Ligand source activities (1 row/activity)



Get vendors


Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
Sel. page Common
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 6861 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 6861 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 6861 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 199608 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 199608 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 131018 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 131018 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 145802 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 145802 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 145802 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 145802 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 144473 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 144473 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 78664 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 78664 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 78664 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 130709 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 130709 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 130712 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 130712 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 130709 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 130709 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 130712 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 130712 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 145817 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 145817 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 144473 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 144473 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 145817 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 145817 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 131035 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 131035 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 131016 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 131016 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 144570 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 144570 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 194416 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 194416 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 144570 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 144570 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 145868 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 145868 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 145868 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 145868 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 145732 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 145732 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 145732 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 145732 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 144607 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 144607 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 145747 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 145747 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 131035 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 131035 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 194415 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 194415 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 144607 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 144607 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 145747 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 145747 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 145820 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 145820 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 188534 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 188534 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 145761 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 145761 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 144475 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 144475 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 144475 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 144475 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 194416 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 194416 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 146870 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 146870 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 144547 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 144547 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 144547 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 144547 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 146870 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 146870 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 131022 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 131022 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 145761 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 145761 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 144540 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 144540 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 144540 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 144540 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 131037 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 131037 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 6822 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 6822 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 6822 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 144543 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 144543 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 144543 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 144543 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 145861 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 145861 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 131019 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 131019 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 145861 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 145861 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 131005 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 131005 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 131032 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 131032 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 194419 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 194419 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 194383 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 194383 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 186865 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 186865 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 146709 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 146709 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 144588 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 144588 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 144609 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 144609 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 146709 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 146709 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 144588 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 144588 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 145822 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 145822 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 145751 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 145751 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 145822 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 145822 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 130853 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 130853 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 146429 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 146429 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 144519 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 144519 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 146429 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 146429 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 144519 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 144519 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 144515 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 144515 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 199608 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 199608 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 144438 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 144438 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 144572 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 144572 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 144515 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 144515 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 144572 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 144572 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 144438 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 144438 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 131026 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 131026 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 187234 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 187234 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 199913 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 199913 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 131031 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 131031 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 131034 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 131034 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 10113 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 10113 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 10113 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 131029 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 131029 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 145762 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 145762 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 194415 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 194415 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 131013 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 131013 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 144508 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 144508 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 145751 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 145751 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 145762 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 145762 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 189409 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 189409 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 144508 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 144508 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 131008 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 131008 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 144473 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 144473 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 144440 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 144440 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 144506 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 144506 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 7868 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 7868 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 7868 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 189300 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 189300 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 144440 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 144440 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 145741 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 145741 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 144626 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 144626 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 131033 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 131033 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 130711 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 130711 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 9070 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 9070 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 9070 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 144626 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 144626 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 146719 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 146719 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 130711 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 130711 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 130706 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 130706 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 130706 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 130706 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 146719 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 146719 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 144609 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 144609 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 145741 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 145741 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 145892 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 145892 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 10113 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 10113 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 10113 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 145892 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 145892 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 10113 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 10113 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 10113 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 145820 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 145820 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 194383 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 194383 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 144420 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 144420 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 144473 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 144473 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 144568 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 144568 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 144568 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 144568 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 144420 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 144420 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 131009 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 131009 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 194083 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 194083 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 145891 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 145891 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 144582 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 144582 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 145891 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 145891 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 144582 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 144582 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 146532 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 146532 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 146532 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 146532 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 10113 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 10113 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 10113 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 10113 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 10113 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 10113 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 131010 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 131010 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 131006 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 131006 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 131036 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 131036 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 130716 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 130716 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 190361 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 190361 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 130710 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 130710 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 130710 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 130710 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 130710 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 130710 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 8860 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 8860 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 8860 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 130708 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 130708 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 130708 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 130708 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 131038 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 131038 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 144630 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 144630 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 144630 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 144630 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 131011 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 131011 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 131025 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 131025 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 145742 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 145742 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 145764 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 145764 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 144427 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 144427 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 145764 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 145764 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 10821 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 10821 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 10821 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 146870 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 146870 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 145801 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 145801 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 145742 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 145742 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 145801 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 145801 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 146870 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 146870 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 145966 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 145966 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 145966 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 145966 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 144427 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 144427 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 194418 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 194418 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 131023 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 131023 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 145759 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 145759 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 10821 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 10821 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 10821 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 10821 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 10821 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 10821 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 145759 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 145759 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 194418 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 194418 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 194016 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 194016 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 194083 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 194083 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 130710 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 130710 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 130710 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 130710 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 144453 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 144453 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 144453 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 144453 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 190308 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 190308 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 6822 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 6822 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 6822 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 108978 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 108978 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 108978 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 8751 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 8751 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 8751 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 8751 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 144561 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 144561 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 194452 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 194452 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 131007 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 131007 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 130704 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 130704 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 130704 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 130704 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 131020 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 131020 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 131027 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 131027 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 144551 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 144551 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 145942 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 145942 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 194419 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 194419 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 144551 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 144551 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 47475 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 47475 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 145942 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 145942 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 131004 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 131004 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 47475 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 47475 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 145852 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 145852 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 145852 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 145852 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 131014 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 131014 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 131015 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 131015 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 131021 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 131021 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 144561 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 144561 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 144612 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 144612 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 144411 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 144411 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 188757 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 188757 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 144411 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 144411 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 7868 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 7868 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 7868 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 144497 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 144497 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 144497 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 144497 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 131017 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 131017 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 144612 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 144612 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 131030 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 131030 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 144536 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 144536 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 130707 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 130707 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 144536 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 144536 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 130707 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 130707 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 130703 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 130703 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 130703 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 130703 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 144585 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 144585 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 10113 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 10113 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 10113 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 144463 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 144463 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 189292 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 189292 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 144585 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 144585 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 145738 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 145738 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 145738 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 145738 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 189674 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 189674 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 190169 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 190169 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 144463 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 144463 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 186359 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 186359 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 144506 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 144506 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 144499 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 144499 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 186731 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 186731 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 