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Compound Detail

CHEMBL1094832

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CCOCCn1nc(CC)c2nc(N3CCC(N)CC3)nc(Nc3cc(C)ccn3)c21

Basic Information

ChEMBL ID CHEMBL1094832
Phase Preclinical
Structure Type MOL
InChI Key LASVKJLQJACNOV-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
6
Publications
0
Known Names

Molecular Properties

424.6
MW (Da)
2.80
ALogP
9
HBA
2
HBD
107.0
PSA (Ų)
0.53
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H32N8O
MW 424.55
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -1.55

Activity Summary

IC50 1 meas. best 9.11

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
cGMP-specific 3',5'-cyclic phosphodiesterase
CHEMBL1827
IC50 9.11 9.11 0.8 1

Pharmacokinetic Data

Parameter Value Units Species
CL 48.0 mL.min-1.kg-1 Canis lupus familiaris
T1/2 11.7 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20443228 10.1016/j.bmcl.2010.03.111 Canis familiaris 3
20443228 10.1016/j.bmcl.2010.03.111 Unchecked 2
20443228 10.1016/j.bmcl.2010.03.111 Voltage-gated inwardly rectifying potassium channel KCNH2 2
20443228 10.1016/j.bmcl.2010.03.111 cGMP-specific 3',5'-cyclic phosphodiesterase 1
20443228 10.1016/j.bmcl.2010.03.111 Liver microsomes 1
20443228 10.1016/j.bmcl.2010.03.111 Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine