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Compound Detail

CHEMBL66716

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Nc1ncnc2c1c(-c1ccc(Oc3ccccc3)cc1)c(Br)n2C1CCCC1

Basic Information

ChEMBL ID CHEMBL66716
Phase Preclinical
Structure Type MOL
InChI Key XPDAMMJGEHXXPI-UHFFFAOYSA-N
4
Targets
6
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

449.4
MW (Da)
6.35
ALogP
5
HBA
1
HBD
66.0
PSA (Ų)
0.39
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H21BrN4O
MW 449.35
Aromatic Rings 4
Heavy Atoms 29
NP-Likeness -0.48

Activity Summary

IC50 6 meas. best 7.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase Lck
CHEMBL258
IC50 7.52 6.58 30.0 2
Unchecked
CHEMBL612545
IC50 7.12 6.025 75.0 2
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 5.8 5.8 1600.0 1
Angiopoietin-1 receptor
CHEMBL4128
IC50 4.96 4.96 11100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11012022 10.1016/s0960-894x(00)00442-x Tyrosine-protein kinase Lck 2
11012022 10.1016/s0960-894x(00)00442-x Unchecked 2
11012022 10.1016/s0960-894x(00)00442-x Proto-oncogene tyrosine-protein kinase Src 1
11012022 10.1016/s0960-894x(00)00442-x Vascular endothelial growth factor receptor 2 1
11012022 10.1016/s0960-894x(00)00442-x Angiopoietin-1 receptor 1

Data from ChEMBL 36 via Core Engine