144499 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 144499 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 144546 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 144546 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 144546 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 144546 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 145970 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 145970 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 153230 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 153230 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 153230 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 145970 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 145970 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 199913 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 199913 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 144504 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 144504 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 144504 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 144504 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 145913 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 145913 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 145913 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 145913 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 146429 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 146429 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 146429 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 146429 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 186683 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 186683 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 131028 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 131028 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 188213 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 188213 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 145743 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 145743 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 190061 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 190061 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 145743 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 145743 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 130709 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 130709 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 130709 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 130709 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 102861 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 102861 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 144523 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 144523 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 144523 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 144523 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 145831 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 145831 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 131012 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 131012 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 145831 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 145831 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 194452 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 194452 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 146719 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 146719 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 146719 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 146719 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 145876 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 145876 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 6822 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 6822 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 6822 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 145876 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 145876 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 131024 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 131024 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 145771 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 145771 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 145771 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 145771 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 145730 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 145730 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 145730 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 145730 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 130705 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 130705 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 130705 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 130705 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 130712 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 130712 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 130712 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 130712 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 188954 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 188954 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 96731 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 96731 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 77747 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 77747 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 155112 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 155112 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 77799 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 77799 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 7763 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 7763 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 7763 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 79987 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 79987 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 90597 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 90597 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 90598 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 90598 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 90599 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 90599 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 6997 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 6997 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 6997 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 6999 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 6999 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 6999 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 69434 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 69434 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 8915 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 8915 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 8915 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 8915 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 7825 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 7825 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 7825 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 69444 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 69444 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 181849 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 181849 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 69518 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 69518 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 204157 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 204157 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 69522 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 69522 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 6999 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 6999 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 6999 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 204126 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 204126 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 77749 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 77749 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 69439 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 69439 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 69437 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 69437 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 69530 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 69530 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 69521 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 69521 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 79992 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 79992 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 205427 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 205427 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 161838 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 161838 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 182330 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 182330 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 98808 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 98808 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 10222 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 10222 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 10222 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 131900 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 131900 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 148849 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 148849 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 93527 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 93527 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 94292 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 94292 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 69441 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 69441 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 99128 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 99128 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 131018 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 131018 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 149121 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 149121 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 101528 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 101528 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 24893 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 24893 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 139882 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 139882 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 69517 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 69517 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 201964 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 201964 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 125688 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 125688 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 25087 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 25087 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 15004 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 15004 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 69429 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 69429 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 195981 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 195981 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 204037 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 204037 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 79988 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 79988 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 161723 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 161723 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 161352 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 161352 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 131878 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 131878 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 131914 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 131914 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 121116 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 121116 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 121116 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 121116 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 91929 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 91929 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 97823 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 97823 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 98796 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 98796 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 77757 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 77757 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 97823 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 97823 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 98796 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 98796 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 131887 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 131887 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 139898 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 139898 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 90590 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 90590 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 155391 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 155391 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 7765 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 7765 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 7765 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 77817 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 77817 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 180088 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 180088 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 69524 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 69524 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 69519 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 69519 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 131035 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 131035 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 69431 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 69431 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 183612 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 183612 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 95248 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 95248 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 139859 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 139859 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 35821 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 35821 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 101440 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 101440 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 91969 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 91969 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 125684 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 125684 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 131016 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 131016 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 77767 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 77767 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 125693 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 125693 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 100705 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 100705 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 121119 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 121119 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 69538 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 69538 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 91584 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 91584 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 91877 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 91877 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 203884 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 203884 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 101529 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 101529 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 131856 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 131856 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 139803 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 139803 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 139820 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 139820 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 94291 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 94291 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 161623 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 161623 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 97824 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 97824 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 77769 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 77769 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 97824 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 97824 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 128984 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 128984 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 121108 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 121108 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 69543 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 69543 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 79997 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 79997 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 97811 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 97811 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 91783 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 91783 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 90601 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 90601 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 77753 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 77753 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 69526 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 69526 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 91838 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 91838 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 130717 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 130717 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 139819 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 139819 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 139821 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 139821 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 139852 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 139852 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 175076 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 175076 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 97811 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 97811 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 112380 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 112380 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 7843 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 7843 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 7843 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 125687 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 125687 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 98804 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 98804 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 131022 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 131022 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 98804 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 98804 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 91843 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 91843 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 145926 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 145926 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 145926 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 145926 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 131895 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 131895 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 90481 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 90481 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 77765 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 77765 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 77813 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 77813 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 77816 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 77816 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 139797 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 139797 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 139823 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 139823 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 131037 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 131037 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 148041 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 148041 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 131032 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 131032 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 182328 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 182328 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 139796 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 139796 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 205109 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 205109 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 204015 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 204015 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 205413 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 205413 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 101492 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 101492 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 131911 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 131911 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 139850 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 139850 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 139887 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 139887 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 139890 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 139890 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 85298 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 85298 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 173957 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 173957 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 145734 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 145734 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 145734 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 145734 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 202555 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 202555 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 90592 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 90592 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 131019 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 131019 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 95850 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 95850 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 95850 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 14693 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 14693 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 69532 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 69532 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 90602 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 90602 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 91997 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 91997 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 183587 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 183587 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 101773 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 101773 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 183674 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 183674 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 8231 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 8231 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 8231 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 131005 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 131005 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 69438 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 69438 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 96994 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 96994 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 7368 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 7368 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 7368 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 183612 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 183612 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 101598 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 101598 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 183610 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 183610 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 139827 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 139827 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 139847 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 139847 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 139870 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 139870 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 97815 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 97815 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 145805 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 145805 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 145814 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 145814 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 121113 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 121113 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 97815 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 97815 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 145805 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 145805 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 145814 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 145814 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 131884 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 131884 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 97817 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 97817 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 97820 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 97820 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 97817 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 97817 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 148506 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 148506 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 148609 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 148609 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 7820 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 7820 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 7820 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 97820 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 97820 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 157049 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 157049 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 69533 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 69533 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 91840 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 91840 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 77770 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 77770 