Skip to main content
Free research Free research Free compound review with research home and workspace preview
Quick search ChEMBL 36
Compound Detail

CHEMBL478392

Enter ChEMBL ID:
Free Research Context This compound will appear in recent viewed items on the research home for this browser.
Research home View demo workspace
COc1cc2c(cc1CN[C@H]1CCCN[C@H]1c1ccccc1)[C@](C)(C(F)(F)F)OCC2

Basic Information

ChEMBL ID CHEMBL478392
Phase Preclinical
Structure Type MOL
InChI Key ODEBBNRINYMIRX-ACIOBRDBSA-N
3
Targets
3
Activities
2
Assay Types
4
PK Parameters
8
Publications
0
Known Names

Molecular Properties

434.5
MW (Da)
4.63
ALogP
4
HBA
2
HBD
42.5
PSA (Ų)
0.72
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H29F3N2O2
MW 434.50
Aromatic Rings 2
Heavy Atoms 31
NP-Likeness 0.02

Activity Summary

IC50 2 meas. best 7.32
Ki 1 meas. best 9.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Substance-P receptor
CHEMBL249
Ki 9.7 9.7 0.2 1
Sodium channel protein type 2 subunit alpha
CHEMBL3399
IC50 7.32 7.32 48.0 1
Unchecked
CHEMBL612545
IC50 6.79 6.79 164.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 11.0 mL.min-1.kg-1 Rattus norvegicus
CL 31.67 mL.min-1.kg-1 Canis lupus familiaris
T1/2 8.8 hr Rattus norvegicus
T1/2 3.8 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18640044 10.1016/j.bmc.2008.06.047 Cytochrome P450 2D6 3
18640044 10.1016/j.bmc.2008.06.047 Substance-P receptor 3
18640044 10.1016/j.bmc.2008.06.047 Rattus norvegicus 3
18640044 10.1016/j.bmc.2008.06.047 Canis familiaris 3
18640044 10.1016/j.bmc.2008.06.047 Gerbillinae 1
18640044 10.1016/j.bmc.2008.06.047 Mustela putorius furo 1
18640044 10.1016/j.bmc.2008.06.047 Unchecked 1
18640044 10.1016/j.bmc.2008.06.047 Sodium channel protein type 2 subunit alpha 1

Data from ChEMBL 36 via Core Engine