8 Functional
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 93452 3 None - 0 Rat 7.8 pKi = 7.8 Functional
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 141584 8 None - 0 Human 6.8 pKi = 6.8 Functional
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 141584 8 None - 0 Human 6.8 pKi = 6.8 Functional
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 70996 0 None - 1 Rat 7.8 pKi = 7.8 Functional
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 70996 0 None - 1 Rat 7.8 pKi = 7.8 Functional
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 62743 0 None - 1 Rat 6.8 pKi = 6.8 Functional
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 62743 0 None - 1 Rat 6.8 pKi = 6.8 Functional
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 171991 0 None - 0 Rat 6.8 pKi = 6.8 Functional
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 171991 0 None - 0 Rat 6.8 pKi = 6.8 Functional
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 206837 1 None - 0 Human 5.8 pKi = 5.8 Functional
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 206837 1 None - 0 Human 5.8 pKi = 5.8 Functional
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 178922 1 None - 0 Rat 5.8 pKi = 5.8 Functional
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 178922 1 None - 0 Rat 5.8 pKi = 5.8 Functional
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 169522 2 None - 0 Rat 7.8 pKi = 7.8 Functional
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 169522 2 None - 0 Rat 7.8 pKi = 7.8 Functional
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 0 None - 2 Rat 7.8 pKi = 7.8 Functional
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 0 None - 2 Rat 7.8 pKi = 7.8 Functional
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 0 None - 2 Rat 7.8 pKi = 7.8 Functional
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 178842 0 None - 0 Rat 6.8 pKi = 6.8 Functional
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 178842 0 None - 0 Rat 6.8 pKi = 6.8 Functional
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 93777 3 None - 0 Rat 6.8 pKi = 6.8 Functional
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 93777 3 None - 0 Rat 6.8 pKi = 6.8 Functional
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 62746 0 None - 1 Rat 7.8 pKi = 7.8 Functional
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 62746 0 None - 1 Rat 7.8 pKi = 7.8 Functional
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 70975 0 None - 2 Rat 7.8 pKi = 7.8 Functional
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 70975 0 None - 2 Rat 7.8 pKi = 7.8 Functional
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 70989 0 None - 1 Rat 7.8 pKi = 7.8 Functional
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 70989 0 None - 1 Rat 7.8 pKi = 7.8 Functional
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 187934 0 None - 0 Rat 6.7 pKi = 6.7 Functional
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 187934 0 None - 0 Rat 6.7 pKi = 6.7 Functional
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 70978 0 None - 1 Rat 7.7 pKi = 7.7 Functional
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 70978 0 None - 1 Rat 7.7 pKi = 7.7 Functional
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 71035 0 None - 1 Rat 7.7 pKi = 7.7 Functional
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 71035 0 None - 1 Rat 7.7 pKi = 7.7 Functional
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 188079 0 None - 0 Rat 6.7 pKi = 6.7 Functional
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 188079 0 None - 0 Rat 6.7 pKi = 6.7 Functional
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 93451 3 None - 0 Rat 8.7 pKi = 8.7 Functional
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 93451 3 None - 0 Rat 8.7 pKi = 8.7 Functional
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 93495 0 None - 0 Rat 8.7 pKi = 8.7 Functional
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 93495 0 None - 0 Rat 8.7 pKi = 8.7 Functional
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 62749 0 None - 1 Rat 8.7 pKi = 8.7 Functional
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 62749 0 None - 1 Rat 8.7 pKi = 8.7 Functional
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 62760 0 None - 1 Rat 8.6 pKi = 8.6 Functional
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 62760 0 None - 1 Rat 8.6 pKi = 8.6 Functional
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 62655 0 None - 1 Rat 8.6 pKi = 8.6 Functional
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 62655 0 None - 1 Rat 8.6 pKi = 8.6 Functional
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 62750 0 None - 1 Rat 8.5 pKi = 8.5 Functional
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 62750 0 None - 1 Rat 8.5 pKi = 8.5 Functional
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 179114 0 None - 0 Rat 7.7 pKi = 7.7 Functional
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 179114 0 None - 0 Rat 7.7 pKi = 7.7 Functional
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 179055 0 None - 0 Rat 6.7 pKi = 6.7 Functional
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 179055 0 None - 0 Rat 6.7 pKi = 6.7 Functional
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 70983 0 None - 1 Rat 6.7 pKi = 6.7 Functional
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 70983 0 None - 1 Rat 6.7 pKi = 6.7 Functional
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 178856 0 None - 0 Rat 7.7 pKi = 7.7 Functional
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 178856 0 None - 0 Rat 7.7 pKi = 7.7 Functional
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 92006 1 None - 0 Rat 7.7 pKi = 7.7 Functional
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 92006 1 None - 0 Rat 7.7 pKi = 7.7 Functional
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 71042 0 None - 1 Rat 7.7 pKi = 7.7 Functional
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 71042 0 None - 1 Rat 7.7 pKi = 7.7 Functional
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 189021 0 None - 0 Rat 5.7 pKi = 5.7 Functional
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 189021 0 None - 0 Rat 5.7 pKi = 5.7 Functional
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 70991 0 None - 1 Rat 7.6 pKi = 7.6 Functional
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 70991 0 None - 1 Rat 7.6 pKi = 7.6 Functional
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 62754 0 None - 1 Rat 7.6 pKi = 7.6 Functional
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 62754 0 None - 1 Rat 7.6 pKi = 7.6 Functional
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 62764 0 None - 1 Rat 7.6 pKi = 7.6 Functional
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 62764 0 None - 1 Rat 7.6 pKi = 7.6 Functional
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 41 None 1 3 Human 4.6 pKi = 4.6 Functional
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 41 None 1 3 Human 4.6 pKi = 4.6 Functional
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 41 None 1 3 Human 4.6 pKi = 4.6 Functional
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 62747 0 None - 1 Rat 7.6 pKi = 7.6 Functional
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 62747 0 None - 1 Rat 7.6 pKi = 7.6 Functional
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 93559 0 None - 0 Rat 7.6 pKi = 7.6 Functional
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 93559 0 None - 0 Rat 7.6 pKi = 7.6 Functional
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 93560 0 None - 0 Rat 7.6 pKi = 7.6 Functional
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 93560 0 None - 0 Rat 7.6 pKi = 7.6 Functional
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 189394 17 None - 0 Rat 7.6 pKi = 7.6 Functional
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 189394 17 None - 0 Rat 7.6 pKi = 7.6 Functional
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 70997 0 None - 1 Rat 6.6 pKi = 6.6 Functional
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 70997 0 None - 1 Rat 6.6 pKi = 6.6 Functional
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 62745 0 None - 1 Rat 7.6 pKi = 7.6 Functional
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 62745 0 None - 1 Rat 7.6 pKi = 7.6 Functional
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 71039 0 None - 1 Rat 7.6 pKi = 7.6 Functional
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 71039 0 None - 1 Rat 7.6 pKi = 7.6 Functional
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 62765 0 None - 1 Rat 7.5 pKi = 7.5 Functional
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 62765 0 None - 1 Rat 7.5 pKi = 7.5 Functional
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 70971 0 None - 1 Rat 7.5 pKi = 7.5 Functional
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 70971 0 None - 1 Rat 7.5 pKi = 7.5 Functional
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 93411 3 None - 0 Rat 8.5 pKi = 8.5 Functional
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 93411 3 None - 0 Rat 8.5 pKi = 8.5 Functional
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 93498 2 None - 0 Rat 8.5 pKi = 8.5 Functional
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 93498 2 None - 0 Rat 8.5 pKi = 8.5 Functional
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 0 None -1 2 Rat 8.5 pKi = 8.5 Functional
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 0 None -1 2 Rat 8.5 pKi = 8.5 Functional
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 0 None -1 2 Rat 8.5 pKi = 8.5 Functional
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 62662 0 None - 1 Rat 8.5 pKi = 8.5 Functional
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 62662 0 None - 1 Rat 8.5 pKi = 8.5 Functional
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 71034 0 None - 1 Rat 8.5 pKi = 8.5 Functional
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 71034 0 None - 1 Rat 8.5 pKi = 8.5 Functional
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 2 None - 1 Rat 8.5 pKi = 8.5 Functional
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 2 None - 1 Rat 8.5 pKi = 8.5 Functional
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 2 None - 1 Rat 8.5 pKi = 8.5 Functional
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 62752 0 None - 1 Rat 8.4 pKi = 8.4 Functional
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 62752 0 None - 1 Rat 8.4 pKi = 8.4 Functional
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 153117 4 None - 0 Rat 7.5 pKi = 7.5 Functional
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 153117 4 None - 0 Rat 7.5 pKi = 7.5 Functional
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 189268 0 None - 0 Rat 6.5 pKi = 6.5 Functional
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 189268 0 None - 0 Rat 6.5 pKi = 6.5 Functional
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 67 None - 4 Human 4.5 pKi = 4.5 Functional
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 67 None - 4 Human 4.5 pKi = 4.5 Functional
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 67 None - 4 Human 4.5 pKi = 4.5 Functional
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 170252 36 None 1 2 Human 4.5 pKi = 4.5 Functional
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 170252 36 None 1 2 Human 4.5 pKi = 4.5 Functional
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 71025 0 None - 1 Rat 6.5 pKi = 6.5 Functional
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 71025 0 None - 1 Rat 6.5 pKi = 6.5 Functional
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 189395 0 None - 0 Rat 7.5 pKi = 7.5 Functional
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 189395 0 None - 0 Rat 7.5 pKi = 7.5 Functional
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 93776 3 None - 0 Rat 6.5 pKi = 6.5 Functional
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 93776 3 None - 0 Rat 6.5 pKi = 6.5 Functional
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 62768 0 None - 1 Rat 7.5 pKi = 7.5 Functional
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 62768 0 None - 1 Rat 7.5 pKi = 7.5 Functional
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 70984 0 None - 1 Rat 7.5 pKi = 7.5 Functional
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 70984 0 None - 1 Rat 7.5 pKi = 7.5 Functional
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 71027 0 None - 1 Rat 7.5 pKi = 7.5 Functional
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 71027 0 None - 1 Rat 7.5 pKi = 7.5 Functional
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 71037 0 None - 1 Rat 7.5 pKi = 7.5 Functional
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 71037 0 None - 1 Rat 7.5 pKi = 7.5 Functional
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 189298 0 None - 0 Rat 7.5 pKi = 7.5 Functional
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 189298 0 None - 0 Rat 7.5 pKi = 7.5 Functional
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 179029 1 None - 0 Rat 7.5 pKi = 7.5 Functional
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 179029 1 None - 0 Rat 7.5 pKi = 7.5 Functional
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 93561 0 None - 0 Rat 7.5 pKi = 7.5 Functional
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 93561 0 None - 0 Rat 7.5 pKi = 7.5 Functional
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 207126 13 None - 0 Human 6.5 pKi = 6.5 Functional
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 207126 13 None - 0 Human 6.5 pKi = 6.5 Functional
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 67 None - 4 Human 7.4 pKi = 7.4 Functional
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 67 None - 4 Human 7.4 pKi = 7.4 Functional
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 67 None - 4 Human 7.4 pKi = 7.4 Functional
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 62756 0 None - 1 Rat 7.4 pKi = 7.4 Functional
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 62756 0 None - 1 Rat 7.4 pKi = 7.4 Functional
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 62767 0 None - 1 Rat 7.4 pKi = 7.4 Functional
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 62767 0 None - 1 Rat 7.4 pKi = 7.4 Functional
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 62661 0 None - 1 Rat 8.4 pKi = 8.4 Functional
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 62661 0 None - 1 Rat 8.4 pKi = 8.4 Functional
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 62762 0 None - 1 Rat 8.4 pKi = 8.4 Functional
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 62762 0 None - 1 Rat 8.4 pKi = 8.4 Functional
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 93453 2 None - 0 Rat 7.4 pKi = 7.4 Functional
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 93453 2 None - 0 Rat 7.4 pKi = 7.4 Functional
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 93779 0 None - 0 Rat 7.4 pKi = 7.4 Functional
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 93779 0 None - 0 Rat 7.4 pKi = 7.4 Functional
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 148300 0 None - 0 Rat 7.4 pKi = 7.4 Functional
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 148300 0 None - 0 Rat 7.4 pKi = 7.4 Functional
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 71026 0 None - 1 Rat 7.4 pKi = 7.4 Functional
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 71026 0 None - 1 Rat 7.4 pKi = 7.4 Functional
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 93663 0 None - 0 Rat 6.4 pKi = 6.4 Functional
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 93663 0 None - 0 Rat 6.4 pKi = 6.4 Functional
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 189339 0 None - 0 Rat 7.4 pKi = 7.4 Functional
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 189339 0 None - 0 Rat 7.4 pKi = 7.4 Functional
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 70985 0 None - 1 Rat 7.4 pKi = 7.4 Functional
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 70985 0 None - 1 Rat 7.4 pKi = 7.4 Functional
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 42 None -4 14 Human 4.4 pKi = 4.4 Functional
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 42 None -4 14 Human 4.4 pKi = 4.4 Functional
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 42 None -4 14 Human 4.4 pKi = 4.4 Functional
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 62758 0 None - 1 Rat 7.4 pKi = 7.4 Functional
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 62758 0 None - 1 Rat 7.4 pKi = 7.4 Functional
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 93780 0 None - 0 Rat 7.4 pKi = 7.4 Functional
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 93780 0 None - 0 Rat 7.4 pKi = 7.4 Functional
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 64 None - 2 Human 4.4 pKi = 4.4 Functional
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 64 None - 2 Human 4.4 pKi = 4.4 Functional
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 64 None - 2 Human 4.4 pKi = 4.4 Functional
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 64 None - 2 Human 4.4 pKi = 4.4 Functional
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 147464 0 None - 0 Rat 7.4 pKi = 7.4 Functional
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 147464 0 None - 0 Rat 7.4 pKi = 7.4 Functional
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 62759 0 None - 1 Rat 7.3 pKi = 7.3 Functional
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 62759 0 None - 1 Rat 7.3 pKi = 7.3 Functional
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 189191 0 None - 0 Rat 8.3 pKi = 8.3 Functional
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 189191 0 None - 0 Rat 8.3 pKi = 8.3 Functional
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 0 None - 1 Rat 8.3 pKi = 8.3 Functional
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 0 None - 1 Rat 8.3 pKi = 8.3 Functional
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 0 None - 1 Rat 8.3 pKi = 8.3 Functional
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 62660 0 None - 1 Rat 8.3 pKi = 8.3 Functional
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 62660 0 None - 1 Rat 8.3 pKi = 8.3 Functional
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 37 None - 11 Human 4.3 pKi = 4.3 Functional
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 37 None - 11 Human 4.3 pKi = 4.3 Functional
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 37 None - 11 Human 4.3 pKi = 4.3 Functional
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 148088 3 None - 0 Rat 6.3 pKi = 6.3 Functional
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 148088 3 None - 0 Rat 6.3 pKi = 6.3 Functional
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 71041 0 None - 1 Rat 7.3 pKi = 7.3 Functional
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 71041 0 None - 1 Rat 7.3 pKi = 7.3 Functional
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 179209 0 None - 0 Rat 7.3 pKi = 7.3 Functional
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 179209 0 None - 0 Rat 7.3 pKi = 7.3 Functional
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 93497 0 None - 0 Rat 7.3 pKi = 7.3 Functional
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 93497 0 None - 0 Rat 7.3 pKi = 7.3 Functional
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 70974 0 None - 1 Rat 7.3 pKi = 7.3 Functional
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 70974 0 None - 1 Rat 7.3 pKi = 7.3 Functional
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 70982 0 None - 1 Rat 6.3 pKi = 6.3 Functional
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 70982 0 None - 1 Rat 6.3 pKi = 6.3 Functional
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 207116 2 None - 0 Human 5.2 pKi = 5.2 Functional
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 207116 2 None - 0 Human 5.2 pKi = 5.2 Functional
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 0 None - 1 Rat 8.2 pKi = 8.2 Functional
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 0 None - 1 Rat 8.2 pKi = 8.2 Functional
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 0 None - 1 Rat 8.2 pKi = 8.2 Functional
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 71024 0 None - 1 Rat 8.2 pKi = 8.2 Functional
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 71024 0 None - 1 Rat 8.2 pKi = 8.2 Functional
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 70981 0 None - 1 Rat 8.2 pKi = 8.2 Functional
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 70981 0 None - 1 Rat 8.2 pKi = 8.2 Functional
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 60 None - 2 Human 8.2 pKi = 8.2 Functional
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 60 None - 2 Human 8.2 pKi = 8.2 Functional
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 60 None - 2 Human 8.2 pKi = 8.2 Functional
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 60 None - 2 Human 8.2 pKi = 8.2 Functional
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 60 None - 2 Human 8.2 pKi = 8.2 Functional
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 60 None - 2 Human 8.2 pKi = 8.2 Functional
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 60 None - 2 Human 8.2 pKi = 8.2 Functional
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 60 None - 2 Human 8.2 pKi = 8.2 Functional
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 105985 0 None - 1 Human 5.2 pKi = 5.2 Functional
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 105985 0 None - 1 Human 5.2 pKi = 5.2 Functional
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 189114 0 None - 0 Rat 5.2 pKi = 5.2 Functional
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 189114 0 None - 0 Rat 5.2 pKi = 5.2 Functional
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 172642 2 None - 0 Rat 5.2 pKi = 5.2 Functional
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 172642 2 None - 0 Rat 5.2 pKi = 5.2 Functional
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 62757 0 None - 1 Rat 7.2 pKi = 7.2 Functional
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 62757 0 None - 1 Rat 7.2 pKi = 7.2 Functional
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 62772 0 None - 1 Rat 7.2 pKi = 7.2 Functional
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 62772 0 None - 1 Rat 7.2 pKi = 7.2 Functional
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 70995 0 None - 1 Rat 7.2 pKi = 7.2 Functional
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 70995 0 None - 1 Rat 7.2 pKi = 7.2 Functional
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 62761 0 None - 1 Rat 7.2 pKi = 7.2 Functional
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 62761 0 None - 1 Rat 7.2 pKi = 7.2 Functional
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 62770 0 None - 1 Rat 7.2 pKi = 7.2 Functional
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 62770 0 None - 1 Rat 7.2 pKi = 7.2 Functional
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 146038 0 None - 0 Rat 6.2 pKi = 6.2 Functional
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 146038 0 None - 0 Rat 6.2 pKi = 6.2 Functional
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 93454 4 None - 0 Rat 5.2 pKi = 5.2 Functional
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 93454 4 None - 0 Rat 5.2 pKi = 5.2 Functional
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 146452 53 None -16 3 Human 5.2 pKi = 5.2 Functional
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 146452 53 None -16 3 Human 5.2 pKi = 5.2 Functional
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 146452 53 None -16 3 Human 5.2 pKi = 5.2 Functional
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 62753 0 None - 1 Rat 7.2 pKi = 7.2 Functional
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 62753 0 None - 1 Rat 7.2 pKi = 7.2 Functional
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 54 None -1047 14 Human 5.2 pKi = 5.2 Functional
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 54 None -1047 14 Human 5.2 pKi = 5.2 Functional
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 54 None -1047 14 Human 5.2 pKi = 5.2 Functional
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 54 None -1047 14 Human 5.2 pKi = 5.2 Functional
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 62773 0 None - 1 Rat 7.2 pKi = 7.2 Functional
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 62773 0 None - 1 Rat 7.2 pKi = 7.2 Functional
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 93412 15 None - 0 Rat 7.2 pKi = 7.2 Functional
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 93412 15 None - 0 Rat 7.2 pKi = 7.2 Functional
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 179112 0 None - 0 Rat 6.2 pKi = 6.2 Functional
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 179112 0 None - 0 Rat 6.2 pKi = 6.2 Functional
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 71032 0 None - 1 Rat 8.1 pKi = 8.1 Functional
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 71032 0 None - 1 Rat 8.1 pKi = 8.1 Functional
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 71033 0 None - 1 Rat 8.1 pKi = 8.1 Functional
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 71033 0 None - 1 Rat 8.1 pKi = 8.1 Functional
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 62751 0 None - 1 Rat 8.1 pKi = 8.1 Functional
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 62751 0 None - 1 Rat 8.1 pKi = 8.1 Functional
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 62659 0 None - 1 Rat 8.1 pKi = 8.1 Functional
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 62659 0 None - 1 Rat 8.1 pKi = 8.1 Functional
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 167055 13 None - 2 Rat 8.1 pKi = 8.1 Functional
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 167055 13 None - 2 Rat 8.1 pKi = 8.1 Functional
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 71028 0 None - 1 Rat 7.2 pKi = 7.2 Functional
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 71028 0 None - 1 Rat 7.2 pKi = 7.2 Functional
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 62766 0 None - 1 Rat 7.1 pKi = 7.1 Functional
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 62766 0 None - 1 Rat 7.1 pKi = 7.1 Functional
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 71036 0 None - 1 Rat 7.1 pKi = 7.1 Functional
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 71036 0 None - 1 Rat 7.1 pKi = 7.1 Functional
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 70988 0 None - 0 Rat 6.1 pKi = 6.1 Functional
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 70988 0 None - 0 Rat 6.1 pKi = 6.1 Functional
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 62748 0 None - 1 Rat 8.1 pKi = 8.1 Functional
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 62748 0 None - 1 Rat 8.1 pKi = 8.1 Functional
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 93499 3 None - 0 Rat 8.1 pKi = 8.1 Functional
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 93499 3 None - 0 Rat 8.1 pKi = 8.1 Functional
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 62763 0 None - 1 Rat 8.1 pKi = 8.1 Functional
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 62763 0 None - 1 Rat 8.1 pKi = 8.1 Functional
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 70990 0 None - 1 Rat 8.1 pKi = 8.1 Functional
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 70990 0 None - 1 Rat 8.1 pKi = 8.1 Functional
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
1418 3449 53 None -1 2 Human 4.1 pKi = 4.1 Functional
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 195 3 3 3 0.5 N[C@@H](c1ccc(cc1)C(=O)O)C(=O)O 10.1021/jm000007r
5311459 3449 53 None -1 2 Human 4.1 pKi = 4.1 Functional
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 195 3 3 3 0.5 N[C@@H](c1ccc(cc1)C(=O)O)C(=O)O 10.1021/jm000007r
CHEMBL94990 3449 53 None -1 2 Human 4.1 pKi = 4.1 Functional
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 195 3 3 3 0.5 N[C@@H](c1ccc(cc1)C(=O)O)C(=O)O 10.1021/jm000007r
44592519 193393 0 None - 0 Rat 6.1 pKi = 6.1 Functional
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 259 5 1 5 2.7 CCCC(C)Nc1ncnc2cnc(N(C)C)cc12 10.1016/j.bmcl.2009.02.106
CHEMBL525546 193393 0 None - 0 Rat 6.1 pKi = 6.1 Functional
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 259 5 1 5 2.7 CCCC(C)Nc1ncnc2cnc(N(C)C)cc12 10.1016/j.bmcl.2009.02.106
57400362 70994 0 None - 1 Rat 7.1 pKi = 7.1 Functional
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat 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 70994 0 None - 1 Rat 7.1 pKi = 7.1 Functional
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat 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
3931705 107052 27 None - 0 Human 5.1 pKi = 5.1 Functional
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 209 3 3 3 0.8 Cc1cc(C(=O)O)ccc1C(N)C(=O)O 10.1021/jm000007r
CHEMBL315591 107052 27 None - 0 Human 5.1 pKi = 5.1 Functional
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 209 3 3 3 0.8 Cc1cc(C(=O)O)ccc1C(N)C(=O)O 10.1021/jm000007r
16216350 93500 0 None - 0 Rat 8.1 pKi = 8.1 Functional
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 332 4 2 5 2.0 C[C@H]1CC[C@H](NC(=O)c2cnc(N3CCC(CO)CC3)cn2)CC1 10.1016/j.bmcl.2006.10.015
CHEMBL246252 93500 0 None - 0 Rat 8.1 pKi = 8.1 Functional
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 332 4 2 5 2.0 C[C@H]1CC[C@H](NC(=O)c2cnc(N3CCC(CO)CC3)cn2)CC1 10.1016/j.bmcl.2006.10.015
16118398 71031 0 None - 1 Rat 8.0 pKi = 8.0 Functional
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat 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 71031 0 None - 1 Rat 8.0 pKi = 8.0 Functional
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat 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
16118535 71029 0 None - 1 Rat 8.0 pKi = 8.0 Functional
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat 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 71029 0 None - 1 Rat 8.0 pKi = 8.0 Functional
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat 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
16117434 71040 0 None - 1 Rat 7.0 pKi = 7.0 Functional
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat 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 71040 0 None - 1 Rat 7.0 pKi = 7.0 Functional
Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat 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
1382 1190 33 None -1 3 Human 5.0 pKi = 5 Functional
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 247 2 1 5 1.6 CCOC(=O)C12CC2/C(=N\O)/c2c(O1)cccc2 10.1021/jm000007r
6278000 1190 33 None -1 3 Human 5.0 pKi = 5 Functional
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 247 2 1 5 1.6 CCOC(=O)C12CC2/C(=N\O)/c2c(O1)cccc2 10.1021/jm000007r
CHEMBL327783 1190 33 None -1 3 Human 5.0 pKi = 5 Functional
Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1
ChEMBL 247 2 1 5 1.6 CCOC(=O)C12CC2/C(=N\O)/c2c(O1)cccc2 10.1021/jm000007r
54582006 62769 0 None - 1 Rat 6.0 pKi = 6 Functional
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 377 3 1 9 2.2 C#CCNc1ncnc2sc3c(=O)n(-c4ccc5c(c4)OCO5)cnc3c12 10.1016/j.bmcl.2009.04.104
CHEMBL1784074 62769 0 None - 1 Rat 6.0 pKi = 6 Functional
Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1
ChEMBL 377 3 1 9 2.2 C#CCNc1ncnc2sc3c(=O)n(-c4ccc5c(c4)OCO5)cnc3c12 10.1016/j.bmcl.2009.04.104
1376 321 55 None - 1 Human 4.2 pA2 = 4.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 221 2 3 3 0.6 OC(=O)c1ccc2c(c1)CCC2(N)C(=O)O 9152378
2071 321 55 None - 1 Human 4.2 pA2 = 4.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 221 2 3 3 0.6 OC(=O)c1ccc2c(c1)CCC2(N)C(=O)O 9152378
CHEMBL313938 321 55 None - 1 Human 4.2 pA2 = 4.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 221 2 3 3 0.6 OC(=O)c1ccc2c(c1)CCC2(N)C(=O)O 9152378
1310 2315 110 None -794 17 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
1369 2315 110 None -794 17 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
33032 2315 110 None -794 17 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
44272391 2315 110 None -794 17 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
88747398 2315 110 None -794 17 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
CHEMBL575060 2315 110 None -794 17 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
DB00142 2315 110 None -794 17 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
1310 2315 110 None -741 17 Human 4.9 pEC50 = 4.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
1369 2315 110 None -741 17 Human 4.9 pEC50 = 4.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
33032 2315 110 None -741 17 Human 4.9 pEC50 = 4.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
44272391 2315 110 None -741 17 Human 4.9 pEC50 = 4.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
88747398 2315 110 None -741 17 Human 4.9 pEC50 = 4.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
CHEMBL575060 2315 110 None -741 17 Human 4.9 pEC50 = 4.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
DB00142 2315 110 None -741 17 Human 4.9 pEC50 = 4.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10443583
1382 1190 33 None 1 3 Rat 5.3 pEC50 = 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 247 2 1 5 1.6 CCOC(=O)C12CC2/C(=N\O)/c2c(O1)cccc2 11961143
6278000 1190 33 None 1 3 Rat 5.3 pEC50 = 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 247 2 1 5 1.6 CCOC(=O)C12CC2/C(=N\O)/c2c(O1)cccc2 11961143
CHEMBL327783 1190 33 None 1 3 Rat 5.3 pEC50 = 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 247 2 1 5 1.6 CCOC(=O)C12CC2/C(=N\O)/c2c(O1)cccc2 11961143
11523834 4057 0 None - 1 Rat 5.6 pEC50 = 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 384 5 1 5 4.7 O=C(c1ccc(cc1)N(=O)=O)Nc1c(cnn1c1ccccc1)c1ccccc1 16099654
6207 4057 0 None - 1 Rat 5.6 pEC50 = 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 384 5 1 5 4.7 O=C(c1ccc(cc1)N(=O)=O)Nc1c(cnn1c1ccccc1)c1ccccc1 16099654
CHEMBL377636 4057 0 None - 1 Rat 5.6 pEC50 = 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 384 5 1 5 4.7 O=C(c1ccc(cc1)N(=O)=O)Nc1c(cnn1c1ccccc1)c1ccccc1 16099654
10009 4049 40 None -1 3 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 445 3 1 4 5.1 Clc1cc(ccc1N1C(=O)c2c(C1=O)c(Cl)ccc2)NC(=O)c1ncccc1Cl 25137254
91885483 4049 40 None -1 3 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 445 3 1 4 5.1 Clc1cc(ccc1N1C(=O)c2c(C1=O)c(Cl)ccc2)NC(=O)c1ncccc1Cl 25137254
CHEMBL3628116 4049 40 None -1 3 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 445 3 1 4 5.1 Clc1cc(ccc1N1C(=O)c2c(C1=O)c(Cl)ccc2)NC(=O)c1ncccc1Cl 25137254
44573698 1082 0 None - 1 Rat 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 307 2 1 5 3.3 O=C(C1c2ccccc2Oc2c1cccc2)Nc1noc(n1)C 16099654
6205 1082 0 None - 1 Rat 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 307 2 1 5 3.3 O=C(C1c2ccccc2Oc2c1cccc2)Nc1noc(n1)C 16099654
CHEMBL492378 1082 0 None - 1 Rat 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 307 2 1 5 3.3 O=C(C1c2ccccc2Oc2c1cccc2)Nc1noc(n1)C 16099654
6206 1107 0 None - 1 Rat 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 321 3 1 6 2.6 CCn1nnc(n1)NC(=O)C1c2ccccc2Oc2c1cccc2 16099654
9923127 1107 0 None - 1 Rat 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 321 3 1 6 2.6 CCn1nnc(n1)NC(=O)C1c2ccccc2Oc2c1cccc2 16099654
10338547 3340 26 None 1 2 Rat 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 360 2 1 4 4.6 O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F 19233648
6204 3340 26 None 1 2 Rat 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 360 2 1 4 4.6 O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F 19233648
CHEMBL521982 3340 26 None 1 2 Rat 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 360 2 1 4 4.6 O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F 19233648
3421 3544 41 None -1 3 Rat 4.2 pIC50 = 4.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 3 3 3 -0.3 OC(=O)[C@H](C12CC(C1)(C2)C(=O)O)N 10428410
5311040 3544 41 None -1 3 Rat 4.2 pIC50 = 4.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 3 3 3 -0.3 OC(=O)[C@H](C12CC(C1)(C2)C(=O)O)N 10428410
CHEMBL43412 3544 41 None -1 3 Rat 4.2 pIC50 = 4.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 185 3 3 3 -0.3 OC(=O)[C@H](C12CC(C1)(C2)C(=O)O)N 10428410
10058919 3690 10 None 1 2 Rat 4.2 pIC50 = 4.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 209 3 3 5 -1.0 OC(=O)[C@H](C12CC(C1)(C2)c1n[nH]nn1)N 11249114
3419 3690 10 None 1 2 Rat 4.2 pIC50 = 4.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 209 3 3 5 -1.0 OC(=O)[C@H](C12CC(C1)(C2)c1n[nH]nn1)N 11249114
CHEMBL2204334 3690 10 None 1 2 Rat 4.2 pIC50 = 4.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 209 3 3 5 -1.0 OC(=O)[C@H](C12CC(C1)(C2)c1n[nH]nn1)N 11249114
1379 2420 44 None - 1 Human 5.1 pIC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 209 3 3 3 0.8 OC(=O)c1ccc(c(c1)C)[C@@H](C(=O)O)N None
