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Compound Detail

CHEMBL205591

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CN(CC(=O)O[C@@H]1CC(=O)c2coc3c2[C@@]1(C)c1ccc2c(c1C3=O)CCC2=O)c1ccc([N+](=O)[O-])c2nonc12

Basic Information

ChEMBL ID CHEMBL205591
Phase Preclinical
Structure Type MOL
InChI Key ZNCVAFNQSVANHZ-NGOKVRLYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

556.5
MW (Da)
3.34
ALogP
12
HBA
0
HBD
175.9
PSA (Ų)
0.20
QED
2
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H20N4O9
MW 556.49
Aromatic Rings 4
Heavy Atoms 41
NP-Likeness 0.44

Activity Summary

IC50 1 meas. best 8.02

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
PI3-kinase p110-alpha/p85-alpha
CHEMBL2111367
IC50 8.02 8.02 9.6 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
PI3-kinase p110-alpha/p85-alpha IC50 = 9.6 nM 8.02 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