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Compound Detail

CHEMBL277004

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O=C(NCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1c(CO)nc2ccccc2c1-c1ccccc1

Basic Information

ChEMBL ID CHEMBL277004
Phase Preclinical
Structure Type MOL
InChI Key YEJPDQREQRKUNO-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

504.4
MW (Da)
6.36
ALogP
3
HBA
2
HBD
62.2
PSA (Ų)
0.31
QED
2
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H18F6N2O2
MW 504.43
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -0.80

Activity Summary

IC50 2 meas. best 6.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Substance-P receptor
CHEMBL249
IC50 6.64 6.64 227.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Substance-P receptor IC50 = 227.0 nM 6.64 Displacement of [125I]BH-SP from human recombinant NK1 receptor expressed in CHO... 21421318

Literature References

PubMed DOI Target Context # Activities
14998319 10.1021/jm034219a NON-PROTEIN TARGET 4
14998319 10.1021/jm034219a Substance-P receptor 2
21421318 10.1016/j.bmc.2011.02.031 Substance-P receptor 1

Data from ChEMBL 36 via Core Engine