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Compound Detail

CHEMBL1242444

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COc1ccccc1N1CCN(C[C@H]2CO[C@](CN3CCCC3=O)(c3ccccc3)O2)CC1

Basic Information

ChEMBL ID CHEMBL1242444
Phase Preclinical
Structure Type MOL
InChI Key AOZOBKDTJZCKJE-NVQXNPDNSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

451.6
MW (Da)
2.71
ALogP
6
HBA
0
HBD
54.5
PSA (Ų)
0.65
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H33N3O4
MW 451.57
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness -0.54

Activity Summary

Ki 4 meas. best 8.86

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-1A adrenergic receptor
CHEMBL229
Ki 8.86 8.86 1.4 1
5-hydroxytryptamine receptor 1A
CHEMBL214
Ki 8.16 8.16 6.9 1
Alpha-1D adrenergic receptor
CHEMBL223
Ki 7.87 7.87 13.5 1
Alpha-1B adrenergic receptor
CHEMBL232
Ki 6.76 6.76 173.8 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20605276 10.1016/j.ejmech.2010.05.023 Unchecked 7
20605276 10.1016/j.ejmech.2010.05.023 Alpha-1A adrenergic receptor 2
20605276 10.1016/j.ejmech.2010.05.023 Alpha-1B adrenergic receptor 2
20605276 10.1016/j.ejmech.2010.05.023 Alpha-1D adrenergic receptor 2
20605276 10.1016/j.ejmech.2010.05.023 5-hydroxytryptamine receptor 1A 2

Data from ChEMBL 36 via Core Engine