BDBM361347 6-((1H-pyrazolo[4,3-b] pyridin- 3-yl)amino)-N-(3,3- difluorocyclobutyl)benzo[d] isothiazole-3-carboxamide::US10221172, Example 4

SMILES FC1(F)CC(C1)NC(=O)c1nsc2cc(Nc3n[nH]c4cccnc34)ccc12

InChI Key InChIKey=NWYHEWQGANWLFU-UHFFFAOYSA-N

Data  4 IC50  4 EC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 8 hits for monomerid = 361347   

TargetMetabotropic glutamate receptor 4(Human)
Vanderbilt University

US Patent
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 Depth
Date in BDB:
10/27/2019
Entry Details
Go to US Patent

TargetMetabotropic glutamate receptor 4(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 Depth
Date in BDB:
2/18/2021
Entry Details Article
PubMed
TargetCytochrome P450 1A2(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 Depth
Date in BDB:
2/18/2021
Entry Details Article
PubMed
TargetCytochrome P450 3A4(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 Depth
Date in BDB:
2/18/2021
Entry Details Article
PubMed
TargetCytochrome P450 2C9(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 Depth
Date in BDB:
2/18/2021
Entry Details Article
PubMed
TargetMetabotropic glutamate receptor 4(Human)
Vanderbilt University

US Patent
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 Depth
Date in BDB:
2/18/2021
Entry Details Article
PubMed
TargetMetabotropic glutamate receptor 4(Human)
Vanderbilt University

US Patent
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 Depth
Date in BDB:
2/18/2021
Entry Details Article
PubMed
TargetCytochrome P450 2D6(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 Depth
Date in BDB:
2/18/2021
Entry Details Article
PubMed