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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
Target
Metabotropic glutamate receptor 5
(Rattus norvegicus (Rat))
Merck Research Laboratories
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Copy SMILES
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Affinity Data
Ki: 0.300nM
More data for this Ligand-Target Pair
Target Info
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Target
Metabotropic glutamate receptor 5
(Rattus norvegicus (Rat))
Merck Research Laboratories
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 3.10nM
More data for this Ligand-Target Pair
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Target
Metabotropic glutamate receptor 5
(Homo sapiens (Human))
F. Hoffmann-La Roche
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 3.30nM
More data for this Ligand-Target Pair
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Target
Metabotropic glutamate receptor 5
(Homo sapiens (Human))
F. Hoffmann-La Roche
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 3.40nM
Assay Description:
Displacement of [3H]-ABP688 from human mGluR5 expressed in HEK293 cells after 60 mins by scintillation counting
More data for this Ligand-Target Pair
Target Info
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Target
Metabotropic glutamate receptor 5
(Homo sapiens (Human))
F. Hoffmann-La Roche
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 3.5nM
Assay Description:
Displacement of [3H]-M-MPEP from mGluR5 StaR domain (569 to 836 residues) (unknown origin) expressed in HEK293 cell membranes
More data for this Ligand-Target Pair
Target Info
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Target
Metabotropic glutamate receptor 5
(Rattus norvegicus (Rat))
Merck Research Laboratories
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 4.70nM
Assay Description:
Displacement of [3H]3methoxy-5-(pyridin-2-ylethynyl)pyridine from rat mGluR5
More data for this Ligand-Target Pair
Target Info
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Target
Metabotropic glutamate receptor 5
(Rattus norvegicus (Rat))
Merck Research Laboratories
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 5.70nM
Assay Description:
Displacement of [3H]MPEP from mGlu5 receptor in rat brain
More data for this Ligand-Target Pair
Target Info
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Target
Metabotropic glutamate receptor 5
(Homo sapiens (Human))
F. Hoffmann-La Roche
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 6.70nM
More data for this Ligand-Target Pair
Target Info
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Copy BDB DOI
Target
Metabotropic glutamate receptor 5
(Rattus norvegicus (Rat))
Merck Research Laboratories
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 8.70nM
More data for this Ligand-Target Pair
Target Info
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Copy BDB DOI
Target
Metabotropic glutamate receptor 5
(Rattus norvegicus (Rat))
Merck Research Laboratories
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 9.60nM
Assay Description:
Displacement of [3H]M-MPEP from mGluR5 in Sprague-Dawley rat cerebrocortical membranes after 60 mins
More data for this Ligand-Target Pair
Target Info
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Target
Metabotropic glutamate receptor 5
(Homo sapiens (Human))
F. Hoffmann-La Roche
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 10nM
Assay Description:
Displacement of [3H]MPEP from human mGlu5 receptor expressed in CHO-TREx cell membranes after 60 mins by liquid scintillation spectrometric analysis
More data for this Ligand-Target Pair
Target Info
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Copy BDB DOI
Target
Metabotropic glutamate receptor 5
(Homo sapiens (Human))
F. Hoffmann-La Roche
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 10nM
Assay Description:
Displacement of [3H]MPEP from human cloned mGluR5 receptor expressed in CHO-T-Rex cells after 60 mins by liquid scintillation spectrometry
More data for this Ligand-Target Pair
Target Info
PDB
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KEGG
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ChEBI
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In Depth
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Article
PubMed
Copy BDB DOI
Target
Metabotropic glutamate receptor 5
(Homo sapiens (Human))
F. Hoffmann-La Roche
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 10nM
Assay Description:
Displacement of [3H]MPEP from human mGlu5 receptor expressed in CHO-TREx cell membranes after 60 mins by liquid scintillation spectrometric analysis
More data for this Ligand-Target Pair
Target Info
PDB
MMDB
Reactome pathway
KEGG
UniProtKB/SwissProt
B.MOAD
DrugBank
antibodypedia
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Copy BDB DOI
Target
Metabotropic glutamate receptor 5
(Rattus norvegicus (Rat))
Merck Research Laboratories
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 12nM
Assay Description:
Tested for displacement of [3H]-3-methoxy-5-(pyridin-2-ylethynyl) pyridine from Metabotropic glutamate receptor 5 in rat cortical membrane
More data for this Ligand-Target Pair
Target Info
PDB
MMDB
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KEGG
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B.MOAD
