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Compound Detail

CHEMBL381040

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COC[C@H]1OC(=O)c2coc3c2[C@@]1(C)C1=C(C3=O)C2CC[C@H](OC(=O)CN(C)c3ccc([N+](=O)[O-])c4nonc34)[C@@]2(C)C[C@H]1OC(C)=O

Basic Information

ChEMBL ID CHEMBL381040
Phase Preclinical
Structure Type MOL
InChI Key KEVHMUKRLYZRKU-WQTLYCGOSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

664.6
MW (Da)
3.46
ALogP
15
HBA
0
HBD
203.6
PSA (Ų)
0.15
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H32N4O12
MW 664.62
Aromatic Rings 3
Heavy Atoms 48
NP-Likeness 1.10

Activity Summary

IC50 1 meas. best 6.65

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
PI3-kinase p110-alpha/p85-alpha
CHEMBL2111367
IC50 6.65 6.65 225.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
PI3-kinase p110-alpha/p85-alpha IC50 = 225.0 nM 6.65 Inhibition of PI3 kinase p110alpha/p85-alpha complex 16464575

Literature References

PubMed DOI Target Context # Activities
16464575 10.1016/j.bmcl.2006.01.091 PI3-kinase p110-alpha/p85-alpha 1

Data from ChEMBL 36 via Core Engine