Ligand source activities (1 row/activity)
| Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
| 1392 | 73 | None | 32 | Rat | Functional | pEC50 | = | 4 | 4.0 | -323 | 4 | Tested for the agonistic activity against Metabotropic glutamate receptor 1Tested for the agonistic activity against Metabotropic glutamate receptor 1 |
ChEMBL | 174 | 2 | 4 | 4 | -1.8 | OC(=O)[C@@H]1NC[C@@](C1)(N)C(=O)O | 10.1016/S0960-894X(97)00068-1 | ||
| 5310984 | 73 | None | 32 | Rat | Functional | pEC50 | = | 4 | 4.0 | -323 | 4 | Tested for the agonistic activity against Metabotropic glutamate receptor 1Tested for the agonistic activity against Metabotropic glutamate receptor 1 |
ChEMBL | 174 | 2 | 4 | 4 | -1.8 | OC(=O)[C@@H]1NC[C@@](C1)(N)C(=O)O | 10.1016/S0960-894X(97)00068-1 | ||
| CHEMBL40086 | 73 | None | 32 | Rat | Functional | pEC50 | = | 4 | 4.0 | -323 | 4 | Tested for the agonistic activity against Metabotropic glutamate receptor 1Tested for the agonistic activity against Metabotropic glutamate receptor 1 |
ChEMBL | 174 | 2 | 4 | 4 | -1.8 | OC(=O)[C@@H]1NC[C@@](C1)(N)C(=O)O | 10.1016/S0960-894X(97)00068-1 | ||
| 44573737 | 192938 | None | 0 | Rat | Functional | pEC50 | = | 7.0 | 7.0 | - | 1 | Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology |
ChEMBL | 378 | 2 | 1 | 4 | 4.7 | O=C(Nc1nc(C(F)(F)F)co1)C1c2ccccc2Oc2c(F)cccc21 | 10.1016/j.bmcl.2009.01.108 | ||
| CHEMBL522161 | 192938 | None | 0 | Rat | Functional | pEC50 | = | 7.0 | 7.0 | - | 1 | Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology |
ChEMBL | 378 | 2 | 1 | 4 | 4.7 | O=C(Nc1nc(C(F)(F)F)co1)C1c2ccccc2Oc2c(F)cccc21 | 10.1016/j.bmcl.2009.01.108 | ||
| 1310 | 2315 | None | 61 | Human | Functional | pEC50 | = | 6.0 | 6.0 | -741 | 17 | Effect of compound on Metabotropic glutamate receptor 1 expressed in HEK 293 cells was determined by measuring IP production relative to glutamateEffect of compound on Metabotropic glutamate receptor 1 expressed in HEK 293 cells was determined by measuring IP production relative to glutamate |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | OC(=O)CC[C@@H](C(=O)O)N | 10.1016/s0960-894x(99)00641-1 | ||
| 1369 | 2315 | None | 61 | Human | Functional | pEC50 | = | 6.0 | 6.0 | -741 | 17 | Effect of compound on Metabotropic glutamate receptor 1 expressed in HEK 293 cells was determined by measuring IP production relative to glutamateEffect of compound on Metabotropic glutamate receptor 1 expressed in HEK 293 cells was determined by measuring IP production relative to glutamate |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | OC(=O)CC[C@@H](C(=O)O)N | 10.1016/s0960-894x(99)00641-1 | ||
| 33032 | 2315 | None | 61 | Human | Functional | pEC50 | = | 6.0 | 6.0 | -741 | 17 | Effect of compound on Metabotropic glutamate receptor 1 expressed in HEK 293 cells was determined by measuring IP production relative to glutamateEffect of compound on Metabotropic glutamate receptor 1 expressed in HEK 293 cells was determined by measuring IP production relative to glutamate |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | OC(=O)CC[C@@H](C(=O)O)N | 10.1016/s0960-894x(99)00641-1 | ||
| 44272391 | 2315 | None | 61 | Human | Functional | pEC50 | = | 6.0 | 6.0 | -741 | 17 | Effect of compound on Metabotropic glutamate receptor 1 expressed in HEK 293 cells was determined by measuring IP production relative to glutamateEffect of compound on Metabotropic glutamate receptor 1 expressed in HEK 293 cells was determined by measuring IP production relative to glutamate |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | OC(=O)CC[C@@H](C(=O)O)N | 10.1016/s0960-894x(99)00641-1 | ||
