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Compound Detail

CHEMBL3781158

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COc1ccc2c(c1)OC(C)(C)c1cn(CCN3CCN(C(=O)c4ccco4)CC3)nc1-2

Basic Information

ChEMBL ID CHEMBL3781158
Phase Preclinical
Structure Type MOL
InChI Key AQWDNHQURKZWRU-UHFFFAOYSA-N
2
Targets
3
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

436.5
MW (Da)
3.24
ALogP
7
HBA
0
HBD
73.0
PSA (Ų)
0.61
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H28N4O4
MW 436.51
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -1.09

Activity Summary

EC50 2 meas. best 9.06
Ki 1 meas. best 6.16

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
G-protein coupled receptor 55
CHEMBL1075322
EC50 9.06 8.38 0.9 2
Cannabinoid receptor 2
CHEMBL253
Ki 6.16 6.16 698.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26789378 10.1021/acs.jmedchem.5b01331 G-protein coupled receptor 55 4
26789378 10.1021/acs.jmedchem.5b01331 Cannabinoid receptor 2 2
26789378 10.1021/acs.jmedchem.5b01331 Cannabinoid receptor 1 1
26789378 10.1021/acs.jmedchem.5b01331 HEK293 1

Data from ChEMBL 36 via Core Engine