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Found 8095 Enz. Inhib. hit(s) with Target = 'Metabotropic glutamate receptor 5'
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
National Institute Of Mental Health

Curated by ChEMBL
LigandPNGBDBM50215552(3-fluoro-5-(2-(2-(fluoromethyl)thiazol-4-yl)ethyny...)
Affinity DataIC50:  0.00100nMAssay Description:Activity at human recombinant mGluR5 in CHO cells assessed as inhibition of quisqualate-stimulated phosphoinositide hydrolysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
National Institute Of Mental Health

Curated by ChEMBL
LigandPNGBDBM50215552(3-fluoro-5-(2-(2-(fluoromethyl)thiazol-4-yl)ethyny...)
Affinity DataIC50:  0.0360nMAssay Description:Displacement of [3H]MPEP from mGluR5 in rat brain membraneMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
National Institute Of Mental Health

Curated by ChEMBL
LigandPNGBDBM50215556(3-(2-(2-(fluoromethyl)thiazol-4-yl)ethynyl)benzoni...)
Affinity DataIC50:  0.0600nMAssay Description:Displacement of [3H]MPEP from mGluR5 in rat brain membraneMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
National Institute Of Mental Health

Curated by ChEMBL
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataIC50:  0.200nMAssay Description:Activity at rat mGlu5 receptor expressed in CHO cells assessed as inhibition of quisqualate-stimulated calcium mobilization by FLIPR assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
National Institute Of Mental Health

Curated by ChEMBL
LigandPNGBDBM50215553(5-(2-(2-fluoromethyl)thiazole-4-yl)ethynyl)pyridin...)
Affinity DataIC50:  0.230nMAssay Description:Displacement of [3H]MPEP from mGluR5 in rat brain membraneMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
H. Lundbeck

US Patent
LigandPNGBDBM141505(US8921370, 126 | US9656975, 126)
Affinity DataIC50:  0.320nMpH: 7.4 T: 2°CAssay Description:The cDNA for rat metabotropic glutamate receptor 5 (rmGluR5) and the cDNA for human metabotropic glutamate receptor 5 (rmGluR5) were generous gifts f...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
National Institute Of Mental Health

Curated by ChEMBL
LigandPNGBDBM50345567(3-(2-(5-methylpyridin-2-yl)ethynyl)-5-fluorobenzon...)
Affinity DataIC50:  0.320nMAssay Description:Antagonist activity at rat mGluR5 expressed in human HEK-293 cells assessed as inhibition of glutamate-induced intracellular calcium mobilizationMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
National Institute Of Mental Health

Curated by ChEMBL
LigandPNGBDBM50345570(3-(2-(pyridin-2-yl)ethynyl)-5-bromonitrobenzene | ...)
Affinity DataIC50:  0.390nMAssay Description:Antagonist activity at rat mGluR5 expressed in human HEK-293 cells assessed as inhibition of glutamate-induced intracellular calcium mobilizationMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
H. Lundbeck

US Patent
LigandPNGBDBM50411769(CHEMBL403390)
Affinity DataIC50:  0.398nMAssay Description:Antagonist activity at human mGluR5 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPRMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
H. Lundbeck

US Patent
LigandPNGBDBM50411838(CHEMBL271276)
Affinity DataIC50:  0.398nMAssay Description:Antagonist activity at human mGluR5 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPRMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
H. Lundbeck

US Patent
LigandPNGBDBM50113479(CHEMBL3603926 | US10246432, Example 22 | US1058411...)
Affinity DataIC50:  0.398nMAssay Description:Negative allosteric modulation at human mGlu5 receptor expressed in HEK293 cells assessed as inhibition of L-quisqualic acid-induced inositol phospha...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
H. Lundbeck

US Patent
LigandPNGBDBM50105833(CHEMBL3597593)
Affinity DataIC50:  0.400nMAssay Description:Negative allosteric modulatory activity at human cloned mGluR5 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced cal...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
National Institute Of Mental Health