GoogleScholar
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In Depth
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Copy BDB DOI
Target
Metabotropic glutamate receptor 5
(Rattus norvegicus (Rat))
Merck Research Laboratories
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 12nM
Assay Description:
Displacement of [3H]MPEP from rat mGluR5
More data for this Ligand-Target Pair
Target Info
PDB
MMDB
Reactome pathway
KEGG
UniProtKB/SwissProt
B.MOAD
GoogleScholar
Ligand Info
Purchase
ChEBI
CHEMBL
MCE
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In Depth
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Article
PubMed
Copy BDB DOI
Target
Metabotropic glutamate receptor 5
(Rattus norvegicus (Rat))
Merck Research Laboratories
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 12nM
Assay Description:
Displacement of [3H]MPEP from rat mGluR5
More data for this Ligand-Target Pair
Target Info
PDB
MMDB
Reactome pathway
KEGG
UniProtKB/SwissProt
B.MOAD
GoogleScholar
Ligand Info
Purchase
ChEBI
CHEMBL
MCE
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PC sid
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In Depth
Details
Article
PubMed
Copy BDB DOI
Target
Metabotropic glutamate receptor 5
(Homo sapiens (Human))
F. Hoffmann-La Roche
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 13nM
Assay Description:
Displacement of [3H]MPEP from cloned mGluR5 (unknown origin) expressed in HEK293T cells by scintillation counting
More data for this Ligand-Target Pair
Target Info
PDB
MMDB
Reactome pathway
KEGG
UniProtKB/SwissProt
B.MOAD
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antibodypedia
GoogleScholar
Ligand Info
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ChEBI
CHEMBL
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In Depth
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Article
PubMed
Copy BDB DOI
Target
Metabotropic glutamate receptor 5
(Rattus norvegicus (Rat))
Merck Research Laboratories
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 13nM
Assay Description:
Displacement of [3H]-MPEP from rat mGluR5
More data for this Ligand-Target Pair
Target Info
PDB
MMDB
Reactome pathway
KEGG
UniProtKB/SwissProt
B.MOAD
GoogleScholar
Ligand Info
Purchase
ChEBI
CHEMBL
MCE
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In Depth
Details
Article
PubMed
Copy BDB DOI
Target
Metabotropic glutamate receptor 5
(Rattus norvegicus (Rat))
Merck Research Laboratories
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 15nM
Assay Description:
Displacement of [3H]MPEP from mGluR5 receptor in Sprague-Dawley rat forebrain membrane after 60 mins by liquid scintillation spectrometry
More data for this Ligand-Target Pair
Target Info
PDB
MMDB
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KEGG
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In Depth
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Copy BDB DOI
Target
Metabotropic glutamate receptor 5
(Rattus norvegicus (Rat))
Merck Research Laboratories
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 15nM
More data for this Ligand-Target Pair
Target Info
PDB
MMDB
Reactome pathway
KEGG
UniProtKB/SwissProt
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Ligand Info
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In Depth
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Copy BDB DOI
Target
Metabotropic glutamate receptor 5
(Rattus norvegicus (Rat))
Merck Research Laboratories
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 16.3nM
Assay Description:
Displacement of [3H]MPEP from mGluR5 in Sprague-Dawley rat brain membrane after 60 mins by liquid scintillation counting
More data for this Ligand-Target Pair
Target Info
PDB
MMDB
Reactome pathway
KEGG
UniProtKB/SwissProt
B.MOAD
GoogleScholar
Ligand Info
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ChEBI
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Copy BDB DOI
Target
Metabotropic glutamate receptor 5
(Rattus norvegicus (Rat))
Merck Research Laboratories
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 18.7nM
Assay Description:
Displacement of [3H]methoxy-PEPY from rat mGluR5 expressed in human HEK-293 cells by liquid scintillation counting
More data for this Ligand-Target Pair
Target Info
PDB
MMDB
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Copy BDB DOI
Target
Metabotropic glutamate receptor 5
(Rattus norvegicus (Rat))
Merck Research Laboratories
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 19nM
Assay Description:
Displacement of [3H]ABP688 from mGluR5 in rat brain membrane
More data for this Ligand-Target Pair
Target Info
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MMDB
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KEGG
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Ligand Info
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ChEBI
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In Depth
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Copy BDB DOI
Target
Metabotropic glutamate receptor 5
(Rattus norvegicus (Rat))
Merck Research Laboratories
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 20nM
Assay Description:
Displacement of [3H]MPEP from mGluR5 in rat brain membrane
More data for this Ligand-Target Pair
Target Info
PDB
MMDB
Reactome pathway
KEGG
UniProtKB/SwissProt
B.MOAD
GoogleScholar
Ligand Info
