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Compound Detail

CHEMBL515935

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COc1ccc(C(C)(OC)C(F)(F)F)cc1CN[C@H]1CCCN[C@H]1c1ccccc1

Basic Information

ChEMBL ID CHEMBL515935
Phase Preclinical
Structure Type MOL
InChI Key KDMRETSUDYJFOO-QUCQDJGISA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

422.5
MW (Da)
4.70
ALogP
4
HBA
2
HBD
42.5
PSA (Ų)
0.68
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H29F3N2O2
MW 422.49
Aromatic Rings 2
Heavy Atoms 30
NP-Likeness -0.27

Activity Summary

IC50 1 meas. best 9.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Substance-P receptor
CHEMBL249
IC50 9.05 9.05 0.9 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Substance-P receptor IC50 = 0.9 nM 9.05 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 Gerbillinae 3
18640044 10.1016/j.bmc.2008.06.047 Substance-P receptor 1
18640044 10.1016/j.bmc.2008.06.047 Cytochrome P450 2D6 1
18640044 10.1016/j.bmc.2008.06.047 Mustela putorius furo 1

Data from ChEMBL 36 via Core Engine