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Compound Detail

CHEMBL1672128

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COc1cccc2c1CC(C(=O)N[C@H]1C[C@@H]1c1ccccc1)CC2

Basic Information

ChEMBL ID CHEMBL1672128
Phase Preclinical
Structure Type MOL
InChI Key GWFJJCPRJHUFIT-QIONWKSUSA-N
2
Targets
3
Activities
1
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

321.4
MW (Da)
3.47
ALogP
2
HBA
1
HBD
38.3
PSA (Ų)
0.94
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H23NO2
MW 321.42
Aromatic Rings 2
Heavy Atoms 24
NP-Likeness -0.29

Activity Summary

IC50 3 meas. best 8.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Bifunctional epoxide hydrolase 2
CHEMBL5669
IC50 8.52 8.52 3.0 1
Bifunctional epoxide hydrolase 2
CHEMBL2409
IC50 8.33 8.26 4.7 2

Pharmacokinetic Data

Parameter Value Units Species
CL 100.0 mL.min-1.g-1 Homo sapiens
CL 100.0 mL.min-1.g-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
21192659 10.1021/jm101273e Bifunctional epoxide hydrolase 2 3
21192659 10.1021/jm101273e Liver microsomes 2
21192659 10.1021/jm101273e No relevant target 1
21192659 10.1021/jm101273e Cytochrome P450 2C19 1

Data from ChEMBL 36 via Core Engine