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ChEBI
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In Depth
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PubMed
Copy BDB DOI
Target
Metabotropic glutamate receptor 5
(Homo sapiens (Human))
F. Hoffmann-La Roche
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 20nM
Assay Description:
Displacement of [3H]ABP688 from human mGluR5 receptor expressed in L (tk-) cells
More data for this Ligand-Target Pair
Target Info
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KEGG
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Copy BDB DOI
Target
Metabotropic glutamate receptor 5
(Rattus norvegicus (Rat))
Merck Research Laboratories
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 21nM
Assay Description:
Displacement of [3H]MPEP from mGluR5 in rat brain membrane
More data for this Ligand-Target Pair
Target Info
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MMDB
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Copy BDB DOI
Target
Metabotropic glutamate receptor 5
(Homo sapiens (Human))
F. Hoffmann-La Roche
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 28nM
More data for this Ligand-Target Pair
Target Info
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Target
Metabotropic glutamate receptor 1
(Homo sapiens (Human))
Gedeon Richter
Curated by
ChEMBL
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Copy SMILES
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Affinity Data
Ki: 36nM
Assay Description:
Antagonist activity at human mGLUR1
More data for this Ligand-Target Pair
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Target
Metabotropic glutamate receptor 5
(Homo sapiens (Human))
F. Hoffmann-La Roche
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 36nM
Assay Description:
Agonist potency against cloned metabotropic glutamate receptor 5
More data for this Ligand-Target Pair
Target Info
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Target
Metabotropic glutamate receptor 5
(Homo sapiens (Human))
F. Hoffmann-La Roche
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 36.3nM
Assay Description:
Binding affinity to human mGluR5
More data for this Ligand-Target Pair
Target Info
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Target
Cytochrome P450 1A2
(Homo sapiens (Human))
Recordati
Curated by
ChEMBL
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 500nM
Assay Description:
Competitive inhibition of CYP1A2 in human liver microsomes using phenacetin as substrate after 20 mins by LC-MS/MS analysis
More data for this Ligand-Target Pair
Target Info
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Target
Cytochrome P450 1A2
(Homo sapiens (Human))
Recordati
Curated by
ChEMBL
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Copy SMILES
Copy InChI
Affinity Data
Ki: 500nM
Assay Description:
Competitive inhibition of CYP1A2 in human liver microsomes using phenacetin as substrate after 20 mins by LC-MS/MS analysis
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Target
Metabotropic glutamate receptor 1
(RAT)
University Of Modena And Reggio Emilia
Curated by
ChEMBL
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
Ki: >1.00E+4nM
Assay Description:
Displacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometry
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Target
Metabotropic glutamate receptor 1
(RAT)
University Of Modena And Reggio Emilia
Curated by
ChEMBL
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
Ki: >1.00E+4nM
Assay Description:
Displacement of [3H]MPEP from rat mGlu1 receptor expressed in CHO-TREx cell membranes after 30 mins by liquid scintillation spectrometric analysis
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Target
Metabotropic glutamate receptor 1
(RAT)
University Of Modena And Reggio Emilia
Curated by
ChEMBL
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
Ki: >1.00E+4nM
Assay Description:
Displacement of [3H]MPEP from rat mGlu1 receptor expressed in CHO-TREx cell membranes after 30 mins by liquid scintillation spectrometric analysis
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Target
Metabotropic glutamate receptor 6
(Homo sapiens (Human))
The Royal Danish School Of Pharmacy
Curated by
ChEMBL
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
Ki: >1.00E+4nM
Assay Description:
Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).
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Target
Metabotropic glutamate receptor 1
(Homo sapiens (Human))
Gedeon Richter
Curated by
ChEMBL
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
Ki: 3.00E+4nM
Assay Description:
Agonist potency against cloned human metabotropic glutamate receptor 1
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Target
Metabotropic glutamate receptor 4
(Homo sapiens (Human))
The Royal Danish School Of Pharmacy
Curated by
ChEMBL
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
Ki: >1.00E+5nM
Assay Description:
Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)
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Target
Metabotropic glutamate receptor 7
(Homo sapiens (Human))
The Royal Danish School Of Pharmacy
Curated by
ChEMBL
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
Ki: >1.00E+5nM
Assay Description:
Agonist potency against cloned Metabotropic glutamate receptor 7 (mGluR-7).