| 88747398 | 2315 | None | 61 | Human | Functional | pEC50 | = | 6.0 | 6.0 | -741 | 17 | Effect of compound on Metabotropic glutamate receptor 1 expressed in HEK 293 cells was determined by measuring IP production relative to glutamateEffect of compound on Metabotropic glutamate receptor 1 expressed in HEK 293 cells was determined by measuring IP production relative to glutamate |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | OC(=O)CC[C@@H](C(=O)O)N | 10.1016/s0960-894x(99)00641-1 | ||
| CHEMBL575060 | 2315 | None | 61 | Human | Functional | pEC50 | = | 6.0 | 6.0 | -741 | 17 | Effect of compound on Metabotropic glutamate receptor 1 expressed in HEK 293 cells was determined by measuring IP production relative to glutamateEffect of compound on Metabotropic glutamate receptor 1 expressed in HEK 293 cells was determined by measuring IP production relative to glutamate |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | OC(=O)CC[C@@H](C(=O)O)N | 10.1016/s0960-894x(99)00641-1 | ||
| DB00142 | 2315 | None | 61 | Human | Functional | pEC50 | = | 6.0 | 6.0 | -741 | 17 | Effect of compound on Metabotropic glutamate receptor 1 expressed in HEK 293 cells was determined by measuring IP production relative to glutamateEffect of compound on Metabotropic glutamate receptor 1 expressed in HEK 293 cells was determined by measuring IP production relative to glutamate |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | OC(=O)CC[C@@H](C(=O)O)N | 10.1016/s0960-894x(99)00641-1 | ||
| 122196105 | 124307 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | 22 | 2 | Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay |
ChEMBL | 448 | 3 | 1 | 4 | 5.3 | Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(C(F)(F)F)c1 | 10.1016/j.bmcl.2015.10.013 | ||
| CHEMBL3634428 | 124307 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | 22 | 2 | Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay |
ChEMBL | 448 | 3 | 1 | 4 | 5.3 | Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(C(F)(F)F)c1 | 10.1016/j.bmcl.2015.10.013 | ||
| 127032507 | 139111 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min |
ChEMBL | 380 | 3 | 1 | 3 | 5.0 | Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(C)cccc3C2=O)c(Cl)c1 | 10.1016/j.bmcl.2016.03.031 | ||
| CHEMBL3785852 | 139111 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min |
ChEMBL | 380 | 3 | 1 | 3 | 5.0 | Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(C)cccc3C2=O)c(Cl)c1 | 10.1016/j.bmcl.2016.03.031 | ||
| 127032507 | 139111 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min |
ChEMBL | 380 | 3 | 1 | 3 | 5.0 | Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(C)cccc3C2=O)c(Cl)c1 | 10.1016/j.bmcl.2016.03.031 | ||
| CHEMBL3785852 | 139111 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min |
ChEMBL | 380 | 3 | 1 | 3 | 5.0 | Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(C)cccc3C2=O)c(Cl)c1 | 10.1016/j.bmcl.2016.03.031 | ||
| 127026165 | 137782 | None | 4 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization |
ChEMBL | 378 | 3 | 1 | 4 | 4.1 | Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3occc3C)c(F)c1)C2=O | 10.1016/j.bmcl.2015.12.104 | ||
| CHEMBL3758746 | 137782 | None | 4 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization |
ChEMBL | 378 | 3 | 1 | 4 | 4.1 | Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3occc3C)c(F)c1)C2=O | 10.1016/j.bmcl.2015.12.104 | ||
| 192790 | 71913 | None | 26 | Rat | Functional | pEC50 | = | 5.0 | 5.0 | 4 | 2 | Agonist activity in rat at mGlu1a receptor expressed in HEK293 cellsAgonist activity in rat at mGlu1a receptor expressed in HEK293 cells |
ChEMBL | 163 | 4 | 4 | 4 | -1.8 | N[C@@H](C[C@H](O)C(=O)O)C(=O)O | 10.1016/s0960-894x(01)00158-5 | ||
| 44286641 | 71913 | None | 26 | Rat | Functional | pEC50 | = | 5.0 | 5.0 | 4 | 2 | Agonist activity in rat at mGlu1a receptor expressed in HEK293 cellsAgonist activity in rat at mGlu1a receptor expressed in HEK293 cells |
ChEMBL | 163 | 4 | 4 | 4 | -1.8 | N[C@@H](C[C@H](O)C(=O)O)C(=O)O | 10.1016/s0960-894x(01)00158-5 | ||
