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Compound Detail

CHEMBL2375900

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COc1ccc(C(=O)Nc2ncccn2)cc1Nc1nccc(-c2cccnc2)n1

Basic Information

ChEMBL ID CHEMBL2375900
Phase Preclinical
Structure Type MOL
InChI Key USIPMCNVJIUSIH-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

399.4
MW (Da)
3.33
ALogP
8
HBA
2
HBD
114.8
PSA (Ų)
0.51
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 C21H17N7O2
MW 399.41
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -1.55

Activity Summary

IC50 1 meas. best 8.42

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Bcr/Abl fusion protein
CHEMBL2096618
IC50 8.42 8.42 3.8 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Bcr/Abl fusion protein IC50 = 3.78 nM 8.42 Inhibition of Bcr-Abl kinase (unknown origin) after 30 mins by HTRF assay 23538233

Literature References

PubMed DOI Target Context # Activities
23538233 10.1016/j.bmc.2013.02.036 K562 1
23538233 10.1016/j.bmc.2013.02.036 Bcr/Abl fusion protein 1

Data from ChEMBL 36 via Core Engine