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 205372 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 205372 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 139860 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 139860 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 202691 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 202691 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 101526 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 101526 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 69549 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 69549 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 145870 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 145870 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 183540 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 183540 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 203885 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 203885 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 130853 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 130853 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 172892 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 172892 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 161588 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 161588 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 180345 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 180345 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 181944 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 181944 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 205707 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 205707 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 131906 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 131906 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 145870 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 145870 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 119321 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 119321 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 125697 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 125697 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 139899 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 139899 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 91894 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 91894 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 121115 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 121115 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 98809 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 98809 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 139884 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 139884 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 98809 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 98809 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 15002 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 15002 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 90479 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 90479 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 90587 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 90587 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 143620 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 143620 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 131034 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 131034 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 82481 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 82481 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 145294 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 145294 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 176885 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 176885 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 94293 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 94293 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 101491 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 101491 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 9198 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 9198 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 9198 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 98801 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 98801 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 98801 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 98801 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 131864 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 131864 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 90474 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 90474 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 77768 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 77768 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 139880 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 139880 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 69442 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 69442 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 159321 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 159321 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 131026 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 131026 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 69428 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 69428 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 90596 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 90596 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 77774 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 77774 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 77808 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 77808 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 7764 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 7764 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 7764 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 7830 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 7830 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 7830 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 7824 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 7824 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 7824 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 95461 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 95461 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 77809 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 77809 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 205274 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 205274 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 95517 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 95517 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 7822 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 7822 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 7822 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 180088 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 180088 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 203638 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 203638 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 7823 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 7823 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 7823 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 90606 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 90606 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 91867 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 91867 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 131031 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 131031 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 204593 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 204593 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 77800 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 77800 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 125690 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 125690 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 90605 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 90605 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 202429 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 202429 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 128979 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 128979 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 131890 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 131890 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 131847 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 131847 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 131029 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 131029 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 69545 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 69545 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 25088 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 25088 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 69546 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 69546 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 87614 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 87614 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 131013 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 131013 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 203639 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 203639 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 203634 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 203634 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 139799 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 139799 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 94617 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 94617 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 101718 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 101718 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 101460 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 101460 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 101460 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 69540 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 69540 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 145830 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 145830 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 145830 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 145830 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 69547 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 69547 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 204067 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 204067 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 139826 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 139826 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 131008 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 131008 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 131033 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 131033 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 182330 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 182330 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 161403 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 161403 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 139888 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 139888 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 131898 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 131898 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 139834 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 139834 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 121121 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 121121 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 121123 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 121123 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 95862 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 95862 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 95862 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 145967 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 145967 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 145790 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 145790 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 145790 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 145790 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 145967 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 145967 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 203369 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 203369 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 99127 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 99127 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 131882 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 131882 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 61483 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 61483 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 91927 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 91927 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 161353 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 161353 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 204537 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 204537 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 101493 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 101493 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 131907 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 131907 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 139835 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 139835 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 101717 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 101717 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 145833 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 145833 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 145901 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 145901 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 145833 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 145833 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 145901 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 145901 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 131881 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 131881 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 95869 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 95869 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 95869 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 125700 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 125700 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 173286 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 173286 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 202561 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 202561 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 202812 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 202812 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 97814 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 97814 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 90588 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 90588 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 195982 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 195982 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 95519 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 95519 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 100376 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 100376 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 100700 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 100700 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 203995 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 203995 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 139893 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 139893 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 69443 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 69443 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 100545 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 100545 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 97814 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 97814 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 145809 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 145809 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 125689 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 125689 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 97826 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 97826 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 97826 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 97826 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 145809 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 145809 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 147116 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 147116 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 205148 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 205148 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 101412 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 101412 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 10317 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 10317 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 10317 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 101436 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 101436 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 161542 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 161542 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 53087 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 53087 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 10317 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 10317 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 10317 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 144321 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 144321 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 82202 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 82202 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 82337 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 82337 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 97807 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 97807 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 121126 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 121126 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 97807 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 97807 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 148689 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 148689 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 131009 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 131009 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 10791 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 10791 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 10791 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 161142 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 161142 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 131875 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 131875 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 97825 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 97825 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 97825 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 97825 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 145908 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 145908 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 7836 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 7836 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 7836 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 77764 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 77764 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 139794 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 139794 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 131010 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 131010 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 128974 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 128974 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 145908 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 145908 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 90595 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 90595 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 95851 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 95851 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 95851 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 9201 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 9201 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 9201 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 131006 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 131006 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 131036 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 131036 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 139810 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 139810 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 148860 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 148860 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 125691 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 125691 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 202628 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 202628 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 159084 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 159084 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 131903 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 131903 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 183611 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 183611 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 125694 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 125694 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 98797 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 98797 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 98797 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 98797 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 202412 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 202412 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 112382 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 112382 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 69536 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 69536 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 90476 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 90476 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 90585 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 90585 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 6998 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 6998 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 6998 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 6998 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 6998 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 6998 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 77806 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 77806 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 6998 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 6998 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 6998 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 7821 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 7821 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 7821 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 8916 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 8916 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 8916 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 8916 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 15246 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 15246 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 77755 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 77755 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 8478 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 8478 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 8478 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 205293 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 205293 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 181571 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 181571 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 77771 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 77771 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 7672 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 7672 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 7672 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 204034 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 204034 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 204034 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 9336 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 9336 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 9336 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 203718 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 203718 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 69520 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 69520 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 69537 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 69537 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 77752 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 77752 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 90480 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 90480 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 157383 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 157383 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 203873 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 203873 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 194857 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 194857 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 101462 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 101462 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 202610 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 202610 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 101411 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 101411 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 139798 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 139798 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 112369 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 112369 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 150927 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 150927 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 125702 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 125702 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 77815 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 77815 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 183587 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 183587 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 139846 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 139846 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 95868 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 95868 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 95868 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 100079 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 100079 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 69548 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 69548 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 125696 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 125696 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 81808 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 81808 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 82699 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 82699 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 79987 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 79987 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 25073 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 