| CHEMBL197110 | 71913 | None | 26 | Rat | Functional | pEC50 | = | 5.0 | 5.0 | 4 | 2 | Agonist activity in rat at mGlu1a receptor expressed in HEK293 cellsAgonist activity in rat at mGlu1a receptor expressed in HEK293 cells |
ChEMBL | 163 | 4 | 4 | 4 | -1.8 | N[C@@H](C[C@H](O)C(=O)O)C(=O)O | 10.1016/s0960-894x(01)00158-5 | ||
| 122193176 | 123998 | None | 0 | Rat | Functional | pEC50 | = | 7.0 | 7.0 | -1 | 3 | Positive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay |
ChEMBL | 414 | 3 | 1 | 4 | 4.9 | Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1 | 10.1021/acs.jmedchem.5b00727 | ||
| CHEMBL3628112 | 123998 | None | 0 | Rat | Functional | pEC50 | = | 7.0 | 7.0 | -1 | 3 | Positive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay |
ChEMBL | 414 | 3 | 1 | 4 | 4.9 | Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1 | 10.1021/acs.jmedchem.5b00727 | ||
| 122193179 | 124001 | None | 0 | Rat | Functional | pEC50 | = | 7.0 | 7.0 | -1 | 2 | Positive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay |
ChEMBL | 381 | 3 | 1 | 5 | 3.7 | Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccncc3C2=O)c(Cl)c1 | 10.1021/acs.jmedchem.5b00727 | ||
| CHEMBL3628115 | 124001 | None | 0 | Rat | Functional | pEC50 | = | 7.0 | 7.0 | -1 | 2 | Positive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay |
ChEMBL | 381 | 3 | 1 | 5 | 3.7 | Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccncc3C2=O)c(Cl)c1 | 10.1021/acs.jmedchem.5b00727 | ||
| 122193176 | 123998 | None | 0 | Rat | Functional | pEC50 | = | 7.0 | 7.0 | -1 | 3 | Positive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay |
ChEMBL | 414 | 3 | 1 | 4 | 4.9 | Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1 | 10.1021/acs.jmedchem.5b00727 | ||
| CHEMBL3628112 | 123998 | None | 0 | Rat | Functional | pEC50 | = | 7.0 | 7.0 | -1 | 3 | Positive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay |
ChEMBL | 414 | 3 | 1 | 4 | 4.9 | Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1 | 10.1021/acs.jmedchem.5b00727 | ||
| 122193179 | 124001 | None | 0 | Rat | Functional | pEC50 | = | 7.0 | 7.0 | -1 | 2 | Positive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay |
ChEMBL | 381 | 3 | 1 | 5 | 3.7 | Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccncc3C2=O)c(Cl)c1 | 10.1021/acs.jmedchem.5b00727 | ||
| CHEMBL3628115 | 124001 | None | 0 | Rat | Functional | pEC50 | = | 7.0 | 7.0 | -1 | 2 | Positive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay |
ChEMBL | 381 | 3 | 1 | 5 | 3.7 | Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccncc3C2=O)c(Cl)c1 | 10.1021/acs.jmedchem.5b00727 | ||
| 127030066 | 139126 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min |
ChEMBL | 434 | 3 | 1 | 3 | 5.7 | Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(cccc3C(F)(F)F)C2=O)c(Cl)c1 | 10.1016/j.bmcl.2016.03.031 | ||
| CHEMBL3785990 | 139126 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min |
ChEMBL | 434 | 3 | 1 | 3 | 5.7 | Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(cccc3C(F)(F)F)C2=O)c(Cl)c1 | 10.1016/j.bmcl.2016.03.031 | ||
| 127026165 | 137782 | None | 4 | Human | Functional | pEC50 | = | 4.9 | 4.9 | - | 1 | Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization |
ChEMBL | 378 | 3 | 1 | 4 | 4.1 | Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3occc3C)c(F)c1)C2=O | 10.1016/j.bmcl.2015.12.104 | ||
| CHEMBL3758746 | 137782 | None | 4 | Human | Functional | pEC50 | = | 4.9 | 4.9 | - | 1 | Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization |
ChEMBL | 378 | 3 | 1 | 4 | 4.1 | Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3occc3C)c(F)c1)C2=O | 10.1016/j.bmcl.2015.12.104 | ||
| 127030066 | 139126 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min |
ChEMBL | 434 | 3 | 1 | 3 | 5.7 | Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(cccc3C(F)(F)F)C2=O)c(Cl)c1 | 10.1016/j.bmcl.2016.03.031 | ||
