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Compound Detail

CHEMBL4284343

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C[N+](C)(CC#CCOc1ccon1)CCCC[N+](C)(C)CCCN1C(=O)c2ccccc2C1=O.[Br-].[Br-]

Basic Information

ChEMBL ID CHEMBL4284343
Phase Preclinical
Structure Type MOL
InChI Key WJBHFLDKGTZYEJ-UHFFFAOYSA-L
Parent Compound CHEMBL4303044
Active Moiety CHEMBL4303044
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

468.6
MW (Da)
2.68
ALogP
5
HBA
0
HBD
72.6
PSA (Ų)
0.21
QED
0
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H36Br2N4O4
MW 628.41
Aromatic Rings 2
Heavy Atoms 34
NP-Likeness -0.53

Activity Summary

IC50 1 meas. best 4.07

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cholinesterase
CHEMBL5763
IC50 4.07 4.07 85113.8 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cholinesterase IC50 = 85113.8 nM 4.07 Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate pre... 30108847

Literature References

PubMed DOI Target Context # Activities
30108847 10.1039/C7MD00149E Acetylcholinesterase 2
30108847 10.1039/C7MD00149E Cholinesterase 2
30108847 10.1039/C7MD00149E HepG2 1
30108847 10.1039/C7MD00149E No relevant target 1

Data from ChEMBL 36 via Core Engine