BDBM329203 4-(5-Chloro-6-((1-Methylcyclopropyl)Methoxy)Pyridin-3-yl)-2-Fluoro-5-Methoxy-N-(Methylsulfonyl)Benzamide::4-(5-chloro-6-(2,5-difluorophenoxy)-3-pyridinyl)-2-fluoro-5-methoxy-N-(methylsulfonyl)benzamide::US9663508, Example 705

SMILES COc1cc(C(=O)NS(C)(=O)=O)c(F)cc1-c1cnc(Oc2cc(F)ccc2F)c(Cl)c1

InChI Key InChIKey=PPKNTGHPZNLOFG-UHFFFAOYSA-N

Data  1 KI  29 IC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
Find this compound or compounds like it in BindingDB:
   Substructure
Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 30 hits for monomerid = 329203   

TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM329203(4-(5-Chloro-6-((1-Methylcyclopropyl)Methoxy)Pyridi...)
Affinity DataKi: >3.00E+4nMAssay Description:Displacement of [3H]dofetilide from human ERG expressed in HEK293 cells after 45 mins by scintillation counting analysisMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetSodium channel protein type 9 subunit alpha(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM329203(4-(5-Chloro-6-((1-Methylcyclopropyl)Methoxy)Pyridi...)
Affinity DataIC50:  69nMAssay Description:Inhibition of human Nav1.7 expressed in HEK293 cells incubated for 3 to 5 mins at -125 mV holding potential by electrophysiology assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C9(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM329203(4-(5-Chloro-6-((1-Methylcyclopropyl)Methoxy)Pyridi...)
Affinity DataIC50:  4.96E+4nMAssay Description:Inhibition of CYP2C9 in human microsomes using diclofenac as substrate incubated with enzyme and NADPH prior to substrate addition by LC-MS/MS analys...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetSodium channel protein type 9 subunit alpha(Mus musculus)
Amgen

