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Compound Detail

CHEMBL426818

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

Basic Information

ChEMBL ID CHEMBL426818
Phase Preclinical
Structure Type MOL
InChI Key UGPPBMDIMQEVBD-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

462.6
MW (Da)
3.15
ALogP
9
HBA
2
HBD
101.4
PSA (Ų)
0.56
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H30N6O3
MW 462.55
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -1.06

Activity Summary

IC50 4 meas. best 8.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 4/cyclin D
CHEMBL2095942
IC50 8.4 8.4 4.0 1
MDA-MB-435
CHEMBL614697
IC50 6.72 6.72 190.0 1
HCT-116
CHEMBL394
IC50 6.47 6.47 340.0 1
Cyclin-dependent kinase 2/cyclin A
CHEMBL2094128
IC50 5.55 5.55 2819.0 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

Data from ChEMBL 36 via Core Engine