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Compound Detail

CHEMBL411234

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O=C(O)c1ccc(Oc2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)cc1

Basic Information

ChEMBL ID CHEMBL411234
Phase Preclinical
Structure Type MOL
InChI Key RKZRYYZYWFDKCO-QFIPXVFZSA-N
1
Targets
2
Activities
1
Assay Types
5
PK Parameters
6
Publications
0
Known Names

Molecular Properties

411.9
MW (Da)
4.70
ALogP
4
HBA
3
HBD
78.8
PSA (Ų)
0.44
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 C23H22ClNO4
MW 411.89
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -0.60

Activity Summary

EC50 2 meas. best 7.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Beta-3 adrenergic receptor
CHEMBL246
EC50 7.0 7.0 100.0 2

Pharmacokinetic Data

Parameter Value Units Species
AUC 2469.9 ng.hr.mL-1 Canis lupus familiaris
CL 4.1 mL.min-1.kg-1 Canis lupus familiaris
Cmax 573.21 nM Canis lupus familiaris
F 40.0 % Canis lupus familiaris
T1/2 6.2 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18307290 10.1021/jm701324c Canis familiaris 7
18307290 10.1021/jm701324c Beta-3 adrenergic receptor 2
18307290 10.1021/jm701324c Beta-1 adrenergic receptor 1
18307290 10.1021/jm701324c Unchecked 1
18752946 10.1016/j.bmcl.2008.08.009 Beta-3 adrenergic receptor 1
18752946 10.1016/j.bmcl.2008.08.009 Beta-1 adrenergic receptor 1

Data from ChEMBL 36 via Core Engine