BDBM217696 US9212182, 672

SMILES COc1cc(ccc1-n1c2ccc(cc2ccc1=O)S(=O)(=O)Nc1ncccn1)-c1cccc(c1)C(F)(F)F

InChI Key InChIKey=HSOCYPPAQYZHMJ-UHFFFAOYSA-N

Data  16 IC50

  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 16 hits for monomerid = 217696   

LigandPNGBDBM217696(US9212182, 672)
Affinity DataIC50: 23nMAssay Description:HEK 293 cells stably transfected with human Nav1.7 were recorded in whole cell voltage clamp mode with the PatchXpress automated electrophysiology sy...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/21/2017
Entry Details
Go to US Patent

LigandPNGBDBM217696(US9212182, 672)
Affinity DataIC50: 650nMAssay Description:Inhibition of human Nav1.6 expressed in HEK293 cells assessed as use-dependent block at pulse 26 after 3 to 8 mins by ionworks quattro electrophysiol...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/26/2019
Entry Details Article
PubMed
LigandPNGBDBM217696(US9212182, 672)
Affinity DataIC50: 30nMAssay Description:Inhibition of mouse Nav1.7 expressed in HEK293 cells measured after 3 to 5 mins by patchXpress electrophysiology assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/26/2019
Entry Details Article
PubMed
TargetCytochrome P450 2C9(Human)
Amgen

Curated by ChEMBL
LigandPNGBDBM217696(US9212182, 672)
Affinity DataIC50: 4.60E+3nMAssay Description:Inhibition of CYP2C9 in human liver microsomes using diclofenac as substrate in presence of NADPHMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/26/2019
Entry Details Article
PubMed
LigandPNGBDBM217696(US9212182, 672)
Affinity DataIC50: 4.25E+4nMAssay Description:Inhibition of human Nav1.4 expressed in HEK293 cells assessed as use-dependent block at pulse 26 after 3 to 8 mins by ionworks quattro electrophysiol...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/26/2019
Entry Details Article
PubMed
TargetCytochrome P450 3A4(Human)
Amgen

Curated by ChEMBL
LigandPNGBDBM217696(US9212182, 672)
Affinity DataIC50: 5.00E+4nMAssay Description:Reversible inhibition of CYP3A4 in human liver microsomes using midazolam as substrate in presence of NADPHMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/26/2019
Entry Details Article
PubMed
TargetCytochrome P450 3A4(Human)
Amgen

Curated by ChEMBL
LigandPNGBDBM217696(US9212182, 672)
Affinity DataIC50: 5.00E+4nMAssay Description:Time-dependent inhibition of CYP3A4 in human liver microsomes using midazolam as substrate preincubated with enzyme in presence of NADPH followed by ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/26/2019
Entry Details Article
PubMed
LigandPNGBDBM217696(US9212182, 672)
Affinity DataIC50: 3.00E+4nMAssay Description:Inhibition of human Nav1.5 expressed in HEK293 cells incubated for 3 to 5 mins at -50 mV holding potential by patchXpress electrophysiology assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/26/2019
Entry Details Article
PubMed
LigandPNGBDBM217696(US9212182, 672)
Affinity DataIC50: 4.25E+4nMAssay Description:Inhibition of human Nav1.1 expressed in HEK293 cells assessed as use-dependent block at pulse 26 after 3 to 8 mins by ionworks quattro electrophysiol...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/26/2019
Entry Details Article
PubMed
LigandPNGBDBM217696(US9212182, 672)
Affinity DataIC50: 4.25E+4nMAssay Description:Inhibition of human Nav1.5 expressed in HEK293 cells assessed as use-dependent block at pulse 26 after 3 to 8 mins by ionworks quattro electrophysiol...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/26/2019
Entry Details Article
PubMed
LigandPNGBDBM217696(US9212182, 672)
Affinity DataIC50: 6nMAssay Description:Inhibition of human Nav1.7 expressed in HEK293 cells assessed as use-dependent block at pulse 26 after 3 to 8 mins by ionworks quattro electrophysiol...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/26/2019
Entry Details Article
PubMed
LigandPNGBDBM217696(US9212182, 672)
Affinity DataIC50: 6.60E+3nMAssay Description:Inhibition of rat Nav1.7 expressed in HEK293T cells measured after 3 to 5 mins by patchXpress electrophysiology assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/26/2019
Entry Details Article
PubMed
LigandPNGBDBM217696(US9212182, 672)
Affinity DataIC50: 21nMAssay Description:Inhibition of human Nav1.7 expressed in HEK293 cells at holding potential yielding 20 to 50% inactivation measured after 3 to 5 mins by patchXpress e...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/26/2019
Entry Details Article
PubMed
LigandPNGBDBM217696(US9212182, 672)
Affinity DataIC50: 4.25E+4nMAssay Description:Inhibition of human Nav1.3 expressed in CHO cells assessed as use-dependent block at pulse 26 after 3 to 8 mins by ionworks quattro electrophysiology...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/26/2019
Entry Details Article
PubMed
LigandPNGBDBM217696(US9212182, 672)
Affinity DataIC50: 5nMAssay Description:Inhibition of slow inactivated human NaV1.7 expressed in HEK293 cells at -20 mV holding potential after 5 mins by IonWorks electrophysiology methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/9/2020
Entry Details Article
PubMed
LigandPNGBDBM217696(US9212182, 672)
Affinity DataIC50: 20nMAssay Description:Inhibition of human NaV1.7 expressed in HEK293 cells at -125 mV holding potential yielding 20 to 50% inactivation after 3 to 5 mins by PatchXpress au...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/9/2020
Entry Details Article
PubMed