5311261 2420 44 None - 1 Human 5.1 pIC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 209 3 3 3 0.8 OC(=O)c1ccc(c(c1)C)[C@@H](C(=O)O)N None
CHEMBL94631 2420 44 None - 1 Human 5.1 pIC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 209 3 3 3 0.8 OC(=O)c1ccc(c(c1)C)[C@@H](C(=O)O)N None
10398360 105 0 None - 1 Rat 5.2 pIC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 215 3 3 4 0.8 OC(=O)c1cc(c(s1)C(C(=O)O)N)C 12015200
3396 105 0 None - 1 Rat 5.2 pIC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 215 3 3 4 0.8 OC(=O)c1cc(c(s1)C(C(=O)O)N)C 12015200
CHEMBL1322301 105 0 None - 1 Rat 5.2 pIC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 215 3 3 4 0.8 OC(=O)c1cc(c(s1)C(C(=O)O)N)C 12015200
1382 1190 33 None -1 3 Human 5.5 pIC50 = 5.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 247 2 1 5 1.6 CCOC(=O)C12CC2/C(=N\O)/c2c(O1)cccc2 10051528
6278000 1190 33 None -1 3 Human 5.5 pIC50 = 5.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 247 2 1 5 1.6 CCOC(=O)C12CC2/C(=N\O)/c2c(O1)cccc2 10051528
CHEMBL327783 1190 33 None -1 3 Human 5.5 pIC50 = 5.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 247 2 1 5 1.6 CCOC(=O)C12CC2/C(=N\O)/c2c(O1)cccc2 10051528
16739288 1033 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 306 3 2 2 3.3 Cc1cc2[nH]c3c(c2cc1OCc1ccccc1)CCNC3=O 17276684
6358 1033 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 306 3 2 2 3.3 Cc1cc2[nH]c3c(c2cc1OCc1ccccc1)CCNC3=O 17276684
CHEMBL396712 1033 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 306 3 2 2 3.3 Cc1cc2[nH]c3c(c2cc1OCc1ccccc1)CCNC3=O 17276684
1390 1556 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 308 2 0 5 2.0 CCn1c(C)nc(c(c1=O)C#N)N1CCc2c(CC1)cccc2 12509432
3363 1556 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 308 2 0 5 2.0 CCn1c(C)nc(c(c1=O)C#N)N1CCc2c(CC1)cccc2 12509432
9904703 1556 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 308 2 0 5 2.0 CCn1c(C)nc(c(c1=O)C#N)N1CCc2c(CC1)cccc2 12509432
3346 2424 14 None - 1 Human 6.9 pIC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 281 4 1 5 3.4 COc1ccc(cc1)Nc1ncnc2c1cc(OC)cc2 24798819
9926999 2424 14 None - 1 Human 6.9 pIC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 281 4 1 5 3.4 COc1ccc(cc1)Nc1ncnc2c1cc(OC)cc2 24798819
CHEMBL254575 2424 14 None - 1 Human 6.9 pIC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 281 4 1 5 3.4 COc1ccc(cc1)Nc1ncnc2c1cc(OC)cc2 24798819
1389 4118 0 None -7 2 Human 6.9 pIC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 342 2 1 5 3.8 CN(C(=O)c1sc2n(c1C)c1c(n2)ccc(c1)N)C1CCCCC1 19559036
5392 4118 0 None -7 2 Human 6.9 pIC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 342 2 1 5 3.8 CN(C(=O)c1sc2n(c1C)c1c(n2)ccc(c1)N)C1CCCCC1 19559036
9819432 4118 0 None -7 2 Human 6.9 pIC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 342 2 1 5 3.8 CN(C(=O)c1sc2n(c1C)c1c(n2)ccc(c1)N)C1CCCCC1 19559036
CHEMBL1517556 4118 0 None -7 2 Human 6.9 pIC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 342 2 1 5 3.8 CN(C(=O)c1sc2n(c1C)c1c(n2)ccc(c1)N)C1CCCCC1 19559036
6337 4048 0 None - 1 Human 7.0 pIC50 = 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 378 2 0 4 3.5 N#Cc1ncccc1N1CCN([C@@H](C1)C)C(=O)C12CC3CC(C2)C(C(C1)C3)C 23727046
73755207 4048 0 None - 1 Human 7.0 pIC50 = 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 378 2 0 4 3.5 N#Cc1ncccc1N1CCN([C@@H](C1)C)C(=O)C12CC3CC(C2)C(C(C1)C3)C 23727046
10245890 1982 7 None 3 2 Human 7.0 pIC50 = 7.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 327 5 0 4 4.2 CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)OC)CC 15771457
6474 1982 7 None 3 2 Human 7.0 pIC50 = 7.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 327 5 0 4 4.2 CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)OC)CC 15771457
CHEMBL175643 1982 7 None 3 2 Human 7.0 pIC50 = 7.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 327 5 0 4 4.2 CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)OC)CC 15771457
6340 884 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 389 5 0 5 4.0 Cc1c(OCCN2CCOCC2)cc2c(c1F)c(=O)c(co2)C1CCCCC1 19559036
73755208 884 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 389 5 0 5 4.0 Cc1c(OCCN2CCOCC2)cc2c(c1F)c(=O)c(co2)C1CCCCC1 19559036
11515548 212 9 None -1 3 Human 7.4 pIC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 336 2 0 6 3.4 Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(cnc1)N(C)C 16279797
6355 212 9 None -1 3 Human 7.4 pIC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 336 2 0 6 3.4 Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(cnc1)N(C)C 16279797
CHEMBL223869 212 9 None -1 3 Human 7.4 pIC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 336 2 0 6 3.4 Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(cnc1)N(C)C 16279797
11515548 212 9 None 1 3 Rat 7.4 pIC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 336 2 0 6 3.4 Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(cnc1)N(C)C 18054908
6355 212 9 None 1 3 Rat 7.4 pIC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 336 2 0 6 3.4 Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(cnc1)N(C)C 18054908
CHEMBL223869 212 9 None 1 3 Rat 7.4 pIC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 336 2 0 6 3.4 Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(cnc1)N(C)C 18054908
1381 581 30 None 3 2 Rat 7.4 pIC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 278 2 0 2 3.9 C=C1C[C@H]2[C@](C1)(Cc1ccc3c(c1)cccc3)C(=O)OC2 11306677
1381 581 30 None 3 2 Rat 7.4 pIC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 278 2 0 2 3.9 C=C1C[C@H]2[C@](C1)(Cc1ccc3c(c1)cccc3)C(=O)OC2 12695537
9903757 581 30 None 3 2 Rat 7.4 pIC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 278 2 0 2 3.9 C=C1C[C@H]2[C@](C1)(Cc1ccc3c(c1)cccc3)C(=O)OC2 11306677
9903757 581 30 None 3 2 Rat 7.4 pIC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 278 2 0 2 3.9 C=C1C[C@H]2[C@](C1)(Cc1ccc3c(c1)cccc3)C(=O)OC2 12695537
CHEMBL254372 581 30 None 3 2 Rat 7.4 pIC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 278 2 0 2 3.9 C=C1C[C@H]2[C@](C1)(Cc1ccc3c(c1)cccc3)C(=O)OC2 11306677
CHEMBL254372 581 30 None 3 2 Rat 7.4 pIC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 278 2 0 2 3.9 C=C1C[C@H]2[C@](C1)(Cc1ccc3c(c1)cccc3)C(=O)OC2 12695537
3347 2423 9 None - 1 Human 7.6 pIC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 341 5 2 5 3.0 OCCSc1nc(NC2Cc3c(C2)cccc3)c2c(n1)CCCC2 19559036
9840951 2423 9 None - 1 Human 7.6 pIC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 341 5 2 5 3.0 OCCSc1nc(NC2Cc3c(C2)cccc3)c2c(n1)CCCC2 19559036
CHEMBL3786530 2423 9 None - 1 Human 7.6 pIC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 341 5 2 5 3.0 OCCSc1nc(NC2Cc3c(C2)cccc3)c2c(n1)CCCC2 19559036
46866192 1050 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 323 1 1 7 2.6 Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(N)nc(n1)C 20346665
6210 1050 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 323 1 1 7 2.6 Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(N)nc(n1)C 20346665
CHEMBL1093901 1050 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 323 1 1 7 2.6 Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(N)nc(n1)C 20346665
11722867 95 3 None - 1 Rat 7.8 pIC50 = 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 309 5 1 4 3.8 CCCOC(=O)c1[nH]c(c(c1C)C(=O)OC(C(C)(C)C)C)C 12470711
3397 95 3 None - 1 Rat 7.8 pIC50 = 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 309 5 1 4 3.8 CCCOC(=O)c1[nH]c(c(c1C)C(=O)OC(C(C)(C)C)C)C 12470711
CHEMBL304824 95 3 None - 1 Rat 7.8 pIC50 = 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 309 5 1 4 3.8 CCCOC(=O)c1[nH]c(c(c1C)C(=O)OC(C(C)(C)C)C)C 12470711
6364 1088 0 None - 1 Rat 7.8 pIC50 = 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 295 5 1 4 3.4 CCCOC(=O)c1[nH]c(c(c1C)C(=O)OCC(C)(C)C)C 12470711
73755211 1088 0 None - 1 Rat 7.8 pIC50 = 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 295 5 1 4 3.4 CCCOC(=O)c1[nH]c(c(c1C)C(=O)OCC(C)(C)C)C 12470711
1389 4118 0 None 7 2 Rat 7.8 pIC50 = 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 342 2 1 5 3.8 CN(C(=O)c1sc2n(c1C)c1c(n2)ccc(c1)N)C1CCCCC1 15976016
5392 4118 0 None 7 2 Rat 7.8 pIC50 = 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 342 2 1 5 3.8 CN(C(=O)c1sc2n(c1C)c1c(n2)ccc(c1)N)C1CCCCC1 15976016
9819432 4118 0 None 7 2 Rat 7.8 pIC50 = 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 342 2 1 5 3.8 CN(C(=O)c1sc2n(c1C)c1c(n2)ccc(c1)N)C1CCCCC1 15976016
CHEMBL1517556 4118 0 None 7 2 Rat 7.8 pIC50 = 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 342 2 1 5 3.8 CN(C(=O)c1sc2n(c1C)c1c(n2)ccc(c1)N)C1CCCCC1 15976016
16118537 978 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 363 4 1 6 4.2 COc1ccc(cc1)n1ccc2c(c1=O)sc1c2c(ccn1)NC1CC1 22266036
6357 978 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 363 4 1 6 4.2 COc1ccc(cc1)n1ccc2c(c1=O)sc1c2c(ccn1)NC1CC1 22266036
CHEMBL1951683 978 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 363 4 1 6 4.2 COc1ccc(cc1)n1ccc2c(c1=O)sc1c2c(ccn1)NC1CC1 22266036
10470232 3269 23 None -1 2 Human 8.0 pIC50 = 8.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 303 3 0 3 4.0 O=C(c1ccc2c(c1)cc1c(n2)OCCC1)Cc1ccccc1 12695537
1391 3269 23 None -1 2 Human 8.0 pIC50 = 8.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 303 3 0 3 4.0 O=C(c1ccc2c(c1)cc1c(n2)OCCC1)Cc1ccccc1 12695537
6336 3269 23 None -1 2 Human 8.0 pIC50 = 8.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 303 3 0 3 4.0 O=C(c1ccc2c(c1)cc1c(n2)OCCC1)Cc1ccccc1 12695537
CHEMBL369459 3269 23 None -1 2 Human 8.0 pIC50 = 8.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 303 3 0 3 4.0 O=C(c1ccc2c(c1)cc1c(n2)OCCC1)Cc1ccccc1 12695537
11537456 209 12 None -3 3 Human 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 342 2 0 6 4.0 CN(c1ccnc2c1c1ncn(c(=O)c1s2)C1CCCCCC1)C 16279797
6354 209 12 None -3 3 Human 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 342 2 0 6 4.0 CN(c1ccnc2c1c1ncn(c(=O)c1s2)C1CCCCCC1)C 16279797
CHEMBL225032 209 12 None -3 3 Human 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 342 2 0 6 4.0 CN(c1ccnc2c1c1ncn(c(=O)c1s2)C1CCCCCC1)C 16279797
11559235 211 42 None -4 3 Human 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 343 2 0 7 2.6 CN(c1ccnc2c1c1ncn(c(=O)c1s2)N1CCCCCC1)C 16279797
3953 211 42 None -4 3 Human 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 343 2 0 7 2.6 CN(c1ccnc2c1c1ncn(c(=O)c1s2)N1CCCCCC1)C 16279797
CHEMBL386565 211 42 None -4 3 Human 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 343 2 0 7 2.6 CN(c1ccnc2c1c1ncn(c(=O)c1s2)N1CCCCCC1)C 16279797
6208 1055 0 None - 1 Rat 8.1 pIC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 318 4 2 5 1.7 OCC1CCN(CC1)c1ncc(nc1)C(=O)NC1CCCCC1 17064898
73755189 1055 0 None - 1 Rat 8.1 pIC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 318 4 2 5 1.7 OCC1CCN(CC1)c1ncc(nc1)C(=O)NC1CCCCC1 17064898
10409562 4116 0 None - 1 Rat 8.1 pIC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 414 7 0 6 4.0 COCCN(Cc1ccc2c(c1)nc1n2cc(s1)C(=O)N(C1CCCCC1)C)C 18164695
6361 4116 0 None - 1 Rat 8.1 pIC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 414 7 0 6 4.0 COCCN(Cc1ccc2c(c1)nc1n2cc(s1)C(=O)N(C1CCCCC1)C)C 18164695
16725048 1153 0 None 1412 2 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 371 3 0 8 2.6 COc1ccc(c(c1)F)n1cnc2c(c1=O)sc1c2c(ncn1)N(C)C 23084894
6362 1153 0 None 1412 2 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 371 3 0 8 2.6 COc1ccc(c(c1)F)n1cnc2c(c1=O)sc1c2c(ncn1)N(C)C 23084894
CHEMBL2205377 1153 0 None 1412 2 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 371 3 0 8 2.6 COc1ccc(c(c1)F)n1cnc2c(c1=O)sc1c2c(ncn1)N(C)C 23084894
16118119 1149 0 None 741 2 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 351 3 0 6 3.7 COc1ccc(cc1)n1ccc2c(c1=O)sc1c2c(ccn1)N(C)C 22266036
6356 1149 0 None 741 2 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 351 3 0 6 3.7 COc1ccc(cc1)n1ccc2c(c1=O)sc1c2c(ccn1)N(C)C 22266036
CHEMBL1951658 1149 0 None 741 2 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 351 3 0 6 3.7 COc1ccc(cc1)n1ccc2c(c1=O)sc1c2c(ccn1)N(C)C 22266036
57559562 966 0 None 1659 2 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 365 4 1 8 3.0 COc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ncn1)NC1CC1 23084894
6365 966 0 None 1659 2 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 365 4 1 8 3.0 COc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ncn1)NC1CC1 23084894
CHEMBL2205915 966 0 None 1659 2 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 365 4 1 8 3.0 COc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ncn1)NC1CC1 23084894
11337722 1070 0 None - 1 Rat 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 371 6 1 7 2.9 C1CCCC(CC1)Nc1ncnc2c1cc(OCCN1CCOCC1)nc2 19289283
6351 1070 0 None - 1 Rat 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 371 6 1 7 2.9 C1CCCC(CC1)Nc1ncnc2c1cc(OCCN1CCOCC1)nc2 19289283
CHEMBL470396 1070 0 None - 1 Rat 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 371 6 1 7 2.9 C1CCCC(CC1)Nc1ncnc2c1cc(OCCN1CCOCC1)nc2 19289283
11245287 1697 34 None -1 4 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 358 3 0 5 2.7 CC(N(C(=O)N1CCC(=CC1)c1nnn(c1C)c1cccnc1F)C)C 17360958
6363 1697 34 None -1 4 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 358 3 0 5 2.7 CC(N(C(=O)N1CCC(=CC1)c1nnn(c1C)c1cccnc1F)C)C 17360958
CHEMBL502882 1697 34 None -1 4 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 358 3 0 5 2.7 CC(N(C(=O)N1CCC(=CC1)c1nnn(c1C)c1cccnc1F)C)C 17360958
6343 971 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 352 2 1 6 2.6 COc1ccc(cc1)N1C=NC2C(C1=O)Sc1c2c2NCCc2cn1 17929793
73755209 971 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 352 2 1 6 2.6 COc1ccc(cc1)N1C=NC2C(C1=O)Sc1c2c2NCCc2cn1 17929793
11245287 1697 34 None -1 4 Rat 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 358 3 0 5 2.7 CC(N(C(=O)N1CCC(=CC1)c1nnn(c1C)c1cccnc1F)C)C 17360958
6363 1697 34 None -1 4 Rat 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 358 3 0 5 2.7 CC(N(C(=O)N1CCC(=CC1)c1nnn(c1C)c1cccnc1F)C)C 17360958
CHEMBL502882 1697 34 None -1 4 Rat 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 358 3 0 5 2.7 CC(N(C(=O)N1CCC(=CC1)c1nnn(c1C)c1cccnc1F)C)C 17360958
11530404 210 14 None -1 4 Rat 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 350 3 0 6 3.6 CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C 18054908
6211 210 14 None -1 4 Rat 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 350 3 0 6 3.6 CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C 18054908
CHEMBL385336 210 14 None -1 4 Rat 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 350 3 0 6 3.6 CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C 18054908
15985251 2558 33 None -1 2 Human 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 368 3 0 4 3.9 Fc1ccc(c(c1)F)n1nnc(c1C)c1ccc2c(c1)CN(C2=O)C(C)C 20524178
6335 2558 33 None -1 2 Human 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 368 3 0 4 3.9 Fc1ccc(c(c1)F)n1nnc(c1C)c1ccc2c(c1)CN(C2=O)C(C)C 20524178
CHEMBL579062 2558 33 None -1 2 Human 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 368 3 0 4 3.9 Fc1ccc(c(c1)F)n1nnc(c1C)c1ccc2c(c1)CN(C2=O)C(C)C 20524178
11530404 210 14 None 1 4 Human 8.5 pIC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 350 3 0 6 3.6 CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C 16279797
6211 210 14 None 1 4 Human 8.5 pIC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 350 3 0 6 3.6 CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C 16279797
CHEMBL385336 210 14 None 1 4 Human 8.5 pIC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 350 3 0 6 3.6 CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C 16279797
11772954 1034 0 None -1 2 Rat 8.5 pIC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 365 8 3 7 2.0 OCCOCCNc1ncc2c(c1)c(ncn2)NC1Cc2c(C1)cccc2 19289283
6349 1034 0 None -1 2 Rat 8.5 pIC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 365 8 3 7 2.0 OCCOCCNc1ncc2c(c1)c(ncn2)NC1Cc2c(C1)cccc2 19289283
CHEMBL469382 1034 0 None -1 2 Rat 8.5 pIC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 365 8 3 7 2.0 OCCOCCNc1ncc2c(c1)c(ncn2)NC1Cc2c(C1)cccc2 19289283
16659801 1036 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 370 1 1 7 3.5 Clc1ccc(cc1)n1cnc2c(c1=O)sc1c2c2NCCOc2cn1 17929793
6346 1036 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 370 1 1 7 3.5 Clc1ccc(cc1)n1cnc2c(c1=O)sc1c2c2NCCOc2cn1 17929793
CHEMBL236994 1036 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 370 1 1 7 3.5 Clc1ccc(cc1)n1cnc2c(c1=O)sc1c2c2NCCOc2cn1 17929793
11175501 885 40 None 1819 2 Human 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 349 3 0 5 2.9 O=C1N(Cc2c1ccc(c2)c1nnn(c1C)c1cccnc1F)C1CC1 19359526
6341 885 40 None 1819 2 Human 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 349 3 0 5 2.9 O=C1N(Cc2c1ccc(c2)c1nnn(c1C)c1cccnc1F)C1CC1 19359526
CHEMBL578995 885 40 None 1819 2 Human 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 349 3 0 5 2.9 O=C1N(Cc2c1ccc(c2)c1nnn(c1C)c1cccnc1F)C1CC1 19359526
16659967 1035 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 366 2 1 8 2.8 COc1ccc(cc1)n1cnc2c(c1=O)sc1c2c2NCCOc2cn1 17929793
6345 1035 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 366 2 1 8 2.8 COc1ccc(cc1)n1cnc2c(c1=O)sc1c2c2NCCOc2cn1 17929793
CHEMBL393922 1035 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 366 2 1 8 2.8 COc1ccc(cc1)n1cnc2c(c1=O)sc1c2c2NCCOc2cn1 17929793
16659803 1037 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 384 1 1 7 3.8 C[C@H]1CNc2c(O1)cnc1c2c2ncn(c(=O)c2s1)c1ccc(cc1)Cl 17929793
6338 1037 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 384 1 1 7 3.8 C[C@H]1CNc2c(O1)cnc1c2c2ncn(c(=O)c2s1)c1ccc(cc1)Cl 17929793
CHEMBL236180 1037 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 384 1 1 7 3.8 C[C@H]1CNc2c(O1)cnc1c2c2ncn(c(=O)c2s1)c1ccc(cc1)Cl 17929793
23634102 977 2 None - 1 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 362 4 1 7 3.0 C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)OC 19433355
6215 977 2 None - 1 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 362 4 1 7 3.0 C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)OC 19433355
CHEMBL1783876 977 2 None - 1 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 362 4 1 7 3.0 C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)OC 19433355
46866191 1044 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 324 1 2 8 1.9 Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(N)nc(n1)N 20346665
6209 1044 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 324 1 2 8 1.9 Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(N)nc(n1)N 20346665
CHEMBL1093560 1044 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 324 1 2 8 1.9 Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(N)nc(n1)N 20346665
16659802 1038 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 384 1 1 7 3.8 C[C@@H]1CNc2c(O1)cnc1c2c2ncn(c(=O)c2s1)c1ccc(cc1)Cl 17929793
6348 1038 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 384 1 1 7 3.8 C[C@@H]1CNc2c(O1)cnc1c2c2ncn(c(=O)c2s1)c1ccc(cc1)Cl 17929793
CHEMBL241327 1038 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 384 1 1 7 3.8 C[C@@H]1CNc2c(O1)cnc1c2c2ncn(c(=O)c2s1)c1ccc(cc1)Cl 17929793
11313361 2134 62 None 3 2 Human 8.9 pIC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 325 3 0 4 3.9 COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1 15555631
1385 2134 62 None 3 2 Human 8.9 pIC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 325 3 0 4 3.9 COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1 15555631
CHEMBL174588 2134 62 None 3 2 Human 8.9 pIC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 325 3 0 4 3.9 COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1 15555631
CHEMBL254574 2134 62 None 3 2 Human 8.9 pIC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 325 3 0 4 3.9 COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1 15555631
11559235 211 42 None 4 3 Rat 9.0 pIC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 343 2 0 7 2.6 CN(c1ccnc2c1c1ncn(c(=O)c1s2)N1CCCCCC1)C 16809035
11559235 211 42 None 4 3 Rat 9.0 pIC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 343 2 0 7 2.6 CN(c1ccnc2c1c1ncn(c(=O)c1s2)N1CCCCCC1)C 18054908
3953 211 42 None 4 3 Rat 9.0 pIC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 343 2 0 7 2.6 CN(c1ccnc2c1c1ncn(c(=O)c1s2)N1CCCCCC1)C 16809035
3953 211 42 None 4 3 Rat 9.0 pIC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 343 2 0 7 2.6 CN(c1ccnc2c1c1ncn(c(=O)c1s2)N1CCCCCC1)C 18054908
CHEMBL386565 211 42 None 4 3 Rat 9.0 pIC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 343 2 0 7 2.6 CN(c1ccnc2c1c1ncn(c(=O)c1s2)N1CCCCCC1)C 16809035
CHEMBL386565 211 42 None 4 3 Rat 9.0 pIC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 343 2 0 7 2.6 CN(c1ccnc2c1c1ncn(c(=O)c1s2)N1CCCCCC1)C 18054908
23634171 976 1 None - 1 Human 9.1 pIC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 366 3 1 6 3.7 C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)Cl 19433355
6214 976 1 None - 1 Human 9.1 pIC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 366 3 1 6 3.7 C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)Cl 19433355
CHEMBL1783874 976 1 None - 1 Human 9.1 pIC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 366 3 1 6 3.7 C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)Cl 19433355
1366 2080 45 None -1 3 Rat 4.9 pIC50 None 4.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 167 2 3 3 0.5 OC(=O)[C@H](c1cccc(c1)O)N 11080213
40428795 2080 45 None -1 3 Rat 4.9 pIC50 None 4.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 167 2 3 3 0.5 OC(=O)[C@H](c1cccc(c1)O)N 11080213
6604712 2080 45 None -1 3 Rat 4.9 pIC50 None 4.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 167 2 3 3 0.5 OC(=O)[C@H](c1cccc(c1)O)N 11080213
CHEMBL442347 2080 45 None -1 3 Rat 4.9 pIC50 None 4.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 167 2 3 3 0.5 OC(=O)[C@H](c1cccc(c1)O)N 11080213
1383 1449 1 None - 1 Rat 7.8 pIC50 None 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 309 5 1 4 3.8 CCCOC(=O)c1[nH]c(c(c1C)C(=O)O[C@H](C(C)(C)C)C)C 12470711
44431042 1449 1 None - 1 Rat 7.8 pIC50 None 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 309 5 1 4 3.8 CCCOC(=O)c1[nH]c(c(c1C)C(=O)O[C@H](C(C)(C)C)C)C 12470711
CHEMBL232052 1449 1 None - 1 Rat 7.8 pIC50 None 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 309 5 1 4 3.8 CCCOC(=O)c1[nH]c(c(c1C)C(=O)O[C@H](C(C)(C)C)C)C 12470711
10009 4049 40 None -1 3 Human 6.0 pKB = 6.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 445 3 1 4 5.1 Clc1cc(ccc1N1C(=O)c2c(C1=O)c(Cl)ccc2)NC(=O)c1ncccc1Cl 29514854
91885483 4049 40 None -1 3 Human 6.0 pKB = 6.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 445 3 1 4 5.1 Clc1cc(ccc1N1C(=O)c2c(C1=O)c(Cl)ccc2)NC(=O)c1ncccc1Cl 29514854
CHEMBL3628116 4049 40 None -1 3 Human 6.0 pKB = 6.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 445 3 1 4 5.1 Clc1cc(ccc1N1C(=O)c2c(C1=O)c(Cl)ccc2)NC(=O)c1ncccc1Cl 29514854


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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
Sel. page Similar-
ity		 Common
name		 GPCRdb
ID		 #Vendors

 Reference
ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 Assay
Type		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
52942855 17298 0 None - 0 Human 6.0 pEC50 = 6 Binding
Positive modulation of GluR1Positive modulation of GluR1
ChEMBL 441 6 2 6 2.8 NC(=O)c1c(NC(=O)Cn2cc(CN3CCC3)c(C(F)(F)F)n2)sc2c1CCCC2 10.1016/j.bmcl.2010.08.063
CHEMBL1257182 17298 0 None - 0 Human 6.0 pEC50 = 6 Binding
Positive modulation of GluR1Positive modulation of GluR1
ChEMBL 441 6 2 6 2.8 NC(=O)c1c(NC(=O)Cn2cc(CN3CCC3)c(C(F)(F)F)n2)sc2c1CCCC2 10.1016/j.bmcl.2010.08.063
44237734 17682 0 None - 0 Human 6.0 pEC50 = 6 Binding
Positive modulation of GluR1Positive modulation of GluR1
ChEMBL 427 4 3 6 2.2 NC(=O)c1c(NC(=O)Cn2nc(C(F)(F)F)c3c2CCNC3)sc2c1CCCC2 10.1016/j.bmcl.2010.08.063
CHEMBL1258461 17682 0 None - 0 Human 6.0 pEC50 = 6 Binding
Positive modulation of GluR1Positive modulation of GluR1
ChEMBL 427 4 3 6 2.2 NC(=O)c1c(NC(=O)Cn2nc(C(F)(F)F)c3c2CCNC3)sc2c1CCCC2 10.1016/j.bmcl.2010.08.063
1310 2315 110 None -4 18 Rat 5.0 pEC50 = 5 Binding
Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 1Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 1
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm020122x
1369 2315 110 None -4 18 Rat 5.0 pEC50 = 5 Binding
Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 1Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 1
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm020122x
33032 2315 110 None -4 18 Rat 5.0 pEC50 = 5 Binding
Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 1Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 1
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm020122x
44272391 2315 110 None -4 18 Rat 5.0 pEC50 = 5 Binding
Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 1Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 1
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm020122x
88747398 2315 110 None -4 18 Rat 5.0 pEC50 = 5 Binding
Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 1Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 1
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm020122x
CHEMBL575060 2315 110 None -4 18 Rat 5.0 pEC50 = 5 Binding
Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 1Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 1
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm020122x
DB00142 2315 110 None -4 18 Rat 5.0 pEC50 = 5 Binding
Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 1Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 1
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm020122x
139054390 204923 106 None - 5 Rat 5.0 pEC50 = 5 Binding
Effect on Metabotropic glutamate receptor 1Effect on Metabotropic glutamate receptor 1
ChEMBL 147 4 3 3 -0.7 N[C@H](CCC(=O)O)C(=O)O 10.1021/jm9703597
23327 204923 106 None - 5 Rat 5.0 pEC50 = 5 Binding
Effect on Metabotropic glutamate receptor 1Effect on Metabotropic glutamate receptor 1
ChEMBL 147 4 3 3 -0.7 N[C@H](CCC(=O)O)C(=O)O 10.1021/jm9703597
CHEMBL76232 204923 106 None - 5 Rat 5.0 pEC50 = 5 Binding
Effect on Metabotropic glutamate receptor 1Effect on Metabotropic glutamate receptor 1
ChEMBL 147 4 3 3 -0.7 N[C@H](CCC(=O)O)C(=O)O 10.1021/jm9703597
1310 2315 110 None -4 18 Rat 4.9 pEC50 = 4.9 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
1369 2315 110 None -4 18 Rat 4.9 pEC50 = 4.9 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
33032 2315 110 None -4 18 Rat 4.9 pEC50 = 4.9 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
44272391 2315 110 None -4 18 Rat 4.9 pEC50 = 4.9 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
88747398 2315 110 None -4 18 Rat 4.9 pEC50 = 4.9 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
CHEMBL575060 2315 110 None -4 18 Rat 4.9 pEC50 = 4.9 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
DB00142 2315 110 None -4 18 Rat 4.9 pEC50 = 4.9 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
49800187 17753 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Positive modulation of GluR1Positive modulation of GluR1
ChEMBL 415 6 3 6 2.3 CNCc1cn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(F)(F)F 10.1016/j.bmcl.2010.08.063
CHEMBL1258681 17753 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Positive modulation of GluR1Positive modulation of GluR1
ChEMBL 415 6 3 6 2.3 CNCc1cn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(F)(F)F 10.1016/j.bmcl.2010.08.063
1310 2315 110 None -4 18 Rat 4.9 pEC50 = 4.9 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1c in ratConcentration for half maximal activation of metabotropic glutamate mGluR1c in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
1369 2315 110 None -4 18 Rat 4.9 pEC50 = 4.9 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1c in ratConcentration for half maximal activation of metabotropic glutamate mGluR1c in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
33032 2315 110 None -4 18 Rat 4.9 pEC50 = 4.9 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1c in ratConcentration for half maximal activation of metabotropic glutamate mGluR1c in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
44272391 2315 110 None -4 18 Rat 4.9 pEC50 = 4.9 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1c in ratConcentration for half maximal activation of metabotropic glutamate mGluR1c in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
88747398 2315 110 None -4 18 Rat 4.9 pEC50 = 4.9 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1c in ratConcentration for half maximal activation of metabotropic glutamate mGluR1c in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
CHEMBL575060 2315 110 None -4 18 Rat 4.9 pEC50 = 4.9 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1c in ratConcentration for half maximal activation of metabotropic glutamate mGluR1c in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
DB00142 2315 110 None -4 18 Rat 4.9 pEC50 = 4.9 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1c in ratConcentration for half maximal activation of metabotropic glutamate mGluR1c in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
10338547 3340 26 None - 0 Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human mGlu1 receptor assessed as glutamate pEC50 at 10 uM (Rvb = 6.007 +/- 0.076 No_unit)Positive allosteric modulation of human mGlu1 receptor assessed as glutamate pEC50 at 10 uM (Rvb = 6.007 +/- 0.076 No_unit)
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 26 None - 0 Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human mGlu1 receptor assessed as glutamate pEC50 at 10 uM (Rvb = 6.007 +/- 0.076 No_unit)Positive allosteric modulation of human mGlu1 receptor assessed as glutamate pEC50 at 10 uM (Rvb = 6.007 +/- 0.076 No_unit)
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 26 None - 0 Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human mGlu1 receptor assessed as glutamate pEC50 at 10 uM (Rvb = 6.007 +/- 0.076 No_unit)Positive allosteric modulation of human mGlu1 receptor assessed as glutamate pEC50 at 10 uM (Rvb = 6.007 +/- 0.076 No_unit)
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 26 None - 0 Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human mGlu1 receptor assessed as glutamate EC50 at 10 uM (Rvb = 983.4 nM)Positive allosteric modulation of human mGlu1 receptor assessed as glutamate EC50 at 10 uM (Rvb = 983.4 nM)
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 26 None - 0 Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human mGlu1 receptor assessed as glutamate EC50 at 10 uM (Rvb = 983.4 nM)Positive allosteric modulation of human mGlu1 receptor assessed as glutamate EC50 at 10 uM (Rvb = 983.4 nM)
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 26 None - 0 Human 6.9 pEC50 = 6.9 Binding
Positive allosteric modulation of human mGlu1 receptor assessed as glutamate EC50 at 10 uM (Rvb = 983.4 nM)Positive allosteric modulation of human mGlu1 receptor assessed as glutamate EC50 at 10 uM (Rvb = 983.4 nM)
ChEMBL 360 2 1 4 4.6 O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F 10.1016/j.bmcl.2016.03.044
104766 33 42 None -26 11 Human 4.8 pEC50 = 4.8 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 1Compound was tested for the inhibition of Metabotropic glutamate receptor 1
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1021/jm970719q
1365 33 42 None -26 11 Human 4.8 pEC50 = 4.8 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 1Compound was tested for the inhibition of Metabotropic glutamate receptor 1
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1021/jm970719q
CHEMBL34453 33 42 None -26 11 Human 4.8 pEC50 = 4.8 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 1Compound was tested for the inhibition of Metabotropic glutamate receptor 1
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1021/jm970719q
52946206 17363 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Positive modulation of GluR1Positive modulation of GluR1
ChEMBL 429 7 3 6 3.1 CC(C)(C)c1nn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)cc1CNC1CC1 10.1016/j.bmcl.2010.08.063
CHEMBL1257414 17363 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Positive modulation of GluR1Positive modulation of GluR1
ChEMBL 429 7 3 6 3.1 CC(C)(C)c1nn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)cc1CNC1CC1 10.1016/j.bmcl.2010.08.063
52941383 17405 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Positive modulation of GluR1Positive modulation of GluR1
ChEMBL 431 7 3 6 3.4 CC(C)NCc1cn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(C)(C)C 10.1016/j.bmcl.2010.08.063
CHEMBL1257527 17405 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Positive modulation of GluR1Positive modulation of GluR1
ChEMBL 431 7 3 6 3.4 CC(C)NCc1cn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(C)(C)C 10.1016/j.bmcl.2010.08.063
52947461 17406 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Positive modulation of GluR1Positive modulation of GluR1
ChEMBL 429 7 3 6 2.7 CNCc1cn(CCC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(F)(F)F 10.1016/j.bmcl.2010.08.063
CHEMBL1257528 17406 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Positive modulation of GluR1Positive modulation of GluR1
ChEMBL 429 7 3 6 2.7 CNCc1cn(CCC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(F)(F)F 10.1016/j.bmcl.2010.08.063
52945583 17481 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Positive modulation of GluR1Positive modulation of GluR1
ChEMBL 429 6 3 6 2.6 CNCc1cn(CC(=O)Nc2sc3c(c2C(=O)NC)CCCC3)nc1C(F)(F)F 10.1016/j.bmcl.2010.08.063
CHEMBL1257768 17481 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Positive modulation of GluR1Positive modulation of GluR1
ChEMBL 429 6 3 6 2.6 CNCc1cn(CC(=O)Nc2sc3c(c2C(=O)NC)CCCC3)nc1C(F)(F)F 10.1016/j.bmcl.2010.08.063
52947637 17824 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Positive modulation of GluR1Positive modulation of GluR1
ChEMBL 459 9 3 7 2.3 COCCNCc1cn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(F)(F)F 10.1016/j.bmcl.2010.08.063
CHEMBL1258915 17824 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Positive modulation of GluR1Positive modulation of GluR1
ChEMBL 459 9 3 7 2.3 COCCNCc1cn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(F)(F)F 10.1016/j.bmcl.2010.08.063
1310 2315 110 None -1 18 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at human mGluR1 receptor expressed in HEK cellsAgonist activity at human mGluR1 receptor expressed in HEK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1039/C1MD00186H
1369 2315 110 None -1 18 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at human mGluR1 receptor expressed in HEK cellsAgonist activity at human mGluR1 receptor expressed in HEK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1039/C1MD00186H
33032 2315 110 None -1 18 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at human mGluR1 receptor expressed in HEK cellsAgonist activity at human mGluR1 receptor expressed in HEK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1039/C1MD00186H
44272391 2315 110 None -1 18 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at human mGluR1 receptor expressed in HEK cellsAgonist activity at human mGluR1 receptor expressed in HEK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1039/C1MD00186H
88747398 2315 110 None -1 18 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at human mGluR1 receptor expressed in HEK cellsAgonist activity at human mGluR1 receptor expressed in HEK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1039/C1MD00186H
CHEMBL575060 2315 110 None -1 18 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at human mGluR1 receptor expressed in HEK cellsAgonist activity at human mGluR1 receptor expressed in HEK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1039/C1MD00186H
DB00142 2315 110 None -1 18 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at human mGluR1 receptor expressed in HEK cellsAgonist activity at human mGluR1 receptor expressed in HEK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1039/C1MD00186H
10846649 101231 4 None - 0 Human 5.8 pEC50 = 5.8 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 1Compound was tested for the inhibition of Metabotropic glutamate receptor 1
ChEMBL 185 2 3 3 -0.5 N[C@@]1(C(=O)O)C[C@@H]2C[C@H]1[C@H]2C(=O)O 10.1021/jm970719q
CHEMBL296054 101231 4 None - 0 Human 5.8 pEC50 = 5.8 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 1Compound was tested for the inhibition of Metabotropic glutamate receptor 1
ChEMBL 185 2 3 3 -0.5 N[C@@]1(C(=O)O)C[C@@H]2C[C@H]1[C@H]2C(=O)O 10.1021/jm970719q
1370 3263 67 None 17 8 Rat 4.8 pEC50 = 4.8 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1b in humanConcentration for half maximal activation of metabotropic glutamate mGluR1b in human
