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Compound Detail

CHEMBL189978

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Cc1c(Br)c(=O)n(C2CCCC2)c2nc(Nc3ccc(N4CC(C)NC(C)C4)cn3)ncc12

Basic Information

ChEMBL ID CHEMBL189978
Phase Preclinical
Structure Type MOL
InChI Key RVRDNOJFPRMUSX-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

512.5
MW (Da)
4.30
ALogP
8
HBA
2
HBD
88.0
PSA (Ų)
0.54
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H30BrN7O
MW 512.46
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -0.95

Activity Summary

IC50 3 meas. best 7.2

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 4/cyclin D1
CHEMBL1907601
IC50 7.2 7.2 63.0 1
Cyclin-dependent kinase 4/cyclin D
CHEMBL2095942
IC50 7.2 7.2 63.0 1
MDA-MB-435
CHEMBL614697
IC50 6.24 6.24 570.0 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