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Compound Detail

CHEMBL4455539

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C[n+]1c(/C=C2\C=CN(CC(=O)NCCN3CCCC3)c3ccccc32)sc2ccccc21.[Br-]

Basic Information

ChEMBL ID CHEMBL4455539
Phase Preclinical
Structure Type MOL
InChI Key WMPVNGKLWXKETG-UHFFFAOYSA-N
Parent Compound CHEMBL4596140
Active Moiety CHEMBL4596140
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

445.6
MW (Da)
3.81
ALogP
4
HBA
1
HBD
39.5
PSA (Ų)
0.59
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H29BrN4OS
MW 525.52
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -1.07

Activity Summary

Kd 1 meas. best 6.42

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
dsDNA
CHEMBL3832741
Kd 6.42 6.42 380.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
dsDNA Kd = 380.0 nM 6.42 Binding affinity to 17 mer duplex D1 DNA (unknown origin) assessed as equilibriu... 31071547

Literature References

PubMed DOI Target Context # Activities
31071547 10.1016/j.ejmech.2019.04.041 quadruplex DNA 6
31071547 10.1016/j.ejmech.2019.04.041 Unchecked 3
31071547 10.1016/j.ejmech.2019.04.041 Telomerase reverse transcriptase 2
31071547 10.1016/j.ejmech.2019.04.041 dsDNA 1

Data from ChEMBL 36 via Core Engine