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Compound Detail

CHEMBL2029730

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CNC(=O)CCCN(C)C(=O)c1ccc2c(c1)c1c(n2C)CC[C@H](C2CCOCC2)C1

Basic Information

ChEMBL ID CHEMBL2029730
Phase Preclinical
Structure Type MOL
InChI Key LYYAOAAEQUTERQ-SFHVURJKSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
5
Publications
0
Known Names

Molecular Properties

425.6
MW (Da)
3.31
ALogP
4
HBA
1
HBD
63.6
PSA (Ų)
0.77
QED
0
Ro5 Violations
6
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 2
Heavy Atoms 31
NP-Likeness -0.72

Activity Summary

Ki 1 meas. best 6.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cannabinoid receptor 1
CHEMBL218
Ki 6.24 6.24 576.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 31.0 mL.min-1.g-1 Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cannabinoid receptor 1 Ki = 576.0 nM 6.24 Displacement of [3H]CP55940 from human CB1 receptor expressed in HEK293 cells 22607668

Literature References

PubMed DOI Target Context # Activities
22607668 10.1016/j.bmcl.2012.04.128 Cannabinoid receptor 1 3
22607668 10.1016/j.bmcl.2012.04.128 Cannabinoid receptor 2 1
22607668 10.1016/j.bmcl.2012.04.128 Liver microsomes 1
22607668 10.1016/j.bmcl.2012.04.128 Voltage-gated inwardly rectifying potassium channel KCNH2 1
22607668 10.1016/j.bmcl.2012.04.128 No relevant target 1

Data from ChEMBL 36 via Core Engine