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Compound Detail

CHEMBL1672331

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Nc1ncc(-c2ccnc(N3CCOCC3)n2)cn1

Basic Information

ChEMBL ID CHEMBL1672331
Phase Preclinical
Structure Type MOL
InChI Key WCSNDONKXWSCEI-UHFFFAOYSA-N
5
Targets
6
Activities
3
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

258.3
MW (Da)
0.35
ALogP
7
HBA
1
HBD
90.0
PSA (Ų)
0.83
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C12H14N6O
MW 258.29
Aromatic Rings 2
Heavy Atoms 19
NP-Likeness -1.72

Activity Summary

Ki 3 meas. best 9.19
EC50 2 meas. best 6.89
IC50 1 meas. best 7.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
PI3-kinase p110-alpha/p85-alpha
CHEMBL2111367
Ki 9.19 9.19 0.6 1
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
CHEMBL4005
IC50 7.85 7.85 14.0 1
PI3K p110 beta/p85 alpha
CHEMBL3038510
Ki 7.82 7.82 15.0 1
PI3-kinase p110-delta/p85-alpha
CHEMBL2111432
Ki 7.09 7.09 81.0 1
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
CHEMBL4005
EC50 6.89 6.89 130.0 1
A2780
CHEMBL614004
EC50 5.3 5.3 4980.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
24900252 10.1021/ml1001932 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform 2
33356246 10.1021/acs.jmedchem.0c01652 No relevant target 2
33356246 10.1021/acs.jmedchem.0c01652 ADMET 2
33356246 10.1021/acs.jmedchem.0c01652 Unchecked 2
24900252 10.1021/ml1001932 A2780 1
33356246 10.1021/acs.jmedchem.0c01652 PI3-kinase p110-alpha/p85-alpha 1
33356246 10.1021/acs.jmedchem.0c01652 PI3K p110 beta/p85 alpha 1
33356246 10.1021/acs.jmedchem.0c01652 PI3-kinase p110-delta/p85-alpha 1

Data from ChEMBL 36 via Core Engine