Curated by ChEMBL
LigandPNGBDBM329203(4-(5-Chloro-6-((1-Methylcyclopropyl)Methoxy)Pyridi...)
Affinity DataIC50:  270nMAssay Description:Inhibition of Nav1.7 in C57BL/6 mouse DRG neurons assessed as reduction in native TTX-S current amplitude by manual patch clamp electrophysiology ass...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetBile salt export pump(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM329203(4-(5-Chloro-6-((1-Methylcyclopropyl)Methoxy)Pyridi...)
Affinity DataIC50:  1.33E+4nMAssay Description:Inhibition of human BSEP in plasma membrane vesicles after 10 mins in presence of [3H]-taurocholate by topcount based transport assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetSodium channel protein type 5 subunit alpha(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM329203(4-(5-Chloro-6-((1-Methylcyclopropyl)Methoxy)Pyridi...)
Affinity DataIC50:  6.90E+3nMAssay Description:Inhibition of human Nav1.5 expressed in HEK293 cells incubated for 3 to 5 mins at -50 mV holding potential by electrophysiology assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetCytochrome P450 3A4(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM329203(4-(5-Chloro-6-((1-Methylcyclopropyl)Methoxy)Pyridi...)
Affinity DataIC50: >5.00E+4nMAssay Description:Inhibition of CYP3A4 in human microsomes using midazolam as substrate coincubated with substrate for 30 mins measured after 5 mins in presence of NAD...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetCytochrome P450 3A4(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM329203(4-(5-Chloro-6-((1-Methylcyclopropyl)Methoxy)Pyridi...)
Affinity DataIC50: >5.00E+4nMAssay Description:Inhibition of CYP3A4 in human microsomes using midazolam as substrate preincubated with enzyme and NADPH prior to substrate addition by LC-MS/MS anal...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetCytochrome P450 2D6(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM329203(4-(5-Chloro-6-((1-Methylcyclopropyl)Methoxy)Pyridi...)
Affinity DataIC50: >5.00E+4nMAssay Description:Inhibition of CYP2D6 in human microsomes using dextromethorphan as substrate incubated with enzyme and NADPH prior to substrate addition by LC-MS/MS ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetSodium channel protein type 9 subunit alpha(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM329203(4-(5-Chloro-6-((1-Methylcyclopropyl)Methoxy)Pyridi...)
Affinity DataIC50:  51nMAssay Description:Inhibition of human Nav1.7 expressed in HEK293 cells assessed as reduction in peak inward current by manual whole cell patch clamp electrophysiology ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetSodium channel protein type 1 subunit alpha(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM329203(4-(5-Chloro-6-((1-Methylcyclopropyl)Methoxy)Pyridi...)
Affinity DataIC50:  8.50E+3nMAssay Description:Inhibition of human Nav1.1 expressed in HEK293 cells assessed as reduction in peak inward current by manual whole cell patch clamp electrophysiology ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetSodium channel protein type 2 subunit alpha(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM329203(4-(5-Chloro-6-((1-Methylcyclopropyl)Methoxy)Pyridi...)
Affinity DataIC50:  9.80E+3nMAssay Description:Inhibition of human Nav1.2 expressed in CHO cells assessed as reduction in peak inward current by manual whole cell patch clamp electrophysiology ass...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetSodium channel protein type 4 subunit alpha(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM329203(4-(5-Chloro-6-((1-Methylcyclopropyl)Methoxy)Pyridi...)
Affinity DataIC50:  1.10E+3nMAssay Description:Inhibition of human Nav1.4 expressed in HEK293 cells assessed as reduction in peak inward current by manual whole cell patch clamp electrophysiology ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetSodium channel protein type 10 subunit alpha(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM329203(4-(5-Chloro-6-((1-Methylcyclopropyl)Methoxy)Pyridi...)
Affinity DataIC50:  1.56E+4nMAssay Description:Inhibition of human Nav1.8 expressed in CHO cells assessed as reduction in peak inward current by manual whole cell patch clamp electrophysiology ass...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetSodium channel protein type 9 subunit alpha(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM329203(4-(5-Chloro-6-((1-Methylcyclopropyl)Methoxy)Pyridi...)
Affinity DataIC50:  42nMAssay Description:Inhibition of human Nav1.7 expressed in HEK293 cells assessed as use-dependent block at pulse 26 by ionworks quattro electrophysiology assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetSodium channel protein type 5 subunit alpha(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM329203(4-(5-Chloro-6-((1-Methylcyclopropyl)Methoxy)Pyridi...)
Affinity DataIC50:  1.36E+4nMAssay Description:Inhibition of human Nav1.5 expressed in HEK293 cells assessed as tonic block at pulse 1 by ionworks quattro electrophysiology assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetSodium channel protein type 9 subunit alpha(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM329203(4-(5-Chloro-6-((1-Methylcyclopropyl)Methoxy)Pyridi...)
Affinity DataIC50: >3.00E+4nMAssay Description:Inhibition of human Nav1.7 at resting/closed state expressed in HEK293 cells at -140 mV holding potential by manual whole cell patch clamp electrophy...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetSodium channel protein type 9 subunit alpha(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM329203(4-(5-Chloro-6-((1-Methylcyclopropyl)Methoxy)Pyridi...)
Affinity DataIC50:  17nMAssay Description:Displacement of [3H]-6,6-fused heteroaryl-sulfonamide derivative from human Nav1.7 expressed in HEK293 cell membranes preincubated for 30 mins follow...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetSodium channel protein type 3 subunit alpha(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM329203(4-(5-Chloro-6-((1-Methylcyclopropyl)Methoxy)Pyridi...)
Affinity DataIC50:  1.25E+4nMAssay Description:Inhibition of human Nav1.3 expressed in CHO cells assessed as reduction in peak inward current by manual whole cell patch clamp electrophysiology ass...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetSodium channel protein type 9 subunit alpha(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM329203(4-(5-Chloro-6-((1-Methylcyclopropyl)Methoxy)Pyridi...)
Affinity DataIC50:  44nMAssay Description:Inhibition of human Nav1.7 expressed in HEK293 cells assessed as tonic block at pulse 1 by ionworks quattro electrophysiology assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetSodium channel protein type 9 subunit alpha(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM329203(4-(5-Chloro-6-((1-Methylcyclopropyl)Methoxy)Pyridi...)
Affinity DataIC50:  51nMAssay Description:Inhibition of human Nav1.7 at 20% inactivated state expressed in HEK293 cells at -140 mV holding potential followed by channel inactivation by manual...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetCytochrome P450 2D6(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM329203(4-(5-Chloro-6-((1-Methylcyclopropyl)Methoxy)Pyridi...)
Affinity DataIC50: >5.00E+4nMAssay Description:Inhibition of CYP2D6 in human microsomes using dextromethorphan as substrate coincubated with substrate for 30 mins measured after 5 mins in presence...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetSodium channel protein type 5 subunit alpha(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM329203(4-(5-Chloro-6-((1-Methylcyclopropyl)Methoxy)Pyridi...)
Affinity DataIC50:  1.19E+4nMAssay Description:Inhibition of human Nav1.5 expressed in HEK293 cells assessed as reduction in peak inward current by manual whole cell patch clamp electrophysiology ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetSodium channel protein type 9 subunit alpha(Rattus norvegicus)
Amgen

