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Compound Detail

CHEMBL230490

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C[C@H](Cc1cccc(CC(=O)NCc2ccc(Cl)c(Cl)c2)c1)NC[C@H](O)c1ccc(O)c(CO)c1

Basic Information

ChEMBL ID CHEMBL230490
Phase Preclinical
Structure Type MOL
InChI Key AOJZKEWJJYTGIX-QUGAMOGWSA-N
1
Targets
2
Activities
1
Assay Types
4
PK Parameters
15
Publications
0
Known Names

Molecular Properties

517.5
MW (Da)
4.30
ALogP
5
HBA
5
HBD
101.8
PSA (Ų)
0.26
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 C27H30Cl2N2O4
MW 517.45
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -0.43

Activity Summary

EC50 2 meas. best 10.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Beta-2 adrenergic receptor
CHEMBL210
EC50 10.62 9.79 0.0 2

Pharmacokinetic Data

Parameter Value Units Species
CL 123.0 mL.min-1.kg-1 Rattus norvegicus
CL 440.0 mL.min-1.g-1 Homo sapiens
T1/2 0.06667 hr Homo sapiens
T1/2 1.5 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17498952 10.1016/j.bmcl.2007.04.081 Rattus norvegicus 3
17498952 10.1016/j.bmcl.2007.04.081 Beta-2 adrenergic receptor 2
20804199 10.1021/jm1005989 NON-PROTEIN TARGET 2
21075627 10.1016/j.bmcl.2010.10.132 Beta-2 adrenergic receptor 2
17498952 10.1016/j.bmcl.2007.04.081 No relevant target 1
17498952 10.1016/j.bmcl.2007.04.081 Caco-2 1
17498952 10.1016/j.bmcl.2007.04.081 Liver microsomes 1
18226900 10.1016/j.bmcl.2008.01.034 No relevant target 1
18226900 10.1016/j.bmcl.2008.01.034 Beta-2 adrenergic receptor 1
18226900 10.1016/j.bmcl.2008.01.034 Unchecked 1
18226900 10.1016/j.bmcl.2008.01.034 Liver microsomes 1
20804199 10.1021/jm1005989 No relevant target 1
20804199 10.1021/jm1005989 Unchecked 1
20804199 10.1021/jm1005989 Beta-2 adrenergic receptor 1
21075627 10.1016/j.bmcl.2010.10.132 Liver microsomes 1

Data from ChEMBL 36 via Core Engine