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Compound Detail

CHEMBL3400594

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Cl.O=C1CCCN1CCCCN1CCN(C(c2ccc(F)cc2)c2ccc(F)cc2)CC1

Basic Information

ChEMBL ID CHEMBL3400594
Phase Preclinical
Structure Type MOL
InChI Key GWZKQAZNJFCKIR-UHFFFAOYSA-N
Parent Compound CHEMBL3547015
Active Moiety CHEMBL3547015
4
Targets
4
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

427.5
MW (Da)
4.07
ALogP
3
HBA
0
HBD
26.8
PSA (Ų)
0.59
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H32ClF2N3O
MW 464.00
Aromatic Rings 2
Heavy Atoms 31
NP-Likeness -1.30

Activity Summary

EC50 2 meas. best 6.88
Ki 2 meas. best 7.07

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adrenergic receptor alpha-1
CHEMBL1907610
Ki 7.07 7.07 85.1 1
Alpha-1B adrenergic receptor
CHEMBL232
EC50 6.88 6.88 131.1 1
Alpha-1A adrenergic receptor
CHEMBL229
EC50 6.48 6.48 329.1 1
Adrenergic receptor alpha-2
CHEMBL2093864
Ki 5.92 5.92 1202.3 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
25813897 10.1016/j.bmc.2015.03.009 Adrenergic receptor alpha-1 1
25813897 10.1016/j.bmc.2015.03.009 Adrenergic receptor alpha-2 1
25813897 10.1016/j.bmc.2015.03.009 Alpha-1A adrenergic receptor 1
25813897 10.1016/j.bmc.2015.03.009 Alpha-1B adrenergic receptor 1

Data from ChEMBL 36 via Core Engine