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Compound Detail

CHEMBL1278056

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COc1cc2ncnc(N(C)c3ccc(F)c(Cl)c3)c2cc1OC

Basic Information

ChEMBL ID CHEMBL1278056
Phase Preclinical
Structure Type MOL
InChI Key SWVFSGKKNRTKGM-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

347.8
MW (Da)
4.21
ALogP
5
HBA
0
HBD
47.5
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 C17H15ClFN3O2
MW 347.78
Aromatic Rings 3
Heavy Atoms 24
NP-Likeness -1.31

Activity Summary

IC50 1 meas. best 5.28

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
HT-29
CHEMBL384
IC50 5.28 5.28 5200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
HT-29 IC50 = 5200.0 nM 5.28 Antiproliferative activity against human HT-29 cells at 10 uM after 72 hrs by MT... 21353546

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 PC-3 1
21353546 10.1016/j.bmcl.2011.01.137 MCF7 1
21353546 10.1016/j.bmcl.2011.01.137 NON-PROTEIN TARGET 1

Data from ChEMBL 36 via Core Engine