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Compound Detail

CHEMBL246492

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Fc1cccc(Cn2ncc3cc(Nc4ncnn5ccc(COC[C@@H]6COCCN6)c45)ccc32)c1

Basic Information

ChEMBL ID CHEMBL246492
Phase Preclinical
Structure Type MOL
InChI Key VLYYUZFBTALINK-QHCPKHFHSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

487.5
MW (Da)
3.52
ALogP
9
HBA
2
HBD
90.5
PSA (Ų)
0.35
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H26FN7O2
MW 487.54
Aromatic Rings 5
Heavy Atoms 36
NP-Likeness -1.52

Activity Summary

IC50 3 meas. best 6.23

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Receptor tyrosine-protein kinase erbB-2
CHEMBL1824
IC50 6.23 6.23 590.0 1
Epidermal growth factor receptor
CHEMBL203
IC50 6.19 6.19 640.0 1
NCI-N87
CHEMBL614197
IC50 5.52 5.52 3000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17270437 10.1016/j.bmcl.2007.01.002 Receptor tyrosine-protein kinase erbB-2 1
17270437 10.1016/j.bmcl.2007.01.002 Epidermal growth factor receptor 1
17270437 10.1016/j.bmcl.2007.01.002 NCI-N87 1
17270437 10.1016/j.bmcl.2007.01.002 A2780 1
17270437 10.1016/j.bmcl.2007.01.002 Liver 1

Data from ChEMBL 36 via Core Engine