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Compound Detail

CHEMBL206319

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Cc1ccc(NC(=O)c2ccc(CN3CC(N(C)C)C3)c(C(F)(F)F)c2)cc1Nc1nccc(-c2cncnc2)n1

Basic Information

ChEMBL ID CHEMBL206319
Phase Preclinical
Structure Type MOL
InChI Key NKEZCSVNPKYVIB-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

562.6
MW (Da)
5.00
ALogP
8
HBA
2
HBD
99.2
PSA (Ų)
0.31
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H29F3N8O
MW 562.60
Aromatic Rings 4
Heavy Atoms 41
NP-Likeness -1.78

Activity Summary

IC50 2 meas. best 7.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Bcr/Abl fusion protein
CHEMBL2096618
IC50 7.77 7.77 17.0 1
K562
CHEMBL385
IC50 7.77 7.77 17.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
K562 IC50 = 17.0 nM 7.77 Antiproliferative activity against K562 cells 16332440
Bcr/Abl fusion protein IC50 = 16.98 nM 7.77 Inhibition of BCR-ABL kinase (unknown origin) 23473682

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
23473682 10.1016/j.bmcl.2013.01.113 Bcr/Abl fusion protein 1

Data from ChEMBL 36 via Core Engine