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Compound Detail

CHEMBL493675

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CC(Oc1ccccc1/C=N/O)C1=NCCN1

Basic Information

ChEMBL ID CHEMBL493675
Phase Preclinical
Structure Type MOL
InChI Key JDVBCCBWSXJBJH-OVCLIPMQSA-N
3
Targets
6
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

233.3
MW (Da)
1.26
ALogP
5
HBA
2
HBD
66.2
PSA (Ų)
0.47
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C12H15N3O2
MW 233.27
Aromatic Rings 1
Heavy Atoms 17
NP-Likeness -0.44

Activity Summary

EC50 3 meas. best 6.9
Ki 3 meas. best 6.54

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-2C adrenergic receptor
CHEMBL1916
EC50 6.9 6.9 125.9 1
Alpha-2A adrenergic receptor
CHEMBL1867
Ki 6.54 6.54 288.4 1
Alpha-2A adrenergic receptor
CHEMBL1867
EC50 6.3 6.3 501.2 1
Alpha-2B adrenergic receptor
CHEMBL1942
Ki 6.15 6.15 708.0 1
Alpha-2C adrenergic receptor
CHEMBL1916
Ki 6.04 6.04 912.0 1
Alpha-2B adrenergic receptor
CHEMBL1942
EC50 5.4 5.4 3981.1 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18578476 10.1021/jm800250z Alpha-2A adrenergic receptor 3
18578476 10.1021/jm800250z Alpha-2B adrenergic receptor 3
18578476 10.1021/jm800250z Alpha-2C adrenergic receptor 3

Data from ChEMBL 36 via Core Engine