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Compound Detail

CHEMBL329642

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C/C=C\C(=O)Nc1ccc2ncnc(Nc3cccc(Br)c3)c2c1

Basic Information

ChEMBL ID CHEMBL329642
Phase Preclinical
Structure Type MOL
InChI Key JPHUTKJINPEEPQ-RQOWECAXSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

383.2
MW (Da)
4.65
ALogP
4
HBA
2
HBD
66.9
PSA (Ų)
0.64
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 C18H15BrN4O
MW 383.25
Aromatic Rings 3
Heavy Atoms 24
NP-Likeness -1.37

Activity Summary

IC50 5 meas. best 6.57

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Epidermal growth factor receptor
CHEMBL203
IC50 6.57 6.57 269.0 1
SK-BR-3
CHEMBL613834
IC50 6.13 6.13 742.0 1
A-431
CHEMBL614069
IC50 5.18 5.18 6610.0 1
SW-620
CHEMBL612262
IC50 4.9 4.9 12540.0 1
Receptor tyrosine-protein kinase erbB-2
CHEMBL1824
IC50 4.66 4.66 21657.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11495584 10.1021/jm0005555 Epidermal growth factor receptor 1
11495584 10.1021/jm0005555 Receptor tyrosine-protein kinase erbB-2 1
11495584 10.1021/jm0005555 A-431 1
11495584 10.1021/jm0005555 SK-BR-3 1
11495584 10.1021/jm0005555 SW-620 1

Data from ChEMBL 36 via Core Engine