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Compound Detail

CHEMBL1090599

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CC(=O)N(C)Cc1cc2nc(-c3cnc(N)nc3)nc(N3CCOCC3)c2s1

Basic Information

ChEMBL ID CHEMBL1090599
Phase Preclinical
Structure Type MOL
InChI Key BQIFXGYWHHKPCK-UHFFFAOYSA-N
3
Targets
3
Activities
3
Assay Types
3
PK Parameters
7
Publications
0
Known Names

Molecular Properties

399.5
MW (Da)
1.55
ALogP
9
HBA
1
HBD
110.4
PSA (Ų)
0.70
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 C18H21N7O2S
MW 399.48
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -1.76

Activity Summary

EC50 1 meas. best 9.72
IC50 1 meas. best 8.3
Ki 1 meas. best 7.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
NON-PROTEIN TARGET
CHEMBL3879801
EC50 9.72 9.72 0.2 1
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
CHEMBL4005
IC50 8.3 8.3 5.0 1
Serine/threonine-protein kinase mTOR
CHEMBL2842
Ki 7.3 7.3 50.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 2.0 mL.min-1.kg-1 Rattus norvegicus
CL 50.0 mL.min-1.kg-1 Rattus norvegicus
CL 94.0 mL.min-1.kg-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20346656 10.1016/j.bmcl.2010.03.046 Rattus norvegicus 2
20346656 10.1016/j.bmcl.2010.03.046 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform 1
20346656 10.1016/j.bmcl.2010.03.046 Serine/threonine-protein kinase mTOR 1
20346656 10.1016/j.bmcl.2010.03.046 NON-PROTEIN TARGET 1
20346656 10.1016/j.bmcl.2010.03.046 No relevant target 1
20346656 10.1016/j.bmcl.2010.03.046 Liver microsomes 1
20346656 10.1016/j.bmcl.2010.03.046 Plasma 1

Data from ChEMBL 36 via Core Engine