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm00009a001
1372 3263 67 None 17 8 Rat 4.8 pEC50 = 4.8 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1b in humanConcentration for half maximal activation of metabotropic glutamate mGluR1b in human
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm00009a001
40539 3263 67 None 17 8 Rat 4.8 pEC50 = 4.8 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1b in humanConcentration for half maximal activation of metabotropic glutamate mGluR1b in human
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm00009a001
6971145 3263 67 None 17 8 Rat 4.8 pEC50 = 4.8 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1b in humanConcentration for half maximal activation of metabotropic glutamate mGluR1b in human
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm00009a001
CHEMBL279956 3263 67 None 17 8 Rat 4.8 pEC50 = 4.8 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1b in humanConcentration for half maximal activation of metabotropic glutamate mGluR1b in human
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm00009a001
DB02999 3263 67 None 17 8 Rat 4.8 pEC50 = 4.8 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1b in humanConcentration for half maximal activation of metabotropic glutamate mGluR1b in human
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm00009a001
127047993 139651 1 None - 0 Human 6.7 pEC50 = 6.7 Binding
Positive allosteric modulation of human mGlu1 receptor assessed as glutamate EC50 at 10 uM (Rvb = 983.4 nM)Positive allosteric modulation of human mGlu1 receptor assessed as glutamate EC50 at 10 uM (Rvb = 983.4 nM)
ChEMBL 333 2 1 5 3.9 N#Cc1csc(NC(=O)C2c3ccccc3Oc3ccccc32)n1 10.1016/j.bmcl.2016.03.044
CHEMBL3797793 139651 1 None - 0 Human 6.7 pEC50 = 6.7 Binding
Positive allosteric modulation of human mGlu1 receptor assessed as glutamate EC50 at 10 uM (Rvb = 983.4 nM)Positive allosteric modulation of human mGlu1 receptor assessed as glutamate EC50 at 10 uM (Rvb = 983.4 nM)
ChEMBL 333 2 1 5 3.9 N#Cc1csc(NC(=O)C2c3ccccc3Oc3ccccc32)n1 10.1016/j.bmcl.2016.03.044
127047993 139651 1 None - 0 Human 6.7 pEC50 = 6.7 Binding
Positive allosteric modulation of human mGlu1 receptor assessed as glutamate pEC50 at 10 uM (Rvb = 6.007 +/- 0.076 No_unit)Positive allosteric modulation of human mGlu1 receptor assessed as glutamate pEC50 at 10 uM (Rvb = 6.007 +/- 0.076 No_unit)
ChEMBL 333 2 1 5 3.9 N#Cc1csc(NC(=O)C2c3ccccc3Oc3ccccc32)n1 10.1016/j.bmcl.2016.03.044
CHEMBL3797793 139651 1 None - 0 Human 6.7 pEC50 = 6.7 Binding
Positive allosteric modulation of human mGlu1 receptor assessed as glutamate pEC50 at 10 uM (Rvb = 6.007 +/- 0.076 No_unit)Positive allosteric modulation of human mGlu1 receptor assessed as glutamate pEC50 at 10 uM (Rvb = 6.007 +/- 0.076 No_unit)
ChEMBL 333 2 1 5 3.9 N#Cc1csc(NC(=O)C2c3ccccc3Oc3ccccc32)n1 10.1016/j.bmcl.2016.03.044
52949928 17445 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Positive modulation of GluR1Positive modulation of GluR1
ChEMBL 471 9 2 6 3.8 CCN(CC)Cc1cn(CCC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(F)(F)F 10.1016/j.bmcl.2010.08.063
CHEMBL1257646 17445 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Positive modulation of GluR1Positive modulation of GluR1
ChEMBL 471 9 2 6 3.8 CCN(CC)Cc1cn(CCC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(F)(F)F 10.1016/j.bmcl.2010.08.063
1370 3263 67 None 17 8 Rat 6.7 pEC50 = 6.7 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm00009a001
1372 3263 67 None 17 8 Rat 6.7 pEC50 = 6.7 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm00009a001
40539 3263 67 None 17 8 Rat 6.7 pEC50 = 6.7 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm00009a001
6971145 3263 67 None 17 8 Rat 6.7 pEC50 = 6.7 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm00009a001
CHEMBL279956 3263 67 None 17 8 Rat 6.7 pEC50 = 6.7 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm00009a001
DB02999 3263 67 None 17 8 Rat 6.7 pEC50 = 6.7 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm00009a001
1370 3263 67 None -66 8 Human 6.7 pEC50 = 6.7 Binding
Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm9601718
1372 3263 67 None -66 8 Human 6.7 pEC50 = 6.7 Binding
Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm9601718
40539 3263 67 None -66 8 Human 6.7 pEC50 = 6.7 Binding
Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm9601718
6971145 3263 67 None -66 8 Human 6.7 pEC50 = 6.7 Binding
Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm9601718
CHEMBL279956 3263 67 None -66 8 Human 6.7 pEC50 = 6.7 Binding
Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm9601718
DB02999 3263 67 None -66 8 Human 6.7 pEC50 = 6.7 Binding
Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm9601718
127046038 139941 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Positive allosteric modulation of human mGlu1 receptor assessed as glutamate pEC50 at 10 uM (Rvb = 6.007 +/- 0.076 No_unit)Positive allosteric modulation of human mGlu1 receptor assessed as glutamate pEC50 at 10 uM (Rvb = 6.007 +/- 0.076 No_unit)
ChEMBL 350 3 1 4 5.1 CC(C)c1csc(NC(=O)C2c3ccccc3Oc3ccccc32)n1 10.1016/j.bmcl.2016.03.044
CHEMBL3799685 139941 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Positive allosteric modulation of human mGlu1 receptor assessed as glutamate pEC50 at 10 uM (Rvb = 6.007 +/- 0.076 No_unit)Positive allosteric modulation of human mGlu1 receptor assessed as glutamate pEC50 at 10 uM (Rvb = 6.007 +/- 0.076 No_unit)
ChEMBL 350 3 1 4 5.1 CC(C)c1csc(NC(=O)C2c3ccccc3Oc3ccccc32)n1 10.1016/j.bmcl.2016.03.044
127046038 139941 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Positive allosteric modulation of human mGlu1 receptor assessed as glutamate EC50 at 10 uM (Rvb = 983.4 nM)Positive allosteric modulation of human mGlu1 receptor assessed as glutamate EC50 at 10 uM (Rvb = 983.4 nM)
ChEMBL 350 3 1 4 5.1 CC(C)c1csc(NC(=O)C2c3ccccc3Oc3ccccc32)n1 10.1016/j.bmcl.2016.03.044
CHEMBL3799685 139941 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Positive allosteric modulation of human mGlu1 receptor assessed as glutamate EC50 at 10 uM (Rvb = 983.4 nM)Positive allosteric modulation of human mGlu1 receptor assessed as glutamate EC50 at 10 uM (Rvb = 983.4 nM)
ChEMBL 350 3 1 4 5.1 CC(C)c1csc(NC(=O)C2c3ccccc3Oc3ccccc32)n1 10.1016/j.bmcl.2016.03.044
104766 33 42 None 3 11 Rat 4.7 pEC50 = 4.7 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1021/jm00009a001
1365 33 42 None 3 11 Rat 4.7 pEC50 = 4.7 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1021/jm00009a001
CHEMBL34453 33 42 None 3 11 Rat 4.7 pEC50 = 4.7 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1021/jm00009a001
104766 33 42 None -26 11 Human 4.7 pEC50 = 4.7 Binding
Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1021/jm9601718
1365 33 42 None -26 11 Human 4.7 pEC50 = 4.7 Binding
Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1021/jm9601718
CHEMBL34453 33 42 None -26 11 Human 4.7 pEC50 = 4.7 Binding
Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1021/jm9601718
1370 3263 67 None 17 8 Rat 5.6 pEC50 = 5.6 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1b in ratConcentration for half maximal activation of metabotropic glutamate mGluR1b in rat
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm00009a001
1372 3263 67 None 17 8 Rat 5.6 pEC50 = 5.6 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1b in ratConcentration for half maximal activation of metabotropic glutamate mGluR1b in rat
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm00009a001
40539 3263 67 None 17 8 Rat 5.6 pEC50 = 5.6 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1b in ratConcentration for half maximal activation of metabotropic glutamate mGluR1b in rat
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm00009a001
6971145 3263 67 None 17 8 Rat 5.6 pEC50 = 5.6 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1b in ratConcentration for half maximal activation of metabotropic glutamate mGluR1b in rat
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm00009a001
CHEMBL279956 3263 67 None 17 8 Rat 5.6 pEC50 = 5.6 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1b in ratConcentration for half maximal activation of metabotropic glutamate mGluR1b in rat
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm00009a001
DB02999 3263 67 None 17 8 Rat 5.6 pEC50 = 5.6 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1b in ratConcentration for half maximal activation of metabotropic glutamate mGluR1b in rat
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm00009a001
46947824 16481 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Positive modulation of GluR1Positive modulation of GluR1
ChEMBL 495 5 3 6 3.5 O=C(Cn1nc(C(F)(F)F)c2c1CCCC2)Nc1sc2c(c1C(=O)N[C@@H]1CCNC1)CCCC2 10.1016/j.bmcl.2010.08.063
CHEMBL1234889 16481 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Positive modulation of GluR1Positive modulation of GluR1
ChEMBL 495 5 3 6 3.5 O=C(Cn1nc(C(F)(F)F)c2c1CCCC2)Nc1sc2c(c1C(=O)N[C@@H]1CCNC1)CCCC2 10.1016/j.bmcl.2010.08.063
52945134 17718 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Positive modulation of GluR1Positive modulation of GluR1
ChEMBL 413 4 2 5 3.9 O=C(Cn1nc(C(F)(F)F)c2c1CCCC2)Nc1sc2c(c1CO)CCCC2 10.1016/j.bmcl.2010.08.063
CHEMBL1258570 17718 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Positive modulation of GluR1Positive modulation of GluR1
ChEMBL 413 4 2 5 3.9 O=C(Cn1nc(C(F)(F)F)c2c1CCCC2)Nc1sc2c(c1CO)CCCC2 10.1016/j.bmcl.2010.08.063
52948725 17444 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Positive modulation of GluR1Positive modulation of GluR1
ChEMBL 443 8 3 6 3.1 CCNCc1cn(CCC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(F)(F)F 10.1016/j.bmcl.2010.08.063
CHEMBL1257645 17444 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Positive modulation of GluR1Positive modulation of GluR1
ChEMBL 443 8 3 6 3.1 CCNCc1cn(CCC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(F)(F)F 10.1016/j.bmcl.2010.08.063
118718092 120595 0 None - 1 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at human mGluR1 receptor expressed in HEK cellsAgonist activity at human mGluR1 receptor expressed in HEK cells
ChEMBL 215 3 3 6 -0.4 N[C@]1(C(=O)O)C[C@H]1Cc1nsnc1O 10.1039/C1MD00186H
CHEMBL3347672 120595 0 None - 1 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at human mGluR1 receptor expressed in HEK cellsAgonist activity at human mGluR1 receptor expressed in HEK cells
ChEMBL 215 3 3 6 -0.4 N[C@]1(C(=O)O)C[C@H]1Cc1nsnc1O 10.1039/C1MD00186H
CHEMBL3545861 120595 0 None - 1 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at human mGluR1 receptor expressed in HEK cellsAgonist activity at human mGluR1 receptor expressed in HEK cells
ChEMBL 215 3 3 6 -0.4 N[C@]1(C(=O)O)C[C@H]1Cc1nsnc1O 10.1039/C1MD00186H
46870038 16480 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Positive modulation of GluR1Positive modulation of GluR1
ChEMBL 403 6 3 6 2.6 CNCc1cn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(C)(C)C 10.1016/j.bmcl.2010.08.063
CHEMBL1234888 16480 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Positive modulation of GluR1Positive modulation of GluR1
ChEMBL 403 6 3 6 2.6 CNCc1cn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(C)(C)C 10.1016/j.bmcl.2010.08.063
24967422 17328 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Positive modulation of GluR1Positive modulation of GluR1
ChEMBL 417 6 2 6 2.9 CN(C)Cc1cn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(C)(C)C 10.1016/j.bmcl.2010.08.063
CHEMBL1257298 17328 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Positive modulation of GluR1Positive modulation of GluR1
ChEMBL 417 6 2 6 2.9 CN(C)Cc1cn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(C)(C)C 10.1016/j.bmcl.2010.08.063
52942778 17792 0 None - 0 Human 5.5 pEC50 = 5.5 Binding
Positive modulation of GluR1Positive modulation of GluR1
ChEMBL 443 7 3 6 3.1 CC(C)NCc1cn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(F)(F)F 10.1016/j.bmcl.2010.08.063
CHEMBL1258796 17792 0 None - 0 Human 5.5 pEC50 = 5.5 Binding
Positive modulation of GluR1Positive modulation of GluR1
ChEMBL 443 7 3 6 3.1 CC(C)NCc1cn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(F)(F)F 10.1016/j.bmcl.2010.08.063
6603885 102201 23 None - 0 Rat 4.5 pEC50 = 4.5 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat
ChEMBL 158 2 3 5 -0.5 N[C@H](C(=O)O)c1cc(O)no1 10.1021/jm00009a001
6971208 102201 23 None - 0 Rat 4.5 pEC50 = 4.5 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat
ChEMBL 158 2 3 5 -0.5 N[C@H](C(=O)O)c1cc(O)no1 10.1021/jm00009a001
CHEMBL30285 102201 23 None - 0 Rat 4.5 pEC50 = 4.5 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat
ChEMBL 158 2 3 5 -0.5 N[C@H](C(=O)O)c1cc(O)no1 10.1021/jm00009a001
6603885 102201 23 None - 0 Rat 4.4 pEC50 = 4.4 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1b in ratConcentration for half maximal activation of metabotropic glutamate mGluR1b in rat
ChEMBL 158 2 3 5 -0.5 N[C@H](C(=O)O)c1cc(O)no1 10.1021/jm00009a001
6971208 102201 23 None - 0 Rat 4.4 pEC50 = 4.4 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1b in ratConcentration for half maximal activation of metabotropic glutamate mGluR1b in rat
ChEMBL 158 2 3 5 -0.5 N[C@H](C(=O)O)c1cc(O)no1 10.1021/jm00009a001
CHEMBL30285 102201 23 None - 0 Rat 4.4 pEC50 = 4.4 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1b in ratConcentration for half maximal activation of metabotropic glutamate mGluR1b in rat
ChEMBL 158 2 3 5 -0.5 N[C@H](C(=O)O)c1cc(O)no1 10.1021/jm00009a001
1310 2315 110 None -1 18 Human 5.3 pEC50 = 5.3 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 1Compound was tested for the inhibition of Metabotropic glutamate receptor 1
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm970719q
1369 2315 110 None -1 18 Human 5.3 pEC50 = 5.3 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 1Compound was tested for the inhibition of Metabotropic glutamate receptor 1
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm970719q
33032 2315 110 None -1 18 Human 5.3 pEC50 = 5.3 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 1Compound was tested for the inhibition of Metabotropic glutamate receptor 1
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm970719q
44272391 2315 110 None -1 18 Human 5.3 pEC50 = 5.3 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 1Compound was tested for the inhibition of Metabotropic glutamate receptor 1
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm970719q
88747398 2315 110 None -1 18 Human 5.3 pEC50 = 5.3 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 1Compound was tested for the inhibition of Metabotropic glutamate receptor 1
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm970719q
CHEMBL575060 2315 110 None -1 18 Human 5.3 pEC50 = 5.3 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 1Compound was tested for the inhibition of Metabotropic glutamate receptor 1
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm970719q
DB00142 2315 110 None -1 18 Human 5.3 pEC50 = 5.3 Binding
Compound was tested for the inhibition of Metabotropic glutamate receptor 1Compound was tested for the inhibition of Metabotropic glutamate receptor 1
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm970719q
104766 33 42 None 3 11 Rat 4.3 pEC50 = 4.3 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1021/jm00009a001
1365 33 42 None 3 11 Rat 4.3 pEC50 = 4.3 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1021/jm00009a001
CHEMBL34453 33 42 None 3 11 Rat 4.3 pEC50 = 4.3 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat
ChEMBL 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 10.1021/jm00009a001
52947627 17791 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Positive modulation of GluR1Positive modulation of GluR1
ChEMBL 429 6 2 6 2.6 CN(C)Cc1cn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(F)(F)F 10.1016/j.bmcl.2010.08.063
CHEMBL1258795 17791 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Positive modulation of GluR1Positive modulation of GluR1
ChEMBL 429 6 2 6 2.6 CN(C)Cc1cn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(F)(F)F 10.1016/j.bmcl.2010.08.063
1310 2315 110 None -4 18 Rat 4.3 pEC50 = 4.3 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1b in ratConcentration for half maximal activation of metabotropic glutamate mGluR1b in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
1369 2315 110 None -4 18 Rat 4.3 pEC50 = 4.3 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1b in ratConcentration for half maximal activation of metabotropic glutamate mGluR1b in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
33032 2315 110 None -4 18 Rat 4.3 pEC50 = 4.3 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1b in ratConcentration for half maximal activation of metabotropic glutamate mGluR1b in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
44272391 2315 110 None -4 18 Rat 4.3 pEC50 = 4.3 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1b in ratConcentration for half maximal activation of metabotropic glutamate mGluR1b in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
88747398 2315 110 None -4 18 Rat 4.3 pEC50 = 4.3 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1b in ratConcentration for half maximal activation of metabotropic glutamate mGluR1b in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
CHEMBL575060 2315 110 None -4 18 Rat 4.3 pEC50 = 4.3 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1b in ratConcentration for half maximal activation of metabotropic glutamate mGluR1b in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
DB00142 2315 110 None -4 18 Rat 4.3 pEC50 = 4.3 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1b in ratConcentration for half maximal activation of metabotropic glutamate mGluR1b in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
6603885 102201 23 None - 0 Rat 5.2 pEC50 = 5.2 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat
ChEMBL 158 2 3 5 -0.5 N[C@H](C(=O)O)c1cc(O)no1 10.1021/jm00009a001
6971208 102201 23 None - 0 Rat 5.2 pEC50 = 5.2 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat
ChEMBL 158 2 3 5 -0.5 N[C@H](C(=O)O)c1cc(O)no1 10.1021/jm00009a001
CHEMBL30285 102201 23 None - 0 Rat 5.2 pEC50 = 5.2 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat
ChEMBL 158 2 3 5 -0.5 N[C@H](C(=O)O)c1cc(O)no1 10.1021/jm00009a001
6603885 102201 23 None - 0 Human 5.2 pEC50 = 5.2 Binding
Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)
ChEMBL 158 2 3 5 -0.5 N[C@H](C(=O)O)c1cc(O)no1 10.1021/jm9601718
6971208 102201 23 None - 0 Human 5.2 pEC50 = 5.2 Binding
Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)
ChEMBL 158 2 3 5 -0.5 N[C@H](C(=O)O)c1cc(O)no1 10.1021/jm9601718
CHEMBL30285 102201 23 None - 0 Human 5.2 pEC50 = 5.2 Binding
Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)
ChEMBL 158 2 3 5 -0.5 N[C@H](C(=O)O)c1cc(O)no1 10.1021/jm9601718
6603885 102201 23 None - 0 Rat 4.2 pEC50 = 4.2 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1c in ratConcentration for half maximal activation of metabotropic glutamate mGluR1c in rat
ChEMBL 158 2 3 5 -0.5 N[C@H](C(=O)O)c1cc(O)no1 10.1021/jm00009a001
6971208 102201 23 None - 0 Rat 4.2 pEC50 = 4.2 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1c in ratConcentration for half maximal activation of metabotropic glutamate mGluR1c in rat
ChEMBL 158 2 3 5 -0.5 N[C@H](C(=O)O)c1cc(O)no1 10.1021/jm00009a001
CHEMBL30285 102201 23 None - 0 Rat 4.2 pEC50 = 4.2 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1c in ratConcentration for half maximal activation of metabotropic glutamate mGluR1c in rat
ChEMBL 158 2 3 5 -0.5 N[C@H](C(=O)O)c1cc(O)no1 10.1021/jm00009a001
45082292 115251 2 None 3 3 Human 5.2 pEC50 = 5.2 Binding
Agonist activity at human mGluR1 receptor expressed in HEK cellsAgonist activity at human mGluR1 receptor expressed in HEK cells
ChEMBL 159 3 3 3 -0.7 N[C@@]1(C(=O)O)C[C@@H]1CC(=O)O 10.1039/C1MD00186H
CHEMBL3347670 115251 2 None 3 3 Human 5.2 pEC50 = 5.2 Binding
Agonist activity at human mGluR1 receptor expressed in HEK cellsAgonist activity at human mGluR1 receptor expressed in HEK cells
ChEMBL 159 3 3 3 -0.7 N[C@@]1(C(=O)O)C[C@@H]1CC(=O)O 10.1039/C1MD00186H
52949785 17297 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Positive modulation of GluR1Positive modulation of GluR1
ChEMBL 457 8 2 6 3.4 CCN(CC)Cc1cn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(F)(F)F 10.1016/j.bmcl.2010.08.063
CHEMBL1257181 17297 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Positive modulation of GluR1Positive modulation of GluR1
ChEMBL 457 8 2 6 3.4 CCN(CC)Cc1cn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(F)(F)F 10.1016/j.bmcl.2010.08.063
52946415 17823 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Positive modulation of GluR1Positive modulation of GluR1
ChEMBL 441 7 3 6 2.8 NC(=O)c1c(NC(=O)Cn2cc(CNC3CC3)c(C(F)(F)F)n2)sc2c1CCCC2 10.1016/j.bmcl.2010.08.063
CHEMBL1258914 17823 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Positive modulation of GluR1Positive modulation of GluR1
ChEMBL 441 7 3 6 2.8 NC(=O)c1c(NC(=O)Cn2cc(CNC3CC3)c(C(F)(F)F)n2)sc2c1CCCC2 10.1016/j.bmcl.2010.08.063
1366 2080 45 None - 0 Human 4.2 pEC50 = 4.2 Binding
Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)
ChEMBL 167 2 3 3 0.5 OC(=O)[C@H](c1cccc(c1)O)N 10.1021/jm9601718
40428795 2080 45 None - 0 Human 4.2 pEC50 = 4.2 Binding
Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)
ChEMBL 167 2 3 3 0.5 OC(=O)[C@H](c1cccc(c1)O)N 10.1021/jm9601718
6604712 2080 45 None - 0 Human 4.2 pEC50 = 4.2 Binding
Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)
ChEMBL 167 2 3 3 0.5 OC(=O)[C@H](c1cccc(c1)O)N 10.1021/jm9601718
CHEMBL442347 2080 45 None - 0 Human 4.2 pEC50 = 4.2 Binding
Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)
ChEMBL 167 2 3 3 0.5 OC(=O)[C@H](c1cccc(c1)O)N 10.1021/jm9601718
1370 3263 67 None 17 8 Rat 6.2 pEC50 = 6.2 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm00009a001
1372 3263 67 None 17 8 Rat 6.2 pEC50 = 6.2 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm00009a001
40539 3263 67 None 17 8 Rat 6.2 pEC50 = 6.2 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm00009a001
6971145 3263 67 None 17 8 Rat 6.2 pEC50 = 6.2 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm00009a001
CHEMBL279956 3263 67 None 17 8 Rat 6.2 pEC50 = 6.2 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm00009a001
DB02999 3263 67 None 17 8 Rat 6.2 pEC50 = 6.2 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm00009a001
1370 3263 67 None 17 8 Rat 6.1 pEC50 = 6.1 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1c in ratConcentration for half maximal activation of metabotropic glutamate mGluR1c in rat
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm00009a001
1372 3263 67 None 17 8 Rat 6.1 pEC50 = 6.1 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1c in ratConcentration for half maximal activation of metabotropic glutamate mGluR1c in rat
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm00009a001
40539 3263 67 None 17 8 Rat 6.1 pEC50 = 6.1 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1c in ratConcentration for half maximal activation of metabotropic glutamate mGluR1c in rat
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm00009a001
6971145 3263 67 None 17 8 Rat 6.1 pEC50 = 6.1 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1c in ratConcentration for half maximal activation of metabotropic glutamate mGluR1c in rat
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm00009a001
CHEMBL279956 3263 67 None 17 8 Rat 6.1 pEC50 = 6.1 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1c in ratConcentration for half maximal activation of metabotropic glutamate mGluR1c in rat
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm00009a001
DB02999 3263 67 None 17 8 Rat 6.1 pEC50 = 6.1 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1c in ratConcentration for half maximal activation of metabotropic glutamate mGluR1c in rat
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm00009a001
24967783 16479 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Positive modulation of GluR1Positive modulation of GluR1
ChEMBL 429 7 3 6 2.7 CCNCc1cn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(F)(F)F 10.1016/j.bmcl.2010.08.063
CHEMBL1234887 16479 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Positive modulation of GluR1Positive modulation of GluR1
ChEMBL 429 7 3 6 2.7 CCNCc1cn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(F)(F)F 10.1016/j.bmcl.2010.08.063
52943768 17364 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Positive modulation of GluR1Positive modulation of GluR1
ChEMBL 417 7 3 6 3.0 CCNCc1cn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(C)(C)C 10.1016/j.bmcl.2010.08.063
CHEMBL1257415 17364 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Positive modulation of GluR1Positive modulation of GluR1
ChEMBL 417 7 3 6 3.0 CCNCc1cn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(C)(C)C 10.1016/j.bmcl.2010.08.063
52941496 17719 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Positive modulation of GluR1Positive modulation of GluR1
ChEMBL 401 5 3 6 2.0 NCc1cn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(F)(F)F 10.1016/j.bmcl.2010.08.063
CHEMBL1258571 17719 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Positive modulation of GluR1Positive modulation of GluR1
ChEMBL 401 5 3 6 2.0 NCc1cn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(F)(F)F 10.1016/j.bmcl.2010.08.063
1310 2315 110 None -4 18 Rat 5.1 pEC50 = 5.1 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
1369 2315 110 None -4 18 Rat 5.1 pEC50 = 5.1 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
33032 2315 110 None -4 18 Rat 5.1 pEC50 = 5.1 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
44272391 2315 110 None -4 18 Rat 5.1 pEC50 = 5.1 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
88747398 2315 110 None -4 18 Rat 5.1 pEC50 = 5.1 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
CHEMBL575060 2315 110 None -4 18 Rat 5.1 pEC50 = 5.1 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
DB00142 2315 110 None -4 18 Rat 5.1 pEC50 = 5.1 Binding
Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm00009a001
22708855 146374 1 None - 0 Human 5.0 pEC50 = 5.0 Binding
Compound was tested for inhibitory binding activity towards metabotropic glutamate receptor (mGluRla) expressed in LLC-PK1 cellsCompound was tested for inhibitory binding activity towards metabotropic glutamate receptor (mGluRla) expressed in LLC-PK1 cells
ChEMBL 199 2 3 3 -0.1 NC1(C(=O)O)CC2CCC1C2C(=O)O 10.1016/0960-894X(95)00457-5
CHEMBL39215 146374 1 None - 0 Human 5.0 pEC50 = 5.0 Binding
Compound was tested for inhibitory binding activity towards metabotropic glutamate receptor (mGluRla) expressed in LLC-PK1 cellsCompound was tested for inhibitory binding activity towards metabotropic glutamate receptor (mGluRla) expressed in LLC-PK1 cells
ChEMBL 199 2 3 3 -0.1 NC1(C(=O)O)CC2CCC1C2C(=O)O 10.1016/0960-894X(95)00457-5
11313361 2134 62 None - 1 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 325 3 0 4 3.9 COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1 10.1021/jm049499o
1385 2134 62 None - 1 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 325 3 0 4 3.9 COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1 10.1021/jm049499o
CHEMBL174588 2134 62 None - 1 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 325 3 0 4 3.9 COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1 10.1021/jm049499o
CHEMBL254574 2134 62 None - 1 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 325 3 0 4 3.9 COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1 10.1021/jm049499o
11483690 63006 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 309 3 0 3 4.1 CO[C@H]1CC[C@@H](C(=O)c2ccc3nc4c(cc3c2)CCC4)CC1 10.1021/jm049499o
CHEMBL178690 63006 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 309 3 0 3 4.1 CO[C@H]1CC[C@@H](C(=O)c2ccc3nc4c(cc3c2)CCC4)CC1 10.1021/jm049499o
11537456 209 12 None - 1 Rat 9.0 pIC50 = 9 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 342 2 0 6 4.0 CN(c1ccnc2c1c1ncn(c(=O)c1s2)C1CCCCCC1)C 10.1016/j.ejmech.2007.06.024
6354 209 12 None - 1 Rat 9.0 pIC50 = 9 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 342 2 0 6 4.0 CN(c1ccnc2c1c1ncn(c(=O)c1s2)C1CCCCCC1)C 10.1016/j.ejmech.2007.06.024
CHEMBL225032 209 12 None - 1 Rat 9.0 pIC50 = 9 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 342 2 0 6 4.0 CN(c1ccnc2c1c1ncn(c(=O)c1s2)C1CCCCCC1)C 10.1016/j.ejmech.2007.06.024
11461116 78928 0 None - 0 Human 9.0 pIC50 = 9 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 312 4 1 4 3.8 CCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1N 10.1021/jm049499o
CHEMBL2112967 78928 0 None - 0 Human 9.0 pIC50 = 9 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 312 4 1 4 3.8 CCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1N 10.1021/jm049499o
11301185 1683 32 None - 1 Mouse 8.9 pIC50 = 8.9 Binding
Binding affinity to mouse mGluR1Binding affinity to mouse mGluR1
ChEMBL 305 2 0 5 3.3 Cc1c(nnn1c1cccnc1F)c1ccc2c(c1)cccn2 10.1016/j.bmc.2010.11.048
6353 1683 32 None - 1 Mouse 8.9 pIC50 = 8.9 Binding
Binding affinity to mouse mGluR1Binding affinity to mouse mGluR1
ChEMBL 305 2 0 5 3.3 Cc1c(nnn1c1cccnc1F)c1ccc2c(c1)cccn2 10.1016/j.bmc.2010.11.048
CHEMBL1645352 1683 32 None - 1 Mouse 8.9 pIC50 = 8.9 Binding
Binding affinity to mouse mGluR1Binding affinity to mouse mGluR1
ChEMBL 305 2 0 5 3.3 Cc1c(nnn1c1cccnc1F)c1ccc2c(c1)cccn2 10.1016/j.bmc.2010.11.048
11559235 211 42 None - 0 Rat 8.0 pIC50 = 8 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 343 2 0 7 2.6 CN(c1ccnc2c1c1ncn(c(=O)c1s2)N1CCCCCC1)C 10.1016/j.ejmech.2007.06.024
3953 211 42 None - 0 Rat 8.0 pIC50 = 8 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 343 2 0 7 2.6 CN(c1ccnc2c1c1ncn(c(=O)c1s2)N1CCCCCC1)C 10.1016/j.ejmech.2007.06.024
CHEMBL386565 211 42 None - 0 Rat 8.0 pIC50 = 8 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 343 2 0 7 2.6 CN(c1ccnc2c1c1ncn(c(=O)c1s2)N1CCCCCC1)C 10.1016/j.ejmech.2007.06.024
10085578 62110 1 None - 0 Rat 8.0 pIC50 = 8 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 289 4 0 2 4.5 CCc1cc2cc(C(=O)Cc3ccccc3)ccc2nc1C 10.1021/jm049499o
CHEMBL177586 62110 1 None - 0 Rat 8.0 pIC50 = 8 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 289 4 0 2 4.5 CCc1cc2cc(C(=O)Cc3ccccc3)ccc2nc1C 10.1021/jm049499o
44306937 101030 3 None - 0 Rat 7.0 pIC50 = 7 Binding
In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.
ChEMBL 281 2 1 4 3.2 Cc1c(C(=O)OC(C)(C)C)c[nH]c1C(=O)OC(C)(C)C 10.1016/s0960-894x(03)00396-2
CHEMBL294550 101030 3 None - 0 Rat 7.0 pIC50 = 7 Binding
In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.
ChEMBL 281 2 1 4 3.2 Cc1c(C(=O)OC(C)(C)C)c[nH]c1C(=O)OC(C)(C)C 10.1016/s0960-894x(03)00396-2
44430067 151902 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibition of recombinant mGluR1a receptor expressed in CHO cellsInhibition of recombinant mGluR1a receptor expressed in CHO cells
ChEMBL 305 4 1 4 3.2 CCOC(=O)c1[nH]c(C)c(C(=O)OC2CC3CCC2C3)c1C 10.1016/j.bmcl.2006.11.039
CHEMBL396594 151902 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibition of recombinant mGluR1a receptor expressed in CHO cellsInhibition of recombinant mGluR1a receptor expressed in CHO cells
ChEMBL 305 4 1 4 3.2 CCOC(=O)c1[nH]c(C)c(C(=O)OC2CC3CCC2C3)c1C 10.1016/j.bmcl.2006.11.039
11654379 142071 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 406 6 0 6 5.0 CCCCc1nc2c(sc3nccc(N(C)C)c32)c(=O)n1-c1ccc(CC)cc1 10.1016/j.ejmech.2007.06.024
CHEMBL387976 142071 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 406 6 0 6 5.0 CCCCc1nc2c(sc3nccc(N(C)C)c32)c(=O)n1-c1ccc(CC)cc1 10.1016/j.ejmech.2007.06.024
44306721 203578 0 None - 0 Rat 6.0 pIC50 = 6 Binding
In vitro inhibitory concentration required against rat mGluR1a in CHO cells using the CDP-DAG accumulation methodIn vitro inhibitory concentration required against rat mGluR1a in CHO cells using the CDP-DAG accumulation method
ChEMBL 295 4 0 5 3.2 CCCOC(=O)c1c(C)c(C(=O)OC(C)(C)C)c(C)n1C 10.1016/s0960-894x(03)00396-2
CHEMBL66794 203578 0 None - 0 Rat 6.0 pIC50 = 6 Binding
In vitro inhibitory concentration required against rat mGluR1a in CHO cells using the CDP-DAG accumulation methodIn vitro inhibitory concentration required against rat mGluR1a in CHO cells using the CDP-DAG accumulation method
ChEMBL 295 4 0 5 3.2 CCCOC(=O)c1c(C)c(C(=O)OC(C)(C)C)c(C)n1C 10.1016/s0960-894x(03)00396-2
44430068 87927 0 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibition of recombinant mGluR1a receptor expressed in CHO cellsInhibition of recombinant mGluR1a receptor expressed in CHO cells
ChEMBL 389 8 3 4 2.6 CC(=O)NCCCCNC(=O)c1[nH]c(C)c(C(=O)OC2CC3CCC2C3)c1C 10.1016/j.bmcl.2006.11.039
CHEMBL233914 87927 0 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibition of recombinant mGluR1a receptor expressed in CHO cellsInhibition of recombinant mGluR1a receptor expressed in CHO cells
ChEMBL 389 8 3 4 2.6 CC(=O)NCCCCNC(=O)c1[nH]c(C)c(C(=O)OC2CC3CCC2C3)c1C 10.1016/j.bmcl.2006.11.039
10018131 57482 2 None - 0 Human 5.0 pIC50 = 5 Binding
Compound was tested for inhibition of glutamate-evoked (10 uM) [Ca2+] mobilization in mGluR1-alpha expressed-CHO cells.Compound was tested for inhibition of glutamate-evoked (10 uM) [Ca2+] mobilization in mGluR1-alpha expressed-CHO cells.
ChEMBL 308 2 1 4 2.7 CN(C(=O)C12CC1/C(=N\O)c1ccccc1O2)c1ccccc1 10.1016/0960-894X(96)00104-7
CHEMBL165828 57482 2 None - 0 Human 5.0 pIC50 = 5 Binding
Compound was tested for inhibition of glutamate-evoked (10 uM) [Ca2+] mobilization in mGluR1-alpha expressed-CHO cells.Compound was tested for inhibition of glutamate-evoked (10 uM) [Ca2+] mobilization in mGluR1-alpha expressed-CHO cells.
ChEMBL 308 2 1 4 2.7 CN(C(=O)C12CC1/C(=N\O)c1ccccc1O2)c1ccccc1 10.1016/0960-894X(96)00104-7
11654379 142071 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 406 6 0 6 5.0 CCCCc1nc2c(sc3nccc(N(C)C)c32)c(=O)n1-c1ccc(CC)cc1 10.1016/j.ejmech.2007.06.024
CHEMBL387976 142071 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 406 6 0 6 5.0 CCCCc1nc2c(sc3nccc(N(C)C)c32)c(=O)n1-c1ccc(CC)cc1 10.1016/j.ejmech.2007.06.024
11485531 129476 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 370 8 1 5 4.2 CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1NCCOC 10.1021/jm049499o
CHEMBL367227 129476 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 370 8 1 5 4.2 CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1NCCOC 10.1021/jm049499o
11313361 2134 62 None - 1 Human 7.0 pIC50 = 7.0 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 325 3 0 4 3.9 COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1 10.1021/jm049499o
1385 2134 62 None - 1 Human 7.0 pIC50 = 7.0 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 325 3 0 4 3.9 COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1 10.1021/jm049499o
CHEMBL174588 2134 62 None - 1 Human 7.0 pIC50 = 7.0 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 325 3 0 4 3.9 COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1 10.1021/jm049499o
CHEMBL254574 2134 62 None - 1 Human 7.0 pIC50 = 7.0 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 325 3 0 4 3.9 COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1 10.1021/jm049499o
11347844 78924 1 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 322 4 0 4 4.1 CCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1C#N 10.1021/jm049499o
CHEMBL2112963 78924 1 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 322 4 0 4 4.1 CCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1C#N 10.1021/jm049499o
11682046 85154 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 362 3 0 6 3.8 CCc1ccc(-n2cnc3c(sc4nccc(N5CCC5)c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
CHEMBL225126 85154 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 362 3 0 6 3.8 CCc1ccc(-n2cnc3c(sc4nccc(N5CCC5)c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
11682046 85154 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 362 3 0 6 3.8 CCc1ccc(-n2cnc3c(sc4nccc(N5CCC5)c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
CHEMBL225126 85154 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 362 3 0 6 3.8 CCc1ccc(-n2cnc3c(sc4nccc(N5CCC5)c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
11461691 62305 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 331 3 0 3 4.5 CCc1cc2cc(C(=O)C3COc4ccccc4C3)ccc2nc1C 10.1021/jm049499o
CHEMBL177866 62305 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 331 3 0 3 4.5 CCc1cc2cc(C(=O)C3COc4ccccc4C3)ccc2nc1C 10.1021/jm049499o
44387723 127820 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 315 3 0 2 4.7 CCc1cc2cc(C(=O)C3Cc4ccccc4C3)ccc2nc1C 10.1021/jm049499o
CHEMBL366448 127820 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 315 3 0 2 4.7 CCc1cc2cc(C(=O)C3Cc4ccccc4C3)ccc2nc1C 10.1021/jm049499o
44307323 202998 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.
