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Compound Detail

CHEMBL611620

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C[C@@H]1CC[C@H](C)N1c1ccc(-c2cncc3ccccc23)nn1

Basic Information

ChEMBL ID CHEMBL611620
Phase Preclinical
Structure Type MOL
InChI Key LAVIXOKYHRWFDZ-OKILXGFUSA-N
2
Targets
2
Activities
1
Assay Types
8
PK Parameters
7
Publications
0
Known Names

Molecular Properties

304.4
MW (Da)
4.07
ALogP
4
HBA
0
HBD
41.9
PSA (Ų)
0.72
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H20N4
MW 304.40
Aromatic Rings 3
Heavy Atoms 23
NP-Likeness -1.07

Activity Summary

EC50 2 meas. best 8.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cannabinoid receptor 2
CHEMBL253
EC50 8.0 8.0 10.0 1
Cannabinoid receptor 1
CHEMBL218
EC50 5.1 5.1 7943.3 1

Pharmacokinetic Data

Parameter Value Units Species
CL 3.7 mL.min-1.g-1 Rattus norvegicus
CL 57.0 mL.min-1.kg-1 Rattus norvegicus
Cmax 6600.0 nM Rattus norvegicus
Cmax 11000.0 nM Rattus norvegicus
Cmax 340.0 nM Rattus norvegicus
F 26.0 % Rattus norvegicus
T1/2 0.3 hr Rattus norvegicus
Tmax 0.9 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cannabinoid receptor 2 EC50 = 10.0 nM 8.0 Agonist activity at human CB2 receptor 20005703
Cannabinoid receptor 1 EC50 = 7943.28 nM 5.1 Agonist activity at human CB1 receptor 20005703

Literature References

PubMed DOI Target Context # Activities
20005703 10.1016/j.bmcl.2009.11.117 Rattus norvegicus 8
20005703 10.1016/j.bmcl.2009.11.117 Blood 3
20005703 10.1016/j.bmcl.2009.11.117 Cannabinoid receptor 2 2
20005703 10.1016/j.bmcl.2009.11.117 Cannabinoid receptor 1 2
20005703 10.1016/j.bmcl.2009.11.117 Liver microsomes 1
20005703 10.1016/j.bmcl.2009.11.117 Brain 1
20005703 10.1016/j.bmcl.2009.11.117 ADMET 1

Data from ChEMBL 36 via Core Engine