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

Found 8 hits in this display   

TargetCytochrome P450 3A4(Homo sapiens (Human))
Vanderbilt University

Curated by ChEMBL
LigandPNGBDBM361347(6-((1H-pyrazolo[4,3-b] pyridin- 3-yl)amino)-N-(3,3...)
Affinity DataIC50: >3.00E+4nMAssay Description:Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 15 mins followed by substrate addition and measured afte...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C9(Homo sapiens (Human))
Vanderbilt University

Curated by ChEMBL
LigandPNGBDBM361347(6-((1H-pyrazolo[4,3-b] pyridin- 3-yl)amino)-N-(3,3...)
Affinity DataIC50: >3.00E+4nMAssay Description:Inhibition of CYP2C9 in human liver microsomes using diclofenac as substrate preincubated for 15 mins followed by substrate addition and measured aft...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2D6(Homo sapiens (Human))
Vanderbilt University

Curated by ChEMBL
LigandPNGBDBM361347(6-((1H-pyrazolo[4,3-b] pyridin- 3-yl)amino)-N-(3,3...)
Affinity DataIC50: >3.00E+4nMAssay Description:Inhibition of CYP2D6 in human liver microsomes using dextromethorphan as substrate preincubated for 15 mins followed by substrate addition and measur...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 1A2(Homo sapiens (Human))
Vanderbilt University

Curated by ChEMBL
LigandPNGBDBM361347(6-((1H-pyrazolo[4,3-b] pyridin- 3-yl)amino)-N-(3,3...)
Affinity DataIC50: >3.00E+4nMAssay Description:Inhibition of CYP1A2 in human liver microsomes using phenacetin as substrate preincubated for 15 mins followed by substrate addition and measured aft...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 4(Homo sapiens (Human))
Vanderbilt University

Curated by ChEMBL
LigandPNGBDBM361347(6-((1H-pyrazolo[4,3-b] pyridin- 3-yl)amino)-N-(3,3...)
Affinity DataEC50:  50nMAssay Description:Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mo...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 4(Homo sapiens (Human))
Vanderbilt University

Curated by ChEMBL
LigandPNGBDBM361347(6-((1H-pyrazolo[4,3-b] pyridin- 3-yl)amino)-N-(3,3...)
Affinity DataEC50:  50nMAssay Description:Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mo...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 4(Rattus norvegicus (Rat))
Vanderbilt University

Curated by ChEMBL
LigandPNGBDBM361347(6-((1H-pyrazolo[4,3-b] pyridin- 3-yl)amino)-N-(3,3...)
Affinity DataEC50:  83nMAssay Description:Positive allosteric modulation of rat mGlu4 receptor expressed in HEK cells co-expressing GIRK1/2 assessed as increase in glutamate-induced thallium ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMetabotropic glutamate receptor 4(Homo sapiens (Human))
Vanderbilt University

Curated by ChEMBL
LigandPNGBDBM361347(6-((1H-pyrazolo[4,3-b] pyridin- 3-yl)amino)-N-(3,3...)
Affinity DataEC50:  32nMAssay Description:In the first mode, a range of concentrations of the disclosed compounds are added to cells, followed by a single fixed concentration of agonist. If t...More data for this Ligand-Target Pair
In DepthDetails US Patent