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Compound Detail

CHEMBL58580

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N#Cc1ccc(C(=O)Nc2cccc(Nc3nccc(-c4cccnc4)n3)c2)cc1

Basic Information

ChEMBL ID CHEMBL58580
Phase Preclinical
Structure Type MOL
InChI Key VKLJXWNPKZRZMV-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

392.4
MW (Da)
4.41
ALogP
6
HBA
2
HBD
103.6
PSA (Ų)
0.52
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H16N6O
MW 392.42
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -1.86

Activity Summary

IC50 4 meas. best 6.46

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein kinase C alpha type
CHEMBL299
IC50 6.46 6.46 350.0 1
Tyrosine-protein kinase ABL1
CHEMBL1862
IC50 5.89 5.89 1300.0 1
Bcr/Abl fusion protein
CHEMBL2096618
IC50 5.89 5.89 1288.2 1
Platelet-derived growth factor receptor
CHEMBL2095189
IC50 5.82 5.82 1500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.1016/S0960-894X(96)00601-4 Tyrosine-protein kinase ABL1 1
- 10.1016/S0960-894X(96)00601-4 Epidermal growth factor receptor 1
- 10.1016/S0960-894X(96)00601-4 Proto-oncogene tyrosine-protein kinase Src 1
- 10.1016/S0960-894X(96)00601-4 Platelet-derived growth factor receptor 1
- 10.1016/S0960-894X(96)00601-4 cAMP-dependent protein kinase (PKA) 1
- 10.1016/S0960-894X(96)00601-4 Protein kinase C alpha type 1
- 10.1016/S0960-894X(96)00601-4 Protein kinase C delta type 1
23473682 10.1016/j.bmcl.2013.01.113 Bcr/Abl fusion protein 1

Data from ChEMBL 36 via Core Engine