ChEMBL 305 4 1 5 3.2 Cc1c(C(=O)OC(C)(C)C)c[nH]c1C(=O)OCc1ccco1 10.1016/s0960-894x(03)00396-2
CHEMBL63161 202998 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.
ChEMBL 305 4 1 5 3.2 Cc1c(C(=O)OC(C)(C)C)c[nH]c1C(=O)OCc1ccco1 10.1016/s0960-894x(03)00396-2
2733519 106913 29 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Compound was tested in vitro for binding affinity against mGluR1a metabotropic glutamate receptor, using [3H]glutamate as the radioligand.Compound was tested in vitro for binding affinity against mGluR1a metabotropic glutamate receptor, using [3H]glutamate as the radioligand.
ChEMBL 159 3 3 3 -0.9 O=C(O)C[C@H]1CN[C@@H]1C(=O)O 10.1016/0960-894X(96)00464-7
CHEMBL314690 106913 29 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Compound was tested in vitro for binding affinity against mGluR1a metabotropic glutamate receptor, using [3H]glutamate as the radioligand.Compound was tested in vitro for binding affinity against mGluR1a metabotropic glutamate receptor, using [3H]glutamate as the radioligand.
ChEMBL 159 3 3 3 -0.9 O=C(O)C[C@H]1CN[C@@H]1C(=O)O 10.1016/0960-894X(96)00464-7
44562546 174467 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 361 2 1 6 3.5 CN(C)c1ccnc2sc3c(=O)n(-c4ccc5cc[nH]c5c4)cnc3c12 10.1016/j.ejmech.2007.06.024
CHEMBL455415 174467 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 361 2 1 6 3.5 CN(C)c1ccnc2sc3c(=O)n(-c4ccc5cc[nH]c5c4)cnc3c12 10.1016/j.ejmech.2007.06.024
44562546 174467 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 361 2 1 6 3.5 CN(C)c1ccnc2sc3c(=O)n(-c4ccc5cc[nH]c5c4)cnc3c12 10.1016/j.ejmech.2007.06.024
CHEMBL455415 174467 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 361 2 1 6 3.5 CN(C)c1ccnc2sc3c(=O)n(-c4ccc5cc[nH]c5c4)cnc3c12 10.1016/j.ejmech.2007.06.024
11220954 78534 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 321 2 0 2 5.5 C[C@H]1CC[C@@H](C(=O)c2ccc3nc4c(cc3c2)CCCCC4)CC1 10.1021/jm049499o
CHEMBL2112048 78534 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 321 2 0 2 5.5 C[C@H]1CC[C@@H](C(=O)c2ccc3nc4c(cc3c2)CCCCC4)CC1 10.1021/jm049499o
11174991 63511 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 333 3 0 2 5.5 CCc1cc2cc(C(=O)C34CC5CC(CC(C5)C3)C4)ccc2nc1C 10.1021/jm049499o
CHEMBL180011 63511 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 333 3 0 2 5.5 CCc1cc2cc(C(=O)C34CC5CC(CC(C5)C3)C4)ccc2nc1C 10.1021/jm049499o
44307362 203613 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.
ChEMBL 379 8 0 7 3.4 C=CCOC(=O)Cn1c(C)c(C(=O)OC(C)(C)C)c(C)c1C(=O)OCCC 10.1016/s0960-894x(03)00396-2
CHEMBL67071 203613 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.
ChEMBL 379 8 0 7 3.4 C=CCOC(=O)Cn1c(C)c(C(=O)OC(C)(C)C)c(C)c1C(=O)OCCC 10.1016/s0960-894x(03)00396-2
11515957 84809 1 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 356 2 0 6 4.4 CN(C)c1ccnc2sc3c(=O)n(C4CCCCCCC4)cnc3c12 10.1016/j.ejmech.2007.06.024
CHEMBL223399 84809 1 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 356 2 0 6 4.4 CN(C)c1ccnc2sc3c(=O)n(C4CCCCCCC4)cnc3c12 10.1016/j.ejmech.2007.06.024
44387711 60280 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 293 3 0 2 4.7 CCc1cc2cc(C(=O)C3CC4CCC3C4)ccc2nc1C 10.1021/jm049499o
CHEMBL174218 60280 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 293 3 0 2 4.7 CCc1cc2cc(C(=O)C3CC4CCC3C4)ccc2nc1C 10.1021/jm049499o
11177701 61467 1 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 423 4 0 3 4.8 CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1I 10.1021/jm049499o
CHEMBL177043 61467 1 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 423 4 0 3 4.8 CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1I 10.1021/jm049499o
16660135 1642 36 None - 1 Rat 7.9 pIC50 = 7.9 Binding
Displacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hrDisplacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hr
ChEMBL 371 5 1 6 3.8 CC(Nc1ncnc(c1)c1csc(n1)N(C(=O)c1ccc(cc1)F)C)C 10.1021/jm201590g
8767 1642 36 None - 1 Rat 7.9 pIC50 = 7.9 Binding
Displacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hrDisplacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hr
ChEMBL 371 5 1 6 3.8 CC(Nc1ncnc(c1)c1csc(n1)N(C(=O)c1ccc(cc1)F)C)C 10.1021/jm201590g
CHEMBL566581 1642 36 None - 1 Rat 7.9 pIC50 = 7.9 Binding
Displacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hrDisplacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hr
ChEMBL 371 5 1 6 3.8 CC(Nc1ncnc(c1)c1csc(n1)N(C(=O)c1ccc(cc1)F)C)C 10.1021/jm201590g
11515679 85102 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 342 2 0 6 3.8 CC1CCCCC1n1cnc2c(sc3nccc(N(C)C)c32)c1=O 10.1016/j.ejmech.2007.06.024
CHEMBL224672 85102 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 342 2 0 6 3.8 CC1CCCCC1n1cnc2c(sc3nccc(N(C)C)c32)c1=O 10.1016/j.ejmech.2007.06.024
11515679 85102 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 342 2 0 6 3.8 CC1CCCCC1n1cnc2c(sc3nccc(N(C)C)c32)c1=O 10.1016/j.ejmech.2007.06.024
CHEMBL224672 85102 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 342 2 0 6 3.8 CC1CCCCC1n1cnc2c(sc3nccc(N(C)C)c32)c1=O 10.1016/j.ejmech.2007.06.024
11681681 85008 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 342 3 0 6 3.7 CN(C)c1ccnc2sc3c(=O)n(CC4CCCCC4)cnc3c12 10.1016/j.ejmech.2007.06.024
CHEMBL223868 85008 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 342 3 0 6 3.7 CN(C)c1ccnc2sc3c(=O)n(CC4CCCCC4)cnc3c12 10.1016/j.ejmech.2007.06.024
11493897 85063 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 342 2 0 6 3.8 CC1CCC(n2cnc3c(sc4nccc(N(C)C)c43)c2=O)CC1 10.1016/j.ejmech.2007.06.024
CHEMBL224315 85063 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 342 2 0 6 3.8 CC1CCC(n2cnc3c(sc4nccc(N(C)C)c43)c2=O)CC1 10.1016/j.ejmech.2007.06.024
10470232 3269 23 None 1 2 Human 7.9 pIC50 = 7.9 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 303 3 0 3 4.0 O=C(c1ccc2c(c1)cc1c(n2)OCCC1)Cc1ccccc1 10.1021/jm049499o
1391 3269 23 None 1 2 Human 7.9 pIC50 = 7.9 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 303 3 0 3 4.0 O=C(c1ccc2c(c1)cc1c(n2)OCCC1)Cc1ccccc1 10.1021/jm049499o
6336 3269 23 None 1 2 Human 7.9 pIC50 = 7.9 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 303 3 0 3 4.0 O=C(c1ccc2c(c1)cc1c(n2)OCCC1)Cc1ccccc1 10.1021/jm049499o
CHEMBL369459 3269 23 None 1 2 Human 7.9 pIC50 = 7.9 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 303 3 0 3 4.0 O=C(c1ccc2c(c1)cc1c(n2)OCCC1)Cc1ccccc1 10.1021/jm049499o
11493897 85063 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 342 2 0 6 3.8 CC1CCC(n2cnc3c(sc4nccc(N(C)C)c43)c2=O)CC1 10.1016/j.ejmech.2007.06.024
CHEMBL224315 85063 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 342 2 0 6 3.8 CC1CCC(n2cnc3c(sc4nccc(N(C)C)c43)c2=O)CC1 10.1016/j.ejmech.2007.06.024
11256015 62987 4 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 331 4 0 3 4.8 CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1Cl 10.1021/jm049499o
CHEMBL178592 62987 4 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 331 4 0 3 4.8 CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1Cl 10.1021/jm049499o
44307128 203732 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.
ChEMBL 331 4 1 6 2.9 Cc1c(C(=O)OC(C)C(C)(C)C)c[nH]c1C(=O)Oc1ccncn1 10.1016/s0960-894x(03)00396-2
CHEMBL67769 203732 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.
ChEMBL 331 4 1 6 2.9 Cc1c(C(=O)OC(C)C(C)(C)C)c[nH]c1C(=O)Oc1ccncn1 10.1016/s0960-894x(03)00396-2
11186076 169335 1 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 313 4 1 4 3.9 CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1O 10.1021/jm049499o
CHEMBL441844 169335 1 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 313 4 1 4 3.9 CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1O 10.1021/jm049499o
44430066 87737 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of recombinant mGluR1a receptor expressed in CHO cellsInhibition of recombinant mGluR1a receptor expressed in CHO cells
ChEMBL 320 6 2 4 2.0 COCCNC(=O)c1[nH]cc(C(=O)OC2CC3CCC2C3)c1C 10.1016/j.bmcl.2006.11.039
CHEMBL233710 87737 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of recombinant mGluR1a receptor expressed in CHO cellsInhibition of recombinant mGluR1a receptor expressed in CHO cells
ChEMBL 320 6 2 4 2.0 COCCNC(=O)c1[nH]cc(C(=O)OC2CC3CCC2C3)c1C 10.1016/j.bmcl.2006.11.039
11722867 95 3 None - 0 Rat 4.8 pIC50 = 4.8 Binding
In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.
ChEMBL 309 5 1 4 3.8 CCCOC(=O)c1[nH]c(c(c1C)C(=O)OC(C(C)(C)C)C)C 10.1016/s0960-894x(03)00396-2
3397 95 3 None - 0 Rat 4.8 pIC50 = 4.8 Binding
In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.
ChEMBL 309 5 1 4 3.8 CCCOC(=O)c1[nH]c(c(c1C)C(=O)OC(C(C)(C)C)C)C 10.1016/s0960-894x(03)00396-2
CHEMBL304824 95 3 None - 0 Rat 4.8 pIC50 = 4.8 Binding
In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.
ChEMBL 309 5 1 4 3.8 CCCOC(=O)c1[nH]c(c(c1C)C(=O)OC(C(C)(C)C)C)C 10.1016/s0960-894x(03)00396-2
1069776 85222 11 None 257 2 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 356 2 0 6 3.7 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12 10.1016/j.ejmech.2007.06.024
CHEMBL225589 85222 11 None 257 2 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 356 2 0 6 3.7 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12 10.1016/j.ejmech.2007.06.024
11220954 78534 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 321 2 0 2 5.5 C[C@H]1CC[C@@H](C(=O)c2ccc3nc4c(cc3c2)CCCCC4)CC1 10.1021/jm049499o
CHEMBL2112048 78534 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 321 2 0 2 5.5 C[C@H]1CC[C@@H](C(=O)c2ccc3nc4c(cc3c2)CCCCC4)CC1 10.1021/jm049499o
11324832 60516 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 325 5 0 3 4.9 CCc1cc2cc(C(=O)C[C@H]3CC[C@@H](OC)CC3)ccc2nc1C 10.1021/jm049499o
CHEMBL175699 60516 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 325 5 0 3 4.9 CCc1cc2cc(C(=O)C[C@H]3CC[C@@H](OC)CC3)ccc2nc1C 10.1021/jm049499o
11688880 85065 0 None 616 2 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 350 2 0 6 3.7 Cc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)c(C)c1 10.1016/j.ejmech.2007.06.024
CHEMBL224356 85065 0 None 616 2 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 350 2 0 6 3.7 Cc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)c(C)c1 10.1016/j.ejmech.2007.06.024
44307138 96805 1 None - 0 Rat 6.8 pIC50 = 6.8 Binding
In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.
ChEMBL 419 4 1 4 4.8 Cc1c(C(=O)OC(C)C(C)(C)C)c[nH]c1C(=O)Oc1c(F)c(F)c(F)c(F)c1F 10.1016/s0960-894x(03)00396-2
CHEMBL265023 96805 1 None - 0 Rat 6.8 pIC50 = 6.8 Binding
In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.
ChEMBL 419 4 1 4 4.8 Cc1c(C(=O)OC(C)C(C)(C)C)c[nH]c1C(=O)Oc1c(F)c(F)c(F)c(F)c1F 10.1016/s0960-894x(03)00396-2
44307429 203569 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.
ChEMBL 329 5 1 4 4.1 CCCOC(=O)c1[nH]c(Cl)c(C(=O)OC(C)C(C)(C)C)c1C 10.1016/s0960-894x(03)00396-2
CHEMBL66728 203569 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.
ChEMBL 329 5 1 4 4.1 CCCOC(=O)c1[nH]c(Cl)c(C(=O)OC(C)C(C)(C)C)c1C 10.1016/s0960-894x(03)00396-2
11347669 120401 1 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 317 4 0 3 4.4 O=C(CCc1ccccc1)c1ccc2nc3c(cc2c1)CCCO3 10.1021/jm049499o
CHEMBL353547 120401 1 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 317 4 0 3 4.4 O=C(CCc1ccccc1)c1ccc2nc3c(cc2c1)CCCO3 10.1021/jm049499o
11184404 60505 1 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 255 4 0 2 4.3 CCc1cc2cc(C(=O)CC(C)C)ccc2nc1C 10.1021/jm049499o
CHEMBL175610 60505 1 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 255 4 0 2 4.3 CCc1cc2cc(C(=O)CC(C)C)ccc2nc1C 10.1021/jm049499o
11666576 141728 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 300 2 0 6 2.8 CN(C)c1ccnc2sc3c(=O)n(C4CCC4)cnc3c12 10.1016/j.ejmech.2007.06.024
CHEMBL385776 141728 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 300 2 0 6 2.8 CN(C)c1ccnc2sc3c(=O)n(C4CCC4)cnc3c12 10.1016/j.ejmech.2007.06.024
44562406 176926 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 358 2 0 6 4.0 C[N+](C)([O-])c1ccnc2sc3c(=O)n(C4CCCCCC4)cnc3c12 10.1016/j.ejmech.2007.06.024
CHEMBL462007 176926 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 358 2 0 6 4.0 C[N+](C)([O-])c1ccnc2sc3c(=O)n(C4CCCCCC4)cnc3c12 10.1016/j.ejmech.2007.06.024
11666576 141728 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 300 2 0 6 2.8 CN(C)c1ccnc2sc3c(=O)n(C4CCC4)cnc3c12 10.1016/j.ejmech.2007.06.024
CHEMBL385776 141728 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 300 2 0 6 2.8 CN(C)c1ccnc2sc3c(=O)n(C4CCC4)cnc3c12 10.1016/j.ejmech.2007.06.024
44562406 176926 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 358 2 0 6 4.0 C[N+](C)([O-])c1ccnc2sc3c(=O)n(C4CCCCCC4)cnc3c12 10.1016/j.ejmech.2007.06.024
CHEMBL462007 176926 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 358 2 0 6 4.0 C[N+](C)([O-])c1ccnc2sc3c(=O)n(C4CCCCCC4)cnc3c12 10.1016/j.ejmech.2007.06.024
44307214 102719 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.
ChEMBL 309 3 1 4 3.9 Cc1c(C(=O)OC(C)C(C)(C)C)c[nH]c1C(=O)OC(C)(C)C 10.1016/s0960-894x(03)00396-2
CHEMBL304866 102719 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.
ChEMBL 309 3 1 4 3.9 Cc1c(C(=O)OC(C)C(C)(C)C)c[nH]c1C(=O)OC(C)(C)C 10.1016/s0960-894x(03)00396-2
11688880 85065 0 None 616 2 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 350 2 0 6 3.7 Cc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)c(C)c1 10.1016/j.ejmech.2007.06.024
CHEMBL224356 85065 0 None 616 2 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 350 2 0 6 3.7 Cc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)c(C)c1 10.1016/j.ejmech.2007.06.024
11347844 78924 1 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 322 4 0 4 4.1 CCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1C#N 10.1021/jm049499o
CHEMBL2112963 78924 1 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 322 4 0 4 4.1 CCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1C#N 10.1021/jm049499o
11530673 166113 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 364 4 0 6 4.0 CCCc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
CHEMBL426018 166113 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 364 4 0 6 4.0 CCCc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
11209923 63012 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 337 3 0 3 4.9 CO[C@H]1CC[C@@H](C(=O)c2ccc3nc4c(cc3c2)CCCCC4)CC1 10.1021/jm049499o
CHEMBL178741 63012 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 337 3 0 3 4.9 CO[C@H]1CC[C@@H](C(=O)c2ccc3nc4c(cc3c2)CCCCC4)CC1 10.1021/jm049499o
11530673 166113 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 364 4 0 6 4.0 CCCc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
CHEMBL426018 166113 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 364 4 0 6 4.0 CCCc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
10245890 1982 7 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 327 5 0 4 4.2 CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)OC)CC 10.1021/jm049499o
6474 1982 7 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 327 5 0 4 4.2 CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)OC)CC 10.1021/jm049499o
CHEMBL175643 1982 7 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 327 5 0 4 4.2 CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)OC)CC 10.1021/jm049499o
44430064 151900 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of recombinant mGluR1a receptor expressed in CHO cellsInhibition of recombinant mGluR1a receptor expressed in CHO cells
ChEMBL 291 4 1 4 2.8 CCOC(=O)c1[nH]cc(C(=O)OC2CC3CCC2C3)c1C 10.1016/j.bmcl.2006.11.039
CHEMBL396593 151900 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of recombinant mGluR1a receptor expressed in CHO cellsInhibition of recombinant mGluR1a receptor expressed in CHO cells
ChEMBL 291 4 1 4 2.8 CCOC(=O)c1[nH]cc(C(=O)OC2CC3CCC2C3)c1C 10.1016/j.bmcl.2006.11.039
11474450 78926 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 379 5 0 4 5.9 CCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1-c1ccsc1 10.1021/jm049499o
CHEMBL2112965 78926 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 379 5 0 4 5.9 CCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1-c1ccsc1 10.1021/jm049499o
44430065 87736 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of recombinant mGluR1a receptor expressed in CHO cellsInhibition of recombinant mGluR1a receptor expressed in CHO cells
ChEMBL 375 8 3 4 2.3 CC(=O)NCCCCNC(=O)c1[nH]cc(C(=O)OC2CC3CCC2C3)c1C 10.1016/j.bmcl.2006.11.039
CHEMBL233709 87736 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of recombinant mGluR1a receptor expressed in CHO cellsInhibition of recombinant mGluR1a receptor expressed in CHO cells
ChEMBL 375 8 3 4 2.3 CC(=O)NCCCCNC(=O)c1[nH]cc(C(=O)OC2CC3CCC2C3)c1C 10.1016/j.bmcl.2006.11.039
11232687 60478 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 327 3 0 4 4.3 CO[C@H]1CC[C@@H](C(=O)c2ccc3nc4c(cc3c2)CCS4)CC1 10.1021/jm049499o
CHEMBL175463 60478 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 327 3 0 4 4.3 CO[C@H]1CC[C@@H](C(=O)c2ccc3nc4c(cc3c2)CCS4)CC1 10.1021/jm049499o
11232687 60478 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 327 3 0 4 4.3 CO[C@H]1CC[C@@H](C(=O)c2ccc3nc4c(cc3c2)CCS4)CC1 10.1021/jm049499o
CHEMBL175463 60478 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 327 3 0 4 4.3 CO[C@H]1CC[C@@H](C(=O)c2ccc3nc4c(cc3c2)CCS4)CC1 10.1021/jm049499o
11530404 210 14 None 38 2 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 350 3 0 6 3.6 CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C 10.1016/j.ejmech.2007.06.024
6211 210 14 None 38 2 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 350 3 0 6 3.6 CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C 10.1016/j.ejmech.2007.06.024
CHEMBL385336 210 14 None 38 2 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 350 3 0 6 3.6 CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C 10.1016/j.ejmech.2007.06.024
699222 85092 11 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 322 2 0 6 3.1 CN(C)c1ccnc2sc3c(=O)n(-c4ccccc4)cnc3c12 10.1016/j.ejmech.2007.06.024
CHEMBL224615 85092 11 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 322 2 0 6 3.1 CN(C)c1ccnc2sc3c(=O)n(-c4ccccc4)cnc3c12 10.1016/j.ejmech.2007.06.024
10245890 1982 7 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against human metabotropic glutamate receptor 1 transmembrane domainInhibitory concentration against human metabotropic glutamate receptor 1 transmembrane domain
ChEMBL 327 5 0 4 4.2 CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)OC)CC 10.1021/jm049499o
6474 1982 7 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against human metabotropic glutamate receptor 1 transmembrane domainInhibitory concentration against human metabotropic glutamate receptor 1 transmembrane domain
ChEMBL 327 5 0 4 4.2 CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)OC)CC 10.1021/jm049499o
CHEMBL175643 1982 7 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against human metabotropic glutamate receptor 1 transmembrane domainInhibitory concentration against human metabotropic glutamate receptor 1 transmembrane domain
ChEMBL 327 5 0 4 4.2 CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)OC)CC 10.1021/jm049499o
44306971 203615 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.
ChEMBL 295 5 1 5 2.7 CCCOC(=O)c1[nH]c(C=O)c(C(=O)OC(C)(C)C)c1C 10.1016/s0960-894x(03)00396-2
CHEMBL67075 203615 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.
ChEMBL 295 5 1 5 2.7 CCCOC(=O)c1[nH]c(C=O)c(C(=O)OC(C)(C)C)c1C 10.1016/s0960-894x(03)00396-2
11667270 85152 0 None - 1 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 340 2 0 6 3.2 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(F)cc4)cnc3c12 10.1016/j.ejmech.2007.06.024
CHEMBL225124 85152 0 None - 1 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 340 2 0 6 3.2 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(F)cc4)cnc3c12 10.1016/j.ejmech.2007.06.024
11667270 85152 0 None - 1 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 340 2 0 6 3.2 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(F)cc4)cnc3c12 10.1016/j.ejmech.2007.06.024
CHEMBL225124 85152 0 None - 1 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 340 2 0 6 3.2 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(F)cc4)cnc3c12 10.1016/j.ejmech.2007.06.024
11483517 60305 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 303 5 0 2 4.9 CCc1cc2cc(C(=O)CCc3ccccc3)ccc2nc1C 10.1021/jm049499o
CHEMBL174382 60305 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 303 5 0 2 4.9 CCc1cc2cc(C(=O)CCc3ccccc3)ccc2nc1C 10.1021/jm049499o
44306730 203790 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
In vitro inhibitory concentration required against rat mGluR1a in CHO cells using the CDP-DAG accumulation methodIn vitro inhibitory concentration required against rat mGluR1a in CHO cells using the CDP-DAG accumulation method
ChEMBL 381 4 0 7 4.4 CCCOC(=O)c1c(C)c(C(=O)OC(C)(C)C)c(C)n1C(=O)OC(C)(C)C 10.1016/s0960-894x(03)00396-2
CHEMBL68250 203790 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
In vitro inhibitory concentration required against rat mGluR1a in CHO cells using the CDP-DAG accumulation methodIn vitro inhibitory concentration required against rat mGluR1a in CHO cells using the CDP-DAG accumulation method
ChEMBL 381 4 0 7 4.4 CCCOC(=O)c1c(C)c(C(=O)OC(C)(C)C)c(C)n1C(=O)OC(C)(C)C 10.1016/s0960-894x(03)00396-2
1382 1190 33 None -1 2 Human 4.6 pIC50 = 4.6 Binding
Compound was tested for inhibition of glutamate-evoked (10 uM) [Ca2+] mobilization in mGluR1-alpha expressed-CHO cells.Compound was tested for inhibition of glutamate-evoked (10 uM) [Ca2+] mobilization in mGluR1-alpha expressed-CHO cells.
ChEMBL 247 2 1 5 1.6 CCOC(=O)C12CC2/C(=N\O)/c2c(O1)cccc2 10.1016/0960-894X(96)00104-7
6278000 1190 33 None -1 2 Human 4.6 pIC50 = 4.6 Binding
Compound was tested for inhibition of glutamate-evoked (10 uM) [Ca2+] mobilization in mGluR1-alpha expressed-CHO cells.Compound was tested for inhibition of glutamate-evoked (10 uM) [Ca2+] mobilization in mGluR1-alpha expressed-CHO cells.
ChEMBL 247 2 1 5 1.6 CCOC(=O)C12CC2/C(=N\O)/c2c(O1)cccc2 10.1016/0960-894X(96)00104-7
CHEMBL327783 1190 33 None -1 2 Human 4.6 pIC50 = 4.6 Binding
Compound was tested for inhibition of glutamate-evoked (10 uM) [Ca2+] mobilization in mGluR1-alpha expressed-CHO cells.Compound was tested for inhibition of glutamate-evoked (10 uM) [Ca2+] mobilization in mGluR1-alpha expressed-CHO cells.
ChEMBL 247 2 1 5 1.6 CCOC(=O)C12CC2/C(=N\O)/c2c(O1)cccc2 10.1016/0960-894X(96)00104-7
10245890 1982 7 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 327 5 0 4 4.2 CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)OC)CC 10.1021/jm049499o
6474 1982 7 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 327 5 0 4 4.2 CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)OC)CC 10.1021/jm049499o
CHEMBL175643 1982 7 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 327 5 0 4 4.2 CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)OC)CC 10.1021/jm049499o
44307328 103591 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.
ChEMBL 364 7 2 5 3.0 CCCOC(=O)c1[nH]c(C(=O)NCC2CC2)c(C(=O)OC(C)(C)C)c1C 10.1016/s0960-894x(03)00396-2
CHEMBL308641 103591 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.
ChEMBL 364 7 2 5 3.0 CCCOC(=O)c1[nH]c(C(=O)NCC2CC2)c(C(=O)OC(C)(C)C)c1C 10.1016/s0960-894x(03)00396-2
3421 3544 41 None - 1 Human 4.6 pIC50 = 4.6 Binding
Antagonist activity at mGluR1alpha (unknown origin)Antagonist activity at mGluR1alpha (unknown origin)
ChEMBL 185 3 3 3 -0.3 OC(=O)[C@H](C12CC(C1)(C2)C(=O)O)N 10.1021/acs.jmedchem.1c01215
5311040 3544 41 None - 1 Human 4.6 pIC50 = 4.6 Binding
Antagonist activity at mGluR1alpha (unknown origin)Antagonist activity at mGluR1alpha (unknown origin)
ChEMBL 185 3 3 3 -0.3 OC(=O)[C@H](C12CC(C1)(C2)C(=O)O)N 10.1021/acs.jmedchem.1c01215
CHEMBL43412 3544 41 None - 1 Human 4.6 pIC50 = 4.6 Binding
Antagonist activity at mGluR1alpha (unknown origin)Antagonist activity at mGluR1alpha (unknown origin)
ChEMBL 185 3 3 3 -0.3 OC(=O)[C@H](C12CC(C1)(C2)C(=O)O)N 10.1021/acs.jmedchem.1c01215
3421 3544 41 None - 1 Human 4.6 pIC50 = 4.6 Binding
Inhibition of mGluR1a receptorInhibition of mGluR1a receptor
ChEMBL 185 3 3 3 -0.3 OC(=O)[C@H](C12CC(C1)(C2)C(=O)O)N 10.1021/jm1013693
5311040 3544 41 None - 1 Human 4.6 pIC50 = 4.6 Binding
Inhibition of mGluR1a receptorInhibition of mGluR1a receptor
ChEMBL 185 3 3 3 -0.3 OC(=O)[C@H](C12CC(C1)(C2)C(=O)O)N 10.1021/jm1013693
CHEMBL43412 3544 41 None - 1 Human 4.6 pIC50 = 4.6 Binding
Inhibition of mGluR1a receptorInhibition of mGluR1a receptor
ChEMBL 185 3 3 3 -0.3 OC(=O)[C@H](C12CC(C1)(C2)C(=O)O)N 10.1021/jm1013693
3421 3544 41 None - 1 Rat 4.6 pIC50 = 4.6 Binding
Inhibitory activity against Metabotropic glutamate receptor 1 in the rat LLC-PK1/HEK 293 cells.Inhibitory activity against Metabotropic glutamate receptor 1 in the rat LLC-PK1/HEK 293 cells.
ChEMBL 185 3 3 3 -0.3 OC(=O)[C@H](C12CC(C1)(C2)C(=O)O)N 10.1021/jm980571q
5311040 3544 41 None - 1 Rat 4.6 pIC50 = 4.6 Binding
Inhibitory activity against Metabotropic glutamate receptor 1 in the rat LLC-PK1/HEK 293 cells.Inhibitory activity against Metabotropic glutamate receptor 1 in the rat LLC-PK1/HEK 293 cells.
ChEMBL 185 3 3 3 -0.3 OC(=O)[C@H](C12CC(C1)(C2)C(=O)O)N 10.1021/jm980571q
CHEMBL43412 3544 41 None - 1 Rat 4.6 pIC50 = 4.6 Binding
Inhibitory activity against Metabotropic glutamate receptor 1 in the rat LLC-PK1/HEK 293 cells.Inhibitory activity against Metabotropic glutamate receptor 1 in the rat LLC-PK1/HEK 293 cells.
ChEMBL 185 3 3 3 -0.3 OC(=O)[C@H](C12CC(C1)(C2)C(=O)O)N 10.1021/jm980571q
11501188 137543 0 None - 1 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 350 3 0 6 3.6 CCc1ccccc1-n1cnc2c(sc3nccc(N(C)C)c32)c1=O 10.1016/j.ejmech.2007.06.024
CHEMBL375439 137543 0 None - 1 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 350 3 0 6 3.6 CCc1ccccc1-n1cnc2c(sc3nccc(N(C)C)c32)c1=O 10.1016/j.ejmech.2007.06.024
11501188 137543 0 None - 1 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 350 3 0 6 3.6 CCc1ccccc1-n1cnc2c(sc3nccc(N(C)C)c32)c1=O 10.1016/j.ejmech.2007.06.024
CHEMBL375439 137543 0 None - 1 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 350 3 0 6 3.6 CCc1ccccc1-n1cnc2c(sc3nccc(N(C)C)c32)c1=O 10.1016/j.ejmech.2007.06.024
11631279 141911 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 328 3 0 6 3.3 CN(C)c1ccnc2sc3c(=O)n(CC4CCCC4)cnc3c12 10.1016/j.ejmech.2007.06.024
CHEMBL386935 141911 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 328 3 0 6 3.3 CN(C)c1ccnc2sc3c(=O)n(CC4CCCC4)cnc3c12 10.1016/j.ejmech.2007.06.024
71459305 83032 0 None - 1 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [18F]FITM from mGlu1 receptor in rat brain homogenates after 1 hr by gamma countingDisplacement of [18F]FITM from mGlu1 receptor in rat brain homogenates after 1 hr by gamma counting
ChEMBL 367 5 1 6 4.0 Cc1ccc(C(=O)N(C)c2nc(-c3cc(NC(C)C)ncn3)cs2)cc1 10.1021/jm301597s
CHEMBL2181520 83032 0 None - 1 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [18F]FITM from mGlu1 receptor in rat brain homogenates after 1 hr by gamma countingDisplacement of [18F]FITM from mGlu1 receptor in rat brain homogenates after 1 hr by gamma counting
ChEMBL 367 5 1 6 4.0 Cc1ccc(C(=O)N(C)c2nc(-c3cc(NC(C)C)ncn3)cs2)cc1 10.1021/jm301597s
44307139 203628 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.
ChEMBL 350 5 1 5 3.2 CCN1CCC(OC(=O)c2[nH]cc(C(=O)OC(C)C(C)(C)C)c2C)C1 10.1016/s0960-894x(03)00396-2
CHEMBL67143 203628 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.
ChEMBL 350 5 1 5 3.2 CCN1CCC(OC(=O)c2[nH]cc(C(=O)OC(C)C(C)(C)C)c2C)C1 10.1016/s0960-894x(03)00396-2
11461525 60517 1 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 325 5 0 3 5.0 C=C(c1ccc2nc(OC)c(CC)cc2c1)[C@H]1CC[C@@H](OC)CC1 10.1021/jm049499o
CHEMBL175700 60517 1 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 325 5 0 3 5.0 C=C(c1ccc2nc(OC)c(CC)cc2c1)[C@H]1CC[C@@H](OC)CC1 10.1021/jm049499o
44307263 203033 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.
ChEMBL 339 6 1 6 2.9 CCCOC(=O)c1[nH]c(COC(C)=O)c(C(=O)OC(C)(C)C)c1C 10.1016/s0960-894x(03)00396-2
CHEMBL63393 203033 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.
ChEMBL 339 6 1 6 2.9 CCCOC(=O)c1[nH]c(COC(C)=O)c(C(=O)OC(C)(C)C)c1C 10.1016/s0960-894x(03)00396-2
657896 142082 10 None - 1 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 336 3 0 6 3.1 CN(C)c1ccnc2sc3c(=O)n(Cc4ccccc4)cnc3c12 10.1016/j.ejmech.2007.06.024
CHEMBL388087 142082 10 None - 1 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 336 3 0 6 3.1 CN(C)c1ccnc2sc3c(=O)n(Cc4ccccc4)cnc3c12 10.1016/j.ejmech.2007.06.024
657896 142082 10 None - 1 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 336 3 0 6 3.1 CN(C)c1ccnc2sc3c(=O)n(Cc4ccccc4)cnc3c12 10.1016/j.ejmech.2007.06.024
CHEMBL388087 142082 10 None - 1 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 336 3 0 6 3.1 CN(C)c1ccnc2sc3c(=O)n(Cc4ccccc4)cnc3c12 10.1016/j.ejmech.2007.06.024
11450605 60279 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 338 3 0 4 4.0 CO[C@H]1CC[C@@H](C(=O)c2ccc3nc4c(cc3c2)CCCN4C)CC1 10.1021/jm049499o
CHEMBL174216 60279 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 338 3 0 4 4.0 CO[C@H]1CC[C@@H](C(=O)c2ccc3nc4c(cc3c2)CCCN4C)CC1 10.1021/jm049499o
11530404 210 14 None 38 2 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 350 3 0 6 3.6 CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C 10.1016/j.ejmech.2007.06.024
6211 210 14 None 38 2 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 350 3 0 6 3.6 CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C 10.1016/j.ejmech.2007.06.024
CHEMBL385336 210 14 None 38 2 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 350 3 0 6 3.6 CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C 10.1016/j.ejmech.2007.06.024
11255377 61026 1 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 311 5 0 3 4.6 CCCc1ccc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2n1 10.1021/jm049499o
CHEMBL176279 61026 1 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 311 5 0 3 4.6 CCCc1ccc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2n1 10.1021/jm049499o
11313361 2134 62 None - 1 Rat 8.5 pIC50 = 8.5 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 325 3 0 4 3.9 COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1 10.1021/jm049499o
1385 2134 62 None - 1 Rat 8.5 pIC50 = 8.5 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 325 3 0 4 3.9 COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1 10.1021/jm049499o
CHEMBL174588 2134 62 None - 1 Rat 8.5 pIC50 = 8.5 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 325 3 0 4 3.9 COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1 10.1021/jm049499o
CHEMBL254574 2134 62 None - 1 Rat 8.5 pIC50 = 8.5 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 325 3 0 4 3.9 COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1 10.1021/jm049499o
44387697 60467 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 325 5 0 3 4.7 CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1CC 10.1021/jm049499o
CHEMBL175377 60467 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 325 5 0 3 4.7 CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1CC 10.1021/jm049499o
11301185 1683 32 None - 1 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to human mGluR1Binding affinity to human mGluR1
ChEMBL 305 2 0 5 3.3 Cc1c(nnn1c1cccnc1F)c1ccc2c(c1)cccn2 10.1016/j.bmc.2010.11.048
6353 1683 32 None - 1 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to human mGluR1Binding affinity to human mGluR1
ChEMBL 305 2 0 5 3.3 Cc1c(nnn1c1cccnc1F)c1ccc2c(c1)cccn2 10.1016/j.bmc.2010.11.048
CHEMBL1645352 1683 32 None - 1 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to human mGluR1Binding affinity to human mGluR1
ChEMBL 305 2 0 5 3.3 Cc1c(nnn1c1cccnc1F)c1ccc2c(c1)cccn2 10.1016/j.bmc.2010.11.048
44430062 88482 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of recombinant mGluR1a receptor expressed in CHO cellsInhibition of recombinant mGluR1a receptor expressed in CHO cells
ChEMBL 295 5 1 4 3.5 CCCOC(=O)c1[nH]cc(C(=O)O[C@@H](C)C(C)(C)C)c1C 10.1016/j.bmcl.2006.11.039
CHEMBL234972 88482 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of recombinant mGluR1a receptor expressed in CHO cellsInhibition of recombinant mGluR1a receptor expressed in CHO cells
ChEMBL 295 5 1 4 3.5 CCCOC(=O)c1[nH]cc(C(=O)O[C@@H](C)C(C)(C)C)c1C 10.1016/j.bmcl.2006.11.039
11574901 85224 0 None - 1 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 400 2 0 6 3.8 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12 10.1016/j.ejmech.2007.06.024
CHEMBL225590 85224 0 None - 1 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 400 2 0 6 3.8 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12 10.1016/j.ejmech.2007.06.024
1416 3093 41 None - 0 Human 5.5 pIC50 = 5.5 Binding
Compound was tested for inhibition of glutamate-evoked (10 uM) [Ca2+] mobilization in mGluR1-alpha expressed-CHO cells.Compound was tested for inhibition of glutamate-evoked (10 uM) [Ca2+] mobilization in mGluR1-alpha expressed-CHO cells.
