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Compound Detail

CHEMBL190096

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CCOC(=O)c1c(C)c2cnc(Nc3ccc(N4CCNCC4)cc3)nc2n(C2CCCC2)c1=O

Basic Information

ChEMBL ID CHEMBL190096
Phase Preclinical
Structure Type MOL
InChI Key HWESTUDJJGQKRI-UHFFFAOYSA-N
4
Targets
6
Activities
1
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

476.6
MW (Da)
3.54
ALogP
9
HBA
2
HBD
101.4
PSA (Ų)
0.52
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H32N6O3
MW 476.58
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -1.12

Activity Summary

IC50 6 meas. best 8.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 4/cyclin D
CHEMBL2095942
IC50 8.22 8.22 6.0 2
MDA-MB-435
CHEMBL614697
IC50 6.77 6.77 170.0 2
HCT-116
CHEMBL394
IC50 6.08 6.08 830.0 1
Cyclin-dependent kinase 2/cyclin A
CHEMBL2094128
IC50 5.3 5.3 5000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15801830 10.1021/jm049355+ Cyclin-dependent kinase 4/cyclin D 1
15801830 10.1021/jm049355+ Cyclin-dependent kinase 1/cyclin B 1
15801830 10.1021/jm049355+ Cyclin-dependent kinase 2/cyclin A 1
15801830 10.1021/jm049355+ Cyclin-dependent kinase 2/cyclin E 1
15801830 10.1021/jm049355+ HCT-116 1
15801830 10.1021/jm049355+ MDA-MB-435 1
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
15801831 10.1021/jm049354h MDA-MB-468 1

Data from ChEMBL 36 via Core Engine