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Compound Detail

CHEMBL144286

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COc1cc2nc3c(c(N)c2cc1OC)CCC(CNC(=O)c1ccco1)C3

Basic Information

ChEMBL ID CHEMBL144286
Phase Preclinical
Structure Type MOL
InChI Key SGZPGIWGYCHZFH-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

381.4
MW (Da)
2.96
ALogP
6
HBA
2
HBD
99.6
PSA (Ų)
0.70
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 C21H23N3O4
MW 381.43
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -0.64

Activity Summary

Ki 3 meas. best 7.91

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-1B adrenergic receptor
CHEMBL232
Ki 7.91 7.91 12.3 1
Alpha-1D adrenergic receptor
CHEMBL223
Ki 7.8 7.8 15.8 1
Alpha-1A adrenergic receptor
CHEMBL229
Ki 7.02 7.02 95.5 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
14584940 10.1021/jm030952q Alpha-1A adrenergic receptor 2
14584940 10.1021/jm030952q Alpha-1B adrenergic receptor 2
14584940 10.1021/jm030952q Alpha-1D adrenergic receptor 2

Data from ChEMBL 36 via Core Engine