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Compound Detail

CHEMBL91009

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COCC#CC(=O)Nc1ccc2ncnc(Nc3cccc(Br)c3)c2c1

Basic Information

ChEMBL ID CHEMBL91009
Phase Preclinical
Structure Type MOL
InChI Key VKFHLVGNIPONMR-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

411.3
MW (Da)
3.72
ALogP
5
HBA
2
HBD
76.1
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 C19H15BrN4O2
MW 411.26
Aromatic Rings 3
Heavy Atoms 26
NP-Likeness -1.20

Activity Summary

IC50 5 meas. best 8.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Epidermal growth factor receptor
CHEMBL203
IC50 8.05 8.05 9.0 1
Receptor tyrosine-protein kinase erbB-2
CHEMBL1824
IC50 7.48 7.48 33.0 1
SK-BR-3
CHEMBL613834
IC50 7.34 7.34 46.0 1
A-431
CHEMBL614069
IC50 6.57 6.57 268.0 1
SW-620
CHEMBL612262
IC50 5.76 5.76 1730.0 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