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Compound Detail

CHEMBL245874

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O=C(O)c1ccoc1-c1cccc(NCCNC[C@H](O)c2cccc(Cl)c2)c1

Basic Information

ChEMBL ID CHEMBL245874
Phase Preclinical
Structure Type MOL
InChI Key HMWZLYLDLHPPCO-IBGZPJMESA-N
3
Targets
3
Activities
1
Assay Types
3
PK Parameters
6
Publications
0
Known Names

Molecular Properties

400.9
MW (Da)
4.03
ALogP
5
HBA
4
HBD
94.7
PSA (Ų)
0.40
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 C21H21ClN2O4
MW 400.86
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -0.77

Activity Summary

EC50 3 meas. best 8.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Beta-3 adrenergic receptor
CHEMBL246
EC50 8.1 8.1 7.9 1
Beta-2 adrenergic receptor
CHEMBL210
EC50 5.6 5.6 2511.9 1
Beta-1 adrenergic receptor
CHEMBL213
EC50 5.3 5.3 5011.9 1

Pharmacokinetic Data

Parameter Value Units Species
CL 0.65 mL.min-1.kg-1 Canis lupus familiaris
F 60.0 % Canis lupus familiaris
T1/2 6.1 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17560786 10.1016/j.bmcl.2007.05.069 Mus musculus 4
17560786 10.1016/j.bmcl.2007.05.069 Canis familiaris 3
17560786 10.1016/j.bmcl.2007.05.069 Beta-3 adrenergic receptor 2
17560786 10.1016/j.bmcl.2007.05.069 Beta-2 adrenergic receptor 2
17560786 10.1016/j.bmcl.2007.05.069 Beta-1 adrenergic receptor 2
17560786 10.1016/j.bmcl.2007.05.069 Unchecked 2

Data from ChEMBL 36 via Core Engine