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Compound Detail

CHEMBL154980

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COc1cc2nc(NCCNC(=O)c3ccco3)nc(N)c2cc1OC

Basic Information

ChEMBL ID CHEMBL154980
Phase Preclinical
Structure Type MOL
InChI Key AXVOGPRNZOJHRV-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

357.4
MW (Da)
1.66
ALogP
8
HBA
3
HBD
124.5
PSA (Ų)
0.55
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H19N5O4
MW 357.37
Aromatic Rings 3
Heavy Atoms 26
NP-Likeness -1.27

Activity Summary

Kd 2 meas. best 8.28

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adrenergic receptor alpha-1
CHEMBL1907610
Kd 8.28 8.28 5.2 1
Adrenergic receptor alpha-2
CHEMBL2093864
Kd 5.73 5.73 1862.1 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
2562855 10.1021/jm00121a011 Adrenergic receptor alpha-1 1
2562855 10.1021/jm00121a011 Adrenergic receptor alpha-2 1
2562855 10.1021/jm00121a011 Adrenergic receptor alpha 1

Data from ChEMBL 36 via Core Engine