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Compound Detail

CHEMBL92731

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CCCN(C/C=C/C(=O)Nc1ccc2ncnc(Nc3cccc(Br)c3)c2c1)CCC

Basic Information

ChEMBL ID CHEMBL92731
Phase Preclinical
Structure Type MOL
InChI Key BLCWDFQAJUMTGJ-RMKNXTFCSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

482.4
MW (Da)
5.75
ALogP
5
HBA
2
HBD
70.2
PSA (Ų)
0.36
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H28BrN5O
MW 482.43
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -1.43

Activity Summary

IC50 5 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
SK-BR-3
CHEMBL613834
IC50 8.7 8.7 2.0 1
Epidermal growth factor receptor
CHEMBL203
IC50 7.05 7.05 90.0 1
A-431
CHEMBL614069
IC50 6.84 6.84 145.0 1
Receptor tyrosine-protein kinase erbB-2
CHEMBL1824
IC50 5.84 5.84 1428.0 1
SW-620
CHEMBL612262
IC50 5.64 5.64 2282.0 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