ChEMBL 294 2 2 4 2.7 O/N=C\1/c2ccccc2OC2(C1C2)C(=O)Nc1ccccc1 10.1016/0960-894X(96)00104-7
5866327 3093 41 None - 0 Human 5.5 pIC50 = 5.5 Binding
Compound was tested for inhibition of glutamate-evoked (10 uM) [Ca2+] mobilization in mGluR1-alpha expressed-CHO cells.Compound was tested for inhibition of glutamate-evoked (10 uM) [Ca2+] mobilization in mGluR1-alpha expressed-CHO cells.
ChEMBL 294 2 2 4 2.7 O/N=C\1/c2ccccc2OC2(C1C2)C(=O)Nc1ccccc1 10.1016/0960-894X(96)00104-7
CHEMBL164770 3093 41 None - 0 Human 5.5 pIC50 = 5.5 Binding
Compound was tested for inhibition of glutamate-evoked (10 uM) [Ca2+] mobilization in mGluR1-alpha expressed-CHO cells.Compound was tested for inhibition of glutamate-evoked (10 uM) [Ca2+] mobilization in mGluR1-alpha expressed-CHO cells.
ChEMBL 294 2 2 4 2.7 O/N=C\1/c2ccccc2OC2(C1C2)C(=O)Nc1ccccc1 10.1016/0960-894X(96)00104-7
44307322 203047 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.
ChEMBL 318 3 1 5 3.6 Cc1c(C(=O)OC(C)(C)C)c[nH]c1C(=O)Sc1ccccn1 10.1016/s0960-894x(03)00396-2
CHEMBL63539 203047 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.
ChEMBL 318 3 1 5 3.6 Cc1c(C(=O)OC(C)(C)C)c[nH]c1C(=O)Sc1ccccn1 10.1016/s0960-894x(03)00396-2
11639210 144149 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 366 3 0 6 3.6 CCc1ccc(-n2cnc3c(sc4nccc([N+](C)(C)[O-])c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
CHEMBL390391 144149 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 366 3 0 6 3.6 CCc1ccc(-n2cnc3c(sc4nccc([N+](C)(C)[O-])c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
11639210 144149 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 366 3 0 6 3.6 CCc1ccc(-n2cnc3c(sc4nccc([N+](C)(C)[O-])c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
CHEMBL390391 144149 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 366 3 0 6 3.6 CCc1ccc(-n2cnc3c(sc4nccc([N+](C)(C)[O-])c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
44430063 87735 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of recombinant mGluR1a receptor expressed in CHO cellsInhibition of recombinant mGluR1a receptor expressed in CHO cells
ChEMBL 310 6 2 4 2.3 COCCNC(=O)c1[nH]cc(C(=O)O[C@@H](C)C(C)(C)C)c1C 10.1016/j.bmcl.2006.11.039
CHEMBL233708 87735 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of recombinant mGluR1a receptor expressed in CHO cellsInhibition of recombinant mGluR1a receptor expressed in CHO cells
ChEMBL 310 6 2 4 2.3 COCCNC(=O)c1[nH]cc(C(=O)O[C@@H](C)C(C)(C)C)c1C 10.1016/j.bmcl.2006.11.039
11560185 85067 0 None - 1 Rat 7.5 pIC50 = 7.5 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 390 2 0 6 4.1 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(C(F)(F)F)cc4)cnc3c12 10.1016/j.ejmech.2007.06.024
CHEMBL224375 85067 0 None - 1 Rat 7.5 pIC50 = 7.5 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 390 2 0 6 4.1 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(C(F)(F)F)cc4)cnc3c12 10.1016/j.ejmech.2007.06.024
44430069 167024 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of recombinant mGluR1a receptor expressed in CHO cellsInhibition of recombinant mGluR1a receptor expressed in CHO cells
ChEMBL 334 6 2 4 2.4 COCCNC(=O)c1[nH]c(C)c(C(=O)OC2CC3CCC2C3)c1C 10.1016/j.bmcl.2006.11.039
CHEMBL428850 167024 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of recombinant mGluR1a receptor expressed in CHO cellsInhibition of recombinant mGluR1a receptor expressed in CHO cells
ChEMBL 334 6 2 4 2.4 COCCNC(=O)c1[nH]c(C)c(C(=O)OC2CC3CCC2C3)c1C 10.1016/j.bmcl.2006.11.039
11560185 85067 0 None - 1 Rat 7.5 pIC50 = 7.5 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 390 2 0 6 4.1 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(C(F)(F)F)cc4)cnc3c12 10.1016/j.ejmech.2007.06.024
CHEMBL224375 85067 0 None - 1 Rat 7.5 pIC50 = 7.5 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 390 2 0 6 4.1 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(C(F)(F)F)cc4)cnc3c12 10.1016/j.ejmech.2007.06.024
16660470 76629 0 None - 1 Rat 7.5 pIC50 = 7.5 Binding
Displacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hrDisplacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hr
ChEMBL 383 6 1 7 3.7 COc1ccc(C(=O)N(C)c2nc(-c3cc(NC(C)C)ncn3)cs2)cc1 10.1021/jm201590g
CHEMBL2063722 76629 0 None - 1 Rat 7.5 pIC50 = 7.5 Binding
Displacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hrDisplacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hr
ChEMBL 383 6 1 7 3.7 COc1ccc(C(=O)N(C)c2nc(-c3cc(NC(C)C)ncn3)cs2)cc1 10.1021/jm201590g
CHEMBL177736 62132 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 341 5 1 5 3.7 CCc1cc2cc(/C(=N\N)[C@H]3CC[C@@H](OC)CC3)ccc2nc1OC 10.1021/jm049499o
44307059 102084 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.
ChEMBL 404 6 1 7 4.2 CCCOC(=O)c1[nH]c(C(=O)Sc2ccccn2)c(C(=O)OC(C)(C)C)c1C 10.1016/s0960-894x(03)00396-2
CHEMBL302153 102084 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.
ChEMBL 404 6 1 7 4.2 CCCOC(=O)c1[nH]c(C(=O)Sc2ccccn2)c(C(=O)OC(C)(C)C)c1C 10.1016/s0960-894x(03)00396-2
44307336 203685 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.
ChEMBL 325 5 1 6 2.6 CCCOC(=O)c1[nH]c(C(=O)OC)c(C(=O)OC(C)(C)C)c1C 10.1016/s0960-894x(03)00396-2
CHEMBL67472 203685 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.
ChEMBL 325 5 1 6 2.6 CCCOC(=O)c1[nH]c(C(=O)OC)c(C(=O)OC(C)(C)C)c1C 10.1016/s0960-894x(03)00396-2
3421 3544 41 None - 1 Human 4.5 pIC50 = 4.5 Binding
Inhibitory activity against mGluR1 receptorInhibitory activity against mGluR1 receptor
ChEMBL 185 3 3 3 -0.3 OC(=O)[C@H](C12CC(C1)(C2)C(=O)O)N 10.1016/s0960-894x(98)00265-0
5311040 3544 41 None - 1 Human 4.5 pIC50 = 4.5 Binding
Inhibitory activity against mGluR1 receptorInhibitory activity against mGluR1 receptor
ChEMBL 185 3 3 3 -0.3 OC(=O)[C@H](C12CC(C1)(C2)C(=O)O)N 10.1016/s0960-894x(98)00265-0
CHEMBL43412 3544 41 None - 1 Human 4.5 pIC50 = 4.5 Binding
Inhibitory activity against mGluR1 receptorInhibitory activity against mGluR1 receptor
ChEMBL 185 3 3 3 -0.3 OC(=O)[C@H](C12CC(C1)(C2)C(=O)O)N 10.1016/s0960-894x(98)00265-0
11222713 60805 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 379 5 0 4 5.9 CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1-c1cccs1 10.1021/jm049499o
CHEMBL176174 60805 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 379 5 0 4 5.9 CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1-c1cccs1 10.1021/jm049499o
11594849 84998 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 316 4 0 6 3.4 CCC(CC)n1cnc2c(sc3nccc(N(C)C)c32)c1=O 10.1016/j.ejmech.2007.06.024
CHEMBL223819 84998 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 316 4 0 6 3.4 CCC(CC)n1cnc2c(sc3nccc(N(C)C)c32)c1=O 10.1016/j.ejmech.2007.06.024
11594849 84998 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 316 4 0 6 3.4 CCC(CC)n1cnc2c(sc3nccc(N(C)C)c32)c1=O 10.1016/j.ejmech.2007.06.024
CHEMBL223819 84998 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 316 4 0 6 3.4 CCC(CC)n1cnc2c(sc3nccc(N(C)C)c32)c1=O 10.1016/j.ejmech.2007.06.024
72163432 92027 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Negative allosteric modulation of rat mGlu1 receptorNegative allosteric modulation of rat mGlu1 receptor
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 92027 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Negative allosteric modulation of rat mGlu1 receptorNegative allosteric modulation of rat mGlu1 receptor
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
44306948 102233 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.
ChEMBL 253 3 1 4 2.5 CCOC(=O)c1[nH]cc(C(=O)OC(C)(C)C)c1C 10.1016/s0960-894x(03)00396-2
CHEMBL303018 102233 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.
ChEMBL 253 3 1 4 2.5 CCOC(=O)c1[nH]cc(C(=O)OC(C)(C)C)c1C 10.1016/s0960-894x(03)00396-2
11383509 78927 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 383 6 0 5 4.8 CCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1C(=O)OC(C)C 10.1021/jm049499o
CHEMBL2112966 78927 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 383 6 0 5 4.8 CCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1C(=O)OC(C)C 10.1021/jm049499o
11639176 84847 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 364 4 0 6 4.0 CCc1ccc(-n2cnc3c(sc4nccc(N(C)CC)c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
CHEMBL223543 84847 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 364 4 0 6 4.0 CCc1ccc(-n2cnc3c(sc4nccc(N(C)CC)c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
11639176 84847 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 364 4 0 6 4.0 CCc1ccc(-n2cnc3c(sc4nccc(N(C)CC)c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
CHEMBL223543 84847 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 364 4 0 6 4.0 CCc1ccc(-n2cnc3c(sc4nccc(N(C)CC)c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
11717319 143494 0 None - 1 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 353 3 0 8 2.5 COc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cn1 10.1016/j.ejmech.2007.06.024
CHEMBL389870 143494 0 None - 1 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 353 3 0 8 2.5 COc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cn1 10.1016/j.ejmech.2007.06.024
11717319 143494 0 None - 1 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 353 3 0 8 2.5 COc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cn1 10.1016/j.ejmech.2007.06.024
CHEMBL389870 143494 0 None - 1 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 353 3 0 8 2.5 COc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cn1 10.1016/j.ejmech.2007.06.024
44307245 203639 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.
ChEMBL 338 6 1 5 3.0 Cc1c(C(=O)OC(C)C(C)(C)C)c[nH]c1C(=O)OC(C)CN(C)C 10.1016/s0960-894x(03)00396-2
CHEMBL67197 203639 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.
ChEMBL 338 6 1 5 3.0 Cc1c(C(=O)OC(C)C(C)(C)C)c[nH]c1C(=O)OC(C)CN(C)C 10.1016/s0960-894x(03)00396-2
70688666 76630 0 None - 1 Rat 6.4 pIC50 = 6.4 Binding
Displacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hrDisplacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hr
ChEMBL 415 8 1 7 4.0 CC(C)Nc1cc(-c2csc(N(C)C(=O)c3ccc(OCCF)cc3)n2)ncn1 10.1021/jm201590g
CHEMBL2063723 76630 0 None - 1 Rat 6.4 pIC50 = 6.4 Binding
Displacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hrDisplacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hr
ChEMBL 415 8 1 7 4.0 CC(C)Nc1cc(-c2csc(N(C)C(=O)c3ccc(OCCF)cc3)n2)ncn1 10.1021/jm201590g
44307069 100881 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.
ChEMBL 295 5 1 4 3.5 CCCOC(=O)c1[nH]cc(C(=O)OC(C)C(C)(C)C)c1C 10.1016/s0960-894x(03)00396-2
CHEMBL293665 100881 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.
ChEMBL 295 5 1 4 3.5 CCCOC(=O)c1[nH]cc(C(=O)OC(C)C(C)(C)C)c1C 10.1016/s0960-894x(03)00396-2
11574901 85224 0 None - 1 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 400 2 0 6 3.8 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12 10.1016/j.ejmech.2007.06.024
CHEMBL225590 85224 0 None - 1 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 400 2 0 6 3.8 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12 10.1016/j.ejmech.2007.06.024
11256015 62987 4 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 331 4 0 3 4.8 CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1Cl 10.1021/jm049499o
CHEMBL178592 62987 4 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 331 4 0 3 4.8 CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1Cl 10.1021/jm049499o
11483690 63006 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 309 3 0 3 4.1 CO[C@H]1CC[C@@H](C(=O)c2ccc3nc4c(cc3c2)CCC4)CC1 10.1021/jm049499o
CHEMBL178690 63006 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 309 3 0 3 4.1 CO[C@H]1CC[C@@H](C(=O)c2ccc3nc4c(cc3c2)CCC4)CC1 10.1021/jm049499o
11220222 63541 1 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 297 4 0 3 4.2 CCc1cnc2ccc(C(=O)C3CCC(OC)CC3)cc2c1 10.1021/jm049499o
CHEMBL180021 63541 1 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 297 4 0 3 4.2 CCc1cnc2ccc(C(=O)C3CCC(OC)CC3)cc2c1 10.1021/jm049499o
11174504 78925 4 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 315 4 0 3 4.3 CCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1F 10.1021/jm049499o
CHEMBL2112964 78925 4 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 315 4 0 3 4.3 CCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1F 10.1021/jm049499o
1374 2081 35 None - 2 Rat 4.4 pIC50 = 4.4 Binding
Inhibitory activity against Metabotropic glutamate receptor 1 in the rat LLC-PK1/HEK 293 cellsInhibitory activity against Metabotropic glutamate receptor 1 in the rat LLC-PK1/HEK 293 cells
ChEMBL 211 3 4 4 0.2 N[C@@H](c1ccc(c(c1)O)C(=O)O)C(=O)O 10.1021/jm980571q
5311455 2081 35 None - 2 Rat 4.4 pIC50 = 4.4 Binding
Inhibitory activity against Metabotropic glutamate receptor 1 in the rat LLC-PK1/HEK 293 cellsInhibitory activity against Metabotropic glutamate receptor 1 in the rat LLC-PK1/HEK 293 cells
ChEMBL 211 3 4 4 0.2 N[C@@H](c1ccc(c(c1)O)C(=O)O)C(=O)O 10.1021/jm980571q
CHEMBL39372 2081 35 None - 2 Rat 4.4 pIC50 = 4.4 Binding
Inhibitory activity against Metabotropic glutamate receptor 1 in the rat LLC-PK1/HEK 293 cellsInhibitory activity against Metabotropic glutamate receptor 1 in the rat LLC-PK1/HEK 293 cells
ChEMBL 211 3 4 4 0.2 N[C@@H](c1ccc(c(c1)O)C(=O)O)C(=O)O 10.1021/jm980571q
1374 2081 35 None 12 2 Human 4.4 pIC50 = 4.4 Binding
Inhibitory concentration for half maximal inhibition of PI hydrolysis (mGluR1a)Inhibitory concentration for half maximal inhibition of PI hydrolysis (mGluR1a)
ChEMBL 211 3 4 4 0.2 N[C@@H](c1ccc(c(c1)O)C(=O)O)C(=O)O 10.1021/jm9601718
5311455 2081 35 None 12 2 Human 4.4 pIC50 = 4.4 Binding
Inhibitory concentration for half maximal inhibition of PI hydrolysis (mGluR1a)Inhibitory concentration for half maximal inhibition of PI hydrolysis (mGluR1a)
ChEMBL 211 3 4 4 0.2 N[C@@H](c1ccc(c(c1)O)C(=O)O)C(=O)O 10.1021/jm9601718
CHEMBL39372 2081 35 None 12 2 Human 4.4 pIC50 = 4.4 Binding
Inhibitory concentration for half maximal inhibition of PI hydrolysis (mGluR1a)Inhibitory concentration for half maximal inhibition of PI hydrolysis (mGluR1a)
ChEMBL 211 3 4 4 0.2 N[C@@H](c1ccc(c(c1)O)C(=O)O)C(=O)O 10.1021/jm9601718
11552320 136827 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 364 3 0 6 4.2 CC(C)c1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
CHEMBL374167 136827 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 364 3 0 6 4.2 CC(C)c1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
11552320 136827 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 364 3 0 6 4.2 CC(C)c1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
CHEMBL374167 136827 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 364 3 0 6 4.2 CC(C)c1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
11660540 85039 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 362 4 1 6 4.1 CCc1ccc(-n2cnc3c(sc4nccc(NC5CC5)c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
CHEMBL224088 85039 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 362 4 1 6 4.1 CCc1ccc(-n2cnc3c(sc4nccc(NC5CC5)c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
11660540 85039 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 362 4 1 6 4.1 CCc1ccc(-n2cnc3c(sc4nccc(NC5CC5)c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
CHEMBL224088 85039 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 362 4 1 6 4.1 CCc1ccc(-n2cnc3c(sc4nccc(NC5CC5)c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
11660511 166143 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 361 4 1 7 3.5 CCc1ccc(-n2cnc3c(sc4nccc(NCC#N)c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
CHEMBL426190 166143 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 361 4 1 7 3.5 CCc1ccc(-n2cnc3c(sc4nccc(NCC#N)c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
11501465 85103 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 364 3 0 6 3.9 CCc1ccc(-n2c(C)nc3c(sc4nccc(N(C)C)c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
CHEMBL224673 85103 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 364 3 0 6 3.9 CCc1ccc(-n2c(C)nc3c(sc4nccc(N(C)C)c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
11232413 60476 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 319 5 0 3 4.5 CCc1cc2cc(C(=O)Cc3cccc(OC)c3)ccc2nc1C 10.1021/jm049499o
CHEMBL175446 60476 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 319 5 0 3 4.5 CCc1cc2cc(C(=O)Cc3cccc(OC)c3)ccc2nc1C 10.1021/jm049499o
CHEMBL177736 62132 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 341 5 1 5 3.7 CCc1cc2cc(/C(=N\N)[C@H]3CC[C@@H](OC)CC3)ccc2nc1OC 10.1021/jm049499o
11501465 85103 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 364 3 0 6 3.9 CCc1ccc(-n2c(C)nc3c(sc4nccc(N(C)C)c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
CHEMBL224673 85103 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 364 3 0 6 3.9 CCc1ccc(-n2c(C)nc3c(sc4nccc(N(C)C)c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
11661106 85133 0 None 208 2 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 390 2 0 6 4.4 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4Cl)cnc3c12 10.1016/j.ejmech.2007.06.024
CHEMBL224898 85133 0 None 208 2 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 390 2 0 6 4.4 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4Cl)cnc3c12 10.1016/j.ejmech.2007.06.024
11661106 85133 0 None 208 2 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 390 2 0 6 4.4 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4Cl)cnc3c12 10.1016/j.ejmech.2007.06.024
CHEMBL224898 85133 0 None 208 2 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 390 2 0 6 4.4 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4Cl)cnc3c12 10.1016/j.ejmech.2007.06.024
11313361 2134 62 None - 1 Rat 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 325 3 0 4 3.9 COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1 10.1021/jm049499o
1385 2134 62 None - 1 Rat 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 325 3 0 4 3.9 COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1 10.1021/jm049499o
CHEMBL174588 2134 62 None - 1 Rat 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 325 3 0 4 3.9 COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1 10.1021/jm049499o
CHEMBL254574 2134 62 None - 1 Rat 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 325 3 0 4 3.9 COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1 10.1021/jm049499o
11382171 60715 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 338 4 0 6 3.2 CCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2n2nnnc12 10.1021/jm049499o
CHEMBL176068 60715 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 338 4 0 6 3.2 CCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2n2nnnc12 10.1021/jm049499o
11382171 60715 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 338 4 0 6 3.2 CCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2n2nnnc12 10.1021/jm049499o
CHEMBL176068 60715 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 338 4 0 6 3.2 CCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2n2nnnc12 10.1021/jm049499o
71452099 83033 0 None - 1 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [18F]FITM from mGlu1 receptor in rat brain homogenates after 1 hr by gamma countingDisplacement of [18F]FITM from mGlu1 receptor in rat brain homogenates after 1 hr by gamma counting
ChEMBL 387 5 1 6 4.4 CC(C)Nc1cc(-c2csc(N(C)C(=O)c3ccc(Cl)cc3)n2)ncn1 10.1021/jm301597s
CHEMBL2181521 83033 0 None - 1 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [18F]FITM from mGlu1 receptor in rat brain homogenates after 1 hr by gamma countingDisplacement of [18F]FITM from mGlu1 receptor in rat brain homogenates after 1 hr by gamma counting
ChEMBL 387 5 1 6 4.4 CC(C)Nc1cc(-c2csc(N(C)C(=O)c3ccc(Cl)cc3)n2)ncn1 10.1021/jm301597s
44307299 102184 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.
ChEMBL 279 4 1 4 2.8 Cc1c(C(=O)OC(C)(C)C)c[nH]c1C(=O)OCC1CC1 10.1016/s0960-894x(03)00396-2
CHEMBL302781 102184 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.
ChEMBL 279 4 1 4 2.8 Cc1c(C(=O)OC(C)(C)C)c[nH]c1C(=O)OCC1CC1 10.1016/s0960-894x(03)00396-2
11681680 142356 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 342 2 0 6 3.8 CC1CCCC(n2cnc3c(sc4nccc(N(C)C)c43)c2=O)C1 10.1016/j.ejmech.2007.06.024
CHEMBL388827 142356 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 342 2 0 6 3.8 CC1CCCC(n2cnc3c(sc4nccc(N(C)C)c43)c2=O)C1 10.1016/j.ejmech.2007.06.024
11681680 142356 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 342 2 0 6 3.8 CC1CCCC(n2cnc3c(sc4nccc(N(C)C)c43)c2=O)C1 10.1016/j.ejmech.2007.06.024
CHEMBL388827 142356 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 342 2 0 6 3.8 CC1CCCC(n2cnc3c(sc4nccc(N(C)C)c43)c2=O)C1 10.1016/j.ejmech.2007.06.024
11660511 166143 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 361 4 1 7 3.5 CCc1ccc(-n2cnc3c(sc4nccc(NCC#N)c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
CHEMBL426190 166143 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 361 4 1 7 3.5 CCc1ccc(-n2cnc3c(sc4nccc(NCC#N)c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
744275 84844 14 None 251 2 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 336 2 0 6 3.4 Cc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
CHEMBL223496 84844 14 None 251 2 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 336 2 0 6 3.4 Cc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
11609353 85093 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 314 2 0 6 3.2 CN(C)c1ccnc2sc3c(=O)n(C4CCCC4)cnc3c12 10.1016/j.ejmech.2007.06.024
CHEMBL224617 85093 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 314 2 0 6 3.2 CN(C)c1ccnc2sc3c(=O)n(C4CCCC4)cnc3c12 10.1016/j.ejmech.2007.06.024
11255377 61026 1 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 311 5 0 3 4.6 CCCc1ccc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2n1 10.1021/jm049499o
CHEMBL176279 61026 1 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 311 5 0 3 4.6 CCCc1ccc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2n1 10.1021/jm049499o
11256015 62987 4 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 331 4 0 3 4.8 CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1Cl 10.1021/jm049499o
CHEMBL178592 62987 4 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 331 4 0 3 4.8 CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1Cl 10.1021/jm049499o
11695588 143239 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 328 2 0 6 3.6 CN(C)c1ccnc2sc3c(=O)n(C4CCCCC4)cnc3c12 10.1016/j.ejmech.2007.06.024
CHEMBL389655 143239 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 328 2 0 6 3.6 CN(C)c1ccnc2sc3c(=O)n(C4CCCCC4)cnc3c12 10.1016/j.ejmech.2007.06.024
11695769 143538 0 None - 1 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 338 2 1 7 2.8 CN(C)c1ccnc2sc3c(=O)n(-c4ccccc4O)cnc3c12 10.1016/j.ejmech.2007.06.024
CHEMBL389897 143538 0 None - 1 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 338 2 1 7 2.8 CN(C)c1ccnc2sc3c(=O)n(-c4ccccc4O)cnc3c12 10.1016/j.ejmech.2007.06.024
11403753 62109 1 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 297 3 1 3 3.8 CCc1cc2cc(C(=O)C3CCC(O)CC3)ccc2nc1C 10.1021/jm049499o
CHEMBL177585 62109 1 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 297 3 1 3 3.8 CCc1cc2cc(C(=O)C3CCC(O)CC3)ccc2nc1C 10.1021/jm049499o
44387705 62396 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibitory concentration against human metabotropic glutamate receptor 1 transmembrane domainInhibitory concentration against human metabotropic glutamate receptor 1 transmembrane domain
ChEMBL 288 2 1 3 4.1 Cc1cc2cc(C(C)(C#N)c3ccccc3)ccc2nc1O 10.1021/jm049499o
CHEMBL177962 62396 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibitory concentration against human metabotropic glutamate receptor 1 transmembrane domainInhibitory concentration against human metabotropic glutamate receptor 1 transmembrane domain
ChEMBL 288 2 1 3 4.1 Cc1cc2cc(C(C)(C#N)c3ccccc3)ccc2nc1O 10.1021/jm049499o
11462007 78533 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 342 5 1 5 4.2 CCc1cc2cc(/C(=N/O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1OC 10.1021/jm049499o
CHEMBL2112047 78533 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 342 5 1 5 4.2 CCc1cc2cc(/C(=N/O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1OC 10.1021/jm049499o
10085578 62110 1 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 289 4 0 2 4.5 CCc1cc2cc(C(=O)Cc3ccccc3)ccc2nc1C 10.1021/jm049499o
CHEMBL177586 62110 1 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 289 4 0 2 4.5 CCc1cc2cc(C(=O)Cc3ccccc3)ccc2nc1C 10.1021/jm049499o
44416780 80231 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 441 6 0 7 4.6 CCc1ccc(-n2cnc3c(sc4nccc(N(C)CCc5ccccn5)c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
CHEMBL213760 80231 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 441 6 0 7 4.6 CCc1ccc(-n2cnc3c(sc4nccc(N(C)CCc5ccccn5)c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
44387723 127820 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 315 3 0 2 4.7 CCc1cc2cc(C(=O)C3Cc4ccccc4C3)ccc2nc1C 10.1021/jm049499o
CHEMBL366448 127820 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 315 3 0 2 4.7 CCc1cc2cc(C(=O)C3Cc4ccccc4C3)ccc2nc1C 10.1021/jm049499o
44307338 203799 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.
ChEMBL 339 7 1 6 3.0 CCCOC(=O)c1c(C)c(C(=O)OC(C)(C)C)c(C)n1CCCO 10.1016/s0960-894x(03)00396-2
CHEMBL68305 203799 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.
ChEMBL 339 7 1 6 3.0 CCCOC(=O)c1c(C)c(C(=O)OC(C)(C)C)c(C)n1CCCO 10.1016/s0960-894x(03)00396-2
11232604 122949 1 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 325 5 0 3 4.9 CCCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1C 10.1021/jm049499o
CHEMBL360728 122949 1 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 325 5 0 3 4.9 CCCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1C 10.1021/jm049499o
10470232 3269 23 None -1 2 Rat 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 303 3 0 3 4.0 O=C(c1ccc2c(c1)cc1c(n2)OCCC1)Cc1ccccc1 10.1021/jm049499o
1391 3269 23 None -1 2 Rat 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 303 3 0 3 4.0 O=C(c1ccc2c(c1)cc1c(n2)OCCC1)Cc1ccccc1 10.1021/jm049499o
6336 3269 23 None -1 2 Rat 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 303 3 0 3 4.0 O=C(c1ccc2c(c1)cc1c(n2)OCCC1)Cc1ccccc1 10.1021/jm049499o
CHEMBL369459 3269 23 None -1 2 Rat 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 303 3 0 3 4.0 O=C(c1ccc2c(c1)cc1c(n2)OCCC1)Cc1ccccc1 10.1021/jm049499o
11177701 61467 1 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 423 4 0 3 4.8 CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1I 10.1021/jm049499o
CHEMBL177043 61467 1 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 423 4 0 3 4.8 CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1I 10.1021/jm049499o
11383509 78927 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 383 6 0 5 4.8 CCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1C(=O)OC(C)C 10.1021/jm049499o
CHEMBL2112966 78927 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 383 6 0 5 4.8 CCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1C(=O)OC(C)C 10.1021/jm049499o
11565466 85046 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 286 2 0 6 2.4 CN(C)c1ccnc2sc3c(=O)n(C4CC4)cnc3c12 10.1016/j.ejmech.2007.06.024
CHEMBL224135 85046 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 286 2 0 6 2.4 CN(C)c1ccnc2sc3c(=O)n(C4CC4)cnc3c12 10.1016/j.ejmech.2007.06.024
11565466 85046 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 286 2 0 6 2.4 CN(C)c1ccnc2sc3c(=O)n(C4CC4)cnc3c12 10.1016/j.ejmech.2007.06.024
CHEMBL224135 85046 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 286 2 0 6 2.4 CN(C)c1ccnc2sc3c(=O)n(C4CC4)cnc3c12 10.1016/j.ejmech.2007.06.024
71457446 83030 0 None - 1 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [18F]FITM from mGlu1 receptor in rat brain homogenates after 1 hr by gamma countingDisplacement of [18F]FITM from mGlu1 receptor in rat brain homogenates after 1 hr by gamma counting
ChEMBL 378 5 1 7 3.6 CC(C)Nc1cc(-c2csc(N(C)C(=O)c3ccc(C#N)cc3)n2)ncn1 10.1021/jm301597s
CHEMBL2181519 83030 0 None - 1 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [18F]FITM from mGlu1 receptor in rat brain homogenates after 1 hr by gamma countingDisplacement of [18F]FITM from mGlu1 receptor in rat brain homogenates after 1 hr by gamma counting
ChEMBL 378 5 1 7 3.6 CC(C)Nc1cc(-c2csc(N(C)C(=O)c3ccc(C#N)cc3)n2)ncn1 10.1021/jm301597s
11186617 60571 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 332 5 0 3 4.6 CCc1cc2cc(C(=O)Cc3ccc(N(C)C)cc3)ccc2nc1C 10.1021/jm049499o
CHEMBL175997 60571 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 332 5 0 3 4.6 CCc1cc2cc(C(=O)Cc3ccc(N(C)C)cc3)ccc2nc1C 10.1021/jm049499o
44387697 60467 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 325 5 0 3 4.7 CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1CC 10.1021/jm049499o
CHEMBL175377 60467 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 325 5 0 3 4.7 CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1CC 10.1021/jm049499o
1418 3449 53 None -21 2 Human 4.2 pIC50 = 4.2 Binding
Antagonist activity at mGluR1alpha (unknown origin)Antagonist activity at mGluR1alpha (unknown origin)
ChEMBL 195 3 3 3 0.5 N[C@@H](c1ccc(cc1)C(=O)O)C(=O)O 10.1021/acs.jmedchem.1c01215
5311459 3449 53 None -21 2 Human 4.2 pIC50 = 4.2 Binding
Antagonist activity at mGluR1alpha (unknown origin)Antagonist activity at mGluR1alpha (unknown origin)
ChEMBL 195 3 3 3 0.5 N[C@@H](c1ccc(cc1)C(=O)O)C(=O)O 10.1021/acs.jmedchem.1c01215
CHEMBL94990 3449 53 None -21 2 Human 4.2 pIC50 = 4.2 Binding
Antagonist activity at mGluR1alpha (unknown origin)Antagonist activity at mGluR1alpha (unknown origin)
ChEMBL 195 3 3 3 0.5 N[C@@H](c1ccc(cc1)C(=O)O)C(=O)O 10.1021/acs.jmedchem.1c01215
1418 3449 53 None -21 2 Human 4.2 pIC50 = 4.2 Binding
Inhibitory concentration for half maximal inhibition of PI hydrolysis (mGluR1a)Inhibitory concentration for half maximal inhibition of PI hydrolysis (mGluR1a)
ChEMBL 195 3 3 3 0.5 N[C@@H](c1ccc(cc1)C(=O)O)C(=O)O 10.1021/jm9601718
5311459 3449 53 None -21 2 Human 4.2 pIC50 = 4.2 Binding
Inhibitory concentration for half maximal inhibition of PI hydrolysis (mGluR1a)Inhibitory concentration for half maximal inhibition of PI hydrolysis (mGluR1a)
ChEMBL 195 3 3 3 0.5 N[C@@H](c1ccc(cc1)C(=O)O)C(=O)O 10.1021/jm9601718
CHEMBL94990 3449 53 None -21 2 Human 4.2 pIC50 = 4.2 Binding
Inhibitory concentration for half maximal inhibition of PI hydrolysis (mGluR1a)Inhibitory concentration for half maximal inhibition of PI hydrolysis (mGluR1a)
ChEMBL 195 3 3 3 0.5 N[C@@H](c1ccc(cc1)C(=O)O)C(=O)O 10.1021/jm9601718
10058919 3690 10 None - 0 Human 4.2 pIC50 = 4.2 Binding
Antagonist activity at mGluR1alpha (unknown origin)Antagonist activity at mGluR1alpha (unknown origin)
ChEMBL 209 3 3 5 -1.0 OC(=O)[C@H](C12CC(C1)(C2)c1n[nH]nn1)N 10.1021/acs.jmedchem.1c01215
3419 3690 10 None - 0 Human 4.2 pIC50 = 4.2 Binding
Antagonist activity at mGluR1alpha (unknown origin)Antagonist activity at mGluR1alpha (unknown origin)
ChEMBL 209 3 3 5 -1.0 OC(=O)[C@H](C12CC(C1)(C2)c1n[nH]nn1)N 10.1021/acs.jmedchem.1c01215
CHEMBL2204334 3690 10 None - 0 Human 4.2 pIC50 = 4.2 Binding
Antagonist activity at mGluR1alpha (unknown origin)Antagonist activity at mGluR1alpha (unknown origin)
ChEMBL 209 3 3 5 -1.0 OC(=O)[C@H](C12CC(C1)(C2)c1n[nH]nn1)N 10.1021/acs.jmedchem.1c01215
10058919 3690 10 None - 0 Human 4.2 pIC50 = 4.2 Binding
Inhibition of mGluR1a receptorInhibition of mGluR1a receptor
ChEMBL 209 3 3 5 -1.0 OC(=O)[C@H](C12CC(C1)(C2)c1n[nH]nn1)N 10.1021/jm1013693
3419 3690 10 None - 0 Human 4.2 pIC50 = 4.2 Binding
Inhibition of mGluR1a receptorInhibition of mGluR1a receptor
ChEMBL 209 3 3 5 -1.0 OC(=O)[C@H](C12CC(C1)(C2)c1n[nH]nn1)N 10.1021/jm1013693
CHEMBL2204334 3690 10 None - 0 Human 4.2 pIC50 = 4.2 Binding
Inhibition of mGluR1a receptorInhibition of mGluR1a receptor
ChEMBL 209 3 3 5 -1.0 OC(=O)[C@H](C12CC(C1)(C2)c1n[nH]nn1)N 10.1021/jm1013693
11232871 62098 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 333 3 0 4 4.1 CCc1cc2cc(C(=O)C3COc4ccccc4O3)ccc2nc1C 10.1021/jm049499o
CHEMBL177519 62098 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 333 3 0 4 4.1 CCc1cc2cc(C(=O)C3COc4ccccc4O3)ccc2nc1C 10.1021/jm049499o
11185961 63013 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 309 3 0 4 4.0 O=C(Cc1ccsc1)c1ccc2nc3c(cc2c1)CCCO3 10.1021/jm049499o
CHEMBL178742 63013 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 309 3 0 4 4.0 O=C(Cc1ccsc1)c1ccc2nc3c(cc2c1)CCCO3 10.1021/jm049499o
11461116 78928 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 312 4 1 4 3.8 CCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1N 10.1021/jm049499o
CHEMBL2112967 78928 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 312 4 1 4 3.8 CCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1N 10.1021/jm049499o
11232604 122949 1 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 325 5 0 3 4.9 CCCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1C 10.1021/jm049499o
CHEMBL360728 122949 1 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 325 5 0 3 4.9 CCCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1C 10.1021/jm049499o
11581985 85153 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 394 6 0 7 3.6 CCc1ccc(-n2cnc3c(sc4nccc(N(C)CCOC)c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
CHEMBL225125 85153 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 394 6 0 7 3.6 CCc1ccc(-n2cnc3c(sc4nccc(N(C)CCOC)c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
11581985 85153 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 394 6 0 7 3.6 CCc1ccc(-n2cnc3c(sc4nccc(N(C)CCOC)c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
CHEMBL225125 85153 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 394 6 0 7 3.6 CCc1ccc(-n2cnc3c(sc4nccc(N(C)CCOC)c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
44307129 203825 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.
