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Compound Detail

CHEMBL579031

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CCc1nn(CCO)c(CC)c1Oc1cccc(C#N)c1

Basic Information

ChEMBL ID CHEMBL579031
Phase Preclinical
Structure Type MOL
InChI Key LEIYXLSSQXYLEO-UHFFFAOYSA-N
1
Targets
3
Activities
1
Assay Types
9
PK Parameters
8
Publications
0
Known Names

Molecular Properties

285.4
MW (Da)
2.66
ALogP
5
HBA
1
HBD
71.1
PSA (Ų)
0.89
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H19N3O2
MW 285.35
Aromatic Rings 2
Heavy Atoms 21
NP-Likeness -1.46

Activity Summary

IC50 3 meas. best 6.46

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 6.46 6.46 350.0 3

Pharmacokinetic Data

Parameter Value Units Species
CL 100.0 mL.min-1.kg-1 Rattus norvegicus
CL 100.0 mL.min-1.kg-1 Rattus norvegicus
Fu 0.8 - Homo sapiens
Fu 0.8 - Homo sapiens
T1/2 0.45 hr Homo sapiens
T1/2 0.45 hr Homo sapiens
T1/2 0.1 hr Rattus norvegicus
T1/2 0.1 hr Rattus norvegicus
Vd 1.3 L.kg-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19717303 10.1016/j.bmcl.2009.08.043 Unchecked 11
19748778 10.1016/j.bmcl.2009.08.080 Unchecked 11
19748778 10.1016/j.bmcl.2009.08.080 Rattus norvegicus 3
19717303 10.1016/j.bmcl.2009.08.043 Liver microsomes 2
19748778 10.1016/j.bmcl.2009.08.080 Liver microsomes 2
20804202 10.1021/jm100762r Rattus norvegicus 2
19748778 10.1016/j.bmcl.2009.08.080 No relevant target 1
20804202 10.1021/jm100762r Unchecked 1

Data from ChEMBL 36 via Core Engine