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Compound Detail

CHEMBL176705

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COc1ccc(-c2cn(-c3ccccc3)c3ncnc(N)c23)cc1

Basic Information

ChEMBL ID CHEMBL176705
Phase Preclinical
Structure Type MOL
InChI Key KOFGCEDKGQUYDQ-UHFFFAOYSA-N
5
Targets
6
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

316.4
MW (Da)
3.68
ALogP
5
HBA
1
HBD
66.0
PSA (Ų)
0.63
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H16N4O
MW 316.36
Aromatic Rings 4
Heavy Atoms 24
NP-Likeness -0.85

Activity Summary

IC50 6 meas. best 6.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Proto-oncogene tyrosine-protein kinase Src
CHEMBL3655
IC50 6.82 6.82 150.0 1
Proto-oncogene tyrosine-protein kinase Src
CHEMBL267
IC50 6.8 6.8 158.5 2
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 6.7 6.7 200.0 1
Epidermal growth factor receptor
CHEMBL203
IC50 6.46 6.46 350.0 1
Tyrosine-protein kinase ABL
CHEMBL2111414
IC50 6.4 6.4 400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10853665 10.1016/s0960-894x(00)00131-1 Proto-oncogene tyrosine-protein kinase Src 1
10853665 10.1016/s0960-894x(00)00131-1 Epidermal growth factor receptor 1
10853665 10.1016/s0960-894x(00)00131-1 Vascular endothelial growth factor receptor 2 1
10853665 10.1016/s0960-894x(00)00131-1 Tyrosine-protein kinase ABL 1
10853665 10.1016/s0960-894x(00)00131-1 Cyclin-dependent kinase 1 1
18722033 10.1016/j.ejmech.2008.07.002 Proto-oncogene tyrosine-protein kinase Src 1
- 10.1007/s00044-012-0308-3 Proto-oncogene tyrosine-protein kinase Src 1

Data from ChEMBL 36 via Core Engine