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Compound Detail

CHEMBL220515

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COc1ccc(Cl)cc1N1CCN(CCn2c(C)nc3c([nH]c4ccccc43)c2=O)CC1

Basic Information

ChEMBL ID CHEMBL220515
Phase Preclinical
Structure Type MOL
InChI Key AMDQVJAWEJXJFN-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

452.0
MW (Da)
3.67
ALogP
6
HBA
1
HBD
66.4
PSA (Ų)
0.50
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 C24H26ClN5O2
MW 451.96
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness -1.40

Activity Summary

Ki 3 meas. best 9.78

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-1D adrenergic receptor
CHEMBL223
Ki 9.78 9.78 0.2 1
Alpha-1A adrenergic receptor
CHEMBL229
Ki 8.88 8.88 1.3 1
Alpha-1B adrenergic receptor
CHEMBL232
Ki 8.35 8.35 4.5 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17027264 10.1016/j.bmcl.2006.09.034 Alpha-1A adrenergic receptor 2
17027264 10.1016/j.bmcl.2006.09.034 Alpha-1B adrenergic receptor 2
17027264 10.1016/j.bmcl.2006.09.034 Alpha-1D adrenergic receptor 2

Data from ChEMBL 36 via Core Engine