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Compound Detail

CHEMBL165350

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Cc1nc2ccc(Br)cn2c(=O)c1CCN1CCc2oc3ccccc3c2C1

Basic Information

ChEMBL ID CHEMBL165350
Phase Preclinical
Structure Type MOL
InChI Key BRKWIMBSEICBCU-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

438.3
MW (Da)
4.11
ALogP
5
HBA
0
HBD
50.8
PSA (Ų)
0.48
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H20BrN3O2
MW 438.33
Aromatic Rings 4
Heavy Atoms 28
NP-Likeness -1.35

Activity Summary

IC50 4 meas. best 9.45

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-2A adrenergic receptor
CHEMBL1867
IC50 9.45 9.45 0.4 1
Alpha-2C adrenergic receptor
CHEMBL1916
IC50 9.16 9.16 0.7 1
Alpha-2B adrenergic receptor
CHEMBL1942
IC50 8.87 8.87 1.3 1
Alpha-1A adrenergic receptor
CHEMBL229
IC50 6.05 6.05 891.2 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10636247 10.1016/s0960-894x(99)00591-0 Rattus norvegicus 2
10636247 10.1016/s0960-894x(99)00591-0 Alpha-1A adrenergic receptor 1
10636247 10.1016/s0960-894x(99)00591-0 Alpha-2A adrenergic receptor 1
10636247 10.1016/s0960-894x(99)00591-0 Alpha-2B adrenergic receptor 1
10636247 10.1016/s0960-894x(99)00591-0 Alpha-2C adrenergic receptor 1

Data from ChEMBL 36 via Core Engine