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Compound Detail

CHEMBL243228

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CC(C)Oc1ccccc1N1CCN(C2CCC(N3C(=O)c4cccnc4C3=O)CC2)CC1

Basic Information

ChEMBL ID CHEMBL243228
Phase Preclinical
Structure Type MOL
InChI Key BXZWRAYRDLNDSN-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

448.6
MW (Da)
3.60
ALogP
6
HBA
0
HBD
66.0
PSA (Ų)
0.65
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 C26H32N4O3
MW 448.57
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness -1.00

Activity Summary

Ki 3 meas. best 9.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-1A adrenergic receptor
CHEMBL229
Ki 9.1 9.1 0.8 1
Alpha-1D adrenergic receptor
CHEMBL223
Ki 8.82 8.82 1.5 1
Alpha-1B adrenergic receptor
CHEMBL232
Ki 7.35 7.35 44.6 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17254786 10.1016/j.bmcl.2006.12.111 Alpha-1A adrenergic receptor 1
17254786 10.1016/j.bmcl.2006.12.111 Alpha-1B adrenergic receptor 1
17254786 10.1016/j.bmcl.2006.12.111 Alpha-1D adrenergic receptor 1
17254786 10.1016/j.bmcl.2006.12.111 Adrenergic receptors; alpha-1 A & B 1
17254786 10.1016/j.bmcl.2006.12.111 Unchecked 1

Data from ChEMBL 36 via Core Engine