| CHEMBL3785990 | 139126 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min |
ChEMBL | 434 | 3 | 1 | 3 | 5.7 | Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(cccc3C(F)(F)F)C2=O)c(Cl)c1 | 10.1016/j.bmcl.2016.03.031 | ||
| 122196123 | 124324 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min |
ChEMBL | 364 | 3 | 1 | 4 | 3.8 | Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)cc1F | 10.1016/j.bmcl.2016.03.031 | ||
| CHEMBL3634445 | 124324 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min |
ChEMBL | 364 | 3 | 1 | 4 | 3.8 | Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)cc1F | 10.1016/j.bmcl.2016.03.031 | ||
| 122196103 | 124305 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | 53 | 2 | Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay |
ChEMBL | 414 | 3 | 1 | 4 | 4.7 | Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(C(F)(F)F)c1 | 10.1016/j.bmcl.2015.10.013 | ||
| CHEMBL3634426 | 124305 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | 53 | 2 | Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay |
ChEMBL | 414 | 3 | 1 | 4 | 4.7 | Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(C(F)(F)F)c1 | 10.1016/j.bmcl.2015.10.013 | ||
| 127029303 | 137879 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization |
ChEMBL | 380 | 3 | 2 | 4 | 3.4 | Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1 | 10.1016/j.bmcl.2015.12.104 | ||
| CHEMBL3759563 | 137879 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization |
ChEMBL | 380 | 3 | 2 | 4 | 3.4 | Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1 | 10.1016/j.bmcl.2015.12.104 | ||
| 44573779 | 187743 | None | 0 | Rat | Functional | pEC50 | = | 6.9 | 6.9 | - | 1 | Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay |
ChEMBL | 328 | 2 | 1 | 4 | 3.8 | O=C(Nc1ncco1)C1c2cc(F)ccc2Oc2ccc(F)cc21 | 10.1016/j.bmcl.2009.01.108 | ||
| CHEMBL494961 | 187743 | None | 0 | Rat | Functional | pEC50 | = | 6.9 | 6.9 | - | 1 | Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay |
ChEMBL | 328 | 2 | 1 | 4 | 3.8 | O=C(Nc1ncco1)C1c2cc(F)ccc2Oc2ccc(F)cc21 | 10.1016/j.bmcl.2009.01.108 | ||
| 127029303 | 137879 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization |
ChEMBL | 380 | 3 | 2 | 4 | 3.4 | Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1 | 10.1016/j.bmcl.2015.12.104 | ||
| CHEMBL3759563 | 137879 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization |
ChEMBL | 380 | 3 | 2 | 4 | 3.4 | Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1 | 10.1016/j.bmcl.2015.12.104 | ||
| 127033422 | 139177 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min |
ChEMBL | 384 | 3 | 1 | 3 | 4.8 | Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(Cl)cccc3C2=O)cc1F | 10.1016/j.bmcl.2016.03.031 | ||
| CHEMBL3786552 | 139177 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min |
ChEMBL | 384 | 3 | 1 | 3 | 4.8 | Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(Cl)cccc3C2=O)cc1F | 10.1016/j.bmcl.2016.03.031 | ||
| 127033422 | 139177 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min |
ChEMBL | 384 | 3 | 1 | 3 | 4.8 | Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(Cl)cccc3C2=O)cc1F | 10.1016/j.bmcl.2016.03.031 | ||
Showing 1 to 50 of 2,895 entries
| Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
| 52942855 | 17305 | None | 0 | Human | Binding | pEC50 | = | 6 | 6.0 | - | 0 | 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 | 17305 | None | 0 | Human | Binding | pEC50 | = | 6 | 6.0 | - | 0 | 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 | 17689 | None | 0 | Human | Binding | pEC50 | = | 6 | 6.0 | - | 0 | 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 | 17689 | None | 0 | Human | Binding | pEC50 | = | 6 | 6.0 | - | 0 | Positive modulation of GluR1Positive modulation of GluR1 |
ChEMBL | 427 | 4 | 3 | 6 | 2.2 | NC(=O)c1c(NC(=O)Cn2nc(C(F)(F)F)c3c2CCNC3)sc2c1CCCC2 | 10.1016/j.bmcl.2010.08.063 | ||
