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Compound Detail

CHEMBL554004

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Br.Oc1ccc2c(c1O)CCCCC2C1=NCCN1

Basic Information

ChEMBL ID CHEMBL554004
Phase Preclinical
Structure Type MOL
InChI Key PFYZCTXCJPDITQ-UHFFFAOYSA-N
Parent Compound CHEMBL1195183
Active Moiety CHEMBL1195183
2
Targets
4
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

246.3
MW (Da)
1.91
ALogP
4
HBA
3
HBD
64.8
PSA (Ų)
0.52
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C14H19BrN2O2
MW 327.22
Aromatic Rings 1
Heavy Atoms 18
NP-Likeness 0.91

Activity Summary

IC50 2 meas. best 5.38
Ki 2 meas. best 5.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adrenergic receptor alpha-2
CHEMBL2093864
Ki 5.4 5.4 4000.0 1
Adrenergic receptor alpha-2
CHEMBL2093864
IC50 5.38 5.38 4200.0 1
Adrenergic receptor alpha-1
CHEMBL1907610
Ki 4.89 4.89 13000.0 1
Adrenergic receptor alpha-1
CHEMBL1907610
IC50 4.25 4.25 56000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
2870187 10.1021/jm00154a006 Adrenergic receptor alpha-1 3
2870187 10.1021/jm00154a006 Adrenergic receptor alpha-2 3
2870187 10.1021/jm00154a006 Oryctolagus cuniculus 2
2870187 10.1021/jm00154a006 Canis familiaris 2

Data from ChEMBL 36 via Core Engine