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Compound Detail

CHEMBL217758

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O=C(NC1CCN(C(=O)C(F)(F)F)CC1)NC12CC3CC(CC(C3)C1)C2

Basic Information

ChEMBL ID CHEMBL217758
Phase Preclinical
Structure Type MOL
InChI Key SZMZZNRRWJYDIB-UHFFFAOYSA-N
2
Targets
4
Activities
1
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

373.4
MW (Da)
2.81
ALogP
2
HBA
2
HBD
61.4
PSA (Ų)
0.78
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H26F3N3O2
MW 373.42
Aromatic Rings 0
Heavy Atoms 26
NP-Likeness -1.35

Activity Summary

IC50 4 meas. best 8.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Epoxide hydrolase 1
CHEMBL1968
IC50 8.96 8.865 1.1 2
Bifunctional epoxide hydrolase 2
CHEMBL2409
IC50 8.96 8.96 1.1 2

Pharmacokinetic Data

Parameter Value Units Species
AUC 20.54 ng.hr.mL-1 Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16870439 10.1016/j.bmcl.2006.07.009 Bifunctional epoxide hydrolase 2 1
16870439 10.1016/j.bmcl.2006.07.009 Canis familiaris 1
22079754 10.1016/j.bmcl.2011.10.074 Bifunctional epoxide hydrolase 2 1

Data from ChEMBL 36 via Core Engine