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Compound Detail

CHEMBL3634323

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O=C1CCc2c(cccc2N2CCN(CC(O)COc3ccccc3C(=O)c3ccccc3)CC2)N1

Basic Information

ChEMBL ID CHEMBL3634323
Phase Preclinical
Structure Type MOL
InChI Key RAWYHWWKZBOKPS-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

485.6
MW (Da)
3.36
ALogP
6
HBA
2
HBD
82.1
PSA (Ų)
0.48
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H31N3O4
MW 485.58
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -0.83

Activity Summary

IC50 4 meas. best 5.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium channel protein type 9 subunit alpha
CHEMBL3414411
IC50 5.62 5.62 2400.0 1
Sodium channel protein type 9 subunit alpha
CHEMBL4296
IC50 5.43 5.43 3700.0 1
Sodium channel protein type 5 subunit alpha
CHEMBL1980
IC50 4.77 4.77 17000.0 1
Sodium channel protein type 1 subunit alpha
CHEMBL1845
IC50 4.68 4.68 21000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26358159 10.1016/j.bmcl.2015.09.005 Sodium channel protein type 9 subunit alpha 2
26358159 10.1016/j.bmcl.2015.09.005 Sodium channel protein type 1 subunit alpha 1
26358159 10.1016/j.bmcl.2015.09.005 Sodium channel protein type 5 subunit alpha 1

Data from ChEMBL 36 via Core Engine