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Compound Detail

CHEMBL54716

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COc1ccccc1N1CCN(CCn2c(=O)c3c(c4ccccc4n3C)n(C)c2=O)CC1

Basic Information

ChEMBL ID CHEMBL54716
Phase Preclinical
Structure Type MOL
InChI Key PORQJIBOYVIPCB-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

447.5
MW (Da)
2.02
ALogP
8
HBA
0
HBD
64.6
PSA (Ų)
0.47
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 C25H29N5O3
MW 447.54
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness -1.11

Activity Summary

Ki 3 meas. best 9.49

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-1A adrenergic receptor
CHEMBL319
Ki 9.49 9.49 0.3 1
5-hydroxytryptamine receptor 1A
CHEMBL273
Ki 8.82 8.82 1.5 1
Adrenergic receptor alpha-2
CHEMBL2095158
Ki 5.66 5.66 2215.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
1648138 10.1021/jm00110a014 Alpha-1A adrenergic receptor 1
1648138 10.1021/jm00110a014 5-hydroxytryptamine receptor 1A 1
1648138 10.1021/jm00110a014 Adrenergic receptor alpha-2 1
1648138 10.1021/jm00110a014 Beta-2 adrenergic receptor 1

Data from ChEMBL 36 via Core Engine