Compile Data Set for Download or QSAR
maximum 50k data

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB (change energy unit to kcal/mol)

Found 85 hits in this display   

TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
Merck Research Laboratories

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataKi:  0.300nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
Merck Research Laboratories

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataKi:  3.10nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
F. Hoffmann-La Roche

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataKi:  3.30nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
F. Hoffmann-La Roche

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataKi:  3.40nMAssay Description:Displacement of [3H]-ABP688 from human mGluR5 expressed in HEK293 cells after 60 mins by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
F. Hoffmann-La Roche

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataKi:  3.5nMAssay Description:Displacement of [3H]-M-MPEP from mGluR5 StaR domain (569 to 836 residues) (unknown origin) expressed in HEK293 cell membranesMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
Merck Research Laboratories

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataKi:  4.70nMAssay Description:Displacement of [3H]3methoxy-5-(pyridin-2-ylethynyl)pyridine from rat mGluR5More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
Merck Research Laboratories

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataKi:  5.70nMAssay Description:Displacement of [3H]MPEP from mGlu5 receptor in rat brainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
F. Hoffmann-La Roche

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataKi:  6.70nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
Merck Research Laboratories

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataKi:  8.70nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
Merck Research Laboratories

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataKi:  9.60nMAssay Description:Displacement of [3H]M-MPEP from mGluR5 in Sprague-Dawley rat cerebrocortical membranes after 60 minsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
F. Hoffmann-La Roche

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataKi:  10nMAssay Description:Displacement of [3H]MPEP from human mGlu5 receptor expressed in CHO-TREx cell membranes after 60 mins by liquid scintillation spectrometric analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
F. Hoffmann-La Roche

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataKi:  10nMAssay Description:Displacement of [3H]MPEP from human cloned mGluR5 receptor expressed in CHO-T-Rex cells after 60 mins by liquid scintillation spectrometryMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
F. Hoffmann-La Roche

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataKi:  10nMAssay Description:Displacement of [3H]MPEP from human mGlu5 receptor expressed in CHO-TREx cell membranes after 60 mins by liquid scintillation spectrometric analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
Merck Research Laboratories

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataKi:  12nMAssay Description:Tested for displacement of [3H]-3-methoxy-5-(pyridin-2-ylethynyl) pyridine from Metabotropic glutamate receptor 5 in rat cortical membraneMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
Merck Research Laboratories

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataKi:  12nMAssay Description:Displacement of [3H]MPEP from rat mGluR5More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
Merck Research Laboratories

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataKi:  12nMAssay Description:Displacement of [3H]MPEP from rat mGluR5More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
F. Hoffmann-La Roche

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataKi:  13nMAssay Description:Displacement of [3H]MPEP from cloned mGluR5 (unknown origin) expressed in HEK293T cells by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
Merck Research Laboratories

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataKi:  13nMAssay Description:Displacement of [3H]-MPEP from rat mGluR5More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
Merck Research Laboratories

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataKi:  15nMAssay Description:Displacement of [3H]MPEP from mGluR5 receptor in Sprague-Dawley rat forebrain membrane after 60 mins by liquid scintillation spectrometryMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
Merck Research Laboratories

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataKi:  15nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
Merck Research Laboratories

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataKi:  16.3nMAssay Description:Displacement of [3H]MPEP from mGluR5 in Sprague-Dawley rat brain membrane after 60 mins by liquid scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
Merck Research Laboratories

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataKi:  18.7nMAssay Description:Displacement of [3H]methoxy-PEPY from rat mGluR5 expressed in human HEK-293 cells by liquid scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
Merck Research Laboratories

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataKi:  19nMAssay Description:Displacement of [3H]ABP688 from mGluR5 in rat brain membraneMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
Merck Research Laboratories

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataKi:  20nMAssay 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))
F. Hoffmann-La Roche

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataKi:  20nMAssay Description:Displacement of [3H]ABP688 from human mGluR5 receptor expressed in L (tk-) cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
Merck Research Laboratories

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataKi:  21nMAssay 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))
F. Hoffmann-La Roche

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataKi:  28nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 1(Homo sapiens (Human))
Gedeon Richter

Curated by ChEMBL
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataKi:  36nMAssay Description:Antagonist activity at human mGLUR1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
F. Hoffmann-La Roche

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataKi:  36nMAssay Description:Agonist potency against cloned metabotropic glutamate receptor 5More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
F. Hoffmann-La Roche

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataKi:  36.3nMAssay Description:Binding affinity to human mGluR5More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 1A2(Homo sapiens (Human))
Recordati

