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Compound Detail

CHEMBL382605

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Cc1ccc(NC(=O)c2ccc(CN3CCN(C)CC3)c(Cl)c2)cc1Nc1nccc(-c2cccnc2)n1

Basic Information

ChEMBL ID CHEMBL382605
Phase Preclinical
Structure Type MOL
InChI Key NRSRGKSRBDKZAU-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

528.1
MW (Da)
5.24
ALogP
7
HBA
2
HBD
86.3
PSA (Ų)
0.34
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H30ClN7O
MW 528.06
Aromatic Rings 4
Heavy Atoms 38
NP-Likeness -2.00

Activity Summary

IC50 3 meas. best 8.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Bcr/Abl fusion protein
CHEMBL2096618
IC50 8.0 8.0 10.0 1
K562
CHEMBL385
IC50 8.0 8.0 10.0 1
U-937
CHEMBL612794
IC50 5.05 5.05 9000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16332440 10.1016/j.bmcl.2005.11.042 K562 1
16332440 10.1016/j.bmcl.2005.11.042 U-937 1
17376680 10.1016/j.bmcl.2007.03.002 Tyrosine-protein kinase ABL1 1
17376680 10.1016/j.bmcl.2007.03.002 Tyrosine-protein kinase Lyn 1
23473682 10.1016/j.bmcl.2013.01.113 Bcr/Abl fusion protein 1

Data from ChEMBL 36 via Core Engine