Curated by ChEMBL
LigandPNGBDBM329203(4-(5-Chloro-6-((1-Methylcyclopropyl)Methoxy)Pyridi...)
Affinity DataIC50:  3.69E+3nMAssay Description:Inhibition of rat Nav1.7 expressed in HEK293T cells incubated for 3 to 5 mins at -125 mV holding potential by electrophysiology assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetSodium channel protein type 8 subunit alpha(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM329203(4-(5-Chloro-6-((1-Methylcyclopropyl)Methoxy)Pyridi...)
Affinity DataIC50:  9.40E+3nMAssay Description:Inhibition of human Nav1.6 expressed in HEK293 cells assessed as reduction in peak inward current by manual whole cell patch clamp electrophysiology ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C9(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM329203(4-(5-Chloro-6-((1-Methylcyclopropyl)Methoxy)Pyridi...)
Affinity DataIC50:  4.53E+4nMAssay Description:Inhibition of CYP2C9 in human microsomes using diclofenac as substrate coincubated with substrate for 30 mins measured after 5 mins in presence of NA...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetSodium channel protein type 9 subunit alpha(Mus musculus)
Amgen

Curated by ChEMBL
LigandPNGBDBM329203(4-(5-Chloro-6-((1-Methylcyclopropyl)Methoxy)Pyridi...)
Affinity DataIC50:  115nMAssay Description:Inhibition of mouse Nav1.7 expressed in HEK293 cells incubated for 3 to 5 mins at -125 mV holding potential by electrophysiology assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetSodium channel protein type 5 subunit alpha(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM329203(4-(5-Chloro-6-((1-Methylcyclopropyl)Methoxy)Pyridi...)
Affinity DataIC50:  1.14E+4nMAssay Description:Inhibition of human Nav1.5 expressed in HEK293 cells assessed as use-dependent block at pulse 26 by ionworks quattro electrophysiology assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetSodium channel protein type 9 subunit alpha(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM329203(4-(5-Chloro-6-((1-Methylcyclopropyl)Methoxy)Pyridi...)
Affinity DataIC50:  130nMAssay 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
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetSodium channel protein type 5 subunit alpha(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM329203(4-(5-Chloro-6-((1-Methylcyclopropyl)Methoxy)Pyridi...)
Affinity DataIC50:  841nMAssay Description:293 cells stably transfected with human Nav 1.5 were recorded in whole cell voltage clamp mode with the PatchXpress automated electrophysiology syste...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent