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Compound Detail

CHEMBL303464

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COc1ccccc1N1CCN(CCn2nc(-c3ccccc3)c3c(C)onc3c2=O)CC1

Basic Information

ChEMBL ID CHEMBL303464
Phase Preclinical
Structure Type MOL
InChI Key VBMWRWYJANTSGH-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

445.5
MW (Da)
3.19
ALogP
8
HBA
0
HBD
76.6
PSA (Ų)
0.45
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H27N5O3
MW 445.52
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness -1.63

Activity Summary

Ki 4 meas. best 8.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-1A adrenergic receptor
CHEMBL229
Ki 8.85 8.85 1.4 1
Alpha-1D adrenergic receptor
CHEMBL223
Ki 8.82 8.82 1.5 1
Alpha-1B adrenergic receptor
CHEMBL232
Ki 7.51 7.51 31.1 1
Adrenergic receptor alpha-1
CHEMBL1907610
Ki 6.83 6.83 147.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11405649 10.1021/jm010821u Adrenergic receptor alpha-1 1
12825930 10.1021/jm0307741 Alpha-1A adrenergic receptor 1
12825930 10.1021/jm0307741 Alpha-1B adrenergic receptor 1
12825930 10.1021/jm0307741 Alpha-1D adrenergic receptor 1
12825930 10.1021/jm0307741 Adrenergic receptor alpha-1 1

Data from ChEMBL 36 via Core Engine