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Compound Detail

CHEMBL545387

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COc1cc2nc(N(C)CCOc3c(OC)cccc3OC)nc(N)c2cc1OC.Cl

Basic Information

ChEMBL ID CHEMBL545387
Phase Preclinical
Structure Type MOL
InChI Key KUWDLLSNJGKPKO-UHFFFAOYSA-N
Parent Compound CHEMBL1193909
Active Moiety CHEMBL1193909
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

414.5
MW (Da)
2.76
ALogP
9
HBA
1
HBD
101.2
PSA (Ų)
0.57
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H27ClN4O5
MW 450.92
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -0.55

Activity Summary

Kd 2 meas. best 7.86

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adrenergic receptor alpha-1
CHEMBL1907610
Kd 7.86 7.86 13.8 1
Adrenergic receptor alpha-2
CHEMBL2093864
Kd 5.91 5.91 1230.3 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
2863379 10.1021/jm00147a042 Adrenergic receptor alpha-1 1
2863379 10.1021/jm00147a042 Adrenergic receptor alpha-2 1
2863379 10.1021/jm00147a042 Unchecked 1

Data from ChEMBL 36 via Core Engine