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Compound Detail

CHEMBL2397139

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CNC(=O)c1ccc(O[C@H]2CC[C@H](NC(=O)NC34CC5CC(CC(C5)C3)C4)CC2)cc1

Basic Information

ChEMBL ID CHEMBL2397139
Phase Preclinical
Structure Type MOL
InChI Key UHCRWCSTKBZBFL-MGAMQBSKSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

425.6
MW (Da)
4.00
ALogP
3
HBA
3
HBD
79.5
PSA (Ų)
0.67
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H35N3O3
MW 425.57
Aromatic Rings 1
Heavy Atoms 31
NP-Likeness -0.75

Activity Summary

IC50 3 meas. best 9.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Bifunctional epoxide hydrolase 2
CHEMBL2409
IC50 9.3 9.3 0.5 2
Unchecked
CHEMBL612545
IC50 8.62 8.62 2.4 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
25479771 10.1016/j.bmcl.2014.11.053 Unchecked 2
25479771 10.1016/j.bmcl.2014.11.053 Liver microsome 2
25479771 10.1016/j.bmcl.2014.11.053 ADMET 2
23726028 10.1016/j.bmcl.2013.05.011 HUVEC 1
23726028 10.1016/j.bmcl.2013.05.011 Huh-7 1
23726028 10.1016/j.bmcl.2013.05.011 HepG2 1
23726028 10.1016/j.bmcl.2013.05.011 RAF proto-oncogene serine/threonine-protein kinase 1
23726028 10.1016/j.bmcl.2013.05.011 Bifunctional epoxide hydrolase 2 1
25479771 10.1016/j.bmcl.2014.11.053 No relevant target 1

Data from ChEMBL 36 via Core Engine