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Compound Detail

CHEMBL246228

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COc1cc2c(cc1OC)CN(Cc1cnc(N)n3nc(-c4ccco4)nc13)CC2

Basic Information

ChEMBL ID CHEMBL246228
Phase Preclinical
Structure Type MOL
InChI Key HXHKXXRIQOWOHI-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

406.4
MW (Da)
2.54
ALogP
9
HBA
1
HBD
103.9
PSA (Ų)
0.54
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H22N6O3
MW 406.45
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -1.22

Activity Summary

Ki 3 meas. best 7.72

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-2C adrenergic receptor
CHEMBL1916
Ki 7.72 7.72 19.0 1
Alpha-2B adrenergic receptor
CHEMBL1942
Ki 6.43 6.43 370.0 1
Alpha-2A adrenergic receptor
CHEMBL1867
Ki 6.4 6.4 400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17257841 10.1016/j.bmcl.2006.12.094 Alpha-2A adrenergic receptor 1
17257841 10.1016/j.bmcl.2006.12.094 Alpha-2B adrenergic receptor 1
17257841 10.1016/j.bmcl.2006.12.094 Alpha-2C adrenergic receptor 1

Data from ChEMBL 36 via Core Engine