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Compound Detail

CHEMBL189543

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COCCOCc1cc2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n(C2CCCC2)c1=O

Basic Information

ChEMBL ID CHEMBL189543
Phase Preclinical
Structure Type MOL
InChI Key USXVSXDTKIDDDT-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

479.6
MW (Da)
2.62
ALogP
10
HBA
2
HBD
106.4
PSA (Ų)
0.45
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H33N7O3
MW 479.59
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -1.21

Activity Summary

IC50 3 meas. best 7.51

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 4/cyclin D1
CHEMBL1907601
IC50 7.51 7.51 31.0 1
Cyclin-dependent kinase 4/cyclin D
CHEMBL2095942
IC50 7.51 7.51 31.0 1
MDA-MB-435
CHEMBL614697
IC50 5.67 5.67 2150.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15801831 10.1021/jm049354h Cyclin-dependent kinase 4/cyclin D 1
15801831 10.1021/jm049354h Cyclin-dependent kinase 2/cyclin A 1
15801831 10.1021/jm049354h MDA-MB-435 1

Data from ChEMBL 36 via Core Engine