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Compound Detail

CHEMBL459908

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Cl.ClC[C@@H]1CO[C@@](CCc2ccc(Cl)cc2)(Cn2ccnc2)O1.O

Basic Information

ChEMBL ID CHEMBL459908
Phase Preclinical
Structure Type MOL
InChI Key LAXAFUZCRXILAV-UWGSCQAASA-N
Parent Compound CHEMBL1186362
Active Moiety CHEMBL1186362
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

341.2
MW (Da)
3.52
ALogP
4
HBA
0
HBD
36.3
PSA (Ų)
0.75
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H21Cl3N2O3
MW 395.71
Aromatic Rings 2
Heavy Atoms 22
NP-Likeness -0.45

Activity Summary

IC50 2 meas. best 5.46

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Heme oxygenase 1
CHEMBL5035
IC50 5.46 5.46 3500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Heme oxygenase 1 IC50 = 3500.0 nM 5.46 Inhibition of heme oxygenase-1 in Sprague-Dawley rat spleen microsomal fraction ... 19268600

Literature References

PubMed DOI Target Context # Activities
19268600 10.1016/j.bmc.2009.01.078 Heme oxygenase 1 1
19268600 10.1016/j.bmc.2009.01.078 Heme oxygenase 2 1
19268600 10.1016/j.bmc.2009.01.078 Unchecked 1

Data from ChEMBL 36 via Core Engine