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Compound Detail

CHEMBL51659

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C=CC(=O)Nc1cc2c(Nc3cccc(Br)c3)ncnc2cn1

Basic Information

ChEMBL ID CHEMBL51659
Phase Preclinical
Structure Type MOL
InChI Key OLYVUTGQXNIQQG-UHFFFAOYSA-N
2
Targets
5
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

370.2
MW (Da)
3.66
ALogP
5
HBA
2
HBD
79.8
PSA (Ų)
0.69
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 C16H12BrN5O
MW 370.21
Aromatic Rings 3
Heavy Atoms 23
NP-Likeness -1.20

Activity Summary

IC50 5 meas. best 9.04

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Epidermal growth factor receptor
CHEMBL203
IC50 9.04 8.755 0.9 4
Receptor tyrosine-protein kinase erbB-2
CHEMBL1824
IC50 8.41 8.41 3.9 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10346932 10.1021/jm9806603 NCI-H125 9
10346932 10.1021/jm9806603 A-431 4
11462982 10.1021/jm000372i Epidermal growth factor receptor 3
10346932 10.1021/jm9806603 Epidermal growth factor receptor 3
10346932 10.1021/jm9806603 Mus musculus 2
10346932 10.1021/jm9806603 Receptor tyrosine-protein kinase erbB-2 1

Data from ChEMBL 36 via Core Engine