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Compound Detail

CHEMBL328106

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COc1cc2ncnc(Nc3ccc(Br)cc3)c2cc1OC

Basic Information

ChEMBL ID CHEMBL328106
Phase Preclinical
Structure Type MOL
InChI Key MCNVTWIIWNZMGB-UHFFFAOYSA-N
2
Targets
4
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

360.2
MW (Da)
4.15
ALogP
5
HBA
1
HBD
56.3
PSA (Ų)
0.76
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 C16H14BrN3O2
MW 360.21
Aromatic Rings 3
Heavy Atoms 22
NP-Likeness -0.92

Activity Summary

IC50 4 meas. best 10.14

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Epidermal growth factor receptor
CHEMBL203
IC50 10.14 8.2 0.1 3
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 6.1 6.1 800.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
8568816 10.1021/jm9503613 Epidermal growth factor receptor 1
18271520 10.1021/jm070654j Epidermal growth factor receptor 1
21033670 10.1021/jm1009605 Calf thymus DNA 1
21033670 10.1021/jm1009605 Nucleic Acid 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 PC-3 1
22229669 10.1021/jm2013453 HT-29 1
22229669 10.1021/jm2013453 MCF7 1

Data from ChEMBL 36 via Core Engine