25073 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 91842 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 91842 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 139848 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 139848 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 139902 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 139902 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 15257 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 15257 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 69535 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 69535 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 204035 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 204035 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 148609 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 148609 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 131886 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 131886 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 131905 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 131905 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 131038 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 131038 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 131889 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 131889 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 91773 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 91773 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 145818 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 145818 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 77812 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 77812 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 131011 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 131011 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 131025 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 131025 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 131899 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 131899 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 139830 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 139830 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 7973 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 7973 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 7973 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 145818 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 145818 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 97810 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 97810 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 97810 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 97810 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 77760 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 77760 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 139820 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 139820 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 100378 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 100378 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 139806 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 139806 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 112378 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 112378 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 69550 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 69550 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 97819 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 97819 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 98799 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 98799 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 97819 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 97819 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 98799 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 98799 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 91622 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 91622 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 96995 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 96995 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 121112 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 121112 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 173379 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 173379 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 139879 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 139879 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 131023 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 131023 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 79995 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 79995 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 150272 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 150272 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 181944 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 181944 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 183540 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 183540 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 128978 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 128978 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 172779 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 172779 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 204036 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 204036 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 202967 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 202967 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 95840 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 95840 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 95840 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 12635 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 12635 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 97812 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 97812 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 81207 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 81207 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 82026 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 82026 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 146586 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 146586 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 97812 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 97812 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 94610 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 94610 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 90600 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 90600 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 91999 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 91999 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 69433 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 69433 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 77807 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 77807 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 69528 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 69528 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 77745 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 77745 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 205602 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 205602 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 96732 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 96732 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 101490 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 101490 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 177031 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 177031 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 8862 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 8862 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 8862 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 25747 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 25747 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 131897 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 131897 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 143605 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 143605 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 121111 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 121111 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 120921 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 120921 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 156524 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 156524 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 7831 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 7831 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 7831 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 24892 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 24892 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 91814 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 91814 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 131888 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 131888 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 161774 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 161774 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 97808 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 97808 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 97808 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 97808 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 139861 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 139861 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 69440 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 69440 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 7000 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 7000 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 7000 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 131007 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 131007 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 85297 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 85297 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 9253 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 9253 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 9253 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 9253 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 9253 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 125686 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 125686 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 91878 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 91878 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 161378 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 161378 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 153167 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 153167 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 155734 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 155734 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 128980 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 128980 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 69544 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 69544 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 91908 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 91908 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 121122 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 121122 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 139843 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 139843 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 101461 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 101461 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 95876 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 95876 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 95876 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 131020 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 131020 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 145760 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 145760 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 100082 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 100082 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 145760 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 145760 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 131027 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 131027 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 77803 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 77803 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 131004 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 131004 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 203643 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 203643 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 125695 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 125695 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 98807 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 98807 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 98807 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 98807 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 145894 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 145894 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 131014 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 131014 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 131015 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 131015 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 131021 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 131021 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 101565 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 101565 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 139817 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 139817 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 149134 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 149134 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 145894 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 145894 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 172922 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 172922 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 182328 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 182328 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 204014 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 204014 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 205375 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 205375 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 131877 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 131877 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 139795 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 139795 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 121114 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 121114 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 90278 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 90278 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 90482 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 90482 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 90593 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 90593 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 91619 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 91619 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 91868 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 91868 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 77754 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 77754 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 6998 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 6998 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 6998 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 9655 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 9655 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 9655 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 8423 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 8423 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 8423 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 77746 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 77746 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 95462 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 95462 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 77762 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 77762 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 205683 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 205683 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 8478 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 8478 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 8478 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 77748 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 77748 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 8478 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 8478 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 8478 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 98763 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 98763 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 150017 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 150017 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 150316 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 150316 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 121117 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 121117 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 82632 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 82632 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 131883 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 131883 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 98800 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 98800 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 98803 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 98803 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 98803 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 98803 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 98800 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 98800 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 87006 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 87006 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 101563 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 101563 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 161544 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 161544 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 139811 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 139811 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 69531 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 69531 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 139804 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 139804 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 101413 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 101413 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 125699 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 125699 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 131017 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 131017 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 131030 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 131030 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 77759 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 77759 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 131902 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 131902 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 174192 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 174192 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 128983 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 128983 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 98795 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 98795 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 115051 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 115051 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 180345 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 180345 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 77766 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 77766 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 128982 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 128982 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 98795 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 98795 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 100083 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 100083 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 98810 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 98810 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 131904 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 131904 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 145851 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 145851 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 139903 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 139903 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 98810 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 98810 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 145851 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 145851 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 158936 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 158936 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 183611 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 183611 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 121120 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 121120 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 205254 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 205254 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 170300 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 170300 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 214533 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 214533 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 205496 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 205496 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 121109 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 121109 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 195981 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 195981 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 121112 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 121112 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 10222 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 10222 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 10222 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 139795 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 139795 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 139885 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 139885 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 112381 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 112381 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 183610 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 183610 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 139871 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 139871 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 139892 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 139892 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 97821 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 97821 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 7753 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 7753 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 7753 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 204590 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 204590 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 156654 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 156654 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 101747 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 101747 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 101525 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 101525 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 183674 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 183674 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 7932 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 7932 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 7932 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 77756 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 77756 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 77810 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 77810 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 77814 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 77814 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 7764 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 7764 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 7764 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 69432 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 69432 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 69539 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 69539 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 69435 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 69435 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 69430 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 69430 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 90594 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 90594 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 125692 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 125692 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 112762 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 112762 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 97821 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 97821 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 205194 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 205194 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 65593 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 65593 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 65593 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 65593 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 91821 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 91821 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 95420 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 95420 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 139889 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 139889 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 131898 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 131898 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 139856 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 139856 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 98473 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 98473 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 95873 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 95873 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 95873 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 79989 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 79989 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 139886 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 139886 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 139845 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 139845 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 118824 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 118824 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 145811 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 145811 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 69436 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 69436 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 121110 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 121110 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 121113 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 121113 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 131874 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 131874 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 