ChEMBL 330 4 1 5 3.5 Cc1c(C(=O)OC(C)C(C)(C)C)c[nH]c1C(=O)Oc1cccnc1 10.1016/s0960-894x(03)00396-2
CHEMBL68471 203825 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.
ChEMBL 330 4 1 5 3.5 Cc1c(C(=O)OC(C)C(C)(C)C)c[nH]c1C(=O)Oc1cccnc1 10.1016/s0960-894x(03)00396-2
11185961 63013 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 309 3 0 4 4.0 O=C(Cc1ccsc1)c1ccc2nc3c(cc2c1)CCCO3 10.1021/jm049499o
CHEMBL178742 63013 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 309 3 0 4 4.0 O=C(Cc1ccsc1)c1ccc2nc3c(cc2c1)CCCO3 10.1021/jm049499o
44306949 203744 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.
ChEMBL 267 4 1 4 2.8 CCCOC(=O)c1[nH]cc(C(=O)OC(C)(C)C)c1C 10.1016/s0960-894x(03)00396-2
CHEMBL67833 203744 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.
ChEMBL 267 4 1 4 2.8 CCCOC(=O)c1[nH]cc(C(=O)OC(C)(C)C)c1C 10.1016/s0960-894x(03)00396-2
11696595 85064 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 380 2 0 6 4.0 CN(C)c1ccnc2sc3c(=O)n(C45CC6CC(CC(C6)C4)C5)cnc3c12 10.1016/j.ejmech.2007.06.024
CHEMBL224322 85064 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 380 2 0 6 4.0 CN(C)c1ccnc2sc3c(=O)n(C45CC6CC(CC(C6)C4)C5)cnc3c12 10.1016/j.ejmech.2007.06.024
11696595 85064 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 380 2 0 6 4.0 CN(C)c1ccnc2sc3c(=O)n(C45CC6CC(CC(C6)C4)C5)cnc3c12 10.1016/j.ejmech.2007.06.024
CHEMBL224322 85064 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 380 2 0 6 4.0 CN(C)c1ccnc2sc3c(=O)n(C45CC6CC(CC(C6)C4)C5)cnc3c12 10.1016/j.ejmech.2007.06.024
10198359 73958 9 None - 1 Human 4.1 pIC50 = 4.1 Binding
Inhibition of mGluR1b receptorInhibition of mGluR1b receptor
ChEMBL 221 3 3 3 -0.8 N[C@H](C(=O)O)C12C3C4C1C1C2C3C41C(=O)O 10.1021/jm1013693
CHEMBL2021372 73958 9 None - 1 Human 4.1 pIC50 = 4.1 Binding
Inhibition of mGluR1b receptorInhibition of mGluR1b receptor
ChEMBL 221 3 3 3 -0.8 N[C@H](C(=O)O)C12C3C4C1C1C2C3C41C(=O)O 10.1021/jm1013693
11485531 129476 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 370 8 1 5 4.2 CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1NCCOC 10.1021/jm049499o
CHEMBL367227 129476 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 370 8 1 5 4.2 CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1NCCOC 10.1021/jm049499o
44307277 203727 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.
ChEMBL 297 5 2 5 2.3 CCCOC(=O)c1[nH]c(CO)c(C(=O)OC(C)(C)C)c1C 10.1016/s0960-894x(03)00396-2
CHEMBL67737 203727 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.
ChEMBL 297 5 2 5 2.3 CCCOC(=O)c1[nH]c(CO)c(C(=O)OC(C)(C)C)c1C 10.1016/s0960-894x(03)00396-2
44387697 60467 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 325 5 0 3 4.7 CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1CC 10.1021/jm049499o
CHEMBL175377 60467 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 325 5 0 3 4.7 CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1CC 10.1021/jm049499o
11450605 60279 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 338 3 0 4 4.0 CO[C@H]1CC[C@@H](C(=O)c2ccc3nc4c(cc3c2)CCCN4C)CC1 10.1021/jm049499o
CHEMBL174216 60279 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 338 3 0 4 4.0 CO[C@H]1CC[C@@H](C(=O)c2ccc3nc4c(cc3c2)CCCN4C)CC1 10.1021/jm049499o
11717278 85038 0 None 102 2 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 350 3 0 6 3.6 CCc1cccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)c1 10.1016/j.ejmech.2007.06.024
CHEMBL224084 85038 0 None 102 2 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 350 3 0 6 3.6 CCc1cccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)c1 10.1016/j.ejmech.2007.06.024
11403753 62109 1 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 297 3 1 3 3.8 CCc1cc2cc(C(=O)C3CCC(O)CC3)ccc2nc1C 10.1021/jm049499o
CHEMBL177585 62109 1 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 297 3 1 3 3.8 CCc1cc2cc(C(=O)C3CCC(O)CC3)ccc2nc1C 10.1021/jm049499o
11209923 63012 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 337 3 0 3 4.9 CO[C@H]1CC[C@@H](C(=O)c2ccc3nc4c(cc3c2)CCCCC4)CC1 10.1021/jm049499o
CHEMBL178741 63012 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 337 3 0 3 4.9 CO[C@H]1CC[C@@H](C(=O)c2ccc3nc4c(cc3c2)CCCCC4)CC1 10.1021/jm049499o
1379 2420 44 None - 1 Human 5.1 pIC50 = 5.1 Binding
Negative allosteric modulation of human mGluR1alpha expressed in syrian hamster AV-12 cells assessed as inhibition of quisqualate-induced phosphoinositide hydrolysisNegative allosteric modulation of human mGluR1alpha expressed in syrian hamster AV-12 cells assessed as inhibition of quisqualate-induced phosphoinositide hydrolysis
ChEMBL 209 3 3 3 0.8 OC(=O)c1ccc(c(c1)C)[C@@H](C(=O)O)N 10.1016/j.bmc.2014.12.034
5311261 2420 44 None - 1 Human 5.1 pIC50 = 5.1 Binding
Negative allosteric modulation of human mGluR1alpha expressed in syrian hamster AV-12 cells assessed as inhibition of quisqualate-induced phosphoinositide hydrolysisNegative allosteric modulation of human mGluR1alpha expressed in syrian hamster AV-12 cells assessed as inhibition of quisqualate-induced phosphoinositide hydrolysis
ChEMBL 209 3 3 3 0.8 OC(=O)c1ccc(c(c1)C)[C@@H](C(=O)O)N 10.1016/j.bmc.2014.12.034
CHEMBL94631 2420 44 None - 1 Human 5.1 pIC50 = 5.1 Binding
Negative allosteric modulation of human mGluR1alpha expressed in syrian hamster AV-12 cells assessed as inhibition of quisqualate-induced phosphoinositide hydrolysisNegative allosteric modulation of human mGluR1alpha expressed in syrian hamster AV-12 cells assessed as inhibition of quisqualate-induced phosphoinositide hydrolysis
ChEMBL 209 3 3 3 0.8 OC(=O)c1ccc(c(c1)C)[C@@H](C(=O)O)N 10.1016/j.bmc.2014.12.034
11232871 62098 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 333 3 0 4 4.1 CCc1cc2cc(C(=O)C3COc4ccccc4O3)ccc2nc1C 10.1021/jm049499o
CHEMBL177519 62098 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 333 3 0 4 4.1 CCc1cc2cc(C(=O)C3COc4ccccc4O3)ccc2nc1C 10.1021/jm049499o
11530971 85160 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 378 4 0 6 4.2 CCc1ccc(-n2c(CC)nc3c(sc4nccc(N(C)C)c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
CHEMBL225201 85160 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 378 4 0 6 4.2 CCc1ccc(-n2c(CC)nc3c(sc4nccc(N(C)C)c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
11438114 62488 1 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 303 3 0 3 4.0 O=C(Cc1ccccc1)c1ccc2cc3c(nc2c1)OCCC3 10.1021/jm049499o
CHEMBL178022 62488 1 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 303 3 0 3 4.0 O=C(Cc1ccccc1)c1ccc2cc3c(nc2c1)OCCC3 10.1021/jm049499o
11474450 78926 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 379 5 0 4 5.9 CCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1-c1ccsc1 10.1021/jm049499o
CHEMBL2112965 78926 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 379 5 0 4 5.9 CCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1-c1ccsc1 10.1021/jm049499o
11530971 85160 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 378 4 0 6 4.2 CCc1ccc(-n2c(CC)nc3c(sc4nccc(N(C)C)c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
CHEMBL225201 85160 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 378 4 0 6 4.2 CCc1ccc(-n2c(CC)nc3c(sc4nccc(N(C)C)c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
44421618 85195 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 378 2 0 6 4.4 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(C(C)(C)C)cc4)cnc3c12 10.1016/j.ejmech.2007.06.024
CHEMBL225439 85195 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 378 2 0 6 4.4 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(C(C)(C)C)cc4)cnc3c12 10.1016/j.ejmech.2007.06.024
11324832 60516 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 325 5 0 3 4.9 CCc1cc2cc(C(=O)C[C@H]3CC[C@@H](OC)CC3)ccc2nc1C 10.1021/jm049499o
CHEMBL175699 60516 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 325 5 0 3 4.9 CCc1cc2cc(C(=O)C[C@H]3CC[C@@H](OC)CC3)ccc2nc1C 10.1021/jm049499o
11186076 169335 1 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 313 4 1 4 3.9 CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1O 10.1021/jm049499o
CHEMBL441844 169335 1 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 313 4 1 4 3.9 CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1O 10.1021/jm049499o
11347669 120401 1 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 317 4 0 3 4.4 O=C(CCc1ccccc1)c1ccc2nc3c(cc2c1)CCCO3 10.1021/jm049499o
CHEMBL353547 120401 1 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1
ChEMBL 317 4 0 3 4.4 O=C(CCc1ccccc1)c1ccc2nc3c(cc2c1)CCCO3 10.1021/jm049499o
44421618 85195 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 378 2 0 6 4.4 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(C(C)(C)C)cc4)cnc3c12 10.1016/j.ejmech.2007.06.024
CHEMBL225439 85195 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 378 2 0 6 4.4 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(C(C)(C)C)cc4)cnc3c12 10.1016/j.ejmech.2007.06.024
11588590 142035 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 362 3 0 6 3.9 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(C5CC5)cc4)cnc3c12 10.1016/j.ejmech.2007.06.024
CHEMBL387687 142035 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 362 3 0 6 3.9 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(C5CC5)cc4)cnc3c12 10.1016/j.ejmech.2007.06.024
11588590 142035 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 362 3 0 6 3.9 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(C5CC5)cc4)cnc3c12 10.1016/j.ejmech.2007.06.024
CHEMBL387687 142035 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 362 3 0 6 3.9 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(C5CC5)cc4)cnc3c12 10.1016/j.ejmech.2007.06.024
1378 2417 54 None - 10 Rat 5.1 pIC50 = 5.1 Binding
Concentration required to inhibit metabotropic glutamate receptor 1 activity of rat expressed in CHO cellsConcentration required to inhibit metabotropic glutamate receptor 1 activity of rat expressed in CHO cells
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/jm0400294
1399 2417 54 None - 10 Rat 5.1 pIC50 = 5.1 Binding
Concentration required to inhibit metabotropic glutamate receptor 1 activity of rat expressed in CHO cellsConcentration required to inhibit metabotropic glutamate receptor 1 activity of rat expressed in CHO cells
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/jm0400294
9819927 2417 54 None - 10 Rat 5.1 pIC50 = 5.1 Binding
Concentration required to inhibit metabotropic glutamate receptor 1 activity of rat expressed in CHO cellsConcentration required to inhibit metabotropic glutamate receptor 1 activity of rat expressed in CHO cells
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/jm0400294
CHEMBL432038 2417 54 None - 10 Rat 5.1 pIC50 = 5.1 Binding
Concentration required to inhibit metabotropic glutamate receptor 1 activity of rat expressed in CHO cellsConcentration required to inhibit metabotropic glutamate receptor 1 activity of rat expressed in CHO cells
ChEMBL 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 10.1021/jm0400294
11717278 85038 0 None 102 2 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 350 3 0 6 3.6 CCc1cccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)c1 10.1016/j.ejmech.2007.06.024
CHEMBL224084 85038 0 None 102 2 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 350 3 0 6 3.6 CCc1cccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)c1 10.1016/j.ejmech.2007.06.024
11174504 78925 4 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 315 4 0 3 4.3 CCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1F 10.1021/jm049499o
CHEMBL2112964 78925 4 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 315 4 0 3 4.3 CCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1F 10.1021/jm049499o
1397 2529 15 None - 5 Rat 4.0 pIC50 = 4.0 Binding
Concentration required to inhibit metabotropic glutamate receptor 1 activity of rat expressed in CHO cellsConcentration required to inhibit metabotropic glutamate receptor 1 activity of rat expressed in CHO cells
ChEMBL 377 5 3 4 2.1 OC(=O)[C@]1(N)[C@H](OCc2ccc(c(c2)Cl)Cl)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O 10.1021/jm0400294
9886034 2529 15 None - 5 Rat 4.0 pIC50 = 4.0 Binding
Concentration required to inhibit metabotropic glutamate receptor 1 activity of rat expressed in CHO cellsConcentration required to inhibit metabotropic glutamate receptor 1 activity of rat expressed in CHO cells
ChEMBL 377 5 3 4 2.1 OC(=O)[C@]1(N)[C@H](OCc2ccc(c(c2)Cl)Cl)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O 10.1021/jm0400294
CHEMBL186453 2529 15 None - 5 Rat 4.0 pIC50 = 4.0 Binding
Concentration required to inhibit metabotropic glutamate receptor 1 activity of rat expressed in CHO cellsConcentration required to inhibit metabotropic glutamate receptor 1 activity of rat expressed in CHO cells
ChEMBL 377 5 3 4 2.1 OC(=O)[C@]1(N)[C@H](OCc2ccc(c(c2)Cl)Cl)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O 10.1021/jm0400294
10245890 1982 7 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 327 5 0 4 4.2 CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)OC)CC 10.1021/jm049499o
6474 1982 7 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 327 5 0 4 4.2 CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)OC)CC 10.1021/jm049499o
CHEMBL175643 1982 7 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor
ChEMBL 327 5 0 4 4.2 CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)OC)CC 10.1021/jm049499o
11681575 137177 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 336 3 1 6 3.6 CCc1ccc(-n2cnc3c(sc4nccc(NC)c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
CHEMBL374815 137177 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 336 3 1 6 3.6 CCc1ccc(-n2cnc3c(sc4nccc(NC)c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
11681575 137177 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 336 3 1 6 3.6 CCc1ccc(-n2cnc3c(sc4nccc(NC)c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
CHEMBL374815 137177 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 336 3 1 6 3.6 CCc1ccc(-n2cnc3c(sc4nccc(NC)c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
11582178 137927 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 404 4 1 6 4.5 CCc1ccc(-n2cnc3c(sc4nccc(NCC(F)(F)F)c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
CHEMBL376372 137927 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 404 4 1 6 4.5 CCc1ccc(-n2cnc3c(sc4nccc(NCC(F)(F)F)c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
11582178 137927 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 404 4 1 6 4.5 CCc1ccc(-n2cnc3c(sc4nccc(NCC(F)(F)F)c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
CHEMBL376372 137927 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Inhibition of rat mGluR1Inhibition of rat mGluR1
ChEMBL 404 4 1 6 4.5 CCc1ccc(-n2cnc3c(sc4nccc(NCC(F)(F)F)c43)c2=O)cc1 10.1016/j.ejmech.2007.06.024
16659802 1038 0 None - 1 Rat 9.7 pKi = 9.7 Binding
Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane
ChEMBL 384 1 1 7 3.8 C[C@@H]1CNc2c(O1)cnc1c2c2ncn(c(=O)c2s1)c1ccc(cc1)Cl 10.1021/jm070590c
6348 1038 0 None - 1 Rat 9.7 pKi = 9.7 Binding
Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane
ChEMBL 384 1 1 7 3.8 C[C@@H]1CNc2c(O1)cnc1c2c2ncn(c(=O)c2s1)c1ccc(cc1)Cl 10.1021/jm070590c
CHEMBL241327 1038 0 None - 1 Rat 9.7 pKi = 9.7 Binding
Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane
ChEMBL 384 1 1 7 3.8 C[C@@H]1CNc2c(O1)cnc1c2c2ncn(c(=O)c2s1)c1ccc(cc1)Cl 10.1021/jm070590c
23657393 88742 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane
ChEMBL 380 2 1 8 3.2 COc1ccc(-n2cnc3c(sc4ncc5c(c43)NC[C@@H](C)O5)c2=O)cc1 10.1021/jm070590c
CHEMBL236177 88742 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane
ChEMBL 380 2 1 8 3.2 COc1ccc(-n2cnc3c(sc4ncc5c(c43)NC[C@@H](C)O5)c2=O)cc1 10.1021/jm070590c
11313361 2134 62 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity to mGluR1Binding affinity to mGluR1
ChEMBL 325 3 0 4 3.9 COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1 10.1016/j.bmc.2010.11.048
1385 2134 62 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity to mGluR1Binding affinity to mGluR1
ChEMBL 325 3 0 4 3.9 COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1 10.1016/j.bmc.2010.11.048
CHEMBL174588 2134 62 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity to mGluR1Binding affinity to mGluR1
ChEMBL 325 3 0 4 3.9 COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1 10.1016/j.bmc.2010.11.048
CHEMBL254574 2134 62 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity to mGluR1Binding affinity to mGluR1
ChEMBL 325 3 0 4 3.9 COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1 10.1016/j.bmc.2010.11.048
15985249 197255 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding affinity to mGluR1Binding affinity to mGluR1
ChEMBL 351 4 0 5 3.1 CCCN1Cc2cc(-c3nnn(-c4cccnc4F)c3C)ccc2C1=O 10.1016/j.bmc.2010.11.048
CHEMBL1645349 197255 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding affinity to mGluR1Binding affinity to mGluR1
ChEMBL 351 4 0 5 3.1 CCCN1Cc2cc(-c3nnn(-c4cccnc4F)c3C)ccc2C1=O 10.1016/j.bmc.2010.11.048
CHEMBL568443 197255 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding affinity to mGluR1Binding affinity to mGluR1
ChEMBL 351 4 0 5 3.1 CCCN1Cc2cc(-c3nnn(-c4cccnc4F)c3C)ccc2C1=O 10.1016/j.bmc.2010.11.048
15985249 197255 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding affinity to mGluR1 by PET analysisBinding affinity to mGluR1 by PET analysis
ChEMBL 351 4 0 5 3.1 CCCN1Cc2cc(-c3nnn(-c4cccnc4F)c3C)ccc2C1=O 10.1016/j.bmcl.2011.03.046
CHEMBL1645349 197255 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding affinity to mGluR1 by PET analysisBinding affinity to mGluR1 by PET analysis
ChEMBL 351 4 0 5 3.1 CCCN1Cc2cc(-c3nnn(-c4cccnc4F)c3C)ccc2C1=O 10.1016/j.bmcl.2011.03.046
CHEMBL568443 197255 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding affinity to mGluR1 by PET analysisBinding affinity to mGluR1 by PET analysis
ChEMBL 351 4 0 5 3.1 CCCN1Cc2cc(-c3nnn(-c4cccnc4F)c3C)ccc2C1=O 10.1016/j.bmcl.2011.03.046
16659801 1036 0 None - 1 Rat 9.4 pKi = 9.4 Binding
Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane
ChEMBL 370 1 1 7 3.5 Clc1ccc(cc1)n1cnc2c(c1=O)sc1c2c2NCCOc2cn1 10.1021/jm070590c
6346 1036 0 None - 1 Rat 9.4 pKi = 9.4 Binding
Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane
ChEMBL 370 1 1 7 3.5 Clc1ccc(cc1)n1cnc2c(c1=O)sc1c2c2NCCOc2cn1 10.1021/jm070590c
CHEMBL236994 1036 0 None - 1 Rat 9.4 pKi = 9.4 Binding
Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane
ChEMBL 370 1 1 7 3.5 Clc1ccc(cc1)n1cnc2c(c1=O)sc1c2c2NCCOc2cn1 10.1021/jm070590c
16659966 88686 0 None - 1 Rat 9.3 pKi = 9.3 Binding
Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane
ChEMBL 350 1 1 7 3.1 Cc1ccc(-n2cnc3c(sc4ncc5c(c43)NCCO5)c2=O)cc1 10.1021/jm070590c
CHEMBL235975 88686 0 None - 1 Rat 9.3 pKi = 9.3 Binding
Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane
ChEMBL 350 1 1 7 3.1 Cc1ccc(-n2cnc3c(sc4ncc5c(c43)NCCO5)c2=O)cc1 10.1021/jm070590c
16659805 148612 0 None - 1 Rat 9.3 pKi = 9.3 Binding
Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane
ChEMBL 384 1 1 7 3.8 C[C@H]1COc2cnc3sc4c(=O)n(-c5ccc(Cl)cc5)cnc4c3c2N1 10.1021/jm070590c
CHEMBL393923 148612 0 None - 1 Rat 9.3 pKi = 9.3 Binding
Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane
ChEMBL 384 1 1 7 3.8 C[C@H]1COc2cnc3sc4c(=O)n(-c5ccc(Cl)cc5)cnc4c3c2N1 10.1021/jm070590c
16659968 88687 0 None - 1 Rat 9.2 pKi = 9.2 Binding
Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane
ChEMBL 364 1 1 7 3.5 Cc1ccc(-n2cnc3c(sc4ncc5c(c43)NC[C@@H](C)O5)c2=O)cc1 10.1021/jm070590c
CHEMBL235977 88687 0 None - 1 Rat 9.2 pKi = 9.2 Binding
Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane
ChEMBL 364 1 1 7 3.5 Cc1ccc(-n2cnc3c(sc4ncc5c(c43)NC[C@@H](C)O5)c2=O)cc1 10.1021/jm070590c
7442 2135 6 None 1 3 Human 9.1 pKi = 9.1 Binding
Binding affinity to mGluR1Binding affinity to mGluR1
ChEMBL 311 4 0 3 4.5 CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)C)CC 10.1016/j.bmc.2010.11.048
9948645 2135 6 None 1 3 Human 9.1 pKi = 9.1 Binding
Binding affinity to mGluR1Binding affinity to mGluR1
ChEMBL 311 4 0 3 4.5 CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)C)CC 10.1016/j.bmc.2010.11.048
CHEMBL188906 2135 6 None 1 3 Human 9.1 pKi = 9.1 Binding
Binding affinity to mGluR1Binding affinity to mGluR1
ChEMBL 311 4 0 3 4.5 CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)C)CC 10.1016/j.bmc.2010.11.048
CHEMBL253345 2135 6 None 1 3 Human 9.1 pKi = 9.1 Binding
Binding affinity to mGluR1Binding affinity to mGluR1
ChEMBL 311 4 0 3 4.5 CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)C)CC 10.1016/j.bmc.2010.11.048
7442 2135 6 None 1 3 Human 9.1 pKi = 9.1 Binding
Binding affinity to mGluR1 by PET analysisBinding affinity to mGluR1 by PET analysis
ChEMBL 311 4 0 3 4.5 CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)C)CC 10.1016/j.bmcl.2011.03.046
9948645 2135 6 None 1 3 Human 9.1 pKi = 9.1 Binding
Binding affinity to mGluR1 by PET analysisBinding affinity to mGluR1 by PET analysis
ChEMBL 311 4 0 3 4.5 CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)C)CC 10.1016/j.bmcl.2011.03.046
CHEMBL188906 2135 6 None 1 3 Human 9.1 pKi = 9.1 Binding
Binding affinity to mGluR1 by PET analysisBinding affinity to mGluR1 by PET analysis
ChEMBL 311 4 0 3 4.5 CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)C)CC 10.1016/j.bmcl.2011.03.046
CHEMBL253345 2135 6 None 1 3 Human 9.1 pKi = 9.1 Binding
Binding affinity to mGluR1 by PET analysisBinding affinity to mGluR1 by PET analysis
ChEMBL 311 4 0 3 4.5 CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)C)CC 10.1016/j.bmcl.2011.03.046
7442 2135 6 None -1 3 Rat 9.1 pKi = 9.1 Binding
In vitro affinity for cloned rat metabotropic glutamate 1 receptors stably expressed on CHO cells determined using [3H]-R214127 as radioligandIn vitro affinity for cloned rat metabotropic glutamate 1 receptors stably expressed on CHO cells determined using [3H]-R214127 as radioligand
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/jm050263+
9948645 2135 6 None -1 3 Rat 9.1 pKi = 9.1 Binding
In vitro affinity for cloned rat metabotropic glutamate 1 receptors stably expressed on CHO cells determined using [3H]-R214127 as radioligandIn vitro affinity for cloned rat metabotropic glutamate 1 receptors stably expressed on CHO cells determined using [3H]-R214127 as radioligand
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/jm050263+
CHEMBL188906 2135 6 None -1 3 Rat 9.1 pKi = 9.1 Binding
In vitro affinity for cloned rat metabotropic glutamate 1 receptors stably expressed on CHO cells determined using [3H]-R214127 as radioligandIn vitro affinity for cloned rat metabotropic glutamate 1 receptors stably expressed on CHO cells determined using [3H]-R214127 as radioligand
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/jm050263+
CHEMBL253345 2135 6 None -1 3 Rat 9.1 pKi = 9.1 Binding
In vitro affinity for cloned rat metabotropic glutamate 1 receptors stably expressed on CHO cells determined using [3H]-R214127 as radioligandIn vitro affinity for cloned rat metabotropic glutamate 1 receptors stably expressed on CHO cells determined using [3H]-R214127 as radioligand
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/jm050263+
16659967 1035 0 None - 1 Rat 9.0 pKi = 9 Binding
Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane
ChEMBL 366 2 1 8 2.8 COc1ccc(cc1)n1cnc2c(c1=O)sc1c2c2NCCOc2cn1 10.1021/jm070590c
6345 1035 0 None - 1 Rat 9.0 pKi = 9 Binding
Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane
ChEMBL 366 2 1 8 2.8 COc1ccc(cc1)n1cnc2c(c1=O)sc1c2c2NCCOc2cn1 10.1021/jm070590c
CHEMBL393922 1035 0 None - 1 Rat 9.0 pKi = 9 Binding
Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane
ChEMBL 366 2 1 8 2.8 COc1ccc(cc1)n1cnc2c(c1=O)sc1c2c2NCCOc2cn1 10.1021/jm070590c
11574901 85224 0 None - 1 Rat 9.0 pKi = 9 Binding
Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes
ChEMBL 400 2 0 6 3.8 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12 10.1021/jm0504407
CHEMBL225590 85224 0 None - 1 Rat 9.0 pKi = 9 Binding
Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes
ChEMBL 400 2 0 6 3.8 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12 10.1021/jm0504407
16659803 1037 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane
ChEMBL 384 1 1 7 3.8 C[C@H]1CNc2c(O1)cnc1c2c2ncn(c(=O)c2s1)c1ccc(cc1)Cl 10.1021/jm070590c
6338 1037 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane
ChEMBL 384 1 1 7 3.8 C[C@H]1CNc2c(O1)cnc1c2c2ncn(c(=O)c2s1)c1ccc(cc1)Cl 10.1021/jm070590c
CHEMBL236180 1037 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane
ChEMBL 384 1 1 7 3.8 C[C@H]1CNc2c(O1)cnc1c2c2ncn(c(=O)c2s1)c1ccc(cc1)Cl 10.1021/jm070590c
1370 3263 67 None 17 8 Rat 8.0 pKi = 8 Binding
Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cellsInhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm010323l
1372 3263 67 None 17 8 Rat 8.0 pKi = 8 Binding
Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cellsInhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm010323l
40539 3263 67 None 17 8 Rat 8.0 pKi = 8 Binding
Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cellsInhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm010323l
6971145 3263 67 None 17 8 Rat 8.0 pKi = 8 Binding
Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cellsInhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm010323l
CHEMBL279956 3263 67 None 17 8 Rat 8.0 pKi = 8 Binding
Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cellsInhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm010323l
DB02999 3263 67 None 17 8 Rat 8.0 pKi = 8 Binding
Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cellsInhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells
ChEMBL 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 10.1021/jm010323l
16659963 149875 0 None - 1 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane
ChEMBL 353 1 1 6 3.5 O=c1c2sc3ncc4nc[nH]c4c3c2ncn1-c1ccc(Cl)cc1 10.1021/jm070590c
CHEMBL394914 149875 0 None - 1 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane
ChEMBL 353 1 1 6 3.5 O=c1c2sc3ncc4nc[nH]c4c3c2ncn1-c1ccc(Cl)cc1 10.1021/jm070590c
16659799 146389 0 None - 1 Rat 6.0 pKi = 6 Binding
Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane
ChEMBL 366 1 1 7 3.2 Cc1ccc(-n2cnc3c(sc4ncc5sc(=O)[nH]c5c43)c2=O)cc1 10.1021/jm070590c
CHEMBL392164 146389 0 None - 1 Rat 6.0 pKi = 6 Binding
Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane
ChEMBL 366 1 1 7 3.2 Cc1ccc(-n2cnc3c(sc4ncc5sc(=O)[nH]c5c43)c2=O)cc1 10.1021/jm070590c
16659647 167413 0 None - 1 Rat 6.0 pKi = 6 Binding
Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane
ChEMBL 382 1 1 7 4.6 Cc1ccc(-n2cnc3c(sc4ncc5sc(=S)[nH]c5c43)c2=O)cc1 10.1021/jm070590c
CHEMBL429635 167413 0 None - 1 Rat 6.0 pKi = 6 Binding
Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane
ChEMBL 382 1 1 7 4.6 Cc1ccc(-n2cnc3c(sc4ncc5sc(=S)[nH]c5c43)c2=O)cc1 10.1021/jm070590c
16659964 89960 0 None - 1 Rat 7.0 pKi = 7.0 Binding
Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane
ChEMBL 367 1 0 7 3.5 Cn1cnc2cnc3sc4c(=O)n(-c5ccc(Cl)cc5)cnc4c3c21 10.1021/jm070590c
CHEMBL238090 89960 0 None - 1 Rat 7.0 pKi = 7.0 Binding
Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane
ChEMBL 367 1 0 7 3.5 Cn1cnc2cnc3sc4c(=O)n(-c5ccc(Cl)cc5)cnc4c3c21 10.1021/jm070590c
11661106 85133 0 None 208 2 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes
ChEMBL 390 2 0 6 4.4 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4Cl)cnc3c12 10.1021/jm0504407
CHEMBL224898 85133 0 None 208 2 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes
ChEMBL 390 2 0 6 4.4 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4Cl)cnc3c12 10.1021/jm0504407
25067015 195613 0 None -4 3 Human 7.0 pKi = 7.0 Binding
Binding affinity to human GluR1 by FLIPR assayBinding affinity to human GluR1 by FLIPR assay
ChEMBL 366 4 0 4 3.8 O=C(C1CC1c1ccc(N2CCOCC2)nc1)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmc.2009.05.072
CHEMBL556070 195613 0 None -4 3 Human 7.0 pKi = 7.0 Binding
Binding affinity to human GluR1 by FLIPR assayBinding affinity to human GluR1 by FLIPR assay
ChEMBL 366 4 0 4 3.8 O=C(C1CC1c1ccc(N2CCOCC2)nc1)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmc.2009.05.072
16660470 76629 0 None - 1 Rat 7.9 pKi = 7.9 Binding
Displacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hrDisplacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hr
ChEMBL 383 6 1 7 3.7 COc1ccc(C(=O)N(C)c2nc(-c3cc(NC(C)C)ncn3)cs2)cc1 10.1021/jm201590g
CHEMBL2063722 76629 0 None - 1 Rat 7.9 pKi = 7.9 Binding
Displacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hrDisplacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hr
ChEMBL 383 6 1 7 3.7 COc1ccc(C(=O)N(C)c2nc(-c3cc(NC(C)C)ncn3)cs2)cc1 10.1021/jm201590g
71459305 83032 0 None - 1 Rat 7.9 pKi = 7.9 Binding
Displacement of [18F]FITM from mGlu1 receptor in rat brain homogenates after 1 hr by gamma countingDisplacement of [18F]FITM from mGlu1 receptor in rat brain homogenates after 1 hr by gamma counting
ChEMBL 367 5 1 6 4.0 Cc1ccc(C(=O)N(C)c2nc(-c3cc(NC(C)C)ncn3)cs2)cc1 10.1021/jm301597s
CHEMBL2181520 83032 0 None - 1 Rat 7.9 pKi = 7.9 Binding
Displacement of [18F]FITM from mGlu1 receptor in rat brain homogenates after 1 hr by gamma countingDisplacement of [18F]FITM from mGlu1 receptor in rat brain homogenates after 1 hr by gamma counting
ChEMBL 367 5 1 6 4.0 Cc1ccc(C(=O)N(C)c2nc(-c3cc(NC(C)C)ncn3)cs2)cc1 10.1021/jm301597s
24759782 196640 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation countingDisplacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation counting
ChEMBL 331 3 0 2 5.1 O=C(C1CC1c1cnc2ccccc2c1)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmc.2009.05.072
CHEMBL564327 196640 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation countingDisplacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation counting
ChEMBL 331 3 0 2 5.1 O=C(C1CC1c1cnc2ccccc2c1)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmc.2009.05.072
11501188 137543 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes
ChEMBL 350 3 0 6 3.6 CCc1ccccc1-n1cnc2c(sc3nccc(N(C)C)c32)c1=O 10.1021/jm0504407
CHEMBL375439 137543 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes
ChEMBL 350 3 0 6 3.6 CCc1ccccc1-n1cnc2c(sc3nccc(N(C)C)c32)c1=O 10.1021/jm0504407
70688666 76630 0 None - 1 Rat 6.8 pKi = 6.8 Binding
Displacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hrDisplacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hr
ChEMBL 415 8 1 7 4.0 CC(C)Nc1cc(-c2csc(N(C)C(=O)c3ccc(OCCF)cc3)n2)ncn1 10.1021/jm201590g
CHEMBL2063723 76630 0 None - 1 Rat 6.8 pKi = 6.8 Binding
Displacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hrDisplacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hr
ChEMBL 415 8 1 7 4.0 CC(C)Nc1cc(-c2csc(N(C)C(=O)c3ccc(OCCF)cc3)n2)ncn1 10.1021/jm201590g
1310 2315 110 None -1 18 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cellsDisplacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1039/C1MD00186H
1369 2315 110 None -1 18 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cellsDisplacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1039/C1MD00186H
33032 2315 110 None -1 18 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cellsDisplacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1039/C1MD00186H
44272391 2315 110 None -1 18 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cellsDisplacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1039/C1MD00186H
88747398 2315 110 None -1 18 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cellsDisplacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1039/C1MD00186H
CHEMBL575060 2315 110 None -1 18 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cellsDisplacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1039/C1MD00186H