Curated by ChEMBL
LigandPNGBDBM50160632(3-(6-Methyl-pyridin-2-ylethynyl)-benzonitrile | 3-...)
Affinity DataIC50:  0.420nMAssay Description:Antagonist activity at rat mGluR5 expressed in HEK293A cells assessed as glutamate-induced calcium flux preincubated for 140 sec before glutamate cha...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
National Institute Of Mental Health

Curated by ChEMBL
LigandPNGBDBM50215555(2-(fluoromethyl)-4-(2-(3-fluorophenyl)ethynylthiaz...)
Affinity DataIC50:  0.480nMAssay Description:Displacement of [3H]MPEP from mGluR5 in rat brain membraneMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
H. Lundbeck

US Patent
LigandPNGBDBM50149801(2-Phenyl-5-(2-methylthiazol-4ylethynyl)pyridine | ...)
Affinity DataIC50:  0.5nMAssay Description:In vitro potency against human recombinant mGlu5 receptor was determined by [Ca2+] flux assay using glutamate as agonistMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
H. Lundbeck

US Patent
LigandPNGBDBM50113476(CHEMBL3603923 | US10246432, Example 17 | US1058411...)
Affinity DataIC50:  0.501nMAssay Description:Inhibition of mGLU5 (unknown origin)More data for this Ligand-Target Pair
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
National Institute Of Mental Health

Curated by ChEMBL
LigandPNGBDBM50215554(2-(fluoromethyl)4-(2-(3-methoxyphenyl)ethynyl)thia...)
Affinity DataIC50:  0.520nMAssay Description:Displacement of [3H]MPEP from mGluR5 in rat brain membraneMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
National Institute Of Mental Health

Curated by ChEMBL
LigandPNGBDBM50345555(3-(2-(2-methylthiazol-4-yl)ethynyl)-5-nitrofluorob...)
Affinity DataIC50:  0.610nMAssay Description:Antagonist activity at rat mGluR5 expressed in human HEK-293 cells assessed as inhibition of glutamate-induced intracellular calcium mobilizationMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
National Institute Of Mental Health

Curated by ChEMBL
LigandPNGBDBM50345560(3-(2-(6-methylpyridin-2-yl)ethynyl)-5-nitrobromobe...)
Affinity DataIC50:  0.630nMAssay Description:Antagonist activity at rat mGluR5 expressed in human HEK-293 cells assessed as inhibition of glutamate-induced intracellular calcium mobilizationMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
H. Lundbeck

US Patent
LigandPNGBDBM50113476(CHEMBL3603923 | US10246432, Example 17 | US1058411...)
Affinity DataIC50:  0.631nMAssay Description:Negative allosteric modulation at human mGlu5 receptor expressed in HEK293 cells assessed as inhibition of L-quisqualic acid-induced inositol phospha...More data for this Ligand-Target Pair
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
H. Lundbeck

US Patent
LigandPNGBDBM50113477(CHEMBL3603924 | US10246432, Example 3 | US10584111...)
Affinity DataIC50:  0.631nMAssay Description:Negative allosteric modulation at human mGlu5 receptor expressed in HEK293 cells assessed as inhibition of L-quisqualic acid-induced inositol phospha...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
National Institute Of Mental Health

Curated by ChEMBL
LigandPNGBDBM50345572(3-(2-(pyridin-2-yl)ethynyl)-5-fluorobenzonitrile |...)
Affinity DataIC50:  0.660nMAssay Description:Antagonist activity at rat mGluR5 expressed in human HEK-293 cells assessed as inhibition of glutamate-induced intracellular calcium mobilizationMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
National Institute Of Mental Health

Curated by ChEMBL
LigandPNGBDBM50345573(3-(2-(pyridin-2-yl)ethynyl)-5-iodobenzonitrile | C...)
Affinity DataIC50:  0.660nMAssay Description:Antagonist activity at rat mGluR5 expressed in human HEK-293 cells assessed as inhibition of glutamate-induced intracellular calcium mobilizationMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
National Institute Of Mental Health