7973 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 7973 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 7973 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 97818 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 97818 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 145811 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 145811 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 121124 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 121124 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 97818 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 97818 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 98805 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 98805 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 79996 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 79996 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 131176 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 131176 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 98805 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 98805 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 120921 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 120921 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 15003 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 15003 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 77772 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 77772 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 93526 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 93526 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 139901 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 139901 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 95877 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 95877 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 95877 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 205303 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 205303 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 145938 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 145938 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 145938 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 145938 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 139802 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 139802 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 139824 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 139824 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 79991 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 79991 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 79994 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 79994 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 7936 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 7936 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 7936 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 90584 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 90584 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 90604 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 90604 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 181849 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 181849 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 181571 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 181571 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 69523 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 69523 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 77804 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 77804 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 90478 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 90478 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 7109 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 7109 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 7109 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 101564 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 101564 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 131879 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 131879 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 131846 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 131846 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 97809 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 97809 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 97822 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 97822 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 91928 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 91928 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 93498 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 93498 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 149122 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 149122 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 131910 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 131910 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 97809 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 97809 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 12275 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 12275 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 97822 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 97822 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 69527 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 69527 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 119299 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 119299 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 131860 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 131860 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 95833 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 95833 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 95833 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 121118 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 121118 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 121118 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 121118 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 202696 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 202696 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 161773 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 161773 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 121125 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 121125 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 77801 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 77801 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 145786 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 145786 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 131028 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 131028 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 145786 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 145786 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 91839 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 91839 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 100429 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 100429 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 161453 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 161453 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 139881 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 139881 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 98798 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 98798 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 205648 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 205648 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 98798 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 98798 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 100699 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 100699 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 161543 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 161543 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 9195 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 9195 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 9195 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 9195 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 77761 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 77761 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 101689 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 101689 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 90603 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 90603 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 139818 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 139818 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 77751 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 77751 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 69541 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 69541 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 77750 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 77750 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 69534 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 69534 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 205096 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 205096 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 157239 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 157239 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 100428 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 100428 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 139809 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 139809 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 203888 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 203888 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 131849 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 131849 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 90477 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 90477 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 91828 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 91828 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 139897 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 139897 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 205430 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 205430 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 145840 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 145840 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 98811 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 98811 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 98811 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 98811 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 91935 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 91935 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 145840 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 145840 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 69542 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 69542 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 77758 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 77758 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 98802 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 98802 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 98802 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 98802 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 202928 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 202928 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 91970 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 91970 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 90589 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 90589 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 24891 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 24891 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 148813 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 148813 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 77802 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 77802 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 77811 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 77811 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 205131 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 205131 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 9198 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 9198 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 9198 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 9198 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 9198 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 9198 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 145765 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 145765 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 131012 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 131012 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 131876 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 131876 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 139844 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 139844 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 94295 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 94295 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 145765 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 145765 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 79987 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 79987 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 79993 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 79993 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 90475 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 90475 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 90591 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 90591 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 91813 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 91813 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 79987 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 79987 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 173834 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 173834 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 173834 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 173834 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 173834 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 173834 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 69525 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 69525 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 195982 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 195982 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 96735 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 96735 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 77805 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 77805 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 100663 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 100663 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 79990 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 79990 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 93499 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 93499 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 139822 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 139822 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 98806 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 98806 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 145823 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 145823 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 98806 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 98806 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 145823 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 145823 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 145945 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 145945 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 85296 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 85296 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 131869 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 131869 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 105637 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 105637 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 145945 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 145945 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 139801 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 139801 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 150343 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 150343 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 131024 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 131024 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 94294 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 94294 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 69529 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 69529 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 12248 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 12248 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 9202 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 9202 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 9202 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 97813 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 97813 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 97816 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 97816 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 143955 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 143955 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 204594 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 204594 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 100512 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 100512 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 97816 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 97816 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 144705 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 144705 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 97813 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 97813 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 97813 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 97813 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 69438 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 69438 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 69439 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 69439 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 77748 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 77748 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 7763 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 7763 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 7763 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 69431 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 69431 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 69518 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 69518 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 69428 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 69428 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 69430 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 69430 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 69437 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 69437 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 69440 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 69440 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 69444 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 69444 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 77745 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 77745 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 77747 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 77747 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 185835 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 185835 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 69529 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 69529 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 168071 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 168071 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 185867 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 185867 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 185619 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 185619 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 69545 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 69545 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 77768 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 77768 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 100482 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 100482 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 100271 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 100271 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 185620 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 185620 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 77751 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 77751 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 77754 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 77754 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 10037 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 10037 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 10037 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 10037 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 10037 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 10037 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 196257 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 196257 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 77761 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 77761 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 77755 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 77755 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 77805 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 77805 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 100626 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 100626 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 159895 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 159895 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 177061 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 177061 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 196177 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 196177 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 69441 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 69441 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 69442 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 69442 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 77752 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 77752 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 77774 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 77774 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 77813 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 77813 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 7936 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 7936 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 7936 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 77767 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 77767 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 69432 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 69432 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 69443 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 69443 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 154525 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 154525 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 185989 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 185989 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 77762 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 77762 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 7753 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 7753 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 7753 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 194859 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 194859 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 100227 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 100227 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 148362 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 148362 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 77771 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 77771 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 69517 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 69517 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 178770 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 178770 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 213616 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 213616 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 185701 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 185701 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 176301 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 176301 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 7932 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 7932 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 7932 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 185621 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 185621 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 100552 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 100552 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 69520 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 69520 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 77750 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 77750 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 77764 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 77764 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 194713 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 194713 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 77753 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 77753 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 77810 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 77810 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 194858 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 194858 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 100226 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 100226 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 100270 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 100270 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 69523 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 69523 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 69534 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 69534 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 69429 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 69429 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 69524 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 69524 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 185893 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 185893 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 185834 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 185834 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 77758 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 77758 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 185635 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 185635 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 98781 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 98781 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 77817 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 77817 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 195800 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 195800 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 77766 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 77766 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 69528 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 69528 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 69538 