Curated by ChEMBL
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataKi:  500nMAssay Description:Competitive inhibition of CYP1A2 in human liver microsomes using phenacetin as substrate after 20 mins by LC-MS/MS analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 1A2(Homo sapiens (Human))
Recordati

Curated by ChEMBL
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataKi:  500nMAssay Description:Competitive inhibition of CYP1A2 in human liver microsomes using phenacetin as substrate after 20 mins by LC-MS/MS analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 1(RAT)
University Of Modena And Reggio Emilia

Curated by ChEMBL
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataKi: >1.00E+4nMAssay Description:Displacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometryMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 1(RAT)
University Of Modena And Reggio Emilia

Curated by ChEMBL
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataKi: >1.00E+4nMAssay Description:Displacement of [3H]MPEP from rat mGlu1 receptor expressed in CHO-TREx cell membranes after 30 mins by liquid scintillation spectrometric analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 1(RAT)
University Of Modena And Reggio Emilia

Curated by ChEMBL
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataKi: >1.00E+4nMAssay Description:Displacement of [3H]MPEP from rat mGlu1 receptor expressed in CHO-TREx cell membranes after 30 mins by liquid scintillation spectrometric analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 6(Homo sapiens (Human))
The Royal Danish School Of Pharmacy

Curated by ChEMBL
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataKi: >1.00E+4nMAssay Description:Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 1(Homo sapiens (Human))
Gedeon Richter

Curated by ChEMBL
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataKi:  3.00E+4nMAssay Description:Agonist potency against cloned human metabotropic glutamate receptor 1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 4(Homo sapiens (Human))
The Royal Danish School Of Pharmacy

Curated by ChEMBL
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataKi: >1.00E+5nMAssay Description:Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 7(Homo sapiens (Human))
The Royal Danish School Of Pharmacy

Curated by ChEMBL
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataKi: >1.00E+5nMAssay Description:Agonist potency against cloned Metabotropic glutamate receptor 7 (mGluR-7).More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 3(Homo sapiens (Human))
The Royal Danish School Of Pharmacy

Curated by ChEMBL
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataKi: >1.00E+5nMAssay Description:Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 8(Homo sapiens (Human))
The Royal Danish School Of Pharmacy

Curated by ChEMBL
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataKi: >1.00E+5nMAssay Description:Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 2(Homo sapiens (Human))
The Royal Danish School Of Pharmacy

Curated by ChEMBL
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataKi: >1.00E+5nMAssay Description:Antagonist potency against cloned Metabotropic glutamate receptor 2More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
Merck Research Laboratories

Curated by PDSP Ki Database
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(Homo sapiens (Human))
F. Hoffmann-La Roche

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataIC50:  1.5nMAssay Description:Antagonist activity at human mGluR5 receptor expressed in CHOK1 cells assessed as inhibition of glutamate-mediated internal calcium mobilizationMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
F. Hoffmann-La Roche

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataIC50:  2nMAssay 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))
F. Hoffmann-La Roche

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataIC50:  2nMAssay 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))
F. Hoffmann-La Roche

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataIC50:  2.30nMAssay Description:Antagonist activity at human mGluR5 expressed in HEK293 cells assessed as inhibition of Ca2+ mobilization by FLIPR assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
Merck Research Laboratories

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataIC50:  2.93nMAssay 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))
Merck Research Laboratories

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataIC50:  3.5nMAssay 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))
Merck Research Laboratories

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataIC50:  3.5nMAssay Description:Antagonist activity at rat mGluR5 expressed in HEK293T cells assessed as inhibition of glutamate-induced calcium flux by calcium fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
F. Hoffmann-La Roche

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataIC50:  4nMAssay Description:Displacement of [3H]MPEP from mGlu5 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
F. Hoffmann-La Roche

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataIC50:  10nMAssay 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))
F. Hoffmann-La Roche

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataIC50:  11nMAssay 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))
F. Hoffmann-La Roche

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataIC50:  11nMAssay Description:Binding affinity towards human mGlu5 receptors expressed in LtK-cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
F. Hoffmann-La Roche

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataIC50:  11nMAssay 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))
F. Hoffmann-La Roche

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataIC50:  11nMAssay 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))
Merck Research Laboratories

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataIC50:  13nMAssay Description:Inhibition of [3H]MPEP binding to mGluR5 in rat brain membraneMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
F. Hoffmann-La Roche

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataIC50:  20nMAssay Description:In vitro for inhibitory activity of compound against recombinant Metabotropic glutamate receptor 5 evaluated as inhibition of quisqualate-stimulated ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
Merck Research Laboratories

