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Compound Detail

CHEMBL545092

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Br.Oc1ccc2c(c1O)CCC2C1=NCCN1

Basic Information

ChEMBL ID CHEMBL545092
Phase Preclinical
Structure Type MOL
InChI Key MSIDWFAXXKQUIV-UHFFFAOYSA-N
Parent Compound CHEMBL1193647
Active Moiety CHEMBL1193647
2
Targets
4
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

218.3
MW (Da)
1.13
ALogP
4
HBA
3
HBD
64.8
PSA (Ų)
0.62
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 C12H15BrN2O2
MW 299.17
Aromatic Rings 1
Heavy Atoms 16
NP-Likeness 1.14

Activity Summary

IC50 2 meas. best 8.48
Ki 2 meas. best 8.51

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adrenergic receptor alpha-2
CHEMBL2093864
Ki 8.51 8.51 3.1 1
Adrenergic receptor alpha-2
CHEMBL2093864
IC50 8.48 8.48 3.3 1
Adrenergic receptor alpha-1
CHEMBL1907610
Ki 6.46 6.46 350.0 1
Adrenergic receptor alpha-1
CHEMBL1907610
IC50 5.8 5.8 1570.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

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

Data from ChEMBL 36 via Core Engine