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Target
Metabotropic glutamate receptor 3
(Homo sapiens (Human))
The Royal Danish School Of Pharmacy
Curated by
ChEMBL
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
Ki: >1.00E+5nM
Assay Description:
Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).
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Target
Metabotropic glutamate receptor 8
(Homo sapiens (Human))
The Royal Danish School Of Pharmacy
Curated by
ChEMBL
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
Ki: >1.00E+5nM
Assay Description:
Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).
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Target
Metabotropic glutamate receptor 2
(Homo sapiens (Human))
The Royal Danish School Of Pharmacy
Curated by
ChEMBL
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
Ki: >1.00E+5nM
Assay Description:
Antagonist potency against cloned Metabotropic glutamate receptor 2
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Target
Metabotropic glutamate receptor 5
(Rattus norvegicus (Rat))
Merck Research Laboratories
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
IC50: 0.200nM
Assay Description:
Activity at rat mGlu5 receptor expressed in CHO cells assessed as inhibition of quisqualate-stimulated calcium mobilization by FLIPR assay
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Target
Metabotropic glutamate receptor 5
(Homo sapiens (Human))
F. Hoffmann-La Roche
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
IC50: 1.5nM
Assay Description:
Antagonist activity at human mGluR5 receptor expressed in CHOK1 cells assessed as inhibition of glutamate-mediated internal calcium mobilization
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Target
Metabotropic glutamate receptor 5
(Homo sapiens (Human))
F. Hoffmann-La Roche
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
IC50: 2nM
Assay Description:
In vitro functional potency using an automated assay employing LtK-cells stably expressing human recombinant mGlu5 receptor by measuring changes in c...
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Target
Metabotropic glutamate receptor 5
(Homo sapiens (Human))
F. Hoffmann-La Roche
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
IC50: 2nM
Assay Description:
Tested in vitro against human recombinant Metabotropic glutamate receptor 5 stably expressed in LtK cells by [Ca2+] flux assay using glutamate as ant...
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Target
Metabotropic glutamate receptor 5
(Homo sapiens (Human))
F. Hoffmann-La Roche
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
IC50: 2.30nM
Assay Description:
Antagonist activity at human mGluR5 expressed in HEK293 cells assessed as inhibition of Ca2+ mobilization by FLIPR assay
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Target
Metabotropic glutamate receptor 5
(Rattus norvegicus (Rat))
Merck Research Laboratories
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
IC50: 2.93nM
Assay Description:
Antagonist activity at rat mGluR5 expressed in human HEK-293 cells assessed as inhibition of glutamate-induced intracellular calcium mobilization
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Target
Metabotropic glutamate receptor 5
(Rattus norvegicus (Rat))
Merck Research Laboratories
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
IC50: 3.5nM
Assay Description:
Antagonist activity at rat mGluR5 expressed in HEK293A cells assessed as glutamate-induced calcium flux preincubated for 140 sec before glutamate cha...
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Target
Metabotropic glutamate receptor 5
(Rattus norvegicus (Rat))
Merck Research Laboratories
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
IC50: 3.5nM
Assay Description:
Antagonist activity at rat mGluR5 expressed in HEK293T cells assessed as inhibition of glutamate-induced calcium flux by calcium fluorescence assay
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Target
Metabotropic glutamate receptor 5
(Homo sapiens (Human))
F. Hoffmann-La Roche
Curated by
PDSP K
i
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Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
IC50: 4nM
Assay Description:
Displacement of [3H]MPEP from mGlu5 receptor
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Target
Metabotropic glutamate receptor 5
(Homo sapiens (Human))
F. Hoffmann-La Roche
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
IC50: 10nM
Assay Description:
Antagonist activity at human mGluR5 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR
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Target
Metabotropic glutamate receptor 5
(Homo sapiens (Human))
F. Hoffmann-La Roche
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
IC50: 11nM
Assay Description:
Negative allosteric modulatory activity at human cloned mGluR5 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced cal...
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Target
Metabotropic glutamate receptor 5
(Homo sapiens (Human))
F. Hoffmann-La Roche
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
IC50: 11nM
Assay Description:
Binding affinity towards human mGlu5 receptors expressed in LtK-cells
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Target
Metabotropic glutamate receptor 5
(Homo sapiens (Human))
F. Hoffmann-La Roche
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
IC50: 11nM
Assay Description:
Negative allosteric modulation of human mGlu5 receptor expressed in CHO-TREx cell membranes assessed as reduction in quisqualate-induced Ca2+ mobiliz...
