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Compound Detail

CHEMBL1086005

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C=CCc1ccccc1OCC(O)CN1CCC(CN2C(=O)c3cccc4cccc(c34)C2=O)CC1

Basic Information

ChEMBL ID CHEMBL1086005
Phase Preclinical
Structure Type MOL
InChI Key XNVACWCCVJPZOD-UHFFFAOYSA-N
3
Targets
4
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

484.6
MW (Da)
4.32
ALogP
5
HBA
1
HBD
70.1
PSA (Ų)
0.36
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 C30H32N2O4
MW 484.60
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -0.69

Activity Summary

Ki 3 meas. best 7.1
EC50 1 meas. best 5.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Beta-2 adrenergic receptor
CHEMBL210
Ki 7.1 7.1 80.0 1
Beta-1 adrenergic receptor
CHEMBL213
Ki 7.1 7.1 80.0 1
Beta-3 adrenergic receptor
CHEMBL246
Ki 6.39 6.39 409.0 1
Beta-3 adrenergic receptor
CHEMBL246
EC50 5.62 5.62 2400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20434333 10.1016/j.bmcl.2010.04.009 Beta-3 adrenergic receptor 3
20434333 10.1016/j.bmcl.2010.04.009 Beta-1 adrenergic receptor 2
20434333 10.1016/j.bmcl.2010.04.009 Beta-2 adrenergic receptor 1

Data from ChEMBL 36 via Core Engine