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Compound Detail

CHEMBL1645474

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NC1CCN(Cc2ccn3ncnc(Nc4cccc(Br)c4)c23)CC1

Basic Information

ChEMBL ID CHEMBL1645474
Phase Preclinical
Structure Type MOL
InChI Key DJURWFMQIHTKEM-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

401.3
MW (Da)
3.16
ALogP
6
HBA
2
HBD
71.5
PSA (Ų)
0.70
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 C18H21BrN6
MW 401.31
Aromatic Rings 3
Heavy Atoms 25
NP-Likeness -1.55

Activity Summary

IC50 4 meas. best 8.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Receptor tyrosine-protein kinase erbB-2
CHEMBL1824
IC50 8.4 8.4 4.0 1
Epidermal growth factor receptor
CHEMBL203
IC50 8.22 8.22 6.0 1
NCI-N87
CHEMBL614197
IC50 7.3 7.3 50.0 1
A2780
CHEMBL614004
IC50 5.58 5.58 2600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
21177105 10.1016/j.bmcl.2010.11.100 Receptor tyrosine-protein kinase erbB-2 1
21177105 10.1016/j.bmcl.2010.11.100 Epidermal growth factor receptor 1
21177105 10.1016/j.bmcl.2010.11.100 NCI-N87 1
21177105 10.1016/j.bmcl.2010.11.100 A2780 1

Data from ChEMBL 36 via Core Engine