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Compound Detail

CHEMBL136058

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O=C(/C=C/C(=O)Nc1cc2c(Nc3cccc(Br)c3)ncnc2cn1)NCCCN1CCOCC1

Basic Information

ChEMBL ID CHEMBL136058
Phase Preclinical
Structure Type MOL
InChI Key JPHMUYSWHKPNKF-AATRIKPKSA-N
2
Targets
4
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

540.4
MW (Da)
2.86
ALogP
8
HBA
3
HBD
121.4
PSA (Ų)
0.28
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H26BrN7O3
MW 540.42
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -1.45

Activity Summary

IC50 4 meas. best 9.09

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Epidermal growth factor receptor
CHEMBL203
IC50 9.09 8.4033 0.8 3
Receptor tyrosine-protein kinase erbB-2
CHEMBL1824
IC50 8.3 8.3 5.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11462982 10.1021/jm000372i Epidermal growth factor receptor 4
11462982 10.1021/jm000372i Receptor tyrosine-protein kinase erbB-2 1

Data from ChEMBL 36 via Core Engine