DB00142 2315 110 None -1 18 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cellsDisplacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1039/C1MD00186H
16659645 148333 0 None - 1 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane
ChEMBL 332 1 1 5 3.8 Cc1ccc(-n2cnc3c(sc4ncc5cc[nH]c5c43)c2=O)cc1 10.1021/jm070590c
CHEMBL393705 148333 0 None - 1 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane
ChEMBL 332 1 1 5 3.8 Cc1ccc(-n2cnc3c(sc4ncc5cc[nH]c5c43)c2=O)cc1 10.1021/jm070590c
16038352 90219 0 None - 1 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane
ChEMBL 333 1 1 6 3.2 Cc1ccc(-n2cnc3c(sc4ncc5cn[nH]c5c43)c2=O)cc1 10.1021/jm070590c
CHEMBL238262 90219 0 None - 1 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane
ChEMBL 333 1 1 6 3.2 Cc1ccc(-n2cnc3c(sc4ncc5cn[nH]c5c43)c2=O)cc1 10.1021/jm070590c
5766228 195633 20 None - 1 Rat 4.8 pKi = 4.8 Binding
Displacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation countingDisplacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by 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 195633 20 None - 1 Rat 4.8 pKi = 4.8 Binding
Displacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation countingDisplacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by 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
87549991 122205 0 None -61 3 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometry
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 122205 0 None -61 3 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometry
ChEMBL 333 2 0 4 3.9 Cc1cccc(C#CC=C2CCN(c3ncccc3[N+](=O)[O-])CC2)c1 10.1016/j.bmc.2015.05.008
87550873 122206 0 None -46 3 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometry
ChEMBL 353 2 0 4 4.2 O=[N+]([O-])c1cccnc1N1CCC(=CC#Cc2cccc(Cl)c2)CC1 10.1016/j.bmc.2015.05.008
CHEMBL3597598 122206 0 None -46 3 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometry
ChEMBL 353 2 0 4 4.2 O=[N+]([O-])c1cccnc1N1CCC(=CC#Cc2cccc(Cl)c2)CC1 10.1016/j.bmc.2015.05.008
25183668 122202 0 None -6025 3 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]MPEP from rat mGlu1 receptor expressed in CHO-TREx cell membranes after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]MPEP from rat mGlu1 receptor expressed in CHO-TREx cell membranes after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 334 2 0 5 3.3 Cc1cccc(C#CC=C2CCN(c3ncccc3[N+](=O)[O-])CC2)n1 10.1021/acs.jmedchem.8b01226
CHEMBL3597594 122202 0 None -6025 3 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]MPEP from rat mGlu1 receptor expressed in CHO-TREx cell membranes after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]MPEP from rat mGlu1 receptor expressed in CHO-TREx cell membranes after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 334 2 0 5 3.3 Cc1cccc(C#CC=C2CCN(c3ncccc3[N+](=O)[O-])CC2)n1 10.1021/acs.jmedchem.8b01226
25183668 122202 0 None -6025 3 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometry
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 122202 0 None -6025 3 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometry
ChEMBL 334 2 0 5 3.3 Cc1cccc(C#CC=C2CCN(c3ncccc3[N+](=O)[O-])CC2)n1 10.1016/j.bmc.2015.05.008
122183738 122208 0 None -630 3 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometry
ChEMBL 359 2 0 6 3.1 Cc1ccc([N+](=O)[O-])c(N2CCC(=CC#Cc3ccc(C#N)cn3)CC2)n1 10.1016/j.bmc.2015.05.008
CHEMBL3597600 122208 0 None -630 3 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometry
ChEMBL 359 2 0 6 3.1 Cc1ccc([N+](=O)[O-])c(N2CCC(=CC#Cc3ccc(C#N)cn3)CC2)n1 10.1016/j.bmc.2015.05.008
16659642 90220 0 None - 1 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane
ChEMBL 353 1 1 6 3.5 O=c1c2sc3ncc4cn[nH]c4c3c2ncn1-c1ccc(Cl)cc1 10.1021/jm070590c
CHEMBL238263 90220 0 None - 1 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane
ChEMBL 353 1 1 6 3.5 O=c1c2sc3ncc4cn[nH]c4c3c2ncn1-c1ccc(Cl)cc1 10.1021/jm070590c
11245287 1697 34 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to mGluR1 by PET analysisBinding affinity to mGluR1 by PET analysis
ChEMBL 358 3 0 5 2.7 CC(N(C(=O)N1CCC(=CC1)c1nnn(c1C)c1cccnc1F)C)C 10.1016/j.bmcl.2011.03.046
6363 1697 34 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to mGluR1 by PET analysisBinding affinity to mGluR1 by PET analysis
ChEMBL 358 3 0 5 2.7 CC(N(C(=O)N1CCC(=CC1)c1nnn(c1C)c1cccnc1F)C)C 10.1016/j.bmcl.2011.03.046
CHEMBL502882 1697 34 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to mGluR1 by PET analysisBinding affinity to mGluR1 by PET analysis
ChEMBL 358 3 0 5 2.7 CC(N(C(=O)N1CCC(=CC1)c1nnn(c1C)c1cccnc1F)C)C 10.1016/j.bmcl.2011.03.046
744275 84844 14 None 251 2 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes
ChEMBL 336 2 0 6 3.4 Cc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1 10.1021/jm0504407
CHEMBL223496 84844 14 None 251 2 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes
ChEMBL 336 2 0 6 3.4 Cc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1 10.1021/jm0504407
16659643 89956 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane
ChEMBL 352 1 1 5 4.1 O=c1c2sc3ncc4cc[nH]c4c3c2ncn1-c1ccc(Cl)cc1 10.1021/jm070590c
CHEMBL238077 89956 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane
ChEMBL 352 1 1 5 4.1 O=c1c2sc3ncc4cc[nH]c4c3c2ncn1-c1ccc(Cl)cc1 10.1021/jm070590c
44517772 195556 0 None 38 2 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation countingDisplacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation counting
ChEMBL 317 3 0 2 5.0 O=C(/C=C/c1cnc2ccccc2c1)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmc.2009.05.072
CHEMBL554700 195556 0 None 38 2 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation countingDisplacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation counting
ChEMBL 317 3 0 2 5.0 O=C(/C=C/c1cnc2ccccc2c1)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmc.2009.05.072
71452099 83033 0 None - 1 Rat 7.7 pKi = 7.7 Binding
Displacement of [18F]FITM from mGlu1 receptor in rat brain homogenates after 1 hr by gamma countingDisplacement of [18F]FITM from mGlu1 receptor in rat brain homogenates after 1 hr by gamma counting
ChEMBL 387 5 1 6 4.4 CC(C)Nc1cc(-c2csc(N(C)C(=O)c3ccc(Cl)cc3)n2)ncn1 10.1021/jm301597s
CHEMBL2181521 83033 0 None - 1 Rat 7.7 pKi = 7.7 Binding
Displacement of [18F]FITM from mGlu1 receptor in rat brain homogenates after 1 hr by gamma countingDisplacement of [18F]FITM from mGlu1 receptor in rat brain homogenates after 1 hr by gamma counting
ChEMBL 387 5 1 6 4.4 CC(C)Nc1cc(-c2csc(N(C)C(=O)c3ccc(Cl)cc3)n2)ncn1 10.1021/jm301597s
25067015 195613 0 None 4 3 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation countingDisplacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation counting
ChEMBL 366 4 0 4 3.8 O=C(C1CC1c1ccc(N2CCOCC2)nc1)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmc.2009.05.072
CHEMBL556070 195613 0 None 4 3 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation countingDisplacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation counting
ChEMBL 366 4 0 4 3.8 O=C(C1CC1c1ccc(N2CCOCC2)nc1)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmc.2009.05.072
1310 2315 110 None -1 18 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cellsDisplacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm070322e
1369 2315 110 None -1 18 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cellsDisplacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm070322e
33032 2315 110 None -1 18 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cellsDisplacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm070322e
44272391 2315 110 None -1 18 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cellsDisplacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm070322e
88747398 2315 110 None -1 18 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cellsDisplacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm070322e
CHEMBL575060 2315 110 None -1 18 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cellsDisplacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm070322e
DB00142 2315 110 None -1 18 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cellsDisplacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm070322e
11717319 143494 0 None - 1 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes
ChEMBL 353 3 0 8 2.5 COc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cn1 10.1021/jm0504407
CHEMBL389870 143494 0 None - 1 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes
ChEMBL 353 3 0 8 2.5 COc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cn1 10.1021/jm0504407
71457446 83030 0 None - 1 Rat 7.6 pKi = 7.6 Binding
Displacement of [18F]FITM from mGlu1 receptor in rat brain homogenates after 1 hr by gamma countingDisplacement of [18F]FITM from mGlu1 receptor in rat brain homogenates after 1 hr by gamma counting
ChEMBL 378 5 1 7 3.6 CC(C)Nc1cc(-c2csc(N(C)C(=O)c3ccc(C#N)cc3)n2)ncn1 10.1021/jm301597s
CHEMBL2181519 83030 0 None - 1 Rat 7.6 pKi = 7.6 Binding
Displacement of [18F]FITM from mGlu1 receptor in rat brain homogenates after 1 hr by gamma countingDisplacement of [18F]FITM from mGlu1 receptor in rat brain homogenates after 1 hr by gamma counting
ChEMBL 378 5 1 7 3.6 CC(C)Nc1cc(-c2csc(N(C)C(=O)c3ccc(C#N)cc3)n2)ncn1 10.1021/jm301597s
44404948 70554 0 None - 1 Rat 4.6 pKi = 4.6 Binding
Binding affinity for mGluR1 receptor expressed in CHO cellsBinding affinity for mGluR1 receptor expressed in CHO cells
ChEMBL 214 2 3 5 -1.0 NC1(C(=O)O)CC2ON=C(C(=O)O)C2C1 10.1021/jm0504499
CHEMBL194787 70554 0 None - 1 Rat 4.6 pKi = 4.6 Binding
Binding affinity for mGluR1 receptor expressed in CHO cellsBinding affinity for mGluR1 receptor expressed in CHO cells
ChEMBL 214 2 3 5 -1.0 NC1(C(=O)O)CC2ON=C(C(=O)O)C2C1 10.1021/jm0504499
10976811 109713 0 None - 1 Rat 4.6 pKi = 4.6 Binding
Inhibitory constant against cloned rat Metabotropic glutamate receptor 1 expressed in Chinese Hamster Ovary (CHO) cellsInhibitory constant against cloned rat Metabotropic glutamate receptor 1 expressed in Chinese Hamster Ovary (CHO) cells
ChEMBL 214 2 3 5 -1.0 N[C@]1(C(=O)O)C[C@@H]2ON=C(C(=O)O)[C@@H]2C1 10.1021/jm0308085
CHEMBL322887 109713 0 None - 1 Rat 4.6 pKi = 4.6 Binding
Inhibitory constant against cloned rat Metabotropic glutamate receptor 1 expressed in Chinese Hamster Ovary (CHO) cellsInhibitory constant against cloned rat Metabotropic glutamate receptor 1 expressed in Chinese Hamster Ovary (CHO) cells
ChEMBL 214 2 3 5 -1.0 N[C@]1(C(=O)O)C[C@@H]2ON=C(C(=O)O)[C@@H]2C1 10.1021/jm0308085
16659646 89957 0 None - 1 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane
ChEMBL 348 2 1 6 3.5 COc1ccc(-n2cnc3c(sc4ncc5cc[nH]c5c43)c2=O)cc1 10.1021/jm070590c
CHEMBL238079 89957 0 None - 1 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane
ChEMBL 348 2 1 6 3.5 COc1ccc(-n2cnc3c(sc4ncc5cc[nH]c5c43)c2=O)cc1 10.1021/jm070590c
45273580 196603 0 None 17 2 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation countingDisplacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation counting
ChEMBL 311 4 0 3 4.2 COc1ncc(/C=C/C(=O)C23CC4CC(CC(C4)C2)C3)cc1C 10.1016/j.bmc.2009.05.072
CHEMBL564089 196603 0 None 17 2 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation countingDisplacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation counting
ChEMBL 311 4 0 3 4.2 COc1ncc(/C=C/C(=O)C23CC4CC(CC(C4)C2)C3)cc1C 10.1016/j.bmc.2009.05.072
11245287 1697 34 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to mGluR1Binding affinity to mGluR1
ChEMBL 358 3 0 5 2.7 CC(N(C(=O)N1CCC(=CC1)c1nnn(c1C)c1cccnc1F)C)C 10.1016/j.bmc.2010.11.048
6363 1697 34 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to mGluR1Binding affinity to mGluR1
ChEMBL 358 3 0 5 2.7 CC(N(C(=O)N1CCC(=CC1)c1nnn(c1C)c1cccnc1F)C)C 10.1016/j.bmc.2010.11.048
CHEMBL502882 1697 34 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to mGluR1Binding affinity to mGluR1
ChEMBL 358 3 0 5 2.7 CC(N(C(=O)N1CCC(=CC1)c1nnn(c1C)c1cccnc1F)C)C 10.1016/j.bmc.2010.11.048
118718092 120595 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cellsDisplacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cells
ChEMBL 215 3 3 6 -0.4 N[C@]1(C(=O)O)C[C@H]1Cc1nsnc1O 10.1039/C1MD00186H
CHEMBL3347672 120595 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cellsDisplacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cells
ChEMBL 215 3 3 6 -0.4 N[C@]1(C(=O)O)C[C@H]1Cc1nsnc1O 10.1039/C1MD00186H
CHEMBL3545861 120595 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cellsDisplacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cells
ChEMBL 215 3 3 6 -0.4 N[C@]1(C(=O)O)C[C@H]1Cc1nsnc1O 10.1039/C1MD00186H
25066817 195307 0 None 60 2 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation countingDisplacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation counting
ChEMBL 311 4 0 3 4.0 COc1ccc(C2CC2C(=O)C23CC4CC(CC(C4)C2)C3)cn1 10.1016/j.bmc.2009.05.072
CHEMBL551469 195307 0 None 60 2 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation countingDisplacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation counting
ChEMBL 311 4 0 3 4.0 COc1ccc(C2CC2C(=O)C23CC4CC(CC(C4)C2)C3)cn1 10.1016/j.bmc.2009.05.072
12991435 72292 0 None - 1 Rat 4.5 pKi = 4.5 Binding
Binding affinity for mGluR1 receptor expressed in CHO cellsBinding affinity for mGluR1 receptor expressed in CHO cells
ChEMBL 214 2 3 5 -1.0 N[C@@]1(C(=O)O)C[C@H]2ON=C(C(=O)O)[C@H]2C1 10.1021/jm0504499
CHEMBL198310 72292 0 None - 1 Rat 4.5 pKi = 4.5 Binding
Binding affinity for mGluR1 receptor expressed in CHO cellsBinding affinity for mGluR1 receptor expressed in CHO cells
ChEMBL 214 2 3 5 -1.0 N[C@@]1(C(=O)O)C[C@H]2ON=C(C(=O)O)[C@H]2C1 10.1021/jm0504499
1310 2315 110 None -4 18 Rat 6.5 pKi = 6.5 Binding
Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cellsInhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm010323l
1369 2315 110 None -4 18 Rat 6.5 pKi = 6.5 Binding
Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cellsInhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm010323l
33032 2315 110 None -4 18 Rat 6.5 pKi = 6.5 Binding
Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cellsInhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm010323l
44272391 2315 110 None -4 18 Rat 6.5 pKi = 6.5 Binding
Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cellsInhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm010323l
88747398 2315 110 None -4 18 Rat 6.5 pKi = 6.5 Binding
Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cellsInhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm010323l
CHEMBL575060 2315 110 None -4 18 Rat 6.5 pKi = 6.5 Binding
Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cellsInhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm010323l
DB00142 2315 110 None -4 18 Rat 6.5 pKi = 6.5 Binding
Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cellsInhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1021/jm010323l
17758443 86140 2 None 1 2 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cellsDisplacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cells
ChEMBL 195 3 3 4 -1.3 N[C@H](C(=O)O)[C@H]1C[C@@H]1S(=O)(=O)O 10.1021/jm070322e
CHEMBL231157 86140 2 None 1 2 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cellsDisplacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cells
ChEMBL 195 3 3 4 -1.3 N[C@H](C(=O)O)[C@H]1C[C@@H]1S(=O)(=O)O 10.1021/jm070322e
3115037 195185 7 None - 1 Rat 4.4 pKi = 4.4 Binding
Displacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation countingDisplacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation counting
ChEMBL 282 4 0 3 3.8 CC(CC(=O)c1ccc2c(c1)OCCO2)c1ccccc1 10.1016/j.bmc.2009.05.072
CHEMBL550523 195185 7 None - 1 Rat 4.4 pKi = 4.4 Binding
Displacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation countingDisplacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation counting
ChEMBL 282 4 0 3 3.8 CC(CC(=O)c1ccc2c(c1)OCCO2)c1ccccc1 10.1016/j.bmc.2009.05.072
1418 3449 53 None 21 2 Rat 5.4 pKi = 5.4 Binding
Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cellsInhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells
ChEMBL 195 3 3 3 0.5 N[C@@H](c1ccc(cc1)C(=O)O)C(=O)O 10.1021/jm010323l
5311459 3449 53 None 21 2 Rat 5.4 pKi = 5.4 Binding
Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cellsInhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells
ChEMBL 195 3 3 3 0.5 N[C@@H](c1ccc(cc1)C(=O)O)C(=O)O 10.1021/jm010323l
CHEMBL94990 3449 53 None 21 2 Rat 5.4 pKi = 5.4 Binding
Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cellsInhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells
ChEMBL 195 3 3 3 0.5 N[C@@H](c1ccc(cc1)C(=O)O)C(=O)O 10.1021/jm010323l
86627336 122201 2 None -389 3 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometry
ChEMBL 320 2 0 5 3.0 O=[N+]([O-])c1cccnc1N1CCC(=CC#Cc2ccccn2)CC1 10.1016/j.bmc.2015.05.008
CHEMBL3597593 122201 2 None -389 3 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometry
ChEMBL 320 2 0 5 3.0 O=[N+]([O-])c1cccnc1N1CCC(=CC#Cc2ccccn2)CC1 10.1016/j.bmc.2015.05.008
11688880 85065 0 None 616 2 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes
ChEMBL 350 2 0 6 3.7 Cc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)c(C)c1 10.1021/jm0504407
CHEMBL224356 85065 0 None 616 2 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes
ChEMBL 350 2 0 6 3.7 Cc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)c(C)c1 10.1021/jm0504407
1069776 85222 11 None 257 2 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes
ChEMBL 356 2 0 6 3.7 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12 10.1021/jm0504407
CHEMBL225589 85222 11 None 257 2 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes
ChEMBL 356 2 0 6 3.7 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12 10.1021/jm0504407
18003010 76791 14 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to mGluR1Binding affinity to mGluR1
ChEMBL 414 7 0 6 4.0 COCCN(C)Cc1ccc2nc3sc(C(=O)N(C)C4CCCCC4)cn3c2c1 10.1016/j.bmc.2010.11.048
CHEMBL1645351 76791 14 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to mGluR1Binding affinity to mGluR1
ChEMBL 414 7 0 6 4.0 COCCN(C)Cc1ccc2nc3sc(C(=O)N(C)C4CCCCC4)cn3c2c1 10.1016/j.bmc.2010.11.048
CHEMBL1771388 76791 14 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to mGluR1Binding affinity to mGluR1
ChEMBL 414 7 0 6 4.0 COCCN(C)Cc1ccc2nc3sc(C(=O)N(C)C4CCCCC4)cn3c2c1 10.1016/j.bmc.2010.11.048
CHEMBL2068815 76791 14 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to mGluR1Binding affinity to mGluR1
ChEMBL 414 7 0 6 4.0 COCCN(C)Cc1ccc2nc3sc(C(=O)N(C)C4CCCCC4)cn3c2c1 10.1016/j.bmc.2010.11.048
18003010 76791 14 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to mGluR1 by PET analysisBinding affinity to mGluR1 by PET analysis
ChEMBL 414 7 0 6 4.0 COCCN(C)Cc1ccc2nc3sc(C(=O)N(C)C4CCCCC4)cn3c2c1 10.1016/j.bmcl.2011.03.046
CHEMBL1645351 76791 14 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to mGluR1 by PET analysisBinding affinity to mGluR1 by PET analysis
ChEMBL 414 7 0 6 4.0 COCCN(C)Cc1ccc2nc3sc(C(=O)N(C)C4CCCCC4)cn3c2c1 10.1016/j.bmcl.2011.03.046
CHEMBL1771388 76791 14 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to mGluR1 by PET analysisBinding affinity to mGluR1 by PET analysis
ChEMBL 414 7 0 6 4.0 COCCN(C)Cc1ccc2nc3sc(C(=O)N(C)C4CCCCC4)cn3c2c1 10.1016/j.bmcl.2011.03.046
CHEMBL2068815 76791 14 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to mGluR1 by PET analysisBinding affinity to mGluR1 by PET analysis
ChEMBL 414 7 0 6 4.0 COCCN(C)Cc1ccc2nc3sc(C(=O)N(C)C4CCCCC4)cn3c2c1 10.1016/j.bmcl.2011.03.046
25183673 122200 0 None -12 3 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometry
ChEMBL 319 2 0 4 3.6 O=[N+]([O-])c1cccnc1N1CCC(=CC#Cc2ccccc2)CC1 10.1016/j.bmc.2015.05.008
CHEMBL3597592 122200 0 None -12 3 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometry
ChEMBL 319 2 0 4 3.6 O=[N+]([O-])c1cccnc1N1CCC(=CC#Cc2ccccc2)CC1 10.1016/j.bmc.2015.05.008
155549638 173848 0 None -165 2 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]MPEP from rat mGlu1 receptor expressed in CHO-TREx cell membranes after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]MPEP from rat mGlu1 receptor expressed in CHO-TREx cell membranes after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 360 3 0 3 4.1 Cc1cccc(C#CC=C2CCN(C(=O)OCCc3ccccc3)CC2)n1 10.1021/acs.jmedchem.8b01226
CHEMBL4539036 173848 0 None -165 2 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]MPEP from rat mGlu1 receptor expressed in CHO-TREx cell membranes after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]MPEP from rat mGlu1 receptor expressed in CHO-TREx cell membranes after 30 mins by liquid scintillation spectrometric analysis
ChEMBL 360 3 0 3 4.1 Cc1cccc(C#CC=C2CCN(C(=O)OCCc3ccccc3)CC2)n1 10.1021/acs.jmedchem.8b01226
10513894 79660 0 None - 1 Human 4.4 pKi = 4.4 Binding
Binding affinity towards metabotropic glutamate receptor mGluR1Binding affinity towards metabotropic glutamate receptor mGluR1
ChEMBL 235 4 3 3 0.5 N[C@@H](C(=O)O)[C@@H]1[C@H](C(=O)O)[C@@H]1c1ccccc1 10.1021/jm960059+
CHEMBL2115152 79660 0 None - 1 Human 4.4 pKi = 4.4 Binding
Binding affinity towards metabotropic glutamate receptor mGluR1Binding affinity towards metabotropic glutamate receptor mGluR1
ChEMBL 235 4 3 3 0.5 N[C@@H](C(=O)O)[C@@H]1[C@H](C(=O)O)[C@@H]1c1ccccc1 10.1021/jm960059+
87550659 122209 0 None -891 3 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometry
ChEMBL 390 2 0 4 4.9 Cc1cccc(C#CC=C2CCN(c3ncc(-c4ccccc4)cc3C#N)CC2)n1 10.1016/j.bmc.2015.05.008
CHEMBL3597602 122209 0 None -891 3 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometry
ChEMBL 390 2 0 4 4.9 Cc1cccc(C#CC=C2CCN(c3ncc(-c4ccccc4)cc3C#N)CC2)n1 10.1016/j.bmc.2015.05.008
11530404 210 14 None 38 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes
ChEMBL 350 3 0 6 3.6 CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C 10.1021/jm0504407
6211 210 14 None 38 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes
ChEMBL 350 3 0 6 3.6 CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C 10.1021/jm0504407
CHEMBL385336 210 14 None 38 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes
ChEMBL 350 3 0 6 3.6 CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C 10.1021/jm0504407
16660135 1642 36 None - 1 Rat 8.3 pKi = 8.3 Binding
Displacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hrDisplacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hr
ChEMBL 371 5 1 6 3.8 CC(Nc1ncnc(c1)c1csc(n1)N(C(=O)c1ccc(cc1)F)C)C 10.1021/jm201590g
8767 1642 36 None - 1 Rat 8.3 pKi = 8.3 Binding
Displacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hrDisplacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hr
ChEMBL 371 5 1 6 3.8 CC(Nc1ncnc(c1)c1csc(n1)N(C(=O)c1ccc(cc1)F)C)C 10.1021/jm201590g
CHEMBL566581 1642 36 None - 1 Rat 8.3 pKi = 8.3 Binding
Displacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hrDisplacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hr
ChEMBL 371 5 1 6 3.8 CC(Nc1ncnc(c1)c1csc(n1)N(C(=O)c1ccc(cc1)F)C)C 10.1021/jm201590g
1222 101737 63 None -5 3 Human 4.3 pKi = 4.3 Binding
Binding affinity towards mGluR1a was determinedBinding affinity towards mGluR1a was determined
ChEMBL 209 3 3 3 0.6 CC(N)(C(=O)O)c1ccc(C(=O)O)cc1 10.1021/jm960059+
CHEMBL299683 101737 63 None -5 3 Human 4.3 pKi = 4.3 Binding
Binding affinity towards mGluR1a was determinedBinding affinity towards mGluR1a was determined
ChEMBL 209 3 3 3 0.6 CC(N)(C(=O)O)c1ccc(C(=O)O)cc1 10.1021/jm960059+
11644388 197809 0 None 5 2 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation countingDisplacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation counting
ChEMBL 239 2 0 2 3.9 CC(C)(C)C(=O)/C=C/c1cnc2ccccc2c1 10.1016/j.bmc.2009.05.072
CHEMBL572128 197809 0 None 5 2 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation countingDisplacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation counting
ChEMBL 239 2 0 2 3.9 CC(C)(C)C(=O)/C=C/c1cnc2ccccc2c1 10.1016/j.bmc.2009.05.072
122183732 122198 0 None -41 2 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometry
ChEMBL 362 3 0 5 2.3 C=Cc1ccc([N+](=O)[O-])c(N2CCN(C(=O)C#Cc3ccccc3)CC2)n1 10.1016/j.bmc.2015.05.008
CHEMBL3597586 122198 0 None -41 2 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometry
ChEMBL 362 3 0 5 2.3 C=Cc1ccc([N+](=O)[O-])c(N2CCN(C(=O)C#Cc3ccccc3)CC2)n1 10.1016/j.bmc.2015.05.008
1310 2315 110 None -1 18 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]Quisqualate from human mGluR1A receptor expressed in BHK cellsDisplacement of [3H]Quisqualate from human mGluR1A receptor expressed in BHK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2008.11.015
1369 2315 110 None -1 18 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]Quisqualate from human mGluR1A receptor expressed in BHK cellsDisplacement of [3H]Quisqualate from human mGluR1A receptor expressed in BHK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2008.11.015
33032 2315 110 None -1 18 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]Quisqualate from human mGluR1A receptor expressed in BHK cellsDisplacement of [3H]Quisqualate from human mGluR1A receptor expressed in BHK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2008.11.015
44272391 2315 110 None -1 18 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]Quisqualate from human mGluR1A receptor expressed in BHK cellsDisplacement of [3H]Quisqualate from human mGluR1A receptor expressed in BHK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2008.11.015
88747398 2315 110 None -1 18 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]Quisqualate from human mGluR1A receptor expressed in BHK cellsDisplacement of [3H]Quisqualate from human mGluR1A receptor expressed in BHK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2008.11.015
CHEMBL575060 2315 110 None -1 18 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]Quisqualate from human mGluR1A receptor expressed in BHK cellsDisplacement of [3H]Quisqualate from human mGluR1A receptor expressed in BHK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2008.11.015
DB00142 2315 110 None -1 18 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]Quisqualate from human mGluR1A receptor expressed in BHK cellsDisplacement of [3H]Quisqualate from human mGluR1A receptor expressed in BHK cells
ChEMBL 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 10.1016/j.bmc.2008.11.015
44569859 178584 0 None - 1 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]Quisqualate from human mGluR1A receptor expressed in BHK cellsDisplacement of [3H]Quisqualate from human mGluR1A receptor expressed in BHK cells
ChEMBL 213 5 3 3 0.4 N[C@@H](CC12CC(CC(=O)O)(C1)C2)C(=O)O 10.1016/j.bmc.2008.11.015
CHEMBL467234 178584 0 None - 1 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]Quisqualate from human mGluR1A receptor expressed in BHK cellsDisplacement of [3H]Quisqualate from human mGluR1A receptor expressed in BHK cells
ChEMBL 213 5 3 3 0.4 N[C@@H](CC12CC(CC(=O)O)(C1)C2)C(=O)O 10.1016/j.bmc.2008.11.015
11717278 85038 0 None 102 2 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes
ChEMBL 350 3 0 6 3.6 CCc1cccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)c1 10.1021/jm0504407
CHEMBL224084 85038 0 None 102 2 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes
ChEMBL 350 3 0 6 3.6 CCc1cccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)c1 10.1021/jm0504407
10489913 79550 0 None - 1 Human 4.2 pKi = 4.2 Binding
Binding affinity towards metabotropic glutamate receptor mGluR1Binding affinity towards metabotropic glutamate receptor mGluR1
ChEMBL 235 4 3 3 0.5 N[C@H](C(=O)O)[C@@H]1[C@H](c2ccccc2)[C@H]1C(=O)O 10.1021/jm960059+
CHEMBL2114116 79550 0 None - 1 Human 4.2 pKi = 4.2 Binding
Binding affinity towards metabotropic glutamate receptor mGluR1Binding affinity towards metabotropic glutamate receptor mGluR1
ChEMBL 235 4 3 3 0.5 N[C@H](C(=O)O)[C@@H]1[C@H](c2ccccc2)[C@H]1C(=O)O 10.1021/jm960059+
45082292 115251 2 None 3 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cellsDisplacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cells
ChEMBL 159 3 3 3 -0.7 N[C@@]1(C(=O)O)C[C@@H]1CC(=O)O 10.1039/C1MD00186H
CHEMBL3347670 115251 2 None 3 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cellsDisplacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cells
ChEMBL 159 3 3 3 -0.7 N[C@@]1(C(=O)O)C[C@@H]1CC(=O)O 10.1039/C1MD00186H
11537814 85194 0 None 19 2 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes
ChEMBL 362 2 1 7 2.9 CN(C)c1ccnc2sc3c(=O)n(-c4ccc5cn[nH]c5c4)cnc3c12 10.1021/jm0504407
CHEMBL225438 85194 0 None 19 2 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes
ChEMBL 362 2 1 7 2.9 CN(C)c1ccnc2sc3c(=O)n(-c4ccc5cn[nH]c5c4)cnc3c12 10.1021/jm0504407
45273579 195687 0 None 9 2 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation countingDisplacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation counting
ChEMBL 325 3 0 4 3.7 O=C(/C=C/c1cnc2c(c1)OCCO2)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmc.2009.05.072
CHEMBL556707 195687 0 None 9 2 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation countingDisplacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation counting
ChEMBL 325 3 0 4 3.7 O=C(/C=C/c1cnc2c(c1)OCCO2)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmc.2009.05.072
122183731 122197 0 None -173 3 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometry
ChEMBL 335 2 0 4 2.3 O=C(C#Cc1ccccc1)N1CCN(c2ccccc2[N+](=O)[O-])CC1 10.1016/j.bmc.2015.05.008
CHEMBL3597585 122197 0 None -173 3 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometry
ChEMBL 335 2 0 4 2.3 O=C(C#Cc1ccccc1)N1CCN(c2ccccc2[N+](=O)[O-])CC1 10.1016/j.bmc.2015.05.008
1208332 167055 13 None - 1 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane
ChEMBL 352 3 0 7 3.1 COc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1 10.1021/jm070590c
CHEMBL428909 167055 13 None - 1 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane
ChEMBL 352 3 0 7 3.1 COc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1 10.1021/jm070590c
25183670 122204 0 None -354 3 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometry
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 122204 0 None -354 3 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometry
ChEMBL 333 2 0 4 3.9 Cc1cccc(C#CC=C2CCN(c3ccccc3[N+](=O)[O-])CC2)n1 10.1016/j.bmc.2015.05.008
25066816 194776 0 None 3 2 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation countingDisplacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation counting
ChEMBL 281 3 0 2 4.0 O=C(C1CC1c1cccnc1)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmc.2009.05.072
CHEMBL538307 194776 0 None 3 2 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation countingDisplacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation counting
ChEMBL 281 3 0 2 4.0 O=C(C1CC1c1cccnc1)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmc.2009.05.072
44385546 129025 0 None -1 2 Rat 4.2 pKi = 4.2 Binding
The compound was tested for the receptor binding affinity at Metabotropic glutamate receptor 1 using established second messenger assay systems.The compound was tested for the receptor binding affinity at Metabotropic glutamate receptor 1 using established second messenger assay systems.
ChEMBL 264 4 4 6 0.7 N[C@@H](Cc1onc(O)c1-c1ccc(O)cc1)C(=O)O 10.1021/jm010443t
CHEMBL367027 129025 0 None -1 2 Rat 4.2 pKi = 4.2 Binding
The compound was tested for the receptor binding affinity at Metabotropic glutamate receptor 1 using established second messenger assay systems.The compound was tested for the receptor binding affinity at Metabotropic glutamate receptor 1 using established second messenger assay systems.