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataIC50:  20nMAssay Description:Binding affinity towards mGlu5 receptors in rat brain membranes was evaluatedMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
F. Hoffmann-La Roche

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataIC50:  22nMAssay 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(Homo sapiens (Human))
F. Hoffmann-La Roche

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataIC50:  22nMAssay Description:Inhibition of glutamate-induced calcium influx in human mGluR5d by FLIPRMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
F. Hoffmann-La Roche

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataIC50:  29nMAssay Description:Antagonist activity at mGluR5 by FLIPRMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
F. Hoffmann-La Roche

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataIC50:  31nMAssay Description:Displacement of [3H]M-MPEP from recombinant human mGluR5a expressed in human A18 cell membrane homogenate after 60 minsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
Merck Research Laboratories

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataIC50:  31nMAssay 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))
F. Hoffmann-La Roche

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataIC50:  32nMAssay Description:Negative allosteric modulator activity against human mGluR5 expressed in HEK293 cells assessed as inhibition of glutamate-induced inositol phosphate ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
F. Hoffmann-La Roche

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataIC50:  36nMAssay Description:In vitro for inhibitory activity of compound against recombinant Metabotropic glutamate receptor 5 evaluated as inhibition of quisqualate-stimulated ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
F. Hoffmann-La Roche

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataIC50:  36nMAssay Description:Negative allosteric modulation of recombinant human mGlu5a receptor assessed as inhibition of quisqualate-stimulated phosphoinositide hydrolysis by c...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
F. Hoffmann-La Roche

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataIC50:  36nMAssay Description:Compound was tested for it's antagonist activity against Ser152 and Thr175 (Metabotropic glutamate receptor 5)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Rattus norvegicus (Rat))
Merck Research Laboratories

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataIC50:  36nMAssay Description:Concentration required for 50% growth inhibition of rat metabotropic glutamate receptor 5 was determined using inositol phosphate hydrolysis assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
F. Hoffmann-La Roche

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataIC50:  39nMAssay 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))
F. Hoffmann-La Roche

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataIC50:  39nMAssay 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
TargetMetabotropic glutamate receptor 5(Homo sapiens (Human))
F. Hoffmann-La Roche

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataIC50:  4.00E+3nMAssay Description:Experimental material: HEK293/mGluR5 cell line, Fluo-8 calcium ion fluorescent dye, positive control MPEP, CTEPExperimental instrument: FLIPR Tetra r...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetLuciferin 4-monooxygenase(Photinus pyralis)
National Human Genome Research Institute

Curated by ChEMBL
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataIC50:  4.70E+3nMAssay Description:Inhibition of Photinus pyralis luciferaseMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetLuciferin 4-monooxygenase(Photinus pyralis)
National Human Genome Research Institute

Curated by ChEMBL
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataIC50:  6.60E+3nMAssay Description:Inhibition of Photinus pyralis luciferase by PK-Light assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetLuciferin 4-monooxygenase(Photinus pyralis)
National Human Genome Research Institute

Curated by ChEMBL
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataIC50:  7.40E+3nMAssay Description:Inhibition of Photinus pyralis luciferase by Easy lite assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAmine oxidase [flavin-containing] A(Mus musculus)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataIC50:  8.00E+3nMAssay Description:Tested for in vitro antagonistic activity against Monoamine oxidaseMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, NMDA 2B(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataIC50:  1.80E+4nMAssay Description:Tested for in vitro antagonistic activity against human N-methyl-D-aspartate glutamate receptor 2BMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetLuciferin 4-monooxygenase(Photinus pyralis)
National Human Genome Research Institute

Curated by ChEMBL
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataIC50:  3.00E+4nMAssay Description:Inhibition of Photinus pyralis luciferase by BrightGlo reporter gene assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetLuciferin 4-monooxygenase(Photinus pyralis)
National Human Genome Research Institute

Curated by ChEMBL
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataIC50: >1.00E+5nMAssay Description:Inhibition of Photinus pyralis luciferase by Steady-Glo reporter gene assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 3A4(Homo sapiens (Human))
Recordati

Curated by ChEMBL
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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))
Gedeon Richter

Curated by ChEMBL
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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 2D6(Homo sapiens (Human))
Recordati

Curated by ChEMBL
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataIC50: >1.00E+5nMAssay 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
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataIC50: >1.00E+5nMAssay 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
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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 5(Homo sapiens (Human))
F. Hoffmann-La Roche

Curated by PDSP Ki Database
LigandPNGBDBM50084137(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Affinity DataKd:  8.60nMAssay Description:Binding affinity to human mGluR5 expressed in HEK293 cell membranes expressing GLAST by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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