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 69538 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 10317 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 10317 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 10317 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 69521 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 69521 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 100334 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 100334 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 100335 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 100335 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 196173 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 196173 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 77772 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 77772 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 69519 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 69519 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 77814 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 77814 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 69539 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 69539 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 77746 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 77746 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 100186 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 100186 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 100273 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 100273 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 7821 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 7821 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 7821 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 69436 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 69436 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 77809 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 77809 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 7764 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 7764 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 7764 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 69526 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 69526 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 159896 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 159896 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 196047 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 196047 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 9391 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 9391 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 9391 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 177031 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 177031 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 77800 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 77800 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 196174 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 196174 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 100551 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 100551 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 69542 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 69542 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 77759 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 77759 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 77802 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 77802 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 77812 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 77812 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 196077 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 196077 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 185808 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 185808 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 100336 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 100336 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 213905 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 213905 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 9391 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 9391 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 9391 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 69530 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 69530 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 69541 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 69541 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 69435 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 69435 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 69536 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 69536 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 100228 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 100228 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 100554 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 100554 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 155079 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 155079 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 77801 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 77801 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 100438 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 100438 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 196118 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 196118 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 77760 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 77760 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 6822 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 6822 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 6822 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 69532 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 69532 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 100555 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 100555 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 8751 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 8751 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 8751 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 8751 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 154242 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 154242 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 69533 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 69533 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 195970 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 195970 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 7765 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 7765 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 7765 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 69434 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 69434 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 9070 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 9070 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 9070 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 154867 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 154867 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 77816 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 77816 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 185988 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 185988 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 100272 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 100272 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 77749 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 77749 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 77757 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 77757 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 213895 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 213895 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 7856 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 7856 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 7856 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 77799 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 77799 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 77756 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 77756 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 8408 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 8408 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 8408 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 8408 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 8408 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 8408 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 8408 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 8408 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 112762 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 112762 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 195893 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 195893 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 179421 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 179421 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 69531 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 69531 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 69546 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 69546 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 77770 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 77770 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 69535 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 69535 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 69544 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 69544 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 152816 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 152816 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 100229 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 100229 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 153230 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 153230 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 153230 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 69527 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 69527 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 9195 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 9195 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 9195 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 9195 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 69547 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 69547 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 100187 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 100187 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 185891 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 185891 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 77807 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 77807 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 77808 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 77808 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 69525 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 69525 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 69433 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 69433 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 173834 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 173834 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 77803 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 77803 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 69540 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 69540 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 77811 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 77811 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 77763 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 77763 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 69522 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 69522 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 100274 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 100274 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 69537 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 69537 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 77765 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 77765 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 10222 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 10222 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 10222 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 200172 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 200172 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 77769 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 77769 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 113829 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 113829 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 100275 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 100275 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 77806 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 77806 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 77804 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 77804 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 77815 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 77815 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 7973 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 7973 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 7973 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 69543 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 69543 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 7109 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 7109 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 7109 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 7973 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 7973 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 7973 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 10829 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 10829 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 10829 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 10821 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 10821 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 10821 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 7868 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 7868 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 7868 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 7891 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 7891 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 10113 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 10113 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 10113 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 10317 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 10317 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 10317 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 10462 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 10462 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 10462 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 9198 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 9198 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 9198 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 6893 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 6893 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 6893 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 7973 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 7973 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 7973 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 7820 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 7820 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 7820 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 8337 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 8337 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 8337 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 9202 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 9202 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 9202 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 10890 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 10890 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 10890 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 10890 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 10820 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 10820 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 8763 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 8763 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 8763 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 7671 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 7671 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 7000 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 7000 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 7000 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 7000 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 7000 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 7000 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 7368 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 7368 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 7368 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 7368 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 7368 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 7368 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 9201 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 9201 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 9201 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 7836 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 7836 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 7836 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 6883 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 6883 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 6883 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 7874 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 7874 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 10890 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 10890 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 10890 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 10890 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 7765 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 7765 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 7765 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 10043 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 10043 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 10043 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 10043 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 6997 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 6997 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 6997 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 6999 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 6999 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 6999 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 7841 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 7841 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 10888 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 10888 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 7936 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 7936 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 7936 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 7932 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 7932 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 7932 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 7753 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 7753 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 7753 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 7856 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 7856 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 7856 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 8478 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 8478 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 8478 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 7758 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 7758 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 8478 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 8478 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 8478 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 6998 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 6998 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 6998 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 9336 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 9336 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 9336 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 6998 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 6998 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 6998 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 7821 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 7821 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 7821 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 7823 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 7823 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 7823 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 7672 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 7672 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 7672 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 7822 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 7822 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 7822 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 7824 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 7824 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 7824 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 7764 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 7764 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 7764 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 7830 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 7830 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 7830 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 7825 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 7825 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 7825 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 8915 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 8915 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 8915 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 8915 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 6999 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 6999 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 6999 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 6999 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 6999 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 6999 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 7763 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 7763 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 7763 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 8861 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 8861 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 8861 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 8861 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 8231 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 8231 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 8231 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 10821 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 10821 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 10821 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


Get vendors


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 24070 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 24070 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 24454 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 24454 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 211702 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 211702 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 211702 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 24525 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 24525 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 10113 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 10113 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 10113 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 10113 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 10113 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 10113 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 6822 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 6822 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 6822 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 24135 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 24135 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 24177 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 24177 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 24178 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 24178 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 24253 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 24253 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 24596 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 24596 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 108008 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 108008 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 10037 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 10037 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 10037 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 10037 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 10037 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 10037 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 146429 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 146429 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 146429 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 146429 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 24217 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 24217 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 10037 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 10037 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 10037 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 10037 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 10037 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 10037 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 10037 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 10037 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 10037 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 10037 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 10037 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 10037 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 146719 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 146719 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 146719 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 146719 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 6822 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 6822 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 6822 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 6822 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 6822 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 6822 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 10037 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 10037 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 10037 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 10037 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 10037 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 10037 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 23253 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 23253 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 24490 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 24490 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 24216 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 24216 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 127373 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 127373 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 127373 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 23252 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 23252 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 24100 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 24100 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 24564 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 24564 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 108978 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 108978 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 108978 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 108978 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 108978 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 108978 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 6822 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 6822 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 6822 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 24563 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 24563 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 108978 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 108978 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 108978 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 108978 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 108978 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 108978 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 108978 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 108978 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 108978 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 122029 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 122029 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 24069 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 24069 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 24595 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 24595 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 8861 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 8861 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 8861 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 8861 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 10037 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 10037 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 10037 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 10037 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 10037 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 10037 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 10037 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 10037 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 10037 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 10037 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 10037 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 10037 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 23251 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 23251 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 24136 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 24136 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 24491 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 24491 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 153152 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 153152 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 8915 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 8915 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 8915 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 8915 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 69780 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 69780 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 6997 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 6997 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 6997 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 85703 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 85703 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 8464 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 8464 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 8464 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 6999 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 6999 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 6999 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 68884 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 68884 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 107807 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 107807 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 158681 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 158681 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 148849 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 148849 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 210357 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 210357 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 94702 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 94702 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 64256 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 64256 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 148849 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 148849 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 136254 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 136254 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 8915 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 8915 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 8915 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 8915 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 85699 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 85699 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 91929 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 91929 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 91929 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 91929 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 69079 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 69079 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 134598 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 134598 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 209777 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 209777 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 113690 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 113690 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 181246 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 181246 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 181246 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 181246 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 85309 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 85309 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 70285 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 70285 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 210392 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 210392 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 91584 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 91584 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 67054 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 67054 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 68241 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 68241 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 8423 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 8423 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 8423 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 91877 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 91877 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 91877 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 91877 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 91783 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 91783 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 91838 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 91838 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 10043 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 10043 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 10043 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 10043 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 91838 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 91838 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 69761 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 69761 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 210511 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 210511 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 176114 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 176114 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 94512 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 94512 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 6883 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 6883 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 6883 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 91997 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 91997 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 85309 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 85309 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 67290 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 67290 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 91840 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 91840 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 103580 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 103580 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 210348 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 210348 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 127179 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 127179 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 67279 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 67279 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 148506 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 148506 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 183705 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 183705 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 148506 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 148506 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 183705 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 183705 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 109496 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 109496 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 91840 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 91840 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 85699 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 85699 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 172892 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 172892 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 69786 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 69786 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 172892 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 172892 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 8763 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 8763 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 8763 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 158679 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 158679 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 85701 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 85701 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 94511 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 94511 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 67252 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 67252 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 67252 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 67252 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 6998 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 6998 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 6998 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 91867 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 91867 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 8763 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 8763 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 8763 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 210394 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 210394 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 91927 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 91927 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 91927 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 91927 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 67079 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 67079 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 210569 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 210569 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 7973 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 7973 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 7973 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 8763 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 8763 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 8763 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 110368 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 110368 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 10317 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 10317 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 10317 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 10317 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 10317 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 10317 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 10317 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 10317 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 10317 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 144321 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 144321 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 144321 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 144321 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 148689 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 148689 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 89807 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 89807 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 210407 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 210407 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 67291 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 67291 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 209812 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 209812 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 148860 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 148860 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 148860 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 148860 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 67053 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 67053 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 6998 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 6998 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 6998 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 67800 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 67800 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 8915 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 8915 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 8915 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 8915 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 67241 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 67241 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 8464 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 8464 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 8464 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 95257 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 95257 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 91999 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 91999 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 9867 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 9867 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 9867 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 209826 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 209826 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 150927 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 150927 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 150927 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 150927 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 94510 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 94510 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 91842 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 91842 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 173803 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 173803 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 91842 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 91842 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 83404 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 83404 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 68906 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 108861 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 108861 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 210464 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 210464 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 10317 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 10317 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 10317 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 67579 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 67579 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 91773 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 91773 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 91773 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 91773 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 98802 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 98802 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 109010 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 109010 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 85702 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 85702 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 91622 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 91622 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 91622 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 91622 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 150272 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 150272 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 150272 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 150272 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 210418 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 210418 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 83405 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 83405 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 107658 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 107658 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 91999 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 91999 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 69761 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 69761 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 69780 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 69780 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 70315 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 70315 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 85700 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 85700 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 8862 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 8862 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 8862 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 8862 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 8862 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 8862 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 143605 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 143605 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 143605 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 143605 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 91814 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 91814 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 91814 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 91814 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 172922 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 172922 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 91878 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 91878 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 67250 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 67250 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 68906 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 91878 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 91878 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 91908 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 91908 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 91908 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 91908 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 8915 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 8915 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 8915 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 8915 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 67489 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 67489 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 67489 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 67489 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 89808 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 89808 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 108961 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 108961 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 149134 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 149134 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 149134 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 149134 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 172922 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 172922 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 91619 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 91619 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 91868 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 91868 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 67800 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 67800 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 69761 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 69761 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 150017 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 150017 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 150316 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 150316 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 68883 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 68883 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 69170 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 69170 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 85308 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 85308 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 68884 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 68884 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 87006 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 87006 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 134598 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 134598 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 210578 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 210578 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 129727 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 129727 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 10043 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 10043 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 10043 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 10043 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 68241 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 68241 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 85702 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 85702 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 91821 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 91821 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 91821 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 91821 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 89805 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 89805 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 67345 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 67345 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 67241 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 67241 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 10222 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 10222 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 10222 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 10222 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 10222 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 10222 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 10462 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 10462 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 10462 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 10462 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 10462 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 10462 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 68872 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 68872 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 69787 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 69787 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 85703 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 85703 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 129727 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 129727 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 91928 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 91928 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 91928 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 91928 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 210604 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 210604 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 69787 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 69787 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 210523 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 210523 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 91839 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 91839 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 91839 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 91839 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 80733 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 80733 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 136254 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 136254 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 210506 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 210506 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 67241 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 67241 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 67053 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 67053 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 91813 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 91813 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 68883 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 68883 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 69786 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 69786 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 9198 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 9198 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 9198 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 68872 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 68872 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 91935 