Curated by ChEMBL
LigandPNGBDBM50345574(3-(2-(pyridin-2-yl)ethynyl)-5-nitrofluorobenzene |...)
Affinity DataIC50:  0.660nMAssay Description:Antagonist activity at rat mGluR5 expressed in human HEK-293 cells assessed as inhibition of glutamate-induced intracellular calcium mobilizationMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
National Institute Of Mental Health

Curated by ChEMBL
LigandPNGBDBM50345563(3-(2-(6-methylpyridin-2-yl)ethynyl)-5-iodobenzonit...)
Affinity DataIC50:  0.710nMAssay Description:Antagonist activity at rat mGluR5 expressed in human HEK-293 cells assessed as inhibition of glutamate-induced intracellular calcium mobilizationMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
National Institute Of Mental Health

Curated by ChEMBL
LigandPNGBDBM50220087(2-(3,5-dichlorophenyl)-7-methylpyrido[2,3-d]pyrimi...)
Affinity DataIC50:  0.720nMAssay Description:Antagonistic activity at rat mGluR5 expressed in CHO cells assessed as inhibition of quisqualate stimulated calcium mobilization by FLIPR technologyMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
National Institute Of Mental Health

Curated by ChEMBL
LigandPNGBDBM50345551(3-(2-(2-methylthiazol-4-yl)ethynyl)-5-nitrobromobe...)
Affinity DataIC50:  0.730nMAssay Description:Antagonist activity at rat mGluR5 expressed in human HEK-293 cells assessed as inhibition of glutamate-induced intracellular calcium mobilizationMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
H. Lundbeck

US Patent
LigandPNGBDBM50143544(CHEMBL3759766)
Affinity DataIC50:  0.790nMAssay Description:Antagonist activity at human mGluR5 expressed in CHO cells assessed as inhibition of glutamate-induced effect by aequorin bioluminescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
H. Lundbeck

US Patent
LigandPNGBDBM50411851(CHEMBL257880)
Affinity DataIC50:  0.794nMAssay Description:Antagonist activity at human mGluR5 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPRMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
H. Lundbeck

US Patent
LigandPNGBDBM50105834(CHEMBL3597594)
Affinity DataIC50:  0.800nMAssay Description:Negative allosteric modulatory activity at human cloned mGluR5 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced cal...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
National Institute Of Mental Health

Curated by ChEMBL
LigandPNGBDBM50216746(3-fluoro-5-(2-methylquinolin-7-yl)benzonitrile | C...)
Affinity DataIC50:  0.800nMAssay Description:Activity at rat mGlu5 receptor expressed in CHO cells assessed as inhibition of quisqualate-stimulated calcium mobilization by FLIPR assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
H. Lundbeck

US Patent
LigandPNGBDBM50105834(CHEMBL3597594)
Affinity DataIC50:  0.800nMAssay Description:Negative allosteric modulation of human mGlu5 receptor expressed in CHO-TREx cell membranes assessed as reduction in quisqualate-induced Ca2+ mobiliz...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
H. Lundbeck

US Patent
LigandPNGBDBM50105834(CHEMBL3597594)
Affinity DataIC50:  0.800nMAssay Description:Negative allosteric modulation of human mGlu5 receptor expressed in CHO-TREx cell membranes assessed as reduction in quisqualate-induced Ca2+ mobiliz...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
National Institute Of Mental Health

Curated by ChEMBL
LigandPNGBDBM50258612(3-Fluoro-5-cyano-1-(2-methylthiazol-4-ylethynyl)be...)
Affinity DataIC50:  0.810nMAssay Description:Antagonist activity at rat mGluR5 expressed in HEK293A cells assessed as glutamate-induced calcium flux preincubated for 140 sec before glutamate cha...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
H. Lundbeck

US Patent
LigandPNGBDBM50105831(CHEMBL3597584)
Affinity DataIC50:  0.900nMAssay Description:Negative allosteric modulatory activity at human cloned mGluR5 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced cal...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
H. Lundbeck

US Patent
LigandPNGBDBM50172123(3-Chloro-5-(3-pyridin-2-ylethynyl-cyclohex-2-enylo...)
Affinity DataIC50:  0.900nMAssay Description:In vitro inhibitory concentration against Ca+2 flux mediated by human mGlu5 receptor expressed in Ltk cells using fura-2 dyeMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
H. Lundbeck

