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Compound Detail

CHEMBL556852

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CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccc(N)cc3)cc2)cc1OC1CCCCC1

Basic Information

ChEMBL ID CHEMBL556852
Phase Preclinical
Structure Type MOL
InChI Key VTKMLZIGOBSURB-NDEPHWFRSA-N
1
Targets
1
Activities
1
Assay Types
5
PK Parameters
4
Publications
0
Known Names

Molecular Properties

551.7
MW (Da)
4.20
ALogP
7
HBA
4
HBD
130.8
PSA (Ų)
0.21
QED
1
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H37N3O5S
MW 551.71
Aromatic Rings 3
Heavy Atoms 39
NP-Likeness -0.30

Activity Summary

EC50 1 meas. best 9.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Beta-3 adrenergic receptor
CHEMBL246
EC50 9.3 9.3 0.5 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 212.5 ng.hr.mL-1 Canis lupus familiaris
CL 5.0 mL.min-1.kg-1 Canis lupus familiaris
Cmax 31.72 nM Canis lupus familiaris
F 68.0 % Canis lupus familiaris
T1/2 5.7 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19608416 10.1016/j.bmcl.2009.06.083 Canis familiaris 5
19608416 10.1016/j.bmcl.2009.06.083 Beta-3 adrenergic receptor 1
19608416 10.1016/j.bmcl.2009.06.083 Beta-2 adrenergic receptor 1
19608416 10.1016/j.bmcl.2009.06.083 Beta-1 adrenergic receptor 1

Data from ChEMBL 36 via Core Engine