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Compound Detail

CHEMBL540821

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CC(=O)c1cccc(-c2cccc(NC3=NCCN3)c2C)c1.Cl

Basic Information

ChEMBL ID CHEMBL540821
Phase Preclinical
Structure Type MOL
InChI Key AZQGIDYWQSGYHQ-UHFFFAOYSA-N
Parent Compound CHEMBL1190414
Active Moiety CHEMBL1190414
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

293.4
MW (Da)
3.24
ALogP
4
HBA
2
HBD
53.5
PSA (Ų)
0.85
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 C18H20ClN3O
MW 329.83
Aromatic Rings 2
Heavy Atoms 22
NP-Likeness -0.59

Activity Summary

Ki 3 meas. best 7.49

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adrenergic receptor alpha-2
CHEMBL2093864
Ki 7.49 7.49 32.4 1
Adrenergic receptor alpha-1
CHEMBL1907610
Ki 7.05 7.05 89.1 1
5-hydroxytryptamine receptor 7
CHEMBL3223
Ki 6.81 6.81 154.9 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12482437 10.1016/s0960-894x(02)00925-3 5-hydroxytryptamine receptor 7 1
12482437 10.1016/s0960-894x(02)00925-3 Adrenergic receptor alpha-1 1
12482437 10.1016/s0960-894x(02)00925-3 Adrenergic receptor alpha-2 1

Data from ChEMBL 36 via Core Engine