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Compound Detail

CHEMBL288809

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COc1cccc2c1CCC1CN(CCn3c(=O)[nH]c4c([nH]c5ccccc54)c3=O)CC21

Basic Information

ChEMBL ID CHEMBL288809
Phase Preclinical
Structure Type MOL
InChI Key WIRHRVAPDHCAEN-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

430.5
MW (Da)
2.84
ALogP
5
HBA
2
HBD
83.1
PSA (Ų)
0.52
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 C25H26N4O3
MW 430.51
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness -0.40

Activity Summary

Ki 3 meas. best 9.13

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-1D adrenergic receptor
CHEMBL326
Ki 9.13 9.13 0.7 1
Alpha-1A adrenergic receptor
CHEMBL319
Ki 9.1 9.1 0.8 1
Alpha-1B adrenergic receptor
CHEMBL3122
Ki 8.65 8.65 2.2 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10780916 10.1021/jm990567u Alpha-1A adrenergic receptor 1
10780916 10.1021/jm990567u Alpha-1B adrenergic receptor 1
10780916 10.1021/jm990567u Alpha-1D adrenergic receptor 1
10780916 10.1021/jm990567u Unchecked 1

Data from ChEMBL 36 via Core Engine