| 1310 | 2315 | None | 61 | Rat | Binding | pEC50 | = | 5 | 5.0 | -4 | 18 | Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 1Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 1 |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | OC(=O)CC[C@@H](C(=O)O)N | 10.1021/jm020122x | ||
| 1369 | 2315 | None | 61 | Rat | Binding | pEC50 | = | 5 | 5.0 | -4 | 18 | Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 1Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 1 |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | OC(=O)CC[C@@H](C(=O)O)N | 10.1021/jm020122x | ||
| 33032 | 2315 | None | 61 | Rat | Binding | pEC50 | = | 5 | 5.0 | -4 | 18 | Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 1Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 1 |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | OC(=O)CC[C@@H](C(=O)O)N | 10.1021/jm020122x | ||
| 44272391 | 2315 | None | 61 | Rat | Binding | pEC50 | = | 5 | 5.0 | -4 | 18 | Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 1Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 1 |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | OC(=O)CC[C@@H](C(=O)O)N | 10.1021/jm020122x | ||
| 88747398 | 2315 | None | 61 | Rat | Binding | pEC50 | = | 5 | 5.0 | -4 | 18 | Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 1Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 1 |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | OC(=O)CC[C@@H](C(=O)O)N | 10.1021/jm020122x | ||
| CHEMBL575060 | 2315 | None | 61 | Rat | Binding | pEC50 | = | 5 | 5.0 | -4 | 18 | Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 1Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 1 |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | OC(=O)CC[C@@H](C(=O)O)N | 10.1021/jm020122x | ||
| DB00142 | 2315 | None | 61 | Rat | Binding | pEC50 | = | 5 | 5.0 | -4 | 18 | 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 | 207381 | None | 56 | Rat | Binding | pEC50 | = | 5 | 5.0 | - | 5 | 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 | 207381 | None | 56 | Rat | Binding | pEC50 | = | 5 | 5.0 | - | 5 | 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 | 207381 | None | 56 | Rat | Binding | pEC50 | = | 5 | 5.0 | - | 5 | Effect on Metabotropic glutamate receptor 1Effect on Metabotropic glutamate receptor 1 |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | N[C@H](CCC(=O)O)C(=O)O | 10.1021/jm9703597 | ||
| 1310 | 2315 | None | 61 | Rat | Binding | pEC50 | = | 4.9 | 4.9 | -4 | 18 | Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | OC(=O)CC[C@@H](C(=O)O)N | 10.1021/jm00009a001 | ||
| 1369 | 2315 | None | 61 | Rat | Binding | pEC50 | = | 4.9 | 4.9 | -4 | 18 | Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | OC(=O)CC[C@@H](C(=O)O)N | 10.1021/jm00009a001 | ||
| 33032 | 2315 | None | 61 | Rat | Binding | pEC50 | = | 4.9 | 4.9 | -4 | 18 | Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | OC(=O)CC[C@@H](C(=O)O)N | 10.1021/jm00009a001 | ||
| 44272391 | 2315 | None | 61 | Rat | Binding | pEC50 | = | 4.9 | 4.9 | -4 | 18 | Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | OC(=O)CC[C@@H](C(=O)O)N | 10.1021/jm00009a001 | ||
| 88747398 | 2315 | None | 61 | Rat | Binding | pEC50 | = | 4.9 | 4.9 | -4 | 18 | Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | OC(=O)CC[C@@H](C(=O)O)N | 10.1021/jm00009a001 | ||
| CHEMBL575060 | 2315 | None | 61 | Rat | Binding | pEC50 | = | 4.9 | 4.9 | -4 | 18 | Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | OC(=O)CC[C@@H](C(=O)O)N | 10.1021/jm00009a001 | ||
| DB00142 | 2315 | None | 61 | Rat | Binding | pEC50 | = | 4.9 | 4.9 | -4 | 18 | 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 | 17760 | None | 0 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | 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 | 17760 | None | 0 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | Positive modulation of GluR1Positive modulation of GluR1 |
