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Compound Detail

CHEMBL1092119

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Cn1cc(/C=C2\Oc3cccc(O)c3C2=O)c2c(N3CCC(C(=O)N4CCOCC4)CC3)ccnc21

Basic Information

ChEMBL ID CHEMBL1092119
Phase Preclinical
Structure Type MOL
InChI Key CFYIBWFGBQGKRX-JCMHNJIXSA-N
2
Targets
2
Activities
1
Assay Types
2
PK Parameters
5
Publications
0
Known Names

Molecular Properties

488.5
MW (Da)
2.97
ALogP
8
HBA
1
HBD
97.1
PSA (Ų)
0.57
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H28N4O5
MW 488.54
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -0.79

Activity Summary

IC50 2 meas. best 8.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase mTOR
CHEMBL2842
IC50 8.85 8.85 1.4 1
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
CHEMBL4005
IC50 7.2 7.2 63.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.5 hr Mus musculus
T1/2 0.5 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20188552 10.1016/j.bmcl.2010.01.135 ADMET 2
20188552 10.1016/j.bmcl.2010.01.135 Serine/threonine-protein kinase mTOR 1
20188552 10.1016/j.bmcl.2010.01.135 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform 1
20188552 10.1016/j.bmcl.2010.01.135 Unchecked 1
20188552 10.1016/j.bmcl.2010.01.135 LNCaP 1

Data from ChEMBL 36 via Core Engine