US Patent
LigandPNGBDBM50181745(3-[(2-methyl-4-thiazolyl)ethynyl]benzonitrile | CH...)
Affinity DataIC50:  0.940nMAssay Description:Activity in agonist-induced phosphoinositide hydrolysis in CHO cells expressing mGluR5aMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
H. Lundbeck

US Patent
LigandPNGBDBM136108(US8853203, 123b | US9650377, Example 123b)
Affinity DataIC50:  1nMAssay Description:Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calc...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
H. Lundbeck

US Patent
LigandPNGBDBM136115(US8853203, 128 | US9650377, Example 128)
Affinity DataIC50:  1nMAssay Description:Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calc...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
H. Lundbeck

US Patent
LigandPNGBDBM136115(US8853203, 128 | US9650377, Example 128)
Affinity DataIC50:  1nMAssay Description:Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induce...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
H. Lundbeck

US Patent
LigandPNGBDBM136108(US8853203, 123b | US9650377, Example 123b)
Affinity DataIC50:  1nMAssay Description:Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induce...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
H. Lundbeck

US Patent
LigandPNGBDBM136048(US8853203, 92 | US9650377, Example 92)
Affinity DataIC50: <1nMAssay Description:Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induce...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
H. Lundbeck

US Patent
LigandPNGBDBM50366854(CHEMBL1169452)
Affinity DataIC50:  1nMAssay Description:In vitro functional potency using an automated assay employing LtK-cells stably expressing human recombinant mGlu5 receptor by measuring changes in c...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
H. Lundbeck

US Patent
LigandPNGBDBM136048(US8853203, 92 | US9650377, Example 92)
Affinity DataIC50: <1nMAssay Description:Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calc...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
National Institute Of Mental Health

Curated by ChEMBL
LigandPNGBDBM50345568(3-(2-(5-methylpyridin-2-yl)ethynyl)-5-bromobenzoni...)
Affinity DataIC50:  1.02nMAssay Description:Antagonist activity at rat mGluR5 expressed in human HEK-293 cells assessed as inhibition of glutamate-induced intracellular calcium mobilizationMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
National Institute Of Mental Health

Curated by ChEMBL
LigandPNGBDBM50345571(3-(2-(pyridin-2-yl)ethynyl)-5-chlorobenzonitrile |...)
Affinity DataIC50:  1.03nMAssay Description:Antagonist activity at rat mGluR5 expressed in human HEK-293 cells assessed as inhibition of glutamate-induced intracellular calcium mobilizationMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
National Institute Of Mental Health

Curated by ChEMBL
LigandPNGBDBM50345554(3-(2-(2-methylthiazol-4-yl)ethynyl)-5-iodobenzonit...)
Affinity DataIC50:  1.05nMAssay Description:Antagonist activity at rat mGluR5 expressed in human HEK-293 cells assessed as inhibition of glutamate-induced intracellular calcium mobilizationMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
National Institute Of Mental Health

Curated by ChEMBL
LigandPNGBDBM50345553(3-(2-(2-methylthiazol-4-yl)ethynyl)-5-bromobenzoni...)
Affinity DataIC50:  1.06nMAssay Description:Antagonist activity at rat mGluR5 expressed in human HEK-293 cells assessed as inhibition of glutamate-induced intracellular calcium mobilizationMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
National Institute Of Mental Health

Curated by ChEMBL
LigandPNGBDBM50240888(CHEMBL4094256)
Affinity DataIC50:  1.10nMAssay Description:Negative allosteric modulation of rat mGlu5 expressed in HEK293 cells assessed as inhibition of glutamate-induced intracellular calcium accumulation ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
H. Lundbeck

US Patent
LigandPNGBDBM50431696(CHEMBL2349534)
Affinity DataIC50:  1.10nMAssay Description:Negative allosteric modulation of human mGluR5 expressed in HEK293 cells assessed as calcium mobilization by FLIPR assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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