ChEMBL | 415 | 6 | 3 | 6 | 2.3 | CNCc1cn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(F)(F)F | 10.1016/j.bmcl.2010.08.063 | ||
| 1310 | 2315 | None | 61 | Rat | Binding | pEC50 | = | 4.9 | 4.9 | -4 | 18 | Concentration for half maximal activation of metabotropic glutamate mGluR1c in ratConcentration for half maximal activation of metabotropic glutamate mGluR1c in rat |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | OC(=O)CC[C@@H](C(=O)O)N | 10.1021/jm00009a001 | ||
| 1369 | 2315 | None | 61 | Rat | Binding | pEC50 | = | 4.9 | 4.9 | -4 | 18 | Concentration for half maximal activation of metabotropic glutamate mGluR1c in ratConcentration for half maximal activation of metabotropic glutamate mGluR1c in rat |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | OC(=O)CC[C@@H](C(=O)O)N | 10.1021/jm00009a001 | ||
| 33032 | 2315 | None | 61 | Rat | Binding | pEC50 | = | 4.9 | 4.9 | -4 | 18 | Concentration for half maximal activation of metabotropic glutamate mGluR1c in ratConcentration for half maximal activation of metabotropic glutamate mGluR1c in rat |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | OC(=O)CC[C@@H](C(=O)O)N | 10.1021/jm00009a001 | ||
| 44272391 | 2315 | None | 61 | Rat | Binding | pEC50 | = | 4.9 | 4.9 | -4 | 18 | Concentration for half maximal activation of metabotropic glutamate mGluR1c in ratConcentration for half maximal activation of metabotropic glutamate mGluR1c in rat |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | OC(=O)CC[C@@H](C(=O)O)N | 10.1021/jm00009a001 | ||
| 88747398 | 2315 | None | 61 | Rat | Binding | pEC50 | = | 4.9 | 4.9 | -4 | 18 | Concentration for half maximal activation of metabotropic glutamate mGluR1c in ratConcentration for half maximal activation of metabotropic glutamate mGluR1c in rat |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | OC(=O)CC[C@@H](C(=O)O)N | 10.1021/jm00009a001 | ||
| CHEMBL575060 | 2315 | None | 61 | Rat | Binding | pEC50 | = | 4.9 | 4.9 | -4 | 18 | Concentration for half maximal activation of metabotropic glutamate mGluR1c in ratConcentration for half maximal activation of metabotropic glutamate mGluR1c in rat |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | OC(=O)CC[C@@H](C(=O)O)N | 10.1021/jm00009a001 | ||
| DB00142 | 2315 | None | 61 | Rat | Binding | pEC50 | = | 4.9 | 4.9 | -4 | 18 | Concentration for half maximal activation of metabotropic glutamate mGluR1c in ratConcentration for half maximal activation of metabotropic glutamate mGluR1c in rat |
ChEMBL | 147 | 4 | 3 | 3 | -0.7 | OC(=O)CC[C@@H](C(=O)O)N | 10.1021/jm00009a001 | ||
| 10338547 | 3340 | None | 29 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | Positive allosteric modulation of human mGlu1 receptor assessed as glutamate pEC50 at 10 uM (Rvb = 6.007 +/- 0.076 No_unit)Positive allosteric modulation of human mGlu1 receptor assessed as glutamate pEC50 at 10 uM (Rvb = 6.007 +/- 0.076 No_unit) |
ChEMBL | 360 | 2 | 1 | 4 | 4.6 | O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F | 10.1016/j.bmcl.2016.03.044 | ||
| 6204 | 3340 | None | 29 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | Positive allosteric modulation of human mGlu1 receptor assessed as glutamate pEC50 at 10 uM (Rvb = 6.007 +/- 0.076 No_unit)Positive allosteric modulation of human mGlu1 receptor assessed as glutamate pEC50 at 10 uM (Rvb = 6.007 +/- 0.076 No_unit) |
ChEMBL | 360 | 2 | 1 | 4 | 4.6 | O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F | 10.1016/j.bmcl.2016.03.044 | ||
| CHEMBL521982 | 3340 | None | 29 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | Positive allosteric modulation of human mGlu1 receptor assessed as glutamate pEC50 at 10 uM (Rvb = 6.007 +/- 0.076 No_unit)Positive allosteric modulation of human mGlu1 receptor assessed as glutamate pEC50 at 10 uM (Rvb = 6.007 +/- 0.076 No_unit) |