ChEMBL 264 4 4 6 0.7 N[C@@H](Cc1onc(O)c1-c1ccc(O)cc1)C(=O)O 10.1021/jm010443t
17758554 143114 2 None 1 2 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cellsDisplacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cells
ChEMBL 195 3 3 4 -1.3 N[C@H](C(=O)O)[C@@H]1C[C@H]1S(=O)(=O)O 10.1021/jm070322e
CHEMBL389555 143114 2 None 1 2 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cellsDisplacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cells
ChEMBL 195 3 3 4 -1.3 N[C@H](C(=O)O)[C@@H]1C[C@H]1S(=O)(=O)O 10.1021/jm070322e
1377 1340 26 None -1230 6 Rat 4.1 pKi = 4.1 Binding
Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cellsInhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells
ChEMBL 203 4 4 4 -1.6 N[C@@H](C1[C@H]([C@@H]1C(=O)O)C(=O)O)C(=O)O 10.1021/jm010323l
5310979 1340 26 None -1230 6 Rat 4.1 pKi = 4.1 Binding
Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cellsInhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells
ChEMBL 203 4 4 4 -1.6 N[C@@H](C1[C@H]([C@@H]1C(=O)O)C(=O)O)C(=O)O 10.1021/jm010323l
CHEMBL284193 1340 26 None -1230 6 Rat 4.1 pKi = 4.1 Binding
Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cellsInhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells
ChEMBL 203 4 4 4 -1.6 N[C@@H](C1[C@H]([C@@H]1C(=O)O)C(=O)O)C(=O)O 10.1021/jm010323l
16659798 88645 0 None - 1 Rat 6.1 pKi = 6.1 Binding
Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane
ChEMBL 396 2 0 8 4.6 CSc1nc2c(cnc3sc4c(=O)n(-c5ccc(C)cc5)cnc4c32)s1 10.1021/jm070590c
CHEMBL235767 88645 0 None - 1 Rat 6.1 pKi = 6.1 Binding
Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane
ChEMBL 396 2 0 8 4.6 CSc1nc2c(cnc3sc4c(=O)n(-c5ccc(C)cc5)cnc4c32)s1 10.1021/jm070590c
11560185 85067 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes
ChEMBL 390 2 0 6 4.1 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(C(F)(F)F)cc4)cnc3c12 10.1021/jm0504407
CHEMBL224375 85067 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes
ChEMBL 390 2 0 6 4.1 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(C(F)(F)F)cc4)cnc3c12 10.1021/jm0504407
11667270 85152 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes
ChEMBL 340 2 0 6 3.2 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(F)cc4)cnc3c12 10.1021/jm0504407
CHEMBL225124 85152 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes
ChEMBL 340 2 0 6 3.2 CN(C)c1ccnc2sc3c(=O)n(-c4ccc(F)cc4)cnc3c12 10.1021/jm0504407
657896 142082 10 None - 1 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes
ChEMBL 336 3 0 6 3.1 CN(C)c1ccnc2sc3c(=O)n(Cc4ccccc4)cnc3c12 10.1021/jm0504407
CHEMBL388087 142082 10 None - 1 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes
ChEMBL 336 3 0 6 3.1 CN(C)c1ccnc2sc3c(=O)n(Cc4ccccc4)cnc3c12 10.1021/jm0504407
177491 86089 42 None -1 3 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cellsDisplacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cells
ChEMBL 183 4 3 4 -1.3 N[C@@H](CCS(=O)(=O)O)C(=O)O 10.1021/jm070322e
CHEMBL230951 86089 42 None -1 3 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cellsDisplacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cells
ChEMBL 183 4 3 4 -1.3 N[C@@H](CCS(=O)(=O)O)C(=O)O 10.1021/jm070322e
16659804 88744 0 None - 1 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane
ChEMBL 384 1 1 7 3.8 C[C@@H]1COc2cnc3sc4c(=O)n(-c5ccc(Cl)cc5)cnc4c3c2N1 10.1021/jm070590c
CHEMBL236178 88744 0 None - 1 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane
ChEMBL 384 1 1 7 3.8 C[C@@H]1COc2cnc3sc4c(=O)n(-c5ccc(Cl)cc5)cnc4c3c2N1 10.1021/jm070590c
443586 146452 53 None 2 3 Rat 6.1 pKi = 6.1 Binding
Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cellsInhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells
ChEMBL 183 2 4 4 0.2 N[C@H](C(=O)O)c1cc(O)cc(O)c1 10.1021/jm010323l
71668376 146452 53 None 2 3 Rat 6.1 pKi = 6.1 Binding
Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cellsInhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells
ChEMBL 183 2 4 4 0.2 N[C@H](C(=O)O)c1cc(O)cc(O)c1 10.1021/jm010323l
CHEMBL39221 146452 53 None 2 3 Rat 6.1 pKi = 6.1 Binding
Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cellsInhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells
ChEMBL 183 2 4 4 0.2 N[C@H](C(=O)O)c1cc(O)cc(O)c1 10.1021/jm010323l
5766222 195912 17 None - 1 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation countingDisplacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by 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 195912 17 None - 1 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation countingDisplacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by 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
44386146 129472 0 None -1 2 Rat 4.0 pKi = 4.0 Binding
The compound was tested for the receptor binding affinity at Metabotropic glutamate receptor 1 using established second messenger assay systems.The compound was tested for the receptor binding affinity at Metabotropic glutamate receptor 1 using established second messenger assay systems.
ChEMBL 276 6 3 5 1.1 N[C@@H](Cc1onc(O)c1CCc1ccccc1)C(=O)O 10.1021/jm010443t
CHEMBL367189 129472 0 None -1 2 Rat 4.0 pKi = 4.0 Binding
The compound was tested for the receptor binding affinity at Metabotropic glutamate receptor 1 using established second messenger assay systems.The compound was tested for the receptor binding affinity at Metabotropic glutamate receptor 1 using established second messenger assay systems.
ChEMBL 276 6 3 5 1.1 N[C@@H](Cc1onc(O)c1CCc1ccccc1)C(=O)O 10.1021/jm010443t
44404948 70554 0 None - 1 Rat 4.0 pKi = 4.0 Binding
Binding affinity for mGluR1 receptor expressed in CHO cellsBinding affinity for mGluR1 receptor expressed in CHO cells
ChEMBL 214 2 3 5 -1.0 NC1(C(=O)O)CC2ON=C(C(=O)O)C2C1 10.1021/jm0504499
CHEMBL194787 70554 0 None - 1 Rat 4.0 pKi = 4.0 Binding
Binding affinity for mGluR1 receptor expressed in CHO cellsBinding affinity for mGluR1 receptor expressed in CHO cells
ChEMBL 214 2 3 5 -1.0 NC1(C(=O)O)CC2ON=C(C(=O)O)C2C1 10.1021/jm0504499
10353177 164459 0 None - 1 Rat 4.0 pKi = 4.0 Binding
Inhibitory constant against cloned rat Metabotropic glutamate receptor 1 expressed in Chinese Hamster Ovary (CHO) cellsInhibitory constant against cloned rat Metabotropic glutamate receptor 1 expressed in Chinese Hamster Ovary (CHO) cells
ChEMBL 214 2 3 5 -1.0 N[C@@]1(C(=O)O)C[C@@H]2ON=C(C(=O)O)[C@@H]2C1 10.1021/jm0308085
CHEMBL421402 164459 0 None - 1 Rat 4.0 pKi = 4.0 Binding
Inhibitory constant against cloned rat Metabotropic glutamate receptor 1 expressed in Chinese Hamster Ovary (CHO) cellsInhibitory constant against cloned rat Metabotropic glutamate receptor 1 expressed in Chinese Hamster Ovary (CHO) cells
ChEMBL 214 2 3 5 -1.0 N[C@@]1(C(=O)O)C[C@@H]2ON=C(C(=O)O)[C@@H]2C1 10.1021/jm0308085
10353177 164459 0 None - 1 Rat 4.0 pKi = 4.0 Binding
Binding affinity for mGluR1 receptor expressed in CHO cellsBinding affinity for mGluR1 receptor expressed in CHO cells
ChEMBL 214 2 3 5 -1.0 N[C@@]1(C(=O)O)C[C@@H]2ON=C(C(=O)O)[C@@H]2C1 10.1021/jm0504499
CHEMBL421402 164459 0 None - 1 Rat 4.0 pKi = 4.0 Binding
Binding affinity for mGluR1 receptor expressed in CHO cellsBinding affinity for mGluR1 receptor expressed in CHO cells
ChEMBL 214 2 3 5 -1.0 N[C@@]1(C(=O)O)C[C@@H]2ON=C(C(=O)O)[C@@H]2C1 10.1021/jm0504499
10382361 122196 0 None -194 3 Rat 7.0 pKi = 7.0 Binding
Displacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometry
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 122196 0 None -194 3 Rat 7.0 pKi = 7.0 Binding
Displacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometry
ChEMBL 336 2 0 5 1.7 O=C(C#Cc1ccccc1)N1CCN(c2ncccc2[N+](=O)[O-])CC1 10.1016/j.bmc.2015.05.008
11695769 143538 0 None - 1 Rat 7.0 pKi = 7 Binding
Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes
ChEMBL 338 2 1 7 2.8 CN(C)c1ccnc2sc3c(=O)n(-c4ccccc4O)cnc3c12 10.1021/jm0504407
CHEMBL389897 143538 0 None - 1 Rat 7.0 pKi = 7 Binding
Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes
ChEMBL 338 2 1 7 2.8 CN(C)c1ccnc2sc3c(=O)n(-c4ccccc4O)cnc3c12 10.1021/jm0504407
5766229 195917 6 None - 1 Rat 5.0 pKi = 5 Binding
Displacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation countingDisplacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by 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 195917 6 None - 1 Rat 5.0 pKi = 5 Binding
Displacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation countingDisplacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by 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
1389 4118 0 None - 1 Rat 7.5 pKd = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 342 2 1 5 3.8 CN(C(=O)c1sc2n(c1C)c1c(n2)ccc(c1)N)C1CCCCC1 15976016
5392 4118 0 None - 1 Rat 7.5 pKd = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 342 2 1 5 3.8 CN(C(=O)c1sc2n(c1C)c1c(n2)ccc(c1)N)C1CCCCC1 15976016
9819432 4118 0 None - 1 Rat 7.5 pKd = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 342 2 1 5 3.8 CN(C(=O)c1sc2n(c1C)c1c(n2)ccc(c1)N)C1CCCCC1 15976016
CHEMBL1517556 4118 0 None - 1 Rat 7.5 pKd = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 342 2 1 5 3.8 CN(C(=O)c1sc2n(c1C)c1c(n2)ccc(c1)N)C1CCCCC1 15976016
1370 3263 67 None 17 8 Rat 7.6 pKd None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 12509432
1370 3263 67 None 17 8 Rat 7.6 pKd None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 12695537
1372 3263 67 None 17 8 Rat 7.6 pKd None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 12509432
1372 3263 67 None 17 8 Rat 7.6 pKd None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 12695537
40539 3263 67 None 17 8 Rat 7.6 pKd None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 12509432
40539 3263 67 None 17 8 Rat 7.6 pKd None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 12695537
6971145 3263 67 None 17 8 Rat 7.6 pKd None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 12509432
6971145 3263 67 None 17 8 Rat 7.6 pKd None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 12695537
CHEMBL279956 3263 67 None 17 8 Rat 7.6 pKd None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 12509432
CHEMBL279956 3263 67 None 17 8 Rat 7.6 pKd None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 12695537
DB02999 3263 67 None 17 8 Rat 7.6 pKd None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 12509432
DB02999 3263 67 None 17 8 Rat 7.6 pKd None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 12695537
1390 1556 0 None - 1 Rat 8.2 pKd None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 2 0 5 2.0 CCn1c(C)nc(c(c1=O)C#N)N1CCc2c(CC1)cccc2 12509432
3363 1556 0 None - 1 Rat 8.2 pKd None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 2 0 5 2.0 CCn1c(C)nc(c(c1=O)C#N)N1CCc2c(CC1)cccc2 12509432
9904703 1556 0 None - 1 Rat 8.2 pKd None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 2 0 5 2.0 CCn1c(C)nc(c(c1=O)C#N)N1CCc2c(CC1)cccc2 12509432
10470232 3269 23 None 1 2 Human 9.0 pKd None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 3 0 3 4.0 O=C(c1ccc2c(c1)cc1c(n2)OCCC1)Cc1ccccc1 12695537
1391 3269 23 None 1 2 Human 9.0 pKd None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 3 0 3 4.0 O=C(c1ccc2c(c1)cc1c(n2)OCCC1)Cc1ccccc1 12695537
6336 3269 23 None 1 2 Human 9.0 pKd None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 3 0 3 4.0 O=C(c1ccc2c(c1)cc1c(n2)OCCC1)Cc1ccccc1 12695537
CHEMBL369459 3269 23 None 1 2 Human 9.0 pKd None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 3 0 3 4.0 O=C(c1ccc2c(c1)cc1c(n2)OCCC1)Cc1ccccc1 12695537
1310 2315 110 Functional -4 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
1369 2315 110 Functional -4 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
33032 2315 110 Functional -4 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
44272391 2315 110 Functional -4 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
88747398 2315 110 Functional -4 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
CHEMBL575060 2315 110 Functional -4 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
DB00142 2315 110 Functional -4 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
134 2514 24 Functional -8511 67 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2514 24 Functional -8511 67 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2514 24 Functional -8511 67 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2514 24 Functional -8511 67 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2514 24 Functional -8511 67 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
15897 2862 0 Functional -354 36 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 2862 0 Functional -354 36 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 2862 0 Functional -354 36 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
128563 3464 33 Functional -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
1666 3464 33 Functional -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
CHEMBL445332 3464 33 Functional -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
DB12327 3464 33 Functional -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
10297 27112 30 Functional -38 42 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
CHEMBL136560 27112 30 Functional -38 42 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
446220 133521 14 Functional -1778 45 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
CHEMBL370805 133521 14 Functional -1778 45 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
1615 167791 24 Functional -26 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
CHEMBL43048 167791 24 Functional -26 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
162265 202274 22 Functional -239 43 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
4786 202274 22 Functional -239 43 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
CHEMBL61006 202274 22 Functional -239 43 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
3337 206367 27 Functional -1513 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 206367 27 Functional -1513 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 206367 27 Functional -1513 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 206367 27 Functional -1513 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 206367 27 Functional -1513 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
11954224 215953 0 Functional -141253 58 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
6971132 216009 0 3H-YM-298198 -2570 14 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 268 1 2 2 2.1 CN1CC(C=C2C1CC3=CNC4=CC=CC2=C34)C(=O)O None
None 216172 0 Functional -2 7 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 173 2 3 3 -0.3 C1CC(CC1C(=O)O)(C(=O)O)N None
25137849 216179 0 Functional -4 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
71290 216179 0 Functional -4 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
None 216316 0 Functional -1 39 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 3 3 3 -1.4 C(C(C(=O)O)N)S(=O)O None
None 216317 0 Functional -1 38 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 3 3 4 -1.7 C(C(C(=O)O)N)S(=O)(=O)O None
None 216325 0 Functional -13 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 2 1 2 1.2 CC(C(=O)C1=CC=CC=C1)N None
1576 216326 0 Functional -16 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 163 3 1 2 1.5 CC(C(=O)C1=CC=CC=C1)NC None
135398740 217712 0 None -1 2 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 255 5 4 8 -2.0 NC1=NC2=C(N=CN2COC(CO)CO)C(=O)N1 None
1310 2315 110 None -1 18 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cellsDisplacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cells
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
1369 2315 110 None -1 18 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cellsDisplacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cells
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
33032 2315 110 None -1 18 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cellsDisplacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cells
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
44272391 2315 110 None -1 18 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cellsDisplacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cells
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
88747398 2315 110 None -1 18 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cellsDisplacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cells
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
CHEMBL575060 2315 110 None -1 18 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cellsDisplacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cells
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
DB00142 2315 110 None -1 18 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cellsDisplacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cells
Drug Central 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
16660135 1642 36 None - 1 Rat 8.3 pKi = 8.3 Binding
Measured using rat brain homogenate in a competition binding assay displacing [<sup>18</sup>F}-FITM.Measured using rat brain homogenate in a competition binding assay displacing [<sup>18</sup>F}-FITM.
Guide to Pharmacology 371 5 1 6 3.8 CC(Nc1ncnc(c1)c1csc(n1)N(C(=O)c1ccc(cc1)F)C)C 22316010
8767 1642 36 None - 1 Rat 8.3 pKi = 8.3 Binding
Measured using rat brain homogenate in a competition binding assay displacing [<sup>18</sup>F}-FITM.Measured using rat brain homogenate in a competition binding assay displacing [<sup>18</sup>F}-FITM.
Guide to Pharmacology 371 5 1 6 3.8 CC(Nc1ncnc(c1)c1csc(n1)N(C(=O)c1ccc(cc1)F)C)C 22316010
CHEMBL566581 1642 36 None - 1 Rat 8.3 pKi = 8.3 Binding
Measured using rat brain homogenate in a competition binding assay displacing [<sup>18</sup>F}-FITM.Measured using rat brain homogenate in a competition binding assay displacing [<sup>18</sup>F}-FITM.
Guide to Pharmacology 371 5 1 6 3.8 CC(Nc1ncnc(c1)c1csc(n1)N(C(=O)c1ccc(cc1)F)C)C 22316010
1387 3363 0 None - 1 Rat 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 4 1 4 4.0 CCCCOC(=O)NC(=O)C1c2ccccc2Oc2c1cccc2 11606768
9949202 3363 0 None - 1 Rat 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 4 1 4 4.0 CCCCOC(=O)NC(=O)C1c2ccccc2Oc2c1cccc2 11606768
1379 2420 44 None - 1 Rat 5.9 pKi = 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 209 3 3 3 0.8 OC(=O)c1ccc(c(c1)C)[C@@H](C(=O)O)N 12695537
5311261 2420 44 None - 1 Rat 5.9 pKi = 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 209 3 3 3 0.8 OC(=O)c1ccc(c(c1)C)[C@@H](C(=O)O)N 12695537
CHEMBL94631 2420 44 None - 1 Rat 5.9 pKi = 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 209 3 3 3 0.8 OC(=O)c1ccc(c(c1)C)[C@@H](C(=O)O)N 12695537
3347 2423 9 None - 1 Rat 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 5 2 5 3.0 OCCSc1nc(NC2Cc3c(C2)cccc3)c2c(n1)CCCC2 19559036
9840951 2423 9 None - 1 Rat 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 5 2 5 3.0 OCCSc1nc(NC2Cc3c(C2)cccc3)c2c(n1)CCCC2 19559036
CHEMBL3786530 2423 9 None - 1 Rat 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 5 2 5 3.0 OCCSc1nc(NC2Cc3c(C2)cccc3)c2c(n1)CCCC2 19559036
44442431 1057 0 None - 1 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 415 3 1 7 2.2 Clc1ccc(cc1)n1c(C)nc2c(c1=O)cnn2c1ccc(cc1)S(=O)(=O)N 17532216
6342 1057 0 None - 1 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 415 3 1 7 2.2 Clc1ccc(cc1)n1c(C)nc2c(c1=O)cnn2c1ccc(cc1)S(=O)(=O)N 17532216
CHEMBL245990 1057 0 None - 1 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 415 3 1 7 2.2 Clc1ccc(cc1)n1c(C)nc2c(c1=O)cnn2c1ccc(cc1)S(=O)(=O)N 17532216
46866191 1044 0 None -12 3 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 324 1 2 8 1.9 Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(N)nc(n1)N 20346665
46866191 1044 0 None -12 3 Rat 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 324 1 2 8 1.9 Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(N)nc(n1)N 20346665
6209 1044 0 None -12 3 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 324 1 2 8 1.9 Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(N)nc(n1)N 20346665
6209 1044 0 None -12 3 Rat 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 324 1 2 8 1.9 Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(N)nc(n1)N 20346665
CHEMBL1093560 1044 0 None -12 3 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 324 1 2 8 1.9 Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(N)nc(n1)N 20346665
CHEMBL1093560 1044 0 None -12 3 Rat 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 324 1 2 8 1.9 Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(N)nc(n1)N 20346665
1386 3338 0 None - 1 Rat 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 283 4 1 3 3.1 CCOC(=O)NC(=O)C(c1ccccc1)c1ccccc1 11606768
9903898 3338 0 None - 1 Rat 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 283 4 1 3 3.1 CCOC(=O)NC(=O)C(c1ccccc1)c1ccccc1 11606768
1388 3364 0 None - 1 Rat 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 319 3 0 2 3.7 Cc1ccc(cc1)S(=O)(=O)N1CCCC1c1ccc(cc1)F 11606768
17950211 3364 0 None - 1 Rat 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 319 3 0 2 3.7 Cc1ccc(cc1)S(=O)(=O)N1CCCC1c1ccc(cc1)F 11606768
10409562 4116 0 None - 1 Rat 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 414 7 0 6 4.0 COCCN(Cc1ccc2c(c1)nc1n2cc(s1)C(=O)N(C1CCCCC1)C)C 18164695
6361 4116 0 None - 1 Rat 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 414 7 0 6 4.0 COCCN(Cc1ccc2c(c1)nc1n2cc(s1)C(=O)N(C1CCCCC1)C)C 18164695
1390 1556 0 None - 1 Rat 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 2 0 5 2.0 CCn1c(C)nc(c(c1=O)C#N)N1CCc2c(CC1)cccc2 12509432
3363 1556 0 None - 1 Rat 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 2 0 5 2.0 CCn1c(C)nc(c(c1=O)C#N)N1CCc2c(CC1)cccc2 12509432
9904703 1556 0 None - 1 Rat 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 308 2 0 5 2.0 CCn1c(C)nc(c(c1=O)C#N)N1CCc2c(CC1)cccc2 12509432
11301185 1683 32 None - 1 Rat 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 2 0 5 3.3 Cc1c(nnn1c1cccnc1F)c1ccc2c(c1)cccn2 21172734
6353 1683 32 None - 1 Rat 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 2 0 5 3.3 Cc1c(nnn1c1cccnc1F)c1ccc2c(c1)cccn2 21172734
CHEMBL1645352 1683 32 None - 1 Rat 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 2 0 5 3.3 Cc1c(nnn1c1cccnc1F)c1ccc2c(c1)cccn2 21172734
6208 1055 0 None - 1 Rat 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 2 5 1.7 OCC1CCN(CC1)c1ncc(nc1)C(=O)NC1CCCCC1 17064898
73755189 1055 0 None - 1 Rat 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 2 5 1.7 OCC1CCN(CC1)c1ncc(nc1)C(=O)NC1CCCCC1 17064898
46866192 1050 0 None 14 2 Rat 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 1 1 7 2.6 Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(N)nc(n1)C 20346665
6210 1050 0 None 14 2 Rat 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 1 1 7 2.6 Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(N)nc(n1)C 20346665
CHEMBL1093901 1050 0 None 14 2 Rat 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 323 1 1 7 2.6 Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(N)nc(n1)C 20346665
11537456 209 12 None - 1 Rat 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 342 2 0 6 4.0 CN(c1ccnc2c1c1ncn(c(=O)c1s2)C1CCCCCC1)C 18054908
6354 209 12 None - 1 Rat 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 342 2 0 6 4.0 CN(c1ccnc2c1c1ncn(c(=O)c1s2)C1CCCCCC1)C 18054908
CHEMBL225032 209 12 None - 1 Rat 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 342 2 0 6 4.0 CN(c1ccnc2c1c1ncn(c(=O)c1s2)C1CCCCCC1)C 18054908
16118537 978 0 None - 1 Rat 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 363 4 1 6 4.2 COc1ccc(cc1)n1ccc2c(c1=O)sc1c2c(ccn1)NC1CC1 22266036
6357 978 0 None - 1 Rat 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 363 4 1 6 4.2 COc1ccc(cc1)n1ccc2c(c1=O)sc1c2c(ccn1)NC1CC1 22266036
CHEMBL1951683 978 0 None - 1 Rat 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 363 4 1 6 4.2 COc1ccc(cc1)n1ccc2c(c1=O)sc1c2c(ccn1)NC1CC1 22266036
23634102 977 2 None - 1 Rat 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 4 1 7 3.0 C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)OC 19433355
6215 977 2 None - 1 Rat 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 4 1 7 3.0 C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)OC 19433355
CHEMBL1783876 977 2 None - 1 Rat 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 362 4 1 7 3.0 C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)OC 19433355
16739288 1033 0 None - 1 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 306 3 2 2 3.3 Cc1cc2[nH]c3c(c2cc1OCc1ccccc1)CCNC3=O 17276684
6358 1033 0 None - 1 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 306 3 2 2 3.3 Cc1cc2[nH]c3c(c2cc1OCc1ccccc1)CCNC3=O 17276684
CHEMBL396712 1033 0 None - 1 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 306 3 2 2 3.3 Cc1cc2[nH]c3c(c2cc1OCc1ccccc1)CCNC3=O 17276684
16118119 1149 0 None 4 2 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 3 0 6 3.7 COc1ccc(cc1)n1ccc2c(c1=O)sc1c2c(ccn1)N(C)C 22266036
6356 1149 0 None 4 2 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 3 0 6 3.7 COc1ccc(cc1)n1ccc2c(c1=O)sc1c2c(ccn1)N(C)C 22266036
CHEMBL1951658 1149 0 None 4 2 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 3 0 6 3.7 COc1ccc(cc1)n1ccc2c(c1=O)sc1c2c(ccn1)N(C)C 22266036
23634171 976 1 None - 1 Rat 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 366 3 1 6 3.7 C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)Cl 19433355
6214 976 1 None - 1 Rat 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 366 3 1 6 3.7 C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)Cl 19433355
CHEMBL1783874 976 1 None - 1 Rat 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 366 3 1 6 3.7 C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)Cl 19433355
16659801 1036 0 None - 1 Rat 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 370 1 1 7 3.5 Clc1ccc(cc1)n1cnc2c(c1=O)sc1c2c2NCCOc2cn1 17929793
6346 1036 0 None - 1 Rat 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 370 1 1 7 3.5 Clc1ccc(cc1)n1cnc2c(c1=O)sc1c2c2NCCOc2cn1 17929793
CHEMBL236994 1036 0 None - 1 Rat 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 370 1 1 7 3.5 Clc1ccc(cc1)n1cnc2c(c1=O)sc1c2c2NCCOc2cn1 17929793
16659803 1037 0 None - 1 Rat 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 384 1 1 7 3.8 C[C@H]1CNc2c(O1)cnc1c2c2ncn(c(=O)c2s1)c1ccc(cc1)Cl 17929793
6338 1037 0 None - 1 Rat 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 384 1 1 7 3.8 C[C@H]1CNc2c(O1)cnc1c2c2ncn(c(=O)c2s1)c1ccc(cc1)Cl 17929793
CHEMBL236180 1037 0 None - 1 Rat 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 384 1 1 7 3.8 C[C@H]1CNc2c(O1)cnc1c2c2ncn(c(=O)c2s1)c1ccc(cc1)Cl 17929793
7442 2135 6 None -1 3 Rat 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 311 4 0 3 4.5 CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)C)CC 16078827
9948645 2135 6 None -1 3 Rat 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 311 4 0 3 4.5 CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)C)CC 16078827
CHEMBL188906 2135 6 None -1 3 Rat 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 311 4 0 3 4.5 CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)C)CC 16078827
CHEMBL253345 2135 6 None -1 3 Rat 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 311 4 0 3 4.5 CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)C)CC 16078827
10470232 3269 23 None -1 2 Rat 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 3 0 3 4.0 O=C(c1ccc2c(c1)cc1c(n2)OCCC1)Cc1ccccc1 12695537
1391 3269 23 None -1 2 Rat 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 3 0 3 4.0 O=C(c1ccc2c(c1)cc1c(n2)OCCC1)Cc1ccccc1 12695537
6336 3269 23 None -1 2 Rat 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 3 0 3 4.0 O=C(c1ccc2c(c1)cc1c(n2)OCCC1)Cc1ccccc1 12695537
CHEMBL369459 3269 23 None -1 2 Rat 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 303 3 0 3 4.0 O=C(c1ccc2c(c1)cc1c(n2)OCCC1)Cc1ccccc1 12695537
6343 971 0 None - 1 Rat 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 2 1 6 2.6 COc1ccc(cc1)N1C=NC2C(C1=O)Sc1c2c2NCCc2cn1 17929793
73755209 971 0 None - 1 Rat 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 2 1 6 2.6 COc1ccc(cc1)N1C=NC2C(C1=O)Sc1c2c2NCCc2cn1 17929793
16659967 1035 0 None - 1 Rat 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 366 2 1 8 2.8 COc1ccc(cc1)n1cnc2c(c1=O)sc1c2c2NCCOc2cn1 17929793
6345 1035 0 None - 1 Rat 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 366 2 1 8 2.8 COc1ccc(cc1)n1cnc2c(c1=O)sc1c2c2NCCOc2cn1 17929793
CHEMBL393922 1035 0 None - 1 Rat 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 366 2 1 8 2.8 COc1ccc(cc1)n1cnc2c(c1=O)sc1c2c2NCCOc2cn1 17929793
1381 581 30 None - 1 Rat 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 278 2 0 2 3.9 C=C1C[C@H]2[C@](C1)(Cc1ccc3c(c1)cccc3)C(=O)OC2 11306677
9903757 581 30 None - 1 Rat 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 278 2 0 2 3.9 C=C1C[C@H]2[C@](C1)(Cc1ccc3c(c1)cccc3)C(=O)OC2 11306677
CHEMBL254372 581 30 None - 1 Rat 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 278 2 0 2 3.9 C=C1C[C@H]2[C@](C1)(Cc1ccc3c(c1)cccc3)C(=O)OC2 11306677
1373 2475 51 None -6 5 Rat 3.8 pKi None 3.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 209 3 3 3 0.6 OC(=O)c1ccc(cc1)[C@@](C(=O)O)(N)C 12695537
139055582 2475 51 None -6 5 Rat 3.8 pKi None 3.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 209 3 3 3 0.6 OC(=O)c1ccc(cc1)[C@@](C(=O)O)(N)C 12695537
446355 2475 51 None -6 5 Rat 3.8 pKi None 3.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 209 3 3 3 0.6 OC(=O)c1ccc(cc1)[C@@](C(=O)O)(N)C 12695537
CHEMBL257626 2475 51 None -6 5 Rat 3.8 pKi None 3.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 209 3 3 3 0.6 OC(=O)c1ccc(cc1)[C@@](C(=O)O)(N)C 12695537
DB04256 2475 51 None -6 5 Rat 3.8 pKi None 3.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 209 3 3 3 0.6 OC(=O)c1ccc(cc1)[C@@](C(=O)O)(N)C 12695537
1376 321 55 None -91 2 Rat 4.0 pKi None 4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 221 2 3 3 0.6 OC(=O)c1ccc2c(c1)CCC2(N)C(=O)O 12695537
2071 321 55 None -91 2 Rat 4.0 pKi None 4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 221 2 3 3 0.6 OC(=O)c1ccc2c(c1)CCC2(N)C(=O)O 12695537
CHEMBL313938 321 55 None -91 2 Rat 4.0 pKi None 4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 221 2 3 3 0.6 OC(=O)c1ccc2c(c1)CCC2(N)C(=O)O 12695537
1377 1340 26 None -1230 6 Rat 4.1 pKi None 4.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 4 4 4 -1.6 N[C@@H](C1[C@H]([C@@H]1C(=O)O)C(=O)O)C(=O)O 11080213
5310979 1340 26 None -1230 6 Rat 4.1 pKi None 4.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 4 4 4 -1.6 N[C@@H](C1[C@H]([C@@H]1C(=O)O)C(=O)O)C(=O)O 11080213
CHEMBL284193 1340 26 None -1230 6 Rat 4.1 pKi None 4.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 4 4 4 -1.6 N[C@@H](C1[C@H]([C@@H]1C(=O)O)C(=O)O)C(=O)O 11080213
1382 1190 33 None 1 2 Rat 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 2 1 5 1.6 CCOC(=O)C12CC2/C(=N\O)/c2c(O1)cccc2 12695537
6278000 1190 33 None 1 2 Rat 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 2 1 5 1.6 CCOC(=O)C12CC2/C(=N\O)/c2c(O1)cccc2 12695537
CHEMBL327783 1190 33 None 1 2 Rat 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 2 1 5 1.6 CCOC(=O)C12CC2/C(=N\O)/c2c(O1)cccc2 12695537
1418 3449 53 None 21 2 Rat 5.4 pKi None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 195 3 3 3 0.5 N[C@@H](c1ccc(cc1)C(=O)O)C(=O)O 12695537
5311459 3449 53 None 21 2 Rat 5.4 pKi None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 195 3 3 3 0.5 N[C@@H](c1ccc(cc1)C(=O)O)C(=O)O 12695537
CHEMBL94990 3449 53 None 21 2 Rat 5.4 pKi None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 195 3 3 3 0.5 N[C@@H](c1ccc(cc1)C(=O)O)C(=O)O 12695537
1368 2290 37 None -19 11 Rat 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 11080213
5310956 2290 37 None -19 11 Rat 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 11080213
CHEMBL280563 2290 37 None -19 11 Rat 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 159 3 3 3 -0.9 N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O 11080213
104766 33 42 None 3 11 Rat 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 11080213
104766 33 42 None 3 11 Rat 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 12695537
104766 33 42 None 3 11 Rat 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 7690672
1365 33 42 None 3 11 Rat 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 11080213
1365 33 42 None 3 11 Rat 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 12695537
1365 33 42 None 3 11 Rat 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 7690672
CHEMBL34453 33 42 None 3 11 Rat 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 11080213
CHEMBL34453 33 42 None 3 11 Rat 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 12695537
CHEMBL34453 33 42 None 3 11 Rat 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 173 2 3 3 -0.3 OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O 7690672
108001 93 0 None -53 3 Rat 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 2 4 4 0.2 OC(=O)C(c1cc(O)cc(c1)O)N 12695537
1367 93 0 None -53 3 Rat 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 2 4 4 0.2 OC(=O)C(c1cc(O)cc(c1)O)N 12695537
CHEMBL66105 93 0 None -53 3 Rat 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 183 2 4 4 0.2 OC(=O)C(c1cc(O)cc(c1)O)N 12695537
1374 2081 35 None 12 2 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 3 4 4 0.2 N[C@@H](c1ccc(c(c1)O)C(=O)O)C(=O)O 11080213
1374 2081 35 None 12 2 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 3 4 4 0.2 N[C@@H](c1ccc(c(c1)O)C(=O)O)C(=O)O 12695537
5311455 2081 35 None 12 2 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 3 4 4 0.2 N[C@@H](c1ccc(c(c1)O)C(=O)O)C(=O)O 11080213
5311455 2081 35 None 12 2 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 3 4 4 0.2 N[C@@H](c1ccc(c(c1)O)C(=O)O)C(=O)O 12695537
CHEMBL39372 2081 35 None 12 2 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 3 4 4 0.2 N[C@@H](c1ccc(c(c1)O)C(=O)O)C(=O)O 11080213
CHEMBL39372 2081 35 None 12 2 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 211 3 4 4 0.2 N[C@@H](c1ccc(c(c1)O)C(=O)O)C(=O)O 12695537
12310764 1970 64 None 14 8 Rat 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 158 2 3 4 -0.9 OC(=O)C(c1o[nH]c(=O)c1)N 11080213
12310764 1970 64 None 14 8 Rat 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 158 2 3 4 -0.9 OC(=O)C(c1o[nH]c(=O)c1)N 7690672
1233 1970 64 None 14 8 Rat 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 158 2 3 4 -0.9 OC(=O)C(c1o[nH]c(=O)c1)N 11080213
1233 1970 64 None 14 8 Rat 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 158 2 3 4 -0.9 OC(=O)C(c1o[nH]c(=O)c1)N 7690672
1371 1970 64 None 14 8 Rat 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 158 2 3 4 -0.9 OC(=O)C(c1o[nH]c(=O)c1)N 11080213
1371 1970 64 None 14 8 Rat 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 158 2 3 4 -0.9 OC(=O)C(c1o[nH]c(=O)c1)N 7690672
CHEMBL284895 1970 64 None 14 8 Rat 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 158 2 3 4 -0.9 OC(=O)C(c1o[nH]c(=O)c1)N 11080213
CHEMBL284895 1970 64 None 14 8 Rat 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 158 2 3 4 -0.9 OC(=O)C(c1o[nH]c(=O)c1)N 7690672
1310 2315 110 None -4 18 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 11080213
1310 2315 110 None -4 18 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 12695537
1369 2315 110 None -4 18 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 11080213
1369 2315 110 None -4 18 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 12695537
33032 2315 110 None -4 18 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 11080213
33032 2315 110 None -4 18 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 12695537
44272391 2315 110 None -4 18 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 11080213
44272391 2315 110 None -4 18 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 12695537
88747398 2315 110 None -4 18 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 11080213
88747398 2315 110 None -4 18 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 12695537
CHEMBL575060 2315 110 None -4 18 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 11080213
CHEMBL575060 2315 110 None -4 18 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 12695537
DB00142 2315 110 None -4 18 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 11080213
DB00142 2315 110 None -4 18 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N 12695537
1370 3263 67 None 17 8 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 11080213
1370 3263 67 None 17 8 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 12695537
1372 3263 67 None 17 8 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 11080213
1372 3263 67 None 17 8 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 12695537
40539 3263 67 None 17 8 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 11080213
40539 3263 67 None 17 8 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 12695537
6971145 3263 67 None 17 8 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 11080213
6971145 3263 67 None 17 8 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 12695537
CHEMBL279956 3263 67 None 17 8 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 11080213
CHEMBL279956 3263 67 None 17 8 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 12695537
DB02999 3263 67 None 17 8 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 11080213
DB02999 3263 67 None 17 8 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 189 3 3 6 -2.5 OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N 12695537
1378 2417 54 None -162 10 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 9680254
1399 2417 54 None -162 10 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 9680254
9819927 2417 54 None -162 10 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 9680254
CHEMBL432038 2417 54 None -162 10 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 5 3 4 2.8 OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N 9680254
1384 2880 59 None - 1 Rat 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 2 1 3 3.3 O=C(c1cnc2c(n1)cccc2)NC12CC3CC(C2)CC(C1)C3 12695537
7067728 2880 59 None - 1 Rat 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 2 1 3 3.3 O=C(c1cnc2c(n1)cccc2)NC12CC3CC(C2)CC(C1)C3 12695537
CHEMBL399160 2880 59 None - 1 Rat 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 307 2 1 3 3.3 O=C(c1cnc2c(n1)cccc2)NC12CC3CC(C2)CC(C1)C3 12695537