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Compound Detail

CHEMBL3544913

VIXOTRIGINE
🧪 Phase III
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🧪 Phase III
NC(=O)[C@@H]1CC[C@H](c2ccc(OCc3ccccc3F)cc2)N1

Basic Information

ChEMBL ID CHEMBL3544913
Name VIXOTRIGINE
Phase Phase III
Structure Type MOL
InChI Key JESCETIFNOFKEU-SJORKVTESA-N

Known Names

BIIB-074 BIIB074 CNV-1014802 CNV1014802 GSK-1014802 GSK1014802 Raxatrigine Vixotrigina Vixotrigine
9
Targets
11
Activities
1
Assay Types
0
PK Parameters
12
Publications
9
Known Names
6
Indications
1
Mechanisms

Molecular Properties

314.4
MW (Da)
2.68
ALogP
3
HBA
2
HBD
64.3
PSA (Ų)
0.89
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Single Enantiomer
USAN Stem -trigine
USAN Year 2015

Extended Properties

Molecular Formula C18H19FN2O2
MW 314.36
Aromatic Rings 2
Heavy Atoms 23
NP-Likeness -0.68

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
Sodium channel protein type IX alpha subunit blocker BLOCKER Sodium channel protein type 9 subunit alpha

Indications

Trigeminal Neuralgia Erythromelalgia Neuralgia Radiculopathy Bipolar Disorder Diabetic Neuropathies

Activity Summary

IC50 11 meas. best 5.5

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium channel protein type 5 subunit alpha
CHEMBL1980
IC50 5.5 4.79 3200.0 2
Sodium channel protein type 10 subunit alpha
CHEMBL5451
IC50 5.22 5.22 6000.0 1
Sodium channel protein type 9 subunit alpha
CHEMBL4296
IC50 5.21 5.21 6100.0 1
Sodium channel protein type 4 subunit alpha
CHEMBL2072
IC50 5.0 5.0 10000.0 1
Sodium channel protein type 2 subunit alpha
CHEMBL4187
IC50 4.89 4.89 13000.0 1
Sodium channel protein type 1 subunit alpha
CHEMBL1845
IC50 4.82 4.74 15200.0 2
Sodium channel protein type 8 subunit alpha
CHEMBL5202
IC50 4.82 4.82 15000.0 1
Sodium channel protein type 3 subunit alpha
CHEMBL5163
IC50 4.64 4.64 23000.0 1
Sodium channel protein type 7 subunit alpha
CHEMBL3585
IC50 4.5 4.5 32000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Sodium channel protein type 5 subunit alpha IC50 = 3200.0 nM 5.5 Inhibition of human Nav1.5 at -60 mV holding potential by automated patch-clamp ... 36092147
Sodium channel protein type 10 subunit alpha IC50 = 6000.0 nM 5.22 Inhibition of human Nav1.8 expressed in HEK293 cells by electrophysiology assay 31012583
Sodium channel protein type 9 subunit alpha IC50 = 6100.0 nM 5.21 Inhibition of human Nav1.7 at -60 mV holding potential by automated patch-clamp ... 36092147
Sodium channel protein type 4 subunit alpha IC50 = 10000.0 nM 5.0 Inhibition of human Nav1.4 expressed in HEK293 cells by electrophysiology assay 31012583
Sodium channel protein type 2 subunit alpha IC50 = 13000.0 nM 4.89 Inhibition of human Nav1.2 expressed in HEK293 cells by electrophysiology assay 31012583
Sodium channel protein type 8 subunit alpha IC50 = 15000.0 nM 4.82 Inhibition of human Nav1.6 expressed in HEK293 cells by electrophysiology assay 31012583
Sodium channel protein type 1 subunit alpha IC50 = 15200.0 nM 4.82 Inhibition of human Nav1.1 at -60 mV holding potential by automated patch-clamp ... 36092147
Sodium channel protein type 1 subunit alpha IC50 = 22000.0 nM 4.66 Inhibition of human Nav1.1 expressed in HEK293 cells by electrophysiology assay 31012583
Sodium channel protein type 3 subunit alpha IC50 = 23000.0 nM 4.64 Inhibition of human Nav1.3 expressed in HEK293 cells by electrophysiology assay 31012583
Sodium channel protein type 7 subunit alpha IC50 = 32000.0 nM 4.5 Inhibition of human Nav1.7 expressed in HEK293 cells by electrophysiology assay 31012583
Sodium channel protein type 5 subunit alpha IC50 = 84000.0 nM 4.08 Inhibition of human Nav1.5 expressed in HEK293 cells by electrophysiology assay 31012583

Literature References

PubMed DOI Target Context # Activities
31012583 10.1021/acs.jmedchem.8b01906 Unchecked 7
31012583 10.1021/acs.jmedchem.8b01906 Sodium channel protein type 7 subunit alpha 1
31012583 10.1021/acs.jmedchem.8b01906 Sodium channel protein type 1 subunit alpha 1
31012583 10.1021/acs.jmedchem.8b01906 Sodium channel protein type 2 subunit alpha 1
31012583 10.1021/acs.jmedchem.8b01906 Sodium channel protein type 3 subunit alpha 1
31012583 10.1021/acs.jmedchem.8b01906 Sodium channel protein type 4 subunit alpha 1
31012583 10.1021/acs.jmedchem.8b01906 Sodium channel protein type 5 subunit alpha 1
31012583 10.1021/acs.jmedchem.8b01906 Sodium channel protein type 8 subunit alpha 1
31012583 10.1021/acs.jmedchem.8b01906 Sodium channel protein type 10 subunit alpha 1
36092147 10.1039/d2md00081d Sodium channel protein type 1 subunit alpha 1
36092147 10.1039/d2md00081d Sodium channel protein type 5 subunit alpha 1
36092147 10.1039/d2md00081d Sodium channel protein type 9 subunit alpha 1

Data from ChEMBL 36 via Core Engine