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Compound Detail

CHEMBL3781521

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

Basic Information

ChEMBL ID CHEMBL3781521
Phase Preclinical
Structure Type MOL
InChI Key PUTMHKMKVABQQZ-UHFFFAOYSA-N
2
Targets
3
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

426.6
MW (Da)
3.38
ALogP
6
HBA
0
HBD
59.8
PSA (Ų)
0.75
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 C24H34N4O3
MW 426.56
Aromatic Rings 2
Heavy Atoms 31
NP-Likeness -0.95

Activity Summary

EC50 2 meas. best 9.16
Ki 1 meas. best 5.19

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
G-protein coupled receptor 55
CHEMBL1075322
EC50 9.16 8.41 0.7 2
Cannabinoid receptor 2
CHEMBL253
Ki 5.19 5.19 6392.0 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