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Target
Metabotropic glutamate receptor 5
(Homo sapiens (Human))
F. Hoffmann-La Roche
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
IC50: 11nM
Assay Description:
Negative allosteric modulation of human mGlu5 receptor expressed in CHO-TREx cell membranes assessed as reduction in quisqualate-induced Ca2+ mobiliz...
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Target
Metabotropic glutamate receptor 5
(Rattus norvegicus (Rat))
Merck Research Laboratories
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
IC50: 13nM
Assay Description:
Inhibition of [3H]MPEP binding to mGluR5 in rat brain membrane
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Target
Metabotropic glutamate receptor 5
(Homo sapiens (Human))
F. Hoffmann-La Roche
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
IC50: 20nM
Assay Description:
In vitro for inhibitory activity of compound against recombinant Metabotropic glutamate receptor 5 evaluated as inhibition of quisqualate-stimulated ...
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Target
Metabotropic glutamate receptor 5
(Rattus norvegicus (Rat))
Merck Research Laboratories
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
IC50: 20nM
Assay Description:
Binding affinity towards mGlu5 receptors in rat brain membranes was evaluated
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Target
Metabotropic glutamate receptor 5
(Homo sapiens (Human))
F. Hoffmann-La Roche
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
IC50: 22nM
Assay Description:
Activity at human mGluR5 assessed as effect on glutamate-induced calcium ion mobilization by FLIPR
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Target
Metabotropic glutamate receptor 5
(Homo sapiens (Human))
F. Hoffmann-La Roche
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
IC50: 22nM
Assay Description:
Inhibition of glutamate-induced calcium influx in human mGluR5d by FLIPR
More data for this Ligand-Target Pair
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Target
Metabotropic glutamate receptor 5
(Homo sapiens (Human))
F. Hoffmann-La Roche
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
IC50: 29nM
Assay Description:
Antagonist activity at mGluR5 by FLIPR
More data for this Ligand-Target Pair
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Target
Metabotropic glutamate receptor 5
(Homo sapiens (Human))
F. Hoffmann-La Roche
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
Copy SMILES
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Affinity Data
IC50: 31nM
Assay Description:
Displacement of [3H]M-MPEP from recombinant human mGluR5a expressed in human A18 cell membrane homogenate after 60 mins
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Metabotropic glutamate receptor 5
(Rattus norvegicus (Rat))
Merck Research Laboratories
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
IC50: 31nM
Assay Description:
Inverse agonist activity at rat mGluR5 expressed in HEK293A cells coexpressing Gqalpha assessed as inhibition of quisqualic-induced D-myo-inositol 1 ...
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Metabotropic glutamate receptor 5
(Homo sapiens (Human))
F. Hoffmann-La Roche
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
IC50: 32nM
Assay Description:
Negative allosteric modulator activity against human mGluR5 expressed in HEK293 cells assessed as inhibition of glutamate-induced inositol phosphate ...
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Target
Metabotropic glutamate receptor 5
(Homo sapiens (Human))
F. Hoffmann-La Roche
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
IC50: 36nM
Assay Description:
In vitro for inhibitory activity of compound against recombinant Metabotropic glutamate receptor 5 evaluated as inhibition of quisqualate-stimulated ...
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Target
Metabotropic glutamate receptor 5
(Homo sapiens (Human))
F. Hoffmann-La Roche
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
IC50: 36nM
Assay Description:
Negative allosteric modulation of recombinant human mGlu5a receptor assessed as inhibition of quisqualate-stimulated phosphoinositide hydrolysis by c...
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Target
Metabotropic glutamate receptor 5
(Homo sapiens (Human))
F. Hoffmann-La Roche
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
IC50: 36nM
Assay Description:
Compound was tested for it's antagonist activity against Ser152 and Thr175 (Metabotropic glutamate receptor 5)
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Target
Metabotropic glutamate receptor 5
(Rattus norvegicus (Rat))
Merck Research Laboratories
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
IC50: 36nM
Assay Description:
Concentration required for 50% growth inhibition of rat metabotropic glutamate receptor 5 was determined using inositol phosphate hydrolysis assay
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Target
Metabotropic glutamate receptor 5
(Homo sapiens (Human))
F. Hoffmann-La Roche
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
IC50: 39nM
Assay Description:
Activity in agonist-induced phosphoinositide hydrolysis in CHO cells expressing mGluR5a
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Target
Metabotropic glutamate receptor 5
(Homo sapiens (Human))
F. Hoffmann-La Roche
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
IC50: 39nM
Assay Description:
Antagonist activity against mGluR5 expressed in CHO cells assessed as inhibition of agonist-induced phosphoinositide hydrolysis
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Target
Metabotropic glutamate receptor 5
(Homo sapiens (Human))
F. Hoffmann-La Roche
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
IC50: 4.00E+3nM
Assay Description:
Experimental material: HEK293/mGluR5 cell line, Fluo-8 calcium ion fluorescent dye, positive control MPEP, CTEPExperimental instrument: FLIPR Tetra r...