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 91935 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 69262 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 69262 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 85701 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 85701 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 91935 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 91935 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 91970 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 91970 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 67290 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 67290 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 176114 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 176114 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 127179 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 127179 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 91970 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 91970 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 148813 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 148813 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 148813 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 148813 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 9195 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 9195 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 9195 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 9195 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 91813 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 91813 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 85700 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 85700 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 9307 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 9307 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 9307 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 8763 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 8763 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 8763 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 143955 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 143955 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 143955 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 143955 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 144705 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 144705 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 144705 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 144705 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 7825 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 7825 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 7825 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 95517 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 95517 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 8915 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 8915 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 8915 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 8915 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 204034 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 204034 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 204034 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 204034 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 204034 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 204034 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 7823 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 7823 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 7823 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 95461 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 95461 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 155391 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 155391 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 95462 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 95462 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 8916 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 8916 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 8916 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 8916 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 8916 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 8916 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 8916 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 8916 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 8916 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 8916 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 8916 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 8916 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 7822 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 7822 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 7822 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 91999 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 91999 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 7824 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 7824 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 7824 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 10037 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 10037 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 10037 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 10037 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 10037 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 10037 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 156654 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 156654 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 153167 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 153167 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 174192 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 174192 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 96735 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 96735 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 91908 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 91908 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 202392 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 202392 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 83404 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 83404 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 89807 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 89807 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 203419 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 203419 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 144321 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 144321 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 83405 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 83405 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 155112 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 155112 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 96994 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 96994 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 202412 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 202412 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 128983 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 128983 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 128984 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 128984 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 128980 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 128980 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 128980 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 128980 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 128986 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 128986 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 96995 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 96995 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 8478 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 8478 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 8478 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 91619 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 91619 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 96731 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 96731 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 202335 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 202335 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 89808 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 89808 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 202392 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 202392 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 150272 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 150272 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 89805 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 89805 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 77329 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 77329 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 116490 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 116490 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 96732 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 96732 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 203382 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 203382 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 8478 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 8478 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 8478 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 127373 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 127373 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 127373 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 202086 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 202086 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 79067 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 79067 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 92915 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 92915 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 201964 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 201964 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 10222 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 10222 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 10222 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 128979 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 128979 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 91840 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 91840 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 91997 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 91997 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 83566 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 83566 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 83566 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 83566 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 83566 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 83566 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 83566 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 83566 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 128978 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 128978 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 180627 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 180627 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 86435 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 86435 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 128987 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 128987 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 6998 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 6998 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 6998 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 8423 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 8423 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 8423 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 108514 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 108514 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 204588 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 204588 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 128976 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 128976 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 185363 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 185363 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 91813 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 91813 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 86325 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 86325 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 122029 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 122029 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 91969 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 91969 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 202466 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 202466 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 128975 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 128975 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 173834 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 173834 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 128982 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 128982 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 201555 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 201555 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 135803 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 135803 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 149892 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 149892 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 8122 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 8122 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 8122 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 95420 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 95420 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 91842 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 91842 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 91927 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 91927 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 148860 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 148860 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 92864 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 92864 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 95519 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 95519 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 153230 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 153230 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 153230 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 202691 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 202691 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 136250 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 136250 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 77329 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 77329 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 171238 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 171238 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 171238 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 171238 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 128974 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 128974 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 150316 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 150316 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 202696 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 202696 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 10890 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 10890 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 10890 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 10890 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 10037 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 10037 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 10037 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 10037 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 10037 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 10037 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 10037 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 10037 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 10037 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 10037 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 10037 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 10037 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 8337 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 8337 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 8337 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 10043 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 10043 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 10043 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 10043 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9292 24 Functional -8511 67 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 9292 24 Functional -8511 67 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 9292 24 Functional -8511 67 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 9292 24 Functional -8511 67 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 9292 24 Functional -8511 67 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
15897 9637 0 Functional -354 36 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 9637 0 Functional -354 36 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 9637 0 Functional -354 36 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
128563 10237 33 Functional -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
1666 10237 33 Functional -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
CHEMBL445332 10237 33 Functional -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
DB12327 10237 33 Functional -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
10297 33885 30 Functional -38 43 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
CHEMBL136560 33885 30 Functional -38 43 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
446220 140299 14 Functional -1778 45 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
CHEMBL370805 140299 14 Functional -1778 45 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
1615 174570 24 Functional -26 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
CHEMBL43048 174570 24 Functional -26 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
162265 209053 22 Functional -239 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
4786 209053 22 Functional -239 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
CHEMBL61006 209053 22 Functional -239 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
3337 213146 27 Functional -1513 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 213146 27 Functional -1513 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 213146 27 Functional -1513 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 213146 27 Functional -1513 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 213146 27 Functional -1513 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
11954224 222732 0 Functional -141253 59 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
6971132 222788 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 222951 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 222958 0 Functional -4 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
71290 222958 0 Functional -4 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
None 223095 0 Functional -1 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 3 3 3 -1.4 C(C(C(=O)O)N)S(=O)O None
None 223096 0 Functional -1 39 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 3 3 4 -1.7 C(C(C(=O)O)N)S(=O)(=O)O None
None 223104 0 Functional -13 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 2 1 2 1.2 CC(C(=O)C1=CC=CC=C1)N None
1576 223105 0 Functional -16 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 163 3 1 2 1.5 CC(C(=O)C1=CC=CC=C1)NC None
135398740 224491 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 8423 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 8423 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 8423 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 10136 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 10136 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 9198 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 9198 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 9198 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 9201 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 9201 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 9201 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 7843 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 7843 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 7843 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 7830 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 7830 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 7830 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 7830 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 7830 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 7830 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 10111 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 10111 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 10137 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 10137 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 10888 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 10888 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 8337 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 8337 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 8337 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 8464 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 8464 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 8464 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 7841 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 7841 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 7836 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 7836 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 7836 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 6997 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 6997 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 6997 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 7765 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 7765 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 7765 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 7764 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 7764 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 7764 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 7820 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 7820 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 7820 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 7932 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 7932 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 7932 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 7763 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 7763 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 7763 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 7823 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 7823 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 7823 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 7824 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 7824 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 7824 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 8916 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 8916 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 8916 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 8916 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 10043 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 10043 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 10043 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 10043 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 7758 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 7758 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 7822 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 7822 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 7822 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 7368 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 7368 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 7368 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 9253 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 9253 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 9253 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 9253 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 9253 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 7109 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 7109 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 7109 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 8122 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 8122 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 8122 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 7973 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 7973 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 7973 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 10222 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 10222 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 10222 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 9070 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 9070 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 9070 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 6822 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 6822 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 6822 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 6822 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 6822 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 6822 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 6822 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 6822 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 6822 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 6881 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 6881 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 6881 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 8862 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 8862 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 8862 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 8862 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 8862 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 8862 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 8751 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 8751 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 8751 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 8751 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 8751 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 8751 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 8751 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 8751 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 9095 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 10037 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 10037 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 10037 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 10037 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 10037 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 10037 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 10037 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 10037 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 10037 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 10037 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 10037 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 10037 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 9195 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 9195 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 9195 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 9195 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 9655 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 9655 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 9655 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