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Compound Detail

CHEMBL479049

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COc1cc2c(cc1CN[C@H]1CCCN[C@H]1c1ccccc1)C(C(F)(F)F)CCC2

Basic Information

ChEMBL ID CHEMBL479049
Phase Preclinical
Structure Type MOL
InChI Key UOYMONBFUXQTMB-ZXNYFWILSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

418.5
MW (Da)
5.26
ALogP
3
HBA
2
HBD
33.3
PSA (Ų)
0.69
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H29F3N2O
MW 418.50
Aromatic Rings 2
Heavy Atoms 30
NP-Likeness -0.08

Activity Summary

IC50 1 meas. best 9.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Substance-P receptor
CHEMBL249
IC50 9.3 9.3 0.5 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Substance-P receptor IC50 = 0.5 nM 9.3 Displacement of [3H]spiperone from NK1 receptor in human IM9 cells 18640044

Literature References

PubMed DOI Target Context # Activities
18640044 10.1016/j.bmc.2008.06.047 Mustela putorius furo 4
18640044 10.1016/j.bmc.2008.06.047 Gerbillinae 3
18640044 10.1016/j.bmc.2008.06.047 Substance-P receptor 2
18640044 10.1016/j.bmc.2008.06.047 Cytochrome P450 2D6 2
18640044 10.1016/j.bmc.2008.06.047 Liver microsomes 1

Data from ChEMBL 36 via Core Engine