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Compound Detail

CHEMBL3581059

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CN1Cc2cc(-c3cccc([C@H](O)[C@@H](O)C(N)=O)n3)ccc2Oc2ccc(C(F)(F)F)cc21

Basic Information

ChEMBL ID CHEMBL3581059
Phase Preclinical
Structure Type MOL
InChI Key VOQXWCFJBYADIQ-LEWJYISDSA-N
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

459.4
MW (Da)
3.39
ALogP
6
HBA
3
HBD
108.9
PSA (Ų)
0.55
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H20F3N3O4
MW 459.42
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -0.71

Activity Summary

IC50 1 meas. best 5.98
Ki 1 meas. best 6.04

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium channel protein type 9 subunit alpha
CHEMBL4296
Ki 6.04 6.04 920.0 1
Sodium channel protein type 9 subunit alpha
CHEMBL4296
IC50 5.98 5.98 1050.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
25466191 10.1016/j.bmcl.2014.11.025 Sodium channel protein type 9 subunit alpha 2
25466191 10.1016/j.bmcl.2014.11.025 No relevant target 2
25466191 10.1016/j.bmcl.2014.11.025 Liver microsome 2

Data from ChEMBL 36 via Core Engine