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Compound Detail

CHEMBL216697

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CN(C)c1ccc(-c2c(N)ncnc2C#Cc2ccc(N3CCOCC3)nc2)cc1

Basic Information

ChEMBL ID CHEMBL216697
Phase Preclinical
Structure Type MOL
InChI Key AINVOEOJEKKMKB-UHFFFAOYSA-N
1
Targets
3
Activities
1
Assay Types
5
PK Parameters
6
Publications
0
Known Names

Molecular Properties

400.5
MW (Da)
2.42
ALogP
7
HBA
1
HBD
80.4
PSA (Ų)
0.68
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C23H24N6O
MW 400.49
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -1.47

Activity Summary

IC50 3 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adenosine kinase
CHEMBL3589
IC50 8.7 7.68 2.0 3

Pharmacokinetic Data

Parameter Value Units Species
CL 16.67 mL.min-1.kg-1 Rattus norvegicus
Cmax 199.76 nM Rattus norvegicus
F 9.0 % Rattus norvegicus
T1/2 0.5 hr Rattus norvegicus
Vd 0.7 L.kg-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17197188 10.1016/j.bmc.2006.12.029 Rattus norvegicus 6
17197188 10.1016/j.bmc.2006.12.029 Adenosine kinase 2
17154503 10.1021/jm060189a Adenosine kinase 1
17197188 10.1016/j.bmc.2006.12.029 Mus musculus 1
17197188 10.1016/j.bmc.2006.12.029 Hepatocyte 1
17197188 10.1016/j.bmc.2006.12.029 Liver microsomes 1

Data from ChEMBL 36 via Core Engine