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Compound Detail

CHEMBL1278148

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COc1cc2ncnc(Oc3ccc(F)c(Cl)c3)c2cc1OC

Basic Information

ChEMBL ID CHEMBL1278148
Phase Preclinical
Structure Type MOL
InChI Key FRTNWIZUWYFSFX-UHFFFAOYSA-N
2
Targets
4
Activities
1
Assay Types
0
PK Parameters
16
Publications
0
Known Names

Molecular Properties

334.7
MW (Da)
4.23
ALogP
5
HBA
0
HBD
53.5
PSA (Ų)
0.71
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H12ClFN2O3
MW 334.73
Aromatic Rings 3
Heavy Atoms 23
NP-Likeness -1.36

Activity Summary

IC50 4 meas. best 5.39

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
HT-29
CHEMBL384
IC50 5.39 5.39 4070.0 1
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 5.02 5.0167 9500.0 3

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
21033670 10.1021/jm1009605 Calf thymus DNA 1
21033670 10.1021/jm1009605 Nucleic Acid 1
21353546 10.1016/j.bmcl.2011.01.137 Epidermal growth factor receptor 1
21353546 10.1016/j.bmcl.2011.01.137 Vascular endothelial growth factor receptor 2 1
21353546 10.1016/j.bmcl.2011.01.137 HT-29 1
21353546 10.1016/j.bmcl.2011.01.137 NON-PROTEIN TARGET 1
21353546 10.1016/j.bmcl.2011.01.137 PC-3 1
21353546 10.1016/j.bmcl.2011.01.137 MCF7 1
22229669 10.1021/jm2013453 Epidermal growth factor receptor 1
22229669 10.1021/jm2013453 Vascular endothelial growth factor receptor 2 1
22229669 10.1021/jm2013453 No relevant target 1
22229669 10.1021/jm2013453 PC-3 1
22229669 10.1021/jm2013453 HT-29 1
22229669 10.1021/jm2013453 MCF7 1
26526740 10.1016/j.bmc.2015.10.035 Epidermal growth factor receptor 1
26526740 10.1016/j.bmc.2015.10.035 Vascular endothelial growth factor receptor 2 1

Data from ChEMBL 36 via Core Engine