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Compound Detail

CHEMBL377916

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CN(CC[C@@H]1CC[C@H](OCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)[C@H]1c1ccccc1)Cc1n[nH]c(O)n1

Basic Information

ChEMBL ID CHEMBL377916
Phase Preclinical
Structure Type MOL
InChI Key WKVJTXKYRCNGPX-HARLFGEKSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

542.5
MW (Da)
6.15
ALogP
5
HBA
2
HBD
74.3
PSA (Ų)
0.32
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H28F6N4O2
MW 542.52
Aromatic Rings 3
Heavy Atoms 38
NP-Likeness -0.48

Activity Summary

IC50 1 meas. best 8.31

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Substance-P receptor
CHEMBL249
IC50 8.31 8.31 4.9 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Substance-P receptor IC50 = 4.9 nM 8.31 Displacement of [125I]SP from human cloned NK1 receptor expressed in CHO cells 16824752

Literature References

PubMed DOI Target Context # Activities
16824752 10.1016/j.bmcl.2006.06.035 Substance-P receptor 1
16824752 10.1016/j.bmcl.2006.06.035 No relevant target 1

Data from ChEMBL 36 via Core Engine