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Compound Detail

CHEMBL418270

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O=C(Nc1cccc(Nc2nccc(-c3cccnc3)n2)c1)c1cccnc1

Basic Information

ChEMBL ID CHEMBL418270
Phase Preclinical
Structure Type MOL
InChI Key QOFWWNRCEIPMLU-UHFFFAOYSA-N
6
Targets
6
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

368.4
MW (Da)
3.93
ALogP
6
HBA
2
HBD
92.7
PSA (Ų)
0.55
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 C21H16N6O
MW 368.40
Aromatic Rings 4
Heavy Atoms 28
NP-Likeness -1.62

Activity Summary

IC50 6 meas. best 6.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase ABL1
CHEMBL1862
IC50 6.82 6.82 150.0 1
Bcr/Abl fusion protein
CHEMBL2096618
IC50 6.82 6.82 151.4 1
Protein kinase C alpha type
CHEMBL299
IC50 5.77 5.77 1700.0 1
Proto-oncogene tyrosine-protein kinase Src
CHEMBL267
IC50 5.05 5.05 9000.0 1
Protein kinase C delta type
CHEMBL2996
IC50 4.77 4.77 17000.0 1
Platelet-derived growth factor receptor
CHEMBL2095189
IC50 4.3 4.3 50000.0 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
- 10.1016/S0960-894X(96)00601-4 No relevant target 1
23473682 10.1016/j.bmcl.2013.01.113 Bcr/Abl fusion protein 1

Data from ChEMBL 36 via Core Engine