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Compound Detail

CHEMBL1079113

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Cc1ccc(-c2ccnc(Nc3cc(NC(=O)c4ccc(CN5CCN(C)CC5)cc4)ccc3C)n2)cn1

Basic Information

ChEMBL ID CHEMBL1079113
Phase Preclinical
Structure Type MOL
InChI Key AFMXVBAHMGWYAZ-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

507.6
MW (Da)
4.90
ALogP
7
HBA
2
HBD
86.3
PSA (Ų)
0.37
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H33N7O
MW 507.64
Aromatic Rings 4
Heavy Atoms 38
NP-Likeness -1.76

Activity Summary

IC50 2 meas. best 7.37

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mast/stem cell growth factor receptor Kit
CHEMBL1936
IC50 7.37 7.37 43.0 1
Bcr/Abl fusion protein
CHEMBL2096618
IC50 4.96 4.96 11000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Mast/stem cell growth factor receptor Kit IC50 = 43.0 nM 7.37 Inhibition of KIT 20166671
Bcr/Abl fusion protein IC50 = 11000.0 nM 4.96 Inhibition of wild type Bcr-Abl 20166671

Literature References

PubMed DOI Target Context # Activities
20166671 10.1021/jm901132v Mast/stem cell growth factor receptor Kit 1
20166671 10.1021/jm901132v Bcr/Abl fusion protein 1

Data from ChEMBL 36 via Core Engine