ChEMBL | 360 | 2 | 1 | 4 | 4.6 | O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F | 10.1016/j.bmcl.2016.03.044 | ||
| 10338547 | 3340 | None | 29 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | Positive allosteric modulation of human mGlu1 receptor assessed as glutamate EC50 at 10 uM (Rvb = 983.4 nM)Positive allosteric modulation of human mGlu1 receptor assessed as glutamate EC50 at 10 uM (Rvb = 983.4 nM) |
ChEMBL | 360 | 2 | 1 | 4 | 4.6 | O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F | 10.1016/j.bmcl.2016.03.044 | ||
| 6204 | 3340 | None | 29 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | Positive allosteric modulation of human mGlu1 receptor assessed as glutamate EC50 at 10 uM (Rvb = 983.4 nM)Positive allosteric modulation of human mGlu1 receptor assessed as glutamate EC50 at 10 uM (Rvb = 983.4 nM) |
ChEMBL | 360 | 2 | 1 | 4 | 4.6 | O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F | 10.1016/j.bmcl.2016.03.044 | ||
| CHEMBL521982 | 3340 | None | 29 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | Positive allosteric modulation of human mGlu1 receptor assessed as glutamate EC50 at 10 uM (Rvb = 983.4 nM)Positive allosteric modulation of human mGlu1 receptor assessed as glutamate EC50 at 10 uM (Rvb = 983.4 nM) |
ChEMBL | 360 | 2 | 1 | 4 | 4.6 | O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F | 10.1016/j.bmcl.2016.03.044 | ||
| 104766 | 33 | None | 30 | Human | Binding | pEC50 | = | 4.8 | 4.8 | -26 | 11 | Compound was tested for the inhibition of Metabotropic glutamate receptor 1Compound was tested for the inhibition of Metabotropic glutamate receptor 1 |
ChEMBL | 173 | 2 | 3 | 3 | -0.3 | OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O | 10.1021/jm970719q | ||
| 1365 | 33 | None | 30 | Human | Binding | pEC50 | = | 4.8 | 4.8 | -26 | 11 | Compound was tested for the inhibition of Metabotropic glutamate receptor 1Compound was tested for the inhibition of Metabotropic glutamate receptor 1 |
ChEMBL | 173 | 2 | 3 | 3 | -0.3 | OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O | 10.1021/jm970719q | ||
| CHEMBL34453 | 33 | None | 30 | Human | Binding | pEC50 | = | 4.8 | 4.8 | -26 | 11 | 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 | 17370 | None | 0 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 0 | 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 | 17370 | None | 0 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 0 | 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 | 17412 | None | 0 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 0 | 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 | 17412 | None | 0 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 0 | 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 | 17413 | None | 0 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 0 | 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 | 17413 | None | 0 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 0 | 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 | 17488 | None | 0 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 0 | 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 | 17488 | None | 0 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 0 | 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 | 17831 | None | 0 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 0 | 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 | 17831 | None | 0 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 0 | Positive modulation of GluR1Positive modulation of GluR1 |
ChEMBL | 459 | 9 | 3 | 7 | 2.3 | COCCNCc1cn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(F)(F)F | 10.1016/j.bmcl.2010.08.063 | ||
| 1310 | 2315 | None | 61 | Human | Binding | pEC50 | = | 5.8 | 5.8 | -1 | 18 | 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 | ||
Showing 1 to 50 of 1,144 entries