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Compound Detail

CHEMBL329350

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COc1ccc(-c2cnc3c(-c4ccncc4)cnn3c2)cc1

Basic Information

ChEMBL ID CHEMBL329350
Phase Preclinical
Structure Type MOL
InChI Key ZBCIUJVPXUPSFS-UHFFFAOYSA-N
3
Targets
6
Activities
1
Assay Types
0
PK Parameters
12
Publications
0
Known Names

Molecular Properties

302.3
MW (Da)
3.47
ALogP
5
HBA
0
HBD
52.3
PSA (Ų)
0.58
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 C18H14N4O
MW 302.34
Aromatic Rings 4
Heavy Atoms 23
NP-Likeness -1.25

Activity Summary

IC50 6 meas. best 7.54

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 7.54 7.4667 29.0 3
Vascular endothelial growth factor receptor
CHEMBL2095227
IC50 6.82 6.82 150.0 2
Bone morphogenetic protein 4
CHEMBL5350
IC50 5.19 5.19 6500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12217372 10.1016/s0960-894x(02)00525-5 Vascular endothelial growth factor receptor 2 2
12217372 10.1016/s0960-894x(02)00525-5 VEGF-receptor 2 and PDGF-receptor beta (KDR and PDGFR beta) 1
12217372 10.1016/s0960-894x(02)00525-5 Vascular endothelial growth factor receptor 1 and 2 (Flt-1 and KDR) 1
12217372 10.1016/s0960-894x(02)00525-5 Vascular endothelial growth factor receptor 2 and 3 (KDR and Flt-4) 1
12217372 10.1016/s0960-894x(02)00525-5 VEGF-receptor 2 and Fibroblast growth factor receptor 1 1
12217372 10.1016/s0960-894x(02)00525-5 VEGF-receptor 2 and tyrosine-protein kinase SRC 1
12217372 10.1016/s0960-894x(02)00525-5 Vascular endothelial growth factor receptor 1
12217372 10.1016/s0960-894x(02)00525-5 No relevant target 1
12443771 10.1016/s0960-894x(02)00827-2 Vascular endothelial growth factor receptor 2 1
12443771 10.1016/s0960-894x(02)00827-2 Vascular endothelial growth factor receptor 1
12443771 10.1016/s0960-894x(02)00827-2 No relevant target 1
18621530 10.1016/j.bmcl.2008.06.052 Bone morphogenetic protein 4 1

Data from ChEMBL 36 via Core Engine