Compile Data Set for Download or QSAR
maximum 50k data
Found 21 of ic50 for monomerid = 50122758
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50122758(2-methyl-4-(pyridin-3-ylethynyl)thiazole | 3-(2-(2...)
Affinity DataIC50:  5nMAssay 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(Rattus norvegicus (Rat))
Institute For Neurodegenerative Disorders

Curated by ChEMBL
LigandPNGBDBM50122758(2-methyl-4-(pyridin-3-ylethynyl)thiazole | 3-(2-(2...)
Affinity DataIC50:  5nMAssay 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))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50122758(2-methyl-4-(pyridin-3-ylethynyl)thiazole | 3-(2-(2...)
Affinity DataIC50:  5nMAssay Description:Tested in vitro against human recombinant Metabotropic glutamate receptor 5 stably expressed in LtK cells by [Ca2+] flux assay using glutamate as ant...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50122758(2-methyl-4-(pyridin-3-ylethynyl)thiazole | 3-(2-(2...)
Affinity DataIC50:  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))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50122758(2-methyl-4-(pyridin-3-ylethynyl)thiazole | 3-(2-(2...)
Affinity DataIC50:  5nMAssay Description:Inhibitory concentration against human recombinant metabotropic glutamate receptor 5 (mGlu5) in Ltk cells determined using fluorescence detection met...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50122758(2-methyl-4-(pyridin-3-ylethynyl)thiazole | 3-(2-(2...)
Affinity DataIC50:  12nMAssay 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
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
Institute For Neurodegenerative Disorders

Curated by ChEMBL
LigandPNGBDBM50122758(2-methyl-4-(pyridin-3-ylethynyl)thiazole | 3-(2-(2...)
Affinity DataIC50:  14nMAssay 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))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50122758(2-methyl-4-(pyridin-3-ylethynyl)thiazole | 3-(2-(2...)
Affinity DataIC50:  47nMAssay 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))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50122758(2-methyl-4-(pyridin-3-ylethynyl)thiazole | 3-(2-(2...)
Affinity DataIC50:  47nMAssay 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))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50122758(2-methyl-4-(pyridin-3-ylethynyl)thiazole | 3-(2-(2...)
Affinity DataIC50:  47nMAssay 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))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50122758(2-methyl-4-(pyridin-3-ylethynyl)thiazole | 3-(2-(2...)
Affinity DataIC50:  77nMAssay Description:Activity at human mGluR5 assessed as effect on glutamate-induced calcium ion mobilization by FLIPRMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
Institute For Neurodegenerative Disorders

Curated by ChEMBL
LigandPNGBDBM50122758(2-methyl-4-(pyridin-3-ylethynyl)thiazole | 3-(2-(2...)
Affinity DataIC50:  110nMAssay Description:Inverse agonist activity at rat mGluR5 expressed in HEK293A cells coexpressing Gqalpha assessed as inhibition of quisqualic-induced D-myo-inositol 1 ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50122758(2-methyl-4-(pyridin-3-ylethynyl)thiazole | 3-(2-(2...)
Affinity DataIC50:  462nMAssay 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))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50122758(2-methyl-4-(pyridin-3-ylethynyl)thiazole | 3-(2-(2...)
Affinity DataIC50:  462nMAssay Description:Antagonist activity against mGluR5 expressed in CHO cells assessed as inhibition of agonist-induced phosphoinositide hydrolysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAmine oxidase [flavin-containing] A(Mus musculus)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50122758(2-methyl-4-(pyridin-3-ylethynyl)thiazole | 3-(2-(2...)
Affinity DataIC50:  3.00E+4nMAssay Description:Tested for in vitro antagonistic activity against Monoamine oxidase AMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2D6(Homo sapiens (Human))
Recordati

Curated by ChEMBL
LigandPNGBDBM50122758(2-methyl-4-(pyridin-3-ylethynyl)thiazole | 3-(2-(2...)
Affinity DataIC50:  6.07E+4nMAssay Description:Inhibition of recombinant human CYP2D6 using 3-[2-(N,N-diethylamino)ethyl]-7-methoxy-4-methylcoumarin as substrate preincubated for 10 mins followed ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2D6(Homo sapiens (Human))
Recordati

Curated by ChEMBL
LigandPNGBDBM50122758(2-methyl-4-(pyridin-3-ylethynyl)thiazole | 3-(2-(2...)
Affinity DataIC50:  6.07E+4nMAssay Description:Inhibition of recombinant human CYP2D6 using 3-[2-(N,N-diethylamino)ethyl]-7-methoxy-4-methylcoumarin as substrate preincubated for 10 mins followed ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 3A4(Homo sapiens (Human))
Recordati

Curated by ChEMBL
LigandPNGBDBM50122758(2-methyl-4-(pyridin-3-ylethynyl)thiazole | 3-(2-(2...)
Affinity DataIC50: >1.00E+5nMAssay Description:Inhibition of recombinant human CYP3A4 using 7-benzyloxy-trifluoromethylcoumarin as substrate preincubated for 10 mins followed by substrate addition...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 1(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50122758(2-methyl-4-(pyridin-3-ylethynyl)thiazole | 3-(2-(2...)
Affinity DataIC50: >1.00E+5nMAssay Description:Tested for in vitro antagonistic activity against Metabotropic glutamate receptor 1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 3A4(Homo sapiens (Human))
Recordati

Curated by ChEMBL
LigandPNGBDBM50122758(2-methyl-4-(pyridin-3-ylethynyl)thiazole | 3-(2-(2...)
Affinity DataIC50: >1.00E+5nMAssay Description:Inhibition of recombinant human CYP3A4 using 7-benzyloxy-trifluoromethylcoumarin as substrate preincubated for 10 mins followed by substrate addition...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, NMDA 2B(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50122758(2-methyl-4-(pyridin-3-ylethynyl)thiazole | 3-(2-(2...)
Affinity DataIC50: >3.00E+5nMAssay Description:Tested for in vitro antagonistic activity against recombinat human N-methyl-D-aspartate glutamate receptor 2BMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed