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Compound Detail

CHEMBL186680

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COc1cc(Nc2nccc(-c3cnn4nc(C)ccc34)n2)cc(C(F)(F)F)c1

Basic Information

ChEMBL ID CHEMBL186680
Phase Preclinical
Structure Type MOL
InChI Key ZANNOGKZSUYAAD-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

400.4
MW (Da)
4.27
ALogP
7
HBA
1
HBD
77.2
PSA (Ų)
0.55
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 C19H15F3N6O
MW 400.36
Aromatic Rings 4
Heavy Atoms 29
NP-Likeness -1.63

Activity Summary

Ki 3 meas. best 8.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glycogen synthase kinase-3 beta
CHEMBL262
Ki 8.0 8.0 10.0 1
Cyclin-dependent kinase 2
CHEMBL301
Ki 7.7 7.7 20.0 1
Cyclin-dependent kinase 4
CHEMBL331
Ki 6.41 6.41 390.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15341487 10.1021/jm040063i Glycogen synthase kinase-3 beta 1
15341487 10.1021/jm040063i Cyclin-dependent kinase 2 1
15341487 10.1021/jm040063i Cyclin-dependent kinase 4 1

Data from ChEMBL 36 via Core Engine