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Compound Detail

CHEMBL202201

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CC(=O)c1c(NC(=O)CO)c2cc(-c3ccc(Cl)cc3)c(-c3ccc(Cl)cc3Cl)nc2n(C)c1=O

Basic Information

ChEMBL ID CHEMBL202201
Phase Preclinical
Structure Type MOL
InChI Key XNWFTRFDCMFMOB-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

530.8
MW (Da)
5.36
ALogP
6
HBA
2
HBD
101.3
PSA (Ų)
0.34
QED
2
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H18Cl3N3O4
MW 530.80
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -0.80

Activity Summary

IC50 2 meas. best 7.34

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cannabinoid receptor 1
CHEMBL218
IC50 7.34 7.34 46.0 1
Cannabinoid receptor 2
CHEMBL253
IC50 5.44 5.44 3600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cannabinoid receptor 1 IC50 = 46.0 nM 7.34 Binding affinity at the CB1 receptor 16263284
Cannabinoid receptor 2 IC50 = 3600.0 nM 5.44 Binding affinity at the CB2 receptor 16263284

Literature References

PubMed DOI Target Context # Activities
16263284 10.1016/j.bmcl.2005.10.028 Cannabinoid receptor 1 1
16263284 10.1016/j.bmcl.2005.10.028 Cannabinoid receptor 2 1

Data from ChEMBL 36 via Core Engine