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Compound Detail

CHEMBL4073701

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C[C@@H]1CN(c2c(NC(=O)c3cccc(-c4ccccn4)c3)cccc2C(F)(F)F)C[C@H](C)O1

Basic Information

ChEMBL ID CHEMBL4073701
Phase Preclinical
Structure Type MOL
InChI Key KHTDNEVIFXQOKO-CALCHBBNSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
2
Publications
0
Known Names

Molecular Properties

455.5
MW (Da)
5.63
ALogP
4
HBA
1
HBD
54.5
PSA (Ų)
0.55
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H24F3N3O2
MW 455.48
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -1.49

Activity Summary

IC50 1 meas. best 5.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium channel protein type 9 subunit alpha
CHEMBL4296
IC50 5.77 5.77 1700.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 79.0 mL.min-1.g-1 Homo sapiens
CL 223.0 mL.min-1.g-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28684121 10.1016/j.bmcl.2017.06.054 Liver 2
28684121 10.1016/j.bmcl.2017.06.054 Sodium channel protein type 9 subunit alpha 1

Data from ChEMBL 36 via Core Engine