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Target
Luciferin 4-monooxygenase
(Photinus pyralis)
National Human Genome Research Institute
Curated by
ChEMBL
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
IC50: 4.70E+3nM
Assay Description:
Inhibition of Photinus pyralis luciferase
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Target
Luciferin 4-monooxygenase
(Photinus pyralis)
National Human Genome Research Institute
Curated by
ChEMBL
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
IC50: 6.60E+3nM
Assay Description:
Inhibition of Photinus pyralis luciferase by PK-Light assay
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Target
Luciferin 4-monooxygenase
(Photinus pyralis)
National Human Genome Research Institute
Curated by
ChEMBL
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
IC50: 7.40E+3nM
Assay Description:
Inhibition of Photinus pyralis luciferase by Easy lite assay
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Target
Amine oxidase [flavin-containing] A
(Mus musculus)
Merck Research Laboratories
Curated by
ChEMBL
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
IC50: 8.00E+3nM
Assay Description:
Tested for in vitro antagonistic activity against Monoamine oxidase
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Target
Glutamate receptor ionotropic, NMDA 2B
(Homo sapiens (Human))
Merck Research Laboratories
Curated by
ChEMBL
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
IC50: 1.80E+4nM
Assay Description:
Tested for in vitro antagonistic activity against human N-methyl-D-aspartate glutamate receptor 2B
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Target
Luciferin 4-monooxygenase
(Photinus pyralis)
National Human Genome Research Institute
Curated by
ChEMBL
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
IC50: 3.00E+4nM
Assay Description:
Inhibition of Photinus pyralis luciferase by BrightGlo reporter gene assay
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Target
Luciferin 4-monooxygenase
(Photinus pyralis)
National Human Genome Research Institute
Curated by
ChEMBL
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
IC50: >1.00E+5nM
Assay Description:
Inhibition of Photinus pyralis luciferase by Steady-Glo reporter gene assay
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Target
Cytochrome P450 3A4
(Homo sapiens (Human))
Recordati
Curated by
ChEMBL
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
IC50: >1.00E+5nM
Assay Description:
Inhibition of recombinant human CYP3A4 using 7-benzyloxy-trifluoromethylcoumarin as substrate preincubated for 10 mins followed by substrate addition...
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Target
Metabotropic glutamate receptor 1
(Homo sapiens (Human))
Gedeon Richter
Curated by
ChEMBL
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
IC50: >1.00E+5nM
Assay Description:
Tested for in vitro antagonistic activity against Metabotropic glutamate receptor 1
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Target
Cytochrome P450 2D6
(Homo sapiens (Human))
Recordati
Curated by
ChEMBL
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
IC50: >1.00E+5nM
Assay Description:
Inhibition of recombinant human CYP2D6 using 3-[2-(N,N-diethylamino)ethyl]-7-methoxy-4-methylcoumarin as substrate preincubated for 10 mins followed ...
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Target
Cytochrome P450 2D6
(Homo sapiens (Human))
Recordati
Curated by
ChEMBL
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
IC50: >1.00E+5nM
Assay Description:
Inhibition of recombinant human CYP2D6 using 3-[2-(N,N-diethylamino)ethyl]-7-methoxy-4-methylcoumarin as substrate preincubated for 10 mins followed ...
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Target
Cytochrome P450 3A4
(Homo sapiens (Human))
Recordati
Curated by
ChEMBL
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
IC50: >1.00E+5nM
Assay Description:
Inhibition of recombinant human CYP3A4 using 7-benzyloxy-trifluoromethylcoumarin as substrate preincubated for 10 mins followed by substrate addition...
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Target
Metabotropic glutamate receptor 5
(Homo sapiens (Human))
F. Hoffmann-La Roche
Curated by
PDSP K
i
Database
Ligand
BDBM50084137
(2-Methyl-6-(phenylethynyl)pyridine | 2-Methyl-6-ph...)
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Affinity Data
Kd: 8.60nM
Assay Description:
Binding affinity to human mGluR5 expressed in HEK293 cell membranes expressing GLAST by scintillation counting
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