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Compound Detail

CHEMBL1682274

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CN(Cc1nc(-c2cn(CC3CCOCC3)c3c(Cl)cccc23)no1)[C@@H](CO)C(N)=O

Basic Information

ChEMBL ID CHEMBL1682274
Phase Preclinical
Structure Type MOL
InChI Key YJXIZDCRAMKGID-KRWDZBQOSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

447.9
MW (Da)
2.05
ALogP
8
HBA
2
HBD
119.6
PSA (Ų)
0.54
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H26ClN5O4
MW 447.92
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -1.30

Activity Summary

EC50 1 meas. best 6.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cannabinoid receptor 1
CHEMBL218
EC50 6.6 6.6 251.2 1

Pharmacokinetic Data

Parameter Value Units Species
CL 51000.0 mL.min-1.g-1 Mus musculus
CL 34000.0 mL.min-1.g-1 Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
21316962 10.1016/j.bmcl.2011.01.082 Cannabinoid receptor 1 1
21316962 10.1016/j.bmcl.2011.01.082 No relevant target 1
21316962 10.1016/j.bmcl.2011.01.082 ADMET 1
21316962 10.1016/j.bmcl.2011.01.082 Liver microsomes 1

Data from ChEMBL 36 via Core Engine