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Compound Detail

CHEMBL214435

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O=C1CC[C@@H](CN[C@H]2CC[C@@H](OCc3cc(C(F)(F)F)cc(C(F)(F)F)c3)[C@@H]2c2ccccc2)N1

Basic Information

ChEMBL ID CHEMBL214435
Phase Preclinical
Structure Type MOL
InChI Key XFSJGZVARSALDD-NNXSRULWSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

500.5
MW (Da)
5.42
ALogP
3
HBA
2
HBD
50.4
PSA (Ų)
0.50
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H26F6N2O2
MW 500.48
Aromatic Rings 2
Heavy Atoms 35
NP-Likeness -0.09

Activity Summary

IC50 1 meas. best 6.58

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Substance-P receptor
CHEMBL249
IC50 6.58 6.58 260.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Substance-P receptor IC50 = 260.0 nM 6.58 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

Data from ChEMBL 36 via Core Engine