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Compound Detail

CHEMBL447230

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COc1cc2ncnc(N(C)c3cccc(Br)c3)c2cc1OC

Basic Information

ChEMBL ID CHEMBL447230
Phase Preclinical
Structure Type MOL
InChI Key IPWGDOZPSOZFOD-UHFFFAOYSA-N
4
Targets
7
Activities
2
Assay Types
0
PK Parameters
13
Publications
0
Known Names

Molecular Properties

374.2
MW (Da)
4.18
ALogP
5
HBA
0
HBD
47.5
PSA (Ų)
0.69
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 C17H16BrN3O2
MW 374.24
Aromatic Rings 3
Heavy Atoms 23
NP-Likeness -0.90

Activity Summary

IC50 6 meas. best 6.82
Kd 1 meas.

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Epidermal growth factor receptor
CHEMBL203
IC50 6.82 6.82 152.0 1
NON-PROTEIN TARGET
CHEMBL3879801
IC50 5.4 5.4 3950.0 1
HT-29
CHEMBL384
IC50 5.21 5.21 6100.0 2
MCF7
CHEMBL387
IC50 5.04 5.04 9200.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
21033670 10.1021/jm1009605 Calf thymus DNA 4
21033670 10.1021/jm1009605 Nucleic Acid 3
8568816 10.1021/jm9503613 Epidermal growth factor receptor 1
21033670 10.1021/jm1009605 PC-3 1
21033670 10.1021/jm1009605 HT-29 1
21033670 10.1021/jm1009605 MCF7 1
21033670 10.1021/jm1009605 DNA topoisomerase 1 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 MCF7 1
21353546 10.1016/j.bmcl.2011.01.137 NON-PROTEIN TARGET 1
21353546 10.1016/j.bmcl.2011.01.137 PC-3 1

Data from ChEMBL 36 via Core Engine