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Compound Detail

CHEMBL3633929

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CC(=O)Nc1ccc2ncnc(Nc3ccc(OCc4ccccn4)c(Cl)c3)c2c1

Basic Information

ChEMBL ID CHEMBL3633929
Phase Preclinical
Structure Type MOL
InChI Key JCMIPNLNEAFFHI-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
14
Publications
0
Known Names

Molecular Properties

419.9
MW (Da)
4.96
ALogP
6
HBA
2
HBD
89.0
PSA (Ų)
0.46
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H18ClN5O2
MW 419.87
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -1.85

Activity Summary

IC50 3 meas. best 8.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Epidermal growth factor receptor
CHEMBL203
IC50 8.52 8.52 3.0 1
Receptor tyrosine-protein kinase erbB-2
CHEMBL1824
IC50 7.8 7.8 16.0 1
Tyrosine-protein kinase Lck
CHEMBL258
IC50 5.91 5.91 1220.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26475520 10.1016/j.bmcl.2015.10.003 Receptor tyrosine-protein kinase erbB-2 1
26475520 10.1016/j.bmcl.2015.10.003 Epidermal growth factor receptor 1
26475520 10.1016/j.bmcl.2015.10.003 Cyclin-dependent kinase 2 1
26475520 10.1016/j.bmcl.2015.10.003 Hepatocyte growth factor receptor 1
26475520 10.1016/j.bmcl.2015.10.003 Focal adhesion kinase 1 1
26475520 10.1016/j.bmcl.2015.10.003 Fibroblast growth factor receptor 1 1
26475520 10.1016/j.bmcl.2015.10.003 Insulin-like growth factor 1 receptor 1
26475520 10.1016/j.bmcl.2015.10.003 Vascular endothelial growth factor receptor 2 1
26475520 10.1016/j.bmcl.2015.10.003 Tyrosine-protein kinase Lck 1
26475520 10.1016/j.bmcl.2015.10.003 cAMP-dependent protein kinase (PKA) 1
26475520 10.1016/j.bmcl.2015.10.003 Mitogen-activated protein kinase 14 1
26475520 10.1016/j.bmcl.2015.10.003 MAP kinase-activated protein kinase 2 1
26475520 10.1016/j.bmcl.2015.10.003 BT-474 1
26475520 10.1016/j.bmcl.2015.10.003 ADMET 1

Data from ChEMBL 36 via Core Engine