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Compound Detail

CHEMBL1078495

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O=C(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccccc1COc1ccccc1

Basic Information

ChEMBL ID CHEMBL1078495
Phase Preclinical
Structure Type MOL
InChI Key HIIVUZRNMMABGG-NDEPHWFRSA-N
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

467.6
MW (Da)
4.78
ALogP
5
HBA
3
HBD
83.5
PSA (Ų)
0.28
QED
0
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H29N3O3
MW 467.57
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -1.10

Activity Summary

IC50 2 meas. best 5.33
EC50 1 meas. best 7.33

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Beta-3 adrenergic receptor
CHEMBL246
EC50 7.33 7.33 47.0 1
Beta-2 adrenergic receptor
CHEMBL210
IC50 5.33 5.33 4700.0 1
Beta-1 adrenergic receptor
CHEMBL213
IC50 5.01 5.01 9800.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20181479 10.1016/j.bmcl.2010.01.130 Beta-3 adrenergic receptor 2
20181479 10.1016/j.bmcl.2010.01.130 Beta-2 adrenergic receptor 1
20181479 10.1016/j.bmcl.2010.01.130 Beta-1 adrenergic